MXPA99007670A - N - Google Patents
NInfo
- Publication number
- MXPA99007670A MXPA99007670A MXPA/A/1999/007670A MX9907670A MXPA99007670A MX PA99007670 A MXPA99007670 A MX PA99007670A MX 9907670 A MX9907670 A MX 9907670A MX PA99007670 A MXPA99007670 A MX PA99007670A
- Authority
- MX
- Mexico
- Prior art keywords
- imidazol
- methyl
- acetamide
- pyrimidin
- ethyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims abstract description 239
- 230000002194 synthesizing Effects 0.000 claims abstract description 6
- 238000000034 method Methods 0.000 claims abstract description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 5
- -1 monoalkylamino Chemical group 0.000 claims description 1027
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 679
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 660
- 125000000217 alkyl group Chemical group 0.000 claims description 439
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims description 420
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 387
- 229910052739 hydrogen Inorganic materials 0.000 claims description 248
- 239000001257 hydrogen Substances 0.000 claims description 248
- 150000002431 hydrogen Chemical class 0.000 claims description 192
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 155
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 147
- 125000003545 alkoxy group Chemical group 0.000 claims description 134
- 125000005843 halogen group Chemical group 0.000 claims description 131
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 121
- 125000003107 substituted aryl group Chemical group 0.000 claims description 121
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 119
- 229910052757 nitrogen Inorganic materials 0.000 claims description 104
- 125000000623 heterocyclic group Chemical group 0.000 claims description 88
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 82
- 125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims description 79
- 125000001188 haloalkyl group Chemical group 0.000 claims description 78
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 78
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 63
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims description 62
- 229910052799 carbon Inorganic materials 0.000 claims description 53
- MWUXSHHQAYIFBG-UHFFFAOYSA-N nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 51
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 48
- 125000001424 substituent group Chemical group 0.000 claims description 46
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 44
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 43
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 43
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 42
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 42
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 39
- 125000005842 heteroatoms Chemical group 0.000 claims description 39
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 39
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 35
- 239000000203 mixture Substances 0.000 claims description 29
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 27
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 25
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims description 24
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 24
- 125000000539 amino acid group Chemical group 0.000 claims description 23
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 23
- 125000002883 imidazolyl group Chemical group 0.000 claims description 23
- 150000002829 nitrogen Chemical group 0.000 claims description 23
- 125000002252 acyl group Chemical group 0.000 claims description 22
- 125000004442 acylamino group Chemical group 0.000 claims description 22
- 125000004104 aryloxy group Chemical group 0.000 claims description 22
- 239000011780 sodium chloride Substances 0.000 claims description 22
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 21
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 21
- 125000005141 aryl amino sulfonyl group Chemical group 0.000 claims description 21
- 125000004472 dialkylaminosulfonyl group Chemical group 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 21
- 125000005422 alkyl sulfonamido group Chemical group 0.000 claims description 20
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims description 20
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 20
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims description 19
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 19
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 18
- DLFVBJFMPXGRIB-UHFFFAOYSA-N acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 18
- 125000005147 toluenesulfonyl group Chemical group C=1(C(=CC=CC1)S(=O)(=O)*)C 0.000 claims description 18
- 239000002253 acid Substances 0.000 claims description 17
- 101700067413 CR19 Proteins 0.000 claims description 16
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims description 16
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 16
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 15
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims description 15
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 15
- 229910052717 sulfur Inorganic materials 0.000 claims description 15
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 14
- 125000000304 alkynyl group Chemical group 0.000 claims description 14
- 239000007787 solid Substances 0.000 claims description 14
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 13
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 13
- 238000004519 manufacturing process Methods 0.000 claims description 12
- 150000001413 amino acids Chemical class 0.000 claims description 11
- 239000000758 substrate Substances 0.000 claims description 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 10
- 125000002757 morpholinyl group Chemical group 0.000 claims description 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 10
- HCUOEKSZWPGJIM-YBRHCDHNSA-N (E,2E)-2-hydroxyimino-6-methoxy-4-methyl-5-nitrohex-3-enamide Chemical compound COCC([N+]([O-])=O)\C(C)=C\C(=N/O)\C(N)=O HCUOEKSZWPGJIM-YBRHCDHNSA-N 0.000 claims description 9
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 9
- 101700000225 NR4A3 Proteins 0.000 claims description 9
- 102100001666 OSCP1 Human genes 0.000 claims description 9
- 101700064966 OSCP1 Proteins 0.000 claims description 9
- 101710013972 PLSCR1 Proteins 0.000 claims description 9
- 101700036345 SGE1 Proteins 0.000 claims description 9
- 229910052760 oxygen Inorganic materials 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 125000004193 piperazinyl group Chemical group 0.000 claims description 8
- 125000003386 piperidinyl group Chemical group 0.000 claims description 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 7
- 125000002947 alkylene group Chemical group 0.000 claims description 7
- 125000006263 dimethyl aminosulfonyl group Chemical compound [H]C([H])([H])N(C([H])([H])[H])S(*)(=O)=O 0.000 claims description 7
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Substances C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 7
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims description 7
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 claims description 6
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 6
- 125000000068 chlorophenyl group Chemical group 0.000 claims description 6
- 125000005805 dimethoxy phenyl group Chemical group 0.000 claims description 6
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 6
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 6
- 125000003944 tolyl group Chemical group 0.000 claims description 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 5
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 5
- 208000001953 Hypotension Diseases 0.000 claims description 5
- 241000124008 Mammalia Species 0.000 claims description 5
- 230000027455 binding Effects 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 230000036543 hypotension Effects 0.000 claims description 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 4
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 4
- 206010012601 Diabetes mellitus Diseases 0.000 claims description 4
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims description 4
- 206010040070 Septic shock Diseases 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 125000001041 indolyl group Chemical group 0.000 claims description 4
- 230000002757 inflammatory Effects 0.000 claims description 4
- 230000001404 mediated Effects 0.000 claims description 4
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- 239000002245 particle Substances 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 230000036303 septic shock Effects 0.000 claims description 4
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 4
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 3
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 3
- 206010056370 Congestive cardiomyopathy Diseases 0.000 claims description 3
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims description 3
- 102000004877 Insulin Human genes 0.000 claims description 3
- 108090001061 Insulin Proteins 0.000 claims description 3
- 201000006474 brain ischemia Diseases 0.000 claims description 3
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims description 3
- 201000006233 congestive heart failure Diseases 0.000 claims description 3
- 201000010046 dilated cardiomyopathy Diseases 0.000 claims description 3
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 3
- 239000003446 ligand Substances 0.000 claims description 3
- BXPFAYHUZWALPV-UHFFFAOYSA-N 1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)-N-[2-(4-methoxyphenyl)ethyl]pyrrolidine-2-carboxamide Chemical compound C1=CC(OC)=CC=C1CCNC(=O)C1N(C=2N=C(N=C(C)C=2)N2C=NC=C2)CCC1 BXPFAYHUZWALPV-UHFFFAOYSA-N 0.000 claims description 2
- GOKCJCODOLGYQD-UHFFFAOYSA-N 4,6-dichloro-2-imidazol-1-ylpyrimidine Chemical compound ClC1=CC(Cl)=NC(N2C=NC=C2)=N1 GOKCJCODOLGYQD-UHFFFAOYSA-N 0.000 claims description 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 2
- 208000006673 Asthma Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 206010011401 Crohn's disease Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathy Diseases 0.000 claims description 2
- 208000001636 Diabetic Neuropathy Diseases 0.000 claims description 2
- 206010061835 Diabetic nephropathy Diseases 0.000 claims description 2
- 206010012680 Diabetic neuropathy Diseases 0.000 claims description 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims description 2
- 206010018651 Graft versus host disease Diseases 0.000 claims description 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 2
- 206010022114 Injury Diseases 0.000 claims description 2
- QZMBUROFNSSUCP-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[1-(6-ethyl-2-imidazol-1-ylpyrimidin-4-yl)pyrrolidin-2-yl]acetamide Chemical compound N=1C(CC)=CC(N2C(CCC2)CC(=O)NCC=2C=C3OCOC3=CC=2)=NC=1N1C=CN=C1 QZMBUROFNSSUCP-UHFFFAOYSA-N 0.000 claims description 2
- CGNZRUKEFUYULD-UHFFFAOYSA-N N-(1,3-dioxolan-4-ylmethyl)-2-[1-(2-imidazol-1-ylpyrimidin-4-yl)azepan-2-yl]acetamide Chemical compound C1OCOC1CNC(=O)CC1CCCCCN1C(N=1)=CC=NC=1N1C=CN=C1 CGNZRUKEFUYULD-UHFFFAOYSA-N 0.000 claims description 2
- DJKVXSGGVXKZBQ-UHFFFAOYSA-N N-[(3,4-dimethoxyphenyl)methyl]-2-[1-(2-imidazol-1-ylpyrimidin-4-yl)pyrrolidin-2-yl]acetamide Chemical compound C1=C(OC)C(OC)=CC=C1CNC(=O)CC1N(C=2N=C(N=CC=2)N2C=NC=C2)CCC1 DJKVXSGGVXKZBQ-UHFFFAOYSA-N 0.000 claims description 2
- BXVNHBCLUUHXBC-UHFFFAOYSA-N N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-(6-ethyl-2-imidazol-1-ylpyrimidin-4-yl)pyrrolidine-2-carboxamide Chemical compound N=1C(CC)=CC(N2C(CCC2)C(=O)NCCC=2C=C3OCOC3=CC=2)=NC=1N1C=CN=C1 BXVNHBCLUUHXBC-UHFFFAOYSA-N 0.000 claims description 2
- 206010061536 Parkinson's disease Diseases 0.000 claims description 2
- 206010035664 Pneumonia Diseases 0.000 claims description 2
- 206010049771 Shock haemorrhagic Diseases 0.000 claims description 2
- 241000580858 Simian-Human immunodeficiency virus Species 0.000 claims description 2
- 208000006641 Skin Disease Diseases 0.000 claims description 2
- 206010052779 Transplant rejections Diseases 0.000 claims description 2
- 230000001154 acute Effects 0.000 claims description 2
- 125000005418 aryl aryl group Chemical group 0.000 claims description 2
- 201000001320 atherosclerosis Diseases 0.000 claims description 2
- 230000001684 chronic Effects 0.000 claims description 2
- 231100000516 lung damage Toxicity 0.000 claims description 2
- 201000009906 meningitis Diseases 0.000 claims description 2
- 210000000056 organs Anatomy 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 230000001717 pathogenic Effects 0.000 claims description 2
- 244000052769 pathogens Species 0.000 claims description 2
- 201000004681 psoriasis Diseases 0.000 claims description 2
- 200000000008 restenosis Diseases 0.000 claims description 2
- 230000000391 smoking Effects 0.000 claims description 2
- 230000036262 stenosis Effects 0.000 claims description 2
- 200000000009 stenosis Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 201000006704 ulcerative colitis Diseases 0.000 claims description 2
- NMPGHGKEQNHEMI-UHFFFAOYSA-N 2-piperazin-2-ylacetamide Chemical compound NC(=O)CC1CNCCN1 NMPGHGKEQNHEMI-UHFFFAOYSA-N 0.000 claims 217
- BRYCUMKDWMEGMK-UHFFFAOYSA-N piperazine-2-carboxamide Chemical compound NC(=O)C1CNCCN1 BRYCUMKDWMEGMK-UHFFFAOYSA-N 0.000 claims 76
- 241000009298 Trigla lyra Species 0.000 claims 40
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 39
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 33
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 19
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 19
- DGEZNRSVGBDHLK-UHFFFAOYSA-N [1,10]phenanthroline Chemical compound C1=CN=C2C3=NC=CC=C3C=CC2=C1 DGEZNRSVGBDHLK-UHFFFAOYSA-N 0.000 claims 15
- GLUUGHFHXGJENI-UHFFFAOYSA-N piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 15
- IAVUPBUMOXMJKJ-UHFFFAOYSA-N azepane-2-carboxamide Chemical compound NC(=O)C1CCCCCN1 IAVUPBUMOXMJKJ-UHFFFAOYSA-N 0.000 claims 14
- 125000003277 amino group Chemical compound 0.000 claims 13
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 12
- RNGRYWXHDOJTFX-UHFFFAOYSA-N 2-piperidin-2-ylacetamide Chemical compound NC(=O)CC1CCCCN1 RNGRYWXHDOJTFX-UHFFFAOYSA-N 0.000 claims 11
- JQJMHECJBDLIIW-UHFFFAOYSA-N 2-(azepan-2-yl)acetamide Chemical compound NC(=O)CC1CCCCCN1 JQJMHECJBDLIIW-UHFFFAOYSA-N 0.000 claims 9
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 claims 8
- 125000006606 n-butoxy group Chemical group 0.000 claims 8
- 101700040321 pdm2 Proteins 0.000 claims 7
- 125000001617 2,3-dimethoxy phenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C(OC([H])([H])[H])=C1[H] 0.000 claims 6
- HSUIVCLOAAJSRE-UHFFFAOYSA-N bis(2-methoxyethyl) benzene-1,2-dicarboxylate Chemical compound COCCOC(=O)C1=CC=CC=C1C(=O)OCCOC HSUIVCLOAAJSRE-UHFFFAOYSA-N 0.000 claims 6
- YKYIFUROKBDHCY-ONEGZZNKSA-N (E)-4-ethoxy-1,1,1-trifluorobut-3-en-2-one Chemical group CCO\C=C\C(=O)C(F)(F)F YKYIFUROKBDHCY-ONEGZZNKSA-N 0.000 claims 5
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 5
- XNEFVTBPCXGIRX-UHFFFAOYSA-M methanesulfinate Chemical compound CS([O-])=O XNEFVTBPCXGIRX-UHFFFAOYSA-M 0.000 claims 5
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 4
- 125000001847 2-phenylcyclopropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 150000003869 acetamides Chemical compound 0.000 claims 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 4
- FTNJQNQLEGKTGD-UHFFFAOYSA-N 1,3-Benzodioxole Chemical compound C1=CC=C2OCOC2=C1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 claims 3
- 125000004204 2-methoxyphenyl group Chemical compound [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 3
- VGEOCVZKPBSYQC-UHFFFAOYSA-N 2-piperazin-1-ium-2-ylacetate Chemical compound OC(=O)CC1CNCCN1 VGEOCVZKPBSYQC-UHFFFAOYSA-N 0.000 claims 3
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 3
- CMWTZPSULFXXJA-VIFPVBQESA-N Naproxen Chemical group C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 3
- QLNJFJADRCOGBJ-UHFFFAOYSA-N Propanamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 3
- 125000000484 butyl group Chemical compound [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 239000002131 composite material Substances 0.000 claims 3
- YPSPPJRTCRMQGD-UHFFFAOYSA-N morpholine-3-carboxamide Chemical compound NC(=O)C1COCCN1 YPSPPJRTCRMQGD-UHFFFAOYSA-N 0.000 claims 3
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 3
- DTBHRRDGLARWLZ-UHFFFAOYSA-N 2-Methylbenzyl radical Chemical compound [CH2]C1=CC=CC=C1C DTBHRRDGLARWLZ-UHFFFAOYSA-N 0.000 claims 2
- ASQUQUOEFDHYGP-UHFFFAOYSA-N 2-methoxyethanolate Chemical group COCC[O-] ASQUQUOEFDHYGP-UHFFFAOYSA-N 0.000 claims 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004863 4-trifluoromethoxyphenyl group Chemical compound [H]C1=C([H])C(OC(F)(F)F)=C([H])C([H])=C1* 0.000 claims 2
- RNOLFZACEWWIHP-UHFFFAOYSA-N 6-chloro-1,4-dihydroquinoxaline-2,3-dione Chemical compound N1C(=O)C(=O)NC2=CC(Cl)=CC=C21 RNOLFZACEWWIHP-UHFFFAOYSA-N 0.000 claims 2
- BNBQRQQYDMDJAH-UHFFFAOYSA-N Benzodioxan Chemical compound C1=CC=C2OCCOC2=C1 BNBQRQQYDMDJAH-UHFFFAOYSA-N 0.000 claims 2
- 229940047583 Cetamide Drugs 0.000 claims 2
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Exidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 claims 2
- SKZKKFZAGNVIMN-UHFFFAOYSA-N Salicilamide Chemical compound NC(=O)C1=CC=CC=C1O SKZKKFZAGNVIMN-UHFFFAOYSA-N 0.000 claims 2
- 240000003670 Sesamum indicum Species 0.000 claims 2
- 125000004744 butyloxycarbonyl group Chemical group 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- YSPVHAUJXLGZHP-UHFFFAOYSA-N ethyl piperidine-1-carboxylate Chemical compound CCOC(=O)N1CCCCC1 YSPVHAUJXLGZHP-UHFFFAOYSA-N 0.000 claims 2
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 2
- 150000003230 pyrimidines Chemical class 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 150000005529 1,3-benzodioxoles Chemical compound 0.000 claims 1
- HLVHORUZEKFUPM-UHFFFAOYSA-N 1-(2-imidazol-1-ylpyrimidin-4-yl)-N-[(2-methoxyphenyl)methyl]-4-methylpiperazine-2-carboxamide Chemical compound COC1=CC=CC=C1CNC(=O)C1N(C=2N=C(N=CC=2)N2C=NC=C2)CCN(C)C1 HLVHORUZEKFUPM-UHFFFAOYSA-N 0.000 claims 1
- HBFFKFRHTZVEEV-UHFFFAOYSA-N 1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-N-[2-(3,4-dimethoxyphenyl)ethyl]azepane-2-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1CCNC(=O)C1N(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)CCCCC1 HBFFKFRHTZVEEV-UHFFFAOYSA-N 0.000 claims 1
- JDYSOSZDHZDDBZ-UHFFFAOYSA-N 1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)azepane Chemical compound N=1C(Cl)=CC(N2CCCCCC2)=NC=1N1C=CN=C1 JDYSOSZDHZDDBZ-UHFFFAOYSA-N 0.000 claims 1
- JLUGJJKDLMHJTF-UHFFFAOYSA-N 1-[[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]methyl]-3-(4-methoxyphenyl)urea Chemical compound C1=CC(OC)=CC=C1NC(=O)NCC1N(C=2N=C(N=CC=2)N2C=NC=C2)CCCC1 JLUGJJKDLMHJTF-UHFFFAOYSA-N 0.000 claims 1
- UHJWZORSTYATLW-UHFFFAOYSA-N 1-phenoxy-2-phenylbenzene Chemical compound C=1C=CC=C(C=2C=CC=CC=2)C=1OC1=CC=CC=C1 UHJWZORSTYATLW-UHFFFAOYSA-N 0.000 claims 1
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- JHKUFUGKXIQNPC-UHFFFAOYSA-N 2,4-di(imidazol-1-yl)-6-methylpyrimidine Chemical compound N=1C(C)=CC(N2C=NC=C2)=NC=1N1C=CN=C1 JHKUFUGKXIQNPC-UHFFFAOYSA-N 0.000 claims 1
- JEHKSGBXJLNTDZ-UHFFFAOYSA-N 2,4-dichloro-6-imidazol-1-ylpyrimidine Chemical compound ClC1=NC(Cl)=CC(N2C=NC=C2)=N1 JEHKSGBXJLNTDZ-UHFFFAOYSA-N 0.000 claims 1
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 1
- CHLNGHNJFWAWRU-UHFFFAOYSA-N 2-(1,3-benzodioxol-5-yl)-1$l^{4},3,2-benzodithiazole 1-oxide Chemical compound C1=C2OCOC2=CC(N2S(C3=CC=CC=C3S2)=O)=C1 CHLNGHNJFWAWRU-UHFFFAOYSA-N 0.000 claims 1
- GUEWNORIPIUWSP-UHFFFAOYSA-N 2-(1,3-benzodioxol-5-yl)-N-[[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]methyl]acetamide Chemical compound C=1C=C2OCOC2=CC=1CC(=O)NCC1CCCCN1C(N=1)=CC=NC=1N1C=CN=C1 GUEWNORIPIUWSP-UHFFFAOYSA-N 0.000 claims 1
- AQLZTHZLYFFVIJ-UHFFFAOYSA-N 2-(2-aminopropan-2-yl)-N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-6-oxopyrimidine-4-carboxamide Chemical compound O=C1N(C)C(C(C)(C)N)=NC(C(=O)NCC=2C=CC(F)=CC=2)=C1O AQLZTHZLYFFVIJ-UHFFFAOYSA-N 0.000 claims 1
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 claims 1
- HWPDQKCDOOFRGP-UHFFFAOYSA-N 2-[(2-imidazol-1-yl-6-methylpyrimidin-4-yl)-methylamino]-N-octylacetamide Chemical compound CCCCCCCCNC(=O)CN(C)C1=CC(C)=NC(N2C=NC=C2)=N1 HWPDQKCDOOFRGP-UHFFFAOYSA-N 0.000 claims 1
- OAJCHGCRINIFNZ-UHFFFAOYSA-N 2-[(2-imidazol-1-yl-6-methylpyrimidin-4-yl)amino]-N-[(4-methoxyphenyl)methyl]-4-methylsulfonylbutanamide Chemical compound C1=CC(OC)=CC=C1CNC(=O)C(CCS(C)(=O)=O)NC1=CC(C)=NC(N2C=NC=C2)=N1 OAJCHGCRINIFNZ-UHFFFAOYSA-N 0.000 claims 1
- LPCDYAMNXGQOOY-UHFFFAOYSA-N 2-[1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperidin-2-yl]-N-pentylacetamide Chemical compound CCCCCNC(=O)CC1CCCCN1C1=CC(C)=NC(N2C=NC=C2)=N1 LPCDYAMNXGQOOY-UHFFFAOYSA-N 0.000 claims 1
- RYSNMHVDIZLRJE-UHFFFAOYSA-N 2-[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]-N-pentylacetamide Chemical compound CCCCCNC(=O)CC1CCCCN1C1=CC=NC(N2C=NC=C2)=N1 RYSNMHVDIZLRJE-UHFFFAOYSA-N 0.000 claims 1
- HXCXURNDERDTGC-UHFFFAOYSA-N 2-[1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]-N-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)acetamide Chemical compound C=1C=C2OCCOC2=CC=1CNC(=O)CC1CN(C)CCN1C(N=1)=CC(Cl)=NC=1N1C=CN=C1 HXCXURNDERDTGC-UHFFFAOYSA-N 0.000 claims 1
- CEDUUMWLYYBLBW-UHFFFAOYSA-N 2-[1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]-N-[(3-chloro-4-methoxyphenyl)methyl]acetamide Chemical compound C1=C(Cl)C(OC)=CC=C1CNC(=O)CC1N(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)CCN(C)C1 CEDUUMWLYYBLBW-UHFFFAOYSA-N 0.000 claims 1
- WFBXIGFKTCYZOK-UHFFFAOYSA-N 2-[1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]-N-[(4-chlorophenyl)methyl]acetamide Chemical compound C1N(C)CCN(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(Cl)C=C1 WFBXIGFKTCYZOK-UHFFFAOYSA-N 0.000 claims 1
- BKNUAJLJPKQQDA-UHFFFAOYSA-N 2-[1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]-N-[(4-methoxyphenyl)methyl]acetamide Chemical compound C1=CC(OC)=CC=C1CNC(=O)CC1N(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)CCN(C)C1 BKNUAJLJPKQQDA-UHFFFAOYSA-N 0.000 claims 1
- PAXMSXORINSACX-UHFFFAOYSA-N 2-[1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]-N-[2-(3-methoxyphenyl)ethyl]acetamide Chemical compound COC1=CC=CC(CCNC(=O)CC2N(CCN(C)C2)C=2N=C(N=C(Cl)C=2)N2C=NC=C2)=C1 PAXMSXORINSACX-UHFFFAOYSA-N 0.000 claims 1
- OQYASOVHPRIMPJ-UHFFFAOYSA-N 2-[1-[2-(2-imidazol-1-ylethyl)-6-methylpyrimidin-4-yl]piperidin-2-yl]-N-[[4-(trifluoromethyl)phenyl]methyl]acetamide Chemical compound N=1C(C)=CC(N2C(CCCC2)CC(=O)NCC=2C=CC(=CC=2)C(F)(F)F)=NC=1CCN1C=CN=C1 OQYASOVHPRIMPJ-UHFFFAOYSA-N 0.000 claims 1
- MSZHJRJLACIVSF-UHFFFAOYSA-N 2-[4-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)-1-methylpiperazin-2-yl]-N-[(4-methylphenyl)methyl]acetamide Chemical compound CN1CCN(C=2N=C(N=C(C)C=2)N2C=NC=C2)CC1CC(=O)NCC1=CC=C(C)C=C1 MSZHJRJLACIVSF-UHFFFAOYSA-N 0.000 claims 1
- MLVWJRGIJOAAPY-UHFFFAOYSA-N 2-[4-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-1-methylpiperazin-2-yl]-N-[(3,4,5-trimethoxyphenyl)methyl]acetamide Chemical compound COC1=C(OC)C(OC)=CC(CNC(=O)CC2N(CCN(C2)C=2N=C(N=C(Cl)C=2)N2C=NC=C2)C)=C1 MLVWJRGIJOAAPY-UHFFFAOYSA-N 0.000 claims 1
- RFYGOJPSAVTJJX-UHFFFAOYSA-N 2-[4-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)-1-methylpiperazin-2-yl]-N-[(4-methylphenyl)methyl]acetamide Chemical compound CN1CCN(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)CC1CC(=O)NCC1=CC=C(C)C=C1 RFYGOJPSAVTJJX-UHFFFAOYSA-N 0.000 claims 1
- PBZLBOMDGMZBID-UHFFFAOYSA-N 2-[4-acetyl-1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperazin-2-yl]-N-[(3,4-dimethoxyphenyl)methyl]acetamide Chemical compound C1=C(OC)C(OC)=CC=C1CNC(=O)CC1N(C=2N=C(N=C(C)C=2)N2C=NC=C2)CCN(C(C)=O)C1 PBZLBOMDGMZBID-UHFFFAOYSA-N 0.000 claims 1
- QZMWZWRXXHPWGN-UHFFFAOYSA-N 2-[4-acetyl-1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(3,4-dimethoxyphenyl)ethyl]acetamide Chemical compound C1=C(OC)C(OC)=CC=C1CCNC(=O)CC1N(C=2N=C(N=C(C)C=2)N2C=NC=C2)CCN(C(C)=O)C1 QZMWZWRXXHPWGN-UHFFFAOYSA-N 0.000 claims 1
- RBPOXFMOEAPUJE-UHFFFAOYSA-N 2-[4-acetyl-1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(4-methoxyphenyl)ethyl]acetamide Chemical compound C1=CC(OC)=CC=C1CCNC(=O)CC1N(C=2N=C(N=C(C)C=2)N2C=NC=C2)CCN(C(C)=O)C1 RBPOXFMOEAPUJE-UHFFFAOYSA-N 0.000 claims 1
- NKUYAQJMCHLEFG-UHFFFAOYSA-N 2-[4-acetyl-1-(2-imidazol-1-yl-6-propan-2-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methylphenyl)methyl]acetamide Chemical compound N=1C(C(C)C)=CC(N2C(CN(CC2)C(C)=O)CC(=O)NCC=2C=CC(C)=CC=2)=NC=1N1C=CN=C1 NKUYAQJMCHLEFG-UHFFFAOYSA-N 0.000 claims 1
- OCVPFXLBCHGLLG-UHFFFAOYSA-N 2-[4-acetyl-1-(2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(3-chloro-4-methoxyphenyl)methyl]acetamide Chemical compound C1=C(Cl)C(OC)=CC=C1CNC(=O)CC1N(C=2N=C(N=CC=2)N2C=NC=C2)CCN(C(C)=O)C1 OCVPFXLBCHGLLG-UHFFFAOYSA-N 0.000 claims 1
- HHMPTLCIJNXYBX-UHFFFAOYSA-N 2-[4-acetyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)acetamide Chemical compound C=1C=C2OCCOC2=CC=1CNC(=O)CC1CN(C(=O)C)CCN1C(N=1)=CC(Cl)=NC=1N1C=CN=C1 HHMPTLCIJNXYBX-UHFFFAOYSA-N 0.000 claims 1
- KOAXJQKLOUWSDU-UHFFFAOYSA-N 2-[4-acetyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methylphenyl)methyl]acetamide Chemical compound C1N(C(=O)C)CCN(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(C)C=C1 KOAXJQKLOUWSDU-UHFFFAOYSA-N 0.000 claims 1
- PFMRCPXGJNHCEG-UHFFFAOYSA-N 2-[4-acetyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(1,3-benzodioxol-5-yl)ethyl]acetamide Chemical compound C=1C=C2OCOC2=CC=1CCNC(=O)CC1CN(C(=O)C)CCN1C(N=1)=CC(Cl)=NC=1N1C=CN=C1 PFMRCPXGJNHCEG-UHFFFAOYSA-N 0.000 claims 1
- WZGVSJJQNMXIPM-UHFFFAOYSA-N 2-[4-acetyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(3,4-dimethoxyphenyl)ethyl]acetamide Chemical compound C1=C(OC)C(OC)=CC=C1CCNC(=O)CC1N(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)CCN(C(C)=O)C1 WZGVSJJQNMXIPM-UHFFFAOYSA-N 0.000 claims 1
- XWMDXIAGFYJZEB-UHFFFAOYSA-N 2-[4-acetyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(3-chloro-4-methoxyphenyl)ethyl]acetamide Chemical compound C1=C(Cl)C(OC)=CC=C1CCNC(=O)CC1N(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)CCN(C(C)=O)C1 XWMDXIAGFYJZEB-UHFFFAOYSA-N 0.000 claims 1
- CNFGTWYMHAEBTL-UHFFFAOYSA-N 2-[4-acetyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(3-methoxyphenyl)ethyl]acetamide Chemical compound COC1=CC=CC(CCNC(=O)CC2N(CCN(C2)C(C)=O)C=2N=C(N=C(Cl)C=2)N2C=NC=C2)=C1 CNFGTWYMHAEBTL-UHFFFAOYSA-N 0.000 claims 1
- SEXFYLPBIZMMBX-UHFFFAOYSA-N 2-[4-butyl-1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-ethoxyphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=C(C)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OCC)C=C1 SEXFYLPBIZMMBX-UHFFFAOYSA-N 0.000 claims 1
- VGCWXHMAYZYBPD-UHFFFAOYSA-N 2-[4-butyl-1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methoxyphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=C(C)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OC)C=C1 VGCWXHMAYZYBPD-UHFFFAOYSA-N 0.000 claims 1
- QYXSBXQHNSHUJI-UHFFFAOYSA-N 2-[4-butyl-1-(2-imidazol-1-yl-6-propan-2-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methoxyphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=C(C=2)C(C)C)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OC)C=C1 QYXSBXQHNSHUJI-UHFFFAOYSA-N 0.000 claims 1
- WPTAMRONKFBEPY-UHFFFAOYSA-N 2-[4-butyl-1-(2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methoxyphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=CC=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OC)C=C1 WPTAMRONKFBEPY-UHFFFAOYSA-N 0.000 claims 1
- OIQBHZKPPPDQAR-UHFFFAOYSA-N 2-[4-butyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(3-chloro-4-methoxyphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OC)C(Cl)=C1 OIQBHZKPPPDQAR-UHFFFAOYSA-N 0.000 claims 1
- ZPNASQWCRFAURQ-UHFFFAOYSA-N 2-[4-butyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methoxyphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OC)C=C1 ZPNASQWCRFAURQ-UHFFFAOYSA-N 0.000 claims 1
- KGIDJJVGJURKDK-UHFFFAOYSA-N 2-[4-butyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[(4-methylphenyl)methyl]acetamide Chemical compound C1N(CCCC)CCN(C=2N=C(N=C(Cl)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(C)C=C1 KGIDJJVGJURKDK-UHFFFAOYSA-N 0.000 claims 1
- IJVBFEDERNQTIG-UHFFFAOYSA-N 2-[4-butyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]-N-[2-(2,3-dihydro-1,4-benzodioxin-6-yl)ethyl]acetamide Chemical compound C=1C=C2OCCOC2=CC=1CCNC(=O)CC1CN(CCCC)CCN1C(N=1)=CC(Cl)=NC=1N1C=CN=C1 IJVBFEDERNQTIG-UHFFFAOYSA-N 0.000 claims 1
- FEYJYPBJNXHKEE-UHFFFAOYSA-N 2-imidazol-1-yl-4-[2-[3-(4-methoxyphenoxy)propyl]pyrrolidin-1-yl]pyrimidine Chemical compound C1=CC(OC)=CC=C1OCCCC1N(C=2N=C(N=CC=2)N2C=NC=C2)CCC1 FEYJYPBJNXHKEE-UHFFFAOYSA-N 0.000 claims 1
- IEVJVQXLBZUEMH-UHFFFAOYSA-N 2-piperidin-2-ylethanamine Chemical compound NCCC1CCCCN1 IEVJVQXLBZUEMH-UHFFFAOYSA-N 0.000 claims 1
- OFMALDSHFYWVKM-UHFFFAOYSA-N 2-pyrrolidin-2-ylacetamide Chemical compound NC(=O)CC1CCCN1 OFMALDSHFYWVKM-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N 289-95-2 Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- LLQGBIJPNCHLET-UHFFFAOYSA-N 3-[2-[(3-chloro-4-methoxyphenyl)methylamino]-2-oxoethyl]-4-(2-imidazol-1-ylpyrimidin-4-yl)-N-propylpiperazine-1-carboxamide Chemical compound C1N(C(=O)NCCC)CCN(C=2N=C(N=CC=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(OC)C(Cl)=C1 LLQGBIJPNCHLET-UHFFFAOYSA-N 0.000 claims 1
- 125000006201 3-phenylpropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- MMCMQHRSBRWQPT-UHFFFAOYSA-N 3-pyrrolidin-2-ylpropanamide Chemical compound NC(=O)CCC1CCCN1 MMCMQHRSBRWQPT-UHFFFAOYSA-N 0.000 claims 1
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- ZMHRQBGNOZMZRF-UHFFFAOYSA-N 4-[2-[3-(1,3-benzodioxol-5-yl)prop-2-enyl]pyrrolidin-1-yl]-2-imidazol-1-ylpyrimidine Chemical compound C=1C=C2OCOC2=CC=1C=CCC1CCCN1C(N=1)=CC=NC=1N1C=CN=C1 ZMHRQBGNOZMZRF-UHFFFAOYSA-N 0.000 claims 1
- LCKZUKPSXMCMLU-UHFFFAOYSA-N 4-acetyl-N-[2-(3,5-dimethoxyphenyl)ethyl]-1-(2-imidazol-1-yl-6-propan-2-ylpyrimidin-4-yl)piperazine-2-carboxamide Chemical compound COC1=CC(OC)=CC(CCNC(=O)C2N(CCN(C2)C(C)=O)C=2N=C(N=C(C=2)C(C)C)N2C=NC=C2)=C1 LCKZUKPSXMCMLU-UHFFFAOYSA-N 0.000 claims 1
- FBCOPXKJAQMYIJ-UHFFFAOYSA-N 4-chloro-2-imidazol-1-yl-6-piperidin-1-ylpyrimidine Chemical compound N=1C(Cl)=CC(N2CCCCC2)=NC=1N1C=CN=C1 FBCOPXKJAQMYIJ-UHFFFAOYSA-N 0.000 claims 1
- PTNWPWDZSBJFFE-UHFFFAOYSA-N 4-chloro-6-(2-ethylpiperidin-1-yl)-2-imidazol-1-ylpyrimidine Chemical compound CCC1CCCCN1C1=CC(Cl)=NC(N2C=NC=C2)=N1 PTNWPWDZSBJFFE-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 1
- OHDMIERTIPXMBO-CFCGPWAMSA-N 5-acetyl-3-[(2R,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1H-imidazol-2-one Chemical compound O=C1NC(C(=O)C)=CN1[C@@H]1O[C@H](CO)C(O)C1 OHDMIERTIPXMBO-CFCGPWAMSA-N 0.000 claims 1
- AJGLCXBDYCEVIE-UHFFFAOYSA-N 5-chloro-3-hydroxy-1H-pyridin-2-one Chemical compound OC1=CC(Cl)=CN=C1O AJGLCXBDYCEVIE-UHFFFAOYSA-N 0.000 claims 1
- KWAOVDVRSBRTRU-UHFFFAOYSA-N 6-chloro-2-imidazol-1-yl-N-(2-methoxyphenyl)pyrimidin-4-amine Chemical compound COC1=CC=CC=C1NC1=CC(Cl)=NC(N2C=NC=C2)=N1 KWAOVDVRSBRTRU-UHFFFAOYSA-N 0.000 claims 1
- 206010065040 AIDS dementia complex Diseases 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- QBSNSBYIQIGHBJ-UHFFFAOYSA-N C(C)(=O)NCC(NC1=NC(=NC(=C1)C)N1C=NC=C1)C1=CC(=C(C=C1)OC)Cl Chemical compound C(C)(=O)NCC(NC1=NC(=NC(=C1)C)N1C=NC=C1)C1=CC(=C(C=C1)OC)Cl QBSNSBYIQIGHBJ-UHFFFAOYSA-N 0.000 claims 1
- 229910014585 C2-Ce Inorganic materials 0.000 claims 1
- 235000008733 Citrus aurantifolia Nutrition 0.000 claims 1
- 241001435619 Lile Species 0.000 claims 1
- CIFXFCDOVUTHDC-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[(2-imidazol-1-yl-6-methylpyrimidin-4-yl)amino]pentanethioamide Chemical compound C=1C=C2OCOC2=CC=1CNC(=S)C(CCC)NC(N=1)=CC(C)=NC=1N1C=CN=C1 CIFXFCDOVUTHDC-UHFFFAOYSA-N 0.000 claims 1
- XVLIXICFRSHJMT-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)azepan-2-yl]acetamide Chemical compound N=1C(C)=CC(N2C(CCCCC2)CC(=O)NCC=2C=C3OCOC3=CC=2)=NC=1N1C=CN=C1 XVLIXICFRSHJMT-UHFFFAOYSA-N 0.000 claims 1
- NXAPUXYPPQRBTC-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]-N-methylethanamine Chemical compound C=1C=C2OCOC2=CC=1CN(C)CCC1CCCCN1C(N=1)=CC=NC=1N1C=CN=C1 NXAPUXYPPQRBTC-UHFFFAOYSA-N 0.000 claims 1
- IMRLNKLOSQHNRT-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]ethanamine Chemical compound C=1C=C2OCOC2=CC=1CNCCC1CCCCN1C(N=1)=CC=NC=1N1C=CN=C1 IMRLNKLOSQHNRT-UHFFFAOYSA-N 0.000 claims 1
- OABIBZUXKZWTAU-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[4-(2-imidazol-1-yl-6-methoxypyrimidin-4-yl)piperidin-2-yl]acetamide Chemical compound N=1C(OC)=CC(C2CC(CC(=O)NCC=3C=C4OCOC4=CC=3)NCC2)=NC=1N1C=CN=C1 OABIBZUXKZWTAU-UHFFFAOYSA-N 0.000 claims 1
- OKCGEKASOKHRNB-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-2-[4-butyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazin-2-yl]acetamide Chemical compound C=1C=C2OCOC2=CC=1CNC(=O)CC1CN(CCCC)CCN1C(N=1)=CC(Cl)=NC=1N1C=CN=C1 OKCGEKASOKHRNB-UHFFFAOYSA-N 0.000 claims 1
- ZOUXMQJXUZZLNJ-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-3-(2-imidazol-1-ylpyrimidin-4-yl)-4-methoxybenzamide Chemical compound COC1=CC=C(C(=O)NCC=2C=C3OCOC3=CC=2)C=C1C(N=1)=CC=NC=1N1C=CN=C1 ZOUXMQJXUZZLNJ-UHFFFAOYSA-N 0.000 claims 1
- BFXANIGIJVJPAC-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-N-[2-[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]ethyl]acetamide Chemical compound C=1C=C2OCOC2=CC=1CN(C(=O)C)CCC1CCCCN1C(N=1)=CC=NC=1N1C=CN=C1 BFXANIGIJVJPAC-UHFFFAOYSA-N 0.000 claims 1
- ZBMGBVXBUNMMCD-UHFFFAOYSA-N N-(1,3-benzodioxol-5-ylmethyl)-N-[2-[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]ethyl]methanesulfonamide Chemical compound C=1C=C2OCOC2=CC=1CN(S(=O)(=O)C)CCC1CCCCN1C(N=1)=CC=NC=1N1C=CN=C1 ZBMGBVXBUNMMCD-UHFFFAOYSA-N 0.000 claims 1
- LANOYWQRBVPIDX-UHFFFAOYSA-N N-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)-1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)-4-methylpiperazine-2-carboxamide Chemical compound C=1C=C2OCCOC2=CC=1CNC(=O)C1CN(C)CCN1C(N=1)=CC(C)=NC=1N1C=CN=C1 LANOYWQRBVPIDX-UHFFFAOYSA-N 0.000 claims 1
- KJYSVAMLJKSKNF-UHFFFAOYSA-N N-(cyclopropylmethyl)-2-[1-(6-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]acetamide Chemical compound C1N(C)CCN(C=2N=CN=C(C=2)N2C=NC=C2)C1CC(=O)NCC1CC1 KJYSVAMLJKSKNF-UHFFFAOYSA-N 0.000 claims 1
- JRPMWWXRPUZCHU-UHFFFAOYSA-N N-[(3,4-dimethoxyphenyl)methyl]-2-[1-(2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazin-2-yl]acetamide Chemical compound C1=C(OC)C(OC)=CC=C1CNC(=O)CC1N(C=2N=C(N=CC=2)N2C=NC=C2)CCN(C)C1 JRPMWWXRPUZCHU-UHFFFAOYSA-N 0.000 claims 1
- IETACXISRSHZAF-UHFFFAOYSA-N N-[(4-chlorophenyl)methyl]-2-[1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)-4-methylpiperazin-2-yl]acetamide Chemical compound C1N(C)CCN(C=2N=C(N=C(C)C=2)N2C=NC=C2)C1CC(=O)NCC1=CC=C(Cl)C=C1 IETACXISRSHZAF-UHFFFAOYSA-N 0.000 claims 1
- ZLTHNECVRTYOPZ-UHFFFAOYSA-N N-[(4-chlorophenyl)methyl]-3-[2-[(2-imidazol-1-yl-6-methylpyrimidin-4-yl)amino]thiophen-3-yl]propanamide Chemical compound N=1C(N2C=NC=C2)=NC(C)=CC=1NC=1SC=CC=1CCC(=O)NCC1=CC=C(Cl)C=C1 ZLTHNECVRTYOPZ-UHFFFAOYSA-N 0.000 claims 1
- USXUVPVYHIWNFI-UHFFFAOYSA-N N-[(4-methoxyphenyl)methyl]piperazine-2-carboxamide Chemical compound C1=CC(OC)=CC=C1CNC(=O)C1NCCNC1 USXUVPVYHIWNFI-UHFFFAOYSA-N 0.000 claims 1
- CGHKIJQPXACFRJ-UHFFFAOYSA-N N-[2-(1,3-benzodioxol-5-yl)ethyl]-2-[(2-imidazol-1-yl-6-methylpyrimidin-4-yl)amino]pentanethioamide Chemical compound C=1C=C2OCOC2=CC=1CCNC(=S)C(CCC)NC(N=1)=CC(C)=NC=1N1C=CN=C1 CGHKIJQPXACFRJ-UHFFFAOYSA-N 0.000 claims 1
- KNZONLCAAIUDPK-UHFFFAOYSA-N N-[2-(1,3-benzodioxol-5-yl)ethyl]-4-butyl-1-(6-chloro-2-imidazol-1-ylpyrimidin-4-yl)piperazine-2-carboxamide Chemical compound C=1C=C2OCOC2=CC=1CCNC(=O)C1CN(CCCC)CCN1C(N=1)=CC(Cl)=NC=1N1C=CN=C1 KNZONLCAAIUDPK-UHFFFAOYSA-N 0.000 claims 1
- VLPXYVPPEHMULN-UHFFFAOYSA-N N-[2-(3,4-dimethoxyphenyl)ethyl]-2-(2-imidazol-1-ylpyrimidin-4-yl)-3,4-dihydro-1H-isoquinoline-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1CCNC(=O)C1N(C=2N=C(N=CC=2)N2C=NC=C2)CC2=CC=CC=C2C1 VLPXYVPPEHMULN-UHFFFAOYSA-N 0.000 claims 1
- JYVTUNKFNZHYDI-UHFFFAOYSA-N N-[2-(3-chloro-4-methoxyphenyl)ethyl]-1-(2-imidazol-1-ylpyrimidin-4-yl)-4-methylpiperazine-2-carboxamide Chemical compound C1=C(Cl)C(OC)=CC=C1CCNC(=O)C1N(C=2N=C(N=CC=2)N2C=NC=C2)CCN(C)C1 JYVTUNKFNZHYDI-UHFFFAOYSA-N 0.000 claims 1
- IMMNRFRVTDQENP-UHFFFAOYSA-N N-[2-(4-chlorophenyl)ethyl]-2-[1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)-4-methylpiperazin-2-yl]acetamide Chemical compound C1N(C)CCN(C=2N=C(N=C(C)C=2)N2C=NC=C2)C1CC(=O)NCCC1=CC=C(Cl)C=C1 IMMNRFRVTDQENP-UHFFFAOYSA-N 0.000 claims 1
- XRIWLOWFBDPBOC-UHFFFAOYSA-N N-[2-[1-(2-imidazol-1-yl-6-methylpyrimidin-4-yl)piperidin-2-yl]ethyl]-1,3-benzodioxole-5-carboxamide Chemical compound N=1C(C)=CC(N2C(CCCC2)CCNC(=O)C=2C=C3OCOC3=CC=2)=NC=1N1C=CN=C1 XRIWLOWFBDPBOC-UHFFFAOYSA-N 0.000 claims 1
- LHPXASSXMBBLQF-UHFFFAOYSA-N N-[[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]methyl]-2-(4-methoxyphenyl)acetamide Chemical compound C1=CC(OC)=CC=C1CC(=O)NCC1N(C=2N=C(N=CC=2)N2C=NC=C2)CCCC1 LHPXASSXMBBLQF-UHFFFAOYSA-N 0.000 claims 1
- DZEMVFARLGUTHI-UHFFFAOYSA-N N-heptyl-2-[1-[2-(2-imidazol-1-ylethyl)-6-methylpyrimidin-4-yl]piperidin-2-yl]acetamide Chemical compound CCCCCCCNC(=O)CC1CCCCN1C1=CC(C)=NC(CCN2C=NC=C2)=N1 DZEMVFARLGUTHI-UHFFFAOYSA-N 0.000 claims 1
- SBCTXBZIRQYPBK-UHFFFAOYSA-N N-hexyl-2-[1-(2-imidazol-1-ylpyrimidin-4-yl)piperidin-2-yl]acetamide Chemical compound CCCCCCNC(=O)CC1CCCCN1C1=CC=NC(N2C=NC=C2)=N1 SBCTXBZIRQYPBK-UHFFFAOYSA-N 0.000 claims 1
- OZZYAELZRDORGV-UHFFFAOYSA-N N1(C=NC=C1)C1=NC=CC(=N1)N1C(CN(CC1)CCCC)CC(=O)NCCC1=CC2=C(OCCO2)C=C1 Chemical compound N1(C=NC=C1)C1=NC=CC(=N1)N1C(CN(CC1)CCCC)CC(=O)NCCC1=CC2=C(OCCO2)C=C1 OZZYAELZRDORGV-UHFFFAOYSA-N 0.000 claims 1
- 102100006825 OXR1 Human genes 0.000 claims 1
- 108060005791 OXR1 Proteins 0.000 claims 1
- IZUPBVBPLAPZRR-UHFFFAOYSA-N Pentachlorophenol Chemical compound OC1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1Cl IZUPBVBPLAPZRR-UHFFFAOYSA-N 0.000 claims 1
- 241001387976 Pera Species 0.000 claims 1
- 241001401345 Piperia Species 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N THP Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 235000015450 Tilia cordata Nutrition 0.000 claims 1
- 235000011941 Tilia x europaea Nutrition 0.000 claims 1
- 235000018963 Tropaeolum tuberosum Nutrition 0.000 claims 1
- 240000000054 Tropaeolum tuberosum Species 0.000 claims 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 1
- 125000003670 adamantan-2-yl group Chemical group [H]C1([H])C(C2([H])[H])([H])C([H])([H])C3([H])C([*])([H])C1([H])C([H])([H])C2([H])C3([H])[H] 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 125000005167 cycloalkylaminocarbonyl group Chemical group 0.000 claims 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- RNCAJLLRSYSZAM-UHFFFAOYSA-N diazinane-3,6-dione Chemical compound O=C1CCC(=O)NN1 RNCAJLLRSYSZAM-UHFFFAOYSA-N 0.000 claims 1
- ROSDSFDQCJNGOL-UHFFFAOYSA-N dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 claims 1
- 125000004494 ethyl ester group Chemical group 0.000 claims 1
- LNOQURRKNJKKBU-UHFFFAOYSA-N ethyl piperazine-1-carboxylate Chemical compound CCOC(=O)N1CCNCC1 LNOQURRKNJKKBU-UHFFFAOYSA-N 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N furane Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- ALBYIUDWACNRRB-UHFFFAOYSA-N hexanamide Chemical compound CCCCCC(N)=O ALBYIUDWACNRRB-UHFFFAOYSA-N 0.000 claims 1
- 150000003949 imides Chemical class 0.000 claims 1
- 239000004571 lime Substances 0.000 claims 1
- 125000000040 m-tolyl group Chemical compound [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 125000002347 octyl group Chemical compound [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 1
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 1
- NWVVVBRKAWDGAB-UHFFFAOYSA-N p-methoxyphenol Chemical compound COC1=CC=C(O)C=C1 NWVVVBRKAWDGAB-UHFFFAOYSA-N 0.000 claims 1
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 1
- 125000000913 palmityl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- IPWFJLQDVFKJDU-UHFFFAOYSA-N pentanamide Chemical compound CCCCC(N)=O IPWFJLQDVFKJDU-UHFFFAOYSA-N 0.000 claims 1
- RCCYSVYHULFYHE-UHFFFAOYSA-N pentanediamide Chemical compound NC(=O)CCCC(N)=O RCCYSVYHULFYHE-UHFFFAOYSA-N 0.000 claims 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- DNUTZBZXLPWRJG-UHFFFAOYSA-N piperidine-1-carboxylic acid Chemical compound OC(=O)N1CCCCC1 DNUTZBZXLPWRJG-UHFFFAOYSA-N 0.000 claims 1
- 229940080818 propionamide Drugs 0.000 claims 1
- 125000006308 propyl amino group Chemical group 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- OYRRZWATULMEPF-UHFFFAOYSA-N pyrimidin-4-amine Chemical compound NC1=CC=NC=N1 OYRRZWATULMEPF-UHFFFAOYSA-N 0.000 claims 1
- KAESVJOAVNADME-UHFFFAOYSA-N pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 1
- IQHXABCGSFAKPN-UHFFFAOYSA-N pyrrolidine-3-carboxamide Chemical compound NC(=O)C1CCNC1 IQHXABCGSFAKPN-UHFFFAOYSA-N 0.000 claims 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 claims 1
- 102000008299 Nitric Oxide Synthase Human genes 0.000 abstract description 23
- 108010021487 Nitric Oxide Synthase Proteins 0.000 abstract description 23
- 230000002401 inhibitory effect Effects 0.000 abstract description 16
- 239000003112 inhibitor Substances 0.000 abstract description 11
- 150000003254 radicals Chemical class 0.000 description 37
- 125000004432 carbon atoms Chemical group C* 0.000 description 12
- 210000004027 cells Anatomy 0.000 description 11
- 238000004166 bioassay Methods 0.000 description 10
- 230000001939 inductive effect Effects 0.000 description 10
- 235000001014 amino acid Nutrition 0.000 description 8
- 230000015572 biosynthetic process Effects 0.000 description 7
- 102000011779 Nitric Oxide Synthase Type II Human genes 0.000 description 6
- 108010076864 Nitric Oxide Synthase Type II Proteins 0.000 description 6
- 241000700159 Rattus Species 0.000 description 6
- 125000004122 cyclic group Chemical group 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 206010003246 Arthritis Diseases 0.000 description 5
- 235000008206 alpha-amino acids Nutrition 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 230000002522 swelling Effects 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- UCSJYZPVAKXKNQ-HZYVHMACSA-N 1-[(1S,2R,3R,4S,5R,6R)-3-carbamimidamido-6-{[(2R,3R,4R,5S)-3-{[(2S,3S,4S,5R,6S)-4,5-dihydroxy-6-(hydroxymethyl)-3-(methylamino)oxan-2-yl]oxy}-4-formyl-4-hydroxy-5-methyloxolan-2-yl]oxy}-2,4,5-trihydroxycyclohexyl]guanidine Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 4
- 102000002004 Cytochrome P-450 Enzyme System Human genes 0.000 description 4
- 108010015742 Cytochrome P-450 Enzyme System Proteins 0.000 description 4
- 206010015150 Erythema Diseases 0.000 description 4
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 description 4
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 4
- 229910004664 ORa Inorganic materials 0.000 description 4
- 108010029485 Protein Isoforms Proteins 0.000 description 4
- 102000001708 Protein Isoforms Human genes 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 239000002671 adjuvant Substances 0.000 description 4
- 230000000240 adjuvant Effects 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 239000000969 carrier Substances 0.000 description 4
- 239000002158 endotoxin Substances 0.000 description 4
- 125000004438 haloalkoxy group Chemical group 0.000 description 4
- 239000002609 media Substances 0.000 description 4
- IOVCWXUNBOPUCH-UHFFFAOYSA-M nitrite anion Chemical compound [O-]N=O IOVCWXUNBOPUCH-UHFFFAOYSA-M 0.000 description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 4
- 125000003884 phenylalkyl group Chemical group 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 238000003786 synthesis reaction Methods 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- 229960003767 Alanine Drugs 0.000 description 3
- 239000004475 Arginine Substances 0.000 description 3
- 210000004369 Blood Anatomy 0.000 description 3
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- JKMHFZQWWAIEOD-UHFFFAOYSA-N HEPES Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 3
- 229940021015 I.V. solution additive Amino Acids Drugs 0.000 description 3
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 3
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 3
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 description 3
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 3
- 210000003141 Lower Extremity Anatomy 0.000 description 3
- 239000004472 Lysine Substances 0.000 description 3
- 102100002468 NOS1 Human genes 0.000 description 3
- 101700050622 NOS1 Proteins 0.000 description 3
- 101700006637 NOS3 Proteins 0.000 description 3
- 102100000871 NOS3 Human genes 0.000 description 3
- 101710026292 Os02g0104700 Proteins 0.000 description 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 3
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 description 3
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 description 3
- 150000001371 alpha-amino acids Chemical class 0.000 description 3
- 125000004103 aminoalkyl group Chemical group 0.000 description 3
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 description 3
- 230000000708 anti-progestin Effects 0.000 description 3
- 239000003418 antiprogestin Substances 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 3
- 239000011575 calcium Substances 0.000 description 3
- 229910052791 calcium Inorganic materials 0.000 description 3
- PMMYEEVYMWASQN-IMJSIDKUSA-N cis-L-hydroxyproline Chemical compound O[C@@H]1CN[C@H](C(O)=O)C1 PMMYEEVYMWASQN-IMJSIDKUSA-N 0.000 description 3
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000011156 evaluation Methods 0.000 description 3
- 239000012091 fetal bovine serum Substances 0.000 description 3
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 3
- 230000003647 oxidation Effects 0.000 description 3
- 238000007254 oxidation reaction Methods 0.000 description 3
- 230000008506 pathogenesis Effects 0.000 description 3
- 125000002071 phenylalkoxy group Chemical group 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 239000000044 progesterone antagonist Substances 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 238000006467 substitution reaction Methods 0.000 description 3
- 230000001225 therapeutic Effects 0.000 description 3
- 125000000335 thiazolyl group Chemical group 0.000 description 3
- OQEBBZSWEGYTPG-VKHMYHEASA-N (3S)-3-aminobutanoic acid Chemical compound C[C@H](N)CC(O)=O OQEBBZSWEGYTPG-VKHMYHEASA-N 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- MYRTYDVEIRVNKP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene Chemical compound C=CC1=CC=CC=C1C=C MYRTYDVEIRVNKP-UHFFFAOYSA-N 0.000 description 2
- PECYZEOJVXMISF-REOHCLBHSA-N 2,3-Diaminopropionic acid Chemical compound [NH3+]C[C@H](N)C([O-])=O PECYZEOJVXMISF-REOHCLBHSA-N 0.000 description 2
- WTDRDQBEARUVNC-LURJTMIESA-N 3-hydroxy-L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 2
- 206010000210 Abortion Diseases 0.000 description 2
- 229960005261 Aspartic Acid Drugs 0.000 description 2
- 210000004556 Brain Anatomy 0.000 description 2
- 101700033614 COR2 Proteins 0.000 description 2
- 102000000584 Calmodulin Human genes 0.000 description 2
- 108010041952 Calmodulin Proteins 0.000 description 2
- 102000003849 Cytochrome P450 Human genes 0.000 description 2
- 108050008488 Cytochrome P450 Proteins 0.000 description 2
- 102000004127 Cytokines Human genes 0.000 description 2
- 108090000695 Cytokines Proteins 0.000 description 2
- 229960002989 Glutamic Acid Drugs 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 229960000310 ISOLEUCINE Drugs 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 102000014150 Interferons Human genes 0.000 description 2
- 108010050904 Interferons Proteins 0.000 description 2
- 108010044467 Isoenzymes Proteins 0.000 description 2
- 235000014852 L-arginine Nutrition 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline zwitterion Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 description 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 2
- UKAUYVFTDYCKQA-VKHMYHEASA-N L-homoserine zwitterion Chemical compound OC(=O)[C@@H](N)CCO UKAUYVFTDYCKQA-VKHMYHEASA-N 0.000 description 2
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 2
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 2
- VVNCNSJFMMFHPL-GSVOUGTGSA-N L-penicillamine Chemical compound CC(C)(S)[C@H](N)C(O)=O VVNCNSJFMMFHPL-GSVOUGTGSA-N 0.000 description 2
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 2
- 210000002540 Macrophages Anatomy 0.000 description 2
- MBBZMMPHUWSWHV-BDVNFPICSA-N Meglumine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 2
- 229960004452 Methionine Drugs 0.000 description 2
- 229910004755 ORb Inorganic materials 0.000 description 2
- 241000658540 Ora Species 0.000 description 2
- 229940049954 Penicillin Drugs 0.000 description 2
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 2
- 239000004793 Polystyrene Substances 0.000 description 2
- RJKFOVLPORLFTN-STHVQZNPSA-N Progesterone Natural products O=C(C)[C@@H]1[C@@]2(C)[C@H]([C@H]3[C@@H]([C@]4(C)C(=CC(=O)CC4)CC3)CC2)CC1 RJKFOVLPORLFTN-STHVQZNPSA-N 0.000 description 2
- 229960002429 Proline Drugs 0.000 description 2
- 229960005322 Streptomycin Drugs 0.000 description 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Syngestrets Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 2
- 239000004473 Threonine Substances 0.000 description 2
- 101710008836 UQCRC2 Proteins 0.000 description 2
- 231100000176 abortion Toxicity 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 238000007792 addition Methods 0.000 description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 2
- 235000004279 alanine Nutrition 0.000 description 2
- 125000004414 alkyl thio group Chemical group 0.000 description 2
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 description 2
- 230000003042 antagnostic Effects 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 2
- 235000003704 aspartic acid Nutrition 0.000 description 2
- 239000012298 atmosphere Substances 0.000 description 2
- 125000002393 azetidinyl group Chemical group 0.000 description 2
- 229960000626 benzylpenicillin Drugs 0.000 description 2
- 125000002619 bicyclic group Chemical group 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 230000037348 biosynthesis Effects 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000000460 chlorine Substances 0.000 description 2
- 229960002173 citrulline Drugs 0.000 description 2
- 235000013477 citrulline Nutrition 0.000 description 2
- 230000001419 dependent Effects 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 229940079593 drugs Drugs 0.000 description 2
- 230000002357 endometrial Effects 0.000 description 2
- 230000004720 fertilization Effects 0.000 description 2
- 235000013922 glutamic acid Nutrition 0.000 description 2
- 239000004220 glutamic acid Substances 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 230000003053 immunization Effects 0.000 description 2
- 238000002649 immunization Methods 0.000 description 2
- 238000002513 implantation Methods 0.000 description 2
- 200000000018 inflammatory disease Diseases 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 229940079322 interferon Drugs 0.000 description 2
- RRHGJUQNOFWUDK-UHFFFAOYSA-N isoprene Chemical compound CC(=C)C=C RRHGJUQNOFWUDK-UHFFFAOYSA-N 0.000 description 2
- 229960003136 leucine Drugs 0.000 description 2
- 125000005647 linker group Chemical group 0.000 description 2
- 229960003646 lysine Drugs 0.000 description 2
- 235000018977 lysine Nutrition 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- 125000002950 monocyclic group Chemical group 0.000 description 2
- 125000001624 naphthyl group Chemical group 0.000 description 2
- 230000003000 nontoxic Effects 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 235000005985 organic acids Nutrition 0.000 description 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 2
- 229920002223 polystyrene Polymers 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 229960003387 progesterone Drugs 0.000 description 2
- 239000000186 progesterone Substances 0.000 description 2
- 239000000583 progesterone congener Substances 0.000 description 2
- 150000003180 prostaglandins Chemical class 0.000 description 2
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 description 2
- 229960001153 serine Drugs 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 125000003831 tetrazolyl group Chemical group 0.000 description 2
- 229960002898 threonine Drugs 0.000 description 2
- 210000001519 tissues Anatomy 0.000 description 2
- UCMIRNVEIXFBKS-UHFFFAOYSA-N β-Alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 description 2
- USQHEVWOPJDAAX-RITPCOANSA-N (1R,2S)-2-aminocyclohexane-1-carboxylic acid Chemical compound N[C@H]1CCCC[C@H]1C(O)=O USQHEVWOPJDAAX-RITPCOANSA-N 0.000 description 1
- CMUHFUGDYMFHEI-MRVPVSSYSA-N (2R)-2-amino-3-(4-aminophenyl)propanoic acid Chemical compound OC(=O)[C@H](N)CC1=CC=C(N)C=C1 CMUHFUGDYMFHEI-MRVPVSSYSA-N 0.000 description 1
- DLMYFMLKORXJPO-FQEVSTJZSA-N (2R)-2-amino-3-tritylsulfanylpropanoic acid Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(SC[C@H](N)C(O)=O)C1=CC=CC=C1 DLMYFMLKORXJPO-FQEVSTJZSA-N 0.000 description 1
- KKCIOUWDFWQUBT-CQSZACIVSA-N (2R)-2-azaniumyl-3-[4-(4-hydroxyphenoxy)phenyl]propanoate Chemical compound C1=CC(C[C@@H]([NH3+])C([O-])=O)=CC=C1OC1=CC=C(O)C=C1 KKCIOUWDFWQUBT-CQSZACIVSA-N 0.000 description 1
- JTTHKOPSMAVJFE-SECBINFHSA-N (2R)-2-azaniumyl-4-phenylbutanoate Chemical compound [O-]C(=O)[C@H]([NH3+])CCC1=CC=CC=C1 JTTHKOPSMAVJFE-SECBINFHSA-N 0.000 description 1
- OMGHIGVFLOPEHJ-BYPYZUCNSA-N (2S)-2,5-dihydro-1H-pyrrole-2-carboxylic acid Chemical compound OC(=O)[C@H]1NCC=C1 OMGHIGVFLOPEHJ-BYPYZUCNSA-N 0.000 description 1
- QHSCIWIRXWFIGH-LURJTMIESA-N (2S)-2-amino-2-methylpentanedioic acid Chemical compound OC(=O)[C@](N)(C)CCC(O)=O QHSCIWIRXWFIGH-LURJTMIESA-N 0.000 description 1
- POGSZHUEECCEAP-ZETCQYMHSA-N (2S)-2-amino-3-(3-amino-4-hydroxyphenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(N)=C1 POGSZHUEECCEAP-ZETCQYMHSA-N 0.000 description 1
- NIGWMJHCCYYCSF-QMMMGPOBSA-N (2S)-2-amino-3-(4-chlorophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(Cl)C=C1 NIGWMJHCCYYCSF-QMMMGPOBSA-N 0.000 description 1
- GTVVZTAFGPQSPC-QMMMGPOBSA-N (2S)-2-azaniumyl-3-(4-nitrophenyl)propanoate Chemical compound OC(=O)[C@@H](N)CC1=CC=C([N+]([O-])=O)C=C1 GTVVZTAFGPQSPC-QMMMGPOBSA-N 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N 1,2-ethanediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- HHOZSMKHSQQMJS-UHFFFAOYSA-N 1,3-dibromopropane Chemical group BrC[CH]CBr HHOZSMKHSQQMJS-UHFFFAOYSA-N 0.000 description 1
- UDYLPNOMYOUXSA-UHFFFAOYSA-N 1,3-difluoropropane Chemical group FC[CH]CF UDYLPNOMYOUXSA-UHFFFAOYSA-N 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N 1,4-Butanediol, dimethanesulfonate Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- PAJPWUMXBYXFCZ-UHFFFAOYSA-N 1-Aminocyclopropane-1-carboxylic acid Chemical compound OC(=O)C1(N)CC1 PAJPWUMXBYXFCZ-UHFFFAOYSA-N 0.000 description 1
- WOXWUZCRWJWTRT-UHFFFAOYSA-N 1-amino-1-cyclohexanecarboxylic acid Chemical compound OC(=O)C1(N)CCCCC1 WOXWUZCRWJWTRT-UHFFFAOYSA-N 0.000 description 1
- VXNZUUAINFGPBY-UHFFFAOYSA-N 1-butene Chemical group CCC=C VXNZUUAINFGPBY-UHFFFAOYSA-N 0.000 description 1
- 125000004973 1-butenyl group Chemical group C(=CCC)* 0.000 description 1
- 125000004972 1-butynyl group Chemical group [H]C([H])([H])C([H])([H])C#C* 0.000 description 1
- PBLZLIFKVPJDCO-UHFFFAOYSA-N 12-aminododecanoic acid Chemical compound NCCCCCCCCCCCC(O)=O PBLZLIFKVPJDCO-UHFFFAOYSA-N 0.000 description 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 description 1
- OGNSCSPNOLGXSM-UHFFFAOYSA-N 2,4-diaminobutyric acid Chemical compound NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 description 1
- LNDPCYHWPSQBCA-UHFFFAOYSA-N 2,5-diamino-2-methylpentanoic acid Chemical compound OC(=O)C(N)(C)CCCN LNDPCYHWPSQBCA-UHFFFAOYSA-N 0.000 description 1
- HPDVYZIJIBPYHI-UHFFFAOYSA-N 2-amino-3-(4-chlorophenyl)butanoic acid Chemical compound OC(=O)C(N)C(C)C1=CC=C(Cl)C=C1 HPDVYZIJIBPYHI-UHFFFAOYSA-N 0.000 description 1
- AKVBCGQVQXPRLD-UHFFFAOYSA-N 2-aminooctanoic acid Chemical compound CCCCCCC(N)C(O)=O AKVBCGQVQXPRLD-UHFFFAOYSA-N 0.000 description 1
- CGNMJIBUVDGMIY-UHFFFAOYSA-N 2-azaniumyl-2-(2-fluorophenyl)acetate Chemical compound OC(=O)C(N)C1=CC=CC=C1F CGNMJIBUVDGMIY-UHFFFAOYSA-N 0.000 description 1
- NYCRCTMDYITATC-UHFFFAOYSA-N 2-azaniumyl-3-(2-fluorophenyl)propanoate Chemical compound OC(=O)C(N)CC1=CC=CC=C1F NYCRCTMDYITATC-UHFFFAOYSA-N 0.000 description 1
- VWHRYODZTDMVSS-UHFFFAOYSA-N 2-azaniumyl-3-(3-fluorophenyl)propanoate Chemical compound OC(=O)C(N)CC1=CC=CC(F)=C1 VWHRYODZTDMVSS-UHFFFAOYSA-N 0.000 description 1
- PEMUHKUIQHFMTH-UHFFFAOYSA-N 2-azaniumyl-3-(4-bromophenyl)propanoate Chemical compound OC(=O)C(N)CC1=CC=C(Br)C=C1 PEMUHKUIQHFMTH-UHFFFAOYSA-N 0.000 description 1
- IRZQDMYEJPNDEN-UHFFFAOYSA-N 2-azaniumyl-3-phenylbutanoate Chemical compound OC(=O)C(N)C(C)C1=CC=CC=C1 IRZQDMYEJPNDEN-UHFFFAOYSA-N 0.000 description 1
- WTOFYLAWDLQMBZ-UHFFFAOYSA-N 2-azaniumyl-3-thiophen-2-ylpropanoate Chemical compound OC(=O)C(N)CC1=CC=CS1 WTOFYLAWDLQMBZ-UHFFFAOYSA-N 0.000 description 1
- 125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 description 1
- KFTHUBZIEMOORC-UHFFFAOYSA-N 2-methylbut-2-enamide Chemical compound CC=C(C)C(N)=O KFTHUBZIEMOORC-UHFFFAOYSA-N 0.000 description 1
- 125000006088 2-oxoazepinyl group Chemical group 0.000 description 1
- 125000004638 2-oxopiperazinyl group Chemical group O=C1N(CCNC1)* 0.000 description 1
- NYPYHUZRZVSYKL-ZETCQYMHSA-M 3,5-diiodo-L-tyrosinate(1-) Chemical compound [O-]C(=O)[C@@H]([NH3+])CC1=CC(I)=C([O-])C(I)=C1 NYPYHUZRZVSYKL-ZETCQYMHSA-M 0.000 description 1
- SAZOSDSFLRXREA-YFKPBYRVSA-N 3,5-dinitro-L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC([N+]([O-])=O)=C(O)C([N+]([O-])=O)=C1 SAZOSDSFLRXREA-YFKPBYRVSA-N 0.000 description 1
- UQTZMGFTRHFAAM-ZETCQYMHSA-N 3-Iodotyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(I)=C1 UQTZMGFTRHFAAM-ZETCQYMHSA-N 0.000 description 1
- WBXOONOXOHMGQW-UHFFFAOYSA-N 3-aminobicyclo[2.2.1]heptane-4-carboxylic acid Chemical compound C1CC2(C(O)=O)C(N)CC1C2 WBXOONOXOHMGQW-UHFFFAOYSA-N 0.000 description 1
- XXBOYULKNZTOMN-UHFFFAOYSA-N 3-azaniumyl-3-(2-nitrophenyl)propanoate Chemical compound OC(=O)CC(N)C1=CC=CC=C1[N+]([O-])=O XXBOYULKNZTOMN-UHFFFAOYSA-N 0.000 description 1
- XRXQOEWWPPJVII-UHFFFAOYSA-N 3-azaniumyl-4,4,4-trifluorobutanoate Chemical compound FC(F)(F)C(N)CC(O)=O XRXQOEWWPPJVII-UHFFFAOYSA-N 0.000 description 1
- CKTUXQBZPWBFDX-UHFFFAOYSA-N 3-azaniumylcyclohexane-1-carboxylate Chemical compound NC1CCCC(C(O)=O)C1 CKTUXQBZPWBFDX-UHFFFAOYSA-N 0.000 description 1
- VIIAUOZUUGXERI-UHFFFAOYSA-N 3-fluorotyrosine Chemical compound OC(=O)C(N)CC1=CC=C(O)C(F)=C1 VIIAUOZUUGXERI-UHFFFAOYSA-N 0.000 description 1
- AOKCDAVWJLOAHG-UHFFFAOYSA-N 4-(methylamino)butyric acid Chemical compound C[NH2+]CCCC([O-])=O AOKCDAVWJLOAHG-UHFFFAOYSA-N 0.000 description 1
- NIGWMJHCCYYCSF-UHFFFAOYSA-N 4-Chloro-3-phenyl-L-alanine Chemical compound OC(=O)C(N)CC1=CC=C(Cl)C=C1 NIGWMJHCCYYCSF-UHFFFAOYSA-N 0.000 description 1
- GTVVZTAFGPQSPC-UHFFFAOYSA-N 4-nitrophenylalanine Chemical compound OC(=O)C(N)CC1=CC=C([N+]([O-])=O)C=C1 GTVVZTAFGPQSPC-UHFFFAOYSA-N 0.000 description 1
- 125000005986 4-piperidonyl group Chemical group 0.000 description 1
- IPCUHQYGWOKSLR-UHFFFAOYSA-N 5-aminohexanoic acid Chemical compound CC(N)CCCC(O)=O IPCUHQYGWOKSLR-UHFFFAOYSA-N 0.000 description 1
- JJMDCOVWQOJGCB-UHFFFAOYSA-N 5-aminopentanoic acid zwitterion Chemical compound [NH3+]CCCCC([O-])=O JJMDCOVWQOJGCB-UHFFFAOYSA-N 0.000 description 1
- YSMODUONRAFBET-UHFFFAOYSA-N 5-hydroxylysine Chemical compound NCC(O)CCC(N)C(O)=O YSMODUONRAFBET-UHFFFAOYSA-N 0.000 description 1
- YLKRUSPZOTYMAT-UHFFFAOYSA-N 6-hydroxydopa Chemical compound OC(=O)C(N)CC1=CC(O)=C(O)C=C1O YLKRUSPZOTYMAT-UHFFFAOYSA-N 0.000 description 1
- XDOLZJYETYVRKV-UHFFFAOYSA-N 7-aminoheptanoic acid Chemical compound NCCCCCCC(O)=O XDOLZJYETYVRKV-UHFFFAOYSA-N 0.000 description 1
- UQXNEWQGGVUVQA-UHFFFAOYSA-N 8-aminooctanoic acid Chemical compound NCCCCCCCC(O)=O UQXNEWQGGVUVQA-UHFFFAOYSA-N 0.000 description 1
- GYDJEQRTZSCIOI-UHFFFAOYSA-N AMCHA Chemical compound NCC1CCC(C(O)=O)CC1 GYDJEQRTZSCIOI-UHFFFAOYSA-N 0.000 description 1
- QCTBMLYLENLHLA-UHFFFAOYSA-N Aminomethylbenzoic acid Chemical compound NCC1=CC=C(C(O)=O)C=C1 QCTBMLYLENLHLA-UHFFFAOYSA-N 0.000 description 1
- NQRKYASMKDDGHT-UHFFFAOYSA-N Aminooxyacetic acid Chemical compound NOCC(O)=O NQRKYASMKDDGHT-UHFFFAOYSA-N 0.000 description 1
- 229960001230 Asparagine Drugs 0.000 description 1
- 206010003816 Autoimmune disease Diseases 0.000 description 1
- KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 description 1
- 229960000794 Baclofen Drugs 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- JUHORIMYRDESRB-UHFFFAOYSA-N Benzathine Chemical compound C=1C=CC=CC=1CNCCNCC1=CC=CC=C1 JUHORIMYRDESRB-UHFFFAOYSA-N 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N Benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- JAONZGLTYYUPCT-UHFFFAOYSA-K Bismuth subgallate Chemical compound OC(=O)C1=CC(O)=C2O[Bi](O)OC2=C1 JAONZGLTYYUPCT-UHFFFAOYSA-K 0.000 description 1
- 210000001772 Blood Platelets Anatomy 0.000 description 1
- 102100004057 CYP3A4 Human genes 0.000 description 1
- 101710007540 CYP3A4 Proteins 0.000 description 1
- 208000005623 Carcinogenesis Diseases 0.000 description 1
- 210000000845 Cartilage Anatomy 0.000 description 1
- VDANGULDQQJODZ-UHFFFAOYSA-N Chloroprocaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1Cl VDANGULDQQJODZ-UHFFFAOYSA-N 0.000 description 1
- 229960002023 Chloroprocaine Drugs 0.000 description 1
- 229940107161 Cholesterol Drugs 0.000 description 1
- 229960001231 Choline Drugs 0.000 description 1
- 229920002676 Complementary DNA Polymers 0.000 description 1
- NILQLFBWTXNUOE-UHFFFAOYSA-N Cycloleucine Chemical compound OC(=O)C1(N)CCCC1 NILQLFBWTXNUOE-UHFFFAOYSA-N 0.000 description 1
- LRQKBLKVPFOOQJ-RXMQYKEDSA-N D-2-aminohexanoic acid Chemical compound CCCC[C@@H](N)C(O)=O LRQKBLKVPFOOQJ-RXMQYKEDSA-N 0.000 description 1
- SNDPXSYFESPGGJ-SCSAIBSYSA-N D-2-aminopentanoic acid Chemical compound CCC[C@@H](N)C(O)=O SNDPXSYFESPGGJ-SCSAIBSYSA-N 0.000 description 1
- LJCWONGJFPCTTL-SSDOTTSWSA-N D-4-hydroxyphenylglycine zwitterion Chemical compound [O-]C(=O)[C@H]([NH3+])C1=CC=C(O)C=C1 LJCWONGJFPCTTL-SSDOTTSWSA-N 0.000 description 1
- XUJNEKJLAYXESH-UWTATZPHSA-N D-cysteine Chemical compound SC[C@@H](N)C(O)=O XUJNEKJLAYXESH-UWTATZPHSA-N 0.000 description 1
- GGLZPLKKBSSKCX-RXMQYKEDSA-N D-ethionine Chemical compound CCSCC[C@@H](N)C(O)=O GGLZPLKKBSSKCX-RXMQYKEDSA-N 0.000 description 1
- UKAUYVFTDYCKQA-GSVOUGTGSA-N D-homoserine Chemical compound OC(=O)[C@H](N)CCO UKAUYVFTDYCKQA-GSVOUGTGSA-N 0.000 description 1
- AGPKZVBTJJNPAG-RFZPGFLSSA-N D-isoleucine Chemical compound CC[C@@H](C)[C@@H](N)C(O)=O AGPKZVBTJJNPAG-RFZPGFLSSA-N 0.000 description 1
- ROHFNLRQFUQHCH-RXMQYKEDSA-N D-leucine Chemical compound CC(C)C[C@@H](N)C(O)=O ROHFNLRQFUQHCH-RXMQYKEDSA-N 0.000 description 1
- AHLPHDHHMVZTML-SCSAIBSYSA-N D-ornithine Chemical compound NCCC[C@@H](N)C(O)=O AHLPHDHHMVZTML-SCSAIBSYSA-N 0.000 description 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 description 1
- HXEACLLIILLPRG-RXMQYKEDSA-N D-pipecolic acid Chemical compound OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 description 1
- AYFVYJQAPQTCCC-STHAYSLISA-N D-threonine Chemical compound C[C@H](O)[C@@H](N)C(O)=O AYFVYJQAPQTCCC-STHAYSLISA-N 0.000 description 1
- QIVBCDIJIAJPQS-SECBINFHSA-N D-tryptophane Chemical compound C1=CC=C2C(C[C@@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-SECBINFHSA-N 0.000 description 1
- OUYCCCASQSFEME-MRVPVSSYSA-N D-tyrosine Chemical compound OC(=O)[C@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-MRVPVSSYSA-N 0.000 description 1
- ZGUNAGUHMKGQNY-SSDOTTSWSA-N D-α-phenylglycine zwitterion Chemical compound OC(=O)[C@H](N)C1=CC=CC=C1 ZGUNAGUHMKGQNY-SSDOTTSWSA-N 0.000 description 1
- FFFHZYDWPBMWHY-UHFFFAOYSA-N DL-homocysteine Chemical compound OC(=O)C(N)CCS FFFHZYDWPBMWHY-UHFFFAOYSA-N 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N Diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
- 210000003038 Endothelium Anatomy 0.000 description 1
- 210000000981 Epithelium Anatomy 0.000 description 1
- 229940012017 Ethylenediamine Drugs 0.000 description 1
- 206010015548 Euthanasia Diseases 0.000 description 1
- 210000003414 Extremities Anatomy 0.000 description 1
- 102100000899 GNRH1 Human genes 0.000 description 1
- KFNRJXCQEJIBER-UHFFFAOYSA-N Gabaculine Chemical compound NC1CC(C(O)=O)=CC=C1 KFNRJXCQEJIBER-UHFFFAOYSA-N 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-N Gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 1
- WRUZLCLJULHLEY-UHFFFAOYSA-N Glycin Chemical compound OC(=O)CNC1=CC=C(O)C=C1 WRUZLCLJULHLEY-UHFFFAOYSA-N 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 108010084340 Gonadotropin-Releasing Hormone Proteins 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 102100016057 ISYNA1 Human genes 0.000 description 1
- 101710004164 ISYNA1 Proteins 0.000 description 1
- 206010062016 Immunosuppression Diseases 0.000 description 1
- 102000015696 Interleukins Human genes 0.000 description 1
- 108010063738 Interleukins Proteins 0.000 description 1
- SRJOCJYGOFTFLH-UHFFFAOYSA-N Isonipecotic acid Chemical compound OC(=O)C1CCNCC1 SRJOCJYGOFTFLH-UHFFFAOYSA-N 0.000 description 1
- 210000003734 Kidney Anatomy 0.000 description 1
- CMUHFUGDYMFHEI-UHFFFAOYSA-N L-2-Amino-3-(4-aminophenyl)propanoic acid Chemical compound OC(=O)C(N)CC1=CC=C(N)C=C1 CMUHFUGDYMFHEI-UHFFFAOYSA-N 0.000 description 1
- OYIFNHCXNCRBQI-BYPYZUCNSA-N L-2-aminoadipic acid Chemical compound OC(=O)[C@@H](N)CCCC(O)=O OYIFNHCXNCRBQI-BYPYZUCNSA-N 0.000 description 1
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-2-aminohexanoic acid zwitterion Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 description 1
- SNDPXSYFESPGGJ-BYPYZUCNSA-N L-2-aminopentanoic acid zwitterion Chemical compound CCC[C@H](N)C(O)=O SNDPXSYFESPGGJ-BYPYZUCNSA-N 0.000 description 1
- QNAYBMKLOCPYGJ-UWTATZPHSA-N L-Alanine Natural products C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 description 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- GGLZPLKKBSSKCX-YFKPBYRVSA-N L-ethionine Chemical compound CCSCC[C@H](N)C(O)=O GGLZPLKKBSSKCX-YFKPBYRVSA-N 0.000 description 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 1
- JTTHKOPSMAVJFE-VIFPVBQESA-N L-homophenylalanine Chemical compound OC(=O)[C@@H](N)CCC1=CC=CC=C1 JTTHKOPSMAVJFE-VIFPVBQESA-N 0.000 description 1
- 239000004395 L-leucine Substances 0.000 description 1
- 235000019454 L-leucine Nutrition 0.000 description 1
- WZNJWVWKTVETCG-YFKPBYRVSA-N L-mimosine zwitterion Chemical compound OC(=O)[C@@H](N)CN1C=CC(=O)C(O)=C1 WZNJWVWKTVETCG-YFKPBYRVSA-N 0.000 description 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 1
- VHVGNTVUSQUXPS-YUMQZZPRSA-N L-threo-3-phenylserine zwitterion Chemical compound [O-]C(=O)[C@@H]([NH3+])[C@@H](O)C1=CC=CC=C1 VHVGNTVUSQUXPS-YUMQZZPRSA-N 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 description 1
- ZGUNAGUHMKGQNY-ZETCQYMHSA-N L-α-phenylglycine Chemical compound OC(=O)[C@@H](N)C1=CC=CC=C1 ZGUNAGUHMKGQNY-ZETCQYMHSA-N 0.000 description 1
- 229920000126 Latex Polymers 0.000 description 1
- 210000004185 Liver Anatomy 0.000 description 1
- 229960003194 Meglumine Drugs 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 210000002027 Muscle, Skeletal Anatomy 0.000 description 1
- 241000186359 Mycobacterium Species 0.000 description 1
- 208000009525 Myocarditis Diseases 0.000 description 1
- DLAMVQGYEVKIRE-UHFFFAOYSA-N N-Methyl-a-aminoisobutyric acid Chemical compound CNC(C)(C)C(O)=O DLAMVQGYEVKIRE-UHFFFAOYSA-N 0.000 description 1
- XLXSAKCOAKORKW-KPKRHBJMSA-N N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl] Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-KPKRHBJMSA-N 0.000 description 1
- AYGYHGXUJBFUJU-UHFFFAOYSA-N N-[2-(prop-2-enoylamino)ethyl]prop-2-enamide Chemical compound C=CC(=O)NCCNC(=O)C=C AYGYHGXUJBFUJU-UHFFFAOYSA-N 0.000 description 1
- NPKSPKHJBVJUKB-UHFFFAOYSA-N N-phenylglycine Chemical compound OC(=O)CNC1=CC=CC=C1 NPKSPKHJBVJUKB-UHFFFAOYSA-N 0.000 description 1
- UNXRPIAFSZKXFX-UHFFFAOYSA-N N1C(CCCC1)CC(=O)NC1=C2NC=NC2=NC(=N1)N1C=NC=C1 Chemical compound N1C(CCCC1)CC(=O)NC1=C2NC=NC2=NC(=N1)N1C=NC=C1 UNXRPIAFSZKXFX-UHFFFAOYSA-N 0.000 description 1
- XPDJMVZDKBIHND-UHFFFAOYSA-N N1C(CCCC1)CC(=O)NC1=NC(=NC(=C1)Cl)C=1C=NC=CC=1 Chemical compound N1C(CCCC1)CC(=O)NC1=NC(=NC(=C1)Cl)C=1C=NC=CC=1 XPDJMVZDKBIHND-UHFFFAOYSA-N 0.000 description 1
- 101710045272 NANOS1 Proteins 0.000 description 1
- 102100007795 NANOS1 Human genes 0.000 description 1
- 102100007800 NANOS2 Human genes 0.000 description 1
- 101710045273 NANOS2 Proteins 0.000 description 1
- 101710045275 NANOS3 Proteins 0.000 description 1
- 102100007766 NANOS3 Human genes 0.000 description 1
- HOKKHZGPKSLGJE-GSVOUGTGSA-N NMDA Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 description 1
- XJLXINKUBYWONI-NNYOXOHSSA-N Nicotinamide adenine dinucleotide phosphate Chemical compound NC(=O)C1=CC=C[N+]([C@H]2[C@@H]([C@H](O)[C@@H](COP([O-])(=O)OP(O)(=O)OC[C@@H]3[C@H]([C@@H](OP(O)(O)=O)[C@@H](O3)N3C4=NC=NC(N)=C4N=C3)O)O2)O)=C1 XJLXINKUBYWONI-NNYOXOHSSA-N 0.000 description 1
- XJLSEXAGTJCILF-UHFFFAOYSA-N Nipecotic acid Chemical compound OC(=O)C1CCCNC1 XJLSEXAGTJCILF-UHFFFAOYSA-N 0.000 description 1
- FBTSQILOGYXGMD-LURJTMIESA-N Nitrotyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C([N+]([O-])=O)=C1 FBTSQILOGYXGMD-LURJTMIESA-N 0.000 description 1
- JFNLZVQOOSMTJK-UHFFFAOYSA-N Norbornene Chemical compound C1C2CCC1C=C2 JFNLZVQOOSMTJK-UHFFFAOYSA-N 0.000 description 1
- 229960003104 Ornithine Drugs 0.000 description 1
- 229960005190 Phenylalanine Drugs 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N Procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 239000007759 RPMI Media 1640 Substances 0.000 description 1
- 241000219061 Rheum Species 0.000 description 1
- GBFLZEXEOZUWRN-VKHMYHEASA-N S-carboxymethyl-L-cysteine Chemical compound OC(=O)[C@@H](N)CSCC(O)=O GBFLZEXEOZUWRN-VKHMYHEASA-N 0.000 description 1
- IDIDJDIHTAOVLG-VKHMYHEASA-N S-methyl-L-cysteine Chemical compound CSC[C@H](N)C(O)=O IDIDJDIHTAOVLG-VKHMYHEASA-N 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- 229940043230 Sarcosine Drugs 0.000 description 1
- 108010077895 Sarcosine Proteins 0.000 description 1
- 210000000952 Spleen Anatomy 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- FNKQXYHWGSIFBK-RPDRRWSUSA-N Tetrahydrobiopterin Chemical compound N1=C(N)NC(=O)C2=C1NC[C@H]([C@@H](O)[C@@H](O)C)N2 FNKQXYHWGSIFBK-RPDRRWSUSA-N 0.000 description 1
- 241000479530 Thuridilla neona Species 0.000 description 1
- AUYYCJSJGJYCDS-LBPRGKRZSA-N Thyrolar Chemical compound IC1=CC(C[C@H](N)C(O)=O)=CC(I)=C1OC1=CC=C(O)C(I)=C1 AUYYCJSJGJYCDS-LBPRGKRZSA-N 0.000 description 1
- KKCIOUWDFWQUBT-AWEZNQCLSA-N Thyronine Chemical compound C1=CC(C[C@H](N)C(O)=O)=CC=C1OC1=CC=C(O)C=C1 KKCIOUWDFWQUBT-AWEZNQCLSA-N 0.000 description 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 description 1
- 108010001801 Tumor Necrosis Factor-alpha Proteins 0.000 description 1
- 229960004441 Tyrosine Drugs 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 230000002378 acidificating Effects 0.000 description 1
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 description 1
- 125000005354 acylalkyl group Chemical group 0.000 description 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminum Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 description 1
- 230000000843 anti-fungal Effects 0.000 description 1
- 235000009697 arginine Nutrition 0.000 description 1
- 235000009582 asparagine Nutrition 0.000 description 1
- 125000002785 azepinyl group Chemical group 0.000 description 1
- 125000003828 azulenyl group Chemical group 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 description 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 description 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 1
- 229940000635 beta-Alanine Drugs 0.000 description 1
- 150000001576 beta-amino acids Chemical class 0.000 description 1
- GPRLTFBKWDERLU-UHFFFAOYSA-N bicyclo[2.2.2]octane Chemical compound C1CC2CCC1CC2 GPRLTFBKWDERLU-UHFFFAOYSA-N 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M buffer Substances [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 231100000504 carcinogenesis Toxicity 0.000 description 1
- 238000006555 catalytic reaction Methods 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000012069 chiral reagent Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- CRBHXDCYXIISFC-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CC[O-] CRBHXDCYXIISFC-UHFFFAOYSA-N 0.000 description 1
- PMMYEEVYMWASQN-QWWZWVQMSA-N cis-4-hydroxy-D-proline zwitterion Chemical compound O[C@H]1C[NH2+][C@@H](C([O-])=O)C1 PMMYEEVYMWASQN-QWWZWVQMSA-N 0.000 description 1
- 239000002299 complementary DNA Substances 0.000 description 1
- 238000003271 compound fluorescence assay Methods 0.000 description 1
- 239000003636 conditioned culture media Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 210000004748 cultured cells Anatomy 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- 125000005507 decahydroisoquinolyl group Chemical group 0.000 description 1
- 125000004855 decalinyl group Chemical group C1(CCCC2CCCCC12)* 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 229940043237 diethanolamine Drugs 0.000 description 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 125000004276 dioxalanyl group Chemical group 0.000 description 1
- 229910001882 dioxygen Inorganic materials 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N dopa Chemical compound OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 201000009273 endometriosis Diseases 0.000 description 1
- 230000003511 endothelial Effects 0.000 description 1
- 230000002255 enzymatic Effects 0.000 description 1
- 230000003628 erosive Effects 0.000 description 1
- 125000006260 ethylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000006125 ethylsulfonyl group Chemical group 0.000 description 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 235000019162 flavin adenine dinucleotide Nutrition 0.000 description 1
- FVTCRASFADXXNN-SCRDCRAPSA-N flavin mononucleotide Chemical compound OP(=O)(O)OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O FVTCRASFADXXNN-SCRDCRAPSA-N 0.000 description 1
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 description 1
- 239000011737 fluorine Chemical group 0.000 description 1
- 229910052731 fluorine Chemical group 0.000 description 1
- YCKRFDGAMUMZLT-UHFFFAOYSA-N fluorine atom Chemical group [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 1
- 238000005755 formation reaction Methods 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- 239000001963 growth media Substances 0.000 description 1
- ZRALSGWEFCBTJO-UHFFFAOYSA-O guanidinium Chemical group NC(N)=[NH2+] ZRALSGWEFCBTJO-UHFFFAOYSA-O 0.000 description 1
- 150000003278 haem Chemical class 0.000 description 1
- 238000001631 haemodialysis Methods 0.000 description 1
- 230000000322 hemodialysis Effects 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 description 1
- 229920001600 hydrophobic polymer Polymers 0.000 description 1
- 125000002632 imidazolidinyl group Chemical group 0.000 description 1
- 125000002636 imidazolinyl group Chemical group 0.000 description 1
- 230000003832 immune regulation Effects 0.000 description 1
- 230000003308 immunostimulating Effects 0.000 description 1
- 230000001506 immunosuppresive Effects 0.000 description 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 description 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 description 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000011630 iodine Chemical group 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical group II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 description 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 description 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 1
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000003965 isoxazolidinyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 239000004816 latex Substances 0.000 description 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 230000002101 lytic Effects 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 210000004962 mammalian cells Anatomy 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 125000006261 methyl amino sulfonyl group Chemical group [H]N(C([H])([H])[H])S(*)(=O)=O 0.000 description 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 229950002289 mimosine Drugs 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006011 modification reaction Methods 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- XTBLDMQMUSHDEN-UHFFFAOYSA-N naphthalene-2,3-diamine Chemical compound C1=CC=C2C=C(N)C(N)=CC2=C1 XTBLDMQMUSHDEN-UHFFFAOYSA-N 0.000 description 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 description 1
- 230000004703 negative regulation of smooth muscle contraction Effects 0.000 description 1
- 230000001537 neural Effects 0.000 description 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 description 1
- UMRZSTCPUPJPOJ-KNVOCYPGSA-N norbornane Chemical compound C1C[C@H]2CC[C@@H]1C2 UMRZSTCPUPJPOJ-KNVOCYPGSA-N 0.000 description 1
- 239000007764 o/w emulsion Substances 0.000 description 1
- 201000002674 obstructive nephropathy Diseases 0.000 description 1
- 125000005060 octahydroindolyl group Chemical group N1(CCC2CCCCC12)* 0.000 description 1
- 125000005061 octahydroisoindolyl group Chemical group C1(NCC2CCCCC12)* 0.000 description 1
- 230000003287 optical Effects 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000003431 oxalo group Chemical group 0.000 description 1
- 125000000160 oxazolidinyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- CMUHFUGDYMFHEI-QMMMGPOBSA-N para-Amino-phe Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N)C=C1 CMUHFUGDYMFHEI-QMMMGPOBSA-N 0.000 description 1
- 230000018052 penile erection Effects 0.000 description 1
- YIYBQIKDCADOSF-UHFFFAOYSA-N pentenoic acid group Chemical group C(C=CCC)(=O)O YIYBQIKDCADOSF-UHFFFAOYSA-N 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 description 1
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 description 1
- 125000005359 phenoxyalkyl group Chemical group 0.000 description 1
- 125000006678 phenoxycarbonyl group Chemical group 0.000 description 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 229920002401 polyacrylamide Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000005373 porous glass Substances 0.000 description 1
- 231100000683 possible toxicity Toxicity 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000001681 protective Effects 0.000 description 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 1
- 230000002685 pulmonary Effects 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 230000004648 relaxation of smooth muscle Effects 0.000 description 1
- 230000001850 reproductive Effects 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 235000019231 riboflavin-5'-phosphate Nutrition 0.000 description 1
- 229960004617 sapropterin Drugs 0.000 description 1
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine zwitterion Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 231100000486 side effect Toxicity 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 238000003153 stable transfection Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000004434 sulfur atoms Chemical group 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000002459 sustained Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- WCNFFKHKJLERFM-UHFFFAOYSA-N thiomorpholinyl sulfone group Chemical group N1(CCSCC1)S(=O)(=O)N1CCSCC1 WCNFFKHKJLERFM-UHFFFAOYSA-N 0.000 description 1
- ZCAGUOCUDGWENZ-UHFFFAOYSA-N thiomorpholinyl sulfoxide group Chemical group N1(CCSCC1)S(=O)N1CCSCC1 ZCAGUOCUDGWENZ-UHFFFAOYSA-N 0.000 description 1
- 238000003146 transient transfection Methods 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- 229960004295 valine Drugs 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- OYIFNHCXNCRBQI-UHFFFAOYSA-N α-Aminoadipic acid Chemical compound OC(=O)C(N)CCCC(O)=O OYIFNHCXNCRBQI-UHFFFAOYSA-N 0.000 description 1
- HYOWVAAEQCNGLE-UHFFFAOYSA-N α-Methylphenylalanine Chemical compound OC(=O)C(N)(C)CC1=CC=CC=C1 HYOWVAAEQCNGLE-UHFFFAOYSA-N 0.000 description 1
- FUOOLUPWFVMBKG-UHFFFAOYSA-N α-aminoisobutanoic acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 description 1
- YQGDEPYYFWUPGO-UHFFFAOYSA-N γ-amino-β-hydroxybutyric acid zwitterion Chemical compound [NH3+]CC(O)CC([O-])=O YQGDEPYYFWUPGO-UHFFFAOYSA-N 0.000 description 1
Abstract
N-Heterocyclic derivatives of formula (I) are described herein, as well as other N-Heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein
Description
N-HETEROCYCLIC DERIVATIVES NOS INHIBITORS
This application is a continuation in part of the application serial number 08 / 808,975, filed on February 19, 1997, which is hereby incorporated by reference in its entirety.
FIELD OF THE INVENTION
The invention relates to a series of compounds
N-heterocyclics and derivatives useful as inhibitors of nitric oxide synthase (NOS), and with therapy methods for various diseases using these compounds.
BACKGROUND OF THE INVENTION
Nitrogen monoxide (NO) has been linked to many different physiological processes, including smooth muscle relaxation, platelet inhibition, nerve transmission, immune regulation and penile erection. Nitric oxide is produced under various conditions in virtually all nucleated cells of mammals. Numerous pathologies have been ascribed to abnormalities in NO production that include attack, insulin dependent diabetes, hypotension induced by septic shock, rheumatoid arthritis and multiple sclerosis. Nitric oxide is synthesized in biological tissues by an enzyme called nitric oxide synthase (NOS) which uses NADPH and molecular oxygen to oxidize L-arginine to citrulline and nitric oxide. Nitric oxide synthase (NOS) exists in at least three forms, which fall into two main categories: constitutive and inducible. The two constitutive forms, which are dependent on calcium and calmodulin, have been identified, and an inducible isoform has been identified. The constitutive isoforms are: (1) a neuronal isoform, NOS-1 or nNOS, which is found in brain and skeletal muscles, and (2) an endothelial isoform, NOS-3 or eNOS, which is expressed in spleen endothelium blood, the epithelium of the bronchial tree in the brain. These constitutive isoforms are not the target of the NOS inhibitors of the present invention. The inducible isoform (NOS-2 or iNOS) is expressed virtually in all nucleated cells of mammals after exposure to inflammatory cytokines or lipopolysaccharides. Its presence in macrophages and pulmonary hepithelial cells is particularly notable. The inducible isoform is not stimulated by calcium and blocked by calmodulin antagonists. It contains several tightly bonded cofactors, which include FMN, FAD and tetrahydrobiopterin.
Nitric oxide generated by the inducible form of NOS has been implicated in the pathogenesis of inflammatory diseases. In experimental animals, impotention induced by lipopolysaccharide or tumor necrosis factor a can be reversed by NOS inhibitors. Conditions which lead to cytokine-induced hypotension include septic shock, hemodialysis, and interleukin therapy in cancer patients. The iNOS inhibitor is expected to be effective in treating cytokine-induced hypotension. In addition, recent studies have suggested a role for NO in the pathogenesis of inflammation and therefore inhibitors of NOS would have beneficial effects on inflammatory bowel disease, cerebral ischemia and arthritis. NOS inhibitors may also be useful in treating adult respiratory distress syndrome (ARDS) and myocarditis, and may be useful as adjuvants in short-term immunosuppression in transplant therapy. The diversity and ubiquity of the NO function in physiology makes its specific therapeutic objective of the phenomena related to NO an important consideration. Since the production of endogenous NO is the result of the actions of related but different isozymes, the differential inhibition of NOS isozymes allows a more selective therapy with fewer side effects.
BRIEF DESCRIPTION OF THE INVENTION
In one aspect, the invention is directed to compounds of formula (I), formula (II) and formula (III):
wherein: A is -R1, -OR1, -C (0) N (R1) R2, -P (0) [N (R1) R2] 2,
-NfR ^ CfOlR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16,
-S .O. IR1, -S02NHC (0) R1, -NHS02R2 :, -SO? J.R H, -C (0) NHS02R22, and
-CH = N0R1; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, 0 or C (R) H; each is N or CH; Q is chosen from the group consisting of a direct link,
-C (0) -, -0-, -CXN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1;
r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -NYR ^ CfOjNÍR ^ R16, -SFOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -NYR ^ UOJR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -SÍOA-R1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl;
and each R 1 and R 2 are independently selected from the group consisting of hydrogen, C 1 C alkyl ,. optionally substituted, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C6 alkenyl] -R9, - [C2-C6 alkynyl] -R9, - [C2-C6 alkyl] -R10 ( optionally substituted by hydroxy), - [C-C8] -R1: L (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [Ci-C alkyl] -N (R1) R2, - [C_-C8 alkyl] -N (R7R2, - [Ci-CJ-R6 alkyl, - [C2-C8 alkyl] -R10, - [Ci-Cgj-R11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl), or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q -R3 taken together, represent -C (0) OH, -C (0) N (R ^ R2, -C (= NH) -N (RX) R2 or
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -NYRXCtOJN R ^ R16, - N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (0) OR16, - [C0-C8 alkyl] -C (H) [ C (0) OR16] 2 and - [C.sub.C.sub.2 -C.sub.C. R 6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C 1 -C 8 alkyl, - [C 2 -C 8 alkyl] -R 10, - [C 7 -C .. alkyl- R 11, acyl, - C (0) R8, -C (O) ~ [Ci-Cgj-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl , monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R3-N (R1) C (0) -R23-N (R1) R2, -C (0) -N (R1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl;
- each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N0: or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. In another aspect, the invention is directed to compounds of formula (IV):
where: AA is an amino acid; X, Y and Z are independently N or C (R19); U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; W is N or CH; R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C_-C20 alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, - [C2-C8 alkenyl] -R9, - [alkynyl] of C2-C8] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [Ci-Cgj-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl;
R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -NR ^ .CONR ^ R16 , -N (R16) C (0) OR16, -N (R16) C (0) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C (H) ) [C (0) OR16] 2 and - [C0-C8 alkyl] -C (O) N (R1) R16; each R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino,
(triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl;
R19 is hydrogen, alkyl (optionally substituted by hydroxy), cyclopropyl, halo or haloalkyl; each R21 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and t is zero, 1 or 2; as a single isomer or mixture thereof, or a pharmaceutically acceptable salt thereof. In another aspect, the invention is directed to compounds of formula (Va), formula (Vb) or formula (Ve):
wherein B is a 5 or 6 membered carbocyclyl or heterocyclyl, optionally substituted; and wherein: A is -R1, -OR1, -C (O) N (R1) R2, -P (O) [N (R1) R2] ,,
-NR ^ COR2, -N (R16) C (0) OR2, -NR ^ R21, -N (R16) C (O) N (R1) R16, -SOiR1, -C (O) NHS02R22, and - CH = NOR1; each of X, Y and Z are independently N or C (R19); V is N (R4), S, O or C (R4) H;
each is N or CH; Q is chosen from the group consisting of a direct link, -C (0) -. -0-, -C (= N-R:) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R15) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R15, -S (0) tRx (when t is zero) or -NHSO, R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -NfR ^ R21, -N (R16) C (0) N ( R1) R16, -S (0) tRx (when t is zero) or -NHSO: R22, myn can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, [C2-C8 alkenyl] -R9, - [alkynyl] of C2-C8] -R9, - [C: -C8 alkyl] -R10 (optionally substituted by hydroxy), - [C1-C6] -R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [Ci-C alkyl,] -C (O) N (R1) R2, - [C_-CB alkyl] -NYR ^ R2, - [alkyl of C.-Cu.-R8, - [C2-C8 alkyl] -R10, - [Ci-Cgj-R11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C (0) N (R1) R2, -C (= NH) -N (R1) R2 or
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; Rd is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C 1 -C 8 alkyl, - [C 2 -C 8 alkyl] -R 10, - [C 1 -C 10 alkyl, acyl, -C ( 0) R8, -C (O) - [XC ..- R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2 , -C (0) -R23-N (R1) C (0) -R23-N (RX) R2, -C (0) -NÍR1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each Ru is independently chosen from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl;
each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. In another aspect, the invention is directed to a compound of formula (Vía), formula (VIb) or formula (VIc):
wherein B is a 5 or 6 membered carbocyclyl or heterocyclyl, optionally substituted; and wherein: A is -R1, -OR1, -UOJNtR R2, -P (O) [N (R1) R2] 2, -NYR ^ UOJR2, -N (R16) C (0) OR2, -NfR ^ R 1, -N (R 16) C (O) N (R 1) R 16, -S (O) tR 1, -SO ^ NHUOR 1, -NHS02R22, -S02N (R 1) H, -C (O) NHS02R22, and -CH ^ NOR1; each of X, and Z are independently N or C (R19); V is N (R4), S, O or C (R4) H; each W is N or CH;
Q is selected from the group consisting of a direct bond, -C (0) -, -0-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (R:) R21, -NÍR ^ ÍÇÍOJNfR R16, -SÍOXR1 (when t is zero) or -NHS0; R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -NYR ^ UOR2, -N (R16) C (0) OR2, -N (RX) R21, -N (RlS) C (0) N (R1) R16, -YES.R1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, C ^ C alkyl ,. optionally substituted, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C6 alkenyl] -R9, - [C2-C6 alkynyl] -R9, - [C2-C6 alkyl] -R10 ( optionally substituted by hydroxy), - [C1-C2] -R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C-C8 alkyl] -N (R1) R2, - [N (RX) alkyl, - [Ci alkyl] -Cgl-R6, - [C2-C8 alkyl] -R10, - [alkyl of X-CgJ-R11, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -CÍOJNfR R2, -C (= NH) -N (RX) R2 or
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [Cx-Cg.-R8 alkyl, - [C2-C8 alkyl] -R10, - [acyl alkyl, -C (0) R8, - C (O) - [X-CgJ-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl optionally substituted, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0 ) -R23-N (R1) C (0) -R23-N (R1) R2, -C (0) -N (R1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each Ru is independently chosen from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkylene R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl;
each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. In another aspect, the invention is directed to a compound of formula (Vlla), formula (Vllb) or formula (VIIc):
(Vlla);
A is -R1, -OR1, -ClOJNtR1) ^, -P (O) [N (R1) R2] 2,
-N (R C .O'R2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16,
-S .O. tR1. -SO NHCIOJR1, -NHS02R22, -S02N (R1) H, -C (O) NHSO, R22, and
-CH = NOR1; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, O or C (R4) H; each is N or CH;
Q is chosen from the group consisting of a direct link, -C (0) -. -0-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -NR ^ R21, -N (R16) C (0) N (R1) R16, -SÍOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R COR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -S (0) tR1 (when t is zero) or -NHS02R22, myn can not both be zero, t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C_-C2o alkyl, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C8 alkenyl] -R9, - [alkynyl] of C2-C8] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [C_-C8] -Rn (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [alkyl -C (O) N (R1) R2, - [C_-C8 alkyl] -N (RX) R2, - [C 2 -C 8 alkyl] -R 10, - [C 1 -C 8 alkyl] -Ru, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl) ); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C.O.N.R R2, -C (= NH) -N (R1) R2 O
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (R16) C ( 0) N (R1) R16, -N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0 alkyl] -C8] -C (H) [C (0) OR16] 2 and - [C.sub.-Cgl-UOJNIR R16 alkyl; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C2-C8 alkyl] -R10 alkyl, - [Ci-Cgl-R11 alkyl, acyl, -C (0) R8, -C (O) - [XC alkyl -R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, N optionally substituted heterocyclyl, -C (= NH) -N (CN) R1, -C (O) -R23-N (R1) R2, -C (O) -R23-N (R1) C (O) -R23 -N (R1) R2, -C (O) -N (R1) -R23-C (O) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl;
each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. In another aspect, the invention is directed to a compound of formula (VIII):
where two of X, Y and Z are nitrogen and the third is CH. In another aspect, the invention is directed to a compound of formula (IXa), formula (IXb) or formula (IXc):
where
it is a solid substrate; L is bond residue; each of X, Y and Z are independently N or C (R10);
each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, 0 or C (R4) H; each W is N or CH; Q is selected from the group consisting of a direct bond, -C (0) -, -0-, -C ^ N -R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (R2) R21, -NR ^ ÍUOJNÍR ^ R16, -SÍOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -NYR ^ CfOJR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -SÍOXR1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C8 alkenyl] -R9, - [C2 alkynyl] -C8] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [C_-C8] -Ru (optionally substituted by hydroxy), optionally substituted heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [alkyl of -N (R1) R2, - [Cj-Cg alkyl] -N (RX) R2, - [alkyl of Ci-CgUR6, - [C2-C8 alkyl] -R10, - [C_-Cg alkyl] -Rn, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2;
or -Q-R3 taken together, represent -C (0) OH, -C (0) N (R1) R2, -C (= NH) -N (RX) R2 or
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -NfR ^ lCfOlNlR1) ^ 6 , -N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C3 alkyl] -C (H) ) [C (0) OR16] 2 and - [alkyl of Co-CgUUOJNÍR1) R16; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C1-C8 alkyl] -R8, - [C: -C8 alkyl] -R10, - [C-Cg.-R11 alkyl, acyl, -C (0) R8, -C (O) - [C-C8 alkyl] -R8 . alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, N- optionally substituted heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R23-N (R1) C (0) -R23- N (R1) R2, -C (0) -N (R1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl;
each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R6 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. In another aspect, the invention is directed to a pharmaceutical composition comprising a compound of formula (I), formula (II) or formula (III) as described above and a pharmaceutically acceptable carrier. In another aspect, the invention is directed to a process for the synthesis of compounds of formula (I), formula (II) or formula (III):
R20) n
(III);
wherein: A is -R1, -OR1, -CFOINHR ^ R2, -P (O) [N (R1) R2] 2,
-NfR ^ CÍOlR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16,
-SIOltR1, -S02NHC (0) Rx, -NHS02R22, -C (O) NHS02R22, and
-CH ^ NOR1; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, or O; each W is N or CH; Q is chosen from the group consisting of a direct link,
-C (O) -, -O-, -CUN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1;
r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R :) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (Rx) Rlβ , -SÍOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -NR ^ C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N ( R1) R16, -SÍOXR1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl;
and each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C2-C2o alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, [C2-C8 alkenyl] -R9, - [ C2-C8 alkynyl] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [C ^ C -R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [Ci-C alkyl] -C (O) N (R1) R2, - [CX-C8 alkyl] -N (RX) R2, - [Cx-C8 alkyl] -R8. - [C2-C8 alkyl] -R10, - [C de-Cgj-R 11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C.O.N.R1) R2 / -C (= NH) -N (RX) R2 or
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (R ^ .CONR R16, -N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C ( H) [C (0) OR16] 2 and - [C 1 -C 8 alkyl-UOWR R 16; R 6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of X-CgJ-R 8, - [ C2-C3] -R10, - [alkyl of X-Cg.-R11, acyl, -C (0) R8, -C (O) - [C1-C8 alkyl] -R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, aryl l-sulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R23-N (R1) C (0 ) -R23-N (R1) R2, -C (0) -N (R2) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each Ru is independently chosen from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl;
each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; comprising the sequential steps of: (a) reacting an equivalent of a compound of formula (XI):
where W is N or CH; with about one equivalent of a chloro substituted compound of formula (XII):
Cl X:? N: XI
wherein X, Y and Z are independently N or C (R19); U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19, and with the proviso that X, Y and Z can not all be C (R19) when U is C (R5); R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -NÍR ^ UÍOJNÍR R16, - N (R16) C (0) OR16, -N (R16) C (0) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C (H) [ C (0) OR16] 2 and - [Co-C-UJNfR ^ R16 alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl;
- A l eada. R19 is independently hydrogen, alkyl (optionally substituted by hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; and each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; to produce a compound of the formula (XIII):
(b) reacting a compound of formula (XIII) with a compound of formula (XlVa), formula (XlVb), or formula (XIVc):
where: A is -R1, -OR1, -C (0) i (R1) Rz, -P (O) [N (R1) R2] 2, -NÍR ^ CÍOÍR2, -N (R16) C (0) OR2, -N (R1) R21, -N (R16) C (O) N (R1) R16,
-S (0) _Rx, -S02NHC (0) R1, -NHS02R22, -SO? J.RH, -C (O) NHSO, R22, and -CH = NOR1; V is N (R4), S, or O;
Q is chosen from the group consisting of a direct link, -C (0) -. -0-, -C (= N-R1) -, -S (0), and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) CONR ^ R16, -SÍOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R ^ C.O) R :, -N (R16) C (0) OR2, -N.R ^ R21. -N (R16) C (0) N (R1) R16, -SÍOXR1 (when t is zero) or -NHS02R22, m and n can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; and each R1 and R2 are independently selected from the group consisting of hydrogen, X-C alkyl. optionally substituted, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C6 alkenyl] -R9, - [C2-C6 alkynyl] -R9, - [C2-C6 alkyl] -R10 ( optionally substituted by hydroxy), - [X-Cgj-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C-Cg alkyl] -N (R1) R2, - [X-Cg alkyl] -NYR ^ R, - [ XC alkyl -R6, - [C2-C8 alkyl] -R10, - [Ci-Cgj-R11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C (0) ri (R1) R2, -C (= NH) -NtR R2 O
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C1-C8 alkyl] -R8, - [C2-C8 alkyl] -R10, - [alkyl of X-Cgj-R11, acyl, -C (0) R8, -C (O) - [X-Cg.-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1 ) R2, -C (0) -R23-N (R1) C (O) -R23-N (R1) R2, -C (O) -N (R1) -R23-C (O) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl;
each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; to produce a compound of formula (I), formula
(II) or formula (III). In another aspect, the invention is directed to synthesize a compound of formula (I), formula (II) or formula
(III):
H) q - (C (R13) H) -D4- (C (R14) R2 °) n-A
(III);
wherein: A is -C (0) N (Rla) R2; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, 0 or C (R4) H; each W is N or CH; Q is selected from the group consisting of a direct bond, -C (0) -, -O-, -CUN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4;
n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -NYR ^ R21,
-NfR ^ lCfOlNtR'lR16, -SÍOXR1 (when t is zero) or -NHSO: R22, n, q and r can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R2) C (0) R2, -N (R16) C (0) OR2, -NYR ^ R21, -N (R16) C (0) N ( R1) R16, -SFOl.R1 (when t is zero) or -NHS02R22, m and n can not both be zero; t is zero, 1 or 2;
is an optionally substituted N-heterocyclyl;
is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; R: a is hydrogen; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C_-C20 alkyl, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C6 alkenyl] -R9, - [alkynyl] of C2-C6] -R9, - [C2-C6 alkyl] -R10 (optionally substituted by hydroxy), - [C_-C8] -Rn (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C_-C8 alkyl] -N (R1) R2, - [C_-C8 alkyl] -N (RX) R2, - [Cx-C8 alkyl] -R6, - [C2-C8 alkyl] -R10, - [alkyl of X-Cgj-R11, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -CÍOJNÍR ^ R2, -C (= NH) -N (R1) R2 O
R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (R ^ .CON R1) R16, -N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (0) OR16, - [C0-CS alkyl] - C (H) [C (0) OR16] 2 and - [alkyl of R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of X-Cg.-R8, - [C2-C8 alkyl] -R10, - [Ci-Cgj-R11 alkyl, acyl, -C (0) R8, -C (O) - [X-Cg-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylamin ocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R23-N (R1) C (0 ) -R23-N (R1) R2, -C (0) -N (RX) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl;
each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S0R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; which comprises photolytically separating the compound of formula (IXa), formula (IXb) or formula (IXc):
; where U, V,, X, Y and Z are as defined in the above; R2, R3, R12, R13, R14, R15, R17 and R20 are as defined in the above;
it is a solid substrate; and L is the linking residue of the formula (IX);
wherein the valency not satisfied to the right of the formula represents the point of attachment to the solid substrate and the valence not satisfied to the left of the formula represents the point of attachment to the ligand; to form the compound of formula (I), formula (II) and formula (III) as defined above.
In another aspect, the invention is directed to a method for treating a condition resulting from an abnormality in the production of nitric oxide, which comprises administering to a mammal having a condition resulting from an abnormality in the production of nitric oxide, of a therapeutically effective amount of a compound of formula (I), formula (II), formula (III), formula (IV), formula (Va), formula (Vb), formula (Ve), formula (Via), formula (VIb), formula (VIc), formula (Vlla), formula (Vllb), formula (VIIc), as defined in the above.
DETAILED DESCRIPTION OF THE INVENTION
Definitions
As used in this specification and in the accompanying clauses, unless otherwise specified, the following terms have the meaning indicated: "Alkyl" refers to a straight or branched hydrocarbon chain radical consisting solely of carbon atoms and hydrogen, which do not contain saturations, having 1 to 8 carbon atoms, and which is attached to the rest of the molecule by a single bond, for example, methyl, ethyl, n-propyl, 1-methylethyl (isoprene), propyl), n-butyl, n-pentyl, 1,1-dimethylethyl (t-butyl), and the like. Alkyl radicals having more than 8 carbon atoms are indicated herein by the notation "[C -C alkyl]" where x and y indicate the number of carbons present. The alkyl radicals may optionally be substituted by one or more substituents which are independently selected from the group consisting of halo, hydroxy, alkoxy, carboxy, cyano, carbonyl, alkoxycarbonyl, cyano, amino, monoalkylamino, dialkylamino, nitro, alkylthio, amidino, aryl, heterocyclyl, aryloxy, aralkoxy, acylamino, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl. "Alkenyl" refers to a monovalent or divalent radical, straight or branched chain, consisting solely of carbon and hydrogen, containing at least one double bond and having from 1 to 8 carbon atoms, for example, ethenyl, prop-1-enyl, but-1-enyl, pen-1-enyl, penta-1,4-dienyl, and the like. "Alkynyl" refers to a straight or branched chain monovalent or divalent radical consisting solely of carbon and hydrogen, containing at least one triple bond and having from 1 to 8 carbon atoms, for example, ethinyl, propyl 1-butyl, but-1-ynyl, pen-1-ynyl, pent-3-ynyl and the like. "Alkoxy" refers to a radical of the formula -ORa wherein Ra is an alkyl radical as defined above, for example, methoxy, ethoxy, propoxy and the like.
"Alkoxycarbonyl" refers to a radical of the formula -C (0) ORa wherein Ra is an alkyl radical as defined above, for example methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl and the like. "Alkoxycarbonylalkyl" refers to a radical of the formula -Ra-C (0) ORa wherein each Ra is independently an alkyl radical as defined above, for example 2- (methoxycarbonyl) ethyl, 3- (ethoxycarbonyl) propyl, - (n-propoxycarbonyl) butyl and the like. "Alkylsulfonylamino" refers to a radical of the formula -N (H) S (O) 2-Ra wherein Ra is an alkyl radical as defined above, for example methylsulfonylamino, ethylsulfonylamino and the like. "Alkylsulfonyl" refers to a radical of the formula -S (0) 2-Ra wherein Ra is an alkyl radical as defined above, for example methanesulfonyl, ethylsulfonyl and the like. "Alkylthio" refers to a radical of the formula -S-Ra wherein Ra is an alkyl radical as defined above, for example methylthio, ethylthio, n-propylthio and the like. "Amidino" refers to a radical of the formula -C (NH) -NH2. "Amino" refers to a radical of the formula -NH2-. "Aminocarbonyl" refers to a radical of the formula -C (0) NH ,.
"Aminosulfonyl" refers to a radical of the formula -S (0) 2NH2. "Aryl" refers to a phenyl or naphthyl radical. The aryl radical may be optionally substituted by one or more substituents which are selected from the group consisting of hydroxy, mercapto, halo, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, phenylalkenyl, alkoxy, phenoxy, phenylalkoxy, haloalkyl, haloalkoxy, formyl, Nitro, cyano, cycloalkyl, hydroxyalkyl, alkoxyalkyl, phenoxy 1 quxy, phenylalkoxyalkyl, amidino, ureido, alkoxycarbonylamino, amino, monoalkylamino, dialkylamino, mono f in i 1 ami, monophenylalkylamino, sulfonylamino, alkylsulfonylamino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl , monophenylaminoalkyl, monophenylalkylaminoalkyl, acyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminocarbonylalkyl, monoalkylaminocarbonyl and dialkylaminocarbonylalkyl, as defined herein. "Aralkyl" refers to a radical of the formula -RaRb wherein Ra is an alkyl radical as defined above and Rb is an aryl radical as defined above, for example benzyl and the like. The aryl radical may optionally be substituted as described above. "Aryloxy" refers to a radical of the formula -ORb wherein Rb is an aryl radical as defined above, for example phenoxy and naphthoxy, and the like. The aryl radical may optionally be substituted as described above. "Aryloxycarbonyl" refers to a radical of the formula -C (0) ORb wherein Rb is an aryl radical as defined above, for example phenoxycarbonyl. "Aralkoxy" refers to a radical of the formula -0RC wherein Rc is an aralkyl radical as defined above, for example benzyloxy, and the like. The aralkyl radical optionally may be substituted as described above. "Aralkoxycarbonyl" refers to a radical of the formula -C (0) ORc wherein Rc is an aralkyl radical as defined above, for example benzyloxycarbonyl and the like. The aralkyl radical may be optionally substituted as described above. "Arylaminocarbonyl" refers to a radical of the formula -C (O) N (Rb) H wherein RD is an aryl radical as defined above, for example phenylaminocarbonyl and the like. The aryl radical may optionally be substituted as described above. "Arylaminosulfonyl" refers to a radical of the formula -S (0) 2N (Rb) H wherein Rb is an aryl radical as defined above, for example phenylaminosulfonyl and the like. The aryl radical optionally may be substituted as described above. "Aryisulfonyl" refers to a radical of the formula -S (0) 2 -Rb wherein Rb is an aryl radical as defined above, for example phenylsulfonyl and the like. The aryl radical optionally may be substituted as described above. "Arylsulfonylaminocarbonyl" refers to a radical of the formula -C (0) N (H) S (0) 2Rb wherein Rb is an aryl radical as defined above, for example phenylsulfonylaminocarbonyl and the like. The aryl radical optionally may be substituted as described above. "Acyl" refers to a radical of the formula -C (0) -Ra and -C (0) RD wherein Ra is an alkyl radical as defined above, and Rb is an aryl radical as defined above, for example acetyl, propionyl, benzoyl and the like. "Acylamino" refers to a radical of the formula -N (H) -C (0) -Ra and -N (H) -C (0) -Rb wherein Ra is an alkyl radical as defined above, and Rb is an aryl radical as defined above, for example acetylamino, benzoylamino and the like. "Alkylene" refers to a straight or branched chain divalent radical consisting solely of carbon and hydrogen, which does not contain saturations and which has 1 to 8 carbon atoms, for example methylene, ethylene, propylene, n-butylene and the like . The alkylene radical optionally may be substituted by one or more substituents which are selected from the group consisting of alkyl, hydroxy, -N (R16) R24 or -IOINIR'IR16, wherein R1, R16 and R21 are as defined in the foregoing , in the brief description of the invention. "Amino acid" refers to a divalent radical of the formula -N (R1) -R23-C (0) - wherein R1 is as described above in the brief description of the invention for R1 and R23 is an amino acid residue. "Amino acid residue" refers to the alkylene chain between the nitrogen atom and the carboxy group, which is substituted by various "side chains" of known amino acids. For example, the amino acid residues for the α-amino acids include carbon a (to which the carboxy group and the nitrogen atom are attached) and the side chain. For example, the amino acid residue of alanine is -C (CH3) -; the amino acid residue of serine is -C (CH; 0H) -, and so on. Therefore, it is understood that the term "amino acid" includes α-amino acids, β-amino acids, α-amino acids and so on, and all optical isomers thereof. Examples of such amino acids include alanine, asparagine, n-β-trityl-asparagine, aspartic acid, β-t-butylester of aspartic acid, arginine, N-tr-arginine, cysteine, S-trityl-cysteine, glutamic acid,? -t-butylester of glutamic acid, glutamine, N -? - trityl-glutamine, glycine, histidine, Nra-trityl-histidine, isoleucine, leucine, lysine, Nc-Boc-lysine, methionine, phenylalanine, proline, serine, Ot- butyl-serine, threonine, tryptophan, Nn-Boc-tryptophan (tyrosine, valine, sarcosine, L-alanine, chlorine-L-alanine, 2-aminoisobutyric acid, 2- (methylamino) isobutyric acid, D, L-3- acid aminoisobutyric, acid
(R) - (-) -2-aminoisobutyric, (S) - (+) -2-aminoisobutyric acid, D-leucine, L-leucine, D-norvaline, L-norvaline, L-2-amino-4-acid pentenoic, D-isoleucine, L-isoleucine, D-norleucine, 2,3-diaminopropionic acid, L-norleucine, D, L-2-aminocaprylic acid, β-alanine, D, L-3-aminobutyric acid, 4- aminobutyric, acid
4- (methylamino) butyric acid, 5-aminovaleric acid, 5-aminocaproic acid, 7-aminoheptanoic acid, 8-aminocaprylic acid, 11-aminodecanoic acid, 12-aminododecanoic acid, carboxymethoxylamine, D-serine, D-homoserine, L-homoserine , D-halotreonin, L-halotreonin, D-threonine, L-threonine, D, L-4-amino-3-hydroxybutyric acid, D, L-3-hydroxynorvaline, (3S, 4S) - (-) - statin, 5-hydroxy-D, L-lysine, 1-amino-1-cyclopropanecarboxylic acid, 1-amino-1-cyclopentanecarboxylic acid, 1-amino-1-cyclohexanecarboxylic acid, 5-amino-1, 3-cyclohexadiene-1- carboxylic acid, 2-amino-norbornancarboxylic acid, (S) - (-) -2-azetidinocarboxylic acid, cis-4-hydroxy-D-proline, cis-4-hydroxy-L-proline, trans-4-hydroxy-L- proline, 3, 4-dehydro-D, L-proline, 3, 4-dehydro-L-proline, D-pipecolinic acid, L-pipelnylic acid, nipecotic acid, isonipecotic acid, mimosine, 2,3-diaminopropionic acid, acid D, L-2, 4-diaminobutyric acid, (S) - (+) - diaminobutyric acid, D-ornithine, L-ornithine, 2-methylornithine, Ne-methyl-L-lysine, N-methyl-D-aspartic acid, D, L-2-methylglutamic acid, D, L-2-aminoadipic acid, D-2- acid aminoadipic, L-2-aminoadipic acid, (+/-) -3-aminoadipic acid, D-cysteine, L-penicillamine, L-penicillamine, D, L-homocysteine, S-methyl-L-cysteine, L-methionine, D-ethionine, L-ethionine, S-carboxymethyl-L-cysteine, (S) (+) - 2-phenylglycine, (R) (-) -2-phenylglycine, N-phenylglycine, N- (4-hydroxyphenyl) glycine , D-phenylalanine, thienylalanine, (S) - (-) indole-2-carboxylic acid, α-methyl-D, L-phenylalanine, β-methyl-D, L-phenylalanine, D-homophenylalanine, L-homophenylalanine, DL -2-fluorophenylglycine, D, L-2-fluorophenylalanine, DL-3-fluorophenylalanine, D, -4-fluorophenylalanine, DL-4-chlorophenylalanine, L-4-chlorophenylalanine, 4-bromo-D, L-phenylalanine, 4- iodine-D-phenylalanine, 3, 3 ', 5-triiodo-L-thyronine, (+) - 3, 3', 5-triiodo-L-thyronine, D-thyronine, L-thyronine, D, Lm-torosine, D-4-hydroxyphenylglycine, D-tyrosine, t-tyrosine, 0-methyl-L -tyrosine, 3-fluoro-D, L-tyrosine, 3-iodo-L-tyrosine, 3-nitro-L-tyrosine, 3,5-diiodo-L-tyrosine, D, L-dopa, L-dopa, 2 , 4, 5-trihydroxyphenyl-D, L-alanine, 3-amino-L-tyrosine, 4-amino-D-phenylalanine, 4-amino-L-phenylalanine, 4-amino-D, L-phenylalanine, 4-nitro -L-phenylalanine, 4-nitro-D, L-phenylalanine, 3,5-dinitro-L-tyrosine, D, La-methyltyrosine, La-methyltyrosine, (-) -3- (3, 4-dihydroxyphenyl) -2 -methyl-L-alanine, D, L-threo-3-phenylserine, trans-4- (aminomethyl) cyclohexanecarboxylic acid, 4- (aminomethyl) benzoic acid, D, L-3-aminobutyric acid, 3-aminocyclohexanecarboxylic acid, cis-2-amino-1-cyclohexanecarboxylic acid, α-amino-β- (p-chlorophenyl) butyric acid (Baclofen), D, L-3-aminophenylpropionic acid, 3-amino-3- (4-c 1) orophenic acid 1) propionic, 3-amino-3 - (2-nitrophenyl) propionic acid, and 3-amino-4,4,4-trifluorobutyric acid. "Carbocyclyl" refers to a stable 3- to 15-membered ring radical consisting solely of carbon and hydrogen atoms. For purposes of this invention, the carbocyclyl radical may be a monocyclic, bicyclic or tricyclic ring system, and may include fused or bridging ring system, the ring system may be partially or completely saturated, or be aromatic, and carbon atoms in the ring system may optionally be oxidized. Examples of such carbocyclic radicals include, but are not limited to cycloalkyl radicals (as defined herein) norbornane, norbornene, adamantyl, bicyclo [2.2.2] octane, phenyl, naphthalenyl, indanyl, indenyl, azulenyl, fluorenyl, anthracenyl , and similar. The carbocyclyl ring may be substituted by R8 as described above in the brief description of the invention, or by one or more substituents that are selected from the group consisting of hydroxy, mercapto, halo, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, phenylalkenyl, alkoxy, phenoxy, phenylalkoxy, haloalkyl, haloalkoxy, formyl, nitro, cyano, cycloalkyl. , hydroxyalkyl, alkoxyalkyl, phenoxy-1-amino, phenylalkoxyalkyl, amidino, ureido, alkoxycarbonylamino, amino, monoalkylamino, dialkylamino, mon-ofenyl-1-amino, monophenylalkylamino, sulfonylamino, alkylsulfonylamino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, monophenylaminoalkyl, monophenylalkylaminoalkyl, acyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminocarbonylalkyl, monoalkylaminocarbonyl and dialkylaminocarbonylalkyl, as defined herein. "cycloalkyl" refers to a stable monocyclic or bicyclic radical of 3 to 10 members which is saturated, and which consists solely of carbon and hydrogen atoms, for example cyclopropyl, cyclobutyl, cyclohexyl, decalinyl and the like. Unless specifically stated otherwise in the specification, the term "cycloalkyl" means to include cycloalkyl radicals which are optionally substituted by one or more substituents that are independently selected from the group consisting of alkyl, halo, hydroxy, amino, cyano, nitro, alkoxy, carboxy and alkoxycarbonyl. "Carboxi" refers to the radical of the formula -C (0) OH. "Carboxyalkyl" refers to the radical of the formula
-Ra-C (0) OH wherein Ra is an alkyl radical as defined above, for example carboxymethyl, 2-carboxyethyl, 3-carboxypropyl and the like. "Di (alkoxy) alkyl" refers to the radical of the formula -Ra (-ORa) _ wherein each Ra is independently an alkyl radical as defined above, and wherein the -0Ra groups can be attached at any carbon in the Ra group, for example 3, 3-dimethoxypropyl, 2,3-dimethoxypropyl and the like. "Dialkylamino" refers to the radical of the formula -N (Ra) Ra wherein each Ra is independently an alkyl radical as defined above, for example dimethylamino, diethylamino, (methyl) (ethyl) amino and the like. "Dialkylaminocarbonyl" refers to the radical of the formula -C (0) N (Ra) Ra wherein each Ra is independently an alkyl radical as defined above, for example dimethylaminocarbonyl, methylethylaminocarbonyl, diethylaminocarbonyl, dipropylaminocarbonyl, ethylpropylaminocarbonyl and the like. "Dialkylaminosulfonyl" refers to the radical of the formula -S (O) 2N (Ra) Ra wherein each Ra is independently an alkyl radical as defined above, for example dimethylaminosulfonyl, methylethylaminosulfonyl, diethylaminosulfonyl, dipropylaminosulfonyl, ethylpropylaminosulfonyl, and the like . "Halo" refers to bromine, chlorine, iodine or fluorine. "Haloalkyl" refers to an alkyl radical as defined above, which is substituted by one or more halo radicals, as defined above, for example trifluoromethyl, difluoromethyl, trichloromethyl, 2,2,2-trifluoroethyl, 1-fluoromethyl -2-fluoroethyl, 3-bromo-2-fluoropropyl, 1-bromomethyl-2-bromoethyl and the like. "Haloalkoxy" refers to a radical of the formula -0Rd, wherein each Rd is a haloalkyl radical as defined above, for example trifluoromethoxy, difluoromethoxy, trichloromethoxy, 2,2,2-trifluoroethoxy, 1-fluoromethyl-2-fluoroethoxy , 3-bromo-2-fluoropropoxy, 1-bromomethyl-2-bromoethoxy, and the like. "Heterocyclyl" refers to a stable ring radical of 3 to 15 members which consists of carbon atoms and 1 to 5 heteroatoms which are selected from the group consisting of nitrogen, oxygen and sulfur. For purposes of this invention, the heterocyclyl radical may be a bicyclic or tricyclic ring system, which may include fused or bridged ring system; and the nitrogen, carbon or sulfur atoms in the heterocyclyl radical optionally may be oxidized; the nitrogen atom optionally may be in quaternary form; and the heterocyclyl radical may be partially or completely saturated, or be aromatic. The heterocyclyl radical can be attached to the main structure at any heteroatom or carbon atom which results in the creation of a stable compound. Examples of heterocyclyl radicals include, but are not limited to, azepinyl, azetidinyl, acridinyl, benzimidazolyl, benzodioxolyl, benzodioxanyl, benzothiazolyl, benzoxazolyl, benzopyranyl, benzofuranyl, benzothienyl, carbazolyl, cinolinyl, decahydroisoquinolyl, dioxalanyl, furyl, isothiazolyl, quinuclidinyl, imidazolyl, imidazolinyl, imidazolidinyl, isothiazolidinyl, indolyl, isoindolyl, indolinyl, isoindolinyl, indolizinyl, isoxazolyl, isoxazolidinyl, morpholinyl, naphthyridinyl, oxadiazolyl, octahydroindolyl, octahydroisoindolyl, 2-oxopiperazinyl, 2-oxopiperadinyl, 2-oxopyrrolidinyl, 2-oxoazepinyl, oxazolyl, oxazolidinyl, perhydroazepinyl, piperidinyl, piperazinyl, 4-piperidonyl, phenazinyl, phenothiazinyl, phenoxyzinyl, phthalazinyl, pteridinyl, pyrrolyl, pyrrolidinyl, pyrazolyl, pyrazolidinyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, quinazolinyl, quinoxalinyl, quinolinyl, quinuclidinyl, isoquinolinyl, thiazolyl or, thiazolidinyl, tladiazolyl, thiazolyl, tetrazolyl, tetrahydrofuryl, tetrahydropyranyl, tetrahydroisoquinolyl, thienyl, thiomorpholinyl, thiomorpholinyl sulfoxide, and thiomorpholinyl sulfone. The heterocyclyl radical may optionally be substituted by R6 as defined above in the brief description of the invention, or may optionally be substituted by one or more substituents that are selected from the group consisting of hydroxy, mercapto, halo, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, phenylalkenyl, alkoxy, phenoxy, phenylalkoxy, haloalkyl, haloalkoxy, formyl, nitro , cyano, amidino, cycloalkyl, hydroxyalkyl, alkoxyalkyl, phenoxyalkyl, phenylalkoxyalkyl, amidino, ureido, alkoxycarbonylamino, amino, monoalkylamino, dialkylamino, monophenylamino, monophenylalkylamino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, monofeni laminoalkyl, monofeni lalkylaminoalkyl, alkylcarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminocarbonylalkyl, monoalkylaminocarbonyl, dialkylaminocarbonylalkyl and imidazolyl, as defined herein. "Linker residue" refers to any component capable of being selectively separated to release the residue of the compound of the invention from the solid substrate. See, for example, Greene and Wuts, Protective Groups in Organi c Syn thesis, 2nd ed., Willey (1991). The specific linker residues and the separation reagents thereof are described in Table 7 below. "Monoalkylamino" refers to a radical of the formula -N (H) Ra wherein Ra is an alkyl radical as defined above, for example methylamino, ethylamino, propylamino and the like. "Monoalkylaminocarbonyl" refers to a radical of the formula -C (0) N (H) Ra wherein Ra is an alkyl radical as defined above, for example methylaminocarbonyl, ethylaminocarbonyl, propylaminocarbonyl and the like.
"Monoalkylaminosulfonyl" refers to a radical of the formula -S (0) 2N (H) Ra wherein Ra is an alkyl radical as defined above, for example methylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl and the like. "N-heterocyclyl" refers to a heterocyclyl radical as defined above, which contains at least one nitrogen atom and which is attached to the main structure through the nitrogen atom. The N-heterocyclyl radical can contain up to 3 additional heteroatoms. Examples include piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, azetidinyl, indolyl, pyrrolyl, imidazolyl, tetrahydroisoquinolyl, perhydroazepinyl, tetrazolyl, thiazolyl, oxazinyl and the like, and may optionally be substituted as described above for heterocyclyl radicals. In addition to being optionally substituted by the substituents included above for a heterocyclyl radical, the N-heterocyclyl radical may also be optionally substituted by R8 as defined above in the brief description of the invention. "Phenylalkyl" refers to an alkyl radical as defined above substituted by a phenyl radical, for example benzyl and the like. "Optional" or "optionally" means that event described subsequently of circumstances may or may not occur, and that the description includes cases in which such an event or circumstance occurs and cases in which it does not. For example "optionally substituted aryl" means that the aryl radical may or may not be substituted and that the description includes both substituted aryl radicals as well as aryl radicals which have no substitution. The term "- [C2-C8 alkyl] -R10 (optionally substituted by hydroxy)" means that the alkyl has the optional substitution. The same is true for the term "- [C 1 -C 8 alkyl] -R 11 (optionally substituted by hydroxy)". The term "-S (0) tR22 optionally substituted" means that all substituents R22 have the optional substitution. "Phenylalkenyl" refers to an alkenyl radical as defined above substituted by a phenyl radical. The term "pharmaceutically acceptable salt" refers to salts prepared from pharmaceutically acceptable non-toxic acids or bases including inorganic acids and bases and organic acids and bases. When the compounds of the present invention are basic, the salts can be prepared from pharmaceutically acceptable non-toxic acids including inorganic and organic acids. The pharmaceutically acceptable acid addition salts suitable for the compounds of the present invention include acetic acid, benzenesulfonic (besylate), benzoic, camphorsulfonic, citric, otonsulfonic, fumaric, gluconic, glutamic, hydrobromide, hydrochloride, isethonic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, parmoic, pantothenic, phosphoric, succinic, sulfuric, tartaric, p-toluenesulfonic and the like. When the compounds contain an acidic side chain, the pharmaceutically acceptable base addition salts suitable for the compounds of the present invention include metal salts consisting of aluminum, calcium, lithium, magnesium, potassium, sodium and zinc, or organic salts made from Lysine, N, N'-dibenzylethylenediamine, chloroprocaine, choline, diethanolamine, ethylenediamine, meglumine (N-methylglucamine) and procaine. "Solid substrate" refers to a material on which the synthesis of the compounds of the invention is going to be performed, and is also referred to herein as spheres or resins. The term "solid substrate" is intended to include spheres, granules, discs, fibers, gels or particles such as cellulose spheres, porous glass spheres, silica gel, polystyrene spheres optionally crosslinked with divinylbenzene and optionally grafted with polyethylene glycol and optionally functionalized with amino, hydroxy, carboxy or halo groups, copolyzed spheres, polyacrylamide spheres, latex spheres, dimethylacrylamide spheres optionally crosslinked with N, N'-bis-acryloylethylenediamine, glass particles coated with hydrophobic polymer, etc., i.e. , material that has a rigid or semi-rigid surface; and soluble substrates such as low molecular weight, non-crosslinked polystyrene. "Therapeutically effective amount" refers to that amount of a compound of the invention which, when administered to a human in need thereof, is sufficient to carry out the treatment, as defined below, for conditions resulting from an abnormality in the production of nitric oxide. The amount of a compound of the invention which constitutes a "therapeutically effective amount" will vary depending on the compound, the condition and its severity, and the age of the human concerned, but can usually be determined by a person familiar with the art. Take into consideration your own knowledge and this description. "Treat" or "treatment", as used herein, covers the treatment of a condition in a human, a condition which results from an abnormality in the production of nitric oxide, and includes: (i) preventing the occurrence of condition in a human, in particular when such a human is predisposed to the condition but has not yet been diagnosed as a patient who presents it: (ii) inhibition of the condition, ie, suppression of its development; or (iii) release of the condition, that is, regression of the condition. The yield of each of the reactions described herein is expressed as a percentage of the theoretical yield. Most of the compounds described herein contain one or more asymmetric centers and therefore give rise to enantiomers, diastereomers and other stereoisomeric forms which can be defined, in terms of absolute stereochemistry as (R) - or (S) - or, as (D) - or (L) -for amino acids. The present invention is intended to include all of all possible isomers, as well as their racemic and optically pure forms. The optically active isomers
(R) - and (S) - or, (D) - and (L) - can be prepared using chiral synthons or chiral reagents, or they can be separated using conventional techniques. When the compounds described herein contain olefinic double bonds or other centers of geometric asymmetry, unless otherwise specified, it is understood that the compounds include the geometric isomers E and Z. Likewise, all tautomeric forms are also they pretend they are included. The nomenclature used in this is a modification of the naming system of the I.U.P.A.C. wherein the compounds of the invention are referred to herein as amide derivatives. For example, the following compound of the invention:
it is referred to herein as 2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [(4-methoxyphenyl) methyl] -pentanediamine. Unless otherwise indicated, it is intended that the names of the compounds include any simple stereoisomer, enantiomer, racemate or mixtures thereof.
UTILITY OF THE COMPOUNDS OF THE INVENTION:
Nitric oxide generated by the inducible form of nitric oxide synthase (i-NOS) has been implicated in the pathogenesis of many inflammatory and autoimmune diseases and also diseases which are generally not considered to be inflammatory but which nevertheless may involve cytokines which they locally regulate the i-NOS.
The compounds of the invention, alone or in combination with other pharmaceutical agents, are therefore useful for treating mammals, preferably humans, having a condition resulting from an abnormality in the production of nitric oxide.
Such conditions include, but are not limited to the following: Multiple sclerosis (Parkinson, J.F. et al., Mol. Med.
(1997), vol. 75, pp. 174-186); attack or cerebral ischemia (Iadecola, C. et al., J. Neurosci. (1997), vol.17, pp. 9157-9164); Aizheimer's disease (Smith M.A., et al., J. Neurosci.
(1997), vol. 17, pp. 2653-2657; Wallace, M.N. et al. Exp.
Neurol. (1997), vol. 144, pp. 266-272); dementia for HIV
(Adamson D.C., et al., Science (1996), vol 274, pp. 1917-1921); Parkinson's disease (Hunot, S. et al., Neuroscience (1996), vol 72, pp. 355-363); meningitis (Koedel, U. et al., Ann.
Neurol. (1995), vol. 37, pp. 313-323); Dilated cardiomyopathy and congestive heart failure (Satoh M. et al., Am. Coil, Cardiol.
(1997), vol. 29, pp. 716-724); atherosclerosis (Wilcox J.N. et al., Arterioscler, Thromb, Vesc. biol. (1997), vol, 17, pp. 2479- 2488); restenosis or graft stenosis, septic shock and hypotension (Petros, A. et al., Cardiovasc Res (1994), vol 28, pp. 34-39); Hemorrhagic shock (Thiemermann, C. et al., Proc.
Na ti. Acad. Sci. (1993), vol. 90, pp. 267-271); asthma (Barnes, P.J. et al., Ann. Med. (1995), vol.27, pp. 389-393; Flak, T.A.
et al. Am. J. Respir. Crit. Care Med. (1995), vol. 154, pp. 5202-5206); respiratory distress syndrome in adults, smoking habit or particle-mediated lung damage (Ischiropoulos, H. et al., Am. J. Respir. Crit. Care Med. (1994), vol 150, pp. 337-341; Dyke, K., Agents Actions (1994), vol 41, pp. 44-49); pneumonias mediated by pathogens (Adler, H. et al., J. Exp. Med. (1997), vol 185, pp. 1533-1540); traumas of various etiologies (Thomas, K.R. et al., Surgery (1996), vol 119, pp. 61-66); rheumatoid arthritis and osteoarthritis (Grabowski P.S. et al., Br. J. Rheumatol. (1997), vol 36, pp. 651-655); glomerulonephritis (Weinberg, J.B. et al., Exp. Med. (1994), vol 179, pp. 651-660); systemic lupus erythematosus (Belmont, H.M. et al., Arthritis Rheum. (1997), vol 40, pp. 1810-1816); inflammatory bowel diseases such as ulcerative colitis and Crohn's disease (Godkin, JA et al., J. Clin. Invest. (1996), vol.26, pp. 867-872; Singer, II et al., Gastroesterology (1996 ), vol 111, pp. 871-885); insulin-independent diabetes mellitus (McDaniel, M.L. et al., Proc. Soc. Exp. Biol. Med. (1996), vol.211, pp. 24-32); Diabetic neuropathy or nephropathy (Sugimoto, K. and Yagihashi, S. Microvasc. Res. (1997), vol 53, pp. 105-112; Amore A. et al., Kidney Int. (1997), vol 51, pp. 27-35); acute and chronic organ transplant rejection (Worral, N.K. et al., Transplatation (1997), vol 63, pp. 1095-1101); Transplant vasculopathies (Russel, M.E, et al. (1995), vol.92, pp. 457-464); graft versus host disease (Klohian, K. et al J. Immunol. (1996), vol 157, pp. 2851-2856); psoriasis and other inflammatory skin diseases (Bruch-Gerharz, D. et al., J. Exp. Med. (1996), vol 184, pp. 2007-2012); and cancer (Thomsen, L.L., et al.Cancer fies. (1997), vol.57, pp. 3300-3304). The compounds of the present invention may also be useful for the management of male and female reproductive functions when used alone or in combination with other medications commonly used for these indications. Examples, without limitation involved, include: fertilization inhibition, endometrial receptivity and implantation (alone or in combination with a progesterone antagonist); post-coital contraception (alone or in combination with a progesterone antagonist); induction of abortion (in combination with an antiprogestin and in additional combination with a prostaglandin); control and management of labor and delivery; treatment of servical incompetence (alone or in combination with progesterone or a progestin); endometriosis treatment (alone or in combination with other drugs, including LHRH agonist / antagonist, antiprogestin, orprogestins either by sequential application or by simultaneous administration). See, for example, the following references: Chwalisz, K. et a l. J. Soc. Gynecol. Invest. (1997), vol. 4, No. 1 (supplement), page 104a, which discusses the inhibition of fertilization, endometrial receptivity and implantation, or post-coital contraception, alone or in combination with a progesterone antagonist; Chwalisz, K. et al. Prens t. Neona t. Med. (1996), vol. 1, pp. 292-329, which discusses the induction of abortion, in combination with an antiprogestin and in additional combination with a prostaglandin, and the control and management of labor and delivery; and Chwalisz K. et ai. Hum. Reprod. (1997), vol. 12. pp. 101-109, which discusses the treatment of servical incompetence, alone or in combination with progesterone or a progestin. Those familiar with the art will also recognize that the compounds of the present invention include 1-substituted imidazoles. This class of compounds has previously been described as heme-binding inhibitors based on the mechanism of the cytochrome P450 family of enzymes (Maurice, M. et al, FASEB J. (1992), VOL 6, PP 752-8). of nitric oxide synthesis (Chabin, R.NM. et al., Biochemistry (1996), vol.35, pp. 9567-9575). The compounds of the present invention can therefore be useful as inhibitors of selected cytochrome P450 family members of therapeutic interest including, but not limited to, P450 enzymes involved in the biosynthesis of steroids and retinoids
(Masamura et al., Beast Cancer Res. Trea t. (1995), vol 33. pp.
19-26); S art, P. et a l. J. Clin. Endocrinol Metab, vol. 77. pp. 98-102; Docks, P. et al. Br. J. Derma tol. (1995), vol. 133, pp. 426-32) and cholesterol biosynthesis (Burton, P.M. et al.
Biochem. Pharmacol. (1995), vol. 50, pp. 529-544; and S inney, D.C. et al. Biochemistry (1994), vol. 33, pp. 4702-4713). The imidazole-based compounds may also have antifungal activity (Abyama, Y. et al I. Biochem., Pharmacol. (1992), vol 44, pp. 1701-1705). The P450 inhibitory activity of the compounds of the present invention can be determined using appropriate assay systems specific for the P450 isoform of interest. Such assays are included in the references mentioned above. A further example of a mammalian cytochrome P450 isoform that can be inhibited by the compounds of the present invention is cytochrome P450 3A4 which can be tested in a manner similar to the method described in Yamazaki et al. Carcinogenesis (1995), vol. 16, pp. 2167-2170.
PROOF OF THE COMPOUNDS OF THE INVENTION
Nitric oxide synthases are complex enzymes that catalyze the conversion of N-arginine (NO) and citrulline. The catalysis is carried out through two successive oxidations of the guanidinium group of L-arginine. For the evaluation of the compounds of the invention, a cell-based nitric oxide synthase assay was used, which uses the measurement of the oxidation product of nitric oxide, nitrite, in the conditioned medium of cultured cells. The monocytic mouse cell lines RAW 264.7 and J774 are well documented as being able to produce > 10 μM nitrite in response to immunostimulation:
INDUCTION OF INOS IN MOUSE MONOCITE RAW 264.7
RAW 264.7 mouse macrophage cells are obtained from American Type Culture Collection (Rockville, Maryland) and maintained in RPMI 1640 containing 10% fetal bovine serum (FBS), 5,000 units / ml penicillin and streptomycin, and 2 mM glutamine. (maintenance medium). The NOS activity is measured by a fluorescence assay of the nitric oxide oxidation product, nitrite (Diamani et al I. Talan ta (1986), vol 33, pp. 649-652). The induction of iNOS (inducible nitric oxide synthase) is stimulated by treatment of the cell with lipopolysaccharide and interferon? The test method is described below. The cells are harvested, diluted to 500,000 cells / ml with maintenance medium and seeded in 96-well plates at 100 μl / well. The plates are incubated overnight at 37 ° C, under an atmosphere of C02 5%. Then the medium is replaced with 90 μl of BME medium containing 10% FBS, 100 units / ml of penicillin, 100 μl of streptomycin, 2 mM glutamine, 100 units / ml of interferon? and 2 μg / ml of lipopolysaccharide. N-guanidino-methyl-L-arginine (negative control) is added to 4 wells at a final concentration of 200 μM using 10 μl of 2 mM concentrated solution in 100 mM Hepes, pH 7.3 + 0.1% DMSO and 4 wells received only Hepes 100 mM / 0.1% DMSO buffer (positive control). The compounds for evaluation are dissolved 10 times at the desired final concentration in Hepes / DMSO and 10 μl of these solutions are transferred to a 96-well plate. The plates are incubated for 17 h at 37 ° C under an atmosphere of C02 5%. The nitrite accumulated in the culture medium is determined as follows: 15 μl of 2,3-diaminonaphthalene (10 μg / ml in 0.75 M HCl) is added to each well, and incubated for 10 minutes at room temperature. 15 μl of IN NaOH are added and the fluorescence emission is measured at 405 nm, using an excitation wavelength of 365 nm. Enzymatic activity in experimental wells is normalized to the control percent using the positive and negative control values. The ratio of signal to noise is > 10 for the trial. The compounds of the invention, when tested in this assay, demonstrate the ability to inhibit the production of nitric oxide. Various in vivo assays can be used to determine the efficacy of the compounds of the invention to treat a condition resulting from an abnormality in the production of nitric oxide, such as arthritis. The following is a description of such an assay using rats:
EFFECTS OF THE COMPOUNDS OF THE INVENTION ON INDUCED ARTHRITIS BY ADJUVANT IN RATS
Male Lewis rats were injected intradermally (proximal of the tail) with 0.1 ml of Mycobacterium um bu tyri cum in incomplete Freund's adjuvant (10 mg / ml). It is administered subcutaneously (bid) either vehicle (acidified saline solution, 1 ml / kg) or a compound of the invention (3, 10 or 30 mg / kg), starting on the day after adjuvant immunization, and continuing until the end of the experiment (N = 10 rats per treatment group). Clinical classifications (see below) are measured in all extremities, three times a week, during the study. Rats were sacrificed 34-35 days after immunization. At the time of euthanasia, a biological evaluation (see below) of the hind limbs was performed, a blood sample was collected for clinical blood chemistry and drug levels (only the high dose group, 6 to 12 hours after the final dose), a liver section was obtained to measure potential toxicity and the hind limbs were preserved for histopathological determination. Clinical classification - each member was classified according to the following scale: 0 without signs of inflammation 1 moderate redness, first indication of swelling, flexible joint 2 moderate redness, moderate swelling, flexible joint 3 redness, significant swelling and distortion of the leg, the joint begins to fuse 4 redness, thick swelling and distortion of the leg, the joint is completely fused.
Radiological classification - each hind limb is classified on a scale of 0-3 for each of the following parameters: swelling of soft tissue loss of cartilage erosion classification heterotropic
The compounds of the invention, when tested in this assay, demonstrate the ability to treat arthritis present in rats. Those familiar with the art will also recognize that there are numerous assays for the activity of the NOS isoforms (iNOS, nNOS and eNOS) which can be used to evaluate the biological activity of the compounds of the present invention. These incubate assays for native NOS isoforms in tissues studied ex vivo (Mitchell et al., Br. J. Pharmacol. (1991), vol 104. pp. 289-291; Szabo et al., Br. J. Pharmacol., 1993. ), vol.108, pp. 786-792; Joly et al., Br. J. Pharmacol. (1995), vol 115, pp. 491-497) as well as primary cell cultures in cell lines (Forstermann et al. Eur. J. Pharmacol. (1992), vol.225, pp. 161-165; Radmoski et al., Cardiovasc. Res. (1993), vol.27, pp. 1380-1382; Wang et al., J. Pharmacol Exp. Ther. (1994), vol.268, pp. 552-557). Those familiar with the art will also recognize that recombinant NOS enzymes can be expressed in heterologous cells either by transient transfection (Karisen et al., Diabetes (1995), vol.44, p.753-758), stable transfection (McMillan et al. Proc. Nati, Acad. Sci. (1992), vol.89, pp. 11141-11145, Sessa et al., J. Biol. Chem. (1995), vol.270, pp. 17641-17644) or by means of lytic virus transaction use (Buscón &Michel, Mol.Pharmacol. (1995), vol.47, pp. 655-659; List et al., Biochem. J. (1996), vol.315, p. 57-63) using cDNA for NOS. Heterologous expression can be obtained in mammalian cells ((McMillan et al., Proc. Nati, Acad. Sci.
(1992), vol. 89, pp. 11141-11145), insect cells (Buscon &
Michel, Mol. Pharmacol. (1995), vol. 47, pp. 655-659; List et al. Biochem. J. (1996), vol. 315, pp. 57-63), yeast (Sari et al., Biochemistry (1996), vol 35. pp. 7204-7213) or bacteria (Román et al., Proc. Na ti. Acad. Sci. (1995), vol. , pp. 8428-8432; Martasek et al., Biochem. Biophys., Res. Commun. (1996), vol. 219, pp. 359-365). Any of these heterologous expression systems can be used to establish assay systems for iNOS, nNOS and eNOS, to evaluate the biological activity of the compounds of the present invention.
ADMINISTRATION OF THE COMPOUNDS OF THE INVENTION
Any suitable route of administration can be used to provide a patient with an effective dosage of compounds of the invention. For example, oral, rectal, parenteral (subcutaneous, intramuscular, intravenous), transdermal, and similar administration forms can be used. Dosage forms include tablets, troches, dispersions, suspensions, solutions, capsules, patches and the like. The pharmaceutical compositions of the present invention comprise the compounds of the invention as the active ingredient, and may also contain a pharmaceutically acceptable carrier, and optionally other therapeutic ingredients. Carriers such as starches, sugars and microcrystalline cellulose, diluents, granulating agents, lubricants, binders, disintegrating agents and the like are suitable in the case of oral solid preparations (such as powders, capsules and tablets), and oral solid preparations are preferred. about oral liquid preparations. Methods for their preparation are well known in the art. Because of their ease of administration, tablets and capsules represent the most advantageous oral dosage unit forms, in which case solid pharmaceutical carriers are used. If desired, the tablets can be coated by standard aqueous or non-aqueous techniques. In addition to the common dosage forms set forth in the foregoing, the compounds of the present invention may also be administered by a controlled or sustained release means and by delivery device. The pharmaceutical compositions of the present invention suitable for oral administration can be presented as discrete units such as capsules, sachets or tablets, each with a predetermined amount of the active ingredient, as a powder or granules, or as a solution or suspension in a liquid aqueous, a non-aqueous liquid, an oil-in-water emulsion or a water-in-oil liquid emulsion. Such compositions may be prepared by any of the pharmacy methods, but all methods include the step of bringing into association the active ingredient with the carrier which constitutes one or more of the necessary ingredients. In general, the compositions are prepared by uniform and intimate mixing of the active ingredient with liquid carriers or finely divided solid carriers or both and then, if necessary, with formation of the product at the desired presentation.
PREFERRED MODALITIES
In the various aspects of the invention, certain embodiments are preferred. A preferred group of compounds of formula (I), formula (II), and formula (III), are those compounds of formula (I) having the formula (Ia), formula (Ib), or formula of):
A preferred subgroup of this group of compounds are those compounds wherein A is -OR1, -C (O) N (R1) R2, -N R ^ UOJNÍR R16, -NR ^ OJR2 or -N (R2) R24; V is N (R4); and W is CH.
A preferred class of compounds of this subgroup are those compounds wherein A is -C (0) N (R1) R2; q, r and n are zero; R1 is hydrogen; R2 is lower alkyl or - [X-CgJ-R9; R 4 is hydrogen or lower alkyl; and R5 is hydrogen, halo, alkyl or alkoxy. A preferred subclass of compounds of this class of compounds are those compounds wherein R9 is phenyl, tolyl, anisyl, 1,4-benzodioxan-6-yl, 1,3-benzodioxol-5-yl, chlorophenyl, carboxyphenyl, dimethoxyphenyl, 2-thienyl or morpholinyl. Another preferred subgroup of compounds of this group of compounds are those compounds wherein A is -C (0) N (R1) R2; m is zero; Q is a direct link for R3; and R3 is hydrogen. A preferred compound of this subgroup is N - [(1, 3-benzodioxol-5-yl) ethyl] -2- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] acetamide. Another preferred group of compounds of formula (I), formula (II) and formula (III) are the compounds of formula (II), having the formula (lia), formula (Ilb), and formula (lie):
A preferred subgroup of compounds of this group of compounds are those compounds wherein N-heterocyclyl are selected from the group consisting of piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, acetidinyl, indolyl, pyrrolyl, imidazolyl, tetraisoquinolyl and perhydroazepinyl. A preferred class of compounds of this subgroup of compounds are those compounds wherein N-heterocyclyl is piperazinyl substituted by R8, ie, the compounds of formula (lid), formula (He), or formula (Hf):
He); or
A preferred subclass of compounds of this class of compounds are those compounds wherein A is -OR1, -UOWR ^ R2, -NÍR ^ JCÍOÍNÍR ^ R16, -NRXíOR2 O -NfR ^ R24; W is CH; and R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of X-Cg -R8, - [C2-C8 alkyl] -R10, - [Ci-Cg alkyl] -Ru, acyl ,, -C (0) R8, -C (O) - [C_-C8 alkyl] -R8, alkoxycarbonyl, optionally substituted alkoxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted aryisulfonyl , aminocarbonyl, monoalkylcarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (O) -R23-N (R1 ) R2, -C (0) -R23-N (R1) C (0) -R23-N (R1) R2 and -C (O) -N (R1) -R23-C (O) OR1. Of this subclass of compounds, the preferred compounds are those compounds wherein A is -C (O) N (R1) R2; R1 is hydrogen; R2 is lower alkyl, - [alkyl of X-C-R9, or - [C_-C8] -R10; R5 is hydrogen, acetyl, t-butoxycarbonyl, 4-methoxyphenylaminocarbonyl, 4-methoxyphenylmethyl, methoxycarbonyl, methyl or benzyl; R5 is hydrogen, halo, alkyl or alkoxy; and n is zero or 1. Of this group of preferred compounds, the most preferred compounds are those compounds wherein R2 is -CH2-R9 or - [C_-C8] -R10; R9 is aryl or substituted aryl; and R10 is methylthio. Of this group of more preferred compounds, the most preferred compounds are those compounds wherein R2 is -CH2-R9; R6 is hydrogen, acetyl or t-butoxycarbonyl; and R9 is phenyl, tolyl, anisyl, 1,4-benzodioxan-6-yl, 1,3-benzodioxol-5-yl, methylthiophenyl, chlorophenyl, carboxyphenyl, dimethoxyphenyl or 2-thienyl. Of this group of more preferred compounds, the preferred compounds are those compounds wherein R5 is chloro, R8 is acetyl and R9 is p-tolyl, or those compounds wherein R5 is chloro, R6 is hydrogen and R9 is p-tolyl , or those compounds in which R5 is chloro, R6 is hydrogen and R9 is 1,4-benzodioxan-6-yl or 1,3-benzodioxol-5-yl, or those compounds in which R5 is chloro, R6 is t -butoxycarbonyl and R9 is 1,4-benzodioxan-6-yl or 1,3-benzodioxol-5-yl. Preferred compounds of this subset of compounds can be selected from the following list: N- [(1,3-benzodioxol-5-yl) ethyl] -4- [2- (lH-imidazol-1-yl) -6- methylpyrimidin-4-yl] -1- (2-methyl-l-oxopropyl) piperazin-2-acetamide; N- [(1, 3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -4- (methoxycarbonyl) piperazine-2- acetamide; N - [(1,4-benzodioxan-6-yl) methyl] -1- [2- (lH-triazol-1-yl) pyrimidin-4-yl] - A - (dimethylethoxy) piperazine-2-acetamide; N- [(1,3-benzodioxol-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methoxypyrimidin-4-yl] -1- (methoxycarbonyl) piperazin-2 acetamide; 1- (acetyl) -N- [(1,3-benzodioxol-5-yl) methyl] -4- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (methylsul fonyl) piperazin-2 acetamide; and l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(pyridin-3-yl) methyl] -4- (tetrahydro-3-furanoyl) piperazine-2-carboxamide. Another preferred class of compounds of this subgroup of compounds are those compounds wherein N-heterocyclyl is piperidinyl, ie, the compounds of formula (Hg), formula (Hh), or formula (Ili):
A preferred subclass of compounds of this class of compounds are those compounds wherein A is -OR1,
-UOJNtR ^ R2, -N (R16) C (0) N (R1) R16, -NRXfOR2 or -N (RX) R21; and W is CH; Preferred compounds of this subclass of compounds are those compounds wherein A is -C (0) N (R1) R2;
R1 is hydrogen; R2 is lower alkyl or - [alkyl of X-Cgj-R9;
R5 is hydrogen, halo, alkyl or alkoxy; and n is zero or 1. The most preferred compounds of these preferred compounds are those compounds wherein R2 is lower alkyl or -CH2-R9 and R9 is 4-methoxyphenyl, 1, -benzodioxan-6-yl, 1,3-benxodiozole -5-yl or 3,4-dimethoxyphenyl. Preferred compounds of this subgroup of compounds can be selected from the following list: N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4 -yl] piperidin-2-ethane ina; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (morpholin-4-yl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- (methylhexyl) piperidin-2-acetamide; N- [(4-chlorophenyl) methyl] -1- [2,6-bis (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperidin-2-acetamide; and N- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methoxypyrimidin-4-yl] piperidin-2-acetamide. Another preferred class of compounds of this subgroup of compounds are those compounds wherein N-heterocyclyl is pyrrolidinyl, ie, the compound of formula (IIj), formula (Hk), or formula (Hm):
A preferred subclass of compounds of this class of compounds are those compounds wherein A is -OR1,
-C. { 0) li. { R1) R2, -NÍR ^ CÍOJNÍR R16, -NRX (O) R2 O -N (R1) R21; and W is CH; Preferred compounds of this subclass of compounds are those compounds wherein A is -C (O) N (R1) R2; R1 is hydrogen; R2 is lower alkyl or - [alkyl of X-Cgj-R9; R5 is hydrogen, halo, alkyl or alkoxy; and n is zero or 1. The most preferred compounds of these preferred compounds are those compounds having the R-C configuration of the pyrrolidinyl ring. Preferred compounds of this subset of compounds can be selected from the following list: N- [(1,3-benzodioxol-5-yl) ethyl] -4- [2- (lH-imidazol-1-yl) -6- methylpyrimidin-4-yl] -pyrrolidine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] -pyrrolidine-2-carboxamide;
N - [(3,4-dimethoxy phenyl) methyl] -1- [2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -pyrrolidin-2-acetamide; N - [(4-methoxy phenyl) ethyl] -1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -pyrrolidine-2-carboxamide; and N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] -pyrrolidin-2-acetamide. Additional preferred compounds from the group of compounds as defined above may be selected from the following list: 4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3 -benzodioxol-5-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] thiomorpholin-2-acetamide; N- [(1,3-dioxolan-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -perhydroazepin-2-acetamide; N- [(3, -dimethoxyphenyl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -acetidine-2-carboxamide; and 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] morpholine-2-carboxamide. Another preferred group of compounds of formula (I), formula (II), and formula (III) are those compounds of formula (III) having the formula (Illa), formula (IHb), or formula (IIIc): A subgroup Preferred compounds of this group of compounds are those compounds in which
is optionally substituted phenyl or optionally substituted naphthyl. Another preferred group of compounds of formula (I), formula (II), or formula (III) are those compounds in which each of X, Y or Z is C (R19) and each U is C (R6). Another preferred group of compounds of formula (I), formula (II), or formula (III) are those compounds in which each of X, Y or Z is N and each each U is C (R5). Another preferred group of compounds of formula (I), formula (II), or formula (III) are those compounds wherein each of X, Y or Z is C (R19) and each U is N. Another preferred group of compounds of formula (I), formula (II), or formula (III) are those compounds in which, in each formula, one of X, Y and Z is N and the others are C (R19) and U is C ( R5).A preferred group of compounds of formula (IV) are those compounds of formula (IVa), formula (IVb), or formula (IVc):
A preferred subgroup of compounds of this group of compounds are those compounds in which the amino acid is an α-amino acid of the L configuration on the carbon with respect to the acid. Another preferred subgroup of compounds of this group of compounds are those compounds in which the amino acid is an α-amino acid of the D configuration on the carbon with respect to the acid. Another preferred subgroup of compounds of this group of compounds are those compounds wherein R 1 is hydrogen; R2 is lower alkyl or - [alkyl of X-Cg-R9; and R5 is hydrogen, halo, alkyl or alkoxy. A preferred class of compounds of this subgroup of compounds are those compounds wherein R9 is phenyl, tolyl, anisyl, 1,4-benzodiozan-6-yl, 1,3-benzodioxol-5-yl, chlorophenyl, carboxyphenyl, 2- thienyl, dimethoxyphenyl or morpholinyl. A preferred group of compounds of formula (Va), formula (Vb), or formula (Ve) are those compounds wherein each X and each Y is N; each W is CH; and V is an optionally substituted fumed heterocyclyl. A preferred subgroup of compounds of this group of compounds are those compounds having the formula (Vba):
wherein A is -OR1, -C (O) N (R1) R2, -N (R16) C (O) N (R1) R16,
NR! C (0) R2 or -NfR ^ R21; Y
is N-heterocyclyl which is selected from the group consisting of piperidinyl, piperazinyl, pyrrolidinyl or morpholinyl. A preferred compound of this subgroup of compounds is N- [(1,3-benzodioxol-5-yl) methyl] -1 [2- (lH-imidazol-1-yl) purin-6-yl] piperidin-2-acetamide . Of the compounds of formula (Vlla), formula (Vllb), or formula (VIIc), a preferred compound is N- [(1,3-benzodioxol-5-yl) methyl] -l [6-chloro-2- ( pyridin-3-yl) pyrimidin-4-yl] piperidin-2-acetamide. Of the compounds of formula (VIII), preferred are 4,6-dichloro-2- (lH-imidazol-1-yl) pyrimidine and 2,4-dichloro-6- (1-lH-imidazol-1-yl) pyrimidine. Of the binder residues used in this invention, the photolitically separable bond of formula (X) is most preferred:
where the valency not satisfied to the right of the formula represents the point of attachment to the solid substrate, and the valence not satisfied to the left of the formula represents the point of binding to the ligand.
PREPARATION OF THE COMPOUNDS OF THE INVENTION
The compounds of the invention can be synthesized by two general approaches, one of which (solid phase) can be considered as a variant of the other (phase in solution). The generic synthesis of phase in solution is shown in the following reaction scheme 1 which, solely for purposes of illustration, illustrates the synthesis of a compound of formula (I) wherein A is -C (0) N (R1) R2 . It is understood that other compounds of the invention can be prepared in a similar manner. In the following reaction scheme 1, PG is a suitable protecting group; m, n, q, r, Q, U, W, X, Y and Z are as described in the above in the summary of the invention; V is N (R4), S or 0 (wherein R4 is as described in the brief description of the invention); and R1. R2, R3, R12, R13, R14, R15, R17 and R20 are as described above, in the brief description of the invention:
Reaction scheme 1
(XlVaa)
Vbb)
(XIVcc)
In general, the compounds of formula (I) are prepared by first adding one equivalent of a compound of formula
(XI) in one portion, to a solution of one equivalent of a compound of formula (XII) having at least two substituents displaceable by a nucleophile and 1.1 equivalents of trialkylamine base (such as triethylamine) in a non-protic polar solvent such as THF or methylene chloride, to provide the compound of formula (XIII). Upon completion of the reaction, the mixture is purified by conventional methods. The compounds of formula (XIVcc) are synthesized by methods well known in the art of amino acid and peptide synthesis from the appropriate compound of formula (XlVaa) wherein PG is a standard protecting group for the V substituent. The compounds of formula ( XlVaa) are commercially available, usually in protected form, or are easily synthesized by methods well known in the art. Preferred protecting groups are Boc (t-butoxycarbonyl) and Fmoc (fluorenylmethoxycarbonyl), although others, such as CBZ (benzyloxycarbonyl) and Troc (trichloroethoxycarbonyl) can be used for particular circumstances. The side chain functionalities can be protected, as is well known in the peptide art, by Trt (triphenylmethyl), tBu (t-butyl), Acm (acetamidomethyl), etc. The protected compounds of formula (XlVaa) are reacted with the appropriate amine to produce compounds of formula (XlVbb) and deprotected to produce the compound of formula (XIVcc), again by methods well known in the art of peptides.
An equivalent of the compound of formula (XIVcc) is added to a solution of one equivalent of the compound of formula
(XIII) and a base equivalent in an aprotic, polar solvent, such as THF. The reaction is heated to a temperature at which the reaction is carried out cleanly until completion in less than 16 hours. At the end of the reaction, the compound of formula (I) is purified and characterized by conventional methods. The compounds of formula (I) have what is called "reverse amide", that is, wherein A is -N (R1) C (0) R2 and can be manufactured from the appropriate acid of formula
(XlVaa) by Hofmann rearrangement of the acid to an amine, followed by acylation with an appropriate acid under the conditions described above. In many cases, the desired diamine can be obtained commercially. The compounds of formula (I) in which A is a urea can be prepared by reacting a compound of formula (I) wherein A is -NfR ^ R21 (wherein R1 is hydrogen and R21 is hydrogen, alkyl, aryl or aralkyl) with an isocyanate. Similarly, compounds of formula (I) in which A is a carbamate can be prepared by reacting a compound of formula (I) (wherein A is -N (RX) R21 wherein R1 is hydrogen and R21 is hydrogen, alkyl, aryl or aralkyl) with an alkyl chloroformate or by curtius rearrangement of the carboxylic acid azide of the compound of formula (XlVaa) in the presence of the appropriate alcohol. In the reaction scheme 2, a specific embodiment of the generic synthesis of a compound of the invention is shown below, as applied to 6-chloro-2- (1-imidazolyl) -4-pyrimidinamine which incorporates the D-β residue -thienilalanine piperonilamide:
Reaction scheme 2
(Villa)
One equivalent of isobutyl cloformate is added to a solution of N-Boc-D-β-thienylalanine and one equivalent of a phase such as N-methylmorpholine in THF. After two minutes, one equivalent of piperonylamine is added and the mixture is allowed to warm to room temperature. After thirty minutes, the reaction mixture is passed through a Celite bed and all volatile factions are removed under reduced pressure to provide N-Boc-D-β-thienylalanine piperonyl amide. The N-Boc-D-β-thienylalanine piperonyl amide is treated with methanol with acetyl chloride. After 45 minutes, all volatile fractions are removed under reduced pressure to provide D-β-thienylalanine piperonyl amide hydrochloride. One equivalent of imidazole is added in one portion, to a solution of one equivalent of trichloropyrimidine and 1.5 equivalents of triethylamine in THF. After the reaction is complete, the reaction mixture is poured into saturated aqueous ammonium chloride and extracted three times with ethyl acetate. The combined organic layers are washed with brine and dried. The reaction mixture is filtered and all volatile fractions are removed under reduced pressure. The product 2-imidazolyl-4,6-dichloropyrimidine (the compounds of the formula (Villa)) are isolated by flash chromatography (20% ethyl acetate in hexane) as an off-white solid. Two equivalents of D-β-thienylalanine piperonyl amide hydrochloride are added to a solution of one equivalent of 2-imidazolyl-4,6-dichloropyrimidine (the compound of formula (Villa)) and three equivalents of Hünig's base (diisopropylethylamine) in THF . After the reaction is complete, all volatiles are removed and the product is isolated (the compound of formula (Iaa)).
A specific example of the synthesis is given as applied to sarcosine piperonyl amide hydrochloride: Isobutyl chloroformate (226 μL, 1.73 mmol) is added to a solution of N-Boc sarcosine (1.73 mmol) and N-methylmorpholine (192 μL, 1.73 mmoles) in THF. After two minutes, piperonylamine (216 ml, 1.73 mmol) is added and the mixture is allowed to warm to room temperature. After thirty minutes, the reaction mixture is passed through a pad of Celite and all volatiles are removed under reduced pressure to provide N-Boc sarcosine piperonyl amide (531 mg, 95%) as a white solid. XH NMR: (CDC13) d 2.41 (s, 3H), 3.28 (s, 2H), 4.39 (d, 2H), 5.95 (s, 2H), 6.80 (m, 3H), 7.43 (s broad, 1H), 9.04 (broad s, 1H). N-Boc sarcosine piperonilamide (500 mg, 1.54 mmol) in methanol (10 ml) is treated with acetyl chloride (1 ml).
After 45 minutes, all volatiles are removed under reduced pressure to provide the sarcosine piperonyl amide hydrochloride (395 mg, quantitative) as a sticky solid. Imidazole (9.5 g, 140 mmol) is added in one portion to a solution of trichloropyrimidine (24.7 g, 135 mmol) and triethylamine (30 mL, 216 mmol) in THF (500 mL). After
16 h, the reaction mixture is poured into saturated aqueous ammonium chloride and extracted three times with ethyl acetate. The combined organic layers are washed with brine and dried over MgSO .. The reaction mixture is filtered and all volatile fractions are removed under reduced pressure. 2-Imidazolyl-4,6-dichloropyrimidine (the compound of the formula (Villa)) (9.61 g, 33%) is isolated by flash chromatography (20% ethyl acetate in hexane) as an off-white solid. X H NMR: (CDC13) d 7.13 (s, 1 H), 7.25 (s, 1 H), 7.76 (s, 1 H), 8.50 (s, 1 H). Sarcosine piperonyl amide hydrochloride (50 mg, 0.19 mmol) is added to a solution of 2-imidazolyl-4,6-dichloropyrimidine (Villa) (20 mg, 0.093 mmol) and Hünig's base (50 μl, 0.29 mmol) in THF ( 1 ml). After 16 h, all volatile fractions are removed and the product is isolated as a waxy solid (29 mg, 78%). XH NMR: (CDC13) d 3.2 (s, 3H), 4.25 (s, 2H), 4.38 (s, 2H), 5.88 (s, 2H), 6.30 (s broad, 1H), 6.42 (s broad, 2 H) ), 6.65 (m, 3 H), 7.05 (s, 1H), 8.40 (s, 1 H). Another specific example of the synthesis of vun compound of (XIc) is provided: Boc-pyrrolidine (3.0 g, 17.5 mmol) is dissolved in ether (35 ml) and tetraethylethylenediamine (TMEDA) (2.03 g, 17.5 mmol), cooled at -78 ° C and s-butyllithium (1.3 M, 13.5 ml, 18 mmol) is added. After stirring for 1 hour, allyl bromide in ether (5 ml) is added. After warming to room temperature, the reaction is suspended with water and the organic layer is separated. The organic layer is washed with a 1 M solution of NaHP04 and water, and then dried over MgSO4. The solvent is removed in vacuo and the residue is purified by chromatography on silica gel (hexanes / ethyl acetate (9: 1) to give the olefin (0.50 g, 14%, XH NMR: (CDC13) d 5.56-5.85 (m, 1H), 5.00-5.20 (m, 2 H), 3.70-3.90 (m, 1H), 3.20-3.45 (m, 2H), 2.35-2.60 (M, 1H) 2.00-2.20 (m, 1H) ), 1.60-2.00 (m, 4H), 1.45 (s, 9H)). Olefin is dissolved (500 mg, 2.37 mmol), 5-bromo-l, 3-benzodioxolane (476 mg, 2.37 mmol), triethylamine ( 478 mg, 4.74 mmol), tri-o-tolylphosphine (96 mg, 0.31 mmol) and Pd (OAc), (26 mg, 0.12 mmol) in CH3CN, reflux overnight under argon, add 1 additional equivalent (476 mg) of the bromide and Pd (OAC) 2 (52 mg, 0.24 mmol), and the reflux continues for 4.5 hours The reaction is filtered and the solvent is evaporated The residue is taken up in ether and washed successively with water , NaH2P04 1 M, water and brine After drying, the solvent is removed and the product is purified by chromatography (silica gel, hexane: acetamide ethyl acetate, 4: 1) to provide 152 mg (19%) of the Boc-protected [(1,3-benzodiox-5-yl) prop-2-enyl] pyrrolidine (XH NMR: (CDC13) d 6.90 ( s, 1 H), 6.70-6.80 (m. 2H), 6.35 (d, 1H). 3.80-3.95 (m, 1H), 3.25-3.50 (m, 2H), 2.45-2.70 (m, 1H), 2.20-2.35 (M, 1H), 1.70-2.00 (M, 4H), 1.45 (s, 9H) )). The Boc group is removed under standard or conventional conditions. Another specific embodiment of the generic synthesis as applied to a compound of the invention is as follows: To butyl alcohol (3 ml) is added 2-fluoro-4-chloropurine (41 mg, 0.24 mmol), N- [(1, 3-benzodioxol-5-yl) methyl] piperidin-2-acetamide (66 mg, 0.24 mmol) and Hünig's base (diisopropylethylamine) (0.042 ml, 0.24 mmol). After stirring at 90 ° C for 6 hours, the reaction is diluted with ethyl acetate. The organic material is washed with NH 4 Cl and brine, dried (MgSO 4) and the solvent removed in vacuo. Chromatography of the residue (CH2Cl2 / MeOH, 10/1) gives 42 mg of fluoropurine. Fluoropurine (18.9 mg, 0.046 mmol) is dissolved in DMSO and reacted with TMS-imidazole (0.10 g, 0.66 mmol) and CsF (61 mg, 0.40 mmol). After shaking
130 ° C for 72 hours, the reaction is diluted with ethyl acetate and washed with saturated NH 4 Cl and brine. The organic layer is dried (MgSO 4), the solvent is removed in vacuo and the residue is subjected to chromatography (CH 2 Cl 2 / MeOH, 19/1) to provide 12 mg of N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) yl) purin-6-yl] piperidin-2-acetamide. Another specific example of synthesis is provided: To THF (10 ml) is added cyanuric chloride (158 mg, 0.85 mmol), N - [(1,3-benzodioxol-5-yl) methyl] piperidin-2-acetamide (47 mg , 0.17 mmole) and imidazole (58 mg, 0.85 mmole).
After stirring for 12 hours, the reaction is diluted with ethyl acetate. The organic material is washed with saturated NH4C1 and brine, dried (MgSO4) and the solvent removed in vacuo. Chromatography of the residue (hexanes / ethyl acetates 4/1) gives 60 mg of dichlorotriazine. Dichlorotriazine 5 (20 mg, 0.047 mmol) is dissolved in THF and reacted with TMS-imidazole (0.009 ml, 0.06 mmol) and CsF (11 mg, 0.07 mmol) at 0 ° C. After warming to room temperature and stirring for 4 hours, the reaction is diluted with ethyl acetate and washed with saturated NH 4 Cl, water and brine. The organic layer is dried (MgSO.sub.4), the solvent is removed in vacuo and the residue is subjected to chromatography (ethyl acetate / hexanes / MeOH, 4/4/1) to yield 6.5 mg of N- [(l, 3 -benzodioxol-5-yl) methyl] -1- [(3-chloro-5- (lH-imidazol-1-yl) triazin-2-yl] piperidin-2-acetamide Another specific example of synthesis is provided: A a solution of indole-5-carboxylic acid (0.50 g,
3. 1 mmole) in MeOH (25 ml) is added trimethylsilyldiazomethane until no gas production is observed. The solution is concentrated, dissolved in CH2C12 and washed with saturated NaHCO3 and brine. The organic layer is dried (MgSO.sub.4) and the solvent is removed in vacuo to provide 0.54 g of the ester (1ti NMR: (CDC13) d 3.95 (s, 3H), 6.63 (s, 1H), 7.25 (m, 1H), 7.40 (d, 1H), 7.95 (d, 1H), 8.25-8.4 (broad s, 1H), 8.45 (s, 1H)). The ester (100 mg, 0.58 mmol) is dissolved in DMF (10 ml) and 4-chloro-2-imidazol-1-ylpyrimidine (113 mg, 0.63 mmol) is added. After heating at 60 ° C for 18 hours, the solvent is removed in va cuo, the residue is dissolved in CH2C12 and washed with NaHCO3 and brine. The organic layer is dried (MgSO 4), the solvent is removed in vacuo and the residue is subjected to chromatography (CH 2 Cl 2 / MeOH, 19/1) to provide 68 mg, (37%) of the pyrimidine (XH NMR: (CDC13 ) d 3.95 (s, 3H), 6.90 (s, 1H), 7.25 (m, 2H), 7.80 (m, 1H), 7.95 (s, 1H), 8.10 (d, 1H), 8.4 (s, 1H) , 8.50 (d, 1H), 8.70 (m, 2H)). The pyrimidine is dissolved in THF / water (1/1) and LiOH (6 mg, 0.21 mmol) is added. After heating at 60 ° C for 3 h, the solvent is removed in va cuo and acidified with methanolic HCl. The solvent is removed in vacuo, dissolved in DMF and treated with HATU 42 mg, 0.11 mmol), DIEA (37 mg, 0.21 mmol) and piperonyl amine (26 ml, 0.21 mmol). After stirring for 18 hours, the solvent is removed in vacuo, the residue is dissolved in CH2C12 and washed with saturated NaHCO3 and brine. The organic layer is dried (MgSO 4), the solvent is removed in vacuo and the residue is subjected to chromatography (CH 2 Cl 2 / MeOH, 19/1) to provide 2 mg (4%) of N- [(1,3-benzodioxol- 5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] indole-6-carboxamide; XH NMR: (CDC13) d 3.75 (s, 2H), 5.95 (s, 2H), 6.80-6.90 (m, 2H), 7.05-7.15 (m, 2H), 7.25 (m, 2H), 7.75-7.85 ( m, 2H). 8.00 (s, 2H), 8.50-8.60 (m, 2H). 8.70-8.80 (m, 1H); MS: 439.2 M + H) X Another specific embodiment of the generic synthesis as applied to a compound of the invention is N- [(1,3-benzodioxol-5-yl) ethyl] -l- [2- (lH- imide zol-1-yl) pyrimidin-4-yl] pyrrole-2-carboxamide [MS: (403.2 M + H) +], which is prepared in a manner similar to that described above for N- [(1 , 3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] indole-6-carboxamide.
Reaction scheme 3 below shows a method for preparing the compounds of the invention wherein U is CR5 (wherein R6 is hydrogen) and X, Y and Z are CR19 (wherein R19 is hydrogen):
Reaction scheme 3
The above synthesis can be carried out as follows: To benzene (20 ml) is added 1- (3-aminophenyl) imidazole (755 mg, 4.7 mmol), 7-chloro-3-oxoheptanoic acid ethyl ester (982 mg, 4.7 mmoles), Na2HP04 (667 mg, 4.7 mmol), I2 (60 mg, 0.23 mmol) and molecular sieves of 4Á (500 mg). After refluxing for 6 hours, more I, (60 mg) is added. After stirring for 16 hours, the reaction is filtered, the solvent is removed in vacuo and the residues are chromatographed (CH2Cl2MeOH, 98/2) to give 120 mg, (8%) of 1- [3- (lH -imidazol-l-yl) phenyl] piperidin-2-acrylic acid ester (? RMN: (CDC13) d 7.85 (s, 1H), 7.05-7.50 (m, 6H), 4.80 (s, 1H), 4.15 (c, 2H), 3.45 (t, 2H), 2.4 (t, 2H0, 1.5-1.8 (m, 6H, 1.30 (t, 3H)) This ester (120 mg, 0.38 mmol) is dissolved in MeOH ( 20 ml) and reacted with 10% Pd / C (60 mg) and 1 atm of H. After reacting for 60 hours, the reaction is filtered, the solvent is removed in vacuo and the residue is chromatographed. (ethyl acetate / hexanes, 1/1) to provide 24 mg of 1- [3- (1H-imidazol-1-yl) phenyl] piperidin-2-acetic acid ethyl ester (compound of formula (XV)). This ester (24 mg, 0.076 mmol) is dissolved in 5% methanolic NaOH, after stirring for 16 hours, the reaction is acidified with methane HCl. The solvent is removed in vacuo and the residue is dissolved in DMF. Piperonyl amine (1 equivalent) base of Hunig (2 equivalents) and HATU (1 equivalent) are added. After completion of the reaction, the reaction mixture is partitioned with water and ethyl acetate. The organic layer is separated, washed with water and dried. The solvent is removed in vacuo and the residue is subjected to chromatography (ethyl acetate / MeOH, 98/2) to give 6 mg of the compound of formula (Ibb), N- [(1,3-benzodioxol-5-yl) ) methyl] -1- [3- (lH-imidazol-1-yl) phenyl] piperidin-2-acetamide:: H NMR: (CDC13) d 7.80 (s, 1H), 7.10-7.30 (m, 4H), 6.50-6.70 (m, 5H), 5.90 (s, 2H), 4.20-4.35 (m, 2H), 3.85 (s broad, 1H), 3.50 (t, 2H), 2.95 (d, 1H), 2.35-2.55 (m, 2H), 1.4-1.9 (m, 6H); MS: (419 M + H] X The following Reaction Scheme 4, shows a method for preparing compounds of the invention wherein A is -OR1:
Reaction Scheme 4 10 25
The above synthesis can be carried out as follows: To DMF (100 ml) is added 4-chloro-2-imidazol-1-pyrimidine (0.50 g), 2.77 mmole), 2-piperidinetanol (0.359 g, 277 mmole) , and Hünig base (0.536 g, 4.15 mmol). After heating up
80 ° C for 5 hours, the solvent is removed in vacuo and the residue is subjected to chromatography (CH2Cl2 / MeOH, 19/1) to provide 349 mg (46%) of 1- [(1H-imidazole-1) il) pyrimidin-4-yl] piperidin-2-ethanol (the compound of formula XVI)), (XH NMR: (CDC13) d 8.65 (s, 2H), 8.11 (d, 1H), 7.82 (t, 1H) , 7.11 (d,
1H), 6.44 (d, 1H), 3.60 (m, 2H), 3.03 (m, 1H), 1.77 (m); MS: 274 (M + H) +). To a solution of 1- [(lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanol (25 mg, 0.092 mmol) dissolved in DMF (5 ml) is added NaH (60% dispersion in oil , 5.5 mg, 0.14 mmol) followed by piperonyl chloride (17 mg, 5 0.10 mmol) and t-butylammonium chloride. After stirring for 16 hours at 80 ° C, the solvent is removed in vacuo and the residue is partitioned with saturated NH 4 Cl and CH 2 Cl. The organic layer is separated, dried (MgSO 4), the solvent is removed in vacuo and the residue is subjected to chromatography (CH 2 Cl 2 / MeOH, 19/1) to provide 13 mg (35%) of 4- [2- [[ (1,3-benzodioxol-5-yl) methoxy] ethyl] piperidin-1-yl] -2- (1 H -imidazol-1-yl) pyrimidine (the compound of the formula (Ice)); XH NMR: (CDC13) d 8.52 (s, 1H), 8.05 (d, 1H), 7.80 (s, 1H), 7.09 (s, 1H), 6.73 (m, 3H), 6.45 (d,
1H), 5.93 (s, 2H), 4.30 (s, 2H), 3.45 (m, 2H), 2.95 (m, 1H),, 1.55 (m); MS: 408.7 (M + H) X The compounds of formula (XVI) can be used to prepare other compounds of the invention as shown below in Reaction Scheme 5 wherein Rlb is hydrogen or -CH 3, Ms is mesyl and Ac is acetyl:
Reaction Scheme 5
(xvp)
The above synthesis can be carried out as follows: To a solution of 1- [(lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanol (the compound of formula (XVI)) (236 mg , 0.86 mmol) and methanesulfonyl chloride (99 mg, 0.87 mmol) dissolved in CH2C12 (20 ml) was added TEA (87.5 mg, 0.87 mmol). After stirring for 16 hours at 0 ° C, methanesulfonyl chloride (99 mg, 0.87 mmol) and TEA (87.5 mg, 0.87 mmol) are added and the solution is warmed to room temperature. After stirring for 1 hour, the solution is washed with saturated NH 4 Cl and brine, dried (MgSO 4) and the solvent removed in vacuo to provide 276 mg (91%) of the compound of formula (XVII). { l NMR: (CDC13) d 8.72 (s, 1H), 8.15 (d, 1H), 7.89 (s, 1H), 7.18 (s, 1H), 6.46 (d, 1H), 4.24 (m, 3H), 2.95 (s, 3H), 2.18 (m, 6H), 1.76 (m). MS: 352.5 (M + H) +). A solution of the compound of formula (XVII) (100 mg, 0.28 mmol) and a compound of formula (XVIII) (429 mg, 2.84 mmol) dissolved in CH2C12 (7.5 ml) is stirred for 16 hours and then DMF (7.5 ml). After stirring for 2 hours, the solvent is removed in vacuo and the residue is partitioned with saturated NH4C1 and CH2C12. The organic layer is separated, washed with brine, dried (MgSO.sub.4), the solvent is removed in vacuo and the residue is chromatographed.
(CH2Cl2 / MeOH, 19/1) to provide 6.6 mg (21%) of N - [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidine -4-yl] piperidin-2-ethanamine (the compound of the formula (reads)): X H NMR: (CDC 13) δ 8.50 (s, 1 H). 8.08 (d, 1H), 7.77 (s, 1H), 7.08 (s, 1H), 6.66 (m, 3H), 6.43 (d, 1H), 5.91 (s, 2H), 3.60 (d, 2H), 3.00 (m, 1H), 2.57 (m, 2H), 2.02 (m, 1H), 1.65 (m), MS: 407.8 (M + H) XA THF (3 ml) is added N- [(1,3-benzodioxol -5-yl) methyl] -l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanamine (8 mg, 0.03 mmol), Hünig's base (8 mg, 0.06 mmol) ) and acetic anhydride (4 mg, 0.04 mmol). After stirring for 16 hours, the solvent is removed in vacuo and the residue is subjected to chromatography (CH 2 Cl 2 / MeOH, 19/1) to give 8 mg (60%) of N-acetyl-N- [(1, 3 -benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanamine (the compound of the formula Igg)): XH NMR: (CDC13) d 8.48 (s, 1H), 8.08 (d, 1H), 7.76 (s, 1H), 7.09 (s, 1H), 6.66 (m, 3H), 6.33 (m, 1H), 5.94 (s, 1H), 5.91 (s, 1H), 4.43 (m, 3H), 3.40 (m, 2H), 2.11 (d, 3H). 1.14 (m); MS: 450.0 (M + H) X Alternatively, N - [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) is added to THF (3 ml). pyrimidin-4-yl] piperidin-2-ethanamine (8 mg, 0.03 mmol), Hünig's base (8 mg, 0.06 mmol) and methanesulfonyl chloride (4.5 mg, 0.04 mmol). After stirring for 16 hours, the solvent is removed in vacuo and the residue is subjected to chromatography
(CH2Cl2 / MeOH.19 / 1) to provide 7 mg (51%) of N - [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidine -4-yl] - N- (methylsulfonyl) piperidin-2-ethanamine (the compound of the formula (Iff)); 2 H NMR: (CDC13) d 8.10 (s, 1 H), 7.78 (d, 1 H), 7.13 (s, 1 H), 6.82 (s, 1 H), 6.72 (s, 2 H), 6.30 (d, 1 H), 5.94 (s, 2H), 4.23 (m, 3H), 3.20 (m, 2H), 2.80 (s, 3H), 1.14 (m); MS: 485.7 (M + H)? A DMF (5 ml) is added a compound of formula (XVII) (50 mg, 0.14 mmol), Hünig base (28 mg, 0.21 mmol), and N-methyl piperonylamine (28 mg , 0.17 mmole). After stirring at 80 ° C for 16 hours, the solvent is removed in vacuo and the residue partitioned with saturated NH 4 Cl and CH 2 C 12. The organic layer is separated, washed with brine, dried (MgSO 4), the solvent is removed in vacuo and the residue is partitioned with ethyl acetate and water. The organic layer is separated, washed with brine, dried (MgSO.sub.4), the solvent is removed in vacuo and the residue is subjected to chromatography (ethyl acetate / MeOH, 19/1) to give 7 mg (12%). of N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N-methylpiperidin-2-ethanamine (the compound of formula (Idd)); X H NMR: (CDC13) d 8.53 (s, 1H), 8.07 (d, 1H), 7.80 (s, 1H), 7.10 (s, 1H), 6.78 (s, 1H), 6.69 (m, 2H). 6.43 (d, 1H), 5.92 (s, 2H), 3.40 (m, 2H). 2.97 (m, 1H), 1.80 (m); MS: 422.0 (M + H) X Reaction scheme 6 shows another method for preparing compounds of the invention wherein V is C (R) H:
Reaction Scheme 6
The above synthesis can be carried out as follows: To a solution of LDA (1.28 g, 12 mmol) in THF (30 ml) at -78 ° C is added 2,4-dichloro-6-methylpyrimidine (1.96 g, 12 g). mmoles) in THF (15 ml). After stirring for 15 minutes, 3, 3-dimethylallyl bromide (1.79 g, 12 mmol) in THF (5 ml) is added dropwise. After the reaction is warmed to room temperature, water and ethyl acetate are added. The organic layer is separated, the solvent is removed in vacuo and the residue is subjected to chromatography (ethyl acetate / hexane, 1/19) to give 2.06 g (74%) of 2,4-dichloro-6- (4). -methyl-3-pentenyl) pyrimidine (XH NMR: (CDC13) d 7.15 (s, 1H), 5.10 (t, 1H), 2.80 (t, 2H), 2.45 (m, 2H), 1.70 (s, 3H) , 1.55 (s, 3H)). To a solution of NaI04 (17 g, 51 mmol) and KMn04 (251 mg, 1.59 mmol) in water is added K2C03 (1.29 g, 9.38 mmol) and 2,4-dichloro-6- (4-methyl-3-pentenyl). ) pyrimidine (2.06 g, 8.9 mmol) in t-butanol. After stirring for 16 hours, the reaction is acidified to pH 3 and extracted with ethyl acetate. The organic layer is extracted with aqueous NaHCO3. The aqueous layer is acidified to pH 3 and extracted with ethyl acetate. The organic layer is dried and the solvent removed in vacuo to provide 980 mg of 3- (2,4-dichloropyrimidin-6-yl) propionic acid (the compound of formula (XIX)), lti NMR: (CDC13) d 7.30 s, 1H), 3.05 (t, 2H), 2.90 (t, 2H). The acid is coupled to piperonylamine under standard conditions with isobutyl chloroformate and N-methylmorpholine to provide the compound of formula (XX). Imidazole is added under standard conditions (1-trimethylsilylimidazole and CsF in DMF at 60 ° C) to provide N- [(1,3-benzodioxol-5-yl) ethyl] -6-chloro- 2- (1H-imidazole-1) -yl) pyrimidine-4-propionamide (the compound of formula (Ihh)): MS: 386 (M + H) X The generic synthesis in solid phase can be conceptualized as the generic synthesis of reaction scheme 1 in which R1 has has been replaced by a separable linkage to a derivatized polymer resin. At the end of the Synthesis Scheme, the resin is separated and R1 becomes hydrogen. The solid phase synthesis scheme is illustrated in Reaction Scheme 7 as applied to a specific example, as in the foregoing, of a piperonyl amide, but in this case the amino acid is piperazin-2-acetic acid:
Reaction Scheme 7
(XXV) Continuation of Reaction Scheme 7
vulnerability
ation In solid phase synthesis, the group which becomes R1 is bound to the resin through a separable linkage, such as the 2-nitrobenzyl residue, which can be separated photolytically. In the Example shown, the piperonylamine (see above) has been protected with Boc and reacted with 4- (bromomethyl) -3-nitrobenzoic acid to produce the Boc-protected compound of formula (XXI), which is then attached to a free amine of the synthetic support with amino functionality, derivatized with lysine. In this case, a cross-linked polystyrene grafted with polyethylene glycol, cross-linked DVB 1% polystyrene or crosslinked polydimethylacrylamide is suspended in a polar aprotic solvent such as methylene chloride, DMF or THF. An excess of the suitably protected linker synthon is added to the suspended support followed by a coupling reagent such as diisopropylcarbodiimide (DIC), dicyclohexylcarbodiimide (DCC), bis (2-oxo-3-oxazolidinyl) phosphinic (BOP) or O- (7) chloride. α-azabenzotriazol-1-yl) -1, 1, 3, 3-tetramethyluronium-hexafluorophosphate (HATU) and optionally an acylation catalyst such as dimethylaminopyridine (DMAP) or hydroxybenzotriazole (HOBT). The mixture is stirred at room temperature for 1 to 24 hours or until the reaction is complete judging by a ninhydrin test. The resin is washed with an appropriate solvent or solvents several times to remove excess reagents and by-products to provide the resin compound of formula (XXII). The resin compound of formula (XXII) is deprotected to release the compound of formula (XXIII), which is then suspended in a polar aprotic solvent such as methylene chloride or DMF. An excess of an appropriately protected compound of formula (XXIV) is added followed by a coupling agent such as HATU, BOP or DIC with the optional addition of an acylation catalyst such as DMAP or HOBT. Alternatively, an excess of the activated form of the compound of formula (XXIV) such as the symmetric anhydride of acyl fluoride can be added to the resin. The mixture is stirred for 1 to 24 hours at room temperature and then washed several times with an appropriate solvent or with solvents to remove excess reagents and by-products to provide the resin compound of formula (XXV). The resin compound of formula (XXV) is deprotected to release the compound of formula (XXVI), which is then suspended in a polar aprotic solvent such as DMF or THF. An excess of the appropriate compound of formula (Vlllb) is added followed by an excess of a base such as triethylamine or diisopropylethylamine. The mixture is stirred and heated at 50-100 ° C for 1 to 24 hours, then cooled and washed several times with a suitable solvent to remove excess reagents and by-products to provide the resin compound of formula (IXaa) . The resin compound of the formula (IXaa) is optionally treated to release the protected functionality incorporated as part of a synthon to produce the compound of the formula (III). For those compounds in which the piperazine substitution pattern is reversed (for example, in Examples 95 to 102 below), the procedure of the preceding paragraph may be modified slightly. The resin compound of formula (XXV) is deprotected with piperidine to liberate an amine and then dissolved or suspended in an inert solvent, such as methylene dichloride. An excess of a suitably protected acid that will provide the R5 is added, followed by a coupling agent such as HATU, BOP or DIC, with the optional addition of an acylation catalyst such as DMAP or HOBT. Alternatively, an excess of an activated form of the acid, such as the symmetrical anhydride of acyl fluoride, may be added to the resin. The mixture is stirred for 1 to 24 hours at room temperature and then washed several times with an appropriate solvent or with solvents to remove excess reagents. The product is suspended in a polar aprotic solvent, such as DMF or THF. An excess of the appropriate compound of formula (Vlllb) is added followed by an excess of a base such as triethylamine or diisopropylethylamine. The mixture is stirred and heated at 50-100 ° C for 1 to 24 hours, then cooled and washed several times with an appropriate solvent to remove excess reagents and by-products to provide the resin compounds analogous to the resin compound. of formula (IXaa) but having pyrimidine bound to the piperazineacetic acid in the 4-position. The resin compound analogous to the resin compound of the formula (IXaa) is then suspended in a protic solvent such as methanol or acetonitrile-water and stirred and photolysis to separate the product from the resin. Filtration and evaporation of the filtrate provides the untreated product, which is then purified and characterized by standard techniques. In a specific example, 1.57 g of TentaGel resin with amino functionality (0.80 mmol) in 20 ml of methylene chloride is suspended and treated with 1.05 g of linker acid (2.4 mmoles), 0.50 ml of DIC (3.2 mmoles) and mg of DMAP (0.16 mmol). The mixture is stirred at room temperature for 20 hours and then washed with methylene chloride ten times to provide a resin compound of formula (XXII). The resin compound of formula (XXII) is treated with 50% trifluoroacetic acid (TFA) in methylene chloride at room temperature for 2 hours and then washed with methylene chloride ten times, 15% triethylamine in methylene chloride for 10 hours. minutes and again in methylene chloride for 5 times. The deprotected resin compound of formula (XXIII) is then suspended in 12 ml of methylene chloride and treated with 1444 g of the compound of formula (XXIV) (3.2 mmoles), 1,216 g of HATU (3.2 mmoles) and 1.3 ml of diisopropylethylamine (7.2 mmoles). The mixture is stirred for 16 hours at room temperature and then washed five times to provide the resin compound of formula (XXV). Fmoc is removed by treatment with 30% piperidine in DMF and 777 mg of the resulting resin bound compound of formula (XXVI) (0.35 mmol) then reacted with 320 mg of 2-imidazolyl-4-chloropyrimidine (the compound of formula XVIIIb )) in the presence of 0.61 ml of diisopropylethylamine (3.5 mmoles) in 12 ml of DMF at 80 ° C for 15 hours and then cooled to room temperature and washed with DMF and methylene chloride to provide the resin compound of formula ( IXaa). The final product is separated from the resin by photolysis in methanol (MeOH) for 17 hours to provide 54.6 mg of product, a compound of formula (III) (31%). The untreated product is purified by flash chromatography (eluting with 4: 4: 1 ethyl acetate: hexanes: MeOH). The Boc-protected amine product is treated with 3 ml of 30% TFA-methylene chloride for 1 hour and dried in vacuo to provide a quantitative amount of the product. The piperazine acetic acid compound of formula (XXIV) used in the above synthesis and many others in this application, are synthesized as follows: twelve milliliters (50 mmol) of N, N'-dibenzylethylene diamine, 14 ml (100 mmol) are combined. ) of Et3N and 250 ml of toluene at 0 ° C, and 7 ml (50 mmol) of methyl 4-bromocrotonate (7 ml, 50 mmol) are added. The reaction is warmed slowly to room temperature, stirred for 24 hours, filtered, concentrated in vacuo to a residue and treated with 10% aqueous HCl (300 ml). The mixture is filtered again and the filtrate is washed with ethyl acetate (2 x 100 ml). The filtrate is made basic with K2C03 and extracted with ethyl acetate (3 x 150 ml). The combined extracts are washed with brine, dried over MgSO4 and concentrated in vacuo to provide 13.7 g of 1,4-dibenzylpiperazine-2-methyl acetate. XH NMR: (CDC13) d 2.28-2.50 (m, 4H), 2.5-2.75 (m, 4H), 3.1 (broad s, 1H), 3.42 (d, 2H), 3.52 (d, 1H), 3.6 (s) , 3H), 3.75 (d, 1H), 7.15-7.35 (m, 1H). The 13.7 g (40 mmol) of 1,4-dibenzylpiperazine-2-methyl acetate, 150 ml of MeOH, 50 ml of 1 N HCl (aqueous) and 3 g of 10% Pd / C are combined and hydrogenated with H2 (3.5 kg / cm2 (50 psi)) for 24 hours. The reaction is filtered, the filtrate is concentrated in vacuo to remove most of the MeOH and the residue is made basic with K2C03 until pH = 9-10, and 9.8 g (40 mmoles) of BOC- are added slowly at 0 ° C. ON. The reaction is stirred at 0 ° for 1 hour, allowed to warm to room temperature, stirred for 2 hours and extracted with ethyl acetate (2 x 200 ml). The combined extracts are left with 50 ml of 10% HCl (aqueous). The aqueous layer is washed with ethyl acetate, made basic with MgSO 4 and extracted three times with ethyl acetate. The combined organic layers are washed with brine, dried over MgSO4 and concentrated in vacuo to provide 7.89 g of methyl 4-Boc-piperazin-2-acetate; XH NMR: (CDC13) d 1.4 (s, 9H), 2.31 (dd, 1H), 2.37 (dd, 1H), 2.55 (broad, 1H), 2.69-3.02 (m, 4H), 3.75 (s, 3H) , 3.88 (broad, 2H). A portion of the product of methyl 4-Boc-piperazin-2-acetate (5.2 mg, 20 mmol) from the previous step is combined with 60 ml of THF and 60 ml of 1 N NaOH (aqueous) and stirred at room temperature for 6 hours to saponify the methyl ester. The reaction is cooled to 0 ° C, adjusted to pH 9-10 with 10% HCl (aqueous) and 5.2 g (20 mmoles) of FMOC-C1 are added. The reaction is stirred at room temperature for 6 hours (adding 1 N NaOH (aqueous) to maintain pH = 9-10) 1 hour, and then acidified with 10% HCl until pH = 1. The reaction is extracted twice, The combined organic layers are washed with brine, dried over MgSO4 and concentrated in vacuo to provide 8.55 g of the desired 4-Boc-1-Fmoc-piperazine-2-acetic acid (the compound of formula (XXIV)); XH NMR: (CDC13) d 1.4 (s, 9H), 2.5-3.0 (m, 5H), 3.9-4.2 (m, 6H), 4.5 (m, 1H), 7-25 (t, 4H), 7.32 ( t, 4H), 7.48 (d, 4H), 7.75 (d, 4H). In cases where 4-Boc-1-Fmoc-piperazine-2-acetic acid (the compound of formula (XXIV)) is replaced by 4-Boc-1-Fmoc-piperazine-2-carboxylic acid, the material Initial is prepared by dissolving 5.25 g (25.85 mmoles) of 2-piperazinecarboxylic acid-2HC1 in 160 ml of 1: 1 dioxane / H20, and adjusting the pH to 11 with 50% NaOH (aqueous). A solution of 7.21 g (29.28 mmoles) of BOC-ON in 40 ml of dioxane is added slowly (in portions) while maintaining the pH in 11 with 50% NaOH (aqueous) during the addition. The reaction is stirred at room temperature for 5 hours, then cooled to 0 ° C and adjusted to pH 9.5, with 50% NaOH (aqueous). A solution of 7.34 g (28.37 mmoles) of Fmoc-Cl in 40 ml of dioxane is added slowly (in portions), maintaining a pH of 9.5 during the addition of 50% NaOH (aqueous). The mixture is warmed to room temperature, stirred for 20 hours, washed with ethyl ether (3 x 150 ml), adjusted to pH = 2-3 with 6 N HCl (aqueous) and extracted with toluene (3 x 150). ml). The combined extracts are dried over Na 2 SO 4, concentrated in vacuo to a volume of 150 ml and cooled to -20 ° C overnight. The resulting solids are separated by filtration, washed with hexane and dried in vacuo to provide 5.4 g of the desired 4-Boc-1-Fmoc-piperazine-2-carboxylic acid. Alternatively, 4-Boc-morpholine-3-carboxylic acid can be prepared in the following manner, which can be substituted for the compound of formula (XXIV) in Reaction Scheme 7 above to prepare other compounds of the invention. To a solution of the 4-phenylmethylmorpholin-5-one-3-carboxylic acid methyl ester (5.1 g, 20.5 mmol) in 100 mL of THF is added borane / DMS (10 M, 2.6 mL) slowly while cooling to 0 °. C. The solution is allowed to warm to room temperature and is stirred for 18 hours. Water (100 ml) is then added and the mixture is extracted with ethyl acetate. The organic layers are dried over MgSO4 and concentrated. The resulting oil is purified on a column of silica gel eluted with ethyl acetate: hexanes 3: 7 to give the morpholine (3.0 g, 84%). The morpholine (3.0 g, 12.75 mmol) is dissolved in 50 ml of MeOH and 10% Pd / C (10 mg) is added. The mixture is stirred at room temperature under an atmosphere of H2 for 16 hours. The mixture is then filtered through Celite and concentrated. The resulting oil is dissolved in CH2C1, (25 ml) and di-t-butyldicarbonate (2.8 g, 12.75 mmol) is added. After stirring for 4 hours, the mixture is concentrated and taken up in CH2C12 and washed with water, saturated NaHCO3 and brine. The organic layer is dried over MgSO4 and concentrated to provide 2.8 g (89%) of the ester. The ester is dissolved in MeOH (30 ml) and NaOH (1.4 g, 35 mmol) is added. After stirring for 4 hours at reflux, the solution is concentrated, acidified with 1 N HCl and extracted with CH2C12. The organic layer is dried (MgSO 4) and concentrated to give 4-Boc-morpholine-3-carboxylic acid as a white solid (2.4 g., 90%). X H NMR: (CDC13) d 1.40 (m, 9H), 3.20-350 (m, 2H), 3.70 (m, 2H), 3.90 (m, 1H), 4.30-4.65 (m, 2H). The l-Boc-perhydroazepin-2-acetic acid can also be substituted by the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared as follows: N-Boc-perhydroazepine (1.06 g, 5.16) is treated mmoles) in ether with TMEDA (715 mg, 6.16 mmol) followed by sec-butyllithium (1.3 M, 4.74 ml, 6.16 mmol) at -78 ° C. The reaction is warmed slowly to -40 ° C, stirred for 1 hour, cooled to -78 ° C and treated with a solution of 3,3-dimethylallyl bromide (918 mg, 6.16 mmol) in ether. After warming to room temperature and suspending with water, the organic layer is washed with water, 1 M NaH2P04, water and brine. After drying (MgSO 4) the solvent is removed and the product is purified by chromatography (silica gel, hexane: ethyl acetate, 95: 5), to give the olefin (300 mg, 21%, XH NMR: (CDC13) d 5.05-5.20
(m, 1H), 3.55-3.80 (m, 2H), 2.60-2.75 (m, 1H), 1.90-2.20 (M,
3H), 1.10-1.80 (m, 22H). To a solution of NaI04 (2.17 g, 10.2 mmol) and KMn04 (32 mg, 0.2 mmol) in 45 ml of water is added K2C03 (162 mg, 1.18 mmol) and the olefin (300 mg, 1.12 mmol) dissolved in t- butanol (11 ml). After stirring for 3 days, the reaction is acidified to pH 3 and extracted with ethyl acetate. The organic layer is washed with water and brine, dried (MgSO.sub.4) and the solvent removed in vacuo to give l-Boc-perhydroazepine-2-acetic acid (250 mg, 87%):? Ti NMR: (CDC13) d 4.20-4.45 (m, 1H), 3.55-3.80 (m, 1H), 2.00-2.80 (m, 4H), 1.10-1.80 (m, 16H). 4-Boc-morpholine-3-acetic acid may also be substituted for the compound of formula (XXIV) in Reaction Scheme 7, and may be prepared as follows from the methyl ester of 4-benzylmorpholin-3-acid. acetic acid (Brown, GR: Foubister, AJ, Stribling, DJ Chem. Soc. Porkin Trans. 1 (1987), p.547). After hydrogenolysis (Pd (OH) 2.H2) of the benzyl group, the N-Boc derivative is prepared by treatment with di-t-butyl dicarbonate and the ethyl ester is hydrolyzed by an aqueous base to provide the 4-Boc acid. -morpholin-3-acetic. The l-Boc-pyrrolidin-2-propionic acid can also be substituted by the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared in the following manner: Boc-pyrrolidine (5.0 g, 29.2 mmol) is dissolved in ether
(35 ml) and TMEDA (3.0 g, 20 mmol), cooled to -78 ° C and s-butyllithium (1.3 M, 17 ml, 22 mmol) is added. After stirring for 1 hour, allyl bromide (5.1 ml, 57 mmol) is added. After warming to room temperature, the reaction is suspended with water and the organic layer is separated. The organic layer is dried (MgSO4) and the solvent removed in vacuo to give the olefin (2.9 g, 47%, X NMR: (CDC13) d 5.65-5.85 (m, 1H), 5.00-5.20 (m, 2H ), 3.70-3.90 (m, 1H), 3.20-3.45 (m, 2H), 2.35-2.60 (M, 1H), 2.00-2.20 (m, 1H), 1.60-2.00 (m, 4H), 1.45 (s) , 9H)). To the olefin (1.0 g, 4.7 mmol) in THF (20 ml) at 0 ° C borane / THF is added. After warming to room temperature and stirring for 1 hour, H202 (30%, 14 ml) and 3 N NaOH (3.2 ml) are added. The reaction is partitioned with ethyl acetate and separated. The organic layer is dried and concentrated in vacuo.
The residue is added to NaI04 (1.2 g, 5.4 mmol) and Ru04 (10 mg, 0.08 mmol) in water (100 ml) and acetone (10 ml). After stirring for 1 hour, the reaction is concentrated and extracted with CH2C12. The organic layer is extracted with 1N NaOH, the aqueous layer is washed with CH2C12, made acidic with 1 N HCl and extracted with CH2C12. The organic layer is dried (MgSO.) and concentrated to provide 0.14 g (26%) of l-Boc-pyrrolidin-2-propionic acid; XH NMR: (CDC13) d 1.40 (m, 9H), 1.60-2.00 (m, 6H), 2.20 (m, 2H), 2.40 (m, 2H), 3.30 (m, 2H), 3.90 (m, 1H) . 4-Boc-thiomorpholine-3-carboxylic acid can also be substituted by the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared as follows: To THF is added cysteine ethyl ether hydrochloride ( 1.15 g, 6.16 mmol), triethylamine (4.17 ml, 30 mmol) and dibromoethane (2.51 ml, 6.2 mmol). After stirring for 1 hour and refluxing for 16 hours, the solids are removed by filtration. The solvent is removed in vacuo and the residue chromatographed on silica to provide the thiomorpholinocarboxylic acid ethyl ester (0.94 g, 87%). The ester (15.3 g, 95 mmol) is dissolved in dioxane / water (1/1) and di-t-butyl dicarbonate (24 g, 110 mmol) and LiOH are added. After stirring for 3 hours, the solvent is removed in vacuo and the pH adjusted to 3 with KHS03 and extracted with ethyl acetate. The organic layer is separated, washed with brine, dried (MgSO4) and the solvent removed in vacuo to give 17.4 g (78%) of 4-Boc-thiomorpholine-3-carboxylic acid: H NMR: (CDC13) d 1.45 (m, 9H), 2.45 (m, 1H), 2.71 (m, 1H), 2.93 (m, 1H), 3.10
(m, 1H), 3.29 (m, 1H), 4.11 (m, 1H), 4.19 (m, 1H), 5.20 (m, 1H). 4-Boc-thiomorpholine-3-acetic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared as follows: A THF
(50 ml) is added methyl bromocrotonate (1.0 ml, 8.6 mmol), Hünig's base (1.5 ml, 8.6 mmol) and N-Boc-2-aminoethanethiol
(1.5 g, 8.6 mmol). After stirring for 3 hours, the reaction is poured into saturated NH4C1 and extracted with ethyl acetate. The organic layer is washed with brine, dried (MgSO 4) and the solvent removed in vacuo. Chromatography
(hexane / ethyl acetate, 6/1) gives the methyl ester of N-Boc-2-aminoethanethiocrotonic acid. The ester is dissolved in CH2C12 (80 ml) and TFA (20 ml) is added. After shaking during
1 hour, the solvent is removed in va cuo. The residue is added to a solution of toluene and TEA (2.5 ml). After stirring for 16 hours, the solvent is removed and the residue is subjected to chromatography to provide the thiomorpholine. Dissolve the ester (18.0 g, 95 mmol) in dioxane / water (1/1) and add di-t-butyl dicarbonate (19.6 g, 90 mmol) and LiOH.
After stirring for 12 hours, the solvent is removed in vacuo and the pH adjusted to 3 with KHS03 and extracted with ethyl acetate. The organic layer is separated, washed with brine, dried (MgSO4) and the solvent removed in vacuo to give 20.3 g (86%) of 4-Boc-thiomorpholine-3-acetic acid; X NMR: (CDC13) d 1.45 (m, 9H), 2.45 (m, 1H), 2.51 (m, 1H), 2.68 (m, 1H), 2.82 (m, 1H), 3.05 (m, 4H), 4.24 (s, 1H), 4.93 (s, 1H). 4-Boc-thiomorpholino-2-acetic acid can also be substituted by the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared as follows: a THF (100 ml) is added diethyl fumarate ( 3.27 ml, 820 mmol), DBU (7.22 ml, 50 mmol) and aminoethanethiol hydrochloride (2.26 g, 20 mmol). After refluxing for 16 hours, the reaction is poured into saturated NaHCO 3 and extracted with ethyl acetate. The organic layer is washed with brine, dried (MgSO 4) and the solvent removed in vacuo. Chromatography (ethyl acetate) provides thiomorpholinone (2.61 g, 70%). The ester is dissolved in THF (50 ml) and borane / DMS (3 ml, 30 mmol) is added. After stirring for 16 hours, ethanol is added to suspend the reaction. HCl gas is bubbled into the reaction and the mixture is refluxed for 2 hours. The solvent is removed in vacuo and the residue is suspended in 0.5 M NaOH and CH2C12. The organic layer is separated, dried (Na 2 SO 4) and the solvent removed in vacuo. Chromatography on silica
(MeOH / ethyl acetate) provides the starting material (0.71 g,
29%) and thiomorpholine (1.26 g, 56%). The ester (3.0 g, 11.4 mmol) is dissolved in dioxane / water (1/1) and di-t-butyl dicarbonate (2.29 g, 10.5 mmol) and LiOH are added. After stirring for 12 hours, the solvent is removed in vacuo and the pH adjusted to 3 with KHS04 and partitioned with ethyl acetate. The organic layer is separated, washed with brine, dried (MgSO 4) and the solvent removed in vacuo to provide 2.20 g (81%) of 4-Boc-thiomorpholine-2-acetic acid; XH NMR: (CDC13) d 1.44 (m, 9H), 2.59 (m, 4H), 3.17 (m, 1H), 3.2-4.0 (, 4H). Reaction Scheme 7 shows a synthesis in which a preformed protected compound of formula (XXI) is coupled to the resin and deprotected to allow reaction with the protected compound of formula (XXIV). It will be apparent to a person familiar with the art that the sequence of this series of reactions can be altered to provide the same deprotected piperonylamino-methyl-benzoyl resin. Follow an example of such a sequence. This example also illustrates the manner in which one can reverse the substitution pattern of the piperazine acetic acid ring. 4-Bromoethyl-3-nitrobenzoic acid (819 mg, 3.15 mmol) and HOBt (426 mg, 3.15 mmol) in 15 ml of DMF are treated., DIC (795 mg, 6.30 mmol) is added and the contents are stirred for 30 minutes at room temperature. The mixture is then added to the resin and stirred overnight. The resin is filtered, washed and dried as in the above. The resin shows a negative stain with ninhydrin. The resin is taken up in 15 ml of THF containing piperonylamine (1.51 g, 10 mmol) and stirred over a weekend. The resin is filtered, washed and dried (1.507 g). N1-Fmoc-N-Boc-piperazine-2-acetic acid (9.78 mg, 2.1 mmol), HATU (798 mg, 2.1 mmol) and DIEA (542 mg, 4.2 mmol) in 15 ml of DMF are mixed.; and then it is added to the resin. After stirring for 24 hours, the resin is filtered, washed and dried in a conventional manner; the resin weighs 1,693 g. The resin is taken up in 15 ml of 30% v / v piperidine in DMF, and stirred for 2 hours to remove the Fmoc protecting group. After filtration, the resin is subjected to the usual washing and the drying cycle; the resin weighs 1,588 g. The resin, acetic anhydride (591 mg, 5.8 mmol) and DIEA (748 mg, 5.8 mmol) are taken up in 15 ml of methylene chloride and stirred overnight to acetylate in N1. After filtration, the resin is washed with methylene chloride and dried in a vacuum desiccator for 5 hours. The resin is stirred with 15 ml of 1: 1 TFA: methylene chloride for 1 hour to remove the protective group tBoc in N. After filtration, the resin is washed with methylene chloride (5 x 15 ml), followed by 20% triethylamine in methylene chloride (5 x 15 ml) and then again with methylene chloride (5 x 15 ml). After drying, the resin weighs 1294 g. 669 mg of the resin from the previous step, DIEA (116 mg, 0.9 mmol) and 4-chloro-2- (1-imidazole) -6-isopropylpyrimidine (200 mg, 0.9 mmol) are taken up in 6 ml of DMF and heat at 80 ° C for 24 hours. After filtration the resin is washed (DMF, methanol and methylene chloride) and dried. A portion (377 mg) of the resin from the previous step is suspended in methanol and photolyzed at 50 ° C for 6 hours. The solution is filtered, the solvent is removed and the residue is purified by chromatography (silica, methylene chloride: methanol, 95.5), yield 14 mg. The X NMR and MS were consistent with the proposed structure. The following compounds, which are shown in
Table 1 to Table 7 are representative of the compounds of the inventions and are synthesized by the preceding methods. All show inhibitory activity of iNOS at concentrations lower than 25 μM.
TABLE
Ex. # R- R5 Rc R9 -CH.R3
-CH.R9 Cl Ac
CH ^ -CH.R3 Boc
-CH, R9 Boc -CH.R9 Cl Boc CH.
-CXR9 Cl
-CH, R9 Cl
-CH.R9 Cl "N"
-CH-R9
-CH, R9 Cl
- (CH. Cl H R9
-N '
-CH.RS Cl (X
-CH, R9 H
-CH.R9 Cl Boc -N '
80 -. 80 - (CHUR9 Cl Boc
- (CHUR9 CH. Boc
82 -. 82 - (CH,) U Cl Ac
- 17:
: CH -), R3 Cl C (0) CH- CH (CH,)
84 -. 84 - (CHUR5 Cl
85 XHUR9 CH,
86 -. 86 - (CHUR9 Cl Ac
87 -. 87 - (CH,) 2R9 Cl -C (0) CH,
88 -. 88 - (CH, XR3 CH, Ac
- 17:
.76 -
98 -. 98 -CH, R9
99 -. 99 -CH-R9 Cl C (0) OCH,
-CH.R9 0 C (0) OCH3"Cl
.77
- _7¡
- .79
-CH, R9 Cl
-CH, R9 CH,
-CH-R9 IPr
- (CH,) .- Cl R9
1 - . 1 -
TABLE 2 .84
or -
.87 -
8S
TABLE 3 Compound of the invention amino acid derivatives (AA, Q-R3
.92
.93 -
- L94
- 193 - TABLE 4 Compound of the invention amino acid derivatives (AA)
Q- J
TABLE 5 Compound of the invention derived from amino acids 0-R
TABLE 6
Physical data for the compounds of the invention
TABLE 7
Linker group (L)
Linker group (-L) Separating reagent
Light
Light
Light
.B ["R" is H or alkylene is O or NH; X is an electron withdrawing group such as Br, Cl or I; and it is the point of attachment of -C (O) -.]
The following compounds were made according to the methods described herein: l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] piperazin-2- acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-methylphenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3-hydroxy-N - [(1,3-benzodioxol-5-yl) methyl] propanamide; 2- [[2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) methyl] pentanediamine: 2- [[2- (lH -imidazol-1-yl) pyrimidin-4-yl] amino] -5- [[amino (nitroimino) methyl] amino] -N - [(1,3-benzodioxol-5-yl) methyl] pentanamide; 2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3- (thiophen-2-yl) -N- [3- (morpholin-4-yl) propyl] propanamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] piperazin-2-acetamide; N - [(4-chlorophenyl) methyl] -1- [2,6-bis (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetamide;
N- [(1, 3-benzodioxol-5-yl) methyl] -4- [2- (1H-imidazol-1-yl) -6-methoxypyrimidin-4-yl] -1- (methoxycarbonyl) piperazine-2- acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -4- (methoxycarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] piperidine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [phenylmethyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [3-phenylpropyl] piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2-phenylethyl] piperazin-2-acetamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(thiophene-2-yl) methyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (methyl) piperazin-2-acetamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3- (methylthio) -N - [(1,3-benzodioxol-5-yl) methyl] butanamide;
2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4- (methylthio) -N- [(4-methoxyphenyl) methyl] butanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4- (methylthio) -N- [2- (3, 4-dimethoxyphenyl) ethyl] butanamide; 2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4- (methylthio) -N- (methyl) butanamide; 2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -3- [(1,1-dimethylethyl) thio] -N- [3- (methylthio) propyl] ] propanamide; 2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -3- [(1,1-dimethylethyl) thio] -N- [3- (phenyl) propyl] ] propanamide; a - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] -2-thiophenpropanamide; a - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- (butyl) -2-thiophenpropanamide; a - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) methyl] -2-thiophenpropanamide; 2- [[6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] amino] -3 - [(1,1-di? Ethylethyl) thio] - N - [2 - (3 ,.-dimethoxyphenyl) ethyl] propanamide; 2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] acetamide; 2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] propanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] pentanediamide;
2- [[6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] amino] -N- [(4-methoxy phenyl) methyl] pentanediamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] pentanediamide; N- [(1,3-benzodioxol-5-yl) methyl] -2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -5- [[amino (nitroimino) methyl] -amino] pentanamide; 2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -N - [(4-methoxyphenyl) methyl] - 5 - [[imino (amino) methyl] amino] ] pentanamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3,4-dimethoxy phenyl) ethyl] pyr rol idin-2-carboxamide; 2- [[6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] amino] -N- [(4-methoxyphenyl) -etheyl] -5- [[irnino (nitroamino) methyl] - amino] pentanamide; N- [(1, 3-benzodioxol-5-yl) methyl) -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -5- [[amino (imino) methyl] -amino] pentanamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -4-hydroxy-N- [4- (hydroxycarbonyl) phenyl] methyl] pyrrole idin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -3-hydroxypropanamide; 6-amino [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxy phenyl) ethyl] hexanamide;
a- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [3- (methylsulfonyl) propyl] benzene-propanamide; N- [(1,3-benzodioxol-5-yl) methyl] -2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] (methyl) amino] acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -6 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] hexanamide; 5-amino-N- [(1, 3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] pentanamide; 5-amino-N-butyl-2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] pentanamide; 4- [3-hydroxy-3-oxopropyl) amino] -3- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4-oxobutanoic acid; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] (methyl) amino] -N- [(pyridin-4-yl) methyl] acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N-methylpiperidine-2-carboxamide; N- [2- (3, 4-dimethoxyphenyl) ethyl] -α - [[6- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -2-thiophenpropanamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4-methylpentanamide; N- [(1, 3-benzodioxol-5-yl) methyl] -2- [[6-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] pentanediamide; N- [2 (3,4-dimethoxy phenyl) ethyl] -2- [[6- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -4-methylpentanamide;
N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3-hydroxypropanamide; N- [(1,3-benzodioxol-5-yl) methyl] -α- [[6- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] benzenepropanamide; 5 - [[amino (imino) methyl] amino] -6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (phenylmethyl) pentanamide; N- [(1,3-benzodioxol-5-yl) methyl] -1,4-bis [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- [[phenyl] amino] carbonyl] -piperazin-2-acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- [(methoxy) carbonyl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- (acetyl) -N- [(1,3-benzodioxol-5-yl) methyl] -4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperazin-2 -acetamide; 4- [2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -1-methylpiperazin-2-acetamide; 4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -1-methylpiperazin-2-acetamide; N- [(3-chloro-4-methoxyphenyl) methyl] -4- [2- (IH-imidazyl-l-yl) -8-methylpyrimidin-4-yl] -l-methylpiperazin-2-acetamide;
4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -1-methylpiperazine-2-acetamide; 4- [ß-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4,5-trimethoxyphenyl) methyl] -1-methylpiperazin-2-acetamide; N- [2- (1, 4-benzodioxan-6-yl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -l-methylpiperazin-2-acetamide; l-butyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(furan-2-yl) methylpiperazine-2-carboxamide; N - [(4-Benzodioxan-6-yl) methyl] -l-butyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-acetamide; N- [2- (1, 4-benzodioxan-6-yl) ethyl] -l-butyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazin-2 -acetamide; N- [(2,3-dimethoxyphenyl) methyl] -l-butyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperazine-2-acetamide; 4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -1- [(4-methoxyphenyl) methyl] piperazin-2 acetamide; 4- [6-methyl-2- (lH-imidazyl-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -1- [(4-methoxyphenyl) methyl] piperazin-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -1- [(4-methoxyphenyl) ethyl] piperazin-2-acetamide; 4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -l- [(4-methoxyphenyl) methyl] piperazine -2-carboxamide;
4- [6-met il-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -1- [(4-methoxyphenyl) methyl] piperazine- 2-acetamide; 4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -l- [(4-methoxyphenyl) methyl] piperazin-2 -acetamide; 4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methyl) phenyl) ethyl] -1 - [(4-methoxyphenyl) methyl] pipera zin - 2 -acet amide; 4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -1 - [(4-methoxyphenyl) methyl] piperazine -2-acetamide; 4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin-1-yl) -N- [(indan-5-yl) methyl] -l- [(4-methoxyphenyl) methyl] piperazine -2-acetamide; N- [(1, 3-benzodioxol-5-yl) methyl] -l- [(2,3-dichlorophenyl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piper to zin-2 -acet amide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(3,4-dichlorodenyl) methyl] -4- [2- (1H-imidazol-1-yl) -6-met-ilpyrimidin- 4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(3,4-di chlorophenyl) methyl] -4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] ] pipera zin-2 -carboxamide;
4- [6-met? L-2- (lH-? M? Dazol-1-? L) p? Pm? Dm-4-? L] -N- [2- (1,3-benzod? Oxol- 5 -?) Ethyl] -1 - [(3,4-d? Chlorophen? L) met? L] pipera zm-2-ace tamide; N- [(1,3-benzod? Oxol-5? L) met? L] -1- [(1,3-benzod? Oxol-5-yl) methyl] -4- [2- (lH-? m? dazol-1-? l) p? r? m? dm-4-lyl] p? perazm-2-acetamide; N- [(1, 3-benzod? Oxol-5? L) met? L] -1- [(1,3-benzod? Oxol-5-11) me 111] -4- [2- (lH- m? dazol-1-? l) -6-met? lp? nm? d? n-4-yl] p? perazm-2-carboxam? da; N- [(1,3-benzod? Oxol-5? L) met? L] -1- [(1,3-benzod? Oxol-5-11) me 111] -4- [6-chloro-2] - (1H-α-dazol-1-? l) p? r? m? d? n-4-íl] p? peraz? n-2-carboxam? da; N- [(1,3-benzod? Oxol-5? L) met? L] -1- [(1,3-benzod? Oxol-5-yl) methyl] -4- [6- (lH-? m? dazol-l-? l) p? pm? d? n-4-? l] p? perazm-2-carboxamide; N- [2- (1, 3-benzod? Oxol-5? L) ethyl] -1- [(1,3-benzod? Oxol-5? L) met? L] -4- [2- ( lH-? m? dazol-1-? l) -6-met? lp? r? m? d? n-4-íl] pipe razm- 2 -acet amide; N- [2- (1, 3-benzod? Oxol-6? L) ethyl] -1- [(1,3-benzod? Oxol-5? L) met? L] -4- [2- ( 1H-α-dazol-1-yl) -6-met? lp? r? m? dm-4-yl] piper az? n-2-acet amide; N- [(4-methox? Phen?) Met? L] -1- [(1,3-benzod? Oxol-5-11) me 111] -4- [2- (lH-? M? Dazol- 1-? L) -6-met? Lp? R? M? Dm-4-yl] p? Perazm-2-carboxam? Da;
N- [(4-methoxyphenyl) methyl] -l- [(1, 3-benzodioxol-5-y1) me ti 1] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin- 4-yl] piperazin-2-acetamide; N- [(4-methoxyphenyl) methyl] -1- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-l-yl) -6- (iso-propyl) pir imi in- 4-yl] pipera zin-2-acetamide; N- [2- (4-methoxyphenyl) ethyl] -1- [(1,3-benzodioxol-5-y1) me ti 1] -4- [2- (lH-imidazol-1-yl) -6- methylpyrimidin-4-yl] piperazin-2-acetamide; N - [[2- (phenyl) cyclopropyl] amino] -1- [(1,3-benzodioxol-5-yl) methyl] -4- [β-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-carboxamide; N- [(4-ethoxyphenyl) methyl] -1- [(1,3-benzodioxan-6-y1) me ti 1] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin- 4-yl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(1,3-benzodioxan-6-yl) methyl] -4- [2- (lH-imide zol-1-yl) - 6- (iso-propyl) pyrimin din-4-yl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(1,3-benzodioxan-6-yl) methyl] -4- [2- (lH-imi azol-l-yl) pyrimidine -4-yl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1 - [(1,3-benzodioxan-6-yl) methyl] -4- [6- (lH-imidazol-1-yl) pyrimidine- 4-yl] piperazine-2-carboxamide;
N- [2- (1, 3-benzodioxol-5-yl) ethyl] -l - [(1,3-benzodioxan-6-yl) methyl] -4- [2- (lH-imide zol-1-yl ) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1 - [(1,3-benzodioxan-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piper a zin-2 -carboxamide; N- [(4-methoxyphenyl) methyl] -l- [(1, 3-benzodioxan-6-yl) methyl] -4- (1 H -imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine -2-acetamide; N- [(3,4-dimethoxy phenyl) methyl] -1- [(1,3-benzodioxan-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6- ( iso-propyl) pyrimidin-4-yl] piperazin-2-acetamide; N- [(3,4-dimethyl phenyl) methyl] -1- [(1,3-benzodioxan-6-yl) me ti 1] -4- [2- (lH-imidazol-1-yl) - 6-chloropyrimidin-4-yl] piperazin-2-acetamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1- [(pyrimin-3-y1) me ti 1] -A- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [(1,4-Benzodioxan-6-yl) methyl] -1- [(pyridin-3-yl) methyl] -4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperazine-2-carboxamide; N- [2- (1, -benzodixoan-6-yl) ethyl] -1- [(pyridin-3-y1) me ti 1] -4- [2- (lH-imidazol-l-yl) -6 -methylpyrimidin-4-yl] piperazin-2-acet amide;
N- [(4-methoxyphenyl) methyl] -l- [(pyridin-3-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazin-2 -carboxamide; N- [(3,4-dimethoxy phenyl) methyl] -1- [(pyridin-3-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6- (iso-propyl) pyrimidin-4-yl] piperazin-2-acetamide; N- [2- (3,4-dimethoxyphenyl) ethyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] - A - [2- (lH-imidazol-1-yl) -6- (isopropyl) pyrimidin-4-yl] piper to zin-2-acet amide; N- [3- (3,4-dimethoxyphenyl) propyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-imidazol-1-yl) -6- (isopropyl) pyrimidin-4-yl] piperazin-2-acetamide; N- [(4-ethoxyphenyl) methyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-imidazol-l-yl) -6-met-ilpyrimidin-4-yl] piperazin-2-acetamide; N- [2- (4-methylphenoxy) ethyl] -1- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-imide zol-1-yl) -6-chloropyrimidin-4- il] piperazin-2-acetamide; N- [(4-methylphenyl) methyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine -2-acetamide; N- [(4-chlorophenyl) methyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (1 H -imidazol-1-yl) -6-met-ilpyrimidin-4-yl ] piperazin-2-acet amide;
N - [(4-chlorophen? L) met? L] -1 - [(3-fluoro-4-methox? Phen? L) met? L] -4- [2- (lH-? M? Dazol-1 -? l) -6-chlorop? r? m? dm-4-yl] p? perazm-2-acetam? da; N- [(1, 3-benzod? Oxol-5? L) met? L] -l- [(3-fluoro-4-methox? Phen? L) met? L] -4- [2- (lH -? m? dazol-1-? l) -6-chlorop? pm? d? n-4-yl] p? perazm-2-acetam? da; N- [2- (1, 3-benzod? Oxol-5? L) et? L] -l- [(3-fluoro-4-methox? Phen?) Met? L] -4- [2- (lH-? m? dazol-1-? l) -6-met? lp? r? m? dm-4-yl] piperaz? n-2-acet amide; N- (2- (1, 3-benzod? Oxol-5? L) et? L] -l- [(3-fluoro-4-methox? Phen?) Met? L] -4- [2- (lH-? m? dazol-1-? l) p? pm? dm-4-yl] piper az? n-2-acet amide; N- [2- (l, 4-benzod? oxan-6? l) et? l] -l - [(3-fluoro-4-methox? phen? l) met? l] -4- [2- (lH-? m? dazol-1-? l) p? r? m? d? n-4-yl] peraz? n-2-acetam? da; N- [2- (4-methox? phen? l) ethyl] -1- [(3-fluoro-4-methoxy) fen? l) met? l] -4- [2- (lH-? m? dazol-1-? l) -6- (iso-propyl) p? pm? d? n-4-? l] pipera zin-2 -acet amide; N- [(3,4-d? methox? phen?) ethyl] -l-acet? l-4- [2- (1H-? m? dazol-1-? l) -6- (iso-propyl) p? R? M? Dm-4-? L] pipera z? N-2-acetamide; N- [(4-ethoxy? Phen? L) met? L] -l-acet ? l-4- [2- (lH-? m? dazol-1-yl) -6- (iso-propyl) p? r? m? dm-4-? l] pipera z? n-2-carboxam? da; N- [2- (4-meth? lfenox?) ethyl] -l-acet? l-4- [2- (lH-imidazol-l-yl) -6-chlorop? pm? dm-4-? l] peraz? n-2-acetam? da;
N- [2- (3-Chloro-4-methoxyphenyl) ethyl] -1-acetyl-4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazin-2 - carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piper a zin-2 - acet amide; N- [(4-methoxyphenyl) methyl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazine-2-carboxamide; N - [(4-methoxyphenyl) methyl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazin-2-acetamide; N- [2- (3,4-dimethoxy phenyl) ethyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1 H-imidazol-1-yl) -6- (iso-propyl) ) pyrimidin-4-yl] piperazin-2-acetamide; N- [2- (3,4-dimethoxy phenyl) ethyl] -1- (3-met il-1-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidine- 4-yl] piperazine-2-carboxamide; N- [2- (3-Chloro-4-methoxyphenyl) ethyl] -l- [3-met il-1-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4 -yl] piper to zin-2 -carboxamide; N- [2- (3-Chloro-4-methoxyphenyl) ethyl] -1- (3-methyl-l-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4- il] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1H-imidazol-1-yl) pyrimin-4-yl] piperazine-2-carboxamide;
N- [(1,3-benzodioxol-6-yl) methyl] -1- (3-methyl-l-oxobutyl) -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4- il] piper a zin-2 -carboxamide; N- [2- (1, 3-benzodioxan-6-yl) ethyl] -l- (3-methyl-l-oxobutyl-4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4 -yl] piperazine-2-carboxamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1H-imidazole-1 il) -6-chloropyrimidin-4-yl] piperazin-2-carboxamide; N- [2 (1,4-benzodixol-5-yl) ethyl] -l- (3-methyl-l-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine-2-carboxamide; N- [2 (1,4-benzodixol-5-yl) ethyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1H-imidazol-1-yl) -6- (trifluoromethyl) pyrimidin-4-yl] piperazin-2-acetamide; N- [(2,6-dimethoxyphenyl) methyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1H-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine- 2-acetamide; N- [2- (3,4-dimethoxyphenyl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imide zol-1-yl) -6- (iso-propyl) pyrimidin-4-yl ] piperazin-2-acetamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] pipera zin -2-carboxamide;
N- [2- (1, 3-benz odi-oxol-5-yl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imide zol-1-yl) -6-chloropyrimidin-4- il] piperazin-2-acetamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6- (trifluoromethyl) pyrimidin-4-yl ] piperazin-2-acetamide; N- [(3,4-Dimethylphenyl) methyl] -1- (methoxyacetyl) -4- [6- (1H-imidazol-1-yl) -6- (trifluoromethyl) pyrimidin-4-yl] piperazin-2- carboxamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6- (iso-propyl) pyrimidin-4-yl) ] piperazin-2-acetamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6- (iso-propyl) pyrimidin-4-yl ] piperazine-2-carboxamide; N- [2- (1, 4-benzodioxan-6-yl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6- (trifluoromethyl) pyrimidin-4-yl ] piperazin-2-acetamide; N- [(4-methoxy phenyl) methyl] -1- (methoxyacetyl) -4- [2- (1H-imidazol-1-yl) -6-met-ilpyrimidin-4-yl] piperazin-2 -acet amide; N- [2- (3,4-dimethoxy phenyl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-1-yl) -6- chloropyrimidin-4-yl] piperazine-2-carboxamide;
N- [(4-methylphenyl) methyl] -l- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine-2 -acetamide; N- [2- (4-chlorophenyl) ethyl] -l - [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] piperazine -2-acetamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [(tetrahydrofuran-2-yl] carbonyl] -4- [2- (lH-imidazol-l-yl) -6-chloropyrimidin-4-yl ] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (1H-imidazol-1-yl) ) pyrimidin-4-yl] piperazine-2-carboxamide; N - [(1,3-benzodioxol-5-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [6- (1H -imidazol-1-yl) pyrimidin-4-yl] piperazine-2-carboxamide; N- [2 (1,3-benzodioxol-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] - 4- [2- (1H-imidazol-1-yl) -6-pyrimidin-4-yl] piperazine-2-acetamide; N- [2- (1,3-benzodioxol-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazine-2-acetamide; N- [2 (1,3-benzodioxol-5- il) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-l-yl) -6- (iso-propyl) pyrimidin-4-yl] piperazin-2- acetamide;
N- [2 (1,3-benzodioxol-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidine -4-yl] piperazine-2-carboxamide; N- [(1,4-benzodioxol-6-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (1H-imidazol-1-yl) -6- (iso -propyl) pyrimidin-4-yl] piperazin-2-acetamide; N- [(1,4-benz odi oxan-6-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-1-yl) -6- (Chloropyrimidin-4-yl] piperazin-2-acetamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- ( lH-imide zol-1-yl) -6-chloropyrimidin-4-ylpiperazin-2-carboxamide; N- [2- (1,4-benzodioxan-6-yl) ethyl] -1- [(tetrahydrofuran -2-yl) carbonyl] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl}. Piperazine-2-carboxamide; N- [(4-methoxyphenyl) methyl] - l- [(Tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-l-yl) -6-chloropyrimidin-4-yl] piperazin-2 -acetamide; N- [2- (4 -methoxy phenyl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imide zol-1-yl) -6-chloropyrimidin-4-yl] pipe ra zin- 2 - carboxamide; N- [2- (3-methoxy phenyl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-l-yl) -6-chloropyrimidin-4- il] piperazin-2 -carboxamide;
N- [(1,4-benzodioxan-2-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (1H-imidazol-1-yl) -6- (iso- propyl) pyrimidin-4-yl] piperazine-2-carboxamide; N- [(3,4-dimethoxy phenyl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (1H-imidazol-1-yl) -6- (iso-propyl) pyrimidine -4-yl] piperazin-2-acetamide; N- [(3,5-dimethoxy phenyl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazin-2-acetamide; N- [(4-Ethoxyphenyl) methyl] -l- [(2-hydroxy-2-oxoethoxy) acetyl] -4- [2- (IH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine -2-carboxamide; N- [(3-chloro-4-methoxyphenyl) methyl] -l- [(2-hydroxy-2-oxoethoxy) acetyl] -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4 -yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(2-hydroxy-2-oxoethoxy) acetyl] -4- [2- (IH-imidazol-1-yl) -6-methylpyrimidine -4-yl] piperazine-2-carboxamide; N- [2- (3,4-dimethoxy phenyl) ethyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazine-2-acetamide; N- [3- (3, 4-dimethoxyphenyl) propyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazin-2-acetamide; N - [(4-methylphenyl) methyl] -l- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acetamide;
N- [(1,3-benzodioxol-5-yl) methyl] -1- (phenoxyacetyl) -4- [2- (1 H -imidazol-1-yl) pyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- (phenoxyacetyl) -4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-acetamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazine-2-acetamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piperazine- 2-carboxamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- (f-enoxyacetyl) -4- [2- (lH-imide zol-1-yl) -6-chloropyrimidin-4-yl] pipera zin - 2 -acetamide; N- [2- (1,4-benzodioxan-5-yl) ethyl] -1- (f-enoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] piper to zin-2 -acet amide; N - [(4-methoxy phenyl) methyl] -1- (f-enoxyacetyl) -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-acetamide; N - [(4-methoxy phenyl) ethyl] -l- (phenoxyacetyl) -4- [2- (lH-imide zol-1-yl) -6-chloropyrimidin-4-yl] piperazine-2-carboxamide; N- [2- (4-methoxyphenyl) ethyl] -1- (f-enoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [2- (4-methoxy phenyl) ethyl] -1- (f-enoxyacetyl) -4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] pipe ra zin-2 -acet amide; N - [2 - (3,4-d imet ox ifenyl) ethyl] -1 - [(4-e-phenyl phenyl) carbonyl] -4- [2- (lH-imidazol-1-yl) -5-chloropyrimidine- 4-yl] piper a zin-2-acet amide;
N- [(1, 3-benzod? Oxol-5? L) met? L] -4- (6-fluorop? R? Dm-2-yl) -1- [2- (lH-? M? -1-? L) p? R? M? Dm-4-? L] pipe razm- 2 -acet amide; 1- (acetyl) -4- [2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [(4-methylsulfon? Lfen? l) I use] piperazin-2-acet amide; l- [2- (lH-? m? dazol-l-? l) p? r? m? dm-4-? l} -N- [(4-methersulfon? Lfen? L) met? L] pipe ridin-2-acet amide; N- [(1,3-benzod? Oxol -5 -? L) met? l] - 4 - [[2 - (etox? carbon? l) met? l] -l- [2- (lH-? m? dazol-l-? l) p? nm? d? n-4-íl ] p? peraz? n-2-acetam? da; 4- [ammo (idem) methyl] -N- [(1, 3-benzod? Oxol-5? L) methyl] -1- [2- (lH-? M? Dazol-1-? L) p? r? m? dm-4-? l] pipe reason-2 -acet amide; l-methersulfonyl-4- [6-met? l-2- (lH-? m? dazol-1-yl) p? r? m? dm-4-? l] -N- [2- (1,4-benzod? Oxan-6? L) ethyl] p? Peraz? N-2-acetamide; l-methylsulfonyl-4- [2- (lH-? m? dazol-1-? l) p? pm? d? n-4-? l} - N- { 2- (1, 4-benzod? Oxan-6-? L) ethyl] piperazm-2-acet amide; l-methylsulfonyl-4- [6-met? l-2- (lH-? m? dazol-1-? l) p? pm? d? n-4-? l] -N- [2 - (4-methox? Phen? L) et? L] peraz? N-2-acetamide; l-methersulfon? l-4- [6-? so-prop? l-2- (lH-? m? dazol-l-l) p? pm? dm-4-? l] -N- [( 3,4-dimethoxy-enyl] methyl] p? Peraz? N-2-acetamide; l- (n-oct? L) sulfon? L-4- [6-methyl 1-2- (lH-? M? Dazol- 1-?) P? R? M? Dm-4-? L] -N- [2- (3, 4-d? Methox? F enyl) et? L] p? Perazm-2-acetamide;
1- (n-octyl) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methyloxy) methyl) ] piperazin-2-acetamide; 1- (n-octyl) sulphonyl 4- [6- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin - 2 -acet amide; 1- (n-octyl) sulfonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2-acetamide; 1- (n-octyl) sulfonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (n-octyl) sulfonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-methoxyphenyl) methyl] piperazin-2- acetamide; 1- (n-octyl) sulfonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-fluorophenyl) sulfonyl] piperazine-2-acetamide; 1- (4-methylfenyl) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(pyridin-3-yl) methyl] piperazine- 2-carboxamide; 1- (4-methylfenyl) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperazin-2- carboxamide;
1- (4-methylphenyl) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazin-2- carboxamide; 1- (4-methoxyphenyl) sulfonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethyl] piperazine- 2-acetamide; 1- (4-methoxyphenyl) sulfonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazine-2-carboxamide; l- (4-methoxyphenyl) sulfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-6-yl) ethyl] piperazine- 2-carboxamide; 1- (4-methoxyphenyl) sulfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine- 2-acetamide; 1- (4-methoxyphenyl) sulfonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxy phenyl) methyl] piperazine-2 -acetamide; 1- (4-methoxyphenylsulfonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) sulfonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ) methyl] piperazine-2-carboxamide;
1- (4-methoxyphenyl) sulfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(2-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) sul foni 1-4- [6-met i 1-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazin-2-acet amide; 1- (4-methoxy phenyl) sul foni 1-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) sulphonyl 4- [6-methyl-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) sulphonyl 4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxy phenyl) methyl) ] pipera zin-2 -carboxamide; 1- (4-methoxy phenyl) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazine-2 -carboxamide; 1- (4-fluorophenyl) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2-acetamide; 1- (Fluorophenyl) sulfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2 -acetamide;
1- (dimethylamino) sulfonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] pipera zin-2 -acet amide; 1- (dimethylamino) sulfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-chloro-4-methyl-phenyl) ethyl] pipera zin-2 -acetamide; 1- (dimethylamino) sulfonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl) ] piperazin-2-acetamide; 1- (dimethylamino) sulfonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,3-benzodioxol-5-yl) methyl] piperazine-2-carboxamide; 1- (dimethylamino) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2-acetamide; 1- (dimethylamino) sulfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- (dimethylamino) sulfonyl-4- [6-trifluo romet il-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl) ] piper a zin-2 -acet amide; 1- (dimethylamino) sulfonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piper to zin-2 -acet amide;
1- (dimethylamino) sulfonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] pipe ra zin-2-acetamide; 1- (dimethylamino) sulfonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazine-2 -acetamide; 1- (dimethylamino) sulfonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyri my din-4-yl] - N - [(3,4-dimethoxy-enyl) methyl] pipe razin-2 -acet amide; 1- (n-propyl) aminocarbonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [2- (3,4-dimethoxy-enyl) ethyl ] piperazin-2-acetamide; 1- (n-propyl) aminocarbonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2 -carboxamide; 1- (n-propyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-chlorophenyl) ethyl] piperazin-2- carboxamide; 1- (n-propyl) ami noca rbonyl-4- [6-met il-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methyloxy) phenyl ) methyl] piperazin-2-acetamide; 1- (n-propyl) ami noca rbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-chloro-4-methyl) phenyl) ethyl] piperazine-2-carboxamide;
1- (n-propyl) aminocarbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazin-2-carboxamide; 1- (n-propyl) aminocarbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl) ] piperazine-2-carboxamide; 1- (n-propyl) ami noca rbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) I use] pipera zin-2-acetamide; 1- (n-propyl) ami noca rbonyl- 4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5- il) ethyl] pipera zin-2 -carboxamide; 1- (n-propyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2-acetamide; 1- (n-propyl) aminocarbonyl-4- [6- (IH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin - 2-carboxamide; 1- (n-propyl) aminocarbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piper to zin -2 -carboxamide; 1- (n-propyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl] piperazin-2- carboxamide;
1- (n-propyl) aminocarbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy-enyl) methyl] piperazine- 2-acetamide; 1- (cyclohexyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3,4-dimethoxy phenyl) ethyl] pipe -2-acetamide; 1- (cyclohexyl) aminocarbonyl-4- [6-met il-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N - [(4-ethoxy phenyl) methyl] piperazine-2-carboxamide; 1- (cyclohexyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-chloro-4-methyl-phenyl) ethyl] piperazine-2 -acetamide; 1- (cyclohexyl) ami noca rboni 1-4 - [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-chloro-4-methoxyphenyl) ethyl] piperazin-2-acetamide; 1- (cyclohexyl) ami noca rbonyl-4- [6-chloro-2- (1 H-imidazo 1 -1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- (cyclohexyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2- acetamide; 1- (cyclohexyl) aminocarbonyl-4- [6 (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2 carboxamide;
1- (cyclohexyl) aminocarbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] pipera zin-2 -carboxamide; 1- (cyclohexyl) aminocarbonyl-4- [6-met il-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] pipera zin-2-carboxamide; 1- (cyclohexyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] pipera zin - 2-carboxamide; 1- (cyclohexyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-acetamide; 1- (cyclohexyl) aminocarbonyl-4- [6-trifluoromet-il-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (cyclohexyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazine-2-carboxamide; 1- (cyclohexyl) aminocarbonyl-4- [6-met il-2- (1 H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] pipe ra zin-2-carboxamide; 1- (cyclohexyl) amino-ca rbonyl-4 - [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-2-yl) methyl] piper to zin-2-carboxamide;
1- (cyclohexyl) aminocarbon? L-4- [6-? So-prop? L-2- (1H-? M? D a z or l-1-? L) p? r? m? d? n - 4 -? l] - N - [(2,3-dimethoxy-enyl) -methyl] -2-carboxamide; 1- (cyclohexyl) am? Nocarbon? L-4- [6-chloro-2- (lH-imidazol-1-yl) p? Pm? D? N-4-? L] -N- [(2, 3 -d? methox? f enyl) met? l] p? perazm-2-carboxamide; 1- (phenylsulfonyl) am? Nocarbon? L-4- [6-chloro-2- (1H-? M? Da z or l-1-? L) p? r? m? d? n - 4 -? l] -N - [2 - (3,4-dimethoxyphenyl) ethyl] piper a z? n-2-acet amide; l- (p-sulfonyl) ammocarbon-l-4- [6-met? l-2- (lH-? m? dazol-1-? l) p? r? m? dm-4-? l] -N- [(4-etox? Phen? L) methyl] piper azm-2-acetam? Da; 1- (phenylsulfonyl) aminocarbon? L-4- [2- (lH-? M? Dazol-1-yl) p? R? M? Dm-4-? L] -N- [(4-ethoxy? fyl) methyl] piperazn-2-acetyl amide; 1- (phenylsulfonyl) am? Nocarbon? L-4- [6-chloro-2- (1H-? M? D a z or l-l-? L) p? r? m? d? n - 4 -? l] - N - [2 - (4-methylphonoxy) ethyl] piperazn-2-acetyl amide; 1- (phenylsulfonyl) am? Nocarbon? L-4- [6-chloro-2- (lH-imidazol-1-yl) p? R? M? Dm-4-? L] -N- [(4-met L-methyl) methyl] piperaz-2-acetamido; 1- (phenylsulfonyl) aminocarbon? L-4- [6-met 11-2- (1H-? M? Dazol-1-? L) p? R? M? D? N-4-? L] - N- [2- (3-chloro-4-methox? Phen? L) et? L] pipe razm- 2 -acet amide;
1- (phenylsulfonyl) aminocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] p iper to zin-2 -acet amide; 1- (phenylsulfonyl) aminocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazine- 2-carboxamide; 1- (phenylsulfonyl) aminocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin -2 -carboxamide; 1- (phenylsulfonyl) aminocarbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] pipera zin - 2 -acetamide; 1- (phenylsulfonyl) aminocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (phenylsulfonyl) aminoca rbonyl-4 - [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin- 2-acetamide; 1- (phenylsulfonyl) aminocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- (phenylsulfonyl) aminocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(2,5-dimethoxy phenyl) methyl] pipera zin-2 - acetamide;
1- [2- (thien-2-yl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazine-2-carboxamide; l- [2- (Thien-2-yl) ethyl] -4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol- 5-yl) methyl] piperazine-2-carboxamide; 1- [2- (thien-2-yl) ethyl] -4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4- benzodioxan-6-yl) methyl] piperazin-2-acetamide; l- [2- (Thien-2-yl) ethyl] -4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan- 6-yl) methyl] piperazine-2-carboxamide; l- [2- (Thien-2-yl) ethyl] -4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(2,3-dimethoxyphenyl) methyl] piperazin-2-acetamide; l- [2- (Thien-2-yl) ethyl] -4- [6-iso-propyl-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] piperazin-2-acetamide; 1- (4-methoxy phenyl) aminocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] piperazine-2-carboxamide; l- (4-methoxyphenyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (2,4-dimethoxyphenyl) ethyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) aminocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] ] piperazine-2-carboxamide;
1- (4-methoxy phenyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine -2-acetamide; 1- (4-methoxyphenyl) ami noca rbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] pipe -2-carboxamide; 1- (4-methoxyphenyl) aminocarbonyl-4- [6-chloro-2- (1H-im? Dazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piper to zin -2 -carboxamide; l- (4-methoxyphenyl) aminocarbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (4-methoxyphenyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-methoxyphenyl) methyl] piperazine-2-acetamide; 1- (3,4-dichlorophenyl) aminocarbonyl-4- [6-met i 1-2- (1H-imi zol-1-yl) pi rimi di n-4-yl] -N - [2 - ( 3, A-dimethoxyphenyl) ethyl] piperazine-2-acetamide; 1- (3,4-dichlorophenyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2-acetamide; 1- (3,4-dichlorophenyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] pipera zin-2-acetamide;
1- (3, 4-dichlorophenyl) ami noca rbonyl -4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-en-1) methyl] piperazin-2-carboxamide; 1- (3,4-dichlorofenyl) aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] piperazine-2-carboxamide; 1- (methoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3,4-dimethoxy phenyl) ethyl] piperazine- 2-acetamide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin-4-yl] -N- [2- (3,4-dimethoxy phenyl) ethyl] piperazine- 2-carboxamide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro- 4 -met oxy f-ethyl) methyl] piperazin-2-acetamide; 1- (methoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-chloro-4-methoxy phenyl) ethyl] piperazin-2-acetamide; 1- (methoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2-acetamide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2-acetamide;
1- (methoxy) carbonyl-4- [2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4-benzodioxan-6-yl) ethyl] piperazin 2-carboxamide; 1- (methoxy) carbonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piper a zin-2 -acet amide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazine-2-carboxamide; 1- (methoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(cyclopropyl) methyl] piperazine-2-carboxamide; 1- (iso-propoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2- carboxamide; 1- (iso-propoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] piperazine-2-carboxamide; 1- (iso-propoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxole-5 -i 1) me useful] piperazine-2-carboxamide; 1- (iso-propoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin- 2-acetamide;
1- (iso-propoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazine-2-carboxamide; 1- (Iso-propoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [[(3,4-dimethoxyphenyl) methyl] piperazine-2 -carboxamide; 1- (iso-propoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazine- 2-carboxamide; 1- (iso-propoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- (cyclopropyl) piperazine-2-acetamide; 1- (n-butoxy) carboni1-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazin-2- acetamide; 1- (n-butoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3-benzodioxol-5-yl) ethyl] piperazine- 2-acetamide; 1- (n-butoxy) carbonyl-4 [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl) ] piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide;
1- (n-butoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (n-butoxy) carbonyl -4- [6-methyl-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazin-2 -acetamide; 1- (n-butoxy) carbonyl-4- [β-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazin-2- carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-iso-propyl-2- (lH-i midazol-1-yl) pyri my din-4-yl] - N - [3 - (4 - dimethoxyphenyl) propyl] piperazine-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5-yl) ethyl] piperazin-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6) -yl) methyl] piperazin-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N - [(4-benzodioxan-6-yl) methyl] piperazine -2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-met i 1-2- (1 H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4- benzodioxan-6-yl) ethyl] piperazin-2-acetamide;
1- (2- (methoxy) ethoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [2- (4-methoxy-enyl) ethyl ] piperazin-2-acetamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimin-din-4-yl] -N- [2- (3-methoxyphenyl) ethyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2- acetamide; l- ((phenyl) methoxy) carbonyl-4 - [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ) methyl] piperazin-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; l- ((phenyl) methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazine-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-met il-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazine -2-acetamide;
1- ((phenyl) methoxy) carbonyl-4- [6-met il-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] piperazine -2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-iso-propyl-2- (1H-y my da zol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxylated) ) methyl] pipera zin-2 -acet amide; 1- (4-methoxyphenyl) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin -2-acetamide; 1- (4-methoxy phenyl) carbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole-5 -yl) ethyl] pipera zin-2-acetamide; 1- (4-methyl-phenyl) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole-5 -yl) ethyl] piperazine-2-carboxamide; 1- (4-methoxyphenyl) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin -2-acetamide; 1- (4-methoxy phenyl) carbonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N - [(4-benzodioxan-6-yl) methyl ] piperazine-2-carboxamide; 1- (4-methoxy phenyl) carbonyl-4- [6-met il-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine- 2-acetamide;
1- (4-methyl-phenyl) carbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) il) methyl] piperazine-2-carboxamide; l- (pyridin-3-yl) carbonyl-4- [6-met i 1-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethyl] piperazin-2-acetamide; l- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [(1,3-benzodioxol-5-yl) ) methyl] pipera zin-2-carboxamide; l- (pyridin-3-yl) carbonyl-4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2-acetamide; 1- (phenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- (phenoxy) carbonyl -4- [6-iso-propyl-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazin-2 -carboxamide; 1- (4-methoxyphenoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benz odi-oxol-5-yl) methyl] piperazine- 2-carboxamide; 1- (4-methoxy phenoxy) carbonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) useful] piperazine-2-carboxamide;
1- (4-methox? Pheno?) Carbon? L-4- [2- (lH-? M? Dazol-1-yl) p? R? M? Dm-4-? L] -N- [2- (1, 3-benzod? Oxol-5? L) ethyl] p? Perazm-2-acetarruda; 1- (4-methox? F enoxi) carbon? L-4- [6-chloro-2- (lH-? M? Dazol-1-yl) p? R? M? Dm-4-? L] -N - [2- (1, 3-benzod? Oxol-5? L) ethyl] p? Peraz? N-2-carboxamide; 1- (4-methox? Phenox?) Carbon? L-4- [6- (lH-? M? Dazol-1-yl) p? R? M? D? N-4-? L] -N- [ (1,4-benzod? Oxan-6-? L) methyl] piperaz? N-2-carboxamide; l- (4-methox? pheno?) carbon? l-4- [2- (lH-? m? dazol-l-l) p? r? m? dm-4-? l] -N- [2- (1,4-benzod? Oxan-6-? L) ethyl] piperaz? N-2 -carboxamide; 1- (4-methox? Pheno?) Carbon? L-4- [6-chloro-2- (lH-? M? Dazol-1-yl) p? Nm? D? N-4-? L] -N - [2- (4-methox? Phen? L) ethyl] p? Peraz? N-2-acetamide; 1- (4-methox? Pheno?) Carbon? L-4- [6-chloro-2- (lH-? M? Dazol-1-? L) p? R? M? D? N-4-? ] -N - [(2,4-d? Methox? Phen? L) met? L] p? Perazm-2-carboxamide; 1- (4-methox? Pheno?) Carbon? L-4- [6-met? L-2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? ] -N- [(3,4-d? Methox? Phen? L) met? L] p? Perazm-2-carboxamide; 1- ((phenol) methox?) Carbon? L-4- [6-? So-prop? L-2- (1H-? M? D a z or l-1-? L) p? r? m? d? n - 4 -? l] - N - [2 - (4-methylphonoxy) ethyl] p? perazm-2-carboxamide;
1- ((phenyl) methoxy) carbonyl -4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2 -carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin- 2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) methyl] piperazin-2-acetamide; l- ((phenyl) methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) me useful] piperazine-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-met i 1-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5 -yl) ethyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-met i 1-2- (lH-imidazol-1-yl] pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- (1-methylpropoxy) carbonyl-4- [5-chloro-2- (lH-imidazol-1-yl] pyrimidin-4-yl] -N- [(1, 3 - benzodioxol -5-yl) methyl] piperazin-2-acetamide; 1- (1-methylpropoxy) carbonyl-4- [6- (lH-imidazol-1-yl] pyrimidin-4-yl] -N- [(1 , 3-benz odi oxol-5-yl) methyl] piperazine-2-carboxamide;
1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl] pyrimidin-4-yl] -N-. {(1,4-benzodioxan-6-yl) methyl] pipe razin-2-acetamide; 1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl] pyrimidin-4-yl] -N- [(1, 4 -ben z odi oxan-6-yl) methyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6- (lH-imidazol-1-yl] pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [2- (lH-imidazol-1-yl] pyrimidin-4-yl] ] -N- [1- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol- 1-yl] pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-met il-2- (lH-imidazole -1-yl] pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazin-2-acetamide; 1- (phenoxy) -carbonyl-4- [6-iso-propyl-2 - (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2- (3,4-dimethoxy phenyl) ethyl] piperazin-2-acetamide; 1- (phenoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N-. { 2- (3, 4-dimethoxyphenyl) ethyl] piperazine-2-acetamide;
1- (phenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3,4-dimethoxyphenyl) ethyl] piperazin-2- acetamide; 1- (phenoxy) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,3-benzodioxol-5-yl) methyl] piperazine-2-carboxamide; 1- (phenoxy) carbonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(furan-2-yl) methyl] piperazin-2-acetamide; 1- (phenoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-carboxamide; 1- (phenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-carboxamide; 1- (phenoxy) carbonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2- carboxamide; 1- (pyridin-3-yl) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol- 5-yl) ethyl] piperazin-2-acetamide; 1- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; l- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-) il) ethyl] piperazin-2-acetamide;
1- (pyridin-3-yl) ca rboni 1-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl ] piperazine-2-carboxamide; l- [2- (4-methoxyphenyl) ethyl] -4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N-2- (3-chloro-4-methyl-phenyl) ethyl ] pipera zin-2 -carboxamide; 1- [2- (4-methoxy phenyl) ethyl] -4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol- 5-i 1) methyl] pipera zin-2-carboxamide; l- [2- (4-methoxyphenyl) ethyl] -4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol- 5-yl) methyl] piperazin-2-acetamide; 1- [2- (4-methoxy phenyl) ethyl] -4- [6-chloro- 2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benz odi) oxol-5-yl) useful] pipera zin-2-acetamide; 1- [2- (4-methoxyphenyl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine-2-carboxamide; 1- [2- (4-methoxy phenyl) ethyl] -4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan -6-yl) methyl] piperazin-2-acetamide; l- [2- (4-methoxyphenyl) ethyl] -4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) me useful ] pipera zin-2-carboxamide;
l- [2- (4-methoxy phenyl) ethyl] -4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- [2- (4-methoxy phenyl) ethyl] -4 - [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl ] piperazine-2-carboxamide; l- [2- (4-methoxyphenyl) ethyl] -4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] piperazin-2- carboxamide; 1- [(3,4-di-chloro-phenyl) -methyl] -carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) -pyrimidin-4-yl] -N- [2- (3 , 4-dimethoxy phenyl) ethyl] piper to zin-2-acet amide; 1- [(3,4-Dichlorophenyl) methyl] carbonyl-4- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methyl-enyl) -methyl] ] pipera zin-2-carboxamide; 1- [(3, 4- di chlorophenyl) methyl] carbonyl-4- [6-met il-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3-benzadioxol-5-yl) ethyl] piper a zin-2-acet amide; l - [(3,4-Dichlorophenyl) methyl] carbonyl-4- [6-chloro-2- (lH-imide zol-1-yl) pyr imi di n-4-yl] -N - [(3, 4 , 5-trimethoxy-f-enyl-) methyl] piperazine-2-carboxamide; 1- [(3,4-dichlorofenyl) met yl] carbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyr imi din-4-yl] - N - [(3, A -methyl phenyl) methyl] piper to zin-2-carboxamide;
l - [(1, 3-benzodioxol-5-yl) methyl] carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3 , 4-dimethy phenyl) ethyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3- (3,4-dime-to-phenyl) -propyl] -piperazine-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3- (3,4-dimethoxyphenyl) propyl] piperazine-2-acetamide; l - [(1, 3-Benzodioxol-5-yl) methyl] carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5) -yl) methyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-i-sopropyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5-yl) ethyl] piperazin-2-acet amide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5-yl] piper a zin-2-acet amide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6- (1 H -imidazol-1-yl) pyrimidin-4- il] -N- [2- (1, 3-benzodioxol-5-yl) ethyl] pipe razin-2 -carboxamide;
l- [(1, 3-Benzodioxol-5-yl) methyl] carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6) -Il) I piped zin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4 - methoxyphenyl) methyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4 -methoxypheneyl) methyl] piperazin-2-carboxamide; l- [(1, 3-Benzodioxol-5-yl) methyl] carbonyl-4- [6- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] ] pipera zin-2 -carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - (2-phenylcyclopropyl) ) piperazine-2-carboxamide; 1-methyl sulphonyl -4- [2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipe-razin-2 -carboxamide; N- [(3,4-dimethoxy-enyl) methyl] -1- [2- (1 H -imidazol-1-yl) pyrimidin-4-yl] pyrrole idin-2 -carboxamide; N- [(3,4-dimethoxy phenyl) methyl] -l- [2- (IH-imidazol-1-yl) pyrimidin-4-yl] pi r rol idin-2 -acet amide, • N- [(3 , 4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pi r rol i din-2 -acet amide; N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrole idin-2-acet amide;
N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidin-2-acetarruda; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] pyrrolidin-2-acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(3-chloro-4-methoxyphenyl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N - [(4-methoxy phenyl) ethyl] -1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(3,4-dihydroxyphenyl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N-octyl-1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- (phenoxypropyl) -1- [2- (1H-imidazol-1-yl) -6-methyl-pyrimidin-4-yl] pyrrolidine-2-carboxamide;
N - [(pyridin-3-yl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-y1] pyrrolidine-2-carboxamide; N- [(morpholin-4-yl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(2 (methoxypyridin-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidine-2-carboxamide; N- [(2 ( methylpyridin-5-yl) methyl] -1- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] piperidin-2-carboxamide; N- [(1,3-benzodioxol-5- il) ethyl] -2 - [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] acetamide; N - [(1,3-benzodioxol-5-yl) ethyl] ] -2 - [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2 - [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] acetamide; 2- [[- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] (methyl) ) amino] -N-octylacetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2 - [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] ( phenylmethyl) amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2 - [[2- (IH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2 - [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] [(l, 3 -benzodioxol-5-yl) methyl] amino] acetamide; N- [(3, 4-dimethoxyphenyl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino} acetamide;
N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] [(morpholin-4-yl) ethyl] ] amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] (methyl) amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methylethyl) amino] acetamide; N- [(1, 3-benzodioxol-5-oxy) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[4- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-2-yl] amino] acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2 - [[4- (lH-imidazol-1-yl) -6-methylpyrimidin-2-yl] amino] acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -3 - [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] propionamide; 4- [(4-trifluoromethylphenyl) methyl] -3- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] propionamide; N - [(1,3-benzodioxol-5-yl) ethyl] -3- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] propionamide; N- [(1,3-benzodioxol-5-oxy) ethyl] -2- (lH-imidazol-1-yl) pyrimidinopyrimidin-4-amine; N- [(1,3-benzodioxol-5-yl) ethyl] -4- [1- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -1- (2-methyl-l- oxopropyl) piperazin-2-acetamide;
N- [(4-methoxy phenyl) ethyl] -4- [2- (lH-imide zol-1-yl) -6-methylpyrimidin-4-yl) -6-methylpyrimidin-4-yl] -1- (2 -methyl-l-oxopropyl) piperidin-2-acetamide; N- [(4-nitrophenyl) methyl] -l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N- [[4- (acetylamino) phenyl] methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [[4- (Methylsul-fonyl-amino) -phenyl] -methyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N - [(2,3-dihydrobenzofuran-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N - [(indan-5-yl) methyl} -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-y1] piperidin-2-acetamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- (1-oxopropyl) piperazine-2-acetamide; N - [(4-methoxyphenyl) aminocarbonyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-methanamine; N- [(1,3-benzodioxol-5-yl) methylcarbonyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-methanamine; N- [(4-methoxyphenoxy) carbonyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl} piperidin-2-methanamine; N- [(4-methoxyphenyl) methylenedbonyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-methanamine;
N- [(1,3-benzodioxol-5-yl) carbonyl] -1- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] piper i din-2-et anamine; 2,4-bis (lH-imidazol-1-yl) -6-methylpyrimidine; N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -5-methylpyrimidin-4-yl] -4- (f -methylmethyl) piperazin- 3 -acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -6- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N-methyl-5,6,7,8-tetrahydropyrido [5, 6-c] pyrimidin-4-amine; 2- [[2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] amino] -N - [(1,3-benzodioxol-5-yl) methyl] -4-methylthiobutanamide; 2- [[2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-y1] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] -4-methylthiobutanamide; 2- [[2- (1 H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] amino] -N - [(4-methoxy phenyl) methyl] -4-methylsulfonylbutanamide; 2- [[2- (1 H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (butylthio) butanamide; 2- [[2- (1 H-imidazol-1-yl) -6-me t -pyrimidin-4-yl] amino] -N - [(cyclopropyl) methyl] -3 - [(3,4-dimethylphenyl) methylthio] ] propanamide; 2- [[2- (1 H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N - [(2,5-dimethoxyphenyl) ie] 3-me ti 1 -3- [(f-enylmethyl) thio] butanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(4-chlorophenyl) methyl] -3-thiofenpropanamide;
- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N - [(1,3-benzodioxol-5-yl) methyl] pentanamide; 5- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,4-benzodioxol-6-yl) ethyl] pentanamide; 7- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] amino] -N- [2-phenylcyclopropyl) heptanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] - [(3-chloro-4-methoxyphenyl) ethyl] acetamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] acetamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,4-benzodioxan-6-yl) ethyl] acetamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] amino] -N- [(4-methoxyphenyl) ethyl] acetamide; 4- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] butanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(4-chlorophenyl) ethyl] pyridine-3-propanamide; 2- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] isoquinoline-3-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] piperidin-2-acetamide;
l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] piperidin-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-y1] - N - [(4-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperidin-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- [(4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] thiomorpholin-2-acetamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] thiomorpholin-2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (iH-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] piperazine-2 -acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N - [(1,3-benzodioxol-5-yl) methyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- [(1,3-benzodioxol-5-yl) ethyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (IH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazine -2-acetamide;
4- [(dimethylethoxy) carbonyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] piperazine-2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4 -i 1] - N - [(3,4-dimethoxy phenyl) methyl] piperazine -2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] pyrimidine-3-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] pyrimidine-3-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] pyrimidine-3-carboxamide; 1- [2- (1H-imide zol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] pyrimido 3-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] pyrimidine-3-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chloro-4-methoxy phenyl) methyl] pyrimidin-3-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperidin-3-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] piperidin-3-acetamide;
l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperidin-3-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] piperidin-3-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidin-3-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] piperidin-3-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] piperidin-3-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperidin-3-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] pyrrolidine-2-carboxamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] pyrrolidine-2-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N - [(4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] -N- [(1,3-benzodioxol-5-yl) ethyl] acetamide;
1- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] -N - [(1,4-benzodioxan-6-yl) ethyl] acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4-methylpiperazin-2-acetamide; l- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] - N - [(4-chlorophenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) ethyl] -4-methylpiperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] -4-methylpiperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,5-dimethoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-methylpiperazin-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4-methylpiperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(2-methoxyphenyl) methyl] -4-methylpiperazine-2-carboxamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-4-yl] -N- [[4- (2-methoxyethoxy) phenyl) methyl] -4-methylpiperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(indal-5-yl) methyl] -4-methylpiperazin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-butylpiperazine-2-carboxamide; 1- [2- (1 H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; l [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide;
l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2- acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- [(4-methoxyphenyl) methyl] piperazine- 2-acetamide;
l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(4-methoxyphenyl) methyl] ] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(4-methoxyphenyl)] methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(4- methoxyphenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- [(4-methoxy phenyl) methyl] piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4 - [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazine- 2-acetamide;
1- [2- (lH-imidazol-1-yl) -6-trif luor ome thi-pyrimidin-4-yl] -N- [(2-f-enyl-cyclopropyl) -4- [(4-methoxy-enyl) -methyl]] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2 -acetamide; 1- [6-Chloro-2- (1H-imidazol-1-yl) -pyridin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(3,4-dichlorophenyl) methyl] piperazine -2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(3,4-di) chloro phenyl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4 - [(3,4-dichlorophenyl)] methyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-ben z odi oxan-6-yl) methyl] -4- [(3 , 4-di chloro or phenyl) ethyl] pipera zin-2 -acetamide; l- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(3, 4 - dichlorofenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benz odi oxan-6-yl) ethyl] -4 - [(3,4-dichlorophenyl) methyl] piperazin-2-acetamide;
1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- [(3,4-dichlorophenyl) methyl] piperazine -2-acetamide; l- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(1,3-benzodioxole -5- i 1) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzooxyol-5-yl) methyl] -4- [(1,3-benzodioxol-5 -yl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(1, 3- benzodioxol-5-yl) ethyl] piper a zin- 2 -acet amide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) ethyl] -4 - [(1,3-benzodioxol-5- il) methyl] pipera zin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(1, 3- benzodioxol-5-yl) methyl] piperazin-2 -acetamide; 1- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] - A - [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(1,3-benzodioxol-5- il) methyl] piperazin-2 -acetic acid; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- [(1,3-benzodioxol-5- il) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4 - [(1,3-benzodioxol -5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(1,4-benzodioxan-6 il) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-i1] -N- [(4-methylphenyl) methyl] -A- [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide;
l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(3,5-dimethoxy phenyl) methyl] -4- [(1,4-benzodioxan- 6-yl) ethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(1,4-benzodioxan -6-yl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] - A - [(1, 4- benzodioxan-6-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imide zol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(1,4-benzodioxan-6-yl) ) methyl] piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(1,4-benzodioxan-6-yl) methyl] pipe -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4 -i 1] -N- [(3-methoxyphenyl) ethyl] -4- [(1,4-benzodioxan-6-yl) ) methyl] piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2-thiophenyl) ethyl] -4- [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-acetamide; 1- [2- (1 H-imidazol-1-yl) -6-trif luor ome t ilpyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] -4- [(1, 4- benzodioxan-6-yl) methyl] piperazin-2-carboxamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1-adamantyl) methyl] -4- [(1,4-benzodioxan-6-yl) methyl] ] piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(5-indanyl) methyl] -4- [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) propyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide;
l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(pyridin-3-yl) ) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4 - [(pyridin-3- il) methyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(pyridin-3- il) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3-yl) ) methyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridine- 3-yl) methyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3- il) methyl] piperazin-2-acetamide; l- [2- (lH-im? dazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3-yl) ) methyl] piperazin-2-acetamide;
l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine -2 -acetamide; 1- [2- (1H-imide zol-1-yl) -6-me t -pyrimidin-4-yl] -N- [(4-me-to-phenyl) -methyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxy phenyl) methyl] -4- [(pyridin-3-yl) methyl] pipera zin-2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,6-dimethoxy phenyl) methyl] -4- [(pyridin-3- il) methyl] pipera zin-2-carboxamide; l- [2- (IH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- [(pyridin-3- il) methyl] pipe razin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(3-f luoro -4-methoxyphenyl) -methyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(3-f luoro -4-methoxyphenyl) -methyl] piperazin-2-acet amide;
1- [2- (1H-imidazol-1-yl) pyrimin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(3-fluoro-4-methoxyphenyl) ) -methyl] pipera zin-2 -acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(3-fluoro- 4-methoxyphenyl) -methyl] piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4-benzodioxan-6-yl) ethyl] -4- [(3-fluoro-4-methoxyphenyl) -methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- [(3-f luoro-4-methoxy phenyl) methyl] piperazine -2-acetamide; 1- [2- (lH-imide zol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- [(3-f luoro-4-methoxy phenyl) ) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- [(3-f luoro- 4 -me toxy phenyl) ) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(l-adamantyl) methyl] -4- [(3-f luoro-4-methoxy phenyl) methyl] pipera zin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- [(3-f luoro-4-methoxy-enyl) methyl] pipera zin-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-Imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4-acetylpiperazin-2-acetarruda; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(4-methylphenyl) methyl] -4-acetylpiperazine-2-acetarruda; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methylphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-1] - N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide;
l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(3,5-dimethoxyphenyl) ethyl] -4-acetylpiperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4-acetylpiperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4-acetylpiperazin-2- acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4,5-trimethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-acetylpiperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(4-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) ethyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-difluorophenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-phenylcyclopropyl) -4-acetylpiperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(indal-5-yl) methyl] -4-acetylpiperazin-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] - A - (3-methyl-1-oxobutyl) piperazine-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acculent; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (3-methyl-1-oxobutyl) ) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (3-methyl-l-oxobutyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (3-methyl-1-oxobutyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide;
l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (3-methyl-l-oxobutyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -A- (3-methyl) -1-oxobutyl) piperazine-2-carboxamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (3-methyl-1-oxobutyl) pipera zin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (3-methyl-1-oxo-butyl) pipera zin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (3-met i 1 -1-oxobutyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (3-methyl-l-oxobutyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (3-methyl-1 -oxobutyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide;
l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (3-methyl-1-oxo-butyl) -piperazin-2- acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(3-methoxyphenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (3-methyl-1-oxo-butyl) -piperazine-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [([4- (2-methoxyethoxy) phenyl) ethyl] -4- (3-methyl-1-oxobutyl) pipera zin-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-2-yl) ethyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-phenylcyclopropyl) ethyl] -A- (3-methyl-l-oxobutyl) piperazine-2-carboxamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxy phenyl) methyl] -4- (3-met il-1-oxobutyl) pipera zin-2-acetamide;
1- [2- (1 H-imidazol-1-yl) pyrimidin-4-yl] -N- [(indal-2-yl) ethyl] -A- (3-methyl-l-oxobutyl) piperazin-2- carboxamide; 1- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (indal-5-yl) ethyl] -4- (3-met il-1-oxobutyl) pipe razin-2 -ace ago; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (2-methoxy-l-oxoethyl) ) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazine -2-acetamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] -N- [(4-ethoxyphenyl) ethyl] -A- (2-methoxy-l-oxoethyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-1] - N - [(4-ethoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazin-2 acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (2-methoxy-l-oxoethyl) piperazin-2 -acetamide; 1- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(4-chlorophenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazine-2 -acculent; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazin-2- acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide;
l- [6-Chloro-2- (IH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-methoxy-1) -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-methoxy-l- oxoethyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-methoxy) -1-oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (2-methoxy-l-oxoethyl) piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy-1) -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy-l- oxoethyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy) -l-oxoethyl) piperazin-2-acetamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy-l-oxoethyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (2-methoxy-1) -oxoethyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (2-methoxy-1- oxoethyl) piperazin-2-acetamide; 1- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2-methoxy-l-oxoethyl) piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazin- 2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazine -2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- (2-methoxy-l-oxoethyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(indal-5-yl) methyl] -4- (2-methoxy-1-oxoethyl) piperazine -2-acetamide;
1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (tetrahydro-3-) furanoyl) pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) propyl] -4- (tetrahydro-3-furanoyl) pipera z in-2-acetamide; l- [2- (lH-imide zol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-ethoxy phenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) ethyl] -A- (tetrahydro-3-furanyl) piperazine-2 -acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methylphenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-y1] -N- [(4-methyl phenyl) methyl] -4- (tetrahydro-3-furanyl) piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methyl phenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (tetrahydro-3-furanyl) piperazine- 2-acetamide;
1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-met i lpyr imidin-4-yl] - N - [(4-chlorophenyl) methyl] - (4-tetrahydro-3-furanoyl) piperazin- 2 -acetamide; l- [2- (lH-imide zol-1-yl) -6-met-il-pyrimidin-4-yl] -N- [(4-chlorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2- acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-methoxy-3-chlorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazine- 2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (tetrahydro-3-furanoyl) ) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (tetrahydro-3-furanoyl) piperazine -2-acetamide;
l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-di methylphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) pir imidin-4-yl] -N- [(pyridin-3-yl) methyl] -4- (tetrahydro-3-furanoyl) pipera zin-2 -carboxamide; 1- [2- (1H-imide zol-1-yl) -6- (methyl ethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- ( tetrahydro-3-furanoyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (tetrahydro-3-furanoyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (tetrahydro-3-furanyl) piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-phenyl) -ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2- acetamide; 1- [2- (1 H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(3-methoxyphenyl) ethyl] -4-tetrahydro-3-furanoyl) piperazine-2-acetamide;
1- [2- (lH-imide zol-1-yl) pyr imidin-4 -i 1] - N - [(3,4-di fluorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl)? irimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,5-di methoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) butyl] -4- (2-carboxymethoxy-1-oxoethyl) piperazin-2-acetamide; l- [6-Chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (2-carboxymethoxy-1) -oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- (2-carboxymethoxy-l- oxoethyl) piperazin-2-acetamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-y1] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-carboxymethoxy-l-oxoethyl) ) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazine -2-acetamide;
l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-carboxymethoxy-l) -oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (2-carboxymethoxy-1) -oxoethyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazine-2- acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazine-2 -acetamide; l- [6- (lH-imi azol-l-yl) pyrimidin-4-yl] -N - [(2,4-dimethoxyphenyl) methyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazin-2- carboxamide;
1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(2,6-dimethoxyphenyl) methyl] - A - (2-carboxymethoxy-1-oxoethyl) ) piperazin-2-carboxamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,6-dimethoxyphenyl) methyl] -4- (2-carboxymethoxy-1-oxoethyl) piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, 4-dimethoxyphenyl) ethyl] -4- (2-phenoxy-1-oxoethyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) propyl] -4- (2-phenoxy-1-oxoethyl) pipera zin-2 -carboxamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-phenoxy-l) -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-phenoxy-l) -oxoethyl) piperazin-2-acetamide; 1- [2- (1 H-imidazol-1-yl) -6-trif luoromet-ilpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (2-phenoxy-1-oxoethyl) ) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met-il-pyrimidin-4-yl] -N- [(4-me-toxi-phenyl) -methyl] -4- (2-phenoxy-1-oxoethyl) pipera zin-2 -acet amide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxy phenyl) methyl] -4- (2-phenoxy-1-oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxy phenylethyl] -4- (pyridin-3-ylcarbonyl) pipera zin-2 -acetamide; l- [2 (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazin-2- acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) propyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) util] -4- (pyridin-3-ylcarbonyl) piperazin -2-acetamide; l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (pyridine-3 ilcarbonyl) piperazin-2-acetamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] -N- [(4-methyl phenoxy) ethyl] -4- (py idin-3-ylcarbonyl) piperazin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-met i lpyr imidin-4-yl] -N- [(4-met i 1 phenoxy) methyl] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) met il] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide;
l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (pyridin-3-ylcarbonyl) ) piperazin-2-acetamide; l- [2- (lH-imide zol-1-yl) -6-met i lpyr imidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (pyridin-3-) ilcarbonyl) pipera zin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(2,5-dimethoxy phenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazin-2 -carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (pyridin-3-ylca rbonyl ) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine- 2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (pyridin-3-ylcarbonyl ) piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(2,5-dimethylphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine- 2-carboxamide;
l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (pyridin-3-ylcarbonyl ) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (pyridine-3 -carbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met-ilpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine-2 -acetamide; l- [2- (1 H- imidazol-1-yl) -6-met i lpyr imidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -A- (pyridin-3-ylcarbonyl) piperazin-2 -acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-methoxyphenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (pyridin-3-ylcarbonyl) pipera zin- 2 -acet amide;
l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2-thienyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-carboxamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-di fluorophenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] -piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] - 4- (2- (4-methoxyphenyl) -1-oxoethyl] piperazine-2-carboxamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [( 4-methoxy-3-chlorophenyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] -piperazin-2-acetarruda; 1- [2- (lH-imidazol-1-yl) -6- methylpyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] -piperazin-2-acetamide; l- [2- ( lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-methoxy-3-chlorophenyl) methyl] -4- (2- (4-methoxyphenyl) -l-oxoethyl] piperazine-2-acetamide;
l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,5-dimethoxy phenyl) ethyl] -4- (2- (4-methoxy-phenyl) -1 -oxoethyl] piperazin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-trif luoromethylpi rimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) ethyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(3,4-dimethyl phenyl) methyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazole-1- il) pyrimidin-4-yl] -N - [(3,4-dimethyl-yl-enyl) methyl] -A- (2- (4-methoxy-phenyl) -1-oxo-ethyl] -piperazine-2-acetamide; 1- [ 2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethyl-phenyl) -ethyl] -4- (2- (4-methoxyphenyl) - 1-oxoethyl] -piperazin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-trif luoromet-ilpyrimidin-4-yl] -N- [(3-pyridinyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] piperazin-2-carboxamide; l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1 , 4-benzodioxan-6-yl) methyl] -4- (2- (4-methoxyphenyl) - 1 -oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1, 4-benzodioxan-6-yl) methyl] -4- (2- ( 4-methoxy phenyl) -1-oxoethyl] -piperazin-2-acet amide;
1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl ] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- ( 2- (4-methoxyphenyl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [( 3-methoxyphenyl) ethyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N- [(2-thienyl) ethyl] -4- (2- (4-methoxyphenyl) -l-oxoethyl] piperazine-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4- il] -N- [(l-methylpyrrol-2-yl) ethyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] piperazine-2-carboxamide; l- [6-chloro-2- ( lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxy phenyl) methyl] -4- (2- (4-methyl-phenyl) -1-oxoethyl] pipera zin -2-acetamide: 1- [2- (1H-imidazol-1-yl) -6-trif luoromet-ilpyrimidin-4-yl] -N- [(3,4-di-methoxyphenyl) methyl] -4- (2 - (4-methoxyphenyl) -l-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (2- (1,3-benzodioxol-5 -yl) -1-oxoethyl] piperazin-2-carboxamide;
l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (2- (1,3-benzodioxol- 5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piper to zin-2 -acet amide; 1- [6-chloro-2- (lH-imidazol-1-yl) - 6- (Methylethyl) pyrimidin-4-yl] -N- [(2-methoxy phenyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazine-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] - A - (2- (1,3-benzodioxol-5-yl) -1 -oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (2- (1, 3 -benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4 chlorophenyl) methyl] - A - (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl ) pyrimidin-4-yl] -N- [(4-chlorophenyl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [2 - (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (2- (1,3-benzodioxol-5- il) -1-oxoethyl] pipera zin-2-acet amide;
1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) ethyl] -4- (2- (1, 3 -benzodioxol-5-yl) -1-oxoethyl] piperazin-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3 -benzodioxol-5-yl) methyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazole -l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2- ( 1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4 -dimethylphenyl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) ) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] pipera zin- 2 -acetamide; 1- [2- (lH-imidazol-1-yl) pyrimin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (2- (1, 3-benz Hatexol-5-yl) -1-oxoethyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) ) -1-oxoethyl] piperazin-2-acetamide;
1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxy-enyl) -methyl] -4- [2- (1,3-benzodioxole-5 -yl) -1-oxoethyl] piperazin-2 -acetamide; 1- [2- (lH-imidazol-1-yl) -6-trif luoromet-ilpyrimidin-4-yl] -N- [(3-methyl-phenyl) -ethyl] -4- (2- (1,3-benzodioxol) -5-yl) -l-oxoethyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl ) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazine-2-acetamide; l- [2 - (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (2- (1,3-benzodioxol-5) -yl) -1-oxoethyl] piperazin-2 -aceta-1- (2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, 4 -di ethoxyphenyl) methyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6 -methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenylmethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [2 - (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(2-indanyl) met il] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide;
l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (2- (1,3-benzodioxol-5- il) -1-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N- [(4-methylphenyl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [ (4-chlorophenyl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4- methoxy-3-chlorophenyl) methyl] -4- (methylsul fonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [( 1,3-benzodioxol-5-yl) methyl] -4- (methylsulfonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1) , 3-benzodioxol-5-yl) methyl] -4- (methylsulfonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-6-yl) methyl] -4- (methylsu) lfonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-6-yl) ethyl] -4- (methylsulfonyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-6-yl) ethyl] -4- (methylsulfonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (methylsulfonyl) piperazine-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazin-2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (methylsulfonyl) piperazine-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-methoxyphenyl) ethyl] -4- (methylsulfonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (methylsulfonyl) piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (methylsulfonyl) piperazin-2- acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (octylsulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- (octyl sulphonyl) piperazine- 2-acetamide;
l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) ethyl] -4- (octyl sul phonyl) pipera zin -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4- (octylsulfonyl) piperazine -2-acetamide; l- [2- (IH-imidazol-1-yl) -5-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (octylsulfonyl) piperazin-2- acetamide; 1- [2- (IH-imidazol-1-yl) pyrimin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (octylsulfonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4- (octylsulfonyl) piperazin-2 -acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (octylsulfonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (octylsulfonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (octylsulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] -4- (octylsulfonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] - A - (dimethylaminosul fonyl) piperazine-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-trifluoromethylpyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (dimethylaminosulfonyl) piperazin-2- acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (dimethylaminosulfonyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazin-2 -acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazine-2- acetamide;
l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4- (dimethylaminosulfonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] - A - (dimethylaminosulfonyl) piperazin-2 acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (dimethylaminosulfonyl) piperazine -2-carboxamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- (dimethylaminosulfonyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (dimethylaminosul fonyl) pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (dimethylaminosul fonyl) pipera zin-2-acetamide;
1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (dimethylaminosulfonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-2-yl) methyl] -4- (dimethylaminosulfonyl) piperazine-2 -carboxamide; l- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(2,3-di methoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-di methoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (dimethylaminosulfonyl) piperazin- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3,5-dimethoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N - [(2-adamantyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-carboxamide;
l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2,3-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (propylaminocarbonyl) pipera zin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(3,4-dimethoxy phenyl) ethyl] -4- (propylaminocarbonyl) pipera zin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-di methoxyphenyl) propyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3, 4-di methoxyphenyl) butyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxy-phenyl) -methyl] -4- (propylaminocarbonyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -A- (propylaminocarbonyl) p i pera z-2-acet amide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-methylphenoxy) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-1-yl] - N - [(4-methylphenoxy) ethyl] -4- (propylaminocarbonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-y1] - N - [(4-chlorophenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide;
1- [2- (1H-imide zol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(3-cl-4-methyl-to-phenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- (propylaminocarbonyl) -piperazin-2 -acetamide; l- [2- (lH-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(3-chloro-4-methyl-phenyl) ethyl] -4- (propylaminocarbonyl) piperazine -2-acetamide; 1- [6-chloro-2- (1 H-imidazol-1-yl) pyrimidin-4-y1] -N- [(3-cl-oro-4-methyl-phenyl) -ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imide zol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-me toxy phenyl) ethyl] -A- (propylaminocarbonyl) pipera zin-2 -acet amide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imide zol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (propylaminocarbonyl) piperazin-2- acetamide;
1- [(2- (1H-imide zol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4 - (propylaminocarbonyl ) pipe razin-2 -acet amide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (propylaminocarbonyl) piperazine-2- acetamide; 1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [. (1,3-benzodioxol-5-yl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imide zol-1-yl) pyrimin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (propylaminocarbonyl) piperazine-2-carboxamide; l- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethylphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) piperazine -2-acetamide;
l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) piperazin-2 acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) piperazine-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (propylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (propylaminocarbonyl) piperazin-2- acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) piperazine -2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl-4- (propylaminocarbonyl) piperazine-2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -A- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(2-methoxyphenyl) ethyl] - A - (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(2-thienyl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-thienyl) ethyl] -4- [propylaminocarbonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-difluorophenyl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide;
1- [6-chloro-2- (1H-imidazol-1-yl) -pyridin-4-yl-N- [(1,4-benzodioxan-2-yl) methyl] -4- (propylaminocarbonyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] -4- (propylaminocarbonyl) piperazin-2 acetamide; 1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-y1] -N - [(1,4-benzodioxan-2-yl) methyl] -4-propylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(2,5-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxy phenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4 (propylaminocarbonyl) piperazine-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3,4-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imide zol-1-yl) -6-met ilpyr imidin-4-yl] -N- [3,4-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,5-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,5-dimethoxy phenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-4-yl] -N- (cyclopropyl) -4- (propylaminocarbonyl) piperazin-2 -acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- (2-indanyl) -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(5-indanyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imide zol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-Imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- (cyclohexylaminocarbonyl) pi? Erazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazin-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(4-chlorophenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-Imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide;
l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (cydohexylaminocarbonyl) piperazine-2 -acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2- acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] - A - (cyclohexylaminocarbonyl) pipera zin-2 -acet amide; l- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (cyclohexylaminocarbonyl) pipera zin - 2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -A- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) ethyl] - A - (cyclohexylaminocarbonyl) piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(2-methoxyphenyl) ethyl] - A - (cyclohexylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-difluorophenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2,5-dimethoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (cydohexylaminocarbonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl-4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- (2-indanyl) -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4- (phenylsulfonylaminocarbonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (phenylsulfonylaminecarbonyl) piperazine-2 -acetamide;
l- [5-Chloro-2 (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (phenylsulfonylaminocarbonyl) piperazine-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4- (phenylsulfonylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-4-yl] - N - [(2,3-di-metoxyphenyl) methyl] - A - (phenylaminocarbonyl) piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) propyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(4-methylphenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(4-chlorophenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; l ~ [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) ethyl] -4- (phenylaminocarbonyl) piperazine-2-carboxamide; l- [6-Chloro-2- (lH-imidazolo-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-4-yl] -N - [(3-chloro-4-methoxy-phenyl-1-yl) -yl] -4- (phenylaminocarbonyl) piperazine-2 -carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) ethyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (phenylaminocarbonyl) piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl)? irimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (phenylaminocarbonyl) pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (phenylaminocarbonyl) piperazin-2- acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (phenylaminocarbonyl) piperazine-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (phenylaminocarbonyl) pipera zin-2 -acet amide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] -N- [(3-methoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2 -acet amide; l- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (phenylaminocarbonyl) pipe razin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (phenylaminocarbonyl) piperazin-2-acet amide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (phenylaminocarbonyl) piperazin-2-acet amide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl-N- [(3-thienyl) ethyl] -4- (phenylaminocarbonyl) piper a zin-2-acet amide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-difluorophenyl) methyl] -A- (phenylaminocarbonyl) piperazin-2-acetamide;
l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazolo-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin- -i 1] - N - [(3,4-dimethoxy phenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2 -acetamide; l- [6- (1H-imdidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-carboxamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (phenylaminocarbonyl) piper a zin-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimido-4-yl] -N- [(2,3-dimethoxy phenyl) ethyl] -4- [(4-methoxy phenyl) aminocarbonyl] pipera zin -2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,3-dimethoxyphenyl) ethyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine-2-carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine- 2-acetamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] - N - [(4-methoxyphenoxy) ethyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2- carboxamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] - A - [(4-methoxyphenyl) aminocarbonyl] piperazine -2-acetamide;
1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4 - [(4-methoxy-phenyl) aminocarbonyl] piperazin-2-acet amide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) ethyl-4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2,5-dimethoxyphenyl) ethyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-carboxamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] - 4 - [(4 -methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4 - [(4-methoxyphenyl) aminocarboni lpiper to zin-2-carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(1,3-benzodioxol-5-yl) ethyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine-2 -acetamide;
l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazin-2 -acetic acid; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(3,4-dimethyl-yl-enyl) methyl] -4- [(4-methoxy-phenyl) -aminocarbonyl]] piperazin-2-acetamide; l-6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethylphenyl) methyl] -4- [(4-methoxy phenyl) aminocarbonyl] piper a zin-2 - acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2-furyl) methyl] -4- [(4-methoxy phenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (4-methoxyphenyl) aminocarbonyl] pipe razin-2 -acetamide;
1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] - A - [(4-methoxyphenyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4 - [(4-methoxyphenyl) aminocarbonyl] pipera zin -2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2- acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) ethyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1, 4-benzodioxan-2-yl) ethyl] -4 - [(4 - methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [5-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,3-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine- 2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(2,5-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (2-indanyl) -4- [(4-methoxyphenyl) aminocarbonyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(5-indanyl) methyl] -4- [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide;
l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) propyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) butyl] - A - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) ethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- [(3,4-dichlorophenyl) aminocarbonyl] piperazine-2 -acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazine- 2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-i1] -N - [(4-methylphenyl) methyl] -4- [(3,4-dichlorophenyl) aminocarbonyl] piperazine-2 -acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4 - [(3, -dichlorophenyl) aminocarbonyl] piperazin-2 -acetamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -A- [(3,4-dicyclophenyl) aminocarbonyl] piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- [(3,4-dichlorophenyl) aminocarbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) methyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazine- 2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -A - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-y1] -N- [(1,3-benzodioxol-5-yl) methyl] -4 - [(3, A-dichlorophenyl) aminocarbonyl] piper to zin-2-acet amide; l- [2- (lH-imidazol-l-yl) -6-met ilpyr imidin-4-l-N- [(1,3-benzodioxol-5-yl) methyl] -4 - [(3, 4 - dichlorophenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4 - [(3, A -dichlorophenyl) aminocarbonyl] pipera zin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4 - [(3, 4 - dichlorophenyl) aminocarbonyl] piperazine-2-acetamide;
l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acet amide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl-N- [(3,4-dimethylphenyl) methyl] -A - [(3,4-dichlorophenyl) aminocarbonyl] pipe ra zin- 2 -ace tarruda; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] pipera zin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] - A - [(3, 4 - dichlorophenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4 - [(3, A - dichlorophenyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(3,4-dichlorophenyl) aminocarbonyl] piperazine-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(3,4-dichlorophenyl) aminocarbonyl] piperazine- 2-acetamide;
1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- [(3,4-dichlorophenyl) aminocarbonyl] piperazine-2 -acetamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(2,5-dimethoxyphenyl) methyl] - A - (3,4-dichlorophenyl) aminocarbonyl ] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -A - [(3,4-dichlorophenyl) aminocarbonyl] pipera zin-2-acetarruda; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -A - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] - A - [(3, A-dichlorophenyl) aminocarbonyl] piper a zin- 2 -acet amide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] -A- (methoxycarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (methoxycarbonyl) piperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetarruda; l- [6-chloro-2- (IH-imidazol-1-yl) pyrimidin-4-yl-N- [(3-chloro-4-methoxy phenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methyl-pyrimidin-4-yl-N- [(3-chloro-4-methoxy phenyl) ethyl] -A- (methoxycarbonyl) piperazine-2- acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (methoxycarbonyl) pipera zin- 2 -ace ago; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N [(1,3-benzodioxol-5-yl) ethyl] -4- (methoxycarbonyl) piper a zin- 2- acetylamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl-4- (methoxycarbonyl) piperazine-2- acetamide; 1- [2- (1 H-imidazol-1-yl) pi r imidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (methoxycarbonyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (methoxycarbonyl) piperazine-2 -acetamide;
l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methoxycarbonyl) piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (methoxycarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (methoxycarbonyl) piperazine-2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] -4- (methoxycarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(3,4-dimethoxy phenyl) methyl] -4 - (methoxycarbonyl) piperazin-2 acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (meth i letoxy carboni l ) piperazin-2-acetamide;
l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] -4- (methylethoxycarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (butoxycarbonyl) pipera zin-2 -acetamide; l- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl-N- [(1,4-benzodioxan-6-yl) methyl] -4- (butoxycarbonyl) piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6-me-t-ylpyr-imidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (butoxycarbonyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (butoxycarbonyl) piperazin-2-acet amide; 1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-difluorophenyl) methyl] -4- (butoxycarbonyl) pipera zin-2 -carboxamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazin-2- acetamide; 1- [2- (1H-imide zol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methyl-phenyl) -methyl] -4- [(2-methoxyethoxy ) carbonyl] piper to zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4 - [(2 - methoxyethoxy) carbonyl] pipe razin-2-acet amide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(2-methoxyethoxy) carbonyl] ] piperazin-2-acetamide;
1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(2-methoxyethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(2-methoxyethoxy) carbonyl] ] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -5-methylpyrimidin-4-yl-N- (1,4-benzodioxan-6-yl) ethyl] -4- (2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] -4 - [(2-methoxyethoxy) carbonyl] piperazine-2 -acetamide;
1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(phenylmethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imi azol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- [(phenylmethoxy) carbonyl] piperazine-2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(phenylmethoxy) carbonyl] piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] - A - [(phenylmethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(phenylmethoxy) carbonyl] piperazine -2-acetamide;
1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-i 1] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(phenylmethoxy) carbonylpiperazine -2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(phenylmethoxy) ca rbonyl] piperazine-2 -carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(phenylmethoxy) carbonyl] piperazine-2-acetamide; l- [6-Chloro-2- (2 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N - [(4-methoxy phenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- [(phenylmethoxy) carbonyl] piper a zin-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-di-methoxyphenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine-2- acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pir imidin-4-yl-N - [(3,4-di methoxyphenyl) ethyl] -4- [(phenylme toxy) carbonyl] piperazin -2-acetamide;
l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-di methoxyphenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine -2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4- [(1-methylpropoxy) carbonyl] pipera zin -2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) etii] -4- [(1-methylpropoxy) carbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-i 1] -N- [(4-methoxyphenyl) methyl-4- [(1-methylpropoxy) carbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4 - [(4-methoxy phenoxy) ) carbonyl] pipera zin-2 -carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, 4, 5-trimethoxyphenyl) methyl] -4 - [(4-methyl) phenoxy) carbonyl] ipera zin-2 -acet amide; 1- [2- (1 H-imidazol-1-yl) -6-trif luo romet i lp ir imi din-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(4-methoxyphenoxy) carbonyl] piperazine-2-carboxamide;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(4-methoxyphenoxy) carbonyl] ] piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- [(-methoxy phenoxy) carbonyl] piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1-methylpyrrol-2-yl) ethyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine -2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] -4 - [(4-methoxyphenoxy) carbonyl] piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,6-dimethoxyphenyl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine- 2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine-2 -carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylethylpyrimidin-4-yl-N- [1- (phenylimethyl) piperidin-4-yl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-cyanocyclohexyl) piperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- (2, 2-dimethoxyethyl) piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N-tridecylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-hydroxy-4-methylthiobutyl) piperidin-2-acetard; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N, N- [bis (2-cyanoethyl)] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N, N- [bis (2-cyanomethyl)] piperidin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N - [(4,4-diethoxybutyl) piperidin-2-acetamide; l- (4-fluorophenyl) -4- [l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] piperazine; l- [(1, 3-Benzodioxol-5-yl) methyl] -4- [l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] piperazine; 1- (phenylmethyl) -4- [1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -piperidin-2-acetyl] piperazine; 4- [1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] piperazine-1-carboxylic acid ethyl ester,
1- (4-chlorophenyl) -4- [1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] -4-hydroxypiperidine; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(2,3-dihydrobenzofuran-5-yl) methyl) piperidin-2-acetamide;
1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? L] -N- [(mdan-5-? L) methyl) piper? dm-2 -acerate; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? D? N-4-? L] -N- [(cyclohexyl) methyl] pipe ndm- 2 - ace tarruda; 1- [2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [(1,2,3,4-tetrah? Dronaftalen-1- ? l) piper? d? n-2 -acetarr; l- [2- (lH-? m? dazol-l-? l) p? pm? dm-4-? l] -N- [(aftalen-1-yl) methyl) pipe pdm- 2 -aceterate; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? Dm-4-? L] -N- [(1,3-benzod? Oxol -5-? L) methyl] p? Per? Dm-2-acetam? Da; 1- [(2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? Pm? D? N-4-? L] -N- [(4-chlorophen? L) methyl] pipe pdin-2 -acet amide; l- [2- (lH-? m? dazol-1-? l) -6-met? let? lp? r? m? dm-4-? l] -N - (2-et? Lhex? L) pipe pdm- 2 -ace taarruda; l- [2- (lH-? M? Dazol-l-? L) p? R? M? D? N-4-? ] -N- (2-ethylhexyl) pipe ridm- 2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? Dm-4-? ] -N- (2-ethylhexyl) p ipe r? Dm-2-acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M ? dm-4-? l] -N- [2- (morpholm-4-? l) et? l] p? per? d? n-2-acetam? da; 1- [2- (lH-? m ? dazol-1-? l) -6-met? lp? r? m? dm-4-? l] -N- (1-methylhexyl) piper? dm-2-acet amide; 1- [2- (lH -? m? dazol-1- l) -6-met? let? lp? pm? d? n-4-? l] -N- (1-met? lhex? l) p? per? dm-2- acetam? da;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (l-methylhexyl) piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] - N - [(4-methoxyphenyl) methyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (cyclooctyl) piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-ethyl-3-hydroxy-l-hydroxyethylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [3- (morpholin-4-yl) propyl] piperidin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (1-methyl-3-phenylpropyl) piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-y1] -N- (1-methyl-3-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-methyl-3-phenylpropyl) piperidin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (1-methylheptyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-methylheptyl) piperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-methylheptyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-fluorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-fluorophenyl) methyl] piperidin-2-acetarr; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-y1] - N - [(4-methylphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (l-phenylethyl) piperidin-2-acetamide; 1- [2- (1H-imide zol-1-yl) -6-methylpyrimidin-4-yl] -N-phenylimethyl-piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N - [(3,4-dichlorophenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (2-phenylethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- (2-phenylethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [3- (pyrrolidon-1-yl) propyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1, 5-dimethylhexyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1,5-dimethylhexyl) piperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (1,5-dimethylhexyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N- [(2-fluorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2-fluorophenyl) methyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] piperidin-2-acetarruda; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (2-chlorophenyl) ethyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-y1] -N- [(furan-2-yl) methyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- [(furan-2-yl) methyl] piperidin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(furan-2-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(pyridin-2-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(pyridin-2-yl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-y1] -N- [(pyridin-2-yl) methyl] piperidin-2-acetamide;
1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-trifluoromethylphenyl) methyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-trifluoromethylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- (2-phenylpropyl) piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- (2-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (2-methoxyphenyl) ethyl] piperidine-2-acetarruda; l- [2- (lH-imidazol-1-yl) -pyrimidin-4-yl-N- [2- (2-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-y1] -N- (2-hydroxy-4-methylthiobutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (2-hydroxy-4-methylthiobutyl) piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(2,4-dichlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(3-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N - [(3-methylphenyl) methyl] piperidin-2-acetamide;
1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (3-methoxyphenyl) ethyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) pi r imidin-4-i 1] -N- [2- (3-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; l- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- [2- (3, 4-dimethoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3,4-dimethoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (phenylbutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -pyrimidin-4-yl] -N- (phenylbutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-hydroxymethylpentyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- (1-hydroxymethylpentyl) piperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] - N - [(3,5-dimethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,5-dimethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (4-ethoxyphenyl) ethyl] piperidin-2-acetarruda; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-ethoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-ethoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-ethoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (4-bromophenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-bromophenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-bromophenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-brornophenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N-pentylpiperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N-pentylpipe-ridin-2-acetyl amide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N-pentylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [3- (1H-imidazol-1-yl) propyl] pipe-ridin-2-acet amide; 1- [2- (1 H-imidazol-1-yl) -6-met ilp ir imi din-4 -yl] -N- [3- (1 H-imidazol-1-yl) propyl] pipe ridin-2 -ace tarruda; 1- [2- (1H-imide zol-1-yl) -6-met ilpyr imidin-4-yl] -N - [(3-chlorophenyl) methyl] pipe ridin-2 -acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-phenyl) -methyl] -pipe-ridin-2-acetic acid; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(2,4-di chloro phenyl) methyl] piper i din-2-a-cet amide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2,4-dichlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [2- (1-phenyl) ethyl] piper idin-2 -aceta-free; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [1- (phenyl) ethyl] piper i din-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-fluoro-phenyl) -ethyl] -pyridin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- [2- (3-ethoxy-4-methyl-phenyl) ethyl] pipe-ridin-2-acetic acid;
l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (3-ethoxy-4-methoxyphenyl) ethyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-ethoxy-4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-ethoxy-4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-chlorophenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl-N- [2- (4-chlorophenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (5-hydroxypentyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N-butylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-fluorophenyl) (methyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-fluorophenyl) (methyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (2, 5-dimethoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (2, 5-dimethoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (2,5-dimethoxyphenyl) ethyl] pyrrolidine-2-carboxamide;
1- [2- (1H-imidazol-1-yl) -6-met i le t ilpir imidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxy phenyl) ethyl] pipe ridin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6 -methyl-1-yl-imidin-4-yl] -N- [2- (4-methyl-phenyl) -ethyl] piper-idin-2-acetyl-amide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-me-toxi-phenyl) -ethyl] -piper idin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) -6-met-il-pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] pipe-ridin-2 -acetic acid; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1 H-imidazol-1-yl) -6-met-ile-i-pyrimidin-4-yl-N- [3- (methylethoxy) propyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N-hexylpiperidin-2-acetamide; 1- [2- (lH-imi.dazol-1-yl) pyrimidin-4-yl] -N-hexy lp ipe ridin -2 -acet amide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl-N-hexylpiperidin-2-acetamide;
1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (cyclohexen-1-yl) ethyl] pipe ridin-2 -acet amide; l- [2- (lH-imidazol-l-yl) -6-met ilpyr imidin-4 -i 1] -N- [2- (cyclohexen-1-yl) ethyl] pipe ridin-2 -acetic acid; l- [2- (1H-imide zol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-fluoro-5-trifluoromethylphenyl) methyl] pipe ridin-2 -acet amide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-fluoro-5-trifluoromethylphenyl) methyl] piper idin-2 -ace tarea; l- [2- (lH-imidazol-l-yl) -pyrimidin-4-yl] -N- [2- (4-methylphenyl) ethyl] pipe ridin-2-acet amide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N- [2- (4-methylphenyl) ethyl] piper idin-2 -acertrug; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (3-ethoxypropyl) pipe ridin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- (3-ethoxypropyl) piperidin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N-hept i lp ipe ridin -2 -acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N-heptylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilp-ir imi-din-4-yl] -N-heptyl-piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyr imidin-4-yl] -N- (3-methoxypropyl) pipe ridin-2 -acet amide;
1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-cyclohexylethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- (1-cyclohexylethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] - N - [(4-trifluoromethoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-trifluoromethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-fluorophenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-fluorophenyl) ethyl] piperidin-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (3-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (3-phenylpropyl) piperidin-2-acetamide;
1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Nm? D? N-4-? L] -N- (3-phenylpropyl) piper idm-2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? Pm? D? N-4-? L-N-octylpiperidm-2 -acetarrue; l- [2- (lH-? m? dazol-l-? l) -6-met? lp? r? m? d? n-4-? l-N-octylpiperidin-2-acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? D? N-4-? L] -N- (1-h? Drox? -3-met ? lbut? l) pipe ridm- 2 -ace tarruda; 1- [2- (lH-? M? Dazol-1-? L) - 6-met? Let? Lp? R? M? Dm-4-? L] -N- [1- (4-met? Lfen (l) ethyl] p ipe n din-2 -ace tartar; l- [2- (lH-? m? dazol-l-? l) p? r? m? dm-4-? l] -N- [l- (4-methylphenyl) ethyl] p ipe ridm- 2 - ace tarruda; l- [2- (lH-? m? dazol-1-? l) -6-met? lp? r? m? d? n-4-lyl] -N- [1- (4-met? lfen? l) et? l] pipe pdm-2 -acetarrue; l- [2- (lH-? m? dazol-1-? l) -6-met? lp? pm? dm-4-? l] -N- [4, 4-diethoxybutyl) pipe r idm- 2 - acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? Dm-4-? L] -N- [(4-tpf luoromet phenyl) til] piper din-2 -acet amide; l- [2- (lH-? m? dazol-l-? l) -p? r? m? dm-4-? l] -N- [(4-trif luoromet phenyl) useful] pipen din-2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? LN- [(4-tpf luoromet-phenyl) methyl] piper? Dm- 2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? D? N-4-? LN- (3-butoxypropyl) p? Pepdm-2 -acetam? da;
- 3U - l- [2- (lH-? M? Dazol-1-? L) - 6-met? Lp? Pm? Dm-4-? L] -N- (3-butoxypropyl) pipe ridm- 2 - ace tarruda; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? D? N-4-? L] -N- [2- (t? Ofen -2-? L) et? L] pipen din- 2 -ace tarruda; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? D? N-4-? L] -N- [2- (t? Ofen-2-? l) et? l] pipen din-2-a-cet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? Pm? Dm-4-? L] -N- [3- (p? Rrol? D? Nl -? l) prop? l] pipe pdm-2-acet amide; 1- [2- (lH-? M? Dazol-1-? X - 6-met? Let? Lp? R? M? Dm-4-? L] -N- [(cyclohexyl) methyl] p? Per? d-n-2-acetamido; 1- [2- (lH-? m? dazol-1-? l) p? pm? d? n-4-? l] -N- [(cyclohexyl) methyl] pipen din-2-d ce tarruda; ethyl ester of 4- [[1- (2- (lH-? m? dazol-1-? l) pinmidm-4-? l] p? per? d? n-2 -acet? l] ammo] pipen di n-1-carboxyl? co; ethyl ester of the acid 4- [[1- [2- (lH-? m? dazol-1-? l) -6-met? let? lp? r? m? dm-4-? l] p? per? d? n-2-acet? l] amino] pipen di nl-carboxylic acid ethyl ester 4- [[1- (2- (lH -? m? dazol-1-? l) -6-met? lp? r? m? d? n-4-? l] p? per? d? n-2-acet? l] am? no] p ? pepd? nl-carboxylic acid; 1- [2- (lH-? m? dazol-1-? l) -6-met? lp? pm? d? n-4-? l] -N- [(4- fluorofen? l) met? l] pipe r? d? n-2-acet amide; N - [(1, 3-benzod? oxol-5? l) met? l] -l- [3- (lH- m? dazol-1-yl) phenyl] pi-pi-di-n-2-acet amide;
N- [(1,3-benzodioxol-5-yl) methyl] -1- [3-chloro-5- (1H-imidazol-1-yl) triazin-1-yl] piperidin-2-acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) purin-6-yl] piperidin-2-acetamide; N - [(1,3-benzodioxol-5-l) methyl] -l- [6- (lH-imidazol-1-yl) pyrazin-2-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-propionamide; N - [(1, 3-benzodioxol-5-yl) methyl] -2- (lH-imidazol-1-yl) pyrimidin-4-propionamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- (lH-imidazol-1-yl) pyrimidin-4-propionami a; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [2- (1H-imidazol-1-yl) pyrimidin-4-oxy] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [2- (1H-imidazol-1-yl) pyrimidin-4-thio] acetamide; N- [(1, 3-benzodioxol-5? L) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-y1] piperidin-2-ethanamine; N - [(1, 3-benzodioxol-5? L) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N-methylpiper? Din-2-ethanamine; N-acetyl-N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanamine; N- [(1, 3-benzodioxol-5? L) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- (methylsulfonyl) piperidin-2-ethanamine;
4- [2- [[(1,3-benz odi-oxol-5-yl) methoxy] ethyl] pipe-ridin-1-yl] -2- (1H-imidazol-1-yl) pyrimidine; 4- [2 - [[4- (methoxy) phenoxy] propyl] pyr rolidin-1-yl] -2- (1H-imidazol-1-yl) pyrimidine; 4- [2 - [[4- (methoxy) phenoxy] propyl] pyrrolidin-1-yl] -2- (lH-imidazol-1-yl) -6-met ilpyr imi dine; 4- [2 - [(1, 3-benzodioxol-yl) propyl] pyrrolidin-1-yl] -2- (lH-imidazol-1-yl) pyrimidine; 4- [2- [(1, 3-benzodioxol-5-yl) prop-2-enyl] pyr rolidin-1-yl] -2- (lH-imide zol-1-yl) pyrimidine; 4-chloro-2- (1H-imidazol-1-yl) -6- (perhydroazepin-1-yl) pyrimidine; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] piper idin-2-ethanol; 4-chloro-2- (1H-imidazol-1-yl) -6- (piperidin-1-yl) pyrimidine; 4-chloro-2- (1H-imidazol-1-yl) -6- (2-ethylpiperidin-1-yl) pyrimidine; Xfluoro-2- (1H-imidazol-1-yl) -6- [[(3, A-dimethoxyphenyl) ethyl] amino] pyrimidine; 4 - f l u o r o - 2 - (l H - i mi d a z or l - l - i l) - 6 - [[(phenyl) ethyl] amino] pyrimidine; N- [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-triazol-1-yl) pyrimidin-4-yl] -4- [(di-methylkexy) carbonyl] piperazine- 2-acetamide;
N- [(1, 3-benzod? Oxol-5? L) met? L] -l- [6- (morphol? N-4-? L) -2- (lH-? M? Dazol-1- ? l) p? pm? dm-4-? l] pipe ndm- 2 -ace tarruda; N- [(1,3-benzod? Oxol-5? L) met? L] -4- [2- (lH-? M? Dazol-1-yl) -6-methox? P? R? M? dm-4-? l] -p? per? dm-2-acetarruda; N- [(1, 3-benzod? Oxol-5? L) met? L] -4- [6- [bis (ethoxy? Carbon? L) met? L] -2- (lH-? M? -1-? L) p? Pm? D? N-4-? L] -1- [(methoxy) carbonyl] pipera zm-2-acetamide; N- [(1,3-benzod? Oxol-5? L) met? L] -4- [6- (apunocarbonyl) -2- (lH-? M? Dazol-1-? L) p? R? m? d? n-4-? l] -1- [(methoxy) carbonyl] p? peraz? n-2-acetam? da; N - [(1, 3-benzod? Oxol-5? L) met? L] -3- [2- (lH-? M? Dazol-1-yl) p? R? M? D? N-4 -? l] -4-methox? benzam? da; 4-chloro- 2 - (1H-? M? Da zol-1-yl) -6 - [(2-methoxyphenyl) arrimo] pyrimy; N- [(1, 3-benzod? Oxol-5? L) met? L] -1- [2- (lH-? M? Dazol-1-yl) p? R? M? Dm-4-? l] mdol-6-carboxamide; N- [(1,3-benzod? Oxol-5? L) et? L] -l- [2- (lH-imidazol-l-yl) p? R? M? Dm-4-? L] p ? rrol-2-carboxam? da; N - [(3,4-d? Methox? Phen? L) et? L] -2- [2- (lH-? M? Dazol-l-l) p? Pm? Dm-4-? L] - 1,2,3, 4-tetrahydro? Soqu? Nolm-3-carboxam? Da; N- [(1,3-benzod? Oxol-5? L) et? L] -l- [2- (lH-? M? Dazol-1-yl) p? R? M? Dm-4-? l] p? rrol? d? n-2-prop? onam? da; N- [(1,3-benzod? Ox X-5-? L) ethyl] -1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? dm-4-? l] p? rrol? dm-2-prop? onam? da;
N- [(3,4-dimethoxy phenyl) ethyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidine-3-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-3-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] - [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-3-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidin-3-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidin-3-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -acetidine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxan-6-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N - [(1,4-benzodioxan-6-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N - [(4-methoxyphenyl) ethyl] morpholine-2-carboxamide;
4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(3,4-dimethoxyphenyl) ethyl] morpholin-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(4-methoxyphenyl) methyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N- [(4-methoxyphenyl) methyl] morpholin-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] morpholin-2-acetamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] morpholin-2-acetamide; N- [(1, 3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] morpholine-3-carboxamide; N- [(1, 3-benzodioxol-5-yl) methyl] -4- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] morpholine-3-carboxamide; N - [(1, 3-benzodioxol-5-yl) ethyl] -4- [6-ethyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] morpholine-3-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] morpholine-3-carboxamide; N - [(4-methoxy phenyl) met il-4- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N - [(4-chlorophenyl) methyl] -4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide;
N- [(3,4-dichlorophenyl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N - [(4-methylphenyl) methi 1-4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N- [(3,4-Dimethylphenyl) methyl] -4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N- [(1,3-benzodioxol-5? L) methyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] acetamide; N- [(1,4-benzodioxan-6-yl) methyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-y1] perhydroazepin-2-carboxamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,4-benzodioxan-6-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide;
N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) • 6-ethylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1, 3-benzodioxol-5-yl) ethyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1,4-benzodioxan-6-yl) ethyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,4-benzodioxan-6-yl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-ethyl-pyrimidin-4-yl] -perhydroazepin-2-carboxamide; N - [(3,4-dimethoxyphenyl) methyl] -1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepine-2-carboxamide; N- [(3, -dimethoxy phenyl) ethyl] -1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (1H-imidazol-1-yl) -6-ethylpyrimidin-4-yl] perhydroazepin-2-acetamide;
N - [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(3,4-dimethoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(3,4-dimethoxyphenyl) methyl] -l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(3,4-dimethoxyphenyl) ethyl-1- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(-methoxy phenyl) methyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl-l- [6-chloro-2- (pyridin-3-yl) pyrimidin-4-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-ylperhydroazepin-2-acetamide; N- [(4-trifluoromethoxyphenyl) methyl] -1- [(2- (1H-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; and N- [(4-trifluoromethoxyphenyl) methyl] - 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide;
Although the present invention has been described with reference to the specific embodiments thereof, it should be understood by those familiar with the art that various changes can be made and equivalents can be substituted without departing from the true spirit and scope of the invention.
In addition, many modifications can be made to adapt a particular situation, material, composition of matter, process, step or process steps to the object, spirit and scope of the present invention. All such modifications are considered within the scope of the claims appended hereto.
Claims (2)
- CLAIMS 1. Compound of formula (I), formula (II) and formula (neither: - A 'III' wherein: A is -R1, -OR1, -CfO fR ^ R2, -P (O) [N (R1) R2] 2, -n (R1) C (0) R2, -N (Rld) C (0) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16, -StO? R1. -SO NHCÍOJR1, -NHS02R22, -SO, N (R1) H, -C (0) NHSO, R22, and -CH = NOR1; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, O or C (RJ) H; each W is N or CH; Q is chosen from the group consisting of a direct link, -C (O) -, -O-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (RX) R2X -NtR ^ JCtOJNtR ^ R16, -SFOXR1 (when t is zero) or -NHSO, R22, n, qyr can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R1) C (0) R2, -N (Rld) C (0) OR2, -N (R2) R21, -N (R16) C (0) N (R1) R16, -SÍOXR1 (when t is zero) or -NHSO, R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; and each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted XC ^ alkyl, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C2-C6 alkenyl] -R9, - [alkynyl] of C2-C6] -R9, - [C, -C6 alkyl] -R10 (optionally substituted by hydroxy), - [Ci-C-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [XC alkyl] -N (R1) R2, - [C_-Cß alkyl] -N (R2) R2, - [X-CgUR6 alkyl, - [C2-C8 alkyl] -R10, - [X-CgJ-R11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -UOWR ^ R2, -C (= NH) -N (R:) R2 O R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R "can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, aralkyl optionally substituted, aryl optionally substituted, -OR 16 S (0) t-Rlb, -N (Rlb) R21, -NYR ^ JCÍOJNtR ^ R16, -N (R16) C (O) OR16, -N (R16) C (0 ) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C (H) [C (0) 0R16], and - [Co-CeUCIOWR alkyl R16; R6] is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C_-C8 alkyl] -R8, - [C2-C8 alkyl] -R10, - [Ci-Cg alkyl] -R11, acyl, -C (0) R8, -C (O) - [XC.J-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl , monoalkylaminocarbonyl, dialkylaminocarbon ilo, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, - C (0) -R23-N (R1) C (0) -R23-N (R1) R2, -C (0) -N (R1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, NO, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -SO, R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof.
- 2. Compound of formula (I), as described in clause 1, which has the formula (la), formula (Ib) or formula (le): 3. Compound as described in clause 2, wherein: A is -OR1, -ClOlNfR1) ^, -N (R16) C (0) N (R1) R16, -NR ^ tOJR2 or -NRI R2; V is N (R4); V is N (R4); and W is CH. 4. Composite as described in clause 3, where: A is -CFOINTER ^ R2; q, r and n are zero; R1 is hydrogen; and R2 is lower alkyl or - [C_-C8] -R9; R 4 is hydrogen or lower alkyl; and R5 is hydrogen, halo, alkyl or alkoxy. 5. Compound as described in clause 4, wherein R9 is phenyl, tolyl, anisyl, 1,4-benzodioxan-6-yl, 1,3-benzodioxol-5-yl, chlorophenyl, carboxyphenyl, dimethoxyphenyl, 2-thienyl or morpholinyl. 6. Compound as described in clause 2, where: A is -UOJNÍR ^ R2; m is zero; Q is a direct link to R3; and R3 is hydrogen. 7. Compound as described in clause 6, for example N - [(1,3-benzodioxol-5-yl) ethyl] -4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-i1 ] (methyl) amino] acetamide. 8. Compound of formula (II) as described in clause 1, having the formula (lia), formula (Ilb), or formula (lie): IIb); or 9. Compound as described in clause 8, wherein the N-heterocyclyl is selected from the group consisting of piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, acetidinyl, indolyl, pyrrolyl, imidazolyl, tetraisoquinolyl and perhydroazepinyl. 10. Compound as described in clause 9, wherein the N-heterocyclyl is piperazinyl substituted by R5, for example, the compound of formula (lid), formula (lie), or formula (Ilf): 11. Compound as described in clause 10, wherein: A is -OR1, -CtOlNfR1) ^, -NÍR ^ UOjNÍR ^ R16, -NRX (0) R2 or -NfR ^ R21; W is CH; and R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of X-CgJ-R8, - [C2-C8 alkyl] -R10, - [C_-C3 alkyl] -Rn. acyl ,, -C (0) R8, -C (0) - [Ci-CgJ-R8 alkyl, alkoxycarbonyl, optionally substituted alkoxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, aryisulfonyl optionally substituted, aminocarbonyl, monoalkylcarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, N-heterocyclyl optionally substituted, -C (= NH) -N (CN) R1, -C (O) -R23-N (R1) R2, -C (O) -R23-N (R1) C (0) -R23-N (R1) R2 and -C (0) -N (R1) -R23-C (0) OR1. 12. Compound as described in clause 11, wherein A is -C (0) N (R0R2; R1 is hydrogen; R2 is lower alkyl, - [C_-C8 alkyl] -R9, or UX-C8] -R10 Rd is hydrogen, acetyl, t-butoxycarbonyl, 4-methoxyphenylaminocarbonyl, 4-methoxyphenylmethyl, methoxycarbonyl, methyl or benzyl, R5 is hydrogen, halo, alkyl or alkoxy, and n is O or 1. 13. Compound as described in clause 12, wherein: R2 is -CH2-R9 or - [C_-CB] -R10; R9 is aryl or substituted aryl; and R10 is methylthio. 14. Compound as described in clause 13, wherein: R2 is -CH, -R9; R6 is hydrogen, acetyl or t-butoxycarbonyl; and R9 is phenyl, tolyl, anisyl, 1,4-benzodioxan-6-yl, 1,3-benzodioxol-5-yl, methylothiophenyl, chlorophenyl, carboxyphenyl, dimethoxyphenyl or 2-thienyl. 15. Compound as described in clause 14, wherein R5 is chloro, R6 is hydrogen and R9 is p-tolyl. 17. Compound as described in clause 14, wherein R 5 is chloro, R 6 is hydrogen and R 9 is 1,4-benzodioxan-6-yl or 1,3-benzodioxol-5-yl. 18. Compound as described in clause 14, wherein R5 is chloro, R6 is t-butoxycarbonyl and R9 is 1,4-benzodioxan-6-yl or 1,3-benzodioxol-5-yl. 19. Compound as described in clause 10, which is selected from the group consisting of: N- [(1,3-benzodioxol-5-yl) ethyl] -4- [2- (lH-imidazol-1-yl) - 6-methylpyrimidin-4-yl] -1- (2-methyl-l-oxopropyl) piperazin-2-acetamide; N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -4- (methoxycarbonyl) piperazin-2- acetamide; N- [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-triazol-1-yl) pyrimidin-4-yl] -4- (dimethylethoxy) piperazine-2-acetamide; N- [(1,3-benzodioxol-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methoxypyrimidin-4-yl] -1- (methoxycarbonyl) piperazin-2 acetamide; l- (acetyl) -N - [(1,3-benzodioxol-5-yl) methyl] -4- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (methylsul fonyl) piperazin-2- acetamide; and 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(pyridin-3-yl) methyl] -4- (tetrahydro-3-furanoyl) piperazine-2-carboxamide. 20. Compound as described in clause 9, wherein the N-heterocyclyl is optionally substituted by piperidinyl, for example, the compound of formula (Hg), formula (Hh), or formula (Ili): 21. Compound as described in clause 20, where: A is -OR1, -C (0) N (RjR-, -N (R16) C (O) N (R1) R16, -NR1C (0) R2 or -NfR ^ R21; and W is CH. 22. Compound as described in clause 21, where A is -C OjNÍR ^ R2; R1 is hydrogen; R 2 is lower alkyl or - [C 1 C-R 9 alkyl; R5 is hydrogen, halo, alkyl or alkoxy; and n is zero or 1. 23. Compound as described in clause 22, wherein R 2 is lower alkyl or -CH-R 9 and R 9 is 4-methoxyphenyl, 1,4-benzodioxan-6-yl, 1,3-benzodiozol-5-yl or 3, 4 -methoxyphenyl. 24. Compound as described in clause 20, which is selected from the group consisting of: N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidine -4-i1] piperidin-2-ethanamine; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (morpholin-4-yl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (methylhexyl) piperidin-2-acetamide; N- [(4-chlorophenyl) methyl] -1- [2,6-bis (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) pi rimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperidin-2-acetamide; and N- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (1 H -imidazol-1-yl) -6-methoxypyrimidin-4-yl] piperidin-2-acetamide. 25. Compound as described in clause 9, wherein the N-heterocyclyl is optionally substituted by pyrrolidinyl, for example the compound of the formula (IIj), the formula (Hk), or the formula (Hm): 10 25 26. Compound as described in clause 25, where: A is -OR1, -C (0) N (R1) R :, -N (R16) C (0) N (R1) R15, -NR ^ tOJR2 or -NÍR ^ R21; and W is CH. 27. Composite as described in clause 26, where: A is -CFONfR1) ^; R1 is hydrogen; R2 is lower alkyl or - [C_-C8 alkyl] -R9; R5 is hydrogen, halo, alkyl or alkoxy; and n is zero or 1. 28. Compound as described in clause 27, in which it has the R-configuration at C-2 of the pyrrolidinyl ring. 29. Compound as described in clause 25, which is selected from the group consisting of: N- [(1,3-benzodioxol-5-? L) ethyl] -4- [2- (lH-imidazol-1-yl) - 6-methylpyrimidin-4-yl] -pyrrole idin-2 -carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] -pyrrolidin-2-carboxamide; N - [(3,4-dimethoxy phenyl) methyl] -1- [2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -pyrrolidin-2-acetamide; N- [(4-methoxy phenyl) ethyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -pyrrolidine-2-carboxamide; and N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] -pyrrolidin-2-acetamide. 30. Compound as described in clause 9, which is selected from the group consisting of: 4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5 -yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] thiomorpholin-2-acetamide; N- [(1,3-dioxolan-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -perhydroazepin-2-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -acetidine-2-carboxamide; and 4- [2- (lH-imidazol-1-yl) pi rimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] morpholine-2-carboxamide. 31. Compound of formula (III) as described in clause 1, in which it has the formula (Illa), formula (IHb), or formula (lile): TO 33. Compound as described in clause 1, of formula (I), formula (II), or formula (III), wherein each X, Y or Z is C (R19) and each U is C (R6), where each R19 and R5 are as described above in clause 1. 34. Compound as described in clause 1, of formula (I), formula (II), or formula (III), wherein each X, Y or Z is N and each U is C (R5), where each R5 is as described above in clause 1. 35. Compound as described in clause 1, of formula (I), formula (II), or formula (III), wherein each X is N, each Z or Y is C (R19), and each U is N, where each R19 is as described above in clause 1. 36. Compound as described in clause 1, of formula (I), formula (II), or formula (III), in which in each formula, one of X, Y or Z is N and the others are C (R19) , and U is C (R5), where each R19 and R5 are as described above in clause 1. 37. Compound of formula (IV): wherein: AA is an amino acid; X, Y and Z are independently? or C (R19); U is it? or C (R5), with the proviso that U is? only when X is? and Z and Y are CR19; is ? or CH; R1 and R2 are independently selected from the group consisting of hydrogen, alkyl of X-C ,. optionally substituted, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, - [C, -C8 alkenyl] -R9, - [C, -C8 alkynyl] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [X-CgJ-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted? -heterocyclyl; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (Rld) C ( 0) N (R1) R16, -N (R16) C (0) OR: é, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [alkyl] of C0-CS] -C (H) [C (0) OR16] 2 and - [C0-C8 alkyl] -C (O) N (R ^ R ^ - each R9 is independently selected from the group consisting of haloalkyl , cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy), each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R19 is hydrogen, alkyl (optionally substituted by hydroxy), cyclopropyl, halo or haloalkyl; each R21 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with Ri6 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and t is zero, 1 or 2; as a single isomer or mixture thereof, or a pharmaceutically acceptable salt thereof. 38. Compound as described in clause 37, of formula (IVa), formula (IVb), or formula (IVc): 39. Compound as described in clause 38, wherein the amino acid is an a-amino acid of the L configuration on the carbon with respect to the acid. 40. Compound as described in clause 38, wherein the amino acid is an a-amino acid of the D configuration on the carbon with respect to the acid. 41. Compound as described in clause 38, wherein: R1 is hydrogen; R 2 is lower alkyl or - [C 1 C-R 9 alkyl; and R5 is hydrogen, halo, alkyl or alkoxy. 42. Compound as described in clause 41, wherein R9 is phenyl, tolyl, anisyl, 1,4-benzodiozan-6-yl, 1,3-benzodioxol-5-yl, chlorophenyl, carboxyphenyl, 2-thienyl, dimethoxyphenyl or morpholinyl. 43. Compound of the formula (Va), formula (Vb), or formula (Ve): wherein B is a 5 or 6 membered carbocyclyl or heterocyclyl, optionally substituted; and wherein: A is -R1, -OR1, -C (0) N (R1) R2, -P (O) [N (R1) R2] ,, -N (Rx) C (0) R2, -N (R16) C (0) OR2, -N (R1) R: 1 -N (R16) C (O) N (R1) R16, -SfOXR1, -SO .NHCfOJR1, -NHSO, R22, -S02N (R1) H, -C (O) NHSO, R22, and -CH = NOR1; each of X, Y and Z are independently N or C (R19); V is N (R4), S, O or C (R) H; each W is N or CH; Q is selected from the group consisting of a direct bond, -C (0) -, -O-, -CXN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (O) R2, -N (R15) C (O) OR2, -N (RX) R21, -NÍR ^ CÍOÍNÍR R15, -SdXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R1) C (0) R2, -N (Rld) C (O) OR2, -NYR ^ R21, -N (R16) C (O) N ( R1) R16, -SÍOÍt-R1 (when t is zero) or -NHSO: R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, [C-C8 alkenyl] -R9, - [ C2-C8 alkynyl] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [X-Cg] -Ru (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C_-C8 alkyl] -C (0) N (R1) R2, - [C_-C8 alkyl] -N ( RX) R2, - [C_-C8 alkyl] -R8. - [C2-C8 alkyl] -R10, - [C_-C8 alkyl] -Ru, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C (0) N (Rx) R2, -C (= NH) -N (RX) R2 or R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of X-CgJ-R8, - [C, -C8 alkyl] -R10, - [alkyl of X-Cg-R11, acyl, -C (0) R8, -C (O) - [C, -C8] -R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl , aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N ( R1) R2, -C (0) -R23-N (R1) C (0) -R23-N (R1) R2, -C (0) -N (R2) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R1S is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R :: or -SO, R22; or R21 taken together with R- and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. 44. Composite as described in clause 43, in which each X and each Y is N; each is CH; and B an optionally substituted fused heterocyclyl. 45. Compound as described in clause 44, of the formula (Vba): wherein A is -OR1, -C (O) N (R1) R2, -N (R16) C (O) N (R1) R16, NRX (0) R2 or -N (R R21; is N-heterocyclyl which is selected from the group consisting of piperidinyl, piperazinyl, pyrrolidinyl or morpholinyl. 46. Compound as described in clause 45, for example N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -purin-6-yl] piperidin-2-acetamide. 47. Compound of formula (Via), formula (VIb) or formula (VIc): wherein B is a 5 or 6 membered carbocyclyl or heterocyclyl, optionally substituted; and wherein: A is -R1, -OR1, -CfOJNtR ^ R2, -P (0) [N (R1) R2] 2, -NtR'lCIOJR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, S -SYOtR1, -S02NHC (0) R1, -NHSO, R22, -S0, N (R1) H, -C (0) NHSO, R22, and -CH = N0R1; each of X, and Z are independently N or C (R19); V is N (R4), S, 0 or C (R4) H; each is N or CH; 0 Q is chosen from the group consisting of a direct link, -C (0) -, -0-, -CUN-R1) -, -S (0) t. and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; 5 r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -0R1, -N (R1) C (0) R2, -N (R16) C (0) 0R2, -NYR ^ R21, -NÍR ^ UO? NÍR ^ R16, -StOXR1 (when t is zero) or -NHSO, R22, n, q and y can not all be zero; and when Q is a heteroatom and A 0 is -OR1, -NtR ^ UOJR2, -N (R16) C (0) 0R :, -NfR ^ R21, -N (R16) C (0) N (R1) R16, -SdXR1 (when t is zero) or -NHSO: R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, - [C0-C5 alkyl] -R9, [C2-C6 alkenyl] -R9, - [alkynyl] of C, -C6] -R9, - [C2-C6 alkyl] -R10 (optionally substituted by hydroxy), - [C_-C,] -Rn (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C: -C8 alkyl] -N (R1) R2, - [C_-C8 alkyl] -N (RX) R2 , - [C_-C8 alkyl] -Re. - [C2-C8 alkyl] -R10, - [alkyl of X-C-R11, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -UOJNÍR ^ R2, -C (= NH) -NÍR ^ R2 O R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R 6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C 1 -C 8 alkyl, - [C 2 -C 8 alkyl] -R 10, - [C 1 -C 6 alkyl, acyl, -C ( 0) R8, -C (0) - [C1-CJ-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (O) -R23-N (R1) R2 , -C (0) -R23-N (R1) C (0) -R23-N (R1) R2, -C (O) -N (R1) -R23-C (O) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R 12, R 13, R 14, R 15 R: "and R 20 are independently hydrogen or alkylene R 16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, NO, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R :: or -SO, R22; or R21 taken together with R: and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. 48. Compound of formula (Vlla), formula (Vllb) or formula (VIIc): (Vllb); or wherein: A is -R1, -OR-, -UOJNÍR ^ R2, -P (O) [N (R1) R2] 2, -N (RL) C (0) R2, -N (R16) C (0) OR2, -NfR ^ R21, -N (R16) C (O) N (R1) R16, -SYOtR1, -S02NHC (0) R1, -NHS02R22, -SO, N (R1) H, -C (O) NHSO, R22, and -CH = NOR1; each of X, Y and Z are independently N or C (R19); each U is N or C (R7, with the proviso that U is N only when X is N and Z and Y are CR19, V is N (R4), S, O or C (R4) H, each is N o CH; Q is chosen from the group consisting of a direct link, -C (O) -, -O-, -CXN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -NfR ^ R21, -NÍR ^ CÍOJ ÍR ^ R16, -StO-R1 (when t is zero ) or -NHSO, R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R2) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -S (0) tR1 (when t is zero) or -NHSO, R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C-C8 alkenyl] -R9, - [alkynyl] of C2-C8] -R9, - [C2-Ce alkyl] -R10 (optionally substituted by hydroxy), - [C-C8] -Rn (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C_-C8 alkyl] -C (O) N (R1) R2, - [C_-C8 alkyl] -N ( RX) R2, - [C_-C8 alkyl] -R ?, - [C2-C8 alkyl] -R10, - [Ci-CgJ-R11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -CfOJNtR1) ^, -C (= NH) -N (R :) R2 or OR R1:? P R2 R4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -ri. { R16) C (0) i (R1) R16, -N (R16) C (0) OR16, -N (R16) C (0) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C (H) [C (0) OR16] 2 and - [alkyl of R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C_-C8 alkyl] -R8, - [C2-C8 alkyl] -R10, - [C_-C3 alkyl] -Ru. acyl, -C (0) R8, -C (0) - [XC.J-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, arylfulsonyl optionally substituted, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (O) -R23- N (R1) R2, -C (O) -R23-N (R1) C (0) -R23-N (R1) R :, -C (O) -N (R1) -R23-C (O) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents which are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkylene R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R2: or -SO, R22; or R21 taken together with R1 and the nitrogen to which they are attached is optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. 49. Compound as described in clause 48, for example N - [(1, 3-benzodioxol-5-yl) methyl] -1- [6-chloro-2- (pyridin-3-yl) pyrimidin-4-yl] piperidin-2-acetamide. 50. Compound of formula (VIII): HIV) in which two of X, Y and Z are nitrogen and the third is CH. 51. Compound as described in clause 50, which is 4,6-dichloro-2- (lH-imidazol-1-yl) pyrimidine. 52. Compound as described in clause 50, which is 2,4-dichloro-6- (lH-imidazol-1-yl) pyrimidine. 53. Compound of formula (IXa), formula (IXb) or formula (IXc): in that it is a solid substrate; L is bond residue; each of X, Y and Z are independently N or C (R10); each U is N or C (R7, with the proviso that U is N only when X is N and Z and Y are CR19, V is N (R4), S, O or C (R) H, each is N o CH; Q is selected from the group consisting of a direct bond, -C (O) -. -O-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (O) R2, -N (R16) C (O) OR2, -N (RX) R21, -NIR ^ ICIOINIR'IR15, -SdXR1 (when t is zero) or -NHS02R22, n, q and r can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R:) C (0) R2, -N (R16) C (O) OR2, -N (R:) R21, -N (R16) C ( O) N (R1) R16, -SÍOXR1 (when t is zero) or -NHSO-R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; each R 2 is independently selected from the group consisting of hydrogen, C 1 -C alkyl, or optionally substituted, optionally substituted cycloalkyl, C0-C6] -R9, [C2-C8 alkenyl] -R9, - [C2-C8 alkynyl] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [X-C-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [X-Cg alkyl] -N (R1) R2, - [X-Cg alkyl] - N (RX) R2, - [X-Cg alkyl -R0, - [C2-C8 alkyl] -R10, - [X-CeJ-R11 alkyl, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo , alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -CÍOJN R ^ R2, -C (= NH) -N (R2) R: or R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (R16) C ( 0) N (Ri) R16, -N (R16) C, 0) OR-6, -N (R16) C (0) R16, - [C0-C8 alkyl] -C (O) OR16, - [alkyl of C0-C8] -C (H) [C (0) OR16] 2 and - [alkyl of R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C 1 -C 8 alkyl, - [alkyl] of C2-C8] -R10, - [alkyl of C.-Cl-R11, acyl, -C (0) R8, -C (0) - [alkyl of X-CgJ-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonyl nocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R23-N (R1) C (0 ) -R23-N (R1) R, -C (0) -N (R1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxXalkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R-7 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, NO, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R :: or -SO, R22; or R21 taken together with R6 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. 54. Compound as described in clause 53, in which L is a photolitically separable link of formula (X): in which the valency not satisfied to the right of the formula represents the point of attachment to the solid substrate, and the valence not satisfied to the left of the formula represents the point of binding to the ligand. 55. Compound as described in clause 1, which is selected from the group consisting of: l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] piperazin -2-acetarruda; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methylphenyl) methyl] piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pi rimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3-hydroxy-N - [(1,3-benzodioxol-5-yl) methyl] propanamide; 2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) methyl] pentanediamine: 2- [[2- (lH -imidazol-1-yl) pyrimidin-4-yl] amino] -5- [[amino (nitroimino) methyl] amino] -N - [(1,3-benzodioxol-5-yl) methyl] pentanamide; 2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3- (thiophen-2-yl) -N- [3- (morpholin-4-yl) propyl] propanamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-c-loro-phenyl) -methyl] -piperazin-2 -acetic acid; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] piperazin-2-acetamide; N - [(4-chloro-phenyl) methyl] -1- [2,6-bis (1 H -imidazol-1-yl) pyrimidin-4-y1] pipe ridin-2 -acet amide; N- [(1, 3-Benzodioxoi-5-yl) methyl] -4- [2- (1H-imidazol-1-yl) -6-methoxypyrimidin-4-yl] -1- (methoxycarbonyl) piperazine-2 - acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -4- (methoxycarbonyl) pipera zin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] piper idine -2 -acet amide; l- [6-Chloro-2- (lH-imidazol-1-yl)? irimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidine-2-acetarruda; 1- [6-chloro-2- (lH-? Midazol-1-yl) pyrimidin-4-yl] -N- [phenylimethyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-inidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3-phenylpropyl] piperazine-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2-phenylethyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(thiophene-2-yl) methyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-? midazol-1-yl) pyrimidin-4-yl] -N- (methyl) piperazin-2-acetamide; 2- [[6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-y1] amino] -3- (methylthio) -N- [(1,3-benzodioxol-5-yl) methyl] butanamide; 2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -4- (methylthio) -N- [(4-methoxyphenyl) methyl] butanamide; 2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4- (methylthio) -N- [2- (3, 4-dimethoxyphenyl) ethyl] butanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4- (methylthio) -N- (methyl) butanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3 - [(1,1-dimethylethyl) thio] -N- [3- (methylthio) propyl] ] propanamide; 2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] amino] -3 - [(1,1-dimethylethyl) thio] -N- [3- (phenyl) propyl] ] propanamide; a- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] -2-thiophenpropanamide; a - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- (butyl) -2-thiophenpropanamide; a- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] amino] -N - [(1,3-benzodioxol-5-yl) methyl] -2-thiophenpropanamide; 2 - [[6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] amino] -3 - [(1,1-di-methylethyl) thio] - N - [2 - (3 , 4-dimethoxyphenyl) ethyl] propanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, -dimethoxyphenyl) ethyl] acetamide; 2 - [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] propanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-y1] amino] -N- [2- (3, 4-dimethoxyphenyl) ethyl] pentanediamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [(4-methoxyphenyl) methyl] pentanediamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] pentanediamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -5- [[amino (nitroimino) methyl] -amino] pentanamide; 2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -N - [(4-methoxyphenyl) methyl] - 5 - [[imino (amino) methyl] amino] ] peitanamide; 1- [6-chloro-2- (lH-inidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 2- [[6- chloro- 2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -N- [(4-methoxyphenyl) methyl] -5 - [[imino (nitroamino) methyl] -amino] pentanamide; N- [(1,3-benzodioxol-5-yl) methyl) -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] -5- [ [amino (imino) methyl] -amino] pentanamide; l- [6-Chloro-2- (lH-? midazol-l-yl) pyrimidin-4-yl] -4-hydroxy-N- [4- (hydroxycarbonyl) phenyl]] tyl] pyrrole idin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-y1] amino] -3-hydroxypropanamide; 6-amino [[6-chloro-2- (lH-imidazol-1-yl) pyrimin-4-yl] amino] -N- [2- (3, 4-dimethoxy phenyl) ethyl] hexanamide; a- [[6-chloro- 2- (lH-i) zol-l-yl) pyrimidin-4-yl] amino] -N- [3- (methylsul-fonyl) -propyl] -benzene-propanamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] (methyl) amino] acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -6- [[6-chloro-2- (1H-imidazol-1-yl) py [mu] im] din-4-yl] amino] hexanamide; 5-amino-N- [(1, 3-ber z odi oxol-5-yl) methyl] -2- [[6-chloro-2- (1 H-imidazol-1-yl) pyrimidin-yl] amino ] pentanamide; 5-amino-N-butyl-2- [[6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-y1] amino] pentanamide; 4- [3-hydroxy-3-oxopropyl) amino] -3- [[6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] amino] -4-oxobutanoic acid; 2- [[6-chloro-2- (IH-imidazol-1-yl) pyrimidin-4-yl] (methyl) amino] -N- [(pyridin-4-yl) methyl] acetamide; 1- [6-chloro-2- (1H-? Midazol-1-yl) pyrimidin-4-yl] -N-methylpiperidine-2-carboxamide; N- [2- (3, 4-dimethoxy phenyl) ethyl] -α- [[6- (lH-imidazol-1-yl) pyrimidin-4-y1] amino] -2-t? Ofenpropanamide; N- [(1, 3-benzodioxol-5-yl) methyl] -2- [[6- (IH-imidazol-1-yl) pyrimidin-4-y1] amino] -4-methylpentanamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[6-2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] pentanediamide; N- [2 (3,4-dimethoxy phenyl) ethyl] -2 - [[6- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -4-m-thylpentanamide; N- [(1,3-benzodioxol-5-yl) methyl] -2 - [[6- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] -3-h? Droxypropanamide; N- [(1,3-benzodioxol-5-yl) methyl] -α- [[6- (1H-imidazol-1-yl) pyrimidin-4-yl] amino] benzenepropanamide; 5- [[amino (imino) methyl] amino] -6- (lH-imidazol-1-yl) pyrimidin-4-y1] -N- (phenylmethyl) pentanamide; N- [(1,3-benzodioxol-5-yl) methyl] -1,4-bis [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] piperazin-2-acetamide; N- [(1,3-benzodioxU-5-yl) methyl] -1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -4- [[phenyl] amino] carbonyl] -piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- [(methoxy) carbonyl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- (acetyl) -N - [(1,3-benzodioxol-5-yl) methyl] -4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidi-4-yl] piperazin-2 -acetamide; 4- [2- (lH-imidazol-i -yl) -6-methylpyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -1-methylpiperazin-2-acetamide; 4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -1-methylpiperazin-2-acetamide; N- [(3-chloro-4-methoxymethyl) methyl] -4- [2- (lH-imidazyl-1-yl) -8-methylpyrimidin-4-yl] -l-methylpiperazin-2-acetamide; 4- [6-chloro-2- (lH-iridazol-1-yl) pyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] -1-methylpiperazin-2-acetamide; 4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4,5-trimethoxyphenyl) methyl] -1-methylpiperazin-2-acetamide; N- [2- (1,4-benzodium > an-6-yl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -1-methylpiperazine-2-acetamide; l-butyl-4- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-y1] - N - [(furan-2-yl) methylpiperazi- n-2-carboxamide; N- [(4-Benzodioxan-6-yl) methyl] -l-butyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] pipet. : ^ n-2-acetamide; N- [2- (1, 4-benzodi-6-yl) ethyl] -l-butyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] pipera zin- 2 - a ce tarruda; N- [(2,3-dimethoxyphenyl) methyl] -l-butyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-acetamide; 4- [6-chloro-2- (lH-ip ida zol-l-yl) pyr imidin-4 -i 1] -N- [(4-chlorophenyl) methyl] -1- [(4-methoxymethyl) methyl] ] piper a zin-2 -acet ami da; 4- [6-methyl-2- (lH-im? Dazyl-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -1- r (4 - me toxi phenyl) methyl] pipe razin-2-carboxamide; 4- [2- (1H-imidazcI-1-yl) pyrimidin-4-yl] -N- [(4-chloro-phenyl) -methyl] -1- [(4-methoxy-1-phenyl) -ethyl] -piperazine-2 -acetamide; 4- [6- (lH-imidazo-l-yl) pyr imidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -1- [(4-methoxy-enyl) methyl] ] piperazine-2-carboxamide; 4- [6-methyl-2- (lH-ip? Dazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -1- [(4-methoxyphenyl) methyl] piperazine- 2-acetamide; 4- [6-chloro-2- (lH-in ida zol-l-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -1- [(4-methoxy phenyl) methyl] piperazin-2-acetamide; 4- [6-met il-2- (lH-in-idazol-1-yl) -pyridin-4-yl] -N- [(4-methoxy phenyl) ethyl] -1- [(4-methoxy); ifenyl) methyl] piperazin-2-acet amide; 4- [6-methyl-2- (lH-im-dazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -1- [(4-methoxyphenyl) methyl] piperazine -2-acetamide; 4- [6-chloro-2- (1H-: midazol-1-yl) pyrimin-1-yl) -N- [(indan-5-yl) methyl] -1- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; N- [(1, 3-benzod L xol-5-yl) methyl] -l- [(2,3-dichlorophenyl) methyl] -4- [2- (lH-imidazol-l-yl) pyrimidin-4 -yl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(3,4-dichloroyenyl) methyl] -4- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] piperazine-2-carboxamide; N- [(1, 3-benzod? Oxol-5-yl) methyl] -l- [(3,4-dichlorophenyl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidine-4- il] piperazin-2-carboxamide; 4- [6-met il-2- (lH-ipida zol -1-yl) pir imidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] -1 - [ (3,4-dichlorophenyl) methyl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidine- 4-yl] piperazin-2-acetamide; N- [(1,3-benz odi-oxol-5-yl) methyl] -1- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(1,3-benzodioxol-5-y1) me ti 1] -4- [6-chloro-2- (AH-imidazole -l-yl) pyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(1,3-benzodioxol-5-yl) methyl] -4- [6- (lH-imidazol-l-yl) pi r imidin-4-yl] piperazine-2-carboxamide; N- [2- (1, 3-benzodiox-5-yl) ethyl] -l- [(1,3-benzodioxol-5-yl) met il] -4- [2- (lH-imidazol-1-yl) ) -6-methylpyrimidin-4-yl] pipera zin-2 -acet amide; N- [2- (1, 3-benzodiox X-6-yl) ethyl] -l- [(1,3-benzodioxol-5-yl) me ti 1] -4- [2- (lH-imidazol-l -yl) -6-methylpyrimidin-4-yl] piperazin-2-acet amide; N- [(4-methoxyphenU) methyl] -l- [(1, 3-benzodioxol-5-y1) me ti 1] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin- 4-yl] piperazin-2-carboxamide; N- [(4-methyloxy) 1) met yl] -1- [(1, 3-benzodioxol-5-yl) met yl] -4- [2- (lH-imidazol-1-yl) -6 -methylpyrimidin-4-yl] piperazin-2-acetamide; N- [(4-methoxypheni.) Methyl] -l- [(1, 3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6- (iso-propyl) ) pyrimidin-4-yl] piperazin-2-acet amide; N- [2- (4-methoxyphex) ethyl] -1 - [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imide ol-1-yl) -6-methylpyrimidine- 4-yl] piperazin-2-acetamide; N- [[2- (phenyl) cyclopentyl] amino] -1- [(1,3-benzodioxol-5-yl) me tyl] -4- [6-chloro-2- (.H-imidazol- 1-yl) pyrimidin-4-yl] piperazin-2 -carboxamide; N- [(4-Ethoxyphenylmethyl] -1- [(1,3-benzodioxan-6-yl) me ti 1] -4- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4- il] piperazin-2-acet amide; N- [(1,3-benz odi-oxol-5-yl) methyl] -1- [(1,3-benzodioxan-6-yl) methyl] -4- [2 - (lH-imidazol-1-yl) -6- (iso-propyl) pyrimidin-4-yl] piper a zin-2 -acet amide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(1,3-benzodioxan-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-y1] piperazin-2-acetamide; N- [(1 , 3-benzodioxol-5-yl) methyl] -l- [(1,3-benzodioxan-6-yl) methyl] -4- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] piperazine -2-carboxamide; N- [2- (1, 3-benzodioxol-5-yl) ethyl] -1- [(1,3-benzodioxan-6-yl) met i 1] -4- [2- (lH -imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [2- (1,3-benzodiox-5-yl) ethyl] -l- [(1,3-benzodioxan - 6-yl) met i 1] -4- [2- (lH-imide ^ ol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-carboxamide; N- [(4-methoxyphenyl) methyl] -l- [(1, 3-benzodioxan-6-yl) methyl] -4- (lH-imidazol-1-i. ) - 6-chloropi r imidin-4-yl] piperazin-2-acetamide; N- [(3,4-dimethoxy fe Ul) methyl] -1- [(1, 3-benzodioxan-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6- ( iso-propyl) pi r imidin-4-yl] piperazin-2-acetamide; N- [(3, 4-dimethoxy fa Ul) methyl] -l- [(1, 3-benzodioxan-6-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6- chloropyrimidin-4-yl] piperazin-2-acet amide; N- [2- (1, 3-benzodicxol-5-yl) ethyl] -1- [(pyrimin-3-yl) me t yl] -4- [2- (lH-imidazol-1-yl) - 6-methylpyrimidin-4-yl] piperazin-2-acet amide; N- [(1,4-benzodioxan-6-y1) me ti 1] - 1 - [(pyridin-3-yl) methyl] -4- [2- (lH-imidazol-l-yl) pyrimidin-4 -yl] piperazine-2-carboxamide; N- [2- (1, 4-benzodixoan-6-yl) ethyl] -l- [(pyridin-3-yl) methyl] -4- [2- (lH-imide.:ol-l-il) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [(4-methoxy phenyl) ethyl] -1- [(pyridin-3-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6-cl ??: opyrimidin-4- il] piperazine-2-carboxamide; N- [(3,4-dimethoxyphene) methyl] -1- [(pyridin-3-yl) methyl] -4- [2- (lH-imide zol-1-yl) -6- (iso-propyl) pyrimidin-4-yl] piperazin-2-acetamide; N- [2- (3,4-Di methoxyphenyl) ethyl] -1 - [(3-fluoro-4-methoxyphenyl) methyl] - A - [2- (lH-imidazol-1-yl) -6- (isopropyl ) pyrimidin-4-y1] pipera: .in-2-acet amide; N- [3- (3,4-dimetho-> ifenyl) propyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2 - (lH-imidazol-1-yl) -6- (i sopropil) pyrimidin-4-yl] pipera-2-acetamide; N- [(4-ethoxyphenyl) methyl] -1- [(3-fluoro-4-methoxy-phenyl) methyl] -4- [2- (lH-yl my dazol-l-yl) -6-met ilpyr imi din-4-yl] pipera zin-2 -acetic acid; N- [2- (4-Methylphenoxy) ethyl] -1- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (1H- _ da zol-1-yl) -6-chloropyr imidin- 4-yl] piperazin-2 -acetic acid; N- [(4-methylphenyl) methyl] -l- [(3-fluoro-4-me t-oxy phenyl) methyl] -4- [2- (1H-mida zol-1-yl) -6- Chloropyrimidin-4-yl] piperazin-2 -acetic acid; N- [(4-chlorophen Ll) methyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-imide zol-l-yl) -6-met ilpyr imi din - 4-yl] piperazin-2-acet amide; N- [(4-chlorophenyl) methyl] -1- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-i my da zol-l-yl) -6-chloropyr imidin- 4-yl] piperazin-2-acetamide; N- [(1, 3-benzodio> g-ol-5-yl) methyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-mida zol-l- il) -6-chloropyr imidin-4-yl] piperazin-2-acet amide; N- [2- (1, 3-benzodi-xol-5-yl) ethyl] -1- [(3-fluoro-4-methoxy phenyl) ethyl] -4- [2- (1H-. -l-il) -6-met ilpyr imidin-4-yl] piperazin-2-acet amide; N- (2- (1, 3-benzodUxol-5-yl) ethyl] -l - [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- ('. H-imidazol-1-yl) pyrimidin-4-yl] piper a zin-2-acet amide; N- [2- (1, 4-benzodi txan-6? L) ethyl] -l- [(3-fluoro-4-methoxyphenyl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperazin-2-acet amide; N- [2- (4-methoxyphenyl) ethyl] -1- [(3-fluoro-4-methoxyphenyl) methyl] -A- [2- (lH-imidazol-1-yl) -6- (isopropyl) pyrimidine- 4-yl] piperazine-2-acetamide; N- [(3,4-dimethoxyphen 1) ethyl] -l-acetyl-4- [2- (IH-imidazol-1-yl) -6- (iso-propyl) pyrimidir-4-yl] pipera zin-2 -acetamide; N- [(4-ethoxy phenyl) -yl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6- (iso-propyl) pyrimidin-yl] p? Perazin-2 carboxamide; N- [2- (4-methyl-enoxy-ethyl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] pip-2-acetamide; N- [ 2- (3-chloro-4-met-JXI-phenyl) -ethyl] -l-acetyl-4- [2- (1H-imi-zol-1-yl) -6-chloropyrim (? N-4-yl) pipe-ration -2-carboxamide; N- [(1,3-benzodioxcl-5-yl) methyl] -l-acetyl-4- [2- (1H-imidazol-1-yl) -6-methylpyrimic? N-4-yl ] piperazin-2-acetamide; N- [(4-methoxyphenyl) methyl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6-met-ilpyrimidin-4-yl] pip was zi n-2 -carboxamide; N- [(4-methoxyphenyl) methyl] -l-acetyl-4- [2- (lH-imidazol-1-yl) -6-chloropyrimidin-4-yl] pii erazin -2-acetamide; N- [2- (3, 4-dimethoxy-nyl) ethyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1 H-imidazol-1-yl) -6 - (iso-propyl) pir imidin-4-yl] pipera zin-2-acetamide; N- [2- (3, 4-dimeroxif < nil) ethyl] -1- (3-methyl-l-oxobutyl) -4- [2- (lH-imide zol-1-yl) -6-cl oropyrimidine -4-yl] piperazine-2-carboxamide; N- [2- (3-chloro-4-n-toxyphenyl) ethyl] -l- [3-met il-1-oxobutyl) -4- [2- (lH-imida-ol-1-yl) -6- Chloropyrimidin-4-yl] piperazin-2-carboxamide; N- [2- (3-chloro-4-retoxyphenyl) ethyl] -l- (3-met il-1-oxobutyl) -4- [2- (lH-imide ol-1-yl) -6-methylpyrimidin- 4-yl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- (3-met il-1-oxobutyl) -4- [2- (lH-imide zol-1-yl) pyrim. iin-4-yl] piper a zin-2 -carboxamide; N- [(1,3-benzodioxol-d-yl) methyl] -1- (3-methyl-il-1-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-p-ethylpyrimidine -4-yl] piperazine-2-carboxamide; N- [2- (1,3-benzodio? Tn-6-yl) ethyl] -1- (3-methyl-l-oxobutyl-4- [2- (lH-imidazol-1-yl) -6- c .. oropyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,4-benzodioxan-d-yl) methyl] -1- (3-met il-1-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-c-oropyrimidin-4-yl] piperazine-2-carboxamide; N- [2 (1,4-benzodixol X-yl) ethyl] -1- (3-met il- 1-oxobutyl) -4- [2- (1H-imidazol-1-yl) -6-c-loropyrimidin-4-yl] piperazine-2-carboxamide; N- [2 (1,4-benzodixol-S-yl) ethyl] -1- (3-methyl-1-oxobutyl) -4- [2- (1H-imidazol-1-yl) -6- (trifluoromethyl) pyrimidin-4-yl] piper a zin-2-acet amide; N- [(2,6-dimethoxy phen 1) methyl] -1- (3-met il-1-oxobutyl) -4- [2- (lH-imidazol-1-yl) -6-c orop i ' midin-4-yl] piperazin-2-acetamide; N- [2- (3, 4-dimethoxy-enyl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imide zol-1-yl) -6- (iso-p-opyl) pyrimidine- 4- il] piperazin-2-acetamide; N- [2- (1, 3-benzodiox-l, 5-yl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-met lpyrimidin-4-yl] piperazine-2-carboxamide; N- [2- (1, 3-benzodio-1-5-yl) ethyl] -1- (methoxyacetyl) -A- [2- (lH-imide zol-1-yl) -6-chloropi? Lidin-4-yl] piperazin-2-acet amide; N- [2- (1, 3-benzodioxc 1-5-yl) ethyl] -1- (methoxyacetyl) -4- [2- (1 H-imidazol-1-yl) -6- (trifluoro-omethyl) -pyridin - 4-yl] piper to zin-2-acetamide; N- [(3,4-dimethylpheni) methyl] -1- (methoxyacetyl) -4- [6- (1H-imidazol-1-yl) -6- (trifluoroxethyl) pyrimidin-1-yl] piperazine-2-carboxamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6- (iso-p-opyl) pyrimidin-4-yl) ] piperazin-2-acetamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- (methoxyacetyl) -4- [2- (lH-imide zol-1-yl) -6- (iso-p-opyl) -pyridin-4 -yl] piperazine-2-carboxamide; N- [2- (1,4-benzodiox-n-6-yl) ethyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6- (trifluo-omethyl) pyrimidine- 4-yl] piperazin-2-acetamide; N- [(-methoxy phenyl) -. ethyl] -1- (methoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acet amide; N- [2- (3,4-dimethoxy-yl) ethyl] -l- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic azol-1-yl) -6- Chloropyrimidin-4-yl] piperazin-2-carboxamide; N- [(4-methylphenyl netyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic azol-1-yl) -6-chloropyrimidin-4-yl] pipera zin - 2 -acet amide: N- [2- (4-chlorophen: L) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic -i zol-1-yl ) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [(3-chloro-4-methox: phenyl) methyl] -1- [(tetrahydrofuran-2-yl] carbonyl] -4- [2 - (lH-imic isol-l-yl) -6-chloropyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [(tetrahydrofuran-2) -yl) carbonyl] -4- [2- (lH-imidazc-1-yl) pyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol 5-yl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [6- (lH-imidazc Ll -yl) pyrimidin-4-yl] piperazine- 2-carboxamide; N- [2 (1,3-benzodioxo-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (1H-imidazo-1-yl) -6-pyrimidine- 4-yl] piperazin-2-acetamide; N- [2- (1, 3-benzodioxc L-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazc i-1-yl) pyrimidine- 4-yl] piperazin-2-acetamide; N- [2 (1,3-benzodioxo-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazc-l-yl) -6- ( iso-propyl) pyrimidin-yl] piperazin-2-acetamide; N- [2 (1,3-benzodioxo-5-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic azol-1-yl) -6-methylpyrimidine -4-yl] piperazine-2-carboxamide; N- [(1,4-benzodioxol-6-yl) methyl] -l- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazc.-1-yl) -6- (iso -propyl) pyrimidin-4-yl] piperazin-2-acetarr da; N- [(1,4-benzodioxan-Xyl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imid zol-1-yl) -6- (chloropyrimidine- 4 -yl] piperazine-2-acetamide; N- [(1,4-benzodioxan-Xyl) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic? zol-1 -yl) -6-chloropyrimidin-4-yl.} piperazine-2-carboxamide; N- [2- (1, 4-benzodioxa-6-yl) ethyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -A- [2- (IH-imic, azol-1-yl) - 6-methylpyrimidin-4-yl} piperazin-2-carboxamide; N- [(4-methoxyphenylmethyl]] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic azol-1-yl) -6-chloropyrimidin-4-yl] piperazin-2-acetamide; N- [2- (4-methoxypheni) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imic azol-1-yl) -6 -chloropyrimidin-4-yl] piperazine-2-carboxamide; N- [2- (3-methoxyphenyl) ethyl] -l- [(tetrahydrofuran-2-yl) carbonyl] -A- [2- (lH-imic azole - 1-yl) -6-chloropyrimidin-4-yl] piperazin-2 -carboxamide; N- [(1,4-benz odi oxan- 'yl) methyl] -l- [(tetrahydrofuran-2-yl) ) carbonyl] -4- [2- (lH-imidazc-1-yl) -6- (iso-propyl) pi r imidin-4-yl] piperazine-2-carboxamide; N- [(3,4-dimethoxifer 1 ) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] -4- [2- (lH-imidazc-l-yl) -6- (iso-propyl) pi r imidin-4-yl] pipera zin - 2-acetamide: N- [(3,5-dimethoxy fer. 1) methyl] -1- [(tetrahydrofuran-2-yl) carbonyl] - - [2- (lH-imic? Zol-1 -yl) - 6-chloropyrimidin-4-yl] piperazin-2-acetazole; N- [(4-ethoxyphene-1) methy1] -1- [(2-hydroxy-2-oxoet) oxy) acetyl] -4- [2- (lH-ii da zol-l-yl) -6-chloropyr imidin-4-yl] piperazine-2-carboxamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [(2-hydroxy-2-oxoethoxy) acetyl] -4- [2- (lH-i-idazol-1-yl) -6- chloropyrimidin-4-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxc L-5-yl) methyl] -1- [(2-hydroxy-2-oxoethoxy) acetyl] -4- [2- (lH-i: idazol-1-yl) - 6-methylpyrimidin-4-yl] piperazine-2-carboxamide; N- [2- (3,4-dimethoxy-nyl) -ethyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-methylpi? .midin-4-yl] piperazin-2-acetamide; N- [3- (3, 4-dimethoxife XI) propyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-cioropi? .midin-4-yl] piperazin-2-acetamide; N- [(4-methyl phenyl) methyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol-1-yl) -6-methylpyrimic ..n-4-yl] piperazine-2-acetamide; N- [(1,3-benzodioxol- "> -il) methyl] -1- (phenoxyacetyl) -4- [2- (1H-imidazol-1-yl) pyrimidin-1-yl] piperazine-2-carboxamide; N- [(1,3-benzodioxol- -yl) methyl] -1- (phenoxyacetyl) -4- [6- (1H-imidazol-1-yl) pyrimidin-1-yl] piperazine-2-acetarrudate; N - [2- (1, 3-benzodioxo-5-yl) ethyl] -1- (phenoxyacetyl) -4- [2- (1H-imidazol-1-yl) pyrimidin---yl] piperazin-2-acetamide; N- [2- (1,3-benzodioxo-5-yl) ethyl] -1- (phenoxyacetyl) -4- [2- (lH-imide zol-1-y1) - 6-chlor op id imide n- 4-i 1] p ipe ra z in-2 -carboxamide; N- [(1,4-benzodioxan-> -yl) methyl] -1- (phenoxyacetyl) -4- [2- (lH-imidazol- 1-yl) -6-chloropi? .midin-4-y1] piperazin-2-acetamide; N- [2- (1,4-benzodioxa-5-yl) ethyl] -1- (phenoxyacetyl) -4- [ 2- (lH-imidazol-1-yl) -6-chloropi-midin-4-yl] piperazin-2-acetamide; N- [(4-methoxyphenyl) rt.] -1] (f-enoxyacetyl) -4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl Xperazin-2-acetamide; N- [(4-methoxy phenyl) tyl] -1- (phenoxy to cetyl) -4- [2- (lH-imidazol-1-yl) -6-chloropyrimic in-4-yl] piperazin-2-carboxamide; N- [2- (4-methoxyphenyl)] -1- (f-enoxyacetyl) -4- [2- (1H-imidazol-l-yl) -6-methylpyrimic-4-yl] piperazin-2-acetamide; N- [2- (4-methoxy phenyl ethyl] -1- (f-enoxyacetyl) -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl "Xperazin-2 -acetamide; N- [ 2 - (3,4-dimethyl f-ethyl) -1- [(4-methoxyphenyl) carbonyl] -4- [2- (1-imidazol-1-yl) -5-chloropyrimidin-4-yl] piper a zin- 2 -acet amide; N - [(1, 3-benzodioxolX-yl) methyl] -4- (6-f luoropyridin-2-yl) -1- [2- (lH-imide zol -1- il) pi imidin-4-yl] piper to zin-2 -aceta-like; 1- (acetyl) -4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4 -methylsulfonylphenyl) methyl "? perazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl.} - N - [(4-methylsulfonylphenyl) methyl] pipe idin-2- acetamide; N- [(1,3-benzod L-oxol-5-yl) methyl] - A - [[2- (ethoxycarbonyl) methyl] -1- [2 - (lH-imidazol-l-yl) pyrimidin-4 -yl] piperazin-2-acetamide; 4- [amino (imino) metX-N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imide zol-1-yl) pi rim iin-4-yl] pipera zin-2-acet amide; 1-Methylsulfonyl- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4-) enz odi oxan-6-yl) ethyl] pipera zin-2-acetamide;1-met ilsul foni 1-4- [2 (1H-imidazol-1-yl) pyrimidin-4-yl} -N- { 2- (1,4-benzodioxan-6-yl) < ?] pipe razin-2 -acet amide; 1-methylsulfonyl- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2-X-methoxyphenyl) ethyl] piperazine-2-acetamide; l-methylsulfonyl-4-6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-xmethoxyphenyl] methyl] piperazine-2-acetamide; - (n-octyl) f ílfon:? -4 - [6-met il-2 - (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3, -dimethoxy-enyl) ethyl ] piperazin-2-acetamide; 1- (n-octyl) sulphon:.-A- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [X-CIOJ] J-4-methoxyphenyl) methyl] piperazine-2-acetamide; 1- (n-octyl) suí fonil- - [6-lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxc'-5-yl) piperazin-2-acetamide; 1- (n-octyl) sulfon. 4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3- ^ enzodioxol- 5-yl) ethyl] piperazin-2-acetamide; 1- (n-octyl) sulfon: L- 4 - [6-methyl 1-2 - (lH-imidazol-1-yl) pyrimidin-4-yl] - N- [2- (1, 4-jenzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (n-octyl) sulfon: L-4- [6-methyl-2- (lH-imidazol-1 -yl) pyrimin-4-yl] -N- [2- (3-methoxyphenyl) methyl] piperazin-2-acetamide; 1- (n-octyl) sulfon: 1-4- [6-met il-2- (1 H-imide zol-1-yl) pyrimin din-4-yl] -N- [(4-f) lorophenyl) sulfonyl] piperazin-2-acetamide; 1- (4-methyl phenyl) sul on il-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(pi Xdin-3-yl) methyl] piperazine-2-carboxamide; 1- (4-methylphenyl) sul "Dnyl-4- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] piperazine -2-carboxamide; 1- (4-methylphenyl) sul onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [(3, 4- lime toxy phenyl) methyl] piperazine-2-carboxamide; 1- (4-methoxyphenyl) SUJ 2onyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2 - (3, -dimethoxyphenyl) ethyl] piperazin-2-acetamide; 1- (4-methoxy phenyl) su: onyl-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidine- 4- il] -N- [(1,3-b nz odi oxol-5-yl) me useful] piperazine-2-carboxamide; 1- (4-methoxyphenyl); ulfonyl-4- [2- (lH-imidazol- 1-yl) pyrimidin-4-yl] -N- [2- (1, 3 -) -enoxodioxol-6-yl) ethyl] piperazine-2-carboxamide; 1- (4-methoxyphenyl) -sulfonyl-4- [ 2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3) -cyclodol-5-yl) ethyl] piperazin-2-acetamide; 1- (4-methoxy phenyl) sul onyl-4- [6-met il-2- (lH-imide zol-l-yl) pyrimin din-4-yl] -N- [(3,4-limetoxyphenyl) methyl ] piperazin-2-acetamide; 1- (4-methoxy phenyl sul onyl-4- [6-met i 1-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (l, 4- > enzodioxan -6-yl) ethyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) -l-lfonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4) -yl] - N - [(4-methoxy phenyl) methyl] piperazin-2-carboxamide; 1- (4-methoxy-enyl) -ul on on 1 - 4 - [2 - (lH-imide zol-1-yl) pyrimidin-4-yl] - N - [(2-ethoxyphenyl) methyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) sul "onyl -4- [6-met il-2- (lH-imide zol -l-yl) pyrimidin-4-yl] -N- [2-X-methoxyphenyl) ethyl] piperazin-2-acetamide; 1- (4-methoxy phenyl) su: Xnil-4- [6 -chloro- 2 - (1H-imide zol-1-yl) pyrimidin-4-yl] -N- [2-X-methoxyphenyl) ethyl] piperazine-2-carboxamide; 1- (4-methoxyphenyl) sul: onyl-4- [6 -methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3, 4-imethoxy-phenyl) -methyl] -piperazine-2-carboxamide; 1- (4-methoxyphenyl) -i? lfonyl-4- [6-iso-propyl-2- (1H-imi da zol-1-yl) pyrmidin-4-yl] - N - [(3,4-dimetre oxy phenyl) methyl] piperazir-2-carboxamide; 1- (4-methoxy phenyl) its! : onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-limetoxyphenyl) methyl] piperazine-2-carboxamide; 1- (4-f luoro phenyl) sulphonyl 4- [6-chloro-2- (lH-imidazol-1-yl) pir imidin-4-yl] -N- [2- (1, 3-) enzodioxol -5-yl) ethyl] pipera zin-2-acetamide; 1- (Fluorophenyl) s lfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-enzodioxan-6-yl) ethyl] pipera zin -2-acetamide; 1- (dimethylamino) sul onyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methyl) phenyl) methyl] pipera zin-2 - acet amide; 1- (dimethylamino) -helonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-cl r o- 4 -me toxy phenyl) ethyl] piperazin-2-acetamide; 1- (dimethylamino) sul onyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-b nzodioxo 1-5-yl) me useful] pipera zin-2-acetamide; 1- (dimethylamino) s? Lfonil-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-b nzodioxol-5-yl) methyl] pipera zin- 2-carboxamide; 1- (dimethylamino) sul onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3 > in zodioxol- 5- il) ethyl] pipera zin-2-acetamide; 1- (dimethylamino) e? Lfonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-b nzodioxan-6-yl) methyl] pipera zin- 2-acetamide; 1- (dimethylamino) sul onyl-4- [6-trif luoromethyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide a; 1- (dimethylamino) s lfonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4 Ul] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamid; 1- (dimethylamino) sul onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4-enzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (dimethylamino) sul onyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- ('-methoxyphenyl) ethyl] piperazin-2- acetamide; 1- (dimethylamino) s lfonyl-4- [6-iso-propyl-2- (1H-i m i d a z or l-1-i l) p i r m i d i n-4-i l] - N - [(3, A-dimethoxyphenyl) methyl] piperazi. - 2 -a cet ami da; 1- (n-propyl) aminoca: > onyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [2- (3, -dime :: oxy phenyl) ethyl] pipera zin-2 acetamide; 1- (n-propyl) aminoca: jonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (l -methyl phenoxy) ethyl] piperazine -2-carboxamide; 1- (n-propyl) aminocaj) onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (-chlorophenyl) ethyl] piperazin-2 -carboxamide; 1- (n-propyl) aminocay) onyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] pipe ra zin-2-acetamide; 1- (n-propyl) aminocay) onyl-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (3-cl r- 4 -me toxy phenyl) ethyl] pipera zin-2-carboxamide; 1 - (n-propyl) aminoc irboni 1 -4 - [6-i so-propyl-2 - (1H-imidazol-1-yl) pyrimidine-! - i 1] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin-2 -carboxar ida; 1- (n-propyl) aminocaj > onyl-4- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(1,3-b nzodioxol-5-yl) methyl] pipe-2- carboxamide; 1- (n-propyl) aminocayonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pir imidin-4-yl] -N- [(1,3-b nzodioxol-5- il) methyl] pipera zin-2-acetamide; 1- (n-propyl) aminoca:) onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pir imidin-4-yl] -N- [2- (1, 3-) enzodioxol -5-yl) ethyl] piperazine-2-carboxamide; 1- (n-propyl) aminoca:; onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pir imidin-4-yl] -N- [2- (1, 3- jenzodioxol- 5-yl) ethyl] piperazin-2-acetamide; 1- (n-propyl) aminc-arbonyl-4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3-) eno-dioxol-5-yl) ethyl ] pipera zin-2-carboxamide; 1- (n-propyl) aminoc arbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidine-! -i 1] -N- [(1,4-benzodioxan-6-yl) methyl] pipera zin-2 -carboxar '.da; 1- (n-propyl) aminc arbonyl-4- [2- (lH-imidazol-1-yl) pyrimin-4-yl] -N- [2- (1, l-benzodioxan-6-yl] piperazine- 2-carboxamide; 1- (n-propyl) aminoca. -onyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [(3,4- methoxyphenyl) methyl] piperazin-2-acetamide; 1- (cyclohexyl) aminoc-rbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-dimethoxyphenyl) ethyl] piperazin-2-acetamide; 1- (cyclohexyl) aminot-rbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(- -ethoxy phenyl) methyl] piperazine-2-carboxamide; 1- (cyclohexyl) amii) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-Cl ro- 4 -me toxy phenyl) ethyl] piperazin-2-acetamide; 1- (cyclohexyl) amin carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimid n-4-yl] -N- [2- (3-chloro-4-me toxy) phenyl) ethyl] pipe razin-2-acetamide; 1- (cyclohexyl) aminoc-rbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3- in zodi-oxol-5-yl) ) methyl] piperazin-2-acetamide; 1- (cyclohexyl) amylcarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (l, 3-) eno-dioxol-5-yl) ethyl] piperazine- 2-acetamide; 1- (cyclohexyl) ami'ocarbonyl-4- [6 (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3-jenzodioxol-5-yl) ethyl] piperazin- 2-carboxamide; 1- (cyclohexyl) amin carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl) ] pipera zin-2 -carboxai Ida; 1- (cyclohexyl) aminoi. Rbonyl-4- [6-met il-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [(1,4-enzodioxan-6-yl) methyl] piperazine-2-carboxamide; 1- (cyclohexyl) aminoc. Rbonyl-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [(1,4-enzodioxan-6-yl) methyl) ] pipera zin-2 -carboxamide; 1- (cyclohexyl) aminocubonyl-4- [6-chloro-2- (IH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-enzodioxan-6-yl) methyl] piperazin -2-acetamide; 1- (cyclohexyl) amino. .rbonyl-4- [6-trif luoromet i 1-2- (1H-imidazol-1-yl) pyrimidine-. - i 1] - N - [(1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamidr; 1- (cyclohexyl) aminoc i rbonyl- 4- [6-chloro-2- (lH-imide zol-l-yl) pyrimin din-4-yl] -N- [2- t -methoxyphenyl) ethyl] piperazin-2 -carboxamide; 1- (cyclohexyl) aminoc-rbonyl-4- [6-methyl-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-enzodioxan-2-yl) methyl] piperazine-2-carboxamide; 1- (cyclohexyl) amin oarbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-1-yl] -N - [(1,4-benzodioxan-2-yl) methyl) ] piperazine-2-carboxy-ida; 1- (cyclohexyl) amin carbonyl-4- [6-iso-propyl-2- (1 H -i? Idazol-1-yl) pyrmidin-4-yl] - N - [(2,3-dimethoxy phenyl) methyl] piper azi; -2 -carboxamide; 1- (cyclohexyl) aminoc i rbonyl- 4- [6-chloro-2- (lH-imide zol-1-yl) pyrimin din-4-yl] -N - [(2,2-dimethoxyphenyl) methyl] piperazine- 2-carboxamide; 1- (phenylsulfonyl) < ninocarbonyl-4- [6-chloro-2- (1H-imide z ol-1-yl) pi ri i di n-4-yl] -N - [2 - (3,4-dimethoxy phenyl) ethyl] piperazine - 2 -acet amí da; 1- (phenylsulfonyl). ainocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(4-ethoxyphenyl) methyl] piperazin-2-acetamide; 1- (phenylsulfonyl) arcarbonyl-4- [2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] piper a zin-2 -acet amide; 1- (phenylsulfonyl) ninocarbonyl-4- [6-chloro-2- (1H-i m i d a z or l-1-i l) p i r m i d i n-4-i l] - N - [2 - (4-methylphenoxy) ethyl] piperazin-2-acetamide; 1- (phenylsulfonyl) c ninocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(4-methylfenyl) methyl] piperazin-2-acetamide; 1- (phenylsulfonyl) < ? inocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimid n-4-yl] -N- [2- (3-chloro-4-methoxyphenyl) ethyl] piperazin-2-acetamide; 1- (phenylsul fonyl) c-ninocarbonyl-4 - [6-methyl-2 - (1H-imidazol-1-yl) pyrimidin-1-y1] - N - [(1,3-benzodioxol-5-yl) methyl] ] piperazin-2-acetam a; 1- (phenylsulfonyl), ninocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazine -2-carboxa ^ da; 1- (phenylsulfonyl) r ninocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin- 2 -carboxar ¡.da; 1- (phenylsulfonyl), ninocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazine -2-acetamyl '-i, -1- (phenylsulfonyl), ainocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrim? Din-¿l] -N- [2- (1 , 4-benzodioxan-6-yl) ethyl] piperazin-2-acetamid; 1- (phenylsulfonyl) ai .carbonyl-4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (1, 4-) enzodioxan-6-yl) ethyl] pipera zin ^ -acetamide; 1- (phenylsulfonyl) < ninocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] N - [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- (phenylsulfonyl), ninocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrmidin-4-yl] - N - [(2,5-dimethoxyphenyl) methyl] pipe razi '-2 -acetamide; l- [2- (Thien-2-yl) ethyl -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-y) methyl] ] piper a zin -2 -carboxamide; l- [2- (Thien-2-yl) et 1] -4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3- b nzodioxol-5-yl) methyl] piperazin-2-carboxamide; l- [2- (Thien-2-yl) ethyl -4- [6-? so-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4- t nz odi oxan-6-yl) methyl] piperazin-2-acetamide; l- [2- (Thien-2-yl) et l] -4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4 -t nzodioxan-6-yl) methyl] pipera zin-2-carboxamide; l- [2- (thien-2-yl) et l] -4- [6-chloro-2- (lH-imide zol-l-yl) pyrimyne-4-yl] -N- [(2,3 - li methoxyphenyl) methyl] piperazine-2-acetamide; 1- [2- (thien-2-yl) etiJ -4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclo-ro-pyl) methyl] ] piperazin-2-acetamide; 1- (4-methoxy phenyl) ninocarbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl-N - [(4-chloro-enyl) methyl] piperazine-2-carboxamide; 1- (4-methoxyphenyl) ai Anocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (2, -dimethoxy-enyl) ethyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) n -carbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) methyl] pipera zin-2-carboxa Lda; 1- (4-methoxy-enyl) -ai -carbonyl-4- [2- (lH-imidazol-1-yl) -pyridin-4-yl] -N- [2- (1, 3-) -cyclodol-5-yl) ethyl] piperazin-2-acetamide; 1- (4-methoxy phenyl) ai .carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-t nzodioxan-6-yl) methyl] piperazine-2-carboxamide; 1- (4-methoxyphenyl) ninocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazine -2-carboxy .da; 1- (4-methoxyphenyl) -nocarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-1-yl] -N- [2 - (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamid '; 1- (4-methoxyphenyl) ai r_carbonyl-4- [2- (1 H-imidazol-1-yl) pyrimidin-4-yl] - N - [(1, methoxyphenyl) methyl] piperazin-2-acetamide; 1- (3,4-dichlorophenoxycarbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyridin-4-yl] -N- [2- (3, 4-dimethoxyphenyl) ethyl] piperazin-2-acetamide; 1- (3,4-dichlorophenyl-aminocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3- ^ enzodioxol -5-yl) ethyl] piperazin-2-acetamide: 1- (3,4-dichlorophenyl) minocarbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1 , 4-b nzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- (3,4-dichloropheni aminocarbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-) il] N- [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- (3,4-dichlorophenyl) myocarbonyl-4- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,5-! Imethoxyphenyl) methyl] piperazine-2-carboxamide; 1- (methoxy) carboni -4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl ] -N- [2- (3, -dimethoxyphenyl) ethyl] piperazin-2-acetamide; 1- (methoxy) carboni -4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-) il] -N- [2- (3, -dimethoxyphenyl) ethyl] piperazine-2-carboxamide; 1- (methoxy) carboni -4 - [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] - N - [(3-cyano) -4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- (methoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-chloro- 4 -me toxy phenyl) ethyl] piperazin-2-acetamide; l- (methoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1- -1) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazin-2-acetamide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl ] piperazin-2-acetamide; 1- (methoxy) carbonyl -4- [2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4-benzodioxan-6-yl) ethyl] pipera zin- 2-carboxamide; 1- (methoxy) carbonyl-4- [2- (lH-imide zol-1-yl) py imidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] pipera zin -2 -acetamide; 1- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazine-2-carboxamide; l- (me toxi) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperazin-2- carboxamide; l- (methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] piperazin-2 -carboxamide; 1- (iso-propoxy) carbonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2 -carboxamide; 1- (iso-propoxy) carbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] piperazine-2-carboxamide; 1- (iso-propoxy) carbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazine-2-carboxamide; 1- (iso-propoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2 acetamide; 1- (iso-propoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazine-2-carboxamide; 1- (Iso-propoxy) carbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [[(3,4-dimethoxyphenyl) methyl] piperazine-2 -carboxamide; 1- (iso-propoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazine- 2-carboxamide; 1- (iso-propoxy) carbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (cyclopropyl) piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2 acetamide; 1- (n-butoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 3-benzodioxol-5-yl) ethyl] piperazine- 2-acetamide; 1- (n-butoxy) carbonyl-4 [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl) ] piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2-acetamide; 1- (n-butoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazin-2- acetamide; 1- (n-butoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazin-2- carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-iso-propyl-2- (1H-imide zol-1-yl) pyrimidin-4-yl] -N- [3- (4-dimethoxyphenyl) propyl] piperazine-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5-yl) ethyl] piperazine-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6) -yl) methyl] piperazin-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [(4-benz odi oxan-6-yl) methyl] piperazine-2-carboxamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan- 6 -yl) ethyl] pipera zin-2-acetamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazin-2-acetamide; 1- (2- (methoxy) ethoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-methoxyphenyl) ethyl] piperazine -2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2- acetamide; 1- ((phenyl) methoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ) methyl] piperazin-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- ((phenyl) methoxy) carboni 1-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan- 6 -yl) ethyl] piperazine-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-meth i 1-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazin-2-acetamide; 1- ((phenyl) methoxy) carbonyl-4- [6-met il-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazine -2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-iso-propyl-2- (1H-imi dazol-1-yl) pyri my din-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazin-2-acetamide; 1- (4-methoxyphenyl) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine -2-acetamide; 1- (4-methoxyphenyl) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2-acetamide; 1- (4-methoxyphenyl) carboni 1-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5- il) ethyl] pipera zin-2-carboxamide; 1- (4-methoxyphenyl) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2 -acetamide; 1- (4-methoxy phenyl) carbonyl-4- [6-met i 1-2- (lH-imidazol-1-yl) pyrimin din-4-yl] -N- [(4-benzodioxan-6-yl) methyl] piperazine-2-carboxamide; 1- (4-methoxy phenyl) carbonyl-4- [6-met il-2- (lH-imide zol-l-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazin-2 -acetamide; 1- (4-methoxyphenyl) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] piperazin-2-carboxamide; l- (pyridin-3-yl) carbonyl-4- [6-met il-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (3,4-dimethoxy phenyl) ethyl] piperazin-2-acetamide; l- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) methyl] piperazine-2-carboxamide; 1- (pyridin-3-yl) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piper to zin-2-acetamide; 1- (phenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; l- (Phenoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy-enyl) methyl] piperazine -2-carboxamide; 1- (4-methoxyphenoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,3-benzodioxol-5-yl) methyl] pipera zin- 2 -carboxamide; 1- (4-methoxyphenoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazin-2-carboxamide; l- (4-methoxyphenoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine- 2-acetamide; 1- (4-methoxyphenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] pipera zin-2-carboxamide; 1- (4-methoxyphenoxy) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] pipera zin- 2 -carboxamide; 1- (4-methoxyphenoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4-benzodioxan-6-yl) ethyl] pipera zin -2 -carboxamide; 1- (4-methoxyphenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazin-2- acetamide; 1- (4-methoxyphenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] piperazin-2 -carboxamide; 1- (4-methoxy phenoxy) carboni 1-4- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxy phenyl) methyl] piperazine-2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-iso-propyl-2- (1H-i my dazol-1-yl) pyri my din-4-yl] - N - [2 - (4-methylphenoxy) ethyl] piperazine-2-carboxamide; l- ((phenyl) methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methylphenoxy) ethyl] piperazin-2 -carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] pipera zin- 2-carboxamide; 1- ((phenyl) methoxy) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) methyl] piper to zin-2 -acet amide; l- ((phenyl) methoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] ] piperazin-2-carboxamide; 1- ((phenyl) methoxy) carboni 1-4- [6-met il-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol- 5-yl) ethyl] piper to zin-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl] pyridin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl) ] piperazin-2-acetamide; 1- (1-methylpropoxy) carbonyl-4- [5-chloro-2- (lH-imidazol-1-yl] pyrimidin-4-yl] -N- [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- (1-methylpropoxy) carboni 1-4- [6- (lH-imide zol-l-yl] pyrimidin-4-yl] -N- [ (1,3-benzodioxol-5-yl) methyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidine- 4- il] -N-. {(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazole -1-yl] pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazin-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6- ( lH-imidazol-1-yl] pyridin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [ 2- (1H-imidazol-1-yl] pyrimidin-4-yl] -N- [1- (1, 4-benzodioxan-6-yl) ethyl] pipe ra zin-2-acetamide; (1-methylpropoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl] pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-carboxamide; 1- (1-methylpropoxy) carbonyl-4- [6-methyl-2- (lH-imidazol-1-yl] pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] piperazin-2- acetamide; 1- (phenoxy) carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2- (3,4-dimethoxyphenyl) ethyl) ] piperazin-2-acetamide; 1- (phenoxy) carbonyl-4- [6-methyl-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N-. {2- (3, 4-dimethoxyphenyl) ethyl] piperazine-2-acetamide; 1- (phenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- ( 3,4-dimethoxyphenyl) ethyl] piperazine-2-acetamide; 1- (phenoxy) carbonyl-4- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3- benzodioxol-5-yl) methyl] piperazine-2-carboxamide; 1- (phenoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(furan-2- il) methyl] piperazin-2-acetamide; 1- (phenoxy) carbonyl-4- [6-met i 1-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4-benzodioxan-6-yl) methyl] piperazine-2-carboxamide; l- (phenoxy) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4-b Enzydoxan-6-yl) methyl] piperazine-2-carboxamide; 1- (phenoxy) carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,4-benzodioxan-6-yl) ethyl] piperazin-2- carboxamide; 1- (pyridin-3-yl) carbonyl-4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol- 5-yl) ethyl] piperazin-2-acetamide; l- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; l- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1, 4-benzodioxan- 6 -yl) ethyl] piperazin-2-acetamide; l- (pyridin-3-yl) carbonyl-4- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [2- (4-methoxy phenyl) ethyl] piperazine-2-carboxamide; 1- [2- (4-methoxyphenyl) ethyl] -A- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N-2- (3-chloro- 4 -me toxy phenyl) ethyl] pipera zin-2-carboxamide; l- [2- (4-methoxy phenyl) ethyl] -4- [6-methyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol -5 -i 1) methyl] piperazine-2-carboxamide; 1- [2- (4-methoxyphenyl) ethyl] -4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol- 5-yl) methyl] pipera zin-2-acet amide; 1- [2- (4-methoxyphenyl) ethyl] -4- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5- il) methyl] piperazin-2-acetamide; l- [2- (4-methoxyphenyl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine-2-carboxamide; 1- [2- (4-methoxyphenyl) ethyl] -4- [6-iso-propyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan- 6-yl) methyl] piper a zin- 2 -a ce tarruda; 1- [2- (4-methoxyphenyl) ethyl] -A- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piper to zin-2-carboxamide; 1- [2- (4-methoxy phenyl) ethyl] -A- [6-met il-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) me useful] piperazine-2-carboxamide; 1- [2- (4-methoxyphenyl) ethyl] -A- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperazine-2-carboxamide; 1- [2- (4-methoxyphenyl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimin-din-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazin-2 -carboxamide; 1- [(3,4-dichlorophenyl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pi imidin-4-yl] -N- [2- (3, A-dimethoxyphenyl) ethyl] piperazine-2-acetamide; 1- [(3,4-dichlorofenyl) ethyl] carbonyl-4- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylfine) ) methyl] pipera zin-2-carboxamide; l- [(3,4-Dichlorophenyl) methyl] carbonyl-4- [6-methyl-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzadioxole -5-yl) ethyl] piperazin-2-acet amide; 1- [(3,4-dichlorofenyl) ethyl] carbonyl-4- [6-chloro-2- (1H-imide z ol-1-yl) pir imi din- 4 -i 1] -N- [( 3, 4, 5 -tr ime tox ifenil) methyl] pipera zin-2 -carboxamide; 1- [(3,4-Dichlorophenyl) methyl] carbonyl-4- [6-chloro-2- (lH-i my dazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ) methyl] piperazin-2-carboxamide; l- [(1,3-Benzodioxol-5-yl) methyl] carbonyl-4- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (3 , 4-dimethoxyphenyl) ethyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3- (3,4-dimethoxyphenyl) propyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3- (3, 4-dimethoxy-enyl) -propyl] -piperazin-2-acetamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5) -yl) methyl] piper to zin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [( 1,3-benzodioxol-5-yl) methyl] pipe razin-2-carboxamide; l- [(1, 3-Benzodioxol-5-yl) methyl] carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5-yl) ethyl] piperazin-2-acetamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxole -5-yl] piperazin-2-acet amide; 1- [(1, 3-benzodioxol-5-yl) methyl] carbonyl-4- [6- (1H-imidazol-1-yl) pyrimidin-4-yl] ] -N- [2- (1, 3-benzodioxol-5-yl) ethyl] piperazin-2 -carboxamide; 1- [(1,3-benz odi-oxol-5-yl) methyl] -carbonyl-4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) met i lpiperazin-2-carboxamide; 1- [(1,3-benz odi oxo-5-yl) methyl] carbonyl-4- [6-met il-2 - (lH-imi da zol-1-yl) pi r imi di n-4-yl] -N - [(4 - methoxyphenyl) methyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6-iso-propyl-2- (lH-imidazol-l-yl) pyrimidine -4-yl] -N- [(4-methoxy phenyl) methyl] piperazin-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carbonyl-4- [6- (1H -imidazol-1-yl) pyrimidin-4-yl] -N - [(4-methoxy phenyl) methyl] piperazine-2-carboxamide; 1- [(1,3-benzodioxol-5-yl) methyl] carboni 1-4- [ 6-chloro-2- (lH-imi da z or l-1-i l) p i r imi d i n-4-i l] - N - (2-phenylcyclopropyl) pipera zin-2 -carboxamide; 1-methylsulfonyl-4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (1,3-benzodioxol-5-yl) ethyl] piperazine-2-carboxamide; N - [(3,4-dimethoxy phenyl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(3,4-dimethoxyphenyl) methyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-2-acetarruda; N - [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imide zol-l-yl) pyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidin-2-acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-2-acetamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N - [(4-methoxy phenyl) ethyl] -1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(3,4-dihydroxyphenyl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N-octyl-1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- (phenoxypropyl) -1- [2- (1H-imidazol-1-yl) -6-methyl-pyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(pyridin-3-yl) ethyl] -l- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N- [(morpholin-4-yl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidine-2-carboxamide; N - [(2 (methoxypyridin-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidine-2-carboxamide; N- [(2 ( methylpyridin-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidine-2-carboxamide; N- [(1,3-benzodioxol-5- il) ethyl] -2 - [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino} acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] ] -2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] acetamide; 2- [[- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] -N-octylacetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imide zol-l-yl) -6-methylpyrimidin-4-yl] (phenylmethyl) amino] acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2- [[2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] amino] acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2- [[2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-yl] [(1,3-benzodioxol-5) -yl) methyl] amino] acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino} acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] [(morpholin-4-yl) ethyl] ] amino] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) pyrimidin-4-yl] (methyl) amino] acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methylethyl) amino] acetamide; N- [(1,3-benz odi-oxol-5-oxy) ethyl] -2 - [[2- (lH-imide zol-l-yl) -6-methylpyrimidin-4-yl] (methyl) amino] acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2- [[4- (lH-imide zol-1-yl) -6- (methylethyl) pyrimidin-2-yl] amino] acetamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -2- [[4- (lH-imide zol-l-yl) -6-methylpyrimidin-2-yl] amino] acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -3- [[2- (lH-imidazol-1-yl) -6-met ilpyrimidin-yl] amino] propionamide; 4- [(4-trifluoromethylphenyl) methyl] -3- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] propionamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -3- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] propionamide; N- [(1, 3-benzodioxol-5-oxy) ethyl] -2- (lH-imidazol-1-yl) pyrimidopyrimidin-4-amine; N- [(1,3-benzodioxol-5-yl) ethyl] -4- [1- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -l- (2-methyl-1- oxopropyl) piperazin-2-acetamide; N- [(4-methoxy phenyl) ethyl] -4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl) -6-methylpyrimidin-4-yl] -1- (2 - methyl-1-oxopropyl) piperidin-2-acetamide; N- [(4-nitrophenyl) methyl] -l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N- [[4- (acetylamino) phenyl] methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperazin-2-acetamide; N- [[4- (methylsulfonylamino) phenyl] methyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N - [(2,3-dihydrobenzofuran-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N - [(indan-5-yl) methyl} -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetamide; N- [(3-chloro-4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4- (1-oxopropyl) piperazine-2-acetamide; N- [(4-methoxyphenyl) aminocarbonyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-methanamine; N - [(1, 3-benzodioxol-5-yl) methylcarbonyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-methanamine; N- [(4-methoxyphenoxy) carbonyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl} piperidin-2-methanamine; N - [(4-methoxyphenyl) methylcarbonyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-methanamine; N- [(1,3-benzodioxol-5-yl) carbonyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] piperidin-2-ethanamine; 2,4-bis (lH-imidazol-1-yl) -6-methylpyrimidine; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) -5-methylpyrimidin-4-yl] -4- (phenylmethyl) piperazin-3- acetamide; N - [(3,4-dimethoxyphenyl) ethyl] -6- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N-me ti 1-5, 6, 7, 8-tetrahydropyrido [ 5, 6-c] pyrimidin-4-amine; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) methyl] -4-methylthiobutanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] -4-methylthiobutanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(4-methoxyphenyl) methyl] -4-methylsulfonylbutanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (butylthio) butanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N - [(c i c l or p r o p i l) m e t i l] - 3 - [(3,4-dimethylphenyl) methylthio] propanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(2,5-dimethoxy phenyl) methyl] -3-met il-3- [( phenylmethyl) thio] butanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N - [(4-chlorophenyl) methyl] -3-thiophenpropanamide; 5- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N - [(1,3-benzodioxol-5-yl) methyl] pentanamide; 5- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,4-benzodioxol-6-yl) ethyl] pentanamide; 7- [[2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [2-phenylcyclopropyl] heptanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] - [(3-chloro-4-methoxyphenyl) ethyl] acetamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] acetamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] amino] -N- [(1,4-benzodioxan-6-yl) ethyl] acetamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(4-methoxyphenyl) ethyl] acetamide; 4- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-yl] amino] -N- [(1,3-benzodioxol-5-yl) ethyl] butanamide; 2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] -N- [(4-chlorophenyl) ethyl] pyridine-3-propanamide; 2- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] isoquinoline-3-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] piperidin-2-acetard; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-methylphenyl) methyl] piperidin-2-acetarruda; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] piperidin-2-acetamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] thiomorpholin-2-acetamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] thiomorpholin-2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] piperazine-2 -acetamide; 4- [(dimethylethoxy) carbonyl] -l- [2- (lH-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] piperazine -2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] piperazine-2-acetamide; 4- [(dimethylethoxy) carbonyl] -1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] pyrimidine-3-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] pyrimidine-3-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] pyrimidine-3-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] pyrimidine-3-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] pyrimidine-3-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] pyrimidin-3-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] piperidin-3-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] piperidin-3-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] piperidin-3-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] piperidin-3-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperidin-3-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] piperidin-3-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] piperidin-3-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] piperidin-3-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] pyrrolidine-2-carboxamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] pyrrolidine-2-carboxamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-y1] -N- [(4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] -N- [(1,3-benzodioxol-5-yl) ethyl] acetamide; 1- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] (methyl) amino] -N- [(1,4-benzodioxan-6-yl) ethyl] acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) ethyl] -4-methylpiperazine-2-carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] -4-methylpiperazine-2-carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4-methylpiperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-methylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-methoxyphenyl) methyl] -4-methylpiperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-methoxyphenyl) ethyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-pyrimidin-4-yl] -N- [[4- (2-methoxyethoxy) phenyl) methyl] -4-methylpiperazine-2-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-methylpiperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(cyclopropyl) methyl] -4-methylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(indal-5-yl) methyl] -4-methylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,3-benzodioxol-5-yl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-butylpiperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; l [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) ethyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-butylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2- acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- [(-methoxyphenyl) methyl] piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(4- methoxyphenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] - A - [(4-methoxyphenyl) methyl] piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- [(4-methoxyphenyl) methyl] piperazine -2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-trifluoromethyl-4-yl] -N - [(2-phenylcyclopropyl) -4- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxy phenyl) methyl] piperazine- 2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(3,4-dichlorophenyl) methyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- [(3,4-dichlorophenyl) ) methyl] piperazin-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(3, 4) phenyl) useful] piperazine-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4 - [(3, 4 - dichlorophenyl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4 - [(3,4-dichlorophenyl) ) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(3,4-di chlorophenyl) me useful] pipera zin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) -pyridin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- [(3,4-dichlorophenyl) methyl] piperazine -2-acetamide; l- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4 - [(1,3-benzodioxol-5-yl ) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pi r imidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(1,3-benzodioxol- 5-yl) methyl] pipe razin-2-acet amide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) ethyl] -4 - [(1,3-benzodioxole -5- il) met il] pipera z in-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4 - [(1,3-benzodioxol -5-yl) methyl] pipera zin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(1, 3- benzodioxol-5-yl) methyl] piper to zin-2-acet amide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(1,3-benzodioxol-5- il) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4 - [(1, 3- benzodioxol-5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4 - [(1,3-benzodioxol-5- il) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4 - [(1,3-benzodioxol -5-yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- [(1,3-benzodioxol-5-yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imide zol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(1,4-benzodioxan- 6-yl) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(1,4-benzodioxan-6-yl) ) methyl] pipera zin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4 - [(1,4-benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,5-dimethoxy phenyl) methyl] -4 - [(1,4-benzodioxan-6) -yl) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] - A - [(1, 4- benzodioxan-6-yl) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- [(1, -benzodioxan -6-yl) methyl] piper to zin-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- [(1,4-benzodioxan- 6- il) methyl] piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(1,4-benzodioxan-6-yl) methyl] pipera zin -2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4 - [(1,4-benzodioxan-6-yl) ) methyl] piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thiophenyl) ethyl] -4 - [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-acetamide; 1- [2- (lH-imide zol-1-yl) -6-trif luoromet ilpyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] -4- [(1,4-benzodioxan- ß-il) methyl] piperazin-2-carboxamide; 1- [2- (lH-imidazol-1-yl) -6-met ilpyr imidin-4 -i 1] -N- [(1-adamantyl) methyl] -4- [(1,4-benzodioxan-6 il) methyl] piperazine-2-carboxamide; 1- [2- (IH-imidazol-1-yl) pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- [(1,4-benzodioxan-6-yl) methyl] piperazine- 2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) propyl] -4- [(pyro-3- il) methyl] pipera zin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazin-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -A- [(pyridin-3- il) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -A- [(pyridin-3- il) methyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(pyridin-3- il) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(pyridin-3-yl) ) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridine- 3-yl) methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3- il) methyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3-yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(pyridin-3-yl) ) methyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazin-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,6-dimethoxyphenyl) methyl] -4 - [(pyridin-3-yl) methyl] piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- [(piri di n-3 -yl) methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- [(pyridin-3-yl) methyl] piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(3-fluoro-4 -methoxyphenyl) -methyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4 - [(3-fluoro- 4-methoxyphenyl) -methyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(3-fluoro-4-methoxyphenyl) ) -methyl] piperazin-2-acetamide; l- [2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(3-fluoro-4 -methoxyphenyl) -methyl] piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 4-benzodioxan-6-yl) ethyl] -4- [(3-fluoro-4-methoxyphenyl) -methyl] piper to zin-2 -acet amide; 1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- t-urene-phenyl) -ethyl] -4- [(3-fluoro-4-methoxy-phenyl) -methyl] -piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -A - [(3-fluoro-4-methoxyphenyl) methyl] piperazine -2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxypheniDmethyl] -4- [(3-fluoro-4-methoxyphenyl) methyl] piperazin-2- acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(l-adamantyl) methyl] -4- [(3-fluoro-4-methoxyphenyl) methyl] piperazine- 2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- [(3-fluoro-4-methoxyphenyl)] methyl] piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4-acetylpiperazine- 2-acetamide: 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4-acetylpiperazine-2-acetamide; - [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H -imidazol-1-yl) -6-methylpyrimidin-4-y1] -N - [(4-ethoxyphenyl) methyl] -4-acetylpiperazine-2-acetacrudate; 1- [6-chloro-2- (1H-imidazole- 1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methylphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) ethyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [2- (1H-Imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(3,5-dimethoxyphenyl) ethyl] -4-acetylpiperazine-2-carboxamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4-acetylpiperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4,5-trimethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-acetylpiperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-1-yl] - N - [(1,4-benzodioxan-6-yl) ethyl] -4-acetylpiperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4-acetylpiperazine-2-acetarruda; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-difluorophenyl) ethyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4-acetylpiperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2-phenylcyclopropyl) -4-acetylpiperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) -4-acetylpiperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(indal-5-yl) methyl] -4-acetylpiperazin-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (3-methyl-1-oxo-butyl) piperazine -2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin- -i1] - N - [(4-methoxyphenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (3-methyl-l-oxobutyl) piperazin-2 -acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (3-methyl-l-oxobutyl) piperazin-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (3-methyl-l-oxobutyl) ) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (3-methyl-l-oxobutyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (3-methyl-l-oxobutyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (3-methyl-l-oxobutyl) pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (3-methyl) -1-oxobutyl) piperazine-2-carboxamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (3-methyl-l-oxo-butyl) piperazine -2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (3-methyl-l-oxobutyl) piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (3-methyl-l-oxobutyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (3-methyl 1- 1-oxobutyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (3-methyl-1-oxobutyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- (3-methyl-l-oxobutyl) piperazin-2 -acculent; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (3-methyl-l-oxo-butyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (3-methyl-1-oxobutyl) piperazine-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (3-methyl-l-oxobutyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-y1] -N- [([4- (2-methoxyethoxy) phenyl) ethyl] -A- (3-methyl-1-oxobutyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-2-yl) ethyl] -4- (3-methyl-1) -oxobutyl) piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(2-phenylcyclopropyl) ethyl] -A- (3-methyl-l-oxobutyl) piperazine-2-carboxamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxy phenyl) methyl] -4- (3-methyl-l-oxobutyl) piperazin-2-acetamide; l- [2- (1 H-imidazol-1-yl) pir imidi n-4-yl] -N- [(indal-2-yl) ethyl] -4- (3-met il-1-oxobutyl) piperazin -2 -carboxamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (indal-5-yl) ethyl] -4- (3-met il-1-oxobutyl) pipera zin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, 4-dimethoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazine -2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) ethyl] -4- (2-methoxy-l-oxoethyl) piperazine-2 -acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-i1] -N- [(4-ethoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] - A - (2-methoxy-1-oxoethyl) piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazin-2 -acculent; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazin-2- acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-y1] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (2-methoxy-1-oxoethyl) ) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-methoxy-1) -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-methoxy-l- oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-methoxy) -1-oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (2-methoxy-l-oxoethyl) piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy-1) -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy-l- oxoethyl) piperazin-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy) -1-oxoethyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-methoxy-1-oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (2-methoxy-1) -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (2-methoxy-l- oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2-methoxy-1-oxoethyl) piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyridin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2-methyl-1 -oxoethyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- (2-methoxy-1-oxoethyl) pipera zin- 2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (2-methoxy-1-oxoethyl) pipera zin -2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyridin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (2-methyl-oxy) -1-oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(indal-5-yl) methyl] -4- (2-methoxy-1-oxoethyl) pipera zin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (tetrahydro-3-furanyl) ) pipera zin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, -dimethoxy phenyl) propyl] -4- (tetrahydro-3-furanoyl) pipera zin-2-acetamide; 1- [2- (1H-imide zol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(4-ethoxyphenyl) ethyl] -4- (tetrahydro-3-furanyl) piperazine-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methyl-enyl) -ethyl] -A- (tetrahydro-3-furanoyl) -piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-methylphenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2- acetamide; l- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2- acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -A- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-chlorophenyl) methyl] - (4-tetrahydro-3-furanoyl) piperaz in-2 -acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-chlorofenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) pipera zin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4 -i 1] -N- [(4-methoxy-3-chlorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) ) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4- (tetrahydro-3-furanoyl) pipera zin- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (tetrahydro-3-furanoyl) ) piperazin-2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (tetrahydro-3-furanoyl) ) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-di methylphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazine- 2-acetamide; 1- [2- (1 H-imidazol-1-yl) pyrimidin-4-yl] -N- [(pyridin-3-yl) methyl] -4- (tetrahydro-3-furanoyl) piper a zin-2 -carboxamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (tetrahydro-3) -f uranoyl) pipera zin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (tetrahydro-3-furanoyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxy phenyl) methyl] -4- (tetrahydro-3-furanoyl) pipera zin-2 -acetamide; l- [6-chloro-2- (lH-imide zol-l-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; l- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4-tetrahydro-3-furanoyl) piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-difluorophenyl) ethyl] -4- (tetrahydro-3-furanoyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) piperazin-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] -4- (tetrahydro-3-furanoyl) pipera zin-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (2-carboxymethoxy-1-oxoethyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) butyl] -4- (2-carboxymethoxy-1 - oxoethyl) piperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) -pyridin-4-y1] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (2-carboxymethoxy-1) -oxoethyl) piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- (2-carboxymethoxy-l- oxoethyl) piperazin-2-acet amide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benz odi-oxol-5-yl) methyl] -4- (2-carboxymethyl) -1 -oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) ethyl] -A- (2-carboxymethoxy-l-oxoethyl) piperazine -2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2-carboxymethyl) -1-oxoethyl) piperazin-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -A- (2 -carboximet oxy- 1-oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (2-carboxymethoxy-1-oxoethyl) piperazine- 2-acetamide; l- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazine- 2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,4-dimethoxy phenyl) methyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazin-2- carboxamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,6-dimethoxyphenyl) methyl] -4- (2-carboxymethoxy-1-oxoethyl) ) piperazin-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2,6-dimethoxyphenyl) methyl] -4- (2-carboxymethoxy-l-oxoethyl) piperazine-2-carboxamide; l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- (2-phenoxy-1-oxoethyl) ) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) propyl] -4- (2-phenoxy-1-oxoethyl) piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -A- (2-phenoxy-1-l- oxoethyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (2-phenoxy-l) -oxoethyl) piperazin-2-acetamide; 1- [2- (lH-imi da zol-l-yl) -6-trif luoromet i Ipyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] - A - (2-phenoxy-1) -oxoethyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methoxy-enyl) -methyl] -4- (2-phenoxy-1-oxoethyl) pipera zi n-2 -acet amide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (2-phenoxy-1-oxoethyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy-phenylethyl) -4- (pyridin-3-ylcarbonyl) piperazin-2- acetamide; 1- [2 (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-di methoxyphenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) propyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) butyl] -A- (pyridin-3-ylcarbonyl) piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4-methyl phenoxy) methyl] -4- (pyridin-3-ylcarbonyl) pipera zin- 2 -acetamide; 1- [6-Chloro-2- (1H-imidazol-1-yl) -pyridin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazin-2- acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (pyridin-3-ylcarbonyl ) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-me toxy -3-chloro or phenyl) ethyl] -4- (pyro- 3-i Icarboni 1) pipera zin-2-acetamide; 1- [2- (lH-imide zol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4-me t-oxy-3-chlorofenyl) ethyl] -4- (pyro] - 3 -ylcarbonyl) pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met-il-pyrimidin-4-yl] -N- [(2,5-di-toxy-phenyl) -ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (pyridin-3-ylcarbonyl ) piperazin-2-acetamide; 1- [2- (lH-imi da zol-l-il) pi rimidin-4 -yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -A- (pyridin-3-ylca rbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-carboxamide; 1- [2- (lH-imidazol-1-yl) -6-met-il-pyrimidin-4-yl] -N- [(2,5-dimethyl-phenyl) -methyl] -4- (pyridin-3-i-Icarboni 1) pipera zin-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -A- (pyridin-3-ylca rbonyl) pipe razin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (pyridin-3 -i) Icarboni 1) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (pyridin-3-ylca rbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (pyro- 3- ilcarbonyl) piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine-2 -acetamide; l- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4 -i 1] -N- [(4-methoxyphenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazine-2 -acetamide; 1- [6-Chloro-2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N- [(2-methoxyphenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazin-2 -carboxamide; l- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (pyridin-3 -i lea rbonil) pi pera zin-2 -acet ami da, • l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2-thionyl) ethyl] -4- (pyridin- 3 - ilcarbonyl) piper a zin-2 -carboxamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-difluorophenyl) ethyl] -4- (pyridin-3-ylcarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (pyridin-3-ylcarbonyl) ) pipera zin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (pyridin-3-ylcarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (2- (4-methoxyphenyl) ) -1-oxoethyl] -piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] piperazine-2-carboxamide; l- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [ (4-methoxy-3-chlorophenyl) methyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] -piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) - 6-methylpyrimidin-4-yl] - N - [(4-methoxy-3-chlorophenyl) methyl] - A - (2- (4-methoxyphenyl) -1-oxoethyl] -piperazine-2-acetarruda; 1- [2 - (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] piperazine-2 -acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3,5-dimethoxyphenyl) ethyl] -4- (2- (4-methoxyphenyl) -1- oxoethyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4 - (2- (4-methoxyphenyl) -1-oxoethyl] piperaz in-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethyl-1-yl) methyl] -4- (2- (4-methoxy-phenyl) ) -1-Oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethyl-yl-enyl) -methyl] -4 - (2- (4-methoxy phenyl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N- [(3,4-Dimethylphenyl) ethyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] -piperazin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-trif luorome ti Ipyrimidin-4-yl] - N - [(3-pyridinyl) methyl] -4- (2- (4-methoxyphenyl) -1-oxoethyl] piperazin-2 -carboxamide; l- [ 6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (2- (4-methoxy-enyl) - 1-oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6) -yl) methyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] -pipe-2-acet-amide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2- (4-me toxy phenyl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methoxy phenyl) methyl] -4- (2- (4-methoxy phenyl) ) -1-oxoethyl] pipera zin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3-methoxy phenyl) ethyl] -4- (2- (4-methoxy) phenyl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -A- (2 - (4-methoxyphenyl) -1-oxoethyl] piperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1-methylpyrrol-2-yl) ethyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] piperaz in-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl ] -N- [(3,4-dimethoxy phenyl) methyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] pipera zin-2-acetamide; 1- [2- (lH-imide zol-1-yl) -6-trif luorome ti lpi r imidin-4-lyl] -N- [(3,4-di methoxyphenyl) methyl] -4- (2- (4-methoxy phenyl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(2, 5-dimethoxy-f-enyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-carboxamide; l- [6-chloro-2- (lH-imidazol- l-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] pipe ra zin-2 -acet amide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2- (1, 3 -benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2-methyl-phenyl) methyl] -4- (2- ( 1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [6- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ) ethyl] - A - (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acet amide; l- [2- (lH-imidazol-l-yl) pyrimidin-4- il] -N- [(4-chlorofenyl) methyl] - A - (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [6-chloro-2 - (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazine -2-acetamide; l- [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) ethyl] -A- (2- (1, 3 -benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(4 -methoxy-3-chlorophenyl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazine-2-acetamide; 1- [2- (lH-imidazol-1-yl) ) -6- (Methylethyl) pyrimidin-4-yl] -N- [(3,5-dimethoxy) l) ethyl] -4- (2- (1,3-benzodioxol-5 -i 1) -1-oxoethyl] pipe razin-2-carboxamide; l- [2- (lH-imide zol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2- (1 , 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (2- (1 , 3-benzodioxol-5-yl) -1-oxoethyl] pipe ra zin-2 -acet amide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) ethyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2 -acet amide; 1- [6- (lH-imidazole-1 -yl) pyrimidin-4-yl] - N - [(3, 4-dimethylphenyl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -A- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan- 6-yl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [2- (lH-imide zol-1-yl) - 6 -methylpiyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazine-2-acetamide; - [6-chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- [2- (1,3-benzod) ioxol-5-yl) -1-oxoethyl] pipe razin-2 -acet amide; 1- [2- (1 H-imidazol-1-yl) -6-trif luoromet i Ipyrimidin-4-yl] -N- [(3-methyl-phenyl) ethyl] -4- (2- (1, 3 -benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (2- (1,3-benzodioxol-5) -yl) -1-oxoethyl] piperazin-2 -acetic acid; 1- [2- (lH-imide zol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2- thienyl) ethyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2 -acet amide; 1- [2- (lH-imidazol-1-yl) -6- methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] pipera zin-2 - acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-di-methoxyphenyl) methyl] -4- (2- ( 1,3-benzodioxol-5-yl) -1-oxoethyl] piper to zin-2 -acet amide; 1- [2- (lH-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piper to zin-2 -acetamide; l- [2- (lH-imide zol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(2-indanyl) methyl] -4- (2- (1,3-benzodioxol-5-yl) -1-oxoethyl] piperazin-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (2- (1, 3-benzodioxol-5-yl) -1-oxoethyl] pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- (2- (1,3-benzodioxol-5 -yl) -1 -oxoethyl] piperazin-2 -carboxamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (methylsulfonyl) piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy-3-chlorophenyl) methyl] -4- (methyl sulphyl) piperazine-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (methylsulfonyl) piperazine-2 -acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -A - (methylsulfonyl) piperazine-2-acetarruda; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-6-yl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-6-yl) ethyl] -4- (methylsulfonyl) piperazin-2- acetarruda; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-6-yl) ethyl] -4- (methylsulfonyl) piperazine-2 -acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (methylsulfonyl) piperazine-2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazin-2 -acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazin-2 acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methylsulfonyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (methylsulfonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (methylsulfonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (methylsulfonyl) piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (methylsul fonyl) piperazin-2 -acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (methylsulfoyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (octylsulfonyl) piperazin-2-acetamide; 1- [6-Chloro-2- (lH-imidazol-1-) l) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- (octyl sul phonyl) piperazine -2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) ethyl] -4- (octyl sulphonyl) piperazin- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (octylsulfonyl) piperazine -2-acetamide; l- [2- (lH-imidazol-1-yl) -5-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (octylsulfonyl) piperazine-2- acetamide; 1- [2- (1H-imidazol-1-yl) oyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (octylsulfonyl) piperazine-2-acetarruda; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] -4- (octylsulfonyl) piperazin-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (octylsulfonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methyl-pyrimidin-1-yl] - N - [(4-methoxyphenyl) methyl] -4- (octylsulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) ethyl] -4- (octylsulfonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl] -4- (octylsulfonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxy phenyl) ethyl] -4- (dimethylaminosul fonyl) piperazin-2 acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethylpyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) ethyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- (dimethylaminosulfonyl) piperazin-2 acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (dimethylamine sulfonyl) piperazine-2 -acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazine -2-acetamide; l- [2- (IH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazin-2 acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) ethyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-? M? Dazol-1-? L) p? Pm? Dm-4-? L] -N- [(1,4-benzod? Oxan-6-? ) met? l] -4- (d? met am? sulfon? l) p? peraz? n-2-acetanuda; l- [2- (lH-? m? dazol-l-? l) -6-met? lp? r? m? dm-4-? l] -N- [(1,4-benzod? oxan-6 -? l) met? l] -4- (dimethyl aminosulfon? l) p? peraz? n-2-acetamide; l- [2- (lH-? m? dazol-1-? l) -6- (methylethyl) p? pm? dm-4-? l] -N- [(1,4-benzod? oxan-6- ?) methyl] -4- (dimethylaminosulfonyl) piperaz-2-carboxamide; l- [2- (lH-? m? dazol-l-? l) p? pm? d? n-4-? l] -N- [(1,4-benzod? oxan-6-? l) til] -4- (dimethylamino its Ifonil) p? perazm-2-acetamide; l- [6-chloro-2- (lH-? m? dazole -? -? l) p? pm? d? n-4-? l] -N- [(1,4-benzod? oxan-6- ?) ethyl] -4- (dime ti lamí nosul fon íl) p? peraz? n-2-acetamida; 1- [6-chloro-2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [(4-methoxyphenyl) methyl] -4- ( dimethylammosulfonyl) p? peraz? n-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? Dm-4-? L] -N- [(4-methox? Phen? L) meth? ] -A- (dimethylar? Nosulfon? L) p? Peraz? N-2-acetamide; 1- [6-chloro-2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [(4-methoxyphenyl) methyl] -4- ( dimethylaminosulfonyl) pipera z? n-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] -4- (dimethylaminosulfonyl) piperazine- 2-carboxamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(2,3-dimethoxyphenyl) methyl] -4- (dimethylaminosul fonyl) pipera zin-2- acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (dimethylaminosulfonyl) pipera zin-2 acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4- (dimethylaminosulfonyl) piperazin- 2 -acetamide; l- [2- (1H-Imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,5-di methoxyphenyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-adamantyl) methyl] -4- (dimethylaminosulfonyl) piperazine-2-carboxamide; 1- [6- (1H-imidazol-1-yl) pyrimin-din-4-yl] -N- [(2,3-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -A- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) ethyl] -A- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) propyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-di e-toxi phenyl) butyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxy-phenyl) -methyl] -4- (propylaminocarbonyl) piperazin- 2 - acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acet amide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methylphenoxy) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -ι-1-pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- tr if luoromet i Ipyrimidin-4-yl] -N- [(4-methyl phenoxy) ethyl] -4- (propylaminocarbonyl) piper a zin- 2 -carboxamide; l- [6-Chloro-2- (1H-imidazol-l-ii) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (propylammocarbonyl) piperazin-2 -acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (propylaminocarbonyl) pipera zin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-chlorophenyl) ethyl] -4- (propylaminocainyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-1-l) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- (propylaminocarbonyl) piperazine-2- acetamide; 1- [2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -N - [(3-chloro-4-methoxy phenyl) methyl] -4- (propylaminocarbonyl) -piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) - '- methylpyrimidin-4-yl] - N - [(3-chloro-4-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (propylaminocarbonyl) piperazin-2- acetamide; 1- [(2- (1H-imi daz ol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] - A - ( propylaminocarbonyl) piperazin-2-c-atamide; l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] ] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- (propy p -minocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5- il) ethyl] -4- (propylaminocarbonyl) piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethylphenyl) ) methyl] -4- (propylaminocarbonyl) piperazin-2 -acetamide; l- [2- (lH-imidazol-li]) t) irimidin-4-yl] -N- [(1,4-benzodioxan-6-) il) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (prop? Lam? nocarbonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminoca rbonyl) piperazin- 2-acetamide; l- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (propylaminocarbonyl) piperazine -2-acetamide; l- [2- (lH-imidazol-1-? l) -o-met? lpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; l- [2- (lH-? midazole-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (propylaminocarbonyl) piperazine-2 -acetamide; l- [2- (lH-imidazol-1-? l) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (propylaminocarbonyl) pipera zin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl-4- (propylamino rbonyl) piperazin-2 -acetamide; 1- [6-chloro-2- (lH-imi a zol-1 -i 1) pyr imidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (propylamino-oonyl) -piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-methoxyphenyl) ethyl] -4- (propylaminod bonyl) piperazine-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (propylaminecarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(2-methoxyphenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidaz-l-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-thienyl) ethyl] -4- [propylaminocarbonyl) piperazine-2-carboxamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3,4-di fluorophenyl) ethyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazc-i-yl) pyrimidin-4-yl-N- [(1,4-benzodioxan-2-yl) methyl] -4- (propylaminocarbonyl) piperazin-2- acetamide; l- [2- (lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] -4- (propylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1 H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] -4-propylaminocarbonyl) pipera zin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,5-di methoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] -4-propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [3,4-dimethoxyphenyl) methyl] -4- (propy'-aminocarbonyl) piperazin-2- acetamide; l- [2- (lH-imide zol-l-yl) -6-methylpyrimidin-4-yl] -N- [3,4-dimethoxyphenyl) methyl] -4- (propylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [(3,5-dimethoxyphenyl) methyl] -4 - (propii or incarcarbonyl) peratin-2-acetamide; l- [2- (lH-? m? dazol-l-? l) p? r? m? dm-4-? l] -N- [(3,5-d? methox? phen? l) met? l] -4- (propylaminocarbonyl) p? peraz? n-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) -6-tr? F luoromet? Lp? Pm? D? N-4-11] -N- (cyclopropyl) -4- (propi. Auiinocarbonyl) p? peraz? n-2-acetamide; l- [2- (lH-? m? dazol-l-? l) p? r? m? d? n-4-? l] -N- (2-? ndan? l) -4- (propylaminocarbonyl) piperazine z-2-acet amide; l- [6-chloro-2- (lH-? m? dazol-1-? l) p? r? m? d? n-4-? l] -N- [(5-indanyl) methyl] -4 - (propylaminocarbonyl) pipe razm- 2 -acet amide; l- [2- (lH-? m? dazol-1-? l) - et? lp? pm? d? n-4-? l] -N- [(3,4-d? methox? phen? l ) et? l] -4- (cyclohexylammocarbonyl) p? perazm-2-acetamide; 1- [6-chloro-2- (lH-imidaz-l-yl) p? R? M? Dm-4-? L] -N- [(4-ethoxy? Phen? L) meth?] -4- (c? clohex lam? nocarbon? l) p? perazm-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? L] -N- [(4-ethoxy? Phen? L) met ? l] -4- (cyclohexylaminocarbonyl) piperaz? n-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [(4-ethoxy? Phen? L) met? L] -4 - (c? clohex? lam? nocarbon? l) p? peraz? n-2-acetamida; 1- [2- (1H-imidazol-1-yl) -6-met ilpyrimidin-4-yl] -N- [(4-methyl-phenoxy) ethyl] -4- (cyclohexylaminocarbonyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imiaa zol-1-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide; 1- [ß-chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(4-chloro-phenyl) -ethyl] -4- (cyclohexyl ami-noca-rbonyl) piperazin-2 -acetamide; 1- [2- (1H-imidazol-1?) Oir imidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- (cyclohexyl) ^ m -carbonyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- (cyclohex and laminocarbonyl) pipera zin -2-acetamide; l- [2- (lH-imidazol-1-l) -6-methylpyrimidin-4-yl] -N- [(3-cl-4-methyl-4-methoxy-phenyl) ethyl] -4- (cyclohexylaminocarbonyl) pipera z in-2-carboxamide; 1- [2- (1H-imidazol-1 [beta]) pyr imidin-4-yl] -N - [(3-chloro-4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- (cyclohexy and aminecabonal) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2 -acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxo-1-5-yl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2 -acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (cyanohexylaminocarbonyl) piperazine-2- acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (cycloh << <; ... laminocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-ii) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] - A - (cyclohexylaminocarbonyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met-1-pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- (cyanohexylaminocarbonyl) piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1? I) -6-methylpyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (cyclohexyllaminocarbonyl) piperazin- 2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-chloro-2- (1H-imi-zol-1-yl) -pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; 1- [6-Chloro-2- (lH-imide zol-1-yl) pyrimidin-4-yl] -N- [(2-methoxyphenyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazin-2- acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-difluorophenyl) methyl] -4- (cyclohexylaminocarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(2,5-dimethoxyphenyl) methyl] -4- (cyclohexalacarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1? L) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) metii _ -4- (cyclohexylaminocarbonyl) piperazin-2- acetamide; l- [6-Chloro-2- (lH-imidazo-^ -yl) pyrimidin-4-yl] -N- [(2,5-dimethoxy phenyl) methyl] -4- (cyclohex? laminocarbonyl) piperazine-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) methyl-4 - (cycloalkylaminocarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- (2-indanyl) -A- (cyclohexylaminoca bonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-imiaa zol-1-yl) pyrimidin-4-yl] - N - [(4-ethoxyphenyl) methyl] -4- (phenylsuifoniiaminocarbonyl) piperazin-2-acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (phenylsulfonylaminocarbonyl) piperazine- 2-acetamide; l- [5-Chloro-2 (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (phenylsul phonylaminocarbonyl) piperazine-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (phenylsulfonylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1 H -imidazol-1-yl) -6-trifluoromethyl-4-yl] -N - [(2,3-di-me-to-phenyl) -methyl] -4- (phenylaminocarbonyl) piperazine-2 - to j-ooxamide; l- [2- (lH-imidazol-1-? l) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxy phenyl) ethyl] -4- (phenylaminocarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) propyl] -4 - (f ~ m laminocarbonyl) piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (phen-laminocarbonyl-piperazine-2-acetamide; - [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(4-ethoxyphenyl) methyl] -4- (phenylamino-r onyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; 1- [ 6-Chloro-2- (lH-imiaa zol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (phenylalaninecarbonyl) piperazine-2-acetarruda; 1- [2- (lH-imidazol-1-yl) -methyl-pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1? 1) -6-methylpyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- (lH-im? Dazol-1-yl) pyrimidin-4-yl-N- [(4-chlorophenyl) methyl] -4- (phenylammoxyl) piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(4-chlorophenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-chlorophenyl) ethyl] -4- (phenylaminocarbonyl) piperazine-2-carboxamide; l- [6-Chloro-2- (lH-imiaazol o-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- (phenylaminocarbonyl) piperazin-2- acetamide; l- [2- (lH-imidazol-1-yl) -6-tnfluoromethyl-4-yl] -N- [(3-chloro-4-methoxy-phenyl-1-yl] -4- (phenylaminocarbonyl) piperazine] -2- j.boxamide; l- [6-Chloro-2- (lH-im? dazol-1-yl) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenyl) ethyl] -4- (phenylaminocarbonyl) piperazine-2- acetamide; 1- [6-chloro-2- (lH-im? Dazol-1-? L) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- (remlam? nocarbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-i-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (phen? lam-nocarbonyl) piperazine-2 -acetamide; 1- [2- (1H-imidazol-1-U) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (phenylaminocarbonyl) piperazin-2 acetamide; l- [6-Chloro-2- (lH-im? dazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (in Ummocarbonyl) piperazin-2-acetamide; l- [6- (lH-? midazole-l-? l) pyr_midin-4-yl] -N- [(1, 4-benzodioxan-6-yl) methyl] -4- (phen? lam? nocarbonyl) piperazine -2-acetamide; 1- [2- (1H-imidazol-1? I) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (phen? Xm? Nocarbonyl) piperazine -2-acetamide; 1- [6-chloro- 2- (lH-? M? Dazol-1-? L) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (phenyl anu nca rbonyl) pipera zin-2-acetamide; l- [6-chloro-2- (lH-? m? Jazol-l-? l) pyr imidin-4-yl] -N- [(3-methoxifenyl) methyl] -4- (f -nylcarunoyl) pipera zin -2 -acet amide; 1- [2- (1H-imidazol-1-U) -6 -methylpiyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (phenylaponcarbonX) piperaz in-2 -acet amide; l- [2- (lH-imidazole-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) ethyl] -4- (f enylmethyl) pipera razin-2 -acet amide; 1- [2- (1H-imidazol-1-? U p? Pmidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (phenylaminocarbonyl) piperazine-2-acetamide; l- [2 - (lH-imidazol-1-yl) pyrimidin-4-yl-N- [(3-thienyl) ethyl] -4- (phenylaminocarlronyl) p? perazin-2-acetamide; 1- [6-chloro-2- ( lH-im? adZ? l-1-? l) pyrimidin-4-yl] - N - [(3, 4-difluorophenyl) methyl] -4- (fe ni larr nocarbonyl) pipera zin-2-acetamide; - 33 l- [6-chloro-2- (lH-? M? Oazol-1-? L) p? R? M? Din-4-? L] -N- [(2,5-dimethoxyphenyl) me useful ] -4- (phenylaminocarbonyl) p? Perazin-2-acetamide; 1- [6-chloro-2- (lH-? RPi.dazolo-l-? L) p? R? M? D? N-4-? L] -N- [(3,4-dimethoxy phenyl) metu] -4- (f -arylaminocarbonyl) piperazin-2-acetamide; l- [2- (1H-? m? dazol-1-? l) -6- (methylethyl) p? rim? dm-4-yl] -N- [(3, -dime-phenyl) -methyl] -4 - (f eni lamí noca rbonil) piperazin-2-acetamide; l- [6- (lH-? md? dazol-l-? l) p? pm? din-4-yl] -N- [(cyclopropyl) met? l] -4- (fen? lam? nocarbon) ?) prazeran-2-carboxamide; l- [6-chloro-2- (lH-? m? azole-l-? l) p? pm? din-4-? l] -N- [(5-indanyl) methyl] -4- (f enylaminoocc rbonyl) p iper az? n-2-acet amide; l- [6- (lH-? m? dazol -.-? l) p? pm? d? n-4-? l] -N- [(2,3-dimethoxyphenyl) ethyl] -4- [(4 -met? if enyl) ai noca rbonyl] piper to zm-2-carboxamide; 1- [2- (lH-? M? Dazol-1-a.) -6- (metil til) p? Pm? Din-4-? L] -N- [(2, 3-d? Methox? phenol) ethyl] -4 - [(4-methoxy-enyl) -ammocarbonyl] pip ^ razin-2 -carboxamide; 1- [6-chloro-2- (lH-? M? Aazol-1-? L) p? R? M? D? N-4-? L] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-meA.ox: phen? L) am ocarbonyl] pipera zin-2-acetam? Da; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- ['4-methoxy-phenol) aminocarbonyl ] piperazin-2-acetamide; 1- [2- (lH-? Midazoi-1-? L) p? R? Midin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- [(4-methoxy-xenyl) aminocarbonyl] piperazine- 2-acetamide; l- [6-Chloro-2- (lH-yl-yl-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenoxy) ethyl] -4- [(4-methoxyphenyl) aminocarbonyl] ] piperazin-2-acetamide; l- [2- (lH-imidazol-lX) -6-tr? fluoromethy1-pyrimidin-4-yl] - N - [(4-methylphenyl) methyl] -A - [(4-methoxyphenyl) aminocarbonyl] p? perazin-2 -acetamide; 1- [2- (lH-imidazol-1-? L) p? R? Midin-4-yl] -N- [(4-chlorophenyl) met? L] -4- [(4-met? / Renyl) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-l pi r? m? d? n-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4- [(4-met ??? ifenyl) aminocarbonyl] piperazine-2-carboxamide; 1- [2- (lH-imidazol-1-? l) ir? m? d? n-4-yl] -N- [(3-chloro-4- methoxyphenyl) methyl] -4- [(4-methoxy-phenyl) aminocarbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-. 1) -6-me ti Ipyrimidin-4-yl] - N- [(3-chloro-4-methox? Phen?) Methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] p? PA-razin-2-acetamide; l- [6-Chloro-2- (lH-im? dazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) ethyl] -4 - [(4 - methoxyphenyl) aminocarbonyl] pip raz-n-2-acet amide; l- [6-chloro-2- (lH-? m? aazol-1-? lj p? rimidin-4-yl] -N- [(2,5-dimethoxyphenyl) ethyl-4- [(4-metho <? phenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazole -.-? l) p? rimidin-4-yl] -N - [(2,5-dimethoxyphenyl) ethyl] -4 - [(4-met-j? Ifenyl) aminocarbonyl] piperazine-2-carboxamide; l- [2- (lH-imidazole-1-l) p? R? Midin-4-yl] -N - [(1) , 3-benzodioxol-5-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] p? Perazin-2-acetamide; 1- [2- (lH-imidazol-1-y) -6- ( methylethyl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [2-] 6-met? Lpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-l) methyl] -4 - [(4-methoxyphenyl) aminocarbonylpiper? -2 -carboxamide; 1- [6-chloro] -2- (lH-? M? Aazol-1-? L) p? Rimidin-4-yl] -N- [(1,3-benzodioxol-5-l) methyl] - A - [(4-methoxyphenyl) aminocarbonyl] p? pr.razin-2-acetamide; l- [2- (lH-? m? dazoi-l-? l) p? pmidin-4-yl-N- [(l, 3-b) e n z o d i or x o l - 5 -? l) e t i l] -4 - [(4-methoxyphenyl) aminocarbonyl] piperazin-2 -acetamide; - roo - 1- [6-chloro-2- (lH-imidazol-1-? l) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl)] - A - [(4 -methoxyphenyl) aminocarbonyl] pi 'a zin-2 -acetamide; 1- [2- (lH-imidazol-li.) -6-met i Ipyrimidin-4-yl] -N- [(1,3-benzodioxol-5 -? l) ethyl] - A - [(4-methoxy phenyl) aminocarbonyl] piperazin-2-acetamide; 1- [6-chloro-2- (lH-im? c, azol-i-yl) pyrimidine- 4-yl-N- [(3,4-dimethylphenyl) methyl] -4- [(4-metho? Phen?) Aminocarbonyl] piperazine-2-acetamide; l-6- (lH-imidazolU-yl) pyrimidin-4-yl] -N - [(3,4-dimethylphenyl) methyl] -4- [(4-methyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-furyl) methyl] -4- [(4-methoxy-fe il) am- nocarbonyl] piperazine- 2-acetamide; l- [2- (lH-? midazole -_-? l) p? r? midin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4 - [(4 -methoxyphenyl) aminocarbonyl] pip -ua zin-2 -acet amide; l- [6-chloro-2- (lH-imia ^ zol-l-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) meti 1] - A - [( 4-methoxyphenyl) aminocarbonyl] -foot-2-acetamide; 1- [2- (1H-imidazol-1-.) -6-wnetylethyl) pyrimidin-4-yl] -N- [(1,4-benzodioxa-6-yl) methyl] - A - (4 - methoxyphenyl) aminocarbonyl 1 pipara zin-2-cet amide; - X6-l- [2- (lH-imidazol-1-yl) -6-met? Ipyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl] ethyl] - A - [ (4-methoxyphenyl) aminocarbonyl] pi A- -1 .. in -2 -acetamide; l- [2- (lH-imidazole -: -? L) p? Rimidin-4-yl] -N- [(l, 4-benzodioxan-6-yl) ethyl] - A - [(4-methoxyphenyl) aminocarboni jp? Perazin-2-acetamide; l- [6-chloro-2- (lH-im? • zol-1-? ) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4 - [(4-methoxyphenyl) aminocarbonyl] p? p-razine-2-carboxamide; l- [2 - (lH-imidazol-1-) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(4-methyl X emi) ami noca rbonyl] pipera zin-2 -acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- [(4-methoxy-phenyl) aminocarbonyl] piperazine- 2-acetamide: 1- [2- (1H-imidazol-1- ^ X -6-methy1-pyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- [(4-methyl Xenyl) aminocarbonyl] piperazin-2-acetamide; l- [6-chloro-2- (lH-? m_Jazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) eti l] -4- [(4-methox. phenyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) ethyl] -4- [(4-meth? phenyl) aminocarbonyl] piperazine-2-acetamide; - r57 - 1- [2- (lH-? midazol-1-) -6- (methylethyl) pyrimidin-4-yl] - N - [(1,4-benzodioxa - - 2 -? l) ethyl] - 4 - [(4-methoxyphenyl) aminocarbonyl] piperazin-2-acetamide; l- [5-chloro-2- (lH-? m? dazo] -l-yl) pyrimidin-4-yl] -N- [(2,3-dimethoxyphenyl) methyl] -4- [(4-meth roxyphenyl) aminocarbonyl] piperazine-2-acetamide; l- [6-chloro-2- (lH-? mi '=. zol-1-? l) pyrimidin-4-yl-N- [(2,5-dimethoxyphenyl) methyl] -4- [(4-methox fen? l) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-L) -6-met? l-pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methyl-oxyphenyl) aminocarbonyl] ] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imi, zol-1-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methyl-oxyphenyl) aminocarbonyl] piperazine-2-acetamide; 1- [6-chloro-2- (lH-i: dazol-1-yl) pyrimidin-4-yl] -N- [(cyclopropyl) methyl] -4- [(4-me roxyphenyl) aminocarbonyl] piperazine-2 -acetamide; 1- [6-chloro-2- (lH-? _ Azol-1-? L) pyrimidin-4-yl] -N- (2-indanyl) -4- [(4-methoxy phen i 1) ar mocarbonyl] pipe ra zin-2 -acet amide; 1- [2- (1H-imidazol-1-U) -6-methyl-1-pyrimidin-4-yl] -N- [(5-indanyl) methyl] -4- [(4-methox-enyl) aminocarbonyl] ] piperazin-2-acetamide; -: tí - l- [2- (lH-imidazol-1 i) -o-methylpyrimidin-4-yl] -N - [(3,4-dimethoxyphenylethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl ] piperazin-2-acetarruda; l- [6-chloro-2- (lH-im ?: > -.zol-l-yl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ^ or ^ l] - A - [(3,4-dichlorophenyl) aminocarbonyl] p-cerazin-2-acetamide; l- [6-chloro-2- (lH-imi- ~ yol-l-yl) pyrimidin-4 -yl] -N- [(3,4-dimethoxyphenylutyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] picerazine -acetamide; 1- [2- (lH-imidazole-1- •.) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-ethoxyphene)) i]] - 4 - [(3,4-dichlorophenyl) aminocarbonyl] pi r erazin-2 -acetamide; 1- [2- (lH -imidazole-1-U) -6-methy1-pyrimidin-1-yl] -N- [(4-ethoxyphenyl) methyl] -4- [(3,4-dio-orphe-1-aminocarbonyl] piperazine-2-acetamide; 6-chloro-2- (lH-im., Ozol-i-yl) pyrimidin-4-yl] -N- [(4-methylphenoxy) ethyl] -4- [(3,4-dicl-phenyl) aminocarbonyl] piperazine -2-acetamide; 1- [2- (lH-imi dazol-1- i) -6-mer and Ipyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(3, -di:. phenyl) aminocarbonyl] piperazine-2-acetamide; 1- [6-chloro-2- (lH-im; - a zol-1-yl) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- [(3, 4-di or orofe il) aminocarbonyl] piperazin-2-acetamide; - 39 - 1- [2- (lH-imidazol-1-yl-pyrimidin-4-yl] - N - [(4-chlorophenyl) methyl] -4- [(3,4-d? R U? aminocarbonyl] piperazine-2-acetamide; l- [6-chloro-2- (lH-? m-azol-l-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4 - [(3, 4-d? C.rrofeml) aminocarbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-lU) pyrimidin-4-yl] -N- [(3-chloro-4 -me toxy phenyl) methyl] -4 - [(3,4-d? orofen-1 '' aminocarbonyl] piperazine-2-acetamide; l- [6-chloro-2- (lH-im? .- zol-1-? l) pyrimidin-4-yl] -N- [(2,5-dimethoxyphenylmethyl] -4 - [(3, 4-di chlorofenyl) aminocarbonyl] pi e ra zin -2 -acet amide; l- [6-chloro-2- (lH-imi -.zol-1-? L) pyrimidin-4-yl] -N- [ (1,3-benzodioxol-5 -:) meti 1] - 4 - [(3, A-dichlorophenyl) aminocarbonyl] p: ee? Az? N-2 -acetamide; l- [2- (lH-imidazol-1 -A) -6-methylpyrimidin-4-yl-N- [(1,3-benzodioxol-5-y) methyl]] - 4 - [(3,4-di chlorofenyl) aminocarbonyl] p:. 1-acetamide; l- [2- (lH-imidazoI- ^ 1) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] - A - [(3 , A-dichlorophenyl) aminocarbonyl] p: erazin-2-acetamide; l- [6-chloro-2- (lH-i: zol-1-? L) pyrimidin-4-yl] -N- [(1,3 -benzodioxol-5-l) etl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] p: reason -2 -acetamide; - 60 - l- [2- (lH-imidazol-1- '.7 -6-methylpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-. 1) ethyl] -4 - [( 3,4-dichlorophenyl) aminocarbonyl] p.? Ra zin -2 -acet amide; l- [6-chloro-2- (lH-im? ... zol-i-yl) pyrimidin-4-yl-N- [(3,4-Dimethylphenyl) methyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] pr e-n-2 -acetamide; l- [2- (lH-imidazoy-yl) pyrimidine-4- il] -N- [(1,4-benzodioxan-6-yl) me "il] -4 - [(3,4-dichlorophenyl) aminocarbonyl]: - e-reason in -2 -acetamide; 1- [6- chloro-2- (lH-? m?:, azol-l-yl) pyrimidin-4-yl] - N - [(1,4-benzodioxan-6-yl) methyl] - A - [(3, 4 -dichlorophenyl) aminoca bonyl] p. e raz. -2 -acetamide; 1- [2- (lH-imidazol-1.) -6-met? lpyrimidin-4-yl] -N- [(1,4 -benzodioxan-6-1) ethyl] -4 - [(3, A-dichlorophenyl) aminocarbonyl] p '. -razir.-2-acetamide; 1- [2- (lH-imidazof-i-yl) pyrimidine- 4-yl] -N- [(4-me toxi phenyl) methyl] -4- [(3, 4-di-orofenii) aminocar bonil] pipera z in-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(3,4-di-Drophenyl) aminocarbonyl] piperazine -2-acetamide; 1- [6-chloro-2- (lH-i: .azol- -11) pyrimidin-4-yl] -N- [(4-methyloxy phenyl) methyl] -4- [(3,4-di-Drofenil aminocarbonyl] piperazin-2-acetamide; - 61 - 1- [2- (IH-imidazo. - _ - i 1, pyrimidin-4-yl] - N - [(3-methoxyphenyl) methyl] -4 - [(3,4-d-orophenyl) aminocarbonyl ] piperazin-2-acetamide; 1- [2- (1H-im? dazol- -.) -6 -methylpyrimidin-4-yl] -N- [(3-methoxyphenyl) methyl] -4- [( 3, Ad-orophenyl) aminocarbonyl] piperazine-2-acetamide; 1- [6-chloro-2- (lH-i-1, 1- 1) pyrimidin-4-yl] -N- [(-me toxy phenyl) ethyl] -4 - [(3,4-d? _. Propyl) aminocarbonyl] piperazine-2-acetamide; l- [2- (lH-im? Dazol-1- 1-6- (methylethyl) pyrimidin-4-yl) ] -N- [(2, 5-dimethoxy? Pheyl) methyl] -4- (3,4-dichlorofenyl) aminocarbonyl _ -raz? N-2-acetamide; l- [2- (lH-im? dazol-1-, - 6-met ilpyrimidin-4-yl] - N - [(2,5-dimethoxyphenylmethyl] -4 - [(3,4-dichlorophenyl) aminocarbonyl] p. razm-2-acetamide; l- [ 6-chloro-2- (lH-ip rol-1.) P? Rim? Din-4-yl] -N- [(2,5-dimethoxyphenylethyl) -4 - [(3, A -dichlorophenyl) aminocarbonyl] p : erazm-2-acetamide; 1- [2- (lH-im? dazol-1-, -6-met? lpyrimidin-4- il] -N- [(3,4-d i m e t o x i f e n? l n e t • 1] - 4 - [(3,4-di chloro phenyl) ami noca rbonyl _, e raz -2 -acetamide; l- [2- (lH-imidazole-) p? rimidin-4-yl] -N- [(3,4-dimethoxyphenylmethyl) -4 - [(3, A-dichlorofenyl) aminocarbonyl] p erazi '- ". -acetamide; - -62- l- [2- (lH-imidazol-1-6- et? Lpyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] - A - (met-arbonyl) p Perazine-2-acetamide: 1- [6-chloro-2- (lH-i-azol-1- (1-yl) pyrimidin-4-yl] -N- [(4-ethoxyphenyl) methyl] -4- (methoxycycloon) 'piperazin-2-acetamide; l- [6-chloro-2- (IH-im "zol- ^ -1) pyrimidin-4-yl] -N- [(4-methylphenyl) methyl] -4- (methoxy) oonyl i piperazin-2-acetamide; 1- [6-chloro-2- (lH-im., azole-1-? l) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- (methoxy oonyl) piperazin-2-acetamide; 1- [6-chloro-2- (lH-ir a zol-i-U) pyrimidin-4-yl-N- [(3-chloro-4-methoxy phenyl) met 1I] - - (methoxycarbonyl) piperazin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl-N- [(3-chloro-4-methox-phenyl)] ethyl- - (meth i oxycarbonyl) piperazin-2-acetamide; l- [6-chloro-2- (lH-? mL ol-1-? l) pyrimidin-4-yl] -N- [(1, 3- benzodioxol-5-yl) methyl] -4- (me <? caroonil) piperazin-2-acetamide; l- [6-chloro-2- (lH-irr- -.zol-l-yl) pyrimidine-4- il] -N [(1,3-benzodioxol-5-yl) ethyl] -A - (only - Icarronyl) piperazin-2-acetamide; 1- [2- (1H-imidazol- ± - 6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl-4- (methylne) piperazine-2-acetamide; l- [2- (lH-imidazo-yl) p? rimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- (methacryl) piperazine-2 -acetamide; l- [6-chloro-2- (lH-in. ^ ol-i-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- (me carbonyl) piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- (methoxycarbonyl) piperazin-2- acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -A- (methoxycarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(4-methoxyphenyl) methyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl 'pyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (methoxycarbonyl) piperazine-2-acetamide; 1- [ 2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] -4- (methoxycarbonyl) piperazine-2-acetamide; l- [6-chloro- 2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methoxyphenyl) ethyl] -4- (methoxycarbonyl) piperazine-2-acetamide; 1- [6-chloro-2- ( lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-2-yl) methyl] -A- (methoxycarbonyl) piperazine-2-acetamide; l- [2- (lH -imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) methyl] -4- (methoxycarbonyl) piperazin-2-acetamide; 1- [2- ( lH-imidazol-l-yl) -6-met ilpyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) met il] - 4 - (meth i letoxi ca rboni l) pipe ra z in-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- (me ti toxycarbonyl) piperazin-2 -acetamide; l- [2- (1H-imidazol-1-yl) -pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -A- (butoxycarbonyl) piperazine-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl-N - [(1,4-benzodioxan-6-yl) methyl] -4- (butoxycarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (butoxycarbonyl) piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- (butoxycarbonyl) piper a zin-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, 4-di fluorophenyl) methyl] -4- (butoxycarbonyl) pipera zin-2 -carboxamide; 1- [6-Chloro-2- (1H-imi-zol-1-yl) -pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [2- (IH-imide zol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-chloro-4-methoxy phenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] ] piperazin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] - A - [(2 - methoxyethoxy) carbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] -4- [(2-methoxyethoxy) carbonyl ] piperazin-2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazin-2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(2-methoxyethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(2-methoxyethoxy) carbonyl ] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) ethyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -5-methylpyrimidin-4-yl-N- (1,4-benzodioxan-6-yl) ethyl] -4- (2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxyphenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine-2- acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] - A - [(2-methoxyethoxy) carbonyl] piperazine-2 -acetamide; l- [6-Chloro-2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(3,5-dimethoxyphenyl) methyl] -4- [(2-methoxyethoxy) carbonyl] piperazine- 2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-chlorophenyl) methyl] -4- [(phenylmethoxy) carbonyl-Jpiperazin-U-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1, 3-benzodioxol-5-yl) methyl] -4- [(phenylmethoxy) carbonyl] piperazin-2- acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2- acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,3-benzodioxol-5-yl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(phenylmethoxy) carbonyl] piperazin-2- acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(1, 4-benzodioxan-6-yl) methyl] -4 - [(phenylmethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(phenylmethoxy) carbonyl] piperazine -2-acetamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) methyl] -4- [(phenylmethoxy) ca rboni lpipe raz in-2 -acetamide; 1- [6- (lH-imi da zol-l-yl) pyrimin-din-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(phenylmethoxy) carbon il-Piperazin-U- carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) methyl] -4- [(phenylmethoxy) carbonyl] piperazine-2-acetamide; l- [6-Chloro-2- (2H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-methoxy phenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-met i Ipyrimidin-4-l-N- [(4-methoxyphenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(2-thienyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine-2-acetamide; l- [6-Chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl-N- [(3,4-dimethoxy phenyl) ethyl] -A- [(phenylmethoxy) carbonyl] piperazine- 2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N - [(3,4-dimethoxyphenyl) ethyl] -4- [(phenylmetoxy) carbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) ethyl] -4- [(phenylmethoxy) carbonyl] piperazine- 2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) methyl] -4- [(1-methylpropoxy) carbonyl] pipera zin -2 -acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [(1, 3-benzodioxol-5-yl) ethyl] -4- [(1-methylpropoxy) carbonyl] pipe in-2-acetamide; 1- [6-chloro-2- (1H-imidazol-1-yl) pir imidin-4-yl] -N- [(4-methoxyphenyl) methyl-4- [(1-methylpropoxy) carbonyl] piperazin-2- acetamide; l- [6-Chloro-2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-chloro-4-methoxyphenyl) methyl] -4 - [(4-methoxy phenoxy) carbonyl ] pipera zin-2 -carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(3, 4, 5-tr ime toxi nyl) useful] - 4 - [ (4-methoxyphenoxy) carbonyl] piperazine-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-trifluoromethyl-4-y1] - N - [(1,4-benzodioxan-6-yl) methyl] -4- [(4-methoxyphenoxy)] carbonyl] piperazine-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(1,4-benzodioxan-6-yl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine- 2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1,4-benzodioxan-6-yl) ethyl] -4- [(4-methoxyphenoxy) carbonyl] ] piperazin-2-acetamide; l- [6- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-methoxyphenyl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(1-methylpyrrol-2-yl) ethyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine -2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] -N- [(2,4-dimethoxyphenyl) methyl] -4 - [(4-methoxyphenoxy) carbonyl] piperazine-2-carboxamide; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [(2,6-dimethoxyphenyl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine- 2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3,4-dimethoxyphenyl) methyl] -4- [(4-methoxyphenoxy) carbonyl] piperazine-2 -carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- [1- (phenylmethyl) piperidin-4-yl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-cyanocyclohexyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- (2, 2-dimethoxyethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethyl-1-pyrimidin-4-yl-N-trideeylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(2-hydroxy-4-methylthiobutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N, N- [bis (2-cyanoethyl)] piperidin-2-acetamide; 1- [2- (1H-imide zol-1-yl) -6-methyl-1-pyrimidin-4-yl] -N, N- [bis (2-cyanomethyl)] piperidin-2-acetamide; 1- [2- (IH-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(4,4-diethoxybutyl) piperidin-2-acetamide; 1- (4-fluorophenyl) -4- [1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] piperazine; l- [(1, 3-Benzodioxol-5-yl) methyl] -4- [l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] piperazine; 1- (phenylmethyl) -4- [1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -piperidin-2-acetyl] piperazine; 4- [1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] piperazine-1-carboxylic acid ethyl ester, 1- (4-chlorophenyl) -4- [l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] -4-hydroxypiperidine; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2,3-dihydrobenzofuran-5-yl) methyl) piperidin-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? D? N-4-? L] -N- [(mdan-5-? L) methyl) pipen din-2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? D? N-4-? L] -N- [(cyclohexyl) methyl] p ipe ridm- 2 -acet amide; 1- [2- (lH-? M? Dazol-l-? L) p? Pm? D? N-4-? L] -N- [(1,2,3,4-tetrahydronaf talen-il ) pipe pdm-2 -acet amide; 1- [2- (lH-? M? Dazol-l-? L) p? R? M? D? N-4-? L] -N- [(naf talen- 1-íl) useful) pipe ridm - 2 -early; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? Dm-4-? L] -N- [(1,3-benzod? Oxol -5-? L) methyl] piper din-2-acet knots; 1- [(2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? Pm? D? N-4-? L] -N- [(4-chlorophen? L) met? l] pipe pdm- 2 -acet amide; 1- [2- (lH-? m? dazol-1-? l) - 6-met? let? lp? pm? d? n-4-? l] -N- (2-et? Lhex? L) pipe ridin- 2 -acet amide, l- [2- (lH-? M? Dazol-l-? L) p? R? M? Dm-4-? ] -N- (2-ethylhexyl) pipe pdm-2 -aceta-borrant; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? Pm? D? N-4- ? l] -N- (2-ethylhexyl) pipe pdm-2 -acetarate; 1- [2- (lH-? m? dazol-1-? l) -6-met? let? lp? pm? d? n-4-? l] -N- [2- (morpholm-4-? l) et? l] p ipe pdm-2-acet amide; 1- [2- (lH-? m? dazol-1-? l) -6-met? lp? r? m? d? n-4-? l] -N- (1-methylhexyl) pipe pdin-2-acet amide; 1- [2- (lH-? m? dazol -1-? L) -6-met? Let? Lp? R? M? Dm-4-? L] -N- (1-met? Lhex? L) pipe ndin-2-acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-methylhexyl) pipe ridin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(2-methylphenyl) methyl] piper idin-2-acet amide; 1- [2- (lH-imi da zol-l-il) -6 -me ti le ti Ipyrimidin-4-yl] - N - [(4-methoxy phenyl) methyl] piper idin-2-acet amide; l- [2- (1H-imidazol-1-yl) -6-methy1-imidin-4-yl] -N- [(4-methoxy phenyl) methyl] pyridine-2-acetic acid; 1- [2- (1H-imi da zol-1-yl) -6-met i le ti Ipyrimidin-4-yl] -N- (cyclooctyl) pipe ridin-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- (1-ethyl-3-hydroxy-1-hydroxyethyl-1-propyl) piper idin-2-acet amide; 1- [2- (1 H-imidazol-1-yl) -6-met-ilet-1-pyrimidin-4-yl] -N- [3- (morpholin-4-yl) propyl] piper idin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (1-meth i 1-3-phenylpropyl) pipe ridin-2 -aceta-free; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-meth i 1-3-phenylimpropyl) pipe ridin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) -6-methyl-1-pyrimidin-4-y1] -N- (1-methyl-3-phenylpropyl) p ipe ridin-2 -acet ami da; 1- [2- (1H-imidazol-1-yl) -6-meth i le ti Ipyrimidin-4-yl] -N- (1-methylheptyl) pipe ridin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-methylheptyl) pipe ridin-2 -acet amide; l- [2- (lH-? m? dazol-1-? l) -6-met? lp? r? m? dm-4-? l] -N- (1-methylheptyl) pipe ridm- 2 -acet amide; l- [2- (lH-? m? dazol-l-? l) p? r? m? dm-4-? l] -N- [(3-fluorofen? l) met? l] piper? d? n-2- ace tarruda; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? L] -N- [(3-fluorofen? L) met? L ] piper din-2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? Pm? D? N-4-? L] -N- [(4-met? Lfen? L ) methyl] pipe ndm- 2 -acetreate; 1- [2- (lH-? M? Dazol-l-? L) p? Pm? D? N-4-? L] -N- (1-phenylethyl) pipe pdm-2 -acetic acid; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? L] -N-f enylmethylpipe pdm-2 -acet amide; 1- [2- (lH-? Rtudazol-1-? L) -6-met? Let? Lp? Pm? D? N-4-? L] -N- [(3,4-d? Chlorophen? ) met? l] piper í in- 2 -acet knots; l- [2- (lH-? m? dazol-l-? l) p? r? m? d? n-4-? l] -N- (2-phenylethyl) pipe pdm-2-acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? L] -N- (2-phenylethyl) pipe ndm- 2 -acet amide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? D? N-4-? L] -N- [3- (p? Rrol ? don-1-? l) propyl] pipe pdm-2-acet amide; 1- [2- (lH-? M? Dazol-1-? L) p? R? M? D? N-4-? L] -N- (1, 5-dimethylhexyl) pipe r? D? N- 2 -acet amide; l- [2- (lH-? m? dazol-1-? l) -6-met? lp? r? m? dm-4-? l] -N- (1,5-dimethylhexyl) p ipe ridin- 2-acet amide, 1- [2- (1H-imidazol-1-yl) -6-met-ilet-1-pyrimidin-4-yl] -N- (1, 5-dimethylhexyl) piper idin-2 -acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N- [(2-p-fluorophenyl) methyl] pipe-ridin-2 -acetic acid; l- [2- (lH-imidazol-l-yl) -6-met i Ipyrimidin-4-yl] -N- [(2-f luorofenyl) methyl] pipe ridin-2 -acet mide; 1- [2- (1H-imidazol-1-yl) -6-met i let ilpyr imidin-4-yl] -N- [(3,4-dimethoxy phenyl) methyl] pipe ridin-2 -aceta-r; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3, 4-dimethoxyphenyl) methyl] piper idin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (2-chloro-phenyl) -ethyl] -pyridin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) pi r imidin-4-yl] -N- [(f -uran-2-yl) methyl] pipe-ridin-2-acet amide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidi-4-yl] -N- [(furan-2-yl) methyl] p ipe ridin-2 -acet ami da; 1- [2- (1H-imidazol-1-yl) -6-met-ylethylpyrimidin-4-yl] -N- [(furan-2-yl) methyl] piper idin-2 -acet amide; 1- [2- (lH-imi da zol-l-il) -6 -me ti le ti Ipyrimidin-4-yl] - N - [(pyridin-2-yl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(pyridin-2-yl) methyl] pipe-ridin-2 -acertrudate; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(pyridin-2-yl) methyl] pipe ridin-2-a-cet amide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- [(3-trifluoromethyl-phenyl) -methyl] -piperidin-2-acetarruda; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N - [(3-trifluoromethylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (2-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-y1] -N- (2-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (2-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -pyrimidin-4-yl-N- [2- (2-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- (2-hydroxy-4-methylthiobutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (2-hydroxy-4-methylthiobutyl) piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [(2,4-dichlorophenyl) methyl] piperidin-2-ace Lamida; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(3-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(3-methylphenyl) methyl] piperidin-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) - 6-met i let? Lp? R? M? D? N-4-? L] -N- [2- (3-methox F ethyl) ethyl] p ipe pd? n-2 -acet ami a; l- [2- (lH-? m? dazol-l-? l) p? pm? d? n-4-? l] -N- [2- (3-methoxyphenyl) ethyl] pipe pd-2-ace tarruda; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Lp? R? M? Dm-4-? L] -N- [2- (3-methoxyphenyl) ethyl] pipe r? dm-2-acet amide; 1- [2- (lH-? M? Dazol-i-? L) p? R? M? D? N-4-? L] -N- [2- (3-methox? Phen? L) et? l] pyrrolidone-2-carboxamide; 1- [2- (lH-? M? Dazol-1-? L) -6-met? Let? Lp? R? M? D? N-4-? LN- [2- (3, 4-d? methox? phen? l) ethyl] piperidin-2-acetamide; 1- [2- (lH-? M? Dazol-1-? L) p? R? M? Dm-4-? L] -N- [2- (3,4-dimethoxy-enyl) ethyl] p? Pepdm -2-acetam? Da; 1- [2- (IH-ipudazol-lU) -6-met? Lp? Pm? D? N-4-? L] -N- [2- (3, 4-d? Methox? F enyl) ethyl] pipe pdm- 2 -acetart; 1- [2- (lH-? M? Dazol-1-? L) pi rmidmid- 4 -i 1] -N- [2- (3,4-dimethoxyphenyl) ethyl] pyrrolidm-2- carboxam? da; 1- [2- (lH-? M? Dazol-1-U) -6-met? Let? Lp? Pm? D? N-4-? L] -N- (phenylbutyl) p ipe ri din- 2 - ace tñida; 1- [2- (lH-? M? Dazol-1-? L) -p? R? M? D? N-4-? L] -N- (f-enylbutyl) piper? Dm-2-acet amide; 1- [2- (lH-? M? Dazol-1-? L) p? Pm? D? N-4-? L] -N- (1-hydroxymethylpentyl) pipe ridin- -acet amide; 1- [2- (lH-? M? Dazol-1-U) - 6-met? Lp? R? M? D? N-4-? L] -N- (1-hydroxymethylpentyl) piper din- 2 - acet amide; 1- [2- (lH-? M? Dazol-1-U) -6-met? Let? Lp? R? M? D? N-4-? L] -N- [(3, 5-d? methox? f enil) useful] pipe pdin- 2 -ace tarruda; 1- [2- (lH-? M? Dazol -_-? L) p? R? M? D? N-4-? L] -N- [(3,5-dimethoxyphenyl) methyl] pipe ndm- 2 -ace tarruda; l- [2- (lH-? m? dazol-1-? l) -6-met? lp? r? m? d? n-4-? l] -N- [(3,5-dimethoxy-enyl) methyl] pipe pdin- 2 -a cet amide; 1- [2- (lH-? M? Dazol-l-_l) -6-met? Let? Lp? R? M? Dm-4-? L] -N- [2- (4-ethoxy? Fen? l) et? l] pipe ndm- 2 -acetarr; l- [2- (lH-? m? dazol-J-? l) p? r? m? d? n-4-? l] -N- [2- (4-ethoxy? phen? l) et ? l] piperid -2-acetamide; l- [2- (lH-? m? dazol-1-?) -6-met? lp? r? m? d? n-4-? l] -N- [2- (4-ethoxyphenyl) ethyl] pipepd? n-2-acetarruda; l- [2- (lH-? m? dazol -_-? l) p? pm? d? n-4-? l] -N- [2- (4-ethoxyphenyl) ethyl] p? rrol? dm- 2-carboxamide; 1- [2- (lH-? M? Dazol-1- ^ i) -r met? Let? Lp? R? M? Dm-4-? L] -N- [2- (4-bromophenyl) ethyl] piperia -2-acetamide; l- [2- (lH-? m? dazol ---? l) p? r? m? d? n-4-? l] -N- [2- (4-bromophenyl) ethyl] p? per? d? n-2-acetam? da; 1- [2- (lH-? M? Dazol-1 -? ^ -6-met? Lp? Pm? D? N-4-? L] -N- [2- (4-bromophenyl) ethyl] pipe r ? d? n-2 -a cet amide; l- [2- (lH-? m? dazol- -? l) p? r? m? d? n-4-? l] -N- [2- ( 4-bromofenyl) et? L] p? Rrol? Dm-2-L Arboxamide; 1- [2- (lH-? M? Dazol-1-U) -6-met? Let? Lp? R? M? dm-4-? l] -N-pent i lp ipe ri din-2 -acet amide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N -pentylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N-pentylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethyl-pyrimidin-4-yl] -N- [3- (lH-imidazol-1-yl) propyl] piperidin-2-acetamide; 1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [3- (1H-imidazol-1-yl) propyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-chlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(3-chlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(2,4-dichlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidaz ol-1-yl) pi rimin din-4 -yl] -N- [(2,4-dichlorophenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (1-phenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [l- (phenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-fluorophenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- [2- (3-ethoxy-4-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (3-ethoxy-4-methoxy phenyl) ethyl] pipe ridin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-e-toxy-4-methyl-phenyl) ethyl] pipe-ridin-2-acetamide; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-ethoxy-4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-chlorophenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-met ilpyr imidin-4-yl-N- [2- (4-chlorophenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (5-hydroxypentyl) pipe ridin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N-butylpipethrin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) -6-met ilpyr imidin-4-yl] -N- [(4-f-luoro-phenyl) (methyl) methyl] -pipe ridin-2 -acetic acid; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(4-f luoro-phenyl) (methyl) methyl] pipe-ridin-2 -acetic acid; 1- [2- (1 H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (2, 5-dimethoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (IH-imide zol-1-yl) -6-met i Ipyrimidin-4-yl] -N- [2- (2,5-dimethoxy phenyl) ethyl] pipe ridin-2 -acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (2,5-dimethoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-ethoxy-3-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethi-pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- [3- (methylethoxy) propyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylethylpyrimidin-4-yl] -N-hexylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N-hexylpiperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl-N-hexylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (cyclohexen-1-yl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (cyclohexen-1-yl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(3-fluoro-5-trifluoromethylphenyl) methyl] piperidin-2-acetarruda; l- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(3-fluoro-5-trifluoromethylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imide zol-1-yl) -pyrimidin-4-yl] -N- [2- (4-methylphenyl) ethyl] piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N- [2- (4-ethylphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (3-ethoxypropyl) piperidin-2-acetarruda; l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (3-ethoxypropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N-heptylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pi rimidin-4-yl] -N-heptylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methyl-1-pyrimidin-4-y1] -N-heptylpiperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (3-methoxypropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (1-cyclohexylethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-cyclohexylethyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] - N - [(4-trifluoromethoxyphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-trifluoromethyl-to-phenyl) -methyl] -piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (4-fluorophenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (4-fluorophenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] piperidin-2-acetamide; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (3-brorno-4-methoxyphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [2- (3-bromo-4-methoxyphenyl) ethyl] pyrrolidine-2-carboxamide; l- [2- (lH-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- (3-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- (3-phenylpropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- (3-phenylpropyl) piperidin-2-acetarruda; 1- [2- (lH-imidazol-1-yl) -6-methylethyl-pyrimidin-4-yl-N-octylpiperidin-2-acetarruda; l- [2- (lH-imidazol-l-yl) -6-methylpyrimidin-4-yl-N-octylpiperidin-2-acetamide; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- (1-hydroxy-3-methylbutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [1- (4-methylphenyl) ethyl] piperidin-2-acetarruda; l- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] -N- [l- (4-methylphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [1- (4-methylphenyl) ethyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [4, 4-diethoxybutyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(4-trifluoromethyl-phenyl) -methyl] -piperidin-2-acetamide; l- [2- (1H-imidazol-1-yl) -pyrimidin-4-yl] -N - [(4-trifluoromethylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N - [(4-trifluoromethylphenyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl-N- (3-butoxypropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -N- (3-butoxypropyl) piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [2- (thiophen-2-yl) ethyl] piperidin-2-acetarruda; 1- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [2- (thiophen-2-yl) ethyl] piperidin-2-acetamide; 1- [2- (1 H -imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [3- (pyrrolidin-1-yl) propyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] -N- [(cyclohexyl) methyl] piperidin-2-acetamide; 1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N- [(cyclohexyl) methyl] piperidin-2-acetamide; ethyl ester of 4- [[1- (2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-acetyl] amino] piperidine-1-carboxylic acid ethyl ester of 4- [[1 - [2- (1H-imidazol-1-yl) -6-methylethylpyrimidin-4-yl] piperidin-2-acetyl] amino] piperidine-1-carboxylic acid ethyl ester of 4- [[1- (2- ( lH-imidazol-l-yl) -6-methylpyrimidin-4-yl] piperidin-2-acetyl] amino] piperidine-l-carboxylic acid; l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin- 4-yl] -N- [(4-fluorophenyl) methyl] piperidin-2-acetamide; N - [(1,3-benzodioxol-5-yl) methyl] -l- [3- (lH-imidazol-1- il) phenyl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [3-chloro-5- (1H-imidazol-1-yl) triazin-1-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) purin-6-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [6- (lH-imidazol-1-yl) pyrazin-2-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-propionamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- (lH-imidazol-1-yl) pyrimidin-4-propionamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- (lH-imidazol-1-yl) pyrimidin-4-propionamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [2- (lH-imidazol-1-yl) pyrimidin-4-oxy] acetamide; N- [(1,3-benzodioxol-5-yl) ethyl] -2- [2- (lH-imidazol-1-yl) pyrimidin-4-thio] acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanamine; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N-methylpiperidin-2-ethanamine; N-acetyl-N - [(1,3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2-ethanamine; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -N- (methylsulfonyl) piperidin-2-ethanamine; 4- [2- [[(1,3-benzodioxol-5-yl) methoxy] ethyl] pipe ridin-1-yl] -2- (lH-imidazol-1-yl) pyrimidine; 4- [2 - [[4- (methoxy) phenoxy] propyl] pyrrolidin-1-yl] -2- (lH-imidazol-1-yl) pyrimidine; 4- [2 - [[4- (methoxy) phenoxy] propyl] pyrrol idin-1-yl] -2- (lH-imidazol-1-yl) -6-met ilpyr imidine; 4- [2- [(1,3-benzodioxol-yl) propyl] pyrrolidin-1-yl] -2- (1 H -imidazol-1-yl) pyrimidine; 4- [2 - [(1, 3-benzodioxol-5-yl) prop-2-enyl] pyrrolidin-1-yl] -2- (1 H-imidazol-1-yl) pyrimidine; 4-chloro-2- (1H-imidazol-1-yl) -6- (perhydroazepin-1-yl) pyrimidine; 1- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] pipe ridin-2-ethanol; 4-chloro-2- (1H-imidazol-1-yl) -6- (piperidin-1-yl) pyrimidine; 4-chloro-2- (1H-imidazol-1-yl) -6- (2-ethylpiperidin-1-yl) pyrimidine; 4-f luoro-2- (1H-imidazol-1-yl) -6- [[(3, A-dimethoxyphenyl) ethyl] amino] pyrimidine; 4 - f l u o r o - 2 - (l H - i m i d a z or l - l - i l) - 6 - [[(phenyl) ethyl] amino] pyrimidine; N- [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-triazol-1-yl) pyrimidin-4-yl] -4- [(dimethylethoxy) carbonyl] piperazine-2- acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [6- (morpholin-4-yl) -2- (lH-imidazol-1-yl) pyrimidin-4-yl] piperidin-2 -acculent; N- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (1H-imidazol-1-yl) -6-methoxypyrimidin-4-yl] -piperidin-2-acetamide; N- [(1, 3-benzodioxol-5-yl) methyl] -4- [6- [bis (ethoxycarbonyl) methyl] -2- (1H-imidazol-1-yl) pyrimidin-4-yl] -1- [(methoxy) carbonyl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -4- [6- (aminocarbonyl) -2- (1 H -imidazol-1-yl) pyrimidin-4-yl] -1- [(methoxy) carbonyl] piperazin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -3- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -4-methoxybenzamide; 4-chloro-2- (1H-imidazol-1-yl) -6- [(2-methoxyphenyl) amino] pyrimidine; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] indole-6-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrole-2-carboxamide; N- [(3,4-dimethoxy phenyl) ethyl] -2- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] -1,2,3,4-tetrahydroisoquinoline-3-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-2-propionamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] pyrrolidin-2-propionamide; N- [(3,4-dimethoxy phenyl) ethyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidine-3-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] pyrrolidine-3-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] - [2- (lH-imidazol-1-yl) pyrimidin-4-yl] pyrrolidin-3-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] pyrrolidin-3-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -1- [2- (1H-imidazol-1-yl) -6-ethylpyrimidin-4-yl] pyrrolidin-3-acetamide; N - [(3,4-dimethoxyphenyl) ethyl] -1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -acetidine-2-carboxamide; 4- [2- (1H-imide zol-1-yl) pyrimin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) ethyl] morpholin-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] -N - [(1,3-benzodioxan-6-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl-N - [(1,4-benzodioxan-6-yl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl] - N - [(4-methoxyphenyl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N- [(4-methoxyphenyl) ethyl] morpholin-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(3,4-dimethoxyphenyl) ethyl] morpholin-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] - N - [(3,4-dimethoxyphenyl) ethyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) pyrimidin-4-yl-N - [(4-methoxyphenyl) methyl] morpholine-2-carboxamide; 4- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl-N- [(4-methoxyphenyl) methyl] morpholine-2-carboxamide; 4- [2- (1H-imide zol-1-yl) pyrimin-4-yl] -N- [(1,3-benzodioxol-5-yl) methyl] morpholin-2-acetamide; 4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -N - [(1,3-benzodioxol-5-yl) methyl] morpholin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] morpholine-3-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -4- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] morpholine-3-carboxamide; N - [(1, 3-benzodioxol-5-yl) ethyl] -4- [6-ethyl-2- (lH-imidazol-1-yl) pyrimidin-4-yl] morpholine-3-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -4- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] morpholine-3-carboxamide; N - [(4-methoxy phenyl) methyl-4- [2- (lH-imide zol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N- [(4-chlorophenyl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] morpholine-3-carboxamide; N - [(3,4-dichlorophenyl) methyl] -4- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N- [(4-methylphenyl) meth1-4- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] morpholine-3-carboxamide; N- [(3,4-Dimethylphenyl) methyl] -4- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] morpholine-3-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -2- [[2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] acetamide; N- [(1, 4-benzodioxan-6-yl) methyl] -2- [[2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] amino] acetamide; N - [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1, 3-benzodioxol-5-yl) methyl] -l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,4-benzodioxan-6-yl) methyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,4-benzodioxan-6-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-l-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1, 3-benzodioxol-5-yl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-eti-pyrimidin-4-yl] -perhydroazepin-2-carboxamide; N - [(1, 3-benzodioxol-5-yl) ethyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(1,4-benzodioxan-6-yl) ethyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(1,4-benzodioxan-6-yl) ethyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(3,4-dimethoxy phenyl) ethyl] -l- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] perhydroazepin-2-carboxamide; N - [(3,4-dimethoxyphenyl) methyl] -l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepine-2-carboxamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [6-chloro-2- (lH-imidazol-1-yl) pyrimidin-4-yl] -perhydroazepin-2-carboxamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -l- [2- (1H-imidazol-1-yl) -6-methylpyrimidin-4-yl] -perhydroazepin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) -6-ethylpyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(1,4-benzodioxan-6-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(1,4-benzodioxan-6-yl) methyl] -l- [2- (1 H -imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(3,4-dimethoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -perhydroazepin-2-acetamide; N - [(3,4-dimethoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(3,4-dimethoxyphenyl) ethyl] -l- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(3,4-dimethoxyphenyl) ethyl-l- [2- (lH-imidazol-1-yl) -6- (methylethyl) pyrimidin-4-yl] perhydroazepin-2-acetamide; N - [(4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetarruda; N - [(4-methoxyphenyl) methyl] -1- [2- (lH-imidazol-1-yl) -6-methylpyrimidin-4-yl] perhydroazepin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl-1- [6-chloro-2- (pyridin-3-yl) pyrimidin-4-yl] piperidin-2-acetamide; N- [(1,3-benzodioxol-5-yl) methyl] -1- [2- (lH-imidazol-1-yl) pyrimidin-4-ylperhydroazepin-2-acetamide; N- [(4-trifluoromethoxyphenyl) methyl] -1- [(2- (1H-imidazol-1-yl) pyrimidin-4-yl] perhydroazepin-2-acetamide; and N- [(4-trifluoromethoxyphenyl) methyl] - 1- [2- (1H-imidazol-1-yl) -6-methy1-pyrimidin-4-yl] -perhydroazepin-2-acetamide; 56. Pharmaceutical composition comprising a compound of formula (I), formula (II), or formula (III): H) q (C (R13) H) r- D (C (R14) R20) n- A ni); wherein: A is -R1, -OR1, -IOINIR'IR2, -P (0) [N (R1) R2] 2, -N (Rx) C (0) R2, -N (R16) C (0 ) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -StOt-R1, -SOjNHCtOR1, -NHS02R22, -S02N (R1) H, -C (0) NHS02R22, and -CH = N0R2; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, u 0; each W is N or CH; Q is selected from the group consisting of a direct bond, -C (0) -, -0-, -CUN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -NIR ^ lCfOlNlR'lR16, -S (0) tRx (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -0R1, -NfR ^ CtOR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -S OXR1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; and each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-C2Q alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, [C2-C8 alkenyl] -R9, - [ C, -C8 alkynyl] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [X-Cgj-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C_-C8 alkyl] -C (0) N (R1) R2, - [C_-C8 alkyl] -N ( RX) R2, - [C_-C8 alkyl] -R8, - [C2-C8 alkyl] -R10, - [C_-C8 alkyl] -Rn, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) 0H, -CtOJNÍ, -C (= NH) -N (RX) R2 or R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -NtR ^ C OWR R16, -N (R16) C (0) OR16, -N (R16) C (0) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0- alkyl] C 8] -C (H) [C (0) OR 16] 2 and - [C 1 -C 8 alkyl R 16 alkyl; R 6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of X-Cg-R 8, - [C 1 -C 8 alkyl] -R 10, - [C 1 -C 8 alkyl] -Ru, acyl, - C (0) R8, -C (0) - [X-Cg-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl , monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R23-N (Rx) C (0) -R23-N (R1) R2, -C (0) -N (R1) -R23-C (0) 0R1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -SO, R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. 57. Process for synthesizing a compounds of formula (1), formula (II), or formula (III): wherein: A is -R1, -OR1, -C (O) N (R1) R2, -P (O) [N (R1) R2] 2, -NfR ^ CÍOR2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16, -SfOXR1, -SO, NHC (0) R1, -NHSO, R22, -SO, N (R1) H, -C (O) NHSO, R22, and -CH-NOR1; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, or O; each W is N or CH; Q is selected from the group consisting of a direct bond, -C (O) -, -O-, -CXN-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (O) R2, -N (R16) C (O) OR2, -N (RX) R21, -NÍR ^ UO? NÍR ^ R16, -SÍOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -NYR UOJR2, -N (R16) C (O) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16, - SÍOXR1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; and each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C_-C20 alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, [C2-C8 alkenyl] -R9, - [ C2-C8 alkynyl] -R9, - [C, -C8 alkyl] -R10 (optionally substituted by hydroxy), - [XC-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R 3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C 1 -C 8 alkyl] -C (O) N (R 1) R 2, - [C 1 -Cg alkyl] -N (RX) R2, - [C1-C8 alkyl] -R8, - [C2-C8 alkyl] -R10, - [X-Cg alkyl -R11, and heterocyclyl (optionally substituted by 1 or more substituents that are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C (0) N (R1) R2, -C (= NH) -N (R1) R2 or O RZ R 2 R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (R16) C ( 0) N (Rx) R16, -N (R16) C (0) 0R16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0 alkyl] -C8] -C (H) [C (0) OR16] 2 and - [C -C-alkyl-UOlNtR ^ R16; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl] - [alkyl] C, -C 8] -R 10, - [C 1 -C 8 alkyl] -R 11, acyl, -C (0) R 8, -C (O) - [C 1 -C 8 alkyl] -R 8, alkoxycarbonyl, optionally substituted aryloxycarbonyl optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylcarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (O) -R23-N (R1) R2, -C (0) -R23-N (R1) C (0) -R23-N (R1) R2, -C (O) -N (R1) -R23-C (O) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; comprising the sequential steps of: (a) reacting an equivalent of a compound of formula (XI): WiM- l: xi); X / where W is N or CH; with about one equivalent of a chloro substituted compound of formula (XII): Cl X (XII); U "Y'A: l where X, Y and Z are independently N or C (R19), U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19, and with the proviso that X, Y and Z can not all be C (R19) when U is C (R5); R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, aryl optionally substituted, -OR16, -S (0) t-R16, -N (R16) R21, -H (R16) C (0) i (R1) R16, -N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C (H) [C (0) OR16] 2 and - [ C0-C8] -C (O) N (R1) R16, each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl, each R19 is independently hydrogen, alkyl (optionally substituted by hydroxy), cyclopropyl, halo or haloalkyl, each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S 02R22; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; and each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; to produce a compound of the formula (XIII): (xiii); (b) reacting a compound of formula (XIII) on a compound of formula (XlVa), formula (XlVb), or formula (XIVc): Q-R- (¿(R15) H) m 14, / (C (R12) H) q- - (C (R13) H) ¿- (C (R R20) n (XlVa: R17 / (C (R12) H) q- (C (R13) H) r- (c (R14) R20) n-A H (XIVcl) where: A is -R1, -OR1, -CÍONfR ^ R2, -P (O) [N (R1) R2] 2, - ¡(R1) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16, -SIOJ. R1, -SO, NHC (0) R1, -NHS02R22, -S02N (R1) H, - C (O) NHS02R22, and -CH = NOR1; V is N (R4), S, or O; Q is selected from the group consisting of a direct bond, -C (O) -, -O-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (O) R2, -N (R16) C (O) OR2, -N (RX) R21, -N (R16) C (0) N (Rx) R16, -SYOKR1 (when t is zero) or -NHS02R22, n, q and r can not all be zero; and when Q is a heteroatom and A is -OR1, -NYR ^ UOJR2, -N (R16) C (O) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16, -SÍOÍt-R1 (when t is zero) or -NHSO, R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; and each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C_-C20 alkyl, optionally substituted cycloalkyl, - [C0-C6 alkyl] -R9, [C-C5 alkenyl] -R9, - [C2-C6 alkynyl] -R9, - [C, -C6 alkyl] -R10 (optionally substituted by hydroxy), - [X-Cg-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [X-Cg alkyl] -N (R1) R2, - [C_-C8 alkyl] -N (RX) R2, - [C_-C8 alkyl] -R6, - [C, -C8 alkyl] -R10, - [alkyl and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -CtOlNfRU2, -C (= NH) -N (RL) R2 or R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R 6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C 1 -C 8 alkyl] -R 8, - [C 1 -C 8 alkyl] -R 10, - [C 1 -C 11 alkyl-R 11, acyl , -C (0) R8, -C (0) - [C_-Ca] -R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, arylfulsonyl optionally substituted, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23- N (R1) R2, -C (0) -R23-N (R1) C (0) -R23-N (R1) R2, -CfO-NfR1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkylene R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, NO, or toluenesulfonyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -SO, R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; to produce a compound of formula formula II) or formula (III). 58. Process to synthesize a compound of formula (I), formula (II) or formula (III): 2 °) n wherein: A is -C (0) N (Rla) R2; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that ü is N only when X is N and Z and Y are CR19; V is N (R4), S, O or C (R4) H; each W is N or CH; Q is selected from the group consisting of a direct bond, -C (O) -, -O-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (O) R2, -N (R16) C (O) OR2, -NfR ^ R21, -NÍR ^ JCÍOJNÍR R16, -StOXR1 (when t is zero) or -NHSO, R22, n, q and r can not all be zero; and when Q is a heteroatom and A is -OR1, -NYR ^ CIOJR2, -N (R16) C (O) OR2, -N (RX) R21, -N (R16) C (O) N (R1) R16, -SFOít-R1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; Rla is hydrogen; each R1 and R2 are independently selected from the group consisting of hydrogen, X-C ,, alkyl} optionally substituted, optionally substituted cycloalkyl, - [alkyl of C0-C6] -R9, [C2-C6 alkenyl] -R9, - [C2-C6 alkynyl] -R9, - [C2-C6 alkyl] -R10 (optionally substituted by hydroxy), - [X-Cg] -R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [alkyl of -N (R1) R2, - [C_-C8 alkyl] -N (RX) R2, - [ C ^ Cg] -R6, - [C2-C8 alkyl] -R10, - [alkyl of X-Cg-R11, and heterocyclyl (optionally substituted by 1 or more substituents which are selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -CfOJNtR ^ R2, -C (= NH) -N (RX) R2 or R 4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (Rld) R21, -NÍR ^ CÍOJN R ^ R16 , -N (R16) C (0) OR16, -N (R16) C (0) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0-C8 alkyl] -C (H) ) [C (0) OR16] 2 and - [alkyl of Co-CgUUOIN R16; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [C_-C8 alkyl] -R8, - [ C, -C8] -R10, - [C_-C8 alkyl] -Rn, acyl, -C (0) R8, -C (0) - [XC-R8 alkyl, alkoxycarbonyl, optionally substituted aryloxycarbonyl, aralkoxycarbonyl optionally substituted, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, -C (0) -R23-N (R1) C (0) -R23-N (R1) R2, -C (0) -N (R1) -R23-C (O) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, N02 or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -SO, R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; which comprises photolytically separating the compound of formula (IXa), formula (IXb) or formula (IXc): ; where U, V,, X, Y and Z are as defined in the above; R2, R3, R12, R13, R14, R15, R17 and R20 are as defined above; it is a solid substrate; and L is the linking residue of the formula (IX); wherein the valency not satisfied to the right of the formula represents the point of attachment to the solid substrate and the valence not satisfied to the left of the formula represents the point of attachment to the ligand; to form the compound of formula (I), formula (II) and formula (III) as defined above. 59. Method for treating a condition resulting from an abnormality in the production of nitric oxide, which comprises administering to a mammal having a condition resulting from an abnormality in the production of nitric oxide, a therapeutically effective amount of a compound of formula (I), formula (II), formula (III): H) (C (R13) H) r-fí > ) - (C (R14) R20). n -A); where A is -R1, -OR1, -UOJNÍR ^ R2, -P (O) [N (R1) R2] 2, -N (Rx) C (0) R2, -N (R16) C (0) OR2, -NfR ^ R21, -N (R16) C (O) N (R1) R16, -S (0) tR1, -SOjNHCÍOJR1, -NHSO, R22, -S02N (R1) H, -C (O) NHS02R22 , and -CH = NOR2; each of X, Y and Z are independently N or C (R19); each U is N or C (R5), with the proviso that U is N only when X is N and Z and Y are CR19; V is N (R4), S, u 0; each W is N or CH; Q is chosen from the group consisting of a direct link, -C (0) -, -O-, -C (= N-R1) -, -S (0) t, and -N (R6) -; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or 1; r is zero or 1; with the proviso that when Q and V are heteroatoms, m q and r can not all be zero; when A is -OR1, -N (R1) C (0) R2, -N (R16) C (0) OR2, -N (RX) R21, -NfR ^ OJNÍR ^ R16, -SÍOXR1 (when t is zero) or -NHS02R22, n, q and y can not all be zero; and when Q is a heteroatom and A is -OR1, -N (R1) C (0) R2, -N (R16) C (O) OR2, -N (RX) R21, -N (R16) C (0) N (R1) R16, -SÍOJtR1 (when t is zero) or -NHS02R22, myn can not both be zero; t is zero, 1 or 2; N is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl, or optionally substituted N-heterocyclyl; and each R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, - [C0-C8 alkyl] -R9, [C2-C8 alkenyl] -R9, - [ C2-C8 alkynyl] -R9, - [C2-C8 alkyl] -R10 (optionally substituted by hydroxy), - [Cx-C8] -R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is optionally substituted N-heterocyclyl; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, - [C_-C8 alkyl] -C (O) N (R1) R2, - [C_-C8 alkyl] -NfR ^ R2, - [C_-C8 alkyl] -R8, - [C2-C8 alkyl] -R10, - [alkyl of X-Cg-R11, and heterocyclyl (optionally substituted by 1 or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N (R6) - or a direct bond to R3, R3 can additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C (= NR18) -NH2; or -Q-R3 taken together, represent -C (0) OH, -C (0) N (RX) R2, -C (= NH) -N (RX) R2 or R4 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; with the proviso that when A is -R1 or -OR1, R4 can not be hydrogen and when V is CH, R4 can additionally be hydroxy; R5 is selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S (0) t-R16, -N (R16) R21, -N (R16) C ( 0) N (R1) R16, -N (R16) C (0) OR16, -N (R16) C (O) R16, - [C0-C8 alkyl] -C (O) OR16, - [C0 alkyl] -C8] -C (H) [C (0) OR16] 2 and - [C 1 -C 8 -CO 2 R 4 alkyl; R6 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, - [alkyl of XC-R8, - [C, -C8 alkyl] -R10, - [alkyl of XC-R11, acyl, -C (0) R8 , -C (0) - [C_-C8 alkyl] -R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylfulsonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C (= NH) -N (CN) R1, -C (0) -R23-N (R1) R2, - C (O) -R23-N (R1) C (0) -R23-N (R1) R2, -C (0) -N (R1) -R23-C (0) OR1; each of R8 and R9 is independently selected from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents that are selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl, (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently selected from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, -S (0) t-R22 optionally substituted, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl) amino, hydroxy, mercapto, alkylsulfonamido; each R 11 is independently selected from the group consisting of cyano, di (alkoxy) alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15 R17 and R20 are independently hydrogen or alkylene R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; R18 is hydrogen, NO, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C (0) R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached are optionally substituted N-heterocyclyl; or R21, taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixtures thereof, or a pharmaceutically acceptable salt thereof. 60. Method as described in clause 59, in which the condition resulting from an abnormality in the production of nitric oxide, is chosen from the group consisting of multiple sclerosis; attack or cerebral ischemia; Alzheimer's disease, HIV dementia; Parkinson's disease; meningitis; dilated cardiomyopathy and congestive heart failure; atherosclerosis; restenosis or graft stenosis, septic shock and hypotension; hemorrhagic shock; asthma; respiratory distress syndrome in adults, smoking habit or particle-mediated lung damage; pneumonias mediated by pathogens; traumas of various etiologies; rheumatoid arthritis and osteoarthritis; glomerulonephritis; systemic lupus erythematosus; inflammatory bowel diseases such as ulcerative colitis and Crohn's disease; insulin-independent diabetes mellitus; diabetic neuropathy or nephropathy; acute and chronic organ transplant rejection; Transplant vasculopathies; graft versus host disease; psoriasis and other inflammatory skin diseases; and cancer 61. Method as described in clause 60, in which the condition is multiple sclerosis. 62. Method as described in clause 60, in which the condition is rheumatoid arthritis. 63. Method as described in clause 60, in which the condition is dilated cardiomyopathy. 64. Method as described in clause 60, in which the condition is congestive heart failure.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/808,975 | 1997-02-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
MXPA99007670A true MXPA99007670A (en) | 2002-03-26 |
Family
ID=
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EP0968206B1 (en) | N-heterocyclic derivatives as nos inhibitors | |
US6747031B2 (en) | N-heterocyclic derivatives as NOS inhibitors | |
JP2001509156A (en) | Inhibitors of farnesyl protein transferase | |
JPH11505522A (en) | N-aroylamino acid amides as endothelin inhibitors | |
MXPA99007670A (en) | N | |
CZ296799A3 (en) | N-heterocyclic derivatives functioning as NOS inhibitors |