JP2015528821A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015528821A5 JP2015528821A5 JP2015525858A JP2015525858A JP2015528821A5 JP 2015528821 A5 JP2015528821 A5 JP 2015528821A5 JP 2015525858 A JP2015525858 A JP 2015525858A JP 2015525858 A JP2015525858 A JP 2015525858A JP 2015528821 A5 JP2015528821 A5 JP 2015528821A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- oxo
- methylamino
- aryl
- 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
- -1 C 1-6 - alkyl Chemical group 0.000 claims 102
- 125000003118 aryl group Chemical group 0.000 claims 55
- 229910052739 hydrogen Inorganic materials 0.000 claims 53
- 125000004093 cyano group Chemical group *C#N 0.000 claims 45
- 229910052799 carbon Inorganic materials 0.000 claims 31
- 125000001475 halogen functional group Chemical group 0.000 claims 28
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 28
- 125000005605 benzo group Chemical group 0.000 claims 21
- 229910005965 SO 2 Inorganic materials 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 20
- 125000002252 acyl group Chemical group 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 18
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 13
- 150000003857 carboxamides Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 8
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000004549 quinolin-4-yl group Chemical group N1=CC=C(C2=CC=CC=C12)* 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- VHWJSJBTUWUEAL-UHFFFAOYSA-N propanamide;hydrochloride Chemical compound Cl.CCC(N)=O VHWJSJBTUWUEAL-UHFFFAOYSA-N 0.000 claims 2
- LPYCHTYQOLSQKX-CRICUBBOSA-N (2r)-2-amino-n-[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-4-oxospiro[3h-1,5-benzoxazepine-2,4'-oxane]-3-yl]propanamide Chemical compound COC1=CC=C2C=C(Br)C=CC2=C1CN(C([C@H]1NC(=O)[C@@H](C)N)=O)C2=CC=CC=C2OC21CCOCC2 LPYCHTYQOLSQKX-CRICUBBOSA-N 0.000 claims 1
- KPKSKMHWRZUNQJ-AUALFVNHSA-N (2r)-n-[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-2,2-dimethyl-4-oxo-3h-1,5-benzothiazepin-3-yl]-2-(methylamino)propanamide;hydrochloride Chemical compound Cl.C12=CC=CC=C2SC(C)(C)[C@@H](NC(=O)[C@@H](C)NC)C(=O)N1CC1=C(OC)C=CC2=CC(Br)=CC=C12 KPKSKMHWRZUNQJ-AUALFVNHSA-N 0.000 claims 1
- PMTGJZLNFRQBBN-UWJYYQICSA-N (2s)-2-(methylamino)-n-[(3s)-5-[(2-methylnaphthalen-1-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]propanamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC=CC=C2N1CC1=C(C)C=CC2=CC=CC=C12 PMTGJZLNFRQBBN-UWJYYQICSA-N 0.000 claims 1
- JWDWSWYEQALIBS-LPVSMQOSSA-N (2s)-2-(methylamino)-n-[4-oxo-5-[(3-phenylphenyl)methyl]-2,3-dihydro-1,5-benzothiazepin-3-yl]propanamide;hydrochloride Chemical compound Cl.O=C1C(NC(=O)[C@H](C)NC)CSC2=CC=CC=C2N1CC(C=1)=CC=CC=1C1=CC=CC=C1 JWDWSWYEQALIBS-LPVSMQOSSA-N 0.000 claims 1
- AGIOLCPUBSPMLM-UWJYYQICSA-N (2s)-2-amino-n-[(3s)-5-[[1-(2-cyanophenyl)indazol-3-yl]methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]propanamide Chemical compound C([C@@H](C1=O)NC(=O)[C@@H](N)C)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=NN1C1=CC=CC=C1C#N AGIOLCPUBSPMLM-UWJYYQICSA-N 0.000 claims 1
- IDIOSLWBPCKHDR-HBYWCBEISA-N (2s)-n-(5-benzyl-1,1,4-trioxo-2,3-dihydro-1$l^{6},5-benzothiazepin-3-yl)-2-(methylamino)propanamide;hydrochloride Chemical class Cl.O=C1C(NC(=O)[C@H](C)NC)CS(=O)(=O)C2=CC=CC=C2N1CC1=CC=CC=C1 IDIOSLWBPCKHDR-HBYWCBEISA-N 0.000 claims 1
- XQHYGDOJDYACHI-HBYWCBEISA-N (2s)-n-(5-benzyl-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl)-2-(methylamino)propanamide;hydrochloride Chemical compound Cl.O=C1C(NC(=O)[C@H](C)NC)CSC2=CC=CC=C2N1CC1=CC=CC=C1 XQHYGDOJDYACHI-HBYWCBEISA-N 0.000 claims 1
- JVSKHEKKOOIUQG-UXCLVXGESA-N (2s)-n-[(2s,3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-2-methyl-4-oxo-7-(trifluoromethyl)-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O=C1[C@@H](NC(=O)[C@H](C)NC)[C@H](C)OC2=CC=C(C(F)(F)F)C=C2N1CC1=C(OC)C=CC2=CC(Br)=CC=C12 JVSKHEKKOOIUQG-UXCLVXGESA-N 0.000 claims 1
- ASSRMYVHRGCEJC-RIAYWLAYSA-N (2s)-n-[(3r)-9-[[2-(2-methoxyethoxy)acetyl]amino]-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl]-2-(methylamino)propanamide;hydrochloride Chemical compound Cl.O=C1[C@@H](NC(=O)[C@H](C)NC)CSC2=C(NC(=O)COCCOC)C=CC=C2N1CC1=CC=CC2=CC=CC=C12 ASSRMYVHRGCEJC-RIAYWLAYSA-N 0.000 claims 1
- RRRZHUQUSBVQNZ-QNNMEKCMSA-N (2s)-n-[(3r)-9-amino-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl]-2-(methylamino)propanamide;hydrochloride Chemical compound Cl.O=C1[C@@H](NC(=O)[C@H](C)NC)CSC2=C(N)C=CC=C2N1CC1=CC=CC2=CC=CC=C12 RRRZHUQUSBVQNZ-QNNMEKCMSA-N 0.000 claims 1
- IOHRCWWNKMUJHT-CVDCTZTESA-N (2s)-n-[(3s)-5-[(1-benzyl-2-chloroindol-3-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide Chemical compound C([C@@H](C1=O)NC(=O)[C@H](C)NC)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=C(Cl)N1CC1=CC=CC=C1 IOHRCWWNKMUJHT-CVDCTZTESA-N 0.000 claims 1
- FJKGNKQMJJKBRW-YJBOKZPZSA-N (2s)-n-[(3s)-5-[(1-ethyl-2-oxo-3h-indol-4-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide Chemical compound CCN1C(=O)CC2=C1C=CC=C2CN1C2=CC=CC=C2OC[C@H](NC(=O)[C@H](C)NC)C1=O FJKGNKQMJJKBRW-YJBOKZPZSA-N 0.000 claims 1
- NZGXRNHLIKDWHR-BBRMVZONSA-N (2s)-n-[(3s)-5-[(4-chlorophenyl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide Chemical compound C([C@@H](C1=O)NC(=O)[C@H](C)NC)OC2=CC=CC=C2N1CC1=CC=C(Cl)C=C1 NZGXRNHLIKDWHR-BBRMVZONSA-N 0.000 claims 1
- PYGNINGYNZYWBV-GUTACTQSSA-N (2s)-n-[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)butanamide;hydrochloride Chemical compound Cl.O=C1[C@@H](NC(=O)[C@@H](NC)CC)COC2=CC=CC=C2N1CC1=C(OC)C=CC2=CC(Br)=CC=C12 PYGNINGYNZYWBV-GUTACTQSSA-N 0.000 claims 1
- GGXKCOCFMZACLS-QNNMEKCMSA-N (2s)-n-[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC=CC=C2N1CC1=C(OC)C=CC2=CC(Br)=CC=C12 GGXKCOCFMZACLS-QNNMEKCMSA-N 0.000 claims 1
- UFSIJETWBAPLMM-UZTOHYMASA-N (2s)-n-[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-4-oxospiro[3h-1,5-benzoxazepine-2,4'-oxane]-3-yl]-2-(2-hydroxyethylamino)propanamide Chemical compound COC1=CC=C2C=C(Br)C=CC2=C1CN(C([C@H]1NC(=O)[C@H](C)NCCO)=O)C2=CC=CC=C2OC21CCOCC2 UFSIJETWBAPLMM-UZTOHYMASA-N 0.000 claims 1
- YTKHAOHVHVPIRV-DQFHVVJASA-N (2s)-n-[(3s)-5-[(6-cyclopropyl-2-methoxynaphthalen-1-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C([C@@H](C1=O)NC(=O)[C@H](C)NC)OC2=CC=CC=C2N1CC(C1=CC=2)=C(OC)C=CC1=CC=2C1CC1 YTKHAOHVHVPIRV-DQFHVVJASA-N 0.000 claims 1
- PMDXADUCFFKNBG-KSSFIOAISA-N (2s)-n-[(3s)-5-[(6-fluoro-1-methyl-2-oxoquinolin-4-yl)methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC=CC=C2N1CC1=CC(=O)N(C)C2=CC=C(F)C=C12 PMDXADUCFFKNBG-KSSFIOAISA-N 0.000 claims 1
- HCSLWAKAKAIBTE-ZOEDVAEJSA-N (2s)-n-[(3s)-5-[(7-bromo-3-methoxynaphthalen-2-yl)methyl]-8-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC(C)=CC=C2N1CC1=CC2=CC(Br)=CC=C2C=C1OC HCSLWAKAKAIBTE-ZOEDVAEJSA-N 0.000 claims 1
- MIJCTPVXXYDPMK-CVDCTZTESA-N (2s)-n-[(3s)-5-[[1-(2-cyanophenyl)indazol-3-yl]methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(2-hydroxyethylamino)propanamide Chemical compound C([C@@H](C1=O)NC(=O)[C@@H](NCCO)C)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=NN1C1=CC=CC=C1C#N MIJCTPVXXYDPMK-CVDCTZTESA-N 0.000 claims 1
- CHTDNPIBDHVSHN-RDPSFJRHSA-N (2s)-n-[(3s)-5-[[1-(2-cyanophenyl)indazol-3-yl]methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-[(2-hydroxy-2-methylpropyl)amino]propanamide Chemical compound C([C@@H](C1=O)NC(=O)[C@@H](NCC(C)(C)O)C)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=NN1C1=CC=CC=C1C#N CHTDNPIBDHVSHN-RDPSFJRHSA-N 0.000 claims 1
- NNTKWKIMKMYXDE-COBSGTNCSA-N (2s)-n-[(3s)-5-[[1-(benzenesulfonyl)-2-chloroindol-3-yl]methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide;hydrochloride Chemical compound Cl.C([C@@H](C1=O)NC(=O)[C@H](C)NC)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=C(Cl)N1S(=O)(=O)C1=CC=CC=C1 NNTKWKIMKMYXDE-COBSGTNCSA-N 0.000 claims 1
- IHVOEWKFQHMHHV-AVRDEDQJSA-N (2s)-n-[(3s)-5-[[2-chloro-1-(2-cyanophenyl)indol-3-yl]methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide Chemical compound C([C@@H](C1=O)NC(=O)[C@H](C)NC)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=C(Cl)N1C1=CC=CC=C1C#N IHVOEWKFQHMHHV-AVRDEDQJSA-N 0.000 claims 1
- HAYDMSLHIKTULD-ZWHLOQRUSA-N (2s)-n-[(3s)-5-[[2-cyano-1-(2-cyanophenyl)indol-3-yl]methyl]-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-2-(methylamino)propanamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C([C@@H](C1=O)NC(=O)[C@H](C)NC)OC2=CC=CC=C2N1CC(C1=CC=CC=C11)=C(C#N)N1C1=CC=CC=C1C#N HAYDMSLHIKTULD-ZWHLOQRUSA-N 0.000 claims 1
- CWXNEODDUDWHDU-WKRVVKTRSA-N (2s)-n-[(3s)-5-[[2-cyano-1-(2-cyanophenyl)indol-3-yl]methyl]-4-oxospiro[3h-1,5-benzoxazepine-2,4'-oxane]-3-yl]-2-(methylamino)propanamide Chemical compound O=C([C@H](C1(CCOCC1)OC1=CC=CC=C11)NC(=O)[C@H](C)NC)N1CC(C1=CC=CC=C11)=C(C#N)N1C1=CC=CC=C1C#N CWXNEODDUDWHDU-WKRVVKTRSA-N 0.000 claims 1
- LYSWNDFUEAGSOY-DCFHFQCYSA-N 1-acetyl-n-[(3r)-3-[[(2s)-2-(methylamino)propanoyl]amino]-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-9-yl]piperidine-4-carboxamide Chemical compound C([C@@H](C(N(CC=1C2=CC=CC=C2C=CC=1)C1=CC=C2)=O)NC(=O)[C@H](C)NC)SC1=C2NC(=O)C1CCN(C(C)=O)CC1 LYSWNDFUEAGSOY-DCFHFQCYSA-N 0.000 claims 1
- RCQFDAMHGMCSFG-UHFFFAOYSA-N 2-(4-methylindol-1-yl)benzonitrile Chemical compound C1=CC=2C(C)=CC=CC=2N1C1=CC=CC=C1C#N RCQFDAMHGMCSFG-UHFFFAOYSA-N 0.000 claims 1
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- GMEVWRNNKLKAQK-QDMMYLPHSA-N 3,4,5-trimethoxy-n-[(3r)-3-[[(2s)-2-(methylamino)propanoyl]amino]-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-9-yl]benzamide;hydrochloride Chemical compound Cl.C([C@@H](C(N(CC=1C2=CC=CC=C2C=CC=1)C1=CC=C2)=O)NC(=O)[C@H](C)NC)SC1=C2NC(=O)C1=CC(OC)=C(OC)C(OC)=C1 GMEVWRNNKLKAQK-QDMMYLPHSA-N 0.000 claims 1
- QXWFRZXIEMDIMN-AOMKIAJQSA-N 3-[[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-3-[[(2s)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzoxazepine-9-carbonyl]amino]propanoic acid Chemical compound COC=1C=CC2=CC(Br)=CC=C2C=1CN1C(=O)[C@@H](NC(=O)[C@H](C)NC)COC2=C1C=CC=C2C(=O)NCCC(O)=O QXWFRZXIEMDIMN-AOMKIAJQSA-N 0.000 claims 1
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 1
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 claims 1
- MDKSGCZZWJRJNU-JCNFZFLDSA-N 4-[[6-methoxy-7-[[(3s)-3-[[(2s)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzoxazepin-5-yl]methyl]naphthalene-2-carbonyl]amino]butanoic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC=CC=C2N1CC1=CC2=CC(C(=O)NCCCC(O)=O)=CC=C2C=C1OC MDKSGCZZWJRJNU-JCNFZFLDSA-N 0.000 claims 1
- AMMRZWVVBRQWKK-ZLLYMXMVSA-N 6-methoxy-n,n-dimethyl-7-[[(3s)-3-[[(2s)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzoxazepin-5-yl]methyl]naphthalene-2-carboxamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC=CC=C2N1CC1=CC2=CC(C(=O)N(C)C)=CC=C2C=C1OC AMMRZWVVBRQWKK-ZLLYMXMVSA-N 0.000 claims 1
- SZPWXAOBLNYOHY-UHFFFAOYSA-N [C]1=CC=NC2=CC=CC=C12 Chemical group [C]1=CC=NC2=CC=CC=C12 SZPWXAOBLNYOHY-UHFFFAOYSA-N 0.000 claims 1
- BMBANPOHPFKVTA-UHFFFAOYSA-N benzamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.NC(=O)C1=CC=CC=C1 BMBANPOHPFKVTA-UHFFFAOYSA-N 0.000 claims 1
- WAKRDDXHAXBEQA-UHFFFAOYSA-N benzoic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C1=CC=CC=C1 WAKRDDXHAXBEQA-UHFFFAOYSA-N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- BLONQRBSZCSXHN-MMTVBGGISA-N methyl 4-[[[(3s)-5-[(6-bromo-2-methoxynaphthalen-1-yl)methyl]-3-[[(2s)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzoxazepine-9-carbonyl]amino]methyl]benzoate Chemical compound C([C@@H](C(N1CC=2C3=CC=C(Br)C=C3C=CC=2OC)=O)NC(=O)[C@H](C)NC)OC2=C1C=CC=C2C(=O)NCC1=CC=C(C(=O)OC)C=C1 BLONQRBSZCSXHN-MMTVBGGISA-N 0.000 claims 1
- 125000006431 methyl cyclopropyl group Chemical group 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- RJYKNKRUSKXPQI-MBSDFSHPSA-N n-(2-hydroxyethyl)-6-methoxy-n-methyl-7-[[(3s)-3-[[(2s)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzoxazepin-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)COC2=CC=CC=C2N1CC1=CC2=CC(C(=O)N(C)CCO)=CC=C2C=C1OC RJYKNKRUSKXPQI-MBSDFSHPSA-N 0.000 claims 1
- MXKYZTHCPPPSKF-VMZNWUEUSA-N n-[(3r)-3-[[(2s)-2-(methylamino)propanoyl]amino]-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-9-yl]-5-oxohexanamide;hydrochloride Chemical compound Cl.O=C1[C@@H](NC(=O)[C@H](C)NC)CSC2=C(NC(=O)CCCC(C)=O)C=CC=C2N1CC1=CC=CC2=CC=CC=C12 MXKYZTHCPPPSKF-VMZNWUEUSA-N 0.000 claims 1
- GUJYJQYJOLDOHG-SCFGKSIXSA-N n-[(3r)-3-[[(2s)-2-(methylamino)propanoyl]amino]-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-9-yl]-6-oxoheptanamide;hydrochloride Chemical compound Cl.O=C1[C@@H](NC(=O)[C@H](C)NC)CSC2=C(NC(=O)CCCCC(C)=O)C=CC=C2N1CC1=CC=CC2=CC=CC=C12 GUJYJQYJOLDOHG-SCFGKSIXSA-N 0.000 claims 1
- NSIMSTVWDYAFBY-QDMMYLPHSA-N n-[(3r)-3-[[(2s)-2-(methylamino)propanoyl]amino]-5-(naphthalen-1-ylmethyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-9-yl]benzamide;hydrochloride Chemical compound Cl.C([C@@H](C(N(CC=1C2=CC=CC=C2C=CC=1)C1=CC=C2)=O)NC(=O)[C@H](C)NC)SC1=C2NC(=O)C1=CC=CC=C1 NSIMSTVWDYAFBY-QDMMYLPHSA-N 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261681337P | 2012-08-09 | 2012-08-09 | |
| US61/681,337 | 2012-08-09 | ||
| PCT/EP2013/066431 WO2014023708A1 (en) | 2012-08-09 | 2013-08-06 | Substituted hetero-azepinones |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015528821A JP2015528821A (ja) | 2015-10-01 |
| JP2015528821A5 true JP2015528821A5 (https=) | 2017-12-21 |
| JP6266617B2 JP6266617B2 (ja) | 2018-01-24 |
Family
ID=48951449
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015525858A Expired - Fee Related JP6266617B2 (ja) | 2012-08-09 | 2013-08-06 | 置換ヘテロアゼピノン |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9394263B2 (https=) |
| EP (1) | EP2882725A1 (https=) |
| JP (1) | JP6266617B2 (https=) |
| KR (1) | KR20150041647A (https=) |
| CN (1) | CN104470905B (https=) |
| BR (1) | BR112015001830A2 (https=) |
| CA (1) | CA2877048A1 (https=) |
| MX (1) | MX2015001720A (https=) |
| RU (1) | RU2015105561A (https=) |
| WO (1) | WO2014023708A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9422331B2 (en) * | 2012-09-19 | 2016-08-23 | Hoffmann-La Roche Inc. | 2-oxo-2,3,4,5-tetrahydro-1 H-benzo[B]diazepines and their use in the treatment of cancer |
| WO2016079527A1 (en) | 2014-11-19 | 2016-05-26 | Tetralogic Birinapant Uk Ltd | Combination therapy |
| WO2016097773A1 (en) | 2014-12-19 | 2016-06-23 | Children's Cancer Institute | Therapeutic iap antagonists for treating proliferative disorders |
| TWI763630B (zh) | 2015-07-02 | 2022-05-11 | 瑞士商赫孚孟拉羅股份公司 | 雙環內醯胺及其使用方法 |
| CN106467521A (zh) * | 2015-08-14 | 2017-03-01 | 陈志龙 | 一类双苯并咪唑吲哚衍生物的两种制备方法 |
| CN106467515B (zh) * | 2015-08-18 | 2019-09-24 | 宁波洞密生物科技有限公司 | 一类6-吡啶苯并咪唑吲哚衍生物及其制备方法与医药领域的应用 |
| MA44007A (fr) | 2016-02-05 | 2018-12-19 | Denali Therapeutics Inc | Inhibiteurs du récepteur interagissant avec protéine kinase 1 |
| EP3526219B1 (en) | 2016-10-17 | 2021-12-15 | F. Hoffmann-La Roche AG | Bicyclic pyridone lactams and methods of use thereof |
| HRP20220636T1 (hr) | 2016-12-09 | 2022-07-22 | Denali Therapeutics Inc. | Spojevi korisni kao inhibitori ripk1 |
| US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
| WO2019204537A1 (en) | 2018-04-20 | 2019-10-24 | Genentech, Inc. | N-[4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol e-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs) |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| WO2021020585A1 (ja) | 2019-07-31 | 2021-02-04 | ファイメクス株式会社 | 複素環化合物 |
| JP7326584B2 (ja) | 2020-12-17 | 2023-08-15 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 抗ｈｌａ－ｇ抗体及びその使用 |
| JP7821808B2 (ja) * | 2021-02-12 | 2026-02-27 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | がんの治療のための二環式テトラヒドロアゼピン誘導体 |
| CN117980294A (zh) * | 2021-09-01 | 2024-05-03 | 海南先声再明医药股份有限公司 | 泛素特异性蛋白酶1（usp1）抑制剂 |
| IL314082A (en) | 2022-01-12 | 2024-09-01 | Denali Therapeutics Inc | Crystal forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazapin-3-yl)- H4- 1,2,4-triazole-3-carboxamide |
| US20250092029A1 (en) * | 2022-02-07 | 2025-03-20 | The Wistar Institute Of Anatomy And Biology | Novel and highly selective sars-cov-2 mpro inhibitors |
| CR20250043A (es) * | 2022-08-11 | 2025-03-25 | Hoffmann La Roche | Derivados bicíclicos de tetrahidrotiazepina |
| TW202417001A (zh) * | 2022-08-11 | 2024-05-01 | 瑞士商赫孚孟拉羅股份公司 | 雙環四氫吖呯衍生物 |
| WO2024033388A1 (en) * | 2022-08-11 | 2024-02-15 | F. Hoffmann-La Roche Ag | Bicyclic tetrahydrothiazepine derivatives |
| WO2024033457A1 (en) * | 2022-08-11 | 2024-02-15 | F. Hoffmann-La Roche Ag | Bicyclic tetrahydrothiazepine derivatives |
| CN119930413B (zh) * | 2025-04-10 | 2025-07-22 | 山东辉璟生物医药科技有限公司 | 一种萘丁美酮-d3的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9420763D0 (en) | 1994-10-14 | 1994-11-30 | Glaxo Inc | Acetamide derivatives |
| TW200502221A (en) * | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
| EP1831187A1 (en) * | 2004-12-14 | 2007-09-12 | AstraZeneca AB | Novel molecular probes |
| JP2008545780A (ja) * | 2005-06-08 | 2008-12-18 | ノバルティス アクチエンゲゼルシャフト | 有機化合物 |
| WO2007101347A1 (en) * | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| CN101443014A (zh) * | 2006-03-10 | 2009-05-27 | 阿斯利康(瑞典)有限公司 | 化合物 |
| WO2008106077A1 (en) * | 2007-02-28 | 2008-09-04 | Merck & Co., Inc. | Substituted benzodiazepinones, benzoxazepinones and benzothiazepinones as sodium channel blockers |
-
2013
- 2013-08-06 WO PCT/EP2013/066431 patent/WO2014023708A1/en not_active Ceased
- 2013-08-06 RU RU2015105561A patent/RU2015105561A/ru not_active Application Discontinuation
- 2013-08-06 KR KR20157005929A patent/KR20150041647A/ko not_active Withdrawn
- 2013-08-06 CN CN201380035993.XA patent/CN104470905B/zh not_active Expired - Fee Related
- 2013-08-06 CA CA2877048A patent/CA2877048A1/en not_active Abandoned
- 2013-08-06 JP JP2015525858A patent/JP6266617B2/ja not_active Expired - Fee Related
- 2013-08-06 EP EP13747659.4A patent/EP2882725A1/en not_active Withdrawn
- 2013-08-06 MX MX2015001720A patent/MX2015001720A/es unknown
- 2013-08-06 US US14/418,383 patent/US9394263B2/en not_active Expired - Fee Related
- 2013-08-06 BR BR112015001830A patent/BR112015001830A2/pt not_active IP Right Cessation
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2015528821A5 (https=) | ||
| RU2015105561A (ru) | Замещенные гетероазепиноны | |
| ES2617619T3 (es) | Combinaciones de fármacos que comprenden un inhibidor de DGAT y un agonista de PPAR | |
| SI2840080T1 (en) | Nitrogen-containing heterocyclic compound or salt thereof | |
| AR045069A1 (es) | Derivados de pirazol-fenil urea como moduladores del receptor 5ht 2a de serotonina, utiles para la profilaxis y tratamiento de desordenes relacionados con el mismo | |
| HRP20110220T1 (hr) | Inhibitori kinaze | |
| JP2005518414A5 (https=) | ||
| SI2758388T1 (en) | New bicyclic derivatives of dihydroquinolin-2-one | |
| JP2008514643A5 (https=) | ||
| JP2011529037A5 (https=) | ||
| TW200745029A (en) | Sulfonamide derivatives exhibiting PGD2 receptor antagonism | |
| NZ573832A (en) | N-(4-{ 2-[4-aryl-piperazin-1-yl]ethyl} cyclohexyl)-acetamide derivatives for the treatment of neuropsychiatric disorders | |
| HRP20100607T1 (hr) | Spojevi piperidinilamino-tieno(2,3-d) pirimidina | |
| PE20050020A1 (es) | DERIVADOS 4-(2-OXO-2,3-DIHIDRO-1-H-IMIDAZO[4,5-b]PIRIDIN-1-IL)-N-(2-OXO-AZEPAN-3-IL)PIPERIDINIL-1-CARBOXAMIDA SUSTITUIDOS COMO ANTAGONISTAS DEL RECEPTOR CGRP | |
| JP2012502986A5 (https=) | ||
| JPWO2013105608A1 (ja) | Ｐ２ｘ４受容体拮抗剤 | |
| HRP20100477T1 (hr) | Kemijski spojevi | |
| HRP20080592T3 (en) | 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT-2a SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO | |
| PE20140934A1 (es) | Derivados de pirazol | |
| AR068115A1 (es) | Derivado del acido pirazolcarboxilico metodo de produccion del mismo y fungicida | |
| PE20081492A1 (es) | Derivados de sulfonamida heterociclicos como antagonista de edg-1 | |
| CY1111744T1 (el) | Τροποποιητες της δραστηριοτητας toy υποδοχεα χημειοκινων, κρυσταλλικες μορφες και διεργασια | |
| WO2008014381A3 (en) | Modulators of chemokine receptor activity, crystalline forms and process | |
| JP2012527487A5 (https=) | ||
| PE20061163A1 (es) | Compuestos de n-sulfonilaminofeniletil-2-fenoxiacetamida sustituidos |