JP2011528040A5 - - Google Patents
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- Publication number
- JP2011528040A5 JP2011528040A5 JP2011518851A JP2011518851A JP2011528040A5 JP 2011528040 A5 JP2011528040 A5 JP 2011528040A5 JP 2011518851 A JP2011518851 A JP 2011518851A JP 2011518851 A JP2011518851 A JP 2011518851A JP 2011528040 A5 JP2011528040 A5 JP 2011528040A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrimidin
- ylamino
- pyridin
- benzamide
- hydroxy
- 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.)
- Granted
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- -1 cyano, hydroxy, hydroxy Chemical group 0.000 claims description 887
- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims description 152
- 125000000217 alkyl group Chemical group 0.000 claims description 128
- 150000001875 compounds Chemical class 0.000 claims description 87
- 229910052757 nitrogen Inorganic materials 0.000 claims description 50
- 150000003839 salts Chemical class 0.000 claims description 38
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 36
- 125000001188 haloalkyl group Chemical group 0.000 claims description 33
- 125000005843 halogen group Chemical group 0.000 claims description 33
- 125000003118 aryl group Chemical group 0.000 claims description 27
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 25
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 25
- 125000000304 alkynyl group Chemical group 0.000 claims description 22
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 21
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 12
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 12
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims description 12
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 12
- 125000005236 alkanoylamino group Chemical group 0.000 claims description 12
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 12
- 125000001589 carboacyl group Chemical group 0.000 claims description 12
- 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 12
- 201000010099 disease Diseases 0.000 claims description 12
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
- 125000004283 imidazolin-2-yl group Chemical group [H]N1C(*)=NC([H])([H])C1([H])[H] 0.000 claims description 12
- HRDXJKGNWSUIBT-UHFFFAOYSA-N methoxybenzene Chemical group [CH2]OC1=CC=CC=C1 HRDXJKGNWSUIBT-UHFFFAOYSA-N 0.000 claims description 12
- 125000004572 morpholin-3-yl group Chemical group N1C(COCC1)* 0.000 claims description 12
- DILRJUIACXKSQE-UHFFFAOYSA-N n',n'-dimethylethane-1,2-diamine Chemical compound CN(C)CCN DILRJUIACXKSQE-UHFFFAOYSA-N 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 12
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 12
- 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 description 12
- 125000004574 piperidin-2-yl group Chemical group N1C(CCCC1)* 0.000 claims description 12
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 12
- 125000006225 propoxyethyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 12
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 12
- 125000004290 pyrazolidin-3-yl group Chemical group [H]N1N([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 12
- 125000004291 pyrazolin-3-yl group Chemical group [H]C1([H])N=NC([H])(*)C1([H])[H] 0.000 claims description 12
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 11
- 125000001246 bromo group Chemical group Br* 0.000 claims description 11
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 11
- 125000001153 fluoro group Chemical group F* 0.000 claims description 11
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- 239000001257 hydrogen Substances 0.000 claims description 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 11
- 125000002912 morpholin-4-ylsulfonyl group Chemical group O1C([H])([H])C([H])([H])N(S(=O)(=O)[*])C([H])([H])C1([H])[H] 0.000 claims description 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims description 11
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 125000004423 acyloxy group Chemical group 0.000 claims description 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 8
- 125000005110 aryl thio group Chemical group 0.000 claims description 8
- 125000004104 aryloxy group Chemical group 0.000 claims description 8
- ICCBZGUDUOMNOF-UHFFFAOYSA-N azidoamine Chemical compound NN=[N+]=[N-] ICCBZGUDUOMNOF-UHFFFAOYSA-N 0.000 claims description 8
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 8
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 8
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 8
- 125000004468 heterocyclylthio group Chemical group 0.000 claims description 8
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 7
- 125000004282 imidazolidin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])N([H])C1([H])* 0.000 claims description 7
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 7
- 206010016654 Fibrosis Diseases 0.000 claims description 6
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- 230000004761 fibrosis Effects 0.000 claims description 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 6
- 125000003106 haloaryl group Chemical group 0.000 claims description 5
- OESFBXUFIOULLI-UHFFFAOYSA-N 3-[2-[4-(hydroxycarbamoyl)anilino]pyrimidin-4-yl]-2-methylimidazo[1,2-a]pyridine-7-carboxylic acid Chemical compound CC=1N=C2C=C(C(O)=O)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 OESFBXUFIOULLI-UHFFFAOYSA-N 0.000 claims description 4
- CKLAVVIGLANTRR-UHFFFAOYSA-N 3-[2-[4-[(2-aminophenyl)carbamoyl]anilino]pyrimidin-4-yl]-2-methylimidazo[1,2-a]pyridine-7-carboxylic acid Chemical compound CC=1N=C2C=C(C(O)=O)C=CN2C=1C(N=1)=CC=NC=1NC(C=C1)=CC=C1C(=O)NC1=CC=CC=C1N CKLAVVIGLANTRR-UHFFFAOYSA-N 0.000 claims description 4
- BBISEGSBCVOASE-UHFFFAOYSA-N 4-[[4-(7-cyano-2-methylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C=C(C#N)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 BBISEGSBCVOASE-UHFFFAOYSA-N 0.000 claims description 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 4
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- MPNKIHDEASYURU-UHFFFAOYSA-N methyl 3-[2-[4-(hydroxycarbamoyl)anilino]pyrimidin-4-yl]-2-methylimidazo[1,2-a]pyridine-7-carboxylate Chemical compound CC=1N=C2C=C(C(=O)OC)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 MPNKIHDEASYURU-UHFFFAOYSA-N 0.000 claims description 4
- HFXAVTRLAAABKN-UHFFFAOYSA-N methyl 3-[2-[4-[(2-aminophenyl)carbamoyl]anilino]pyrimidin-4-yl]-2-methylimidazo[1,2-a]pyridine-7-carboxylate Chemical compound CC=1N=C2C=C(C(=O)OC)C=CN2C=1C(N=1)=CC=NC=1NC(C=C1)=CC=C1C(=O)NC1=CC=CC=C1N HFXAVTRLAAABKN-UHFFFAOYSA-N 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 241001465754 Metazoa Species 0.000 claims description 3
- 230000024245 cell differentiation Effects 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims description 2
- CAMKEDDAEGTLQE-UHFFFAOYSA-N 3-[2-[4-(hydroxycarbamoyl)anilino]pyrimidin-4-yl]-n-(2-methoxyethyl)-2-methylimidazo[1,2-a]pyridine-6-carboxamide Chemical compound N12C=C(C(=O)NCCOC)C=CC2=NC(C)=C1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 CAMKEDDAEGTLQE-UHFFFAOYSA-N 0.000 claims description 2
- NDPMVITZRVBZIP-UHFFFAOYSA-N 3-[2-[4-(hydroxycarbamoyl)anilino]pyrimidin-4-yl]-n-(2-methoxyethyl)-2-methylimidazo[1,2-a]pyridine-7-carboxamide Chemical compound CC=1N=C2C=C(C(=O)NCCOC)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 NDPMVITZRVBZIP-UHFFFAOYSA-N 0.000 claims description 2
- DAWDFYSVFPONIF-UHFFFAOYSA-N 3-[2-[4-[(2-aminophenyl)carbamoyl]anilino]pyrimidin-4-yl]-n-(2-methoxyethyl)-2-methylimidazo[1,2-a]pyridine-6-carboxamide Chemical compound N12C=C(C(=O)NCCOC)C=CC2=NC(C)=C1C(N=1)=CC=NC=1NC(C=C1)=CC=C1C(=O)NC1=CC=CC=C1N DAWDFYSVFPONIF-UHFFFAOYSA-N 0.000 claims description 2
- SOFKWBBPHGWRDT-UHFFFAOYSA-N 3-[2-[4-[(2-aminophenyl)carbamoyl]anilino]pyrimidin-4-yl]-n-(2-methoxyethyl)-2-methylimidazo[1,2-a]pyridine-7-carboxamide Chemical compound CC=1N=C2C=C(C(=O)NCCOC)C=CN2C=1C(N=1)=CC=NC=1NC(C=C1)=CC=C1C(=O)NC1=CC=CC=C1N SOFKWBBPHGWRDT-UHFFFAOYSA-N 0.000 claims description 2
- RIGBYBCOVJYBBY-UHFFFAOYSA-N 3-[2-[4-[(2-aminophenyl)carbamoyl]anilino]pyrimidin-4-yl]-n-[2-(dimethylamino)ethyl]-2-methylimidazo[1,2-a]pyridine-6-carboxamide Chemical compound N12C=C(C(=O)NCCN(C)C)C=CC2=NC(C)=C1C(N=1)=CC=NC=1NC(C=C1)=CC=C1C(=O)NC1=CC=CC=C1N RIGBYBCOVJYBBY-UHFFFAOYSA-N 0.000 claims description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- KAAFMWRALVXNBT-UHFFFAOYSA-N 4-[(5-fluoro-4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]-n-hydroxybenzamide Chemical compound C1=CC(C(=O)NO)=CC=C1NC1=NC=C(F)C(C=2N3C=CC=CC3=NC=2)=N1 KAAFMWRALVXNBT-UHFFFAOYSA-N 0.000 claims description 2
- AXCRSHHXKNOKDN-UHFFFAOYSA-N 4-[[4-(6-bromo-2-methylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C=CC(Br)=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 AXCRSHHXKNOKDN-UHFFFAOYSA-N 0.000 claims description 2
- DPSUFYYVOMYUMR-UHFFFAOYSA-N 4-[[4-(6-chloro-2-methylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C=CC(Cl)=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 DPSUFYYVOMYUMR-UHFFFAOYSA-N 0.000 claims description 2
- GCFVULJYFNGILX-UHFFFAOYSA-N 4-[[4-(8-fluoro-2-methylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C(F)=CC=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 GCFVULJYFNGILX-UHFFFAOYSA-N 0.000 claims description 2
- YOZOOKSSOZEZFV-UHFFFAOYSA-N 4-[[4-[7-[(dimethylamino)methyl]-2-methylimidazo[1,2-a]pyridin-3-yl]pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C=C(CN(C)C)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 YOZOOKSSOZEZFV-UHFFFAOYSA-N 0.000 claims description 2
- WHQAPHUQNJPKBH-UHFFFAOYSA-N 4-[[4-[7-[(dimethylamino)methyl]imidazo[1,2-a]pyridin-3-yl]pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound C=1N=C2C=C(CN(C)C)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 WHQAPHUQNJPKBH-UHFFFAOYSA-N 0.000 claims description 2
- CFHABVVISFTSNR-UHFFFAOYSA-N 4-[[4-[7-[2-(dimethylamino)ethoxy]-2-methylimidazo[1,2-a]pyridin-3-yl]pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C=C(OCCN(C)C)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 CFHABVVISFTSNR-UHFFFAOYSA-N 0.000 claims description 2
- HYQBPZLHKKSALZ-UHFFFAOYSA-N 4-[[4-[7-[2-(dimethylamino)ethylamino]-2-methylimidazo[1,2-a]pyridin-3-yl]pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound CC=1N=C2C=C(NCCN(C)C)C=CN2C=1C(N=1)=CC=NC=1NC1=CC=C(C(=O)NO)C=C1 HYQBPZLHKKSALZ-UHFFFAOYSA-N 0.000 claims description 2
- XBQQYRDGPWFCPA-UHFFFAOYSA-N 4-[ethyl-(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]-n-hydroxybenzamide Chemical compound N=1C=CC(C=2N3C=CC=CC3=NC=2)=NC=1N(CC)C1=CC=C(C(=O)NO)C=C1 XBQQYRDGPWFCPA-UHFFFAOYSA-N 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- WYWHKKSPHMUBEB-UHFFFAOYSA-N 6-Mercaptoguanine Natural products N1C(N)=NC(=S)C2=C1N=CN2 WYWHKKSPHMUBEB-UHFFFAOYSA-N 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 102000015790 Asparaginase Human genes 0.000 claims description 2
- 108010024976 Asparaginase Proteins 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 108010006654 Bleomycin Proteins 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 2
- 102000003964 Histone deacetylase Human genes 0.000 claims description 2
- 108090000353 Histone deacetylase Proteins 0.000 claims description 2
- 208000024934 IgG4-related mediastinitis Diseases 0.000 claims description 2
- 208000014919 IgG4-related retroperitoneal fibrosis Diseases 0.000 claims description 2
- 208000026350 Inborn Genetic disease Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 2
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- 229930192392 Mitomycin Natural products 0.000 claims description 2
- 206010028594 Myocardial fibrosis Diseases 0.000 claims description 2
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 208000025966 Neurological disease Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 229930012538 Paclitaxel Natural products 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010036805 Progressive massive fibrosis Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 206010038979 Retroperitoneal fibrosis Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims description 2
- JKOQGQFVAUAYPM-UHFFFAOYSA-N amifostine Chemical compound NCCCNCCSP(O)(O)=O JKOQGQFVAUAYPM-UHFFFAOYSA-N 0.000 claims description 2
- 229960001097 amifostine Drugs 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 229960003272 asparaginase Drugs 0.000 claims description 2
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| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2170882A1 (en) * | 2007-06-26 | 2010-04-07 | Gilead Colorado, Inc. | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| TW200922564A (en) | 2007-09-10 | 2009-06-01 | Curis Inc | CDK inhibitors containing a zinc binding moiety |
| JP5640005B2 (ja) * | 2008-07-14 | 2014-12-10 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｄａｃおよび／またはｃｄｋ阻害剤としてのイミダゾシルピリジン化合物 |
| NZ590320A (en) | 2008-07-14 | 2012-12-21 | Gilead Sciences Inc | Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases |
| CA2728228A1 (en) * | 2008-07-14 | 2010-01-21 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
| MX2011001090A (es) * | 2008-07-28 | 2011-03-15 | Gilead Sciences Inc | Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno. |
| WO2010028192A1 (en) | 2008-09-03 | 2010-03-11 | Repligen Corporation | Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors |
| ES2712074T3 (es) | 2008-12-03 | 2019-05-09 | Scripps Research Inst | Cultivos de células madre |
| WO2010075542A1 (en) | 2008-12-23 | 2010-07-01 | Curis, Inc. | Cdk inhibitors |
| MX2011013166A (es) * | 2009-06-08 | 2012-01-30 | Gilead Sciences Inc | Compuestos inhibidores de hdac de cicloalquilcarbamatobenzamida-an ilina. |
| WO2010144371A1 (en) | 2009-06-08 | 2010-12-16 | Gilead Colorado, Inc. | Alkanoylamino benzamide aniline hdac inihibitor compounds |
| PL2475428T3 (pl) | 2009-09-11 | 2015-12-31 | Probiodrug Ag | Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej |
| EA020847B1 (ru) | 2009-10-30 | 2015-02-27 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-b]ПИРИДАЗИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE10 |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| EP3067346A1 (en) * | 2010-11-16 | 2016-09-14 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US9540395B2 (en) | 2011-02-28 | 2017-01-10 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| JP6010557B2 (ja) * | 2011-03-02 | 2016-10-19 | リード ディスカバリー センター ゲーエムベーハー | 薬学的活性化二置換トリアジン誘導体 |
| US9242937B2 (en) | 2011-03-02 | 2016-01-26 | Bayer Intellectual Property Gmbh | Pharmaceutically active disubstituted pyridine derivatives |
| ES2613103T3 (es) | 2011-04-19 | 2017-05-22 | Bayer Intellectual Property Gmbh | 4-Aril-n-fenil-1,3,5-triacin-2-aminas sustituidas |
| TWI555737B (zh) | 2011-05-24 | 2016-11-01 | 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 |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| CN103917527B (zh) | 2011-09-16 | 2017-05-31 | 拜耳知识产权有限责任公司 | 二取代的5‑氟‑嘧啶 |
| US9133171B2 (en) | 2011-09-16 | 2015-09-15 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| HUE030534T2 (hu) | 2012-04-27 | 2017-05-29 | Eisai R&D Man Co Ltd | Eljárás 5-(difluormetil)pirazin-2-karbonsav elõállítására és elõállítási intermediere |
| UA125503C2 (uk) | 2012-06-13 | 2022-04-13 | Інсайт Холдинґс Корпорейшн | Заміщені трициклічні сполуки як інгібітори fgfr |
| EP2863909B1 (en) | 2012-06-26 | 2020-11-04 | Janssen Pharmaceutica N.V. | Combinations comprising 4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline compounds as pde 2 inhibitors and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| MX362197B (es) | 2012-07-09 | 2019-01-08 | Janssen Pharmaceutica Nv | Derivados de imidazo[1,2-b]piridazina e imidazo[1,2-a]pirazina como inhibidores de la fosfodiesterasa 10; y el uso de los mismos en el tratamiento de trastornos neurológicos, psiquiátricos y metabólicos. |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| JP6277195B2 (ja) | 2012-10-18 | 2018-02-07 | バイエル ファーマ アクチエンゲゼルシャフト | スルホン基を含んでいる５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体 |
| ES2597232T3 (es) | 2012-10-18 | 2017-01-17 | Bayer Pharma Aktiengesellschaft | 4-(orto)-fluorofenil-5-fluoropirimidin-2-il aminas que contienen un grupo sulfona |
| 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 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| RU2665554C2 (ru) | 2013-03-15 | 2018-08-31 | Байомарин Фармасьютикал Инк. | Ингибиторы hdac |
| MY181497A (en) | 2013-04-19 | 2020-12-23 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| ES2929576T3 (es) | 2013-10-08 | 2022-11-30 | Acetylon Pharmaceuticals Inc | Combinaciones de inhibidores de histona deacetilasa 6 y el inhibidor de Her2 lapatinib para el uso en el tratamiento del cáncer de mama |
| ES2862126T3 (es) | 2013-10-10 | 2021-10-07 | Acetylon Pharmaceuticals Inc | Compuestos de pirimidín-hidroxiamida como inhibidores de histona desacetilasa |
| EP3060217B1 (en) | 2013-10-24 | 2022-06-08 | Mayo Foundation for Medical Education and Research | Treatment of polycystic diseases with an hdac6 inhibitor |
| MX2016007251A (es) | 2013-12-03 | 2016-09-07 | Acetylon Pharmaceuticals Inc | Combinaciones de inhibidores de histona deacetilasa y farmacos inmunomoduladores. |
| GB201321736D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| PL3091008T3 (pl) * | 2013-12-31 | 2018-12-31 | Xuanzhu Pharma Co., Ltd. | Inhibitor kinazy i jego zastosowanie |
| US9464073B2 (en) | 2014-02-26 | 2016-10-11 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors |
| EA201790142A1 (ru) | 2014-07-07 | 2017-07-31 | Эситайлон Фармасьютикалз, Инк. | Лечение лейкоза ингибиторами гистондеацетилазы |
| CA2964683A1 (en) | 2014-10-16 | 2016-04-21 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| AU2015356779A1 (en) | 2014-12-05 | 2017-07-13 | University of Modena and Reggio Emilia | Combinations of histone deacetylase inhibitors and bendamustine for use in the treatment of lymphoma |
| HK1245260A1 (zh) | 2014-12-23 | 2018-08-24 | Dana-Farber Cancer Institute, Inc. | 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂 |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| EP3273963A1 (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 lymphomas |
| US20180078560A1 (en) | 2015-03-24 | 2018-03-22 | 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 |
| 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 |
| JP6861166B2 (ja) | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| US10272084B2 (en) | 2015-06-01 | 2019-04-30 | Regenacy Pharmaceuticals, Llc | Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy |
| US10695346B2 (en) | 2015-06-26 | 2020-06-30 | Dana-Farber Cancer Institute, Inc. | 4,6-pyrimidinylene derivatives and uses thereof |
| CN105111154A (zh) * | 2015-09-15 | 2015-12-02 | 上海瑞博化学有限公司 | 一种5-氨基吡嗪-2-甲酸合成新工艺 |
| JP6847099B2 (ja) | 2015-09-29 | 2021-03-24 | バイエル ファーマ アクチエンゲゼルシャフト | 新規な大環状スルホンジイミン化合物 |
| ES2819869T3 (es) | 2015-10-08 | 2021-04-19 | Bayer Pharma AG | Nuevos compuestos macrocíclicos modificados |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| EP3445364A4 (en) | 2016-04-19 | 2019-11-27 | Acetylon Pharmaceuticals, Inc. | HDAC INHIBITORS, ONLY OR IN COMBINATION WITH BTK INHIBITORS, FOR THE TREATMENT OF CHRONIC LYMPHOCYTIC LEUKEMIA |
| CN106543041A (zh) * | 2016-05-22 | 2017-03-29 | 上海清松制药有限公司 | 一种对胍基苯甲酸盐酸盐的合成方法 |
| BR112019005526A2 (pt) | 2016-10-20 | 2019-06-18 | Pfizer | agentes antiproliferativos para tratamento de pah |
| EP3544685B1 (en) | 2016-11-22 | 2023-01-04 | Development Center for Biotechnology | Hetroarylamine compounds for modulating the hedgehog pathway and preparing method and uses thereof |
| KR102719387B1 (ko) * | 2017-01-26 | 2024-10-21 | 한미약품 주식회사 | 이미다조피리다진 화합물 |
| SG11201907095UA (en) | 2017-02-01 | 2019-08-27 | Aucentra Therapeutics Pty Ltd | DERIVATIVES OF N-CYCLOALKYL/HETEROCYCLOALKYL-4-(IMIDAZO [1,2-a]PYRIDINE)PYRIMIDIN-2-AMINE AS THERAPEUTIC AGENTS |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| US11242356B2 (en) | 2017-03-28 | 2022-02-08 | Bayer Aktiengesellschaft | PTEFb inhibiting macrocyclic compounds |
| CN110536890B (zh) | 2017-04-26 | 2023-08-15 | 巴斯利尔药物国际股份公司 | 制备呋咱并苯并咪唑及其晶型的方法 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CA3090843A1 (en) | 2018-02-13 | 2019-08-22 | Bayer Aktiengesellschaft | 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 |
| BR112020022392A2 (pt) | 2018-05-04 | 2021-02-02 | Incyte Corporation | formas sólidas de um inibidor de fgfr e processos para preparação das mesmas |
| PE20210919A1 (es) | 2018-05-04 | 2021-05-19 | Incyte Corp | Sales de un inhibidor de fgfr |
| EP3810132A4 (en) | 2018-06-25 | 2022-06-22 | Dana-Farber Cancer Institute, Inc. | TAIRE FAMILY KINASE INHIBITORS AND RELATED USES |
| CA3124422A1 (en) | 2018-12-28 | 2020-07-02 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| CN111925366B (zh) * | 2019-05-13 | 2024-04-09 | 广东阿格蕾雅光电材料有限公司 | 一种咪唑并氮杂环化合物及其应用 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021003517A1 (en) * | 2019-07-10 | 2021-01-14 | Aucentra Therapeutics Pty Ltd | Derivatives of 4-(imidazo[l,2-a]pyridin-3-yl)-n-(pyridinyl)pyrimidin- 2-amine as therapeutic agents |
| CN118955500A (zh) * | 2019-07-24 | 2024-11-15 | 默克专利股份公司 | 4-(咪唑并[1,2-a]吡啶-3-基)-嘧啶衍生物 |
| CN110294759B (zh) * | 2019-08-08 | 2020-05-08 | 河南省人民医院 | Hdac6选择性抑制剂 |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021072475A1 (en) * | 2019-10-15 | 2021-04-22 | Aucentra Therapeutics Pty Ltd | Derivatives of 4-(imidazo[1,2-a]pyridin-3-yl)-n-(pyridin-3-yl) pyrimidin-2- amine for treating proliferative diseases and conditions |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| PE20221504A1 (es) | 2019-12-04 | 2022-09-30 | Incyte Corp | Derivados de un inhibidor de fgfr |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021204626A1 (en) | 2020-04-06 | 2021-10-14 | Almirall, S.A. | Aryl and heteroaryl-carboxamide substituted heteroaryl compounds as tyk2 inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| BR112023022763A2 (pt) | 2021-05-06 | 2024-01-02 | Bayer Ag | Imidazóis anulados substituídos por alquilamida e uso dos mesmos como inseticidas |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313611A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| CN114591229A (zh) * | 2022-03-04 | 2022-06-07 | 苏州金蚕新材料科技有限公司 | 高效安全的2-氨基-5-卤吡啶合成2-氨基-5-羟基吡啶的方法 |
| WO2024127350A1 (en) | 2022-12-16 | 2024-06-20 | Astrazeneca Ab | 2,6,9-trisubstituted purines |
Family Cites Families (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ221798A3 (cs) | 1996-01-16 | 1999-10-13 | Bristol-Myers Squibb Company | Konformačně omezené aromatické inhibitory mikrosomálního proteinu transferu triglycerinu a způsob |
| US20020168761A1 (en) | 2000-01-24 | 2002-11-14 | Gour Barbara J. | Peptidomimetic modulators of cell adhesion |
| US20040006011A1 (en) | 1996-07-12 | 2004-01-08 | Gour Barbara J. | Peptidomimetic modulators of cell adhesion |
| US6174905B1 (en) | 1996-09-30 | 2001-01-16 | Mitsui Chemicals, Inc. | Cell differentiation inducer |
| US5760246A (en) | 1996-12-17 | 1998-06-02 | Biller; Scott A. | Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method |
| US6307049B1 (en) | 1998-09-30 | 2001-10-23 | The Procter & Gamble Co. | Heterocyclic 2-substituted ketoamides |
| GB9919778D0 (en) * | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
| CA2385592C (en) | 1999-09-17 | 2011-01-11 | Bing-Yan Zhu | Benzamides and related inhibitors of factor xa |
| WO2001056989A2 (en) | 2000-02-01 | 2001-08-09 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
| CN1173975C (zh) | 2000-04-27 | 2004-11-03 | 山之内制药株式会社 | 咪唑并吡啶衍生物 |
| US6403588B1 (en) | 2000-04-27 | 2002-06-11 | Yamanouchi Pharmaceutical Co., Ltd. | Imidazopyridine derivatives |
| WO2002000651A2 (en) | 2000-06-27 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Factor xa inhibitors |
| WO2002026712A2 (en) | 2000-09-29 | 2002-04-04 | Millennium Pharmaceuticals, Inc. | Quaternary amines and related inhibitors of factor xa |
| WO2002034748A1 (fr) | 2000-10-24 | 2002-05-02 | Sankyo Company, Limited | Derives d'imidazopyridine |
| US7429599B2 (en) | 2000-12-06 | 2008-09-30 | Signal Pharmaceuticals, Llc | Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK |
| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| ATE416175T1 (de) | 2001-02-20 | 2008-12-15 | Astrazeneca Ab | 2-arylaminopyrimidine zur behandlung von mit gsk3 in zusammenhang stehenden erkrankungen |
| SE0100569D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | New compounds |
| CA2442654A1 (en) | 2001-04-10 | 2002-10-10 | Transtech Pharma, Inc. | Probes, systems, and methods for drug discovery |
| HUP0400266A2 (hu) | 2001-06-21 | 2004-08-30 | Smithkline Beecham Corp. | Imidazo[1,2-a]piridin-származékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk herpeszvírus-fertőzések megelőzésére vagy kezelésére |
| WO2003000682A1 (en) | 2001-06-25 | 2003-01-03 | Merck & Co., Inc. | (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds |
| EP1270551A1 (en) | 2001-06-26 | 2003-01-02 | Aventis Pharma Deutschland GmbH | Urea derivatives with antiproteolytic activity |
| US7868204B2 (en) * | 2001-09-14 | 2011-01-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
| EP1432712B1 (en) | 2001-10-05 | 2006-05-17 | SmithKline Beecham Corporation | Imidazo-pyridine derivatives for use in the treatment of herpes viral infection |
| EP1446115B1 (en) | 2001-11-13 | 2008-02-27 | Merck Frosst Canada Ltd. | Cyanoalkylamino derivatives as protease inhibitors |
| US6995144B2 (en) | 2002-03-14 | 2006-02-07 | Eisai Co., Ltd. | Nitrogen containing heterocyclic compounds and medicines containing the same |
| JP2003313126A (ja) | 2002-04-23 | 2003-11-06 | Sankyo Co Ltd | イミダゾピリジン誘導体を有効成分とする医薬 |
| JP2004002826A (ja) | 2002-04-24 | 2004-01-08 | Sankyo Co Ltd | 高分子イミダゾピリジン誘導体 |
| US20040034084A1 (en) | 2002-05-24 | 2004-02-19 | Celgene Corporation | Methods for using JNK inhibitors for treating or preventing disease-related wasting |
| GB0212049D0 (en) | 2002-05-24 | 2002-07-03 | Merck Sharp & Dohme | Therapeutic agents |
| CA2388358A1 (en) | 2002-05-31 | 2003-11-30 | Voiceage Corporation | A method and device for multi-rate lattice vector quantization |
| UA80296C2 (en) | 2002-09-06 | 2007-09-10 | Biogen Inc | Imidazolopyridines and methods of making and using the same |
| KR20050074487A (ko) | 2002-10-17 | 2005-07-18 | 메틸진, 인크. | 히스톤 데아세틸라아제의 억제제 |
| US20040087642A1 (en) | 2002-10-24 | 2004-05-06 | Zeldis Jerome B. | Methods of using and compositions comprising a JNK inhibitor for the treatment, prevention, management and/or modification of pain |
| US20040092568A1 (en) | 2002-10-31 | 2004-05-13 | Zeldis Jerome B. | Methods for the treatment, prevention and management of macular degeneration |
| BR0316680A (pt) | 2002-11-28 | 2005-10-18 | Schering Ag | Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos |
| US20050019366A1 (en) | 2002-12-31 | 2005-01-27 | Zeldis Jerome B. | Drug-coated stents and methods of use therefor |
| TW200424174A (en) | 2003-02-06 | 2004-11-16 | Hoffmann La Roche | New TP diamide |
| US7208491B2 (en) | 2003-02-07 | 2007-04-24 | Hoffmann-La Roche Inc. | N-monoacylated o-phenylenediamines |
| WO2004076452A1 (en) | 2003-02-26 | 2004-09-10 | Merck Sharp & Dohme Limited | 5,8-DIFLUOROIMIDAZO[1,2-a]PYRIDINES AS GABA-A α2/α3 LIGANDS FOR TREATING ANXIETY AND/OR DEPRESSION |
| US7320989B2 (en) | 2003-02-28 | 2008-01-22 | Encysive Pharmaceuticals, Inc. | Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists |
| AU2004220648B2 (en) | 2003-03-06 | 2010-09-16 | Boehringer Ingelheim Animal Health USA Inc. | Antiprotozoal imidazopyridine compounds |
| HRP20090487T1 (hr) | 2003-04-07 | 2009-12-31 | Pharmacyclics | Hidroksamati kao terapeutski agensi |
| US20050187266A1 (en) | 2003-04-15 | 2005-08-25 | Pfizer Inc | Alpha substituted carboxylic acids |
| US20050234066A1 (en) | 2004-04-15 | 2005-10-20 | Agouron Pharmaceuticals, Inc. | Alpha substituted carboxylic acids |
| AU2004230316A1 (en) | 2003-04-15 | 2004-10-28 | Pfizer Inc. | Alpha substituted carboxylic acid as PPAR modulators |
| MXPA05012281A (es) | 2003-05-14 | 2006-05-19 | Torreypines Therapeutics Inc | Compuestos y uso de los mismos en la modulacion beta amiloide. |
| GB0311274D0 (en) * | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| WO2005006945A2 (en) | 2003-07-03 | 2005-01-27 | The Salk Institute For Biological Studies | Methods for treating neural disorders and compounds useful therefor |
| EP1663953A1 (en) | 2003-09-24 | 2006-06-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| ES2651730T3 (es) | 2003-09-26 | 2018-01-29 | Exelixis, Inc. | Moduladores c-Met y métodos de uso |
| CN1901903A (zh) | 2003-11-06 | 2007-01-24 | 细胞基因公司 | 用于治疗和控制石棉相关性疾病和病症的包含jnk抑制剂的组合物以及其使用方法 |
| US7524851B2 (en) | 2003-12-05 | 2009-04-28 | Robert Bosch Gesellschaft Fur Medizinische Forschung (Rbmf) | Diagnostic methods for therapeutic compounds and methods for monitoring azathioprine therapy |
| US7429590B2 (en) | 2003-12-10 | 2008-09-30 | Merck & Co. Inc. | Antiprotozoal imidazopyridine compounds |
| US7671181B2 (en) | 2004-01-16 | 2010-03-02 | Merck Sharp & Dohme Corp. | Polynucleotides encoding coccidian parasite casein kinase I, a chemotherapeutic target for antiprotozoal agents |
| WO2005077368A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| DE102004008141A1 (de) | 2004-02-19 | 2005-09-01 | Abbott Gmbh & Co. Kg | Guanidinverbindungen und ihre Verwendung als Bindungspartner für 5-HT5-Rezeptoren |
| US20070093492A1 (en) | 2004-03-09 | 2007-04-26 | Weir-Torn Jiaang | Pyrrolidine derivatives |
| MXPA06010900A (es) | 2004-03-26 | 2007-02-21 | Methylgene Inc | Inhibidores de histona desacetilasa. |
| US7253204B2 (en) | 2004-03-26 | 2007-08-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| MXPA06012130A (es) | 2004-04-20 | 2007-01-31 | Transtech Pharma Inc | Derivados de tiazol y pirimidina substituidos como moduladores del receptor de melanocortina. |
| EP1755592A1 (en) | 2004-04-20 | 2007-02-28 | AB Science | Use of c-kit inhibitors for treating inflammatory muscle disorders including myositis and muscular dystrophy |
| WO2005102318A1 (en) | 2004-04-20 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating hiv related diseases |
| US20080004279A1 (en) | 2004-04-23 | 2008-01-03 | Alain Moussy | Use of C-Kit Inhibitors for Treating Plasmodium Related Diseases |
| WO2005102326A2 (en) | 2004-04-23 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating renal diseases |
| CA2564574A1 (en) | 2004-04-23 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating fibrosis |
| US20070249628A1 (en) | 2004-05-18 | 2007-10-25 | Alain Moussy | Use of Mast Cells Inhibitors for Treating Patients Exposed to Chemical or Biological Weapons |
| WO2005115385A1 (en) | 2004-05-24 | 2005-12-08 | Ab Science | Use of c-kit inhibitors for treating acne |
| WO2005115304A2 (en) | 2004-05-24 | 2005-12-08 | Ab Science | Use of c-kit inhibitors for treating fibrodysplasia |
| PL1781639T3 (pl) * | 2004-07-28 | 2012-07-31 | Janssen Pharmaceutica Nv | Podstawione pochodne indolilo-alkiloaminowe jako nowe inhibitory deacetylazy histonowej |
| WO2006038001A1 (en) | 2004-10-06 | 2006-04-13 | Celltech R & D Limited | Aminopyrimidine derivatives as jnk inhibitors |
| JP2008516962A (ja) | 2004-10-15 | 2008-05-22 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | 血管傷害を治療する方法 |
| CN101102767A (zh) | 2004-11-23 | 2008-01-09 | 细胞基因公司 | 用jnk抑制剂治疗和控制中枢神经系统损伤的方法和组合物 |
| MX2007006109A (es) | 2004-12-01 | 2007-10-04 | Devgen Nv | Derivados de tiazol sustituidos en 5-carboxamido que interactuan con canales de iones, en particular con canales ionicos de la familia de kv. |
| AU2005315392B2 (en) | 2004-12-17 | 2010-03-11 | Astrazeneca Ab | 4- (4- (imidazol-4-yl) pyrimidin-2-ylamino) benzamides as CDK inhibitors |
| WO2006070943A1 (ja) | 2004-12-28 | 2006-07-06 | Takeda Pharmaceutical Company Limited | 縮合イミダゾール化合物およびその用途 |
| EP1841766A1 (en) | 2005-01-19 | 2007-10-10 | Biolipox AB | Pyrrolopyridines useful in the treatment of inflammation |
| US20060223807A1 (en) | 2005-03-29 | 2006-10-05 | University Of Massachusetts Medical School, A Massachusetts Corporation | Therapeutic methods for type I diabetes |
| EP1874759A4 (en) | 2005-04-06 | 2009-07-15 | Exelixis Inc | C-MET MODULATORS MODULATORS AND METHODS OF USE |
| CA2607617A1 (en) | 2005-05-09 | 2006-11-16 | Achillion Pharmaceuticals, Inc. | Thiazole compounds and methods of use |
| JP4528918B2 (ja) | 2005-06-21 | 2010-08-25 | 学校法人 関西大学 | カルボキサミド誘導体 |
| CN101223161A (zh) | 2005-06-24 | 2008-07-16 | 健亚生物科技公司 | 治疗病毒感染的杂芳基衍生物 |
| US7309787B2 (en) | 2005-07-13 | 2007-12-18 | Allergan, Inc. | Kinase inhibitors |
| WO2007026251A2 (en) | 2005-07-14 | 2007-03-08 | Ab Science | Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma |
| CN101304736A (zh) | 2005-09-07 | 2008-11-12 | 雪兰诺实验室公司 | 治疗子宫内膜异位症的ikk抑制剂 |
| RU2405770C2 (ru) | 2005-09-27 | 2010-12-10 | Сионоги Энд Ко., Лтд. | Производное сульфонамида, обладающее антагонистической активностью в отношении рецептора pgd2 |
| US7745428B2 (en) | 2005-09-30 | 2010-06-29 | Astrazeneca Ab | Imidazo[1,2-A]pyridine having anti-cell-proliferation activity |
| AR058073A1 (es) | 2005-10-03 | 2008-01-23 | Astrazeneca Ab | Derivados de imidazol 5-il-pirimidina, procesos de obtencion, composiciones farmaceuticas y usos |
| ITMI20060296A1 (it) | 2006-02-17 | 2007-08-18 | Alberto Lodolo | Dispositivo di intercettazione multifunzionale |
| EP1996233A2 (en) | 2006-02-27 | 2008-12-03 | Gilead Colorado, Inc. | Combinations comprising a histone deacetylase inhibiting agent and a nuclear hormone receptor ligand for treating cardiovascular conditions |
| AU2007243519A1 (en) | 2006-04-26 | 2007-11-08 | Merck Sharp & Dohme Corp. | Disubstituted aniline compounds |
| AU2007296744A1 (en) * | 2006-09-11 | 2008-03-20 | Curis, Inc. | Multi-functional small molecules as anti-proliferative agents |
| EP2170882A1 (en) | 2007-06-26 | 2010-04-07 | Gilead Colorado, Inc. | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| CA2728228A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
| NZ590320A (en) | 2008-07-14 | 2012-12-21 | Gilead Sciences Inc | Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases |
| JP5640005B2 (ja) | 2008-07-14 | 2014-12-10 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｄａｃおよび／またはｃｄｋ阻害剤としてのイミダゾシルピリジン化合物 |
| MX2011001090A (es) | 2008-07-28 | 2011-03-15 | Gilead Sciences Inc | Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno. |
| MX2011013166A (es) | 2009-06-08 | 2012-01-30 | Gilead Sciences Inc | Compuestos inhibidores de hdac de cicloalquilcarbamatobenzamida-an ilina. |
| WO2010144371A1 (en) | 2009-06-08 | 2010-12-16 | Gilead Colorado, Inc. | Alkanoylamino benzamide aniline hdac inihibitor compounds |
-
2009
- 2009-07-14 NZ NZ590320A patent/NZ590320A/xx not_active IP Right Cessation
- 2009-07-14 EP EP09790408A patent/EP2303881A2/en not_active Withdrawn
- 2009-07-14 NZ NZ602832A patent/NZ602832A/en not_active IP Right Cessation
- 2009-07-14 CA CA2729965A patent/CA2729965A1/en not_active Abandoned
- 2009-07-14 JP JP2011518851A patent/JP5640006B2/ja not_active Expired - Fee Related
- 2009-07-14 AU AU2009271019A patent/AU2009271019A1/en not_active Abandoned
- 2009-07-14 US US12/502,967 patent/US8124764B2/en not_active Expired - Fee Related
- 2009-07-14 WO PCT/US2009/050577 patent/WO2010009155A2/en not_active Ceased
-
2014
- 2014-01-07 JP JP2014000750A patent/JP2014088420A/ja not_active Withdrawn
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