JP2018536648A5 - - Google Patents
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- Publication number
- JP2018536648A5 JP2018536648A5 JP2018521556A JP2018521556A JP2018536648A5 JP 2018536648 A5 JP2018536648 A5 JP 2018536648A5 JP 2018521556 A JP2018521556 A JP 2018521556A JP 2018521556 A JP2018521556 A JP 2018521556A JP 2018536648 A5 JP2018536648 A5 JP 2018536648A5
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- JP
- Japan
- Prior art keywords
- ring
- optionally
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- atom
- alkyl
- 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
- 125000004432 carbon atom Chemical group C* 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 11
- 229910052731 fluorine Inorganic materials 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- 229920006395 saturated elastomer Polymers 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 5
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 3
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 1
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 229910052789 astatine Inorganic materials 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 230000008728 vascular permeability Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15191757 | 2015-10-27 | ||
| EP15191757.2 | 2015-10-27 | ||
| PCT/EP2016/075221 WO2017072020A1 (en) | 2015-10-27 | 2016-10-20 | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018536648A JP2018536648A (ja) | 2018-12-13 |
| JP2018536648A5 true JP2018536648A5 (enExample) | 2019-12-05 |
| JP6917988B2 JP6917988B2 (ja) | 2021-08-11 |
Family
ID=54539822
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018521556A Active JP6917988B2 (ja) | 2015-10-27 | 2016-10-20 | 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10399961B2 (enExample) |
| EP (1) | EP3368529B1 (enExample) |
| JP (1) | JP6917988B2 (enExample) |
| WO (1) | WO2017072020A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| AU2016224974B2 (en) | 2015-02-27 | 2019-09-26 | Verseon Corporation | Substituted pyrazole compounds as serine protease inhibitors |
| WO2017072021A1 (en) | 2015-10-27 | 2017-05-04 | Boehringer Ingelheim International Gmbh | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| WO2017207983A1 (en) | 2016-05-31 | 2017-12-07 | Kalvista Pharmaceuticals Limited | Pyrazole derivatives as plasma kallikrein inhibitors |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| JP7078722B2 (ja) | 2017-11-29 | 2022-05-31 | カルビスタ・ファーマシューティカルズ・リミテッド | 血漿カリクレイン阻害剤を含む剤形 |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| EP3837252B1 (en) * | 2018-08-16 | 2025-12-10 | Boehringer Ingelheim International GmbH | Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors |
| US12091399B2 (en) | 2018-10-10 | 2024-09-17 | Boehringer Ingelheim International Gmbh | Phenyltetrazole derivatives as plasma kallikrein inhibitors |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| TW202144331A (zh) | 2020-02-13 | 2021-12-01 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| TWI873290B (zh) * | 2020-02-13 | 2025-02-21 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| WO2021198534A1 (en) | 2020-04-04 | 2021-10-07 | Oxurion NV | Plasma kallikrein inhibitors for use in the treatment of coronaviral disease |
| US12528786B2 (en) | 2020-07-10 | 2026-01-20 | Merck Sharp & Dohme Llc | Plasma kallikrein inhibitors |
| 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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI243164B (en) * | 2001-02-13 | 2005-11-11 | Aventis Pharma Gmbh | Acylated indanyl amines and their use as pharmaceuticals |
| US20050090529A1 (en) * | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| MX2009007058A (es) | 2006-12-28 | 2009-07-10 | Takeda Pharmaceutical | Compuesto triciclico y uso farmaceutico del mismo. |
| US8658685B2 (en) * | 2008-01-31 | 2014-02-25 | Activesite Pharmaceuticals, Inc. | Methods for treatment of kallikrein-related disorders |
| US9290485B2 (en) * | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| WO2013111108A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| WO2013111107A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | Aminopyridine derivatives as plasma kallikrein inhibitors |
| BR112015028879B1 (pt) * | 2013-05-23 | 2022-12-20 | Kalvista Pharmaceuticals Limited | Compostos derivados heterocíclicos, composição farmacêutica compreendendo os referidos compostos e usos dos mesmos |
-
2016
- 2016-10-20 WO PCT/EP2016/075221 patent/WO2017072020A1/en not_active Ceased
- 2016-10-20 JP JP2018521556A patent/JP6917988B2/ja active Active
- 2016-10-20 US US15/770,762 patent/US10399961B2/en active Active
- 2016-10-20 EP EP16784206.1A patent/EP3368529B1/en active Active
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