JP2018511626A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018511626A5 JP2018511626A5 JP2017553414A JP2017553414A JP2018511626A5 JP 2018511626 A5 JP2018511626 A5 JP 2018511626A5 JP 2017553414 A JP2017553414 A JP 2017553414A JP 2017553414 A JP2017553414 A JP 2017553414A JP 2018511626 A5 JP2018511626 A5 JP 2018511626A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- pharmaceutically acceptable
- acceptable salt
- cycloalkyl
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 97
- 229910052739 hydrogen Inorganic materials 0.000 claims 77
- 239000001257 hydrogen Substances 0.000 claims 77
- 150000001875 compounds Chemical class 0.000 claims 75
- 150000003839 salts Chemical class 0.000 claims 70
- 150000002431 hydrogen Chemical class 0.000 claims 64
- 125000000623 heterocyclic group Chemical group 0.000 claims 53
- 125000000753 cycloalkyl group Chemical group 0.000 claims 51
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 48
- 229910052736 halogen Inorganic materials 0.000 claims 47
- 150000002367 halogens Chemical class 0.000 claims 47
- 125000003710 aryl alkyl group Chemical group 0.000 claims 46
- 125000003118 aryl group Chemical group 0.000 claims 46
- 125000001072 heteroaryl group Chemical group 0.000 claims 45
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 45
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 45
- VOPWNXZWBYDODV-UHFFFAOYSA-N Chlorodifluoromethane Chemical compound FC(F)Cl VOPWNXZWBYDODV-UHFFFAOYSA-N 0.000 claims 34
- 125000003545 alkoxy group Chemical group 0.000 claims 34
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 18
- 125000004434 sulfur atom Chemical group 0.000 claims 18
- 229910052757 nitrogen Inorganic materials 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 16
- SVSARCCKBMZNMR-UHFFFAOYSA-N [1-[2-[methyl-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethyl]amino]ethyl]pyridin-4-ylidene]methyl-oxoazanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1CCN(C)CCN1C=CC(=C[NH+]=O)C=C1 SVSARCCKBMZNMR-UHFFFAOYSA-N 0.000 claims 12
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000005357 cycloalkylalkynyl group Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 6
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- -1 2-methyl-1-oxo-1,2-dihydroisoquinolin-4-yl Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 2
- BMVGRYYCVHUNTL-UHFFFAOYSA-N 4-(2-cyclopropyl-5-methylsulfonyl-1-benzofuran-7-yl)-2-methylisoquinolin-1-one Chemical compound CN1C=C(C2=C3OC(=CC3=CC(=C2)S(C)(=O)=O)C2CC2)C2=C(C=CC=C2)C1=O BMVGRYYCVHUNTL-UHFFFAOYSA-N 0.000 claims 2
- MJESFBWLZNLWBH-UHFFFAOYSA-N 4-(2-ethyl-5-methylsulfonyl-1-benzofuran-7-yl)-2-methylisoquinolin-1-one Chemical compound CCc1cc2cc(cc(-c3cn(C)c(=O)c4ccccc34)c2o1)S(C)(=O)=O MJESFBWLZNLWBH-UHFFFAOYSA-N 0.000 claims 2
- 102000008157 Histone Demethylases Human genes 0.000 claims 2
- 108010074870 Histone Demethylases Proteins 0.000 claims 2
- IPDVTHZWXBGFMH-UHFFFAOYSA-N N-[6-(1,5-dimethyl-6-oxopyridin-3-yl)-2-methyl-1-(1-phenylethyl)benzimidazol-4-yl]methanesulfonamide Chemical compound CN1C=C(C=C(C1=O)C)C=1C=C(C2=C(N(C(=N2)C)C(C)C2=CC=CC=C2)C=1)NS(=O)(=O)C IPDVTHZWXBGFMH-UHFFFAOYSA-N 0.000 claims 2
- 125000005133 alkynyloxy group Chemical group 0.000 claims 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- ZCRZCMUDOWDGOB-UHFFFAOYSA-N ethanesulfonimidic acid Chemical compound CCS(N)(=O)=O ZCRZCMUDOWDGOB-UHFFFAOYSA-N 0.000 claims 2
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 2
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000001613 neoplastic effect Effects 0.000 claims 2
- NUFBGWIIBRJOFR-UHFFFAOYSA-N 2-methyl-4-(2-oxo-1,3-dihydroindol-6-yl)isoquinolin-1-one Chemical compound Cn1cc(-c2ccc3CC(=O)Nc3c2)c2ccccc2c1=O NUFBGWIIBRJOFR-UHFFFAOYSA-N 0.000 claims 1
- ADKKKJSPASMXOK-UHFFFAOYSA-N 2-methyl-4-(5-methylsulfonyl-2-phenyl-1-benzofuran-7-yl)isoquinolin-1-one Chemical compound CN1C(C2=CC=CC=C2C(=C1)C1=CC(=CC=2C=C(OC=21)C1=CC=CC=C1)S(=O)(=O)C)=O ADKKKJSPASMXOK-UHFFFAOYSA-N 0.000 claims 1
- MLGFKZXLNZKATJ-UHFFFAOYSA-N 4-(1'-cyclobutylspiro[4h-1,3-benzodioxine-2,4'-piperidine]-6-yl)-2-methylisoquinolin-1-one Chemical group C12=CC=CC=C2C(=O)N(C)C=C1C(C=C1CO2)=CC=C1OC2(CC1)CCN1C1CCC1 MLGFKZXLNZKATJ-UHFFFAOYSA-N 0.000 claims 1
- DOBRAOBQHDICGW-UHFFFAOYSA-N 4-(2-ethyl-5-methylsulfonyl-1-benzofuran-7-yl)-2-methyl-1H-isoquinoline Chemical compound CCc1cc2cc(cc(C3=CN(C)Cc4ccccc34)c2o1)S(C)(=O)=O DOBRAOBQHDICGW-UHFFFAOYSA-N 0.000 claims 1
- AVRQZBKJBDYYDC-UHFFFAOYSA-N 4-(3,4-dihydro-2H-1,4-benzoxazin-6-yl)-2-methylisoquinolin-1-one Chemical compound Cn1cc(-c2ccc3OCCNc3c2)c2ccccc2c1=O AVRQZBKJBDYYDC-UHFFFAOYSA-N 0.000 claims 1
- BJRHTEAWPQRZIN-UHFFFAOYSA-N 4-[5-(cyclopropylmethoxy)-1-ethylsulfonyl-2,3-dihydroindol-6-yl]-2-methylisoquinolin-1-one Chemical compound C1(CC1)COC=1C=C2CCN(C2=CC=1C1=CN(C(C2=CC=CC=C12)=O)C)S(=O)(=O)CC BJRHTEAWPQRZIN-UHFFFAOYSA-N 0.000 claims 1
- DQJOEVBOJLGCJO-UHFFFAOYSA-N 4-[5-(cyclopropylmethoxy)-1-methylsulfonyl-2,3-dihydroindol-6-yl]-2-methylisoquinolin-1-one Chemical compound C1(CC1)COC=1C=C2CCN(C2=CC=1C1=CN(C(C2=CC=CC=C12)=O)C)S(=O)(=O)C DQJOEVBOJLGCJO-UHFFFAOYSA-N 0.000 claims 1
- QLSPIGUYWQJFOU-UHFFFAOYSA-N 4-[5-(cyclopropylmethoxy)-2-ethyl-1,1-dioxo-3H-1,2-benzothiazol-6-yl]-2-methylisoquinolin-1-one Chemical compound C1(CC1)COC=1C(=CC2=C(CN(S2(=O)=O)CC)C=1)C1=CN(C(C2=CC=CC=C12)=O)C QLSPIGUYWQJFOU-UHFFFAOYSA-N 0.000 claims 1
- MSZYABAQZIIOQC-UHFFFAOYSA-N 4-[6-(cyclopropylmethoxy)-1-methyl-3-methylsulfonylindazol-5-yl]-2-methylisoquinolin-1-one Chemical compound C1(CC1)COC1=C(C=C2C(=NN(C2=C1)C)S(=O)(=O)C)C1=CN(C(C2=CC=CC=C12)=O)C MSZYABAQZIIOQC-UHFFFAOYSA-N 0.000 claims 1
- AWTVHDWTTKQFKP-UHFFFAOYSA-N 4-[6-(cyclopropylmethoxy)-3-ethylsulfonyl-1-methylindazol-5-yl]-2-methylisoquinolin-1-one Chemical compound C1(CC1)COC1=C(C=C2C(=NN(C2=C1)C)S(=O)(=O)CC)C1=CN(C(C2=CC=CC=C12)=O)C AWTVHDWTTKQFKP-UHFFFAOYSA-N 0.000 claims 1
- PVWHOYFZJDGCRS-UHFFFAOYSA-N 4-[7-(cyclopropylmethoxy)-4-ethylsulfonyl-2,3-dihydro-1,4-benzoxazin-6-yl]-2-methylisoquinolin-1-one Chemical compound C1(CC1)COC1=CC2=C(N(CCO2)S(=O)(=O)CC)C=C1C1=CN(C(C2=CC=CC=C12)=O)C PVWHOYFZJDGCRS-UHFFFAOYSA-N 0.000 claims 1
- QRCGFTXRXYMJOS-UHFFFAOYSA-N 4h-1,4-benzoxazin-3-one Chemical compound C1=CC=C2NC(=O)COC2=C1 QRCGFTXRXYMJOS-UHFFFAOYSA-N 0.000 claims 1
- ZKFVJZHIQVBDKB-UHFFFAOYSA-N N-[1-(cyclopropylmethyl)-6-(1,5-dimethyl-6-oxopyridin-3-yl)-2-(trifluoromethyl)benzimidazol-4-yl]methanesulfonamide Chemical compound CN1C=C(C=C(C)C1=O)C1=CC(NS(C)(=O)=O)=C2N=C(N(CC3CC3)C2=C1)C(F)(F)F ZKFVJZHIQVBDKB-UHFFFAOYSA-N 0.000 claims 1
- AVKXANCJOSSNOQ-UHFFFAOYSA-N N-[1-(cyclopropylmethyl)-6-(1,5-dimethyl-6-oxopyridin-3-yl)-2-ethoxybenzimidazol-4-yl]methanesulfonamide Chemical compound CCOC1=NC2=C(NS(C)(=O)=O)C=C(C=C2N1CC1CC1)C1=CN(C)C(=O)C(C)=C1 AVKXANCJOSSNOQ-UHFFFAOYSA-N 0.000 claims 1
- PYHQYFBCYJDDIJ-UHFFFAOYSA-N N-[1-(cyclopropylmethyl)-6-(1,5-dimethyl-6-oxopyridin-3-yl)-2-methoxybenzimidazol-4-yl]methanesulfonamide Chemical compound COC1=NC2=C(NS(C)(=O)=O)C=C(C=C2N1CC1CC1)C1=CN(C)C(=O)C(C)=C1 PYHQYFBCYJDDIJ-UHFFFAOYSA-N 0.000 claims 1
- XTWBBCAPENQMBM-UHFFFAOYSA-N N-[1-[(2,4-difluorophenyl)methyl]-6-(1,5-dimethyl-6-oxopyridin-3-yl)benzimidazol-4-yl]ethanesulfonamide Chemical compound CCS(=O)(=O)NC1=C2N=CN(CC3=C(F)C=C(F)C=C3)C2=CC(=C1)C1=CN(C)C(=O)C(C)=C1 XTWBBCAPENQMBM-UHFFFAOYSA-N 0.000 claims 1
- GTJDSWUDLHLJSK-UHFFFAOYSA-N N-[1-benzyl-6-(1,5-dimethyl-6-oxopyridin-3-yl)-2,3-dihydroindol-4-yl]methanesulfonamide Chemical compound CN1C=C(C=C(C)C1=O)C1=CC(NS(C)(=O)=O)=C2CCN(CC3=CC=CC=C3)C2=C1 GTJDSWUDLHLJSK-UHFFFAOYSA-N 0.000 claims 1
- VANPZPLAKIRQEF-UHFFFAOYSA-N N-[1-benzyl-6-(1,5-dimethyl-6-oxopyridin-3-yl)benzimidazol-4-yl]methanesulfonamide Chemical compound CN1C=C(C=C(C)C1=O)C1=CC(NS(C)(=O)=O)=C2N=CN(CC3=CC=CC=C3)C2=C1 VANPZPLAKIRQEF-UHFFFAOYSA-N 0.000 claims 1
- UOIQOJYGIIEQTJ-UHFFFAOYSA-N N-[1-benzyl-6-(1,5-dimethyl-6-oxopyridin-3-yl)benzotriazol-4-yl]ethanesulfonamide N-[6-(1,5-dimethyl-6-oxopyridin-3-yl)-1-[(4-fluorophenyl)methyl]benzotriazol-4-yl]ethanesulfonamide Chemical compound CCS(=O)(=O)Nc1cc(cc2n(Cc3ccccc3)nnc12)-c1cc(C)c(=O)n(C)c1.CCS(=O)(=O)Nc1cc(cc2n(Cc3ccc(F)cc3)nnc12)-c1cc(C)c(=O)n(C)c1 UOIQOJYGIIEQTJ-UHFFFAOYSA-N 0.000 claims 1
- GTCDPVRVAVIHAL-UHFFFAOYSA-N N-[1-benzyl-6-(1,5-dimethyl-6-oxopyridin-3-yl)indazol-4-yl]ethanesulfonamide Chemical compound CCS(=O)(=O)NC1=C2C=NN(CC3=CC=CC=C3)C2=CC(=C1)C1=CN(C)C(=O)C(C)=C1 GTCDPVRVAVIHAL-UHFFFAOYSA-N 0.000 claims 1
- BYLPHHUERWNQGX-UHFFFAOYSA-N N-[1-benzyl-6-(1,5-dimethyl-6-oxopyridin-3-yl)indol-4-yl]methanesulfonamide Chemical compound CN1C=C(C=C(C)C1=O)C1=CC(NS(C)(=O)=O)=C2C=CN(CC3=CC=CC=C3)C2=C1 BYLPHHUERWNQGX-UHFFFAOYSA-N 0.000 claims 1
- PGDPQXDDOAIUHI-UHFFFAOYSA-N N-[1-benzyl-6-(2-methyl-1-oxoisoquinolin-4-yl)-2,3-dihydroindol-4-yl]methanesulfonamide Chemical compound C(C1=CC=CC=C1)N1CCC2=C(C=C(C=C12)C1=CN(C(C2=CC=CC=C12)=O)C)NS(=O)(=O)C PGDPQXDDOAIUHI-UHFFFAOYSA-N 0.000 claims 1
- BEARFMQOFNAZGQ-UHFFFAOYSA-N N-[1-benzyl-6-(2-methyl-1-oxoisoquinolin-4-yl)indol-4-yl]methanesulfonamide Chemical compound CN1C=C(C2=CC(NS(C)(=O)=O)=C3C=CN(CC4=CC=CC=C4)C3=C2)C2=C(C=CC=C2)C1=O BEARFMQOFNAZGQ-UHFFFAOYSA-N 0.000 claims 1
- LHEMTKPEUZEKNE-UHFFFAOYSA-N N-[2-cyclopropyl-7-(1,5-dimethyl-6-oxopyridin-3-yl)-1-benzofuran-5-yl]methanesulfonamide Chemical compound C1(CC1)C=1OC2=C(C=1)C=C(C=C2C1=CN(C(C(=C1)C)=O)C)NS(=O)(=O)C LHEMTKPEUZEKNE-UHFFFAOYSA-N 0.000 claims 1
- QOFZCQYGEZDEJL-UHFFFAOYSA-N N-[2-cyclopropyl-7-(2-methyl-1-oxoisoquinolin-4-yl)-1,3-benzoxazol-5-yl]ethanesulfonamide Chemical compound CCS(=O)(=O)NC1=CC2=C(OC(=N2)C2CC2)C(=C1)C1=CN(C)C(=O)C2=C1C=CC=C2 QOFZCQYGEZDEJL-UHFFFAOYSA-N 0.000 claims 1
- MGBSZFGNAZOLFQ-UHFFFAOYSA-N N-[2-cyclopropyl-7-(2-methyl-1-oxoisoquinolin-4-yl)-1-benzofuran-5-yl]ethanesulfonamide Chemical compound C1(CC1)C=1OC2=C(C=1)C=C(C=C2C1=CN(C(C2=CC=CC=C12)=O)C)NS(=O)(=O)CC MGBSZFGNAZOLFQ-UHFFFAOYSA-N 0.000 claims 1
- HCJSMLKOUNMWAY-UHFFFAOYSA-N N-[2-cyclopropyl-7-(2-methyl-1-oxoisoquinolin-4-yl)-1-benzofuran-5-yl]methanesulfonamide Chemical compound C1(CC1)C=1OC2=C(C=1)C=C(C=C2C1=CN(C(C2=CC=CC=C12)=O)C)NS(=O)(=O)C HCJSMLKOUNMWAY-UHFFFAOYSA-N 0.000 claims 1
- HVDXROCUEUZELK-UHFFFAOYSA-N N-[6-(1,5-dimethyl-6-oxopyridin-3-yl)-1-[(3-fluorophenyl)methyl]benzimidazol-4-yl]ethanesulfonamide Chemical compound CN1C=C(C=C(C1=O)C)C=1C=C(C2=C(N(C=N2)CC2=CC(=CC=C2)F)C=1)NS(=O)(=O)CC HVDXROCUEUZELK-UHFFFAOYSA-N 0.000 claims 1
- MJDHWWHBNNBJJP-UHFFFAOYSA-N N-[6-(1,5-dimethyl-6-oxopyridin-3-yl)-1-[(3-fluorophenyl)methyl]benzimidazol-4-yl]methanesulfonamide Chemical compound CN1C=C(C=C(C1=O)C)C=1C=C(C2=C(N(C=N2)CC2=CC(=CC=C2)F)C=1)NS(=O)(=O)C MJDHWWHBNNBJJP-UHFFFAOYSA-N 0.000 claims 1
- UPRXDQXRQLZTBQ-UHFFFAOYSA-N N-[6-(1,5-dimethyl-6-oxopyridin-3-yl)-1-[(4-fluorophenyl)methyl]indazol-4-yl]ethanesulfonamide Chemical compound CN1C=C(C=C(C1=O)C)C1=CC(=C2C=NN(C2=C1)CC1=CC=C(C=C1)F)NS(=O)(=O)CC UPRXDQXRQLZTBQ-UHFFFAOYSA-N 0.000 claims 1
- YBIFRFJARITXLY-UHFFFAOYSA-N N-[7-(2-methyl-1-oxoisoquinolin-4-yl)-2-phenyl-1-benzofuran-5-yl]methanesulfonamide Chemical compound CN1C(C2=CC=CC=C2C(=C1)C1=CC(=CC=2C=C(OC=21)C1=CC=CC=C1)NS(=O)(=O)C)=O YBIFRFJARITXLY-UHFFFAOYSA-N 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 230000001973 epigenetic effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- ONDPHDOFVYQSGI-UHFFFAOYSA-N zinc nitrate Chemical group [Zn+2].[O-][N+]([O-])=O.[O-][N+]([O-])=O ONDPHDOFVYQSGI-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562148098P | 2015-04-15 | 2015-04-15 | |
| US62/148,098 | 2015-04-15 | ||
| PCT/US2016/027874 WO2016168682A2 (en) | 2015-04-15 | 2016-04-15 | Bromodomain inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018511626A JP2018511626A (ja) | 2018-04-26 |
| JP2018511626A5 true JP2018511626A5 (enExample) | 2019-05-23 |
| JP6856543B2 JP6856543B2 (ja) | 2021-04-07 |
Family
ID=57126317
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017553414A Active JP6856543B2 (ja) | 2015-04-15 | 2016-04-15 | ブロモドメイン阻害剤 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US9908885B2 (enExample) |
| EP (2) | EP3831383A1 (enExample) |
| JP (1) | JP6856543B2 (enExample) |
| KR (1) | KR20170135938A (enExample) |
| CN (1) | CN107635558A (enExample) |
| AR (1) | AR104259A1 (enExample) |
| AU (1) | AU2016249273B2 (enExample) |
| CA (1) | CA2982588A1 (enExample) |
| CL (1) | CL2017002606A1 (enExample) |
| CO (1) | CO2017011484A2 (enExample) |
| EA (1) | EA201792229A1 (enExample) |
| EC (1) | ECSP17070706A (enExample) |
| ES (1) | ES2868355T3 (enExample) |
| HK (1) | HK1243326A1 (enExample) |
| IL (1) | IL255006A0 (enExample) |
| MX (1) | MX2017013207A (enExample) |
| PE (1) | PE20180258A1 (enExample) |
| PH (1) | PH12017501888A1 (enExample) |
| SG (1) | SG11201708470SA (enExample) |
| TW (1) | TW201643153A (enExample) |
| WO (1) | WO2016168682A2 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR104259A1 (es) * | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| WO2017024406A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| EP3334717B1 (en) | 2015-08-11 | 2020-07-01 | Neomed Institute | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
| WO2017024412A1 (en) | 2015-08-12 | 2017-02-16 | Neomed Institute | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
| US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
| WO2017127930A1 (en) | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| CN108314680A (zh) * | 2017-01-16 | 2018-07-24 | 凯惠科技发展(上海)有限公司 | 一种含芳环化合物、其制备方法、药物组合物及应用 |
| US10617680B2 (en) * | 2017-04-18 | 2020-04-14 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| CN107098844B (zh) * | 2017-05-17 | 2019-07-30 | 许昌学院 | 一种c-5位硝基取代的酰基吲哚啉类化合物的合成方法 |
| IL275478B2 (en) * | 2017-12-20 | 2024-06-01 | Betta Pharmaceuticals Co Ltd | A preparation that functions as a bromodomain protein inhibitor, and the composition |
| CN112236172A (zh) | 2018-01-30 | 2021-01-15 | 福宏治疗公司 | 用于治疗病症的方法和化合物 |
| CN108516973A (zh) * | 2018-03-30 | 2018-09-11 | 广西师范大学 | 3-苯并噻唑-1-(3-二甲氨基)丙基喹啉-4-酮衍生物及其制备方法和应用 |
| JP7434274B2 (ja) * | 2018-07-23 | 2024-02-20 | セルジーン・クオンティセル・リサーチ・インコーポレイテッド | ブロモドメイン阻害剤の合成方法 |
| CN120365272A (zh) | 2018-10-05 | 2025-07-25 | 安娜普尔纳生物股份有限公司 | 用于治疗与apj受体活性有关的疾病的化合物和组合物 |
| WO2020092638A1 (en) | 2018-10-30 | 2020-05-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| EP3917517A4 (en) | 2019-01-29 | 2023-01-25 | Foghorn Therapeutics Inc. | CONNECTIONS AND USES THEREOF |
| US12384776B2 (en) | 2019-01-29 | 2025-08-12 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| EP3917526A4 (en) | 2019-01-29 | 2022-11-02 | Foghorn Therapeutics Inc. | COMPOUNDS AND THEIR USES |
| EP3917934A4 (en) * | 2019-01-29 | 2023-02-15 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| JP2022053557A (ja) * | 2019-02-08 | 2022-04-06 | マルホ株式会社 | ピリドン誘導体 |
| EP3958867B1 (en) * | 2019-04-24 | 2024-06-26 | Convergene Llc | Small molecule bromodomain inhibitors and uses thereof |
| CN112174945B (zh) * | 2019-07-02 | 2022-06-07 | 四川大学 | 具有抗癌作用的吲唑类化合物及其制备方法和用途 |
| CA3145827A1 (en) | 2019-07-02 | 2021-01-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| US20220289711A1 (en) * | 2019-07-31 | 2022-09-15 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2021155225A1 (en) | 2020-01-29 | 2021-08-05 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
| CN116322780A (zh) * | 2020-07-29 | 2023-06-23 | 福宏治疗公司 | 化合物及其用途 |
| WO2023283263A1 (en) | 2021-07-06 | 2023-01-12 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
| CN114014842B (zh) * | 2021-11-04 | 2024-03-01 | 中国药科大学 | 一种杂环酮类化合物与其组合物及其制备方法和应用 |
| WO2023090859A1 (ko) * | 2021-11-17 | 2023-05-25 | 일동제약(주) | 아이속사졸 유도체의 제조 방법 및 그의 신규한 중간체 |
| GB202213163D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1349418A (en) * | 1919-08-05 | 1920-08-10 | George F Flynn | Motor-support |
| US3590036A (en) * | 1968-11-18 | 1971-06-29 | George Y Lesher | Naphthyridine-3-carboxylic acids,their derivatives and preparation thereof |
| DE2011970A1 (en) | 1970-03-13 | 1971-11-18 | CH. Boehringer Sohn, 6507 Ingelheim | Imidazo-(1, 2-a)- pyrimidines prepn |
| US3635667A (en) | 1970-07-23 | 1972-01-18 | Fmc Corp | Drycleaning with hydrogen peroxide |
| GB1322318A (en) * | 1971-05-19 | 1973-07-04 | Sterling Drug Inc | 1-alkyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids and esters |
| BE786028A (fr) | 1971-07-08 | 1973-01-08 | Boehringer Sohn Ingelheim | 2,3-dihydro-oxo-imidazo(1,2-a)-pyrimidines, leurs sels d'addition avec des acides et procedes pour les fabriquer |
| DE2356005A1 (de) | 1973-11-09 | 1975-05-22 | Boehringer Sohn Ingelheim | Neue 7-amino-imidazo eckige klammer auf 1,2-a eckige klammer zu pyrimidine, diese enthaltende arzneimittel sowie verfahren zu deren herstellung |
| AU577105B2 (en) | 1985-04-02 | 1988-09-15 | T.P.O. :Pharmachim: | Acylaminic penicillin derivatives |
| US6117940A (en) | 1997-10-17 | 2000-09-12 | Mjalli; Adnan M. M. | Amino-ketone solid support templates |
| CN1245386C (zh) * | 2000-06-12 | 2006-03-15 | 卫材株式会社 | 1,2-二氢吡啶化合物及其制备方法和用途 |
| GB0129260D0 (en) * | 2001-12-06 | 2002-01-23 | Eisai London Res Lab Ltd | Pharmaceutical compositions and their uses |
| DE60319254T2 (de) | 2002-09-26 | 2009-02-12 | Pfizer Inc. | Pyrazolamide zur behandlung von hiv-infektionen |
| JP2005089352A (ja) | 2003-09-16 | 2005-04-07 | Kissei Pharmaceut Co Ltd | 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途 |
| AU2004276236B2 (en) | 2003-09-23 | 2008-01-24 | Merck Sharp & Dohme Corp. | Isoquinolinone potassium channel inhibitors |
| US7763614B2 (en) * | 2003-09-23 | 2010-07-27 | Merck Sharp & Dohme Corp. | Isoquinoline potassium channel inhibitors |
| KR100703068B1 (ko) | 2003-12-30 | 2007-04-05 | 에스케이케미칼주식회사 | 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물 |
| TW200536830A (en) * | 2004-02-06 | 2005-11-16 | Chugai Pharmaceutical Co Ltd | 1-(2H)-isoquinolone derivative |
| KR20070008674A (ko) | 2004-04-01 | 2007-01-17 | 아스테라스 세이야쿠 가부시키가이샤 | 피라진 유도체, 및 아데노신 길항제로서의 이의 약학적용도 |
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| KR100781704B1 (ko) | 2005-04-20 | 2007-12-03 | 에스케이케미칼주식회사 | 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물 |
| US7452892B2 (en) | 2005-06-17 | 2008-11-18 | Bristol-Myers Squibb Company | Triazolopyrimidine cannabinoid receptor 1 antagonists |
| ES2372067T3 (es) | 2005-07-26 | 2012-01-13 | Sanofi | Derivados de ciclohexilamina isoquinolona como inhibidores de la rho-quinasa. |
| NZ565668A (en) | 2005-07-26 | 2010-09-30 | Sanofi Aventis | Piperidinyl-substituted isoquinolone derivatives as RHO-kinase inhibitors |
| US20070099911A1 (en) | 2005-10-28 | 2007-05-03 | Wyeth | Pyrroloquinolinone derivatives as 5-hydroxytryptamine-6 ligands |
| KR20080109841A (ko) | 2006-03-10 | 2008-12-17 | 뉴로젠 코포레이션 | 피페라지닐 옥소알킬 테트라히드로이소퀴놀린 및 관련유사체 |
| GB0612428D0 (en) | 2006-06-22 | 2006-08-02 | Prolysis Ltd | Antibacterial agents |
| HRP20100705T1 (hr) | 2006-12-27 | 2011-01-31 | Sanofi-Aventis | Cikloalkilaminski supstituirani izokinolinski i izokinolinonski derivati |
| KR101517154B1 (ko) | 2006-12-27 | 2015-04-30 | 사노피 | Rho-키나제의 억제제로서의 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| CN101595094B (zh) | 2006-12-27 | 2013-02-20 | 塞诺菲-安万特股份有限公司 | 环烷基胺取代的异喹诺酮衍生物 |
| WO2009029214A1 (en) * | 2007-08-23 | 2009-03-05 | Amgen Inc. | Isoquinolone derivatives as phosphodiesterase 10 inhibitors |
| ES2390004T3 (es) | 2008-01-30 | 2012-11-05 | Cephalon, Inc. | Derivados sustituidos de piperidina espirocíclica como ligandos del receptor de la histamina 3(H3) |
| ES2389478T3 (es) | 2008-06-25 | 2012-10-26 | Bristol-Myers Squibb Company | Derivados de dicetopiperidina como inhibidores de la fijación del VIH |
| WO2010039186A2 (en) * | 2008-09-23 | 2010-04-08 | Renovis, Inc. | Compounds useful as faah modulators and uses thereof |
| EP2196465A1 (en) | 2008-12-15 | 2010-06-16 | Almirall, S.A. | (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors |
| WO2010071819A1 (en) * | 2008-12-19 | 2010-06-24 | Schering Corporation | Bicyclic heterocyclic derivatives and methods of use thereof |
| RU2017109664A (ru) | 2009-10-06 | 2019-01-23 | Милленниум Фармасьютикалз, Инк. | Гетероциклические соединения, используемые в качестве ингибиторов pdk1 |
| KR20120123325A (ko) | 2009-12-15 | 2012-11-08 | 시오노기세야쿠 가부시키가이샤 | 혈관 내피 리파아제 저해 활성을 갖는 옥사디아졸 유도체 |
| PE20130376A1 (es) | 2010-06-28 | 2013-03-30 | Merck Patent Gmbh | [1,8]naftiridinas sustituidas por 2,4-diarilo como inhibidores de quinasas para uso contra el cancer |
| WO2012086735A1 (ja) * | 2010-12-22 | 2012-06-28 | 大正製薬株式会社 | 縮合複素環化合物 |
| AU2012258977A1 (en) | 2011-05-23 | 2014-01-16 | Imago Pharmaceuticals, Inc. | Inhibitors of LRRK2 kinase activity |
| RU2477723C2 (ru) * | 2011-06-16 | 2013-03-20 | Общество С Ограниченной Ответственностью "Фьюжн Фарма" | Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе |
| CN102827073A (zh) | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| JP6014155B2 (ja) | 2011-10-31 | 2016-10-25 | ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. | ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用 |
| CN103183675A (zh) | 2011-12-27 | 2013-07-03 | 山东轩竹医药科技有限公司 | 磷酸二酯酶-4抑制剂 |
| US9434743B2 (en) * | 2012-03-02 | 2016-09-06 | Takeda Pharmaceutical Company Limited | Indazole derivatives |
| CN104428293B (zh) * | 2012-06-11 | 2018-06-08 | Ucb生物制药私人有限公司 | 调节TNFα的苯并咪唑类 |
| JP2014024838A (ja) * | 2012-06-21 | 2014-02-06 | Taisho Pharmaceutical Co Ltd | 縮合複素環化合物を有効成分として含有する血糖低下作用薬 |
| WO2014015088A1 (en) * | 2012-07-19 | 2014-01-23 | Bristol-Myers Squibb Company | Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase |
| WO2014080291A2 (en) * | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| WO2014109414A1 (ja) * | 2013-01-11 | 2014-07-17 | 富士フイルム株式会社 | 含窒素複素環化合物またはその塩 |
| CN105377851B (zh) * | 2013-03-11 | 2018-07-20 | 密执安州立大学董事会 | Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法 |
| RU2680100C9 (ru) * | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
| MX2015016344A (es) * | 2013-05-27 | 2016-03-01 | Novartis Ag | Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades. |
| ES2661437T3 (es) * | 2013-06-21 | 2018-04-02 | Zenith Epigenetics Corp. | Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio |
| WO2014205594A1 (en) * | 2013-06-24 | 2014-12-31 | Merck Sharp & Dohme Corp. | Substituted benzofuran compounds and methods of use thereof for treatment of viral diseases |
| NZ754039A (en) * | 2013-06-26 | 2021-06-25 | Abbvie Inc | Primary carboxamides as btk inhibitors |
| PE20161065A1 (es) * | 2013-10-18 | 2016-11-19 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| WO2015081189A1 (en) * | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| JP6469692B2 (ja) * | 2013-12-09 | 2019-02-13 | ユーシービー バイオファルマ エスピーアールエル | Tnf活性のモジュレーターとしてのイミダゾピリジン誘導体 |
| US10173991B2 (en) * | 2014-01-07 | 2019-01-08 | Bristol-Myers Squibb Company | Sulfone amide linked benzothiazole inhibitors of endothelial lipase |
| US9499551B2 (en) | 2014-01-24 | 2016-11-22 | Confluence Life Sciences, Inc. | Substituted pyrrolo[2,3-b]pyridines for treating cancer or inflammatory diseases |
| KR20240134245A (ko) * | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| MA40940A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| WO2016086200A1 (en) * | 2014-11-27 | 2016-06-02 | Genentech, Inc. | 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors |
| WO2016139361A1 (en) * | 2015-03-05 | 2016-09-09 | Boehringer Ingelheim International Gmbh | New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9 |
| AR104259A1 (es) * | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| TW201642860A (zh) * | 2015-04-22 | 2016-12-16 | 塞爾基因定量細胞研究公司 | 布羅莫結構域抑制劑 |
-
2016
- 2016-04-14 AR ARP160101014A patent/AR104259A1/es unknown
- 2016-04-15 TW TW105111879A patent/TW201643153A/zh unknown
- 2016-04-15 ES ES16780891T patent/ES2868355T3/es active Active
- 2016-04-15 EA EA201792229A patent/EA201792229A1/ru unknown
- 2016-04-15 CN CN201680034663.2A patent/CN107635558A/zh active Pending
- 2016-04-15 EP EP20215944.8A patent/EP3831383A1/en not_active Withdrawn
- 2016-04-15 AU AU2016249273A patent/AU2016249273B2/en not_active Ceased
- 2016-04-15 KR KR1020177032364A patent/KR20170135938A/ko not_active Withdrawn
- 2016-04-15 PE PE2017002197A patent/PE20180258A1/es not_active Application Discontinuation
- 2016-04-15 MX MX2017013207A patent/MX2017013207A/es unknown
- 2016-04-15 EP EP16780891.4A patent/EP3283077B1/en active Active
- 2016-04-15 JP JP2017553414A patent/JP6856543B2/ja active Active
- 2016-04-15 CA CA2982588A patent/CA2982588A1/en active Pending
- 2016-04-15 US US15/130,503 patent/US9908885B2/en active Active
- 2016-04-15 SG SG11201708470SA patent/SG11201708470SA/en unknown
- 2016-04-15 WO PCT/US2016/027874 patent/WO2016168682A2/en not_active Ceased
- 2016-04-15 HK HK18102785.5A patent/HK1243326A1/zh unknown
-
2017
- 2017-10-13 CL CL2017002606A patent/CL2017002606A1/es unknown
- 2017-10-15 IL IL255006A patent/IL255006A0/en unknown
- 2017-10-18 PH PH12017501888A patent/PH12017501888A1/en unknown
- 2017-10-24 EC ECIEPI201770706A patent/ECSP17070706A/es unknown
- 2017-11-08 CO CONC2017/0011484A patent/CO2017011484A2/es unknown
-
2018
- 2018-01-12 US US15/870,557 patent/US10494371B2/en active Active
-
2019
- 2019-11-04 US US16/673,839 patent/US10807982B2/en active Active