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 (https=) | 2021-08-26 |
| JP7210540B2 JP7210540B2 (ja) | 2023-01-23 |
Family
ID=63209746
Family Applications (3)
| 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 |
| JP2024008397A Active 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 |
Family Applications After (2)
| 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 |
| JP2024008397A Active 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 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US11168083B2 (https=) |
| EP (2) | EP4494698A3 (https=) |
| JP (3) | JP7210540B2 (https=) |
| AU (3) | AU2018311976B2 (https=) |
| WO (1) | WO2019028362A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7210540B2 (ja) | 2017-08-04 | 2023-01-23 | 武田薬品工業株式会社 | 血漿カリクレインの阻害剤およびその使用 |
| KR20200143376A (ko) * | 2018-03-13 | 2020-12-23 | 샤이어 휴먼 지네틱 테라피즈 인크. | 혈장 칼리크레인 억제제로서의 치환된 이미다조피리딘 및 이의 용도 |
| CN114667289B (zh) | 2019-09-18 | 2025-08-26 | 武田药品工业有限公司 | 杂芳基血浆激肽释放酶抑制剂 |
| EP4031547B1 (en) * | 2019-09-18 | 2024-07-17 | Takeda Pharmaceutical Company Limited | Plasma kallikrein inhibitors and uses thereof |
| US12528880B2 (en) | 2020-01-13 | 2026-01-20 | 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 |
| JP2025531207A (ja) * | 2022-09-15 | 2025-09-19 | 武田薬品工業株式会社 | 遺伝性血管性浮腫の処置のための血漿カリクレイン阻害剤としてのｎ－（（イソキノリン－６イル）メチル）－１ｈ－ピラゾール－４－カルボキサミド誘導体 |
| 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 |
|---|---|---|---|---|
| KR20010083081A (ko) | 1998-06-30 | 2001-08-31 | 실버스타인 아써 에이. | 염증성질환, 자가면역질환 및 호흡기질환을 치료하는데유용한 브이엘에이-4-의존성 세포 결합의 비-펩티딜 억제제 |
| UA96283C2 (uk) * | 2005-12-23 | 2011-10-25 | Зіланд Фарма А/С | Модифіковані міметики лізину |
| 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 |
| US20140378474A1 (en) | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP2817291A1 (en) * | 2012-02-24 | 2014-12-31 | F. Hoffmann-La Roche AG | Antiviral compounds |
| 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 |
| CN107405333A (zh) * | 2015-02-27 | 2017-11-28 | 维颂公司 | 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物 |
| BR112017020864A2 (en) * | 2015-03-30 | 2018-07-10 | Dyax Corp. | plasma kallikrein inhibitors and their uses for the prevention of hereditary angioedema attack |
| WO2017001936A2 (en) | 2015-07-01 | 2017-01-05 | Lifesci Pharmaceuticals, Inc. | Therapeutic inhibitory compounds |
| MY198346A (en) * | 2015-10-01 | 2023-08-28 | Biocryst Pharm Inc | Human plasma kallikrein inhibitors |
| JP7210540B2 (ja) | 2017-08-04 | 2023-01-23 | 武田薬品工業株式会社 | 血漿カリクレインの阻害剤およびその使用 |
| KR20200143376A (ko) * | 2018-03-13 | 2020-12-23 | 샤이어 휴먼 지네틱 테라피즈 인크. | 혈장 칼리크레인 억제제로서의 치환된 이미다조피리딘 및 이의 용도 |
| EP4031547B1 (en) * | 2019-09-18 | 2024-07-17 | Takeda Pharmaceutical Company Limited | Plasma kallikrein inhibitors and uses thereof |
| CN114667289B (zh) * | 2019-09-18 | 2025-08-26 | 武田药品工业有限公司 | 杂芳基血浆激肽释放酶抑制剂 |
| PT4136091T (pt) * | 2020-04-17 | 2025-08-22 | Takeda Pharmaceuticals Co | Formas e composições de inibidores da calicreína plasmática |
-
2018
- 2018-08-03 JP JP2020505842A patent/JP7210540B2/ja active Active
- 2018-08-03 AU AU2018311976A patent/AU2018311976B2/en active Active
- 2018-08-03 EP EP24203482.5A patent/EP4494698A3/en not_active Withdrawn
- 2018-08-03 US US16/636,518 patent/US11168083B2/en 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
-
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
-
2024
- 2024-01-24 JP JP2024008397A patent/JP7785108B2/ja active Active
-
2025
- 2025-06-26 AU AU2025204840A patent/AU2025204840A1/en active Pending
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