JP5566880B2 - プロテインキナーゼの阻害剤としての４，６−二置換アミノピリミジン誘導体 - Google Patents
プロテインキナーゼの阻害剤としての４，６−二置換アミノピリミジン誘導体 Download PDFInfo
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- JP5566880B2 JP5566880B2 JP2010504692A JP2010504692A JP5566880B2 JP 5566880 B2 JP5566880 B2 JP 5566880B2 JP 2010504692 A JP2010504692 A JP 2010504692A JP 2010504692 A JP2010504692 A JP 2010504692A JP 5566880 B2 JP5566880 B2 JP 5566880B2
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- Prior art keywords
- phenyl
- compound
- pyrimidin
- substituted
- methanesulfonamide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- -1 4,6-disubstituted aminopyrimidine Chemical class 0.000 title claims description 96
- 239000003112 inhibitor Substances 0.000 title description 57
- 102000001253 Protein Kinase Human genes 0.000 title description 7
- 108060006633 protein kinase Proteins 0.000 title description 7
- 150000001875 compounds Chemical class 0.000 claims description 203
- 208000002193 Pain Diseases 0.000 claims description 197
- 230000036407 pain Effects 0.000 claims description 149
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 126
- 239000000203 mixture Substances 0.000 claims description 104
- 201000010099 disease Diseases 0.000 claims description 102
- 125000000217 alkyl group Chemical group 0.000 claims description 101
- 229910052739 hydrogen Inorganic materials 0.000 claims description 91
- 239000001257 hydrogen Substances 0.000 claims description 91
- 208000004296 neuralgia Diseases 0.000 claims description 70
- 208000021722 neuropathic pain Diseases 0.000 claims description 69
- 150000002431 hydrogen Chemical class 0.000 claims description 52
- 239000008194 pharmaceutical composition Substances 0.000 claims description 42
- 208000015181 infectious disease Diseases 0.000 claims description 41
- 208000027866 inflammatory disease Diseases 0.000 claims description 41
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 39
- 125000001072 heteroaryl group Chemical group 0.000 claims description 37
- 230000002062 proliferating effect Effects 0.000 claims description 35
- 206010065390 Inflammatory pain Diseases 0.000 claims description 34
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 31
- 208000000094 Chronic Pain Diseases 0.000 claims description 29
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 29
- 125000000623 heterocyclic group Chemical group 0.000 claims description 28
- 125000003545 alkoxy group Chemical group 0.000 claims description 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 25
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 125000001424 substituent group Chemical group 0.000 claims description 25
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 24
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 24
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 23
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 22
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 22
- 230000004770 neurodegeneration Effects 0.000 claims description 21
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 19
- 208000026278 immune system disease Diseases 0.000 claims description 19
- 230000002757 inflammatory effect Effects 0.000 claims description 19
- 125000003342 alkenyl group Chemical group 0.000 claims description 17
- 125000005843 halogen group Chemical group 0.000 claims description 16
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 14
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 13
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 13
- 229910052757 nitrogen Inorganic materials 0.000 claims description 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 12
- 150000003857 carboxamides Chemical group 0.000 claims description 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
- 229910052731 fluorine Inorganic materials 0.000 claims description 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 11
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 239000003937 drug carrier Substances 0.000 claims description 10
- 239000011737 fluorine Substances 0.000 claims description 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 9
- 239000012453 solvate Substances 0.000 claims description 8
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims description 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 6
- 150000001204 N-oxides Chemical class 0.000 claims description 6
- 125000003302 alkenyloxy group Chemical group 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 229940124530 sulfonamide Drugs 0.000 claims description 6
- 150000003456 sulfonamides Chemical class 0.000 claims description 6
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims description 4
- 125000001589 carboacyl group Chemical group 0.000 claims description 4
- 229940125904 compound 1 Drugs 0.000 claims description 4
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 3
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 3
- 125000003386 piperidinyl group Chemical group 0.000 claims description 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 3
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims description 2
- CITCBKKAVRLYPK-UHFFFAOYSA-N [3-[[6-(2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCOC1=CC=CC=C1C1=CC(NC=2C=C(CS(N)(=O)=O)C=CC=2)=NC=N1 CITCBKKAVRLYPK-UHFFFAOYSA-N 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 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 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000006264 diethylaminomethyl group Chemical group [H]C([H])([H])C([H])([H])N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 3
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 3
- GDWVCMUNHLLAQU-UHFFFAOYSA-N 2-[6-[3-(methylsulfonylmethyl)anilino]pyrimidin-4-yl]phenol Chemical compound CS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C(=CC=CC=2)O)=C1 GDWVCMUNHLLAQU-UHFFFAOYSA-N 0.000 claims 2
- OJEBBFHEVUJONE-UHFFFAOYSA-N [2-[6-[3-(methylsulfonylmethyl)anilino]pyrimidin-4-yl]phenyl]methanol Chemical compound CS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C(=CC=CC=2)CO)=C1 OJEBBFHEVUJONE-UHFFFAOYSA-N 0.000 claims 2
- XTOMHCHXLAXPSD-UHFFFAOYSA-N [3-[[6-(2-ethoxy-5-fluorophenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCOC1=CC=C(F)C=C1C1=CC(NC=2C=C(CS(N)(=O)=O)C=CC=2)=NC=N1 XTOMHCHXLAXPSD-UHFFFAOYSA-N 0.000 claims 2
- NMZQJJULBWUWIJ-UHFFFAOYSA-N [3-[[6-(3-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCOC1=CC=CC(C=2N=CN=C(NC=3C=C(CS(N)(=O)=O)C=CC=3)C=2)=C1 NMZQJJULBWUWIJ-UHFFFAOYSA-N 0.000 claims 2
- FYPVPYOTWMTLIL-UHFFFAOYSA-N [3-[[6-(3-fluorophenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=C(F)C=CC=2)=C1 FYPVPYOTWMTLIL-UHFFFAOYSA-N 0.000 claims 2
- JEKAROVFQXTUPL-UHFFFAOYSA-N [3-[[6-(3-phenylmethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=C(OCC=3C=CC=CC=3)C=CC=2)=C1 JEKAROVFQXTUPL-UHFFFAOYSA-N 0.000 claims 2
- SERSRGJYQZHNME-UHFFFAOYSA-N [3-[[6-(4-fluorophenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=CC(F)=CC=2)=C1 SERSRGJYQZHNME-UHFFFAOYSA-N 0.000 claims 2
- LGFYKPSWAJESAR-UHFFFAOYSA-N [3-[[6-[2-(2-methoxyethoxy)phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound COCCOC1=CC=CC=C1C1=CC(NC=2C=C(CS(N)(=O)=O)C=CC=2)=NC=N1 LGFYKPSWAJESAR-UHFFFAOYSA-N 0.000 claims 2
- FNVQNDGVNKTGEI-UHFFFAOYSA-N [3-[[6-[3-(1,2,4-triazol-1-ylmethyl)phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=C(CN3N=CN=C3)C=CC=2)=C1 FNVQNDGVNKTGEI-UHFFFAOYSA-N 0.000 claims 2
- GBAYTJKMNOIBLH-UHFFFAOYSA-N [3-[[6-[3-(diethylaminomethyl)phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCN(CC)CC1=CC=CC(C=2N=CN=C(NC=3C=C(CS(N)(=O)=O)C=CC=3)C=2)=C1 GBAYTJKMNOIBLH-UHFFFAOYSA-N 0.000 claims 2
- ZTGCWIHIQGSMGU-UHFFFAOYSA-N [3-[[6-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound C1CN(C)CCN1CC1=CC=CC(C=2N=CN=C(NC=3C=C(CS(N)(=O)=O)C=CC=3)C=2)=C1 ZTGCWIHIQGSMGU-UHFFFAOYSA-N 0.000 claims 2
- PLVVQSNGBWUHRU-UHFFFAOYSA-N n-[3-(methylsulfonylmethyl)phenyl]-6-(2-phenylmethoxyphenyl)pyrimidin-4-amine Chemical compound CS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C(=CC=CC=2)OCC=2C=CC=CC=2)=C1 PLVVQSNGBWUHRU-UHFFFAOYSA-N 0.000 claims 2
- ASGMFNBUXDJWJJ-JLCFBVMHSA-N (1R,3R)-3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethylcyclopentane-1-carboxamide Chemical compound BrC1=NN(C2=NC(=NC=C21)N[C@H]1C[C@@](CC1)(C(=O)NC)C)C1=CC=C(C=C1)C=1SC(=NN=1)C ASGMFNBUXDJWJJ-JLCFBVMHSA-N 0.000 claims 1
- UAOUIVVJBYDFKD-XKCDOFEDSA-N (1R,9R,10S,11R,12R,15S,18S,21R)-10,11,21-trihydroxy-8,8-dimethyl-14-methylidene-4-(prop-2-enylamino)-20-oxa-5-thia-3-azahexacyclo[9.7.2.112,15.01,9.02,6.012,18]henicosa-2(6),3-dien-13-one Chemical compound C([C@@H]1[C@@H](O)[C@@]23C(C1=C)=O)C[C@H]2[C@]12C(N=C(NCC=C)S4)=C4CC(C)(C)[C@H]1[C@H](O)[C@]3(O)OC2 UAOUIVVJBYDFKD-XKCDOFEDSA-N 0.000 claims 1
- AOSZTAHDEDLTLQ-AZKQZHLXSA-N (1S,2S,4R,8S,9S,11S,12R,13S,19S)-6-[(3-chlorophenyl)methyl]-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-azapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one Chemical compound C([C@@H]1C[C@H]2[C@H]3[C@]([C@]4(C=CC(=O)C=C4[C@@H](F)C3)C)(F)[C@@H](O)C[C@@]2([C@@]1(C1)C(=O)CO)C)N1CC1=CC=CC(Cl)=C1 AOSZTAHDEDLTLQ-AZKQZHLXSA-N 0.000 claims 1
- ABJSOROVZZKJGI-OCYUSGCXSA-N (1r,2r,4r)-2-(4-bromophenyl)-n-[(4-chlorophenyl)-(2-fluoropyridin-4-yl)methyl]-4-morpholin-4-ylcyclohexane-1-carboxamide Chemical compound C1=NC(F)=CC(C(NC(=O)[C@H]2[C@@H](C[C@@H](CC2)N2CCOCC2)C=2C=CC(Br)=CC=2)C=2C=CC(Cl)=CC=2)=C1 ABJSOROVZZKJGI-OCYUSGCXSA-N 0.000 claims 1
- GLGNXYJARSMNGJ-VKTIVEEGSA-N (1s,2s,3r,4r)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3h-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound CCN1C(=O)CCCC2=C(OC)C(NC=3N=C(C(=CN=3)Cl)N[C@H]3[C@H]([C@@]4([H])C[C@@]3(C=C4)[H])C(N)=O)=CC=C21 GLGNXYJARSMNGJ-VKTIVEEGSA-N 0.000 claims 1
- SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
- GHYOCDFICYLMRF-UTIIJYGPSA-N (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1(=CCCC1)C[C@@H](C(=O)[C@@]1(OC1)C)NC([C@H]([C@@H](C1=CC=C(C=C1)OC)O)NC([C@H](C)NC(CN1CCOCC1)=O)=O)=O GHYOCDFICYLMRF-UTIIJYGPSA-N 0.000 claims 1
- GCTFTMWXZFLTRR-GFCCVEGCSA-N (2r)-2-amino-n-[3-(difluoromethoxy)-4-(1,3-oxazol-5-yl)phenyl]-4-methylpentanamide Chemical compound FC(F)OC1=CC(NC(=O)[C@H](N)CC(C)C)=CC=C1C1=CN=CO1 GCTFTMWXZFLTRR-GFCCVEGCSA-N 0.000 claims 1
- IUSARDYWEPUTPN-OZBXUNDUSA-N (2r)-n-[(2s,3r)-4-[[(4s)-6-(2,2-dimethylpropyl)spiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-3-hydroxy-1-[3-(1,3-thiazol-2-yl)phenyl]butan-2-yl]-2-methoxypropanamide Chemical compound C([C@H](NC(=O)[C@@H](C)OC)[C@H](O)CN[C@@H]1C2=CC(CC(C)(C)C)=CN=C2OC2(CCC2)C1)C(C=1)=CC=CC=1C1=NC=CS1 IUSARDYWEPUTPN-OZBXUNDUSA-N 0.000 claims 1
- YJLIKUSWRSEPSM-WGQQHEPDSA-N (2r,3r,4s,5r)-2-[6-amino-8-[(4-phenylphenyl)methylamino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol Chemical compound C=1C=C(C=2C=CC=CC=2)C=CC=1CNC1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O YJLIKUSWRSEPSM-WGQQHEPDSA-N 0.000 claims 1
- VIJSPAIQWVPKQZ-BLECARSGSA-N (2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-4,4-dimethylpentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid Chemical compound NC(=N)NCCC[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(C)=O VIJSPAIQWVPKQZ-BLECARSGSA-N 0.000 claims 1
- WWTBZEKOSBFBEM-SPWPXUSOSA-N (2s)-2-[[2-benzyl-3-[hydroxy-[(1r)-2-phenyl-1-(phenylmethoxycarbonylamino)ethyl]phosphoryl]propanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)O)C(=O)C(CP(O)(=O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WWTBZEKOSBFBEM-SPWPXUSOSA-N 0.000 claims 1
- STBLNCCBQMHSRC-BATDWUPUSA-N (2s)-n-[(3s,4s)-5-acetyl-7-cyano-4-methyl-1-[(2-methylnaphthalen-1-yl)methyl]-2-oxo-3,4-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)[C@H](C)N(C(C)=O)C2=CC(C#N)=CC=C2N1CC1=C(C)C=CC2=CC=CC=C12 STBLNCCBQMHSRC-BATDWUPUSA-N 0.000 claims 1
- QFLWZFQWSBQYPS-AWRAUJHKSA-N (3S)-3-[[(2S)-2-[[(2S)-2-[5-[(3aS,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-[1-bis(4-chlorophenoxy)phosphorylbutylamino]-4-oxobutanoic acid Chemical compound CCCC(NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CCCCC1SC[C@@H]2NC(=O)N[C@H]12)C(C)C)P(=O)(Oc1ccc(Cl)cc1)Oc1ccc(Cl)cc1 QFLWZFQWSBQYPS-AWRAUJHKSA-N 0.000 claims 1
- FNHHVPPSBFQMEL-KQHDFZBMSA-N (3S)-5-N-[(1S,5R)-3-hydroxy-6-bicyclo[3.1.0]hexanyl]-7-N,3-dimethyl-3-phenyl-2H-1-benzofuran-5,7-dicarboxamide Chemical compound CNC(=O)c1cc(cc2c1OC[C@@]2(C)c1ccccc1)C(=O)NC1[C@H]2CC(O)C[C@@H]12 FNHHVPPSBFQMEL-KQHDFZBMSA-N 0.000 claims 1
- IWZSHWBGHQBIML-ZGGLMWTQSA-N (3S,8S,10R,13S,14S,17S)-17-isoquinolin-7-yl-N,N,10,13-tetramethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-amine Chemical compound CN(C)[C@H]1CC[C@]2(C)C3CC[C@@]4(C)[C@@H](CC[C@@H]4c4ccc5ccncc5c4)[C@@H]3CC=C2C1 IWZSHWBGHQBIML-ZGGLMWTQSA-N 0.000 claims 1
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- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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| PCT/EP2008/055017 WO2008129080A1 (en) | 2007-04-24 | 2008-04-24 | 4, 6-disubstituted aminopyrimidine derivatives as inhibitors of protein kinases |
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| US8969372B2 (en) | 2003-11-14 | 2015-03-03 | Aptose Boisciences Inc. | Aryl imidazoles and their use as anti-cancer agents |
| EP2550257B1 (en) * | 2010-03-22 | 2016-12-21 | Lead Discovery Center GmbH | Pharmaceutically active disubstituted triazine derivatives |
| WO2012117059A1 (en) * | 2011-03-02 | 2012-09-07 | Lead Discovery Center Gmbh | Pharmaceutically active disubstituted pyridine derivatives |
| CN103582482B (zh) | 2011-03-02 | 2016-10-12 | 利德探索中心有限公司 | 药学活性的二取代的三嗪衍生物 |
| WO2012143399A1 (en) | 2011-04-19 | 2012-10-26 | Bayer Intellectual Property Gmbh | Substituted 4-aryl-n-phenyl-1,3,5-triazin-2-amines |
| TW201636330A (zh) | 2011-05-24 | 2016-10-16 | 拜耳知識產權公司 | 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺 |
| EP2527332A1 (en) | 2011-05-24 | 2012-11-28 | Bayer Intellectual Property GmbH | 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors |
| ES2588102T3 (es) | 2011-09-16 | 2016-10-28 | Bayer Intellectual Property Gmbh | Derivados de 5-fluoro-pirimidina disustituidos que contienen un grupo sulfoximina |
| EP2755956B1 (en) * | 2011-09-16 | 2016-05-18 | Bayer Intellectual Property GmbH | 2,4-disubstituted 5-fluoro-pyrimidines as selective cdk9 inhibtors |
| US9498471B2 (en) | 2011-10-20 | 2016-11-22 | The Regents Of The University Of California | Use of CDK9 inhibitors to reduce cartilage degradation |
| SG11201501041VA (en) * | 2012-08-23 | 2015-03-30 | Virostatics Srl | Novel 4,6-disubstituted aminopyrimidine derivatives |
| US9670161B2 (en) | 2012-10-18 | 2017-06-06 | Bayer Pharma Aktiengesellschaft | 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group |
| CN105283453B (zh) * | 2012-10-18 | 2018-06-22 | 拜耳药业股份公司 | 含砜基的n-(吡啶-2-基)嘧啶-4-胺衍生物 |
| CA2888381A1 (en) | 2012-10-18 | 2014-04-24 | Bayer Pharma Aktiengesellschaft | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group |
| ES2612978T3 (es) | 2012-11-15 | 2017-05-19 | Bayer Pharma Aktiengesellschaft | Derivados de 5-fluoro-n-(piridin-2-il)piridin-2-amina que contienen un grupo sulfoximina |
| TW201418243A (zh) * | 2012-11-15 | 2014-05-16 | Bayer Pharma AG | 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物 |
| US9499492B2 (en) * | 2012-11-15 | 2016-11-22 | Bayer Pharma Aktiengesellschaft | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfoximine group |
| HK1218296A1 (zh) | 2013-07-04 | 2017-02-10 | Bayer Pharma Aktiengesellschaft | 磺亚胺取代的5-氟-n-(吡啶-2-基)吡啶-2-胺衍生物以及其作爲cdk9激酶抑制剂的用途 |
| JP6946000B2 (ja) * | 2013-10-04 | 2021-10-06 | アプトース バイオサイエンシーズ， インコーポレイテッド | がんの治療用組成物及び方法 |
| AR098394A1 (es) | 2013-11-25 | 2016-05-26 | Lilly Co Eli | Inhibidores de dgat2 (diacilglicerol o-aciltransferasa 2) |
| JP2017508757A (ja) | 2014-03-13 | 2017-03-30 | バイエル ファーマ アクチエンゲゼルシャフト | スルホン基を含有する５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体 |
| JP6503372B2 (ja) | 2014-04-01 | 2019-04-17 | バイエル ファーマ アクチエンゲゼルシャフト | スルホンジイミン基を含むジ置換５−フルオロピリミジン誘導体 |
| CA2944727A1 (en) | 2014-04-04 | 2015-10-08 | Memorial Sloan-Kettering Cancer Center | Method and kits for identifying of cdk9 inhibitors for the treatment of cancer |
| KR102383938B1 (ko) | 2014-04-11 | 2022-04-08 | 바이엘 파마 악티엔게젤샤프트 | 신규한 매크로시클릭 화합물 |
| JP6930913B2 (ja) | 2014-10-14 | 2021-09-01 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアＴｈｅ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｌｉｆｏｒｎｉａ | 炎症を阻害するためのｃｄｋ９及びｂｒｄ４阻害剤の使用法 |
| WO2016059086A1 (en) | 2014-10-16 | 2016-04-21 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group |
| ES2720525T3 (es) | 2014-10-16 | 2019-07-22 | Bayer Pharma AG | Derivados fluorados de benzofuranil-pirimidina que contienen un grupo sulfona |
| WO2016150902A1 (en) | 2015-03-24 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers |
| US20180050040A1 (en) | 2015-03-24 | 2018-02-22 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n--1,3,5-triazin-2-amine for treating lymphomas |
| EP3274338A1 (en) | 2015-03-24 | 2018-01-31 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating multiple myeloma |
| ME03404B (me) | 2015-06-29 | 2020-01-20 | Astrazeneca Ab | Derivati policikličnih amida kao cdk9 inhibitori |
| ES2786552T3 (es) | 2015-09-29 | 2020-10-13 | Bayer Pharma AG | Compuestos de sulfondiimina macrocíclicos nuevos |
| EP3359544B1 (en) | 2015-10-08 | 2020-08-12 | Bayer Pharma Aktiengesellschaft | Novel modified macrocyclic compounds |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| BR112019000796A2 (pt) | 2016-07-16 | 2019-04-24 | Florida State University Research Foundation, Inc. | compostos e métodos para tratamento e prevenção da infecção flavivirus |
| WO2018177889A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| WO2019075011A1 (en) | 2017-10-10 | 2019-04-18 | Florida State University Research Foundation, Inc. | EMETIC COMPOUNDS FOR THE TREATMENT AND PREVENTION OF FLAVIVIRUS INFECTION |
| US11149047B2 (en) | 2017-10-30 | 2021-10-19 | Aptose Biosciences, Inc. | Aryl imidazoles for treatment of cancer |
| IL276437B2 (en) | 2018-02-13 | 2024-03-01 | Bayer Ag | Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma |
| US20220226341A1 (en) * | 2019-05-23 | 2022-07-21 | Kyoto University | Pharmaceutical Composition for Alzheimer's Disease |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
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| GB9319568D0 (en) | 1993-09-22 | 1993-11-10 | Euro Celtique Sa | Pharmaceutical compositions and usages |
| CN100355751C (zh) | 2000-03-29 | 2007-12-19 | 西克拉塞尔有限公司 | 2－取代的4－杂芳基－嘧啶、其组合物及其用途 |
| ES2292753T4 (es) | 2001-03-29 | 2009-02-16 | Vertex Pharmaceuticals Incorporated | Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas. |
| GB0205693D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| US20040106647A1 (en) | 2002-06-28 | 2004-06-03 | Schneider Michael D. | Modulators of Cdk9 as a therapeutic target in cardiac hypertrophy |
| US7576085B2 (en) | 2002-09-23 | 2009-08-18 | Schering Corporation | Imidazopyrazines as cyclin dependent kinase inhibitors |
| US7419984B2 (en) * | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| JP2006507302A (ja) | 2002-10-30 | 2006-03-02 | メルク エンド カムパニー インコーポレーテッド | キナーゼ阻害剤 |
| EP1648877A1 (en) | 2003-07-22 | 2006-04-26 | Neurogen Corporation | Substituted pyridin-2-ylamine analogues |
| AU2004261484A1 (en) | 2003-07-30 | 2005-02-10 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| EP1678147B1 (en) * | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| EP1709007A1 (en) | 2004-01-22 | 2006-10-11 | Altana Pharma AG | N-4-(6-(heteo)aryl-pyrimidin-4-ylaminophenyl)-benzenesulfonamides as kinase inhibitors |
| TW200614993A (en) | 2004-06-11 | 2006-05-16 | Akzo Nobel Nv | 4-phenyl-pyrimidine-2-carbonitrile derivatives |
| US20090221581A1 (en) * | 2005-05-25 | 2009-09-03 | Philipp Wabnitz | Methods of treating pain |
| US8389521B2 (en) * | 2007-04-24 | 2013-03-05 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| US8507511B2 (en) * | 2007-04-24 | 2013-08-13 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| ES2539518T3 (es) * | 2007-04-24 | 2015-07-01 | Astrazeneca Ab | Inhibidores de proteínas quinasas |
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| EP2137166B1 (en) | 2012-05-30 |
| US8507498B2 (en) | 2013-08-13 |
| EP2137166A1 (en) | 2009-12-30 |
| JP2010525025A (ja) | 2010-07-22 |
| WO2008129080A1 (en) | 2008-10-30 |
| US20130338147A1 (en) | 2013-12-19 |
| US20110306602A1 (en) | 2011-12-15 |
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