JP2018528244A5 - - Google Patents

Info

Publication number

JP2018528244A5

JP2018528244A5 JP2018515621A JP2018515621A JP2018528244A5 JP 2018528244 A5 JP2018528244 A5 JP 2018528244A5 JP 2018515621 A JP2018515621 A JP 2018515621A JP 2018515621 A JP2018515621 A JP 2018515621A JP 2018528244 A5 JP2018528244 A5 JP 2018528244A5

Authority

JP

Japan

Prior art keywords

substituted

alkyl

alkoxy

pyrrolo

pyrrole

Prior art date

2016-09-20

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

• Espacenet
• Global Dossier
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• 150000001875 compounds Chemical class 0.000 claims 28
• 125000004076 pyridyl group Chemical group 0.000 claims 22
• 229910052736 halogen Inorganic materials 0.000 claims 15
• 150000002367 halogens Chemical class 0.000 claims 15
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 12
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
• 150000003839 salts Chemical class 0.000 claims 7
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
• 208000024891 symptom Diseases 0.000 claims 4
• 125000001544 thienyl group Chemical group 0.000 claims 4
• VMVMHHKCHQENQR-IERDGZPVSA-N FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)F)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F Chemical compound FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)F)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F VMVMHHKCHQENQR-IERDGZPVSA-N 0.000 claims 3
• VIABIWADPYYFDB-VGSWGCGISA-N FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)OC)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F Chemical compound FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)OC)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F VIABIWADPYYFDB-VGSWGCGISA-N 0.000 claims 3
• 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 3
• 125000004093 cyano group Chemical group *C#N 0.000 claims 3
• 239000008194 pharmaceutical composition Substances 0.000 claims 3
• 125000006621 (C3-C8) cycloalkyl-(C1-C6) alkyl group Chemical group 0.000 claims 2
• BLWDBBGFQGUZAO-NGOKVRLYSA-N 4-[(3aS,6aR)-5-[2-cyclopropyl-6-(oxan-4-ylmethoxy)pyridine-4-carbonyl]-3a-fluoro-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-2-carbonyl]-3-fluorobenzenesulfonamide Chemical compound C1(CC1)C1=NC(=CC(=C1)C(=O)N1C[C@H]2[C@](C1)(CN(C2)C(=O)C1=C(C=C(C=C1)S(=O)(=O)N)F)F)OCC1CCOCC1 BLWDBBGFQGUZAO-NGOKVRLYSA-N 0.000 claims 2
• TZVRREQSYXCEFD-PBBNMVCDSA-N 4-[(3aS,6aR)-5-[2-cyclopropyl-6-(oxan-4-ylmethoxy)pyridine-4-carbonyl]-3a-methoxy-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-2-carbonyl]-3-fluorobenzenesulfonamide Chemical compound C1(CC1)C1=NC(=CC(=C1)C(=O)N1C[C@H]2[C@](C1)(CN(C2)C(=O)C1=C(C=C(C=C1)S(=O)(=O)N)F)OC)OCC1CCOCC1 TZVRREQSYXCEFD-PBBNMVCDSA-N 0.000 claims 2
• TZSGWDNESWOLHK-DWXRJYCRSA-N CC(C(=O)NC=1C(=NC=C(C=1)C(F)(F)F)COC(=O)N1C[C@H]2CN(C[C@@]2(C1)OC)C(C1=CC=C(C=C1)S(N)(=O)=O)=O)(C)C Chemical compound CC(C(=O)NC=1C(=NC=C(C=1)C(F)(F)F)COC(=O)N1C[C@H]2CN(C[C@@]2(C1)OC)C(C1=CC=C(C=C1)S(N)(=O)=O)=O)(C)C TZSGWDNESWOLHK-DWXRJYCRSA-N 0.000 claims 2
• BGHGKELMYMNCFY-VGOFRKELSA-N FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)C)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F Chemical compound FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)C)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F BGHGKELMYMNCFY-VGOFRKELSA-N 0.000 claims 2
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
• AAICNDKQIKYSNG-QZZOKCEJSA-N 4-[(3aR,6aS)-3a-fluoro-2-[(E)-3-[4-(trifluoromethoxy)phenyl]prop-2-enoyl]-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carbonyl]-3-fluorobenzenesulfonamide Chemical compound F[C@@]12[C@H](CN(C1)C(=O)C1=C(C=C(C=C1)S(=O)(=O)N)F)CN(C2)C(\C=C\C1=CC=C(C=C1)OC(F)(F)F)=O AAICNDKQIKYSNG-QZZOKCEJSA-N 0.000 claims 1
• BBKZDEOQJWTOHA-OYHNWAKOSA-N 4-[(3aR,6aS)-3a-fluoro-2-[3-[4-(trifluoromethoxy)phenyl]propanoyl]-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carbonyl]-3-fluorobenzenesulfonamide Chemical compound F[C@@]12[C@H](CN(C1)C(=O)C1=C(C=C(C=C1)S(=O)(=O)N)F)CN(C2)C(CCC1=CC=C(C=C1)OC(F)(F)F)=O BBKZDEOQJWTOHA-OYHNWAKOSA-N 0.000 claims 1
• FRUHHNULBUJYKS-QMHKHESXSA-N 4-[(3aR,6aS)-3a-methoxy-2-[3-[4-(trifluoromethoxy)phenyl]propanoyl]-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carbonyl]-3-fluorobenzenesulfonamide Chemical compound CO[C@@]12[C@H](CN(C1)C(=O)C1=C(C=C(C=C1)S(=O)(=O)N)F)CN(C2)C(CCC1=CC=C(C=C1)OC(F)(F)F)=O FRUHHNULBUJYKS-QMHKHESXSA-N 0.000 claims 1
• MMUCHTMOBQDDBF-YEJXKQKISA-N 4-[(3aS,6aR)-3a-fluoro-2-[2-[4-(trifluoromethoxy)phenoxy]acetyl]-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carbonyl]-3-fluorobenzenesulfonamide Chemical compound F[C@@]12[C@H](CN(C1)C(=O)C1=C(C=C(C=C1)S(=O)(=O)N)F)CN(C2)C(COC1=CC=C(C=C1)OC(F)(F)F)=O MMUCHTMOBQDDBF-YEJXKQKISA-N 0.000 claims 1
• -1 4-sulfamoyl-benzoyl Chemical group 0.000 claims 1
• JJQAUXGBCRMNQO-UHFFFAOYSA-N CC(C(=O)NC=1C(=NC=C(C=1)C(F)(F)F)COC(=O)C1=CC=CN1)(C)C Chemical compound CC(C(=O)NC=1C(=NC=C(C=1)C(F)(F)F)COC(=O)C1=CC=CN1)(C)C JJQAUXGBCRMNQO-UHFFFAOYSA-N 0.000 claims 1
• BGHGKELMYMNCFY-JTSKRJEESA-N FC(OC1=CC=C(COC(=O)N2C[C@@H]3CN(C[C@]3(C2)C)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F Chemical compound FC(OC1=CC=C(COC(=O)N2C[C@@H]3CN(C[C@]3(C2)C)C(C2=CC=C(C=C2)S(N)(=O)=O)=O)C=C1)(F)F BGHGKELMYMNCFY-JTSKRJEESA-N 0.000 claims 1
• FQSCYWBLDBNLFI-DXPJPUQTSA-N [3-(2,2-dimethylpropanoylamino)-5-(trifluoromethyl)pyridin-2-yl]methyl (3aS,6aR)-2-(2-fluoro-4-sulfamoylbenzoyl)-3a-methoxy-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carboxylate Chemical compound CC(C(=O)NC=1C(=NC=C(C=1)C(F)(F)F)COC(=O)N1C[C@H]2CN(C[C@@]2(C1)OC)C(C1=C(C=C(C=C1)S(N)(=O)=O)F)=O)(C)C FQSCYWBLDBNLFI-DXPJPUQTSA-N 0.000 claims 1
• CQRUZVNAXCQQSP-CPJLOUKISA-N [3-(2,2-dimethylpropanoylamino)-5-(trifluoromethyl)pyridin-2-yl]methyl (3aS,6aR)-3a-methoxy-2-(5-sulfamoylpyridine-2-carbonyl)-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carboxylate Chemical compound CC(C(=O)NC=1C(=NC=C(C=1)C(F)(F)F)COC(=O)N1C[C@H]2CN(C[C@@]2(C1)OC)C(=O)C1=NC=C(C=C1)S(N)(=O)=O)(C)C CQRUZVNAXCQQSP-CPJLOUKISA-N 0.000 claims 1
• JZWJHPHUGXKWSV-SZNDQCEHSA-N [4-(trifluoromethoxy)phenyl]methyl (3aS,6aR)-3a-fluoro-2-(2-fluoro-4-sulfamoylbenzoyl)-3,4,6,6a-tetrahydro-1H-pyrrolo[3,4-c]pyrrole-5-carboxylate Chemical compound FC(OC1=CC=C(COC(=O)N2C[C@H]3CN(C[C@@]3(C2)F)C(C2=C(C=C(C=C2)S(N)(=O)=O)F)=O)C=C1)(F)F JZWJHPHUGXKWSV-SZNDQCEHSA-N 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• 239000013543 active substance Substances 0.000 claims 1
• 125000003545 alkoxy group Chemical group 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1