JP2015528821A5 - - Google Patents
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- 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
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- -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
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| PCT/EP2013/066431 WO2014023708A1 (en) | 2012-08-09 | 2013-08-06 | Substituted hetero-azepinones |
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| JP2015528821A JP2015528821A (ja) | 2015-10-01 |
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| JP6302912B2 (ja) * | 2012-09-19 | 2018-03-28 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ２−オキソ−２，３，４，５−テトラヒドロ−１ｈ−ベンゾ［ｂ］ジアゼピン及びがんの治療におけるその使用 |
| 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 |
| CA3094197C (en) | 2015-07-02 | 2023-02-28 | F. Hoffmann-La Roche Ag | Bicyclic lactams and methods of use thereof |
| 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 |
| IL287136B2 (en) | 2016-02-05 | 2023-09-01 | Denali Therapeutics Inc | Receptor inhibitors - interacting with protein kinase 1 |
| JP7349359B2 (ja) | 2016-10-17 | 2023-09-22 | エフ． ホフマン－ラ ロシュ アーゲー | 二環式ピリドンラクタム及びその使用方法。 |
| HUE058802T2 (hu) | 2016-12-09 | 2022-09-28 | Denali Therapeutics Inc | RIPK1 inhibitorokként alkalmas vegyületek |
| US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
| CN112074519B (zh) | 2018-04-20 | 2024-08-02 | 豪夫迈·罗氏有限公司 | 作为rip1激酶抑制剂用于治疗例如肠易激综合征(ibs)的化合物 |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| JP7764027B2 (ja) | 2019-07-31 | 2025-11-05 | ファイメクス株式会社 | 複素環化合物 |
| EP4263609A1 (en) | 2020-12-17 | 2023-10-25 | F. Hoffmann-La Roche AG | Anti-hla-g antibodies and use thereof |
| PE20231505A1 (es) * | 2021-02-12 | 2023-09-26 | Hoffmann La Roche | Derivados de tetrahidroazepina biciclicos para el tratamiento del cancer |
| WO2023030295A1 (zh) * | 2021-09-01 | 2023-03-09 | 先声再明医药有限公司 | 泛素特异性蛋白酶1(usp1)抑制剂 |
| US11999750B2 (en) | 2022-01-12 | 2024-06-04 | Denali Therapeutics Inc. | Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido [3,2-B][1,4]oxazepin-3-yl)-4H-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 |
| JP2025526683A (ja) * | 2022-08-11 | 2025-08-15 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 二環式テトラヒドロチアゼピン誘導体 |
| CN119677732A (zh) * | 2022-08-11 | 2025-03-21 | 豪夫迈·罗氏有限公司 | 双环四氢氮杂䓬衍生物 |
| PE20251399A1 (es) * | 2022-08-11 | 2025-05-22 | Hoffmann La Roche | Derivados de tetrahidrotiazepina biciclicos |
| 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 |
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|---|---|---|---|---|
| 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 |
| CN101115730A (zh) * | 2004-12-14 | 2008-01-30 | 阿斯利康(瑞典)有限公司 | 新分子探针 |
| KR20080022092A (ko) | 2005-06-08 | 2008-03-10 | 노파르티스 아게 | 유기 화합물 |
| WO2007101347A1 (en) * | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| EP1996202A1 (en) * | 2006-03-10 | 2008-12-03 | AstraZeneca AB | Chemical compounds |
| JP2010520237A (ja) * | 2007-02-28 | 2010-06-10 | メルク・シャープ・エンド・ドーム・コーポレイション | ナトリウムチャネル遮断薬としての置換ベンゾジアゼピノン、ベンゾオキサアゼピノン及びベンゾチアゼピノン |
-
2013
- 2013-08-06 US US14/418,383 patent/US9394263B2/en not_active Expired - Fee Related
- 2013-08-06 CN CN201380035993.XA patent/CN104470905B/zh not_active Expired - Fee Related
- 2013-08-06 MX MX2015001720A patent/MX2015001720A/es unknown
- 2013-08-06 BR BR112015001830A patent/BR112015001830A2/pt not_active IP Right Cessation
- 2013-08-06 WO PCT/EP2013/066431 patent/WO2014023708A1/en not_active Ceased
- 2013-08-06 EP EP13747659.4A patent/EP2882725A1/en not_active Withdrawn
- 2013-08-06 RU RU2015105561A patent/RU2015105561A/ru not_active Application Discontinuation
- 2013-08-06 JP JP2015525858A patent/JP6266617B2/ja not_active Expired - Fee Related
- 2013-08-06 KR KR20157005929A patent/KR20150041647A/ko not_active Withdrawn
- 2013-08-06 CA CA2877048A patent/CA2877048A1/en not_active Abandoned
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