JP2021038228A5 - - Google Patents

Info

Publication number

JP2021038228A5

JP2021038228A5 JP2020180340A JP2020180340A JP2021038228A5 JP 2021038228 A5 JP2021038228 A5 JP 2021038228A5 JP 2020180340 A JP2020180340 A JP 2020180340A JP 2020180340 A JP2020180340 A JP 2020180340A JP 2021038228 A5 JP2021038228 A5 JP 2021038228A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

composition according

oxo

methyl

difluorophenyl

Prior art date

2020-10-28

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.)

Withdrawn

Links

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• 239000008194 pharmaceutical composition Substances 0.000 claims 21
• -1 azepine-7-yl Chemical group 0.000 claims 7
• 241000124008 Mammalia Species 0.000 claims 5
• 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 4
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
• 206010011878 Deafness Diseases 0.000 claims 3
• 229940125373 Gamma-Secretase Inhibitor Drugs 0.000 claims 3
• 210000003030 auditory receptor cell Anatomy 0.000 claims 3
• 239000003540 gamma secretase inhibitor Substances 0.000 claims 3
• 231100000888 hearing loss Toxicity 0.000 claims 3
• 230000010370 hearing loss Effects 0.000 claims 3
• 208000016354 hearing loss disease Diseases 0.000 claims 3
• 238000000034 method Methods 0.000 claims 3
• 231100000199 ototoxic Toxicity 0.000 claims 3
• 230000002970 ototoxic effect Effects 0.000 claims 3
• PKXWXXPNHIWQHW-RCBQFDQVSA-N (2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(5S)-3-methyl-4-oxo-2,5-dihydro-1H-3-benzazepin-5-yl]amino]-1-oxopropan-2-yl]butanamide Chemical compound C1CN(C)C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](O)C(C)C)C2=CC=CC=C21 PKXWXXPNHIWQHW-RCBQFDQVSA-N 0.000 claims 2
• IZAOBRWCUGOKNH-OAHLLOKOSA-N 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid Chemical compound C=1C=C(Cl)C=CC=1S(=O)(=O)N([C@H](C)C=1C(=CC(F)=CC=1)CCCC(O)=O)C1=CC(F)=CC=C1F IZAOBRWCUGOKNH-OAHLLOKOSA-N 0.000 claims 2
• DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
• KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
• 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
• 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
• KJSSPOWBVHTGDG-UHFFFAOYSA-N 2-(2,2,3,3,3-pentafluoropropyl)propanediamide Chemical compound NC(=O)C(C(N)=O)CC(F)(F)C(F)(F)F KJSSPOWBVHTGDG-UHFFFAOYSA-N 0.000 claims 1
• XCGJIFAKUZNNOR-UHFFFAOYSA-N 3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid Chemical compound C1CC(CCC(=O)O)CCC1(S(=O)(=O)C=1C=CC(Cl)=CC=1)C1=CC(F)=CC=C1F XCGJIFAKUZNNOR-UHFFFAOYSA-N 0.000 claims 1
• XEAOPVUAMONVLA-QGZVFWFLSA-N Avagacestat Chemical compound C=1C=C(Cl)C=CC=1S(=O)(=O)N([C@H](CCC(F)(F)F)C(=O)N)CC(C(=C1)F)=CC=C1C=1N=CON=1 XEAOPVUAMONVLA-QGZVFWFLSA-N 0.000 claims 1
• DWJXYEABWRJFSP-XOBRGWDASA-N DAPT Chemical compound N([C@@H](C)C(=O)N[C@H](C(=O)OC(C)(C)C)C=1C=CC=CC=1)C(=O)CC1=CC(F)=CC(F)=C1 DWJXYEABWRJFSP-XOBRGWDASA-N 0.000 claims 1
• NGBKFLTYGSREKK-PMACEKPBSA-N Z-Val-Phe-H Chemical compound N([C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C=O)C(=O)OCC1=CC=CC=C1 NGBKFLTYGSREKK-PMACEKPBSA-N 0.000 claims 1
• 150000001408 amides Chemical class 0.000 claims 1
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
• DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims 1
• 108010007877 calpain inhibitor III Proteins 0.000 claims 1
• 230000006727 cell loss Effects 0.000 claims 1
• JNGZXGGOCLZBFB-IVCQMTBJSA-N compound E Chemical compound N([C@@H](C)C(=O)N[C@@H]1C(N(C)C2=CC=CC=C2C(C=2C=CC=CC=2)=N1)=O)C(=O)CC1=CC(F)=CC(F)=C1 JNGZXGGOCLZBFB-IVCQMTBJSA-N 0.000 claims 1
• 125000004212 difluorophenyl group Chemical group 0.000 claims 1
• 238000011977 dual antiplatelet therapy Methods 0.000 claims 1
• 230000035800 maturation Effects 0.000 claims 1
• 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims 1
• QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 229950001900 semagacestat Drugs 0.000 claims 1
• 239000000126 substance Substances 0.000 claims 1
• 238000013268 sustained release Methods 0.000 claims 1
• 239000012730 sustained-release form Substances 0.000 claims 1
• SJMDMGHPMLKLHQ-UHFFFAOYSA-N tert-butyl 2-aminoacetate Chemical compound CC(C)(C)OC(=O)CN SJMDMGHPMLKLHQ-UHFFFAOYSA-N 0.000 claims 1
• MURCDOXDAHPNRQ-PJRHAEEISA-N tert-butyl n-[(2s,3r,5s)-6-[[(2s)-1-[[(2s)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-benzyl-3-hydroxy-6-oxo-1-phenylhexan-2-yl]carbamate Chemical compound C([C@@H]([C@H](O)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)CC=1C=CC=CC=1)NC(=O)OC(C)(C)C)C1=CC=CC=C1 MURCDOXDAHPNRQ-PJRHAEEISA-N 0.000 claims 1
• 229920000428 triblock copolymer Polymers 0.000 claims 1