JP2020529998A5 - - Google Patents
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- Publication number
- JP2020529998A5 JP2020529998A5 JP2020505842A JP2020505842A JP2020529998A5 JP 2020529998 A5 JP2020529998 A5 JP 2020529998A5 JP 2020505842 A JP2020505842 A JP 2020505842A JP 2020505842 A JP2020505842 A JP 2020505842A JP 2020529998 A5 JP2020529998 A5 JP 2020529998A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- thiazole
- substituted
- carboxamide
- pyrrolidine
- 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
- PQQRHWFRZHFGFM-UHFFFAOYSA-N 1,3-thiazole-4-carboxamide Chemical compound NC(=O)C1=CSC=N1 PQQRHWFRZHFGFM-UHFFFAOYSA-N 0.000 claims 105
- -1 pyridin-2-carbonyl Chemical group 0.000 claims 67
- 150000001875 compounds Chemical class 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 2
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- NYCVCXMSZNOGDH-UHFFFAOYSA-N pyrrolidine-1-carboxylic acid Chemical compound OC(=O)N1CCCC1 NYCVCXMSZNOGDH-UHFFFAOYSA-N 0.000 claims 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 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
- 239000004472 Lysine Substances 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- OSILBMSORKFRTB-UHFFFAOYSA-N isoquinolin-1-amine Chemical compound C1=CC=C2C(N)=NC=CC2=C1 OSILBMSORKFRTB-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 0 CC(N(CC(*)C1)[C@]1C(/C=C/C1)=CC=CC=C1C(N*)=O)=O Chemical compound CC(N(CC(*)C1)[C@]1C(/C=C/C1)=CC=CC=C1C(N*)=O)=O 0.000 description 4
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023002547A JP7427812B2 (ja) | 2017-08-04 | 2023-01-11 | 血漿カリクレインの阻害剤およびその使用 |
| JP2024008397A JP7785108B2 (ja) | 2017-08-04 | 2024-01-24 | 血漿カリクレインの阻害剤およびその使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762541403P | 2017-08-04 | 2017-08-04 | |
| US62/541,403 | 2017-08-04 | ||
| PCT/US2018/045183 WO2019028362A1 (en) | 2017-08-04 | 2018-08-03 | INHIBITORS OF PLASMATIC KALLIKREIN AND USES THEREOF |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023002547A Division JP7427812B2 (ja) | 2017-08-04 | 2023-01-11 | 血漿カリクレインの阻害剤およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020529998A JP2020529998A (ja) | 2020-10-15 |
| JP2020529998A5 true JP2020529998A5 (enExample) | 2021-08-26 |
| JP7210540B2 JP7210540B2 (ja) | 2023-01-23 |
Family
ID=63209746
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020505842A Active JP7210540B2 (ja) | 2017-08-04 | 2018-08-03 | 血漿カリクレインの阻害剤およびその使用 |
| JP2023002547A Active JP7427812B2 (ja) | 2017-08-04 | 2023-01-11 | 血漿カリクレインの阻害剤およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023002547A Active JP7427812B2 (ja) | 2017-08-04 | 2023-01-11 | 血漿カリクレインの阻害剤およびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US11168083B2 (enExample) |
| EP (2) | EP3661922B1 (enExample) |
| JP (2) | JP7210540B2 (enExample) |
| AU (3) | AU2018311976B2 (enExample) |
| CA (1) | CA3070717A1 (enExample) |
| WO (1) | WO2019028362A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11168083B2 (en) | 2017-08-04 | 2021-11-09 | Takeda Pharmaceutical Company Limited | Inhibitors of Plasma Kallikrein and uses thereof |
| WO2019178129A1 (en) * | 2018-03-13 | 2019-09-19 | Shire Human Genetic Therapies, Inc. | Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof |
| PT4031547T (pt) * | 2019-09-18 | 2024-08-27 | Takeda Pharmaceuticals Co | Inibidores de calicreína plasmática e utilizações dos mesmos |
| WO2021055589A1 (en) | 2019-09-18 | 2021-03-25 | Shire Human Genetic Therapies, Inc. | Heteroaryl plasma kallikrein inhibitors |
| CA3167336A1 (en) * | 2020-01-13 | 2021-07-22 | Takeda Pharmaceutical Company Limited | Plasma kallikrein inhibitors and uses thereof for treating pediatric hereditary angioedema attack |
| WO2021198534A1 (en) | 2020-04-04 | 2021-10-07 | Oxurion NV | Plasma kallikrein inhibitors for use in the treatment of coronaviral disease |
| WO2023144030A1 (en) | 2022-01-31 | 2023-08-03 | Oxurion NV | Plasma kallikrein inhibitor therapy for anti-vegf sensitization |
| WO2023148016A1 (en) | 2022-02-04 | 2023-08-10 | Oxurion NV | Biomarker for plasma kallikrein inhibitor therapy response |
| WO2024059186A1 (en) * | 2022-09-15 | 2024-03-21 | Takeda Pharmaceutical Company Limited | N-((isoquinolin-6-yl)methyl)-1h-pyrazole-4-carboxamid derivatives as plasma kallikrein inhibitors for the treatment of hereditary angioedema |
| CN116063215A (zh) * | 2023-02-23 | 2023-05-05 | 南京安淮创新药物研究院有限公司 | 一种4-氨基-l-脯氨酸的合成方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA004792B1 (ru) | 1998-06-30 | 2004-08-26 | Пфайзер Продактс Инк. | Непептидные ингибиторы vla-4-зависимого клеточного связывания, полезные в лечении воспалительных, аутоиммунных и респираторных заболеваний |
| CA2634743C (en) * | 2005-12-23 | 2014-07-29 | Zealand Pharma A/S | Modified lysine-mimetic compounds |
| WO2010015090A1 (en) * | 2008-08-07 | 2010-02-11 | Aegera Therapeutics Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
| US9079880B2 (en) * | 2010-07-07 | 2015-07-14 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| EP2807157A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| BR112014015582A8 (pt) * | 2012-02-24 | 2017-07-04 | Hoffmann La Roche | compostos antivirais |
| GB201209138D0 (en) * | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
| JP6337750B2 (ja) * | 2013-11-22 | 2018-06-06 | 小野薬品工業株式会社 | 化合物 |
| SG11201706411YA (en) | 2015-02-27 | 2017-09-28 | Verseon Corp | Substituted pyrazole compounds as serine protease inhibitors |
| CN107614532A (zh) * | 2015-03-30 | 2018-01-19 | 戴埃克斯有限公司 | 血浆激肽释放酶抑制剂及其预防遗传性血管性水肿发作的用途 |
| WO2017001936A2 (en) * | 2015-07-01 | 2017-01-05 | Lifesci Pharmaceuticals, Inc. | Therapeutic inhibitory compounds |
| KR102696432B1 (ko) | 2015-10-01 | 2024-08-16 | 바이오크리스트파마슈티컬즈,인코포레이티드 | 인간 혈장 칼리크레인 저해제 |
| US11168083B2 (en) | 2017-08-04 | 2021-11-09 | Takeda Pharmaceutical Company Limited | Inhibitors of Plasma Kallikrein and uses thereof |
| WO2019178129A1 (en) * | 2018-03-13 | 2019-09-19 | Shire Human Genetic Therapies, Inc. | Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof |
| PT4031547T (pt) * | 2019-09-18 | 2024-08-27 | Takeda Pharmaceuticals Co | Inibidores de calicreína plasmática e utilizações dos mesmos |
| WO2021055589A1 (en) * | 2019-09-18 | 2021-03-25 | Shire Human Genetic Therapies, Inc. | Heteroaryl plasma kallikrein inhibitors |
| DK4136091T3 (da) * | 2020-04-17 | 2025-08-18 | Takeda Pharmaceuticals Co | Former og sammensætninger af plasmakallikreinhæmmere |
-
2018
- 2018-08-03 US US16/636,518 patent/US11168083B2/en active Active
- 2018-08-03 CA CA3070717A patent/CA3070717A1/en active Pending
- 2018-08-03 JP JP2020505842A patent/JP7210540B2/ja active Active
- 2018-08-03 WO PCT/US2018/045183 patent/WO2019028362A1/en not_active Ceased
- 2018-08-03 EP EP18755681.6A patent/EP3661922B1/en active Active
- 2018-08-03 AU AU2018311976A patent/AU2018311976B2/en active Active
- 2018-08-03 EP EP24203482.5A patent/EP4494698A3/en active Pending
-
2021
- 2021-11-04 US US17/519,013 patent/US11905285B2/en active Active
-
2023
- 2023-01-11 JP JP2023002547A patent/JP7427812B2/ja active Active
- 2023-01-12 AU AU2023200156A patent/AU2023200156B2/en active Active
- 2023-12-20 US US18/390,137 patent/US20240199602A1/en active Pending
-
2025
- 2025-06-26 AU AU2025204840A patent/AU2025204840A1/en active Pending
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