HRP20151001T4 - Sredstva kao induktori apoptoze za liječenje raka te imunih i autoimunih bolesti - Google Patents
Sredstva kao induktori apoptoze za liječenje raka te imunih i autoimunih bolesti Download PDFInfo
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- HRP20151001T4 HRP20151001T4 HRP20151001TT HRP20151001T HRP20151001T4 HR P20151001 T4 HRP20151001 T4 HR P20151001T4 HR P20151001T T HRP20151001T T HR P20151001TT HR P20151001 T HRP20151001 T HR P20151001T HR P20151001 T4 HRP20151001 T4 HR P20151001T4
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- Prior art keywords
- nhc
- pyridin
- sulfonyl
- methyl
- piperazin
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- 206010028980 Neoplasm Diseases 0.000 title claims 2
- 201000011510 cancer Diseases 0.000 title claims 2
- 208000023275 Autoimmune disease Diseases 0.000 title 1
- 230000006907 apoptotic process Effects 0.000 title 1
- 208000026278 immune system disease Diseases 0.000 title 1
- 230000001939 inductive effect Effects 0.000 title 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 102
- 101150009274 nhr-1 gene Proteins 0.000 claims 40
- 150000001924 cycloalkanes Chemical class 0.000 claims 35
- 150000001925 cycloalkenes Chemical class 0.000 claims 35
- 150000002390 heteroarenes Chemical class 0.000 claims 35
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 32
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 32
- -1 C(O)N(R1)2 Proteins 0.000 claims 19
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 19
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 19
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 19
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 11
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 11
- 101100294121 Caenorhabditis elegans nhr-57 gene Proteins 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 10
- OTXBWGUYZNKPMG-UHFFFAOYSA-N isofulminic acid Chemical compound O[N+]#[C-] OTXBWGUYZNKPMG-UHFFFAOYSA-N 0.000 claims 9
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 9
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 5
- 101100240518 Caenorhabditis elegans nhr-12 gene Proteins 0.000 claims 5
- 101100240527 Caenorhabditis elegans nhr-22 gene Proteins 0.000 claims 5
- 101100516557 Caenorhabditis elegans nhr-62 gene Proteins 0.000 claims 5
- 101100516560 Caenorhabditis elegans nhr-67 gene Proteins 0.000 claims 5
- 101100516561 Caenorhabditis elegans nhr-68 gene Proteins 0.000 claims 5
- 101100516568 Caenorhabditis elegans nhr-7 gene Proteins 0.000 claims 4
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- 102220516986 Double homeobox protein 4_R23A_mutation Human genes 0.000 claims 3
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- 102220595577 Major vault protein_R24A_mutation Human genes 0.000 claims 3
- 102220544927 Nuclear pore complex protein Nup133_R30A_mutation Human genes 0.000 claims 3
- 102220507264 Rab11 family-interacting protein 1_R29A_mutation Human genes 0.000 claims 3
- 102220507254 Rab11 family-interacting protein 1_R38K_mutation Human genes 0.000 claims 3
- 102220507255 Rab11 family-interacting protein 1_R39K_mutation Human genes 0.000 claims 3
- 125000004957 naphthylene group Chemical group 0.000 claims 3
- 102220497337 14-3-3 protein zeta/delta_R59A_mutation Human genes 0.000 claims 2
- CSBKUBOVPUXFLO-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[(4-methoxycyclohexyl)methylamino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1CC(OC)CCC1CNC1=CC=C(S(=O)(=O)NC(=O)C=2C(=CC(=CC=2)N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)OC=2C=C3C=CNC3=NC=2)C=C1[N+]([O-])=O CSBKUBOVPUXFLO-UHFFFAOYSA-N 0.000 claims 2
- BEABEHQNCJQGIZ-UHFFFAOYSA-N 4-[4-[[4-(4-chlorophenyl)-6,6-dimethyl-2,5-dihydropyran-3-yl]methyl]piperazin-1-yl]-N-[4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1OC(C)(C)CC(C=2C=CC(Cl)=CC=2)=C1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NC(CC1)CCC1N1CCOCC1 BEABEHQNCJQGIZ-UHFFFAOYSA-N 0.000 claims 2
- 102220586234 Chemerin-like receptor 2_R18A_mutation Human genes 0.000 claims 2
- 102220586235 Chemerin-like receptor 2_R63A_mutation Human genes 0.000 claims 2
- 102220586050 Chemerin-like receptor 2_R64A_mutation Human genes 0.000 claims 2
- 102220586191 Chemerin-like receptor 2_R65A_mutation Human genes 0.000 claims 2
- 102220474817 Chemerin-like receptor 2_R69A_mutation Human genes 0.000 claims 2
- 102220586055 Chemerin-like receptor 2_R70A_mutation Human genes 0.000 claims 2
- 102220503974 Endogenous retrovirus group K member 6 Rec protein_R13A_mutation Human genes 0.000 claims 2
- 102220555063 Holliday junction recognition protein_R25A_mutation Human genes 0.000 claims 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims 2
- 102220521126 Ribosome biogenesis protein NSA2 homolog_R58A_mutation Human genes 0.000 claims 2
- 102220521661 Ribosome biogenesis protein NSA2 homolog_R71A_mutation Human genes 0.000 claims 2
- 102220599428 Serum amyloid A-1 protein_R37A_mutation Human genes 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 102200140336 rs786204767 Human genes 0.000 claims 2
- LQBVNQSMGBZMKD-UHFFFAOYSA-N venetoclax Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCC1CCOCC1 LQBVNQSMGBZMKD-UHFFFAOYSA-N 0.000 claims 2
- NKITUFNNDFPWII-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NC(CC1)CCC1N1CCOCC1 NKITUFNNDFPWII-UHFFFAOYSA-N 0.000 claims 1
- WXOWXNJJXWISMF-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[(4-oxo-1h-quinazolin-6-yl)sulfonyl]-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1C(C)(C)CCC(CN2CCN(CC2)C=2C=C(OC=3C=C4C=CNC4=NC=3)C(C(=O)NS(=O)(=O)C=3C=C4C(=O)NC=NC4=CC=3)=CC=2)=C1C1=CC=C(Cl)C=C1 WXOWXNJJXWISMF-UHFFFAOYSA-N 0.000 claims 1
- YGXOOIXZEQFHSN-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[3-nitro-4-(2,2,2-trifluoroethylamino)phenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C1=CC=C(NCC(F)(F)F)C([N+]([O-])=O)=C1 YGXOOIXZEQFHSN-UHFFFAOYSA-N 0.000 claims 1
- MOSZSOAPGWWZGM-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[3-nitro-4-(3,3,3-trifluoropropylamino)phenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C1=CC=C(NCCC(F)(F)F)C([N+]([O-])=O)=C1 MOSZSOAPGWWZGM-UHFFFAOYSA-N 0.000 claims 1
- SWTUOVBEIYFQAW-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[3-nitro-4-(oxan-4-ylmethoxy)phenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1OCC1CCOCC1 SWTUOVBEIYFQAW-UHFFFAOYSA-N 0.000 claims 1
- UWFNVICMJXECTL-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-(1,4-dioxan-2-ylmethylamino)-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCC1COCCO1 UWFNVICMJXECTL-UHFFFAOYSA-N 0.000 claims 1
- ARVNTYAWJFCNBT-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-(2-cyanoethylamino)-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C1=CC=C(NCCC#N)C([N+]([O-])=O)=C1 ARVNTYAWJFCNBT-UHFFFAOYSA-N 0.000 claims 1
- SGFNZHPUMCITBS-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-(2-methoxyethylamino)-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1=C([N+]([O-])=O)C(NCCOC)=CC=C1S(=O)(=O)NC(=O)C1=CC=C(N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)C=C1OC1=CN=C(NC=C2)C2=C1 SGFNZHPUMCITBS-UHFFFAOYSA-N 0.000 claims 1
- XNTSJCOLINDAQV-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-(3-morpholin-4-ylpropylamino)-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCCCN1CCOCC1 XNTSJCOLINDAQV-UHFFFAOYSA-N 0.000 claims 1
- WXLXUGGDJKYDGY-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-(morpholin-3-ylmethylamino)-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCC1COCCN1 WXLXUGGDJKYDGY-UHFFFAOYSA-N 0.000 claims 1
- VWFUWKGATFWYJU-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[(1-methylpiperidin-4-yl)amino]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1CN(C)CCC1NC1=CC=C(S(=O)(=O)NC(=O)C=2C(=CC(=CC=2)N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)OC=2C=C3C=CNC3=NC=2)C=C1[N+]([O-])=O VWFUWKGATFWYJU-UHFFFAOYSA-N 0.000 claims 1
- YYCSXFRYHHWHHR-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[(1-methylpiperidin-4-yl)methoxy]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1CN(C)CCC1COC1=CC=C(S(=O)(=O)NC(=O)C=2C(=CC(=CC=2)N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)OC=2C=C3C=CNC3=NC=2)C=C1[N+]([O-])=O YYCSXFRYHHWHHR-UHFFFAOYSA-N 0.000 claims 1
- YIWCJRDYDWHTFY-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[(1-methylpiperidin-4-yl)methylamino]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1CN(C)CCC1CNC1=CC=C(S(=O)(=O)NC(=O)C=2C(=CC(=CC=2)N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)OC=2C=C3C=CNC3=NC=2)C=C1[N+]([O-])=O YIWCJRDYDWHTFY-UHFFFAOYSA-N 0.000 claims 1
- RSMQQIHISLSANF-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[(1-methylsulfonylpiperidin-4-yl)amino]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NC1CCN(S(C)(=O)=O)CC1 RSMQQIHISLSANF-UHFFFAOYSA-N 0.000 claims 1
- QANMVQFCTLIVEG-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[(4-methylpiperazin-1-yl)amino]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1CN(C)CCN1NC1=CC=C(S(=O)(=O)NC(=O)C=2C(=CC(=CC=2)N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)OC=2C=C3C=CNC3=NC=2)C=C1[N+]([O-])=O QANMVQFCTLIVEG-UHFFFAOYSA-N 0.000 claims 1
- MTYZNVLVSZYNFF-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[2-(2-methoxyethoxy)ethylsulfonyl]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C1=C([N+]([O-])=O)C(S(=O)(=O)CCOCCOC)=CC=C1S(=O)(=O)NC(=O)C1=CC=C(N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)C=C1OC1=CN=C(NC=C2)C2=C1 MTYZNVLVSZYNFF-UHFFFAOYSA-N 0.000 claims 1
- XPJQWWCHHLBCCH-PGUFJCEWSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[[(2r)-1,4-dioxan-2-yl]methoxy]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1OC[C@H]1COCCO1 XPJQWWCHHLBCCH-PGUFJCEWSA-N 0.000 claims 1
- XPJQWWCHHLBCCH-DHUJRADRSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[[(2s)-1,4-dioxan-2-yl]methoxy]-3-nitrophenyl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1OC[C@@H]1COCCO1 XPJQWWCHHLBCCH-DHUJRADRSA-N 0.000 claims 1
- YYYRZMJZVXGSKG-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[5-cyano-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1C#N)=CN=C1OCC1COCCO1 YYYRZMJZVXGSKG-UHFFFAOYSA-N 0.000 claims 1
- IYJJTGJTNSOTQA-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[5-cyano-6-(oxan-4-ylmethoxy)pyridin-3-yl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1C#N)=CN=C1OCC1CCOCC1 IYJJTGJTNSOTQA-UHFFFAOYSA-N 0.000 claims 1
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- LAXFJBRABSDHCS-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[6-(oxan-4-ylmethoxy)-5-propan-2-ylpyridin-3-yl]sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound CC(C)C1=CC(S(=O)(=O)NC(=O)C=2C(=CC(=CC=2)N2CCN(CC=3CCC(C)(C)CC=3C=3C=CC(Cl)=CC=3)CC2)OC=2C=C3C=CNC3=NC=2)=CN=C1OCC1CCOCC1 LAXFJBRABSDHCS-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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Claims (6)
1. Spoj, naznačen time, da ima formulu (II)
[image]
ili njegova terapeutski prihvatljiva sol, gdje
R100 je R57A, R57, OR57, SR57, S(O)R57, SO2R57, C(O)R57, CO(O)R57, OC(O)R57, OC(O)OR57, NH2, NHR57, N(R57)2, NHC(O)R57, NR57C(O)R57, NHS(O)2R57, NR57S(O)2R57, NHC(O)OR57, NR57C(O)OR57, NHC(O)NH2, NHC(O)NHR57, NHC(O)N(R57)2, NR57C(O)NHR57, NR57C(O)N(R57)2, C(O)NH2, C(O)NHR57, C(O)N(R57)2, C(O)NHOH, C(O)NHOR57, C(O)NHSO2R57, C(O)NR57SO2R57, SO2NH2, SO2NHR57, SO2N(R57)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR57, C(N)N(R57)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br ili I;
n je 0, 1, 2, ili 3;
A1 je N ili C(A2);
A2 je H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A;
B1 je H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A;
D1 je H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A;
E1 je H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A; i
Y1 je H, CN, NO2, C(O)OH, F, Cl, Br, I, CF3, OCF3, CF2CF3, OCF2CF3, R17, OR17, C(O)R17, C(O)OR17, SR17, SO2R17, NH2, NHR17, N(R17)2, NHC(O)R17, C(O)NH2, C(O)NHR17, C(O)N(R17)2, NHS(O)R17 ili NHSO2R17; ili
E1 i Y1 zajedno s atomima na koje su vezani, čine benzen, naftilen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken; i
A2, B1 i D1 su neovisno odabrani od sljedećih: H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A; ili
Y1 i B1 zajedno s atomima na koje su vezani, čine benzen, naftilen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken; i
A2, D1 i E1 su neovisno odabrani od sljedećih: H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2ili C(O)OR1A; ili
A2 i B1 zajedno s atomima na koje su vezani, čine benzen, naftilen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken; i
D1, E1 i Y1 su neovisno odabrani od sljedećih: H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A; ili
A2 i D1 zajedno s atomima na koje su vezani, čine benzen, naftalen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken; i
B1, E1 i Y1 su neovisno odabrani od sljedećih: H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, C(O)OR1, OC(O)R1, NHR1, N(R1)2, C(O)NHR1, C(O)N(R1)2, NHC(O)R1, NR1C(O)R1, NHC(O)OR1, NR1C(O)OR1, NHC(O)NH2, NHC(O)NHR1, NHC(O)N(R1)2, NR1C(O)NHR1, NR1C(O)N(R1)2, SO2NH2, SO2NHR1, SO2N(R1)2, NHSO2R1, NR1SO2R1, NHSO2NHR1, NHSO2N(R1)2, NR1SO2NHR1, NR1SO2N(R1)2, C(O)NHNOH, C(O)NHNOR1, C(O)NHSO2R1, C(NH)NH2, C(NH)NHR1, C(NH)N(R1)2 NHSO2NHR1, NHSO2N(CH3)R1, N(CH3)SO2N(CH3)R1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 ili C(O)OR1A;
R1 je R2, R3, R4 ili R5;
R1A je cikloalkil, cikloalkenil ili cikloalkinil;
R2 je fenil koji je nestaljen ili staljen s R2A;
R2A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R3 je heteroaril koji je nestaljen ili staljen s R3A;
R3A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R4 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R4A;
R4A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R5 je alkil, alkenil ili alkinil, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R6, NC(R6A)(R6B), R7, OR7, SR7, S(O)R7, SO2R7, NHR7, N(R7)2, C(O)R7, C(O)NH2, C(O)NHR7, C(O)N(R7)2, NHC(O)R7, NR7C(O)R7, NHSO2R7, NHC(O)OR7, SO2NH2, SO2NHR7, SO2N(R7)2, NHC(O)NH2, NHC(O)NHR7, NHC(O)CH(CH3)NHC(O)CH(CH3)NH2, NHC(O)CH(CH3)NHC(O)CH(CH3)NHR7, OH, (O), C(O)OH, N3, CN, NH2, CF3, CF2CF3, F, Cl, Br i I;
R6 je C2-C5-spiroalkil od kojih je svaki nesupstituiran ili supstituiran s OH, (O), N3, CN, CF3, CF2CF3, F, Cl, Br, I, NH2, NH(CH3) ili N(CH3)2;
R6A i R6B su neovisno odabrani od alkila;
R7 je R8, R9, R10 ili R11;
R8 je fenil koji je nestaljen ili staljen s R8A;
R8A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R9 je heteroaril koji je nestaljen ili staljen s R9A;
R9A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R10 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R10A;
R10A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R11 je alkil, alkenil ili alkinil, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R12, OR12, SR12, S(O)R12, SO2R12, C(O)R12, CO(O)R12, OC(O)R12, OC(O)OR12, NH2, NHR12, N(R12)2, NHC(O)R12, NR12C(O)R12, NHS(O)2R12, NR12S(O)2R12, NHC(O)OR12, NR12C(O)OR12, NHC(O)NH2, NHC(O)NHR12, NHC(O)N(R12)2, NR12C(O)NHR12, NR12C(O)N(R12)2, C(O)NH2, C(O)NHR12, C(O)N(R12)2, C(O)NHOH, C(O)NHOR12, C(O)NHSO2R12, C(O)NR12SO2R12, SO2NH2, SO2NHR12, SO2N(R12)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR12, C(N)N(R12)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3,
OCF2CF3, F, Cl, Br i I;
R12 je R13, R14, R15 ili R16;
R13 je fenil koji je nestaljen ili staljen s R13A;
R13A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R14 je heteroaril koji je nestaljen ili staljen s R14A;
R14A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R15 je cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken, od kojih je svaki nestaljen ili staljen s R15A;
R15A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R16 je alkil, alkenil ili alkinil;
R17 je R18, R19, R20 ili R21;
R18 je fenil koji je nestaljen ili staljen s R18A;
R18A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R19 je heteroaril koji je nestaljen ili staljen s R19A;
R19A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R20 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R20A;
R20A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R21 je alkil, alkenil ili alkinil, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R22, OR22, SR22, S(O)R22, SO2R22, C(O)R22, CO(O)R22, OC(O)R22, OC(O)OR22, NH2, NHR22, N(R22)2, NHC(O)R22, NR22C(O)R22, NHS(O)2R22, NR22S(O)2R22, NHC(O)OR22, NR22C(O)OR22, NHC(O)NH2, NHC(O)NHR22, NHC(O)N(R22)2, NR22C(O)NHR22, NR22C(O)N(R22)2, C(O)NH2, C(O)NHR22, C(O)N(R22)2, C(O)NHOH, C(O)NHOR22, C(O)NHSO2R22, C(O)NR22SO2R22, SO2NH2, SO2NHR22, SO2N(R22)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR22, C(N)N(R22)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R22 je R23, R24 ili R25;
R23 je fenil koji je nestaljen ili staljen s R23A;
R23A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R24 je heteroaren koji je nestaljen ili staljen s R24A;
R24A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R25 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R25A;
R25A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
Z2 je R28, R29 ili R30;
L1 je R37, OR37, SR37, S(O)R37, SO2R37, C(O)R37, CO(O)R37, OC(O)R37, OC(O)OR37, NHR37, C(O)NH, C(O)NR37, C(O)NHOR37, C(O)NHSO2R37, SO2NH, SO2NHR37, C(N)NH ili C(N)NHR37;
R28 je fenilen koji je nestaljen ili staljen s R28A;
R28A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R29 je heteroarilen koji je nestaljen ili staljen s R29A;
R29A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R30 je cikloalkilen, cikloalkenilen, heterocikloalkilen ili heterocikloalkenilen, od kojih je svaki nestaljen ili staljen s R30A;
R30A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R37 je veza ili R37A;
R37A je alkilen, alkenilen ili alkinilen, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R37B, OR37B, SR37B, S(O)R37B, SO2R37B, C(O)R37B, CO(O)R37B, OC(O)R37B, OC(O)OR37B, NH2, NHR37B, N(R37B)2, NHC(O)R37B, NR37BC(O)R37B, NHS(O)2R37B, NR37BS(O)2R37B, NHC(O)OR37B, NR37BC(O)OR37B, NHC(O)NH2, NHC(O)NHR37B, NHC(O)N(R37B)2, NR37BC(O)NHR37B, NR37BC(O)N(R37B)2, C(O)NH2, C(O)NHR37B, C(O)N(R37B)2, C(O)NHOH, C(O)NHOR37B, C(O)NHSO2R37B, C(O)NR37BSO2R37B, SO2NH2, SO2NHR37B, SO2N(R37B)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR37B, C(N)N(R37B)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R37B je alkil, alkenil, alkinil ili R37C;
R37C je fenil, heteroaril, cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil;
Z3 je R38, R39 ili R40;
R38 je fenil koji je nestaljen ili staljen s R38A;
R38A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R39 je heteroaril koji je nestaljen ili staljen s R39A;
R39A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R40 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R40A;
R40A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
pri čemu su ciklički ostaci molekula, koji su predstavljeni preko E1 i Y1 zajedno, Y1 i B1 zajedno, A2 i B1 zajedno, A2 i D1 zajedno, R1A, R2, R2A, R3, R3A, R4, R4A, R6, R8, R8A, R9, R9A, R10, R10A, R13, R13A, R14, R14A, R15, R15A, R18, R18A, R19, R19A, R20, R20A, R23, R23A, R24, R24A, R25, R25A, R28, R28A, R29, R29A, R30, R30A, R38, R38A, R39, R39A, R40 i R40A, neovisno nesupstituirani, supstituirani ili dodatno supstituirani s jednim ili dva ili tri ili četiri ili pet supstituenata neovisno odabranih od R57A, R57, OR57, SR57, S(O)R57, SO2R57, C(O)R57, CO(O)R57, OC(O)R57, OC(O)OR57, NH2, NHR57, N(R57)2, NHC(O)R57, NR57C(O)R57, NHS(O)2R57, NR57S(O)2R57, NHC(O)OR57, NR57C(O)OR57, NHC(O)NH2, NHC(O)NHR57, NHC(O)N(R57)2, NR57C(O)NHR57, NR57C(O)N(R57)2, C(O)NH2, C(O)NHR57, C(O)N(R57)2, C(O)NHOH, C(O)NHOR57, C(O)NHSO2R57, C(O)NR57SO2R57, SO2NH2, SO2NHR57, SO2N(R57)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR57, C(N)N(R57)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R57A je spiroalkil;
R57 je R58, R59, R60 ili R61;
R58 je fenil koji je nestaljen ili staljen s R58A;
R58A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R59 je heteroaril koji je nestaljen ili staljen s R59A;
R59A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R60 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R60A;
R60A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R61 je alkil, alkenil ili alkinil, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R62, OR62, SR62, S(O)R62, SO2R62, C(O)R62, CO(O)R62, OC(O)R62, OC(O)OR62, NH2, NHR62, N(R62)2, NHC(O)R62, NR62C(O)R62, NHS(O)2R62, NR62S(O)2R62, NHC(O)OR62, NR62C(O)OR62, NHC(O)NH2, NHC(O)NHR62, NHC(O)N(R62)2, NR62C(O)NHR62, NR62C(O)N(R62)2, C(O)NH2, C(O)NHR62, C(O)N(R62)2, C(O)NHOH, C(O)NHOR62, C(O)NHSO2R62, C(O)NR62SO2R62, SO2NH2, SO2NHR62, SO2N(R62)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR62, C(N)N(R62)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R62 je R63, R64, R65 ili R66;
R63 je fenil koji je nestaljen ili staljen s R63A;
R63A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R64 je heteroaril koji je nestaljen ili staljen s R64A;
R64A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R65 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R65A;
R65A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R66 je alkil, alkenil ili alkinil, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R67, OR67, SR67, S(O)R67, SO2R67, C(O)R67, CO(O)R67, OC(O)R67, OC(O)OR67, NH2, NHR67, N(R67)2, NHC(O)R67, NR67C(O)R67, NHS(O)2R67, NR67S(O)2R67, NHC(O)OR67, NR67C(O)OR67, NHC(O)NH2, NHC(O)NHR67, NHC(O)N(R67)2, NR67C(O)NHR67, NR67C(O)N(R67)2, C(O)NH2, C(O)NHR67, C(O)N(R67)2, C(O)NHOH, C(O)NHOR67, C(O)NHSO2R67, C(O)NR67SO2R67, SO2NH2, SO2NHR67, SO2N(R67)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR67, C(N)N(R67)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R67 je alkil, alkenil, alkinil, fenil, heteroaril, cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil;
pri čemu su ciklički ostaci molekula, koji su predstavljeni s R57A, R58, R59, R60, R63, R64,
R65 i R67, nesupstituirani ili supstituirani s jednim ili dva ili tri ili četiri supstituenta neovisno odabrana od R68, OR68, SR68, S(O)R68, SO2R68, C(O)R68, CO(O)R68, OC(O)R68, OC(O)OR68, NH2, NHR68, N(R68)2, NHC(O)R68, NR68C(O)R68, NHS(O)2R68, NR68S(O)2R68, NHC(O)OR68, NR68C(O)OR68, NHC(O)NH2, NHC(O)NHR68, NHC(O)N(R68)2, NR68C(O)NHR68, NR68C(O)N(R68)2, C(O)NH2, C(O)NHR68, C(O)N(R68)2, C(O)NHOH, C(O)NHOR68, C(O)NHSO2R68, C(O)NR68SO2R68, SO2NH2, SO2NHR68, SO2N(R68)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR68, C(N)N(R68)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R68 je R69, R70, R71 ili R72;
R69 je fenil koji je nestaljen ili staljen s R69A;
R69A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R70 je heteroaril koji je nestaljen ili staljen s R70A;
R70A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R71 je cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil, od kojih je svaki nestaljen ili staljen s R71A;
R71A je benzen, heteroaren, cikloalkan, cikloalken, heterocikloalkan ili heterocikloalken;
R72 je alkil, alkenil ili alkinil, od kojih je svaki nesupstituiran ili supstituiran s jednim ili dva ili tri supstituenta neovisno odabrana od R73, OR73, SR73, S(O)R73, SO2R73 C(O)R73, CO(O)R73, OC(O)R73, OC(O)OR73, NH2, NHR73, N(R73)2, NHC(O)R73, NR73C(O)R73, NHS(O)2R73, NR73S(O)2R73, NHC(O)OR73, NR73C(O)OR73, NHC(O)NH2, NHC(O)NHR73, NHC(O)N(R73)2, NR73C(O)NHR73, NR73C(O)N(R73)2, C(O)NH2, C(O)NHR73, C(O)N(R73)2, C(O)NHOH, C(O)NHOR73, C(O)NHSO2R73, C(O)NR73SO2R73, SO2NH2, SO2NHR73, SO2N(R73)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR73, C(N)N(R73)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br i I;
R73 je alkil, alkenil ili alkinil, fenil, heteroaril, cikloalkil, cikloalkenil, heterocikloalkil ili heterocikloalkenil; i
pri čemu su ostaci molekula, koji su predstavljeni s R69, R70, i R71, nesupstituirani ili supstituirani s jednim ili dva ili tri ili četiri supstituenta neovisno odabrana od NH2, C(O)NH2, C(O)NHOH, SO2NH2, CF3, CF2CF3, C(O)H, C(O)OH, C(N)NH2, OH, (O), CN, N3, NO2, OCF3, OCF2CF3, F, Cl, Br i I.
2. Spoj ili terapeutski prihvatljiva sol prema patentnom zahtjevu 1, naznačen time, da je:
4-{4-[(4’-kloro-1,1’-bifenil-2-il)metil]piperazin-1-il}-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-{4-[(4’-kloro-1,1’-bifenil-2-il)metil]piperazin-1-il}-N-({4-[(3-morfolin-4-ilpropil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(1-tetrahidro-2H-piran-4-ilpiperidin-4-il)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(1-metilpiperidin-4-il)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(4-metilpiperazin-1-il)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-ilcikloheksil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(2-metoksietil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(3-nitro-4-{[(3S)-tetrahidro-2H-piran-3-ilmetil]amino}fenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[4-(1,4-dioksan-2-ilmetoksi)-3-nitrofenil]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(3-nitro-4-{[(3R)-tetrahidro-2H-piran-3-ilmetil]amino}fenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-(2-naftilsulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(2-metoksietil)amino]-3-[(trifluorometil)sulfonil]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)-N-({4-[(tetrahidro-2H-piran-4-ilmetil)amino]-3-[(trifluorometil)sulfonil]fenil}sulfonil)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[3-nitro-4-(tetrahidro-2H-piran-4-ilmetoksi)fenil]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(1,4-dioksan-2-ilmetil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(2,2,2-trifluoroetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(3,3,3-trifluoropropil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(2S)-1,4-dioksan-2-il-metoksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
cis-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(4-{[(4-metoksi-cikloheksil)metil]amino}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(2R)-1,4-dioksan-2-il-metoksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-({4-[(1,4-dioksan-2-ilmetil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-{[4-(1,4-dioksan-2-ilmetoksi)-3-nitrofenil]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-ilcikloheksil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(4-{[(4-metoksicikloheksil)metil]amino}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-{[5-cijano-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-cijano-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(4-fluorotetrahidro-2H-piran-4-il)metoksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-{[3-(aminokarbonil)-4-(tetrahidro-2H-piran-4-ilmetoksi)fenil]sulfonil}-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
cis-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-il-cikloheksil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-kloro-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-{[5-kloro-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)-N-{[4-[(tetrahidro-2H-piran-4-ilmetil)amino]-3-(trifluorometil)fenil]sulfonil}benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)-N-({4-[(tetrahidro-2H-piran-4-ilmetil)amino]-3-[(trifluorometil)sulfonil]fenil}sulfonil)benzamid;
trans-4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil{piperazin-1-il)-N-({4-[(4-morfolin-4-ilcikloheksil)amino]-3-[(trifluorometil)sulfonil]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-({4-[(1-metilpiperidin-4-il)amino]-3-[(trifluorometil)sulfonil]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
5-({[4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzoil]amino}sulfonil)-2-(tetrahidro-2H-piran-4-ilmetoksi)nikotinamid;
N-({5-bromo-6-[(1-metilpiperidin-4-il)metoksi]piridin-3-il}sulfonil)-4-(4-{[2-(4-klorofenil)-4,4-dimetil-cikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(1-metilpiperidin-4-il)metoksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-cijano-6-(1,4-dioksan-2-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-{[5-bromo-6-(1,4-dioksan-2-ilmetoksi)piridin-3-il]sulfonil}-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(2,2-dimetiltetrahidro-2H-piran-4-il)metoksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-({3-kloro-5-cijano-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-({4-[(1-acetilpiperidin-4-il)amino]-3-nitrofenil}sulfonil)-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-({2-kloro-5-fluoro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(3-morfolin-4-ilpropil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({5-cijano-6-[(4-fluorotetrahidro-2H-piran-4-il)metoksi]piridin-3-il}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-cijano-6-(2-morfolin-4-iletoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-[(3-kloro-4-{[2-(2-metoksietoksi)etil]sulfonil}fenil)sulfonil]-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(4-{[2-(2-metoksietoksi)etil]sulfonil}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-ilcikloheksil)oksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-({5-bromo-6-[(1-tetrahidro-2H-piran-4-ilpiperidin-4-il)amino]piridin-3-il}sulfonil)-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(2-cijanoetil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
cis-4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-ilcikloheksil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-N-{[4-({4-[bis(ciklopropilmetil)amino]cikloheksil}amino)-3-nitrofenil]sulfonil}-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(4-{[(1-metilpiperidin-4-il)metil]amino}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(morfolin-3-ilmetil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-({4-[(4-metil- piperazin-1-il)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-ilbut-2-inil)oksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-etinil-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sufonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(4-okso-3,4-dihidrokinazolin-6-il)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-4-(4-{[8-(4-klorofenil)spiro[4.5]dek-7-en-7-il]metil}piperazin-1-il)-N-({4-[(4-morfolin-4-ilcikloheksil)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
cis-4-(4-{[4-(4-klorofenil)-6,6-dimetil-5,6-dihidro-2H-piran-3-il]metil}piperazin-1-il)-N-[(4-{[(4-metoksicikloheksil)metil]amino}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[8-(4-klorofenil)spiro[4.5]dek-7-en-7-il]metil}piperazin-1-il)-N-({4-[(4-fluorotetrahidro-2H-piran-4-il)metoksi]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
trans-4-(4-{[8-(4-klorofenil)spiro[4.5]dek-7-en-7-il]metil}piperazin-1-il)-N-[(4-{[(4-metoksicikloheksil)metil]amino}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-5,5-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-5,5-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-cijano-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
terc-butil 3-{[4-({[4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzoil]amino}sulfonil)-2-nitrofenoksi]metil}morfolin-4-karboksilat;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[4-(morfolin-3-ilmetoksi)-3-nitrofenil]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[8-(4-klorofenil)spiro[4.5]dek-7-en-7-il]metil}piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(4-{[1-(metilsulfonil)piperidin-4-il]amino}-3-nitrofenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({4-[(1,1-dioksidotetrahidro-2H-tiopiran-4-il)amino]-3-nitrofenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
N-[(4-kloro-3-nitrofenil)sulfonil]-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-[(3-nitro-4-{[1-(2,2,2-trifluoroetil)piperidin-4-il]amino}fenil)sulfonil]-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({5-cijano-6-[(1-tetrahidro-2H-piran-4-ilpiperidin-4-il)oksi]piridin-3-il}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-{[5-izopropil-6-(tetrahidro-2H-piran-4-ilmetoksi)piridin-3-il]sulfonil}-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
Ili
N-({3-kloro-5-fluoro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid;
ili njihova terapeutski prihvatljiva sol.
3. Spoj ili terapeutski prihvatljiva sol prema patentnom zahtjevu 1, naznačen time, da je 4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid ili njegova terapeutski prihvatljiva sol.
4. Spoj ili terapeutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da je za uporabu u liječenju pacijenta od raka mjehura, raka mozga, raka dojke, raka koštane srži, raka grlića maternice, kronične limfocitne leukemije, kolorektalnog raka, raka jednjaka, hepatocelularnog raka, limfoblastične leukemije, folikularnog limfoma, limfoidne malignosti s izvorištem u T stanici ili B stanici, melanoma, mijelogene leukemije, raka usta, raka jajnika, raka pluća nemalih stanica, mijeloma, raka prostate, raka pluća malih stanica ili raka slezene.
5. Farmaceutski pripravak, naznačen time, da sadrži pomoćno sredstvo i spoj ili terapeutski prihvatljivu sol prema bilo kojem od patentnih zahtjeva 1 do 3.
6. Spoj ili terapeutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da se upotrebljava kao lijek.
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