CN111655681B - 杂环基氨基取代的三唑类化合物作为Rho相关蛋白激酶的调节剂 - Google Patents
杂环基氨基取代的三唑类化合物作为Rho相关蛋白激酶的调节剂 Download PDFInfo
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- CN111655681B CN111655681B CN201980010083.3A CN201980010083A CN111655681B CN 111655681 B CN111655681 B CN 111655681B CN 201980010083 A CN201980010083 A CN 201980010083A CN 111655681 B CN111655681 B CN 111655681B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1801226.0 | 2018-01-25 | ||
| GBGB1801226.0A GB201801226D0 (en) | 2018-01-25 | 2018-01-25 | Modulators of Rho-associated protein kinase |
| PCT/GB2019/050215 WO2019145729A1 (en) | 2018-01-25 | 2019-01-25 | Heterocyclylamino-substituted triazoles as modulators of rho-associated protein kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111655681A CN111655681A (zh) | 2020-09-11 |
| CN111655681B true CN111655681B (zh) | 2024-01-05 |
Family
ID=61558335
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980010083.3A Active CN111655681B (zh) | 2018-01-25 | 2019-01-25 | 杂环基氨基取代的三唑类化合物作为Rho相关蛋白激酶的调节剂 |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US11497751B2 (https=) |
| EP (2) | EP4026834A1 (https=) |
| JP (2) | JP7518324B2 (https=) |
| KR (1) | KR102737926B1 (https=) |
| CN (1) | CN111655681B (https=) |
| AU (1) | AU2019213214B2 (https=) |
| CA (1) | CA3088330A1 (https=) |
| CY (1) | CY1125017T1 (https=) |
| DK (1) | DK3743420T3 (https=) |
| EA (1) | EA202091711A1 (https=) |
| ES (1) | ES2907833T3 (https=) |
| GB (1) | GB201801226D0 (https=) |
| HR (1) | HRP20220269T8 (https=) |
| HU (1) | HUE058940T2 (https=) |
| IL (1) | IL275988B2 (https=) |
| LT (1) | LT3743420T (https=) |
| MX (1) | MX2020007898A (https=) |
| PH (1) | PH12020550986A1 (https=) |
| PL (1) | PL3743420T3 (https=) |
| PT (1) | PT3743420T (https=) |
| SG (1) | SG11202006087UA (https=) |
| SI (1) | SI3743420T1 (https=) |
| SM (1) | SMT202200099T1 (https=) |
| WO (1) | WO2019145729A1 (https=) |
| ZA (1) | ZA202003983B (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201801226D0 (en) | 2018-01-25 | 2018-03-14 | Redx Pharma Plc | Modulators of Rho-associated protein kinase |
| BR112021017354A2 (pt) | 2019-03-01 | 2021-11-16 | Beijing Tide Pharmaceutical Co Ltd | Método para o tratamento de doença hepática adiposa e/ou esteatoepatite |
| CN111718310B (zh) * | 2019-08-19 | 2021-06-11 | 中国药科大学 | 苯基取代的五元杂环类化合物及其制备方法、用途和药物组合物 |
| CN110845410B (zh) * | 2019-10-29 | 2021-02-26 | 暨明医药科技（苏州）有限公司 | 一种一锅法制备6,7-二甲氧基-3,4-二氢异喹啉盐酸盐的方法 |
| US20240131029A1 (en) * | 2021-02-04 | 2024-04-25 | President And Fellows Of Harvard College | Selective rock2 inhibition for treatment of edema and associated conditions |
| CA3226387A1 (en) * | 2021-07-26 | 2023-02-02 | Joel D. Moore | Rock2 inhibitors and uses thereof |
| CN113999211B (zh) * | 2021-11-23 | 2022-11-29 | 郑州大学 | 一类特异性抗前列腺癌活性的含1,2,3-三氮唑的吲唑骨架衍生物 |
| GB202200735D0 (en) * | 2022-01-20 | 2022-03-09 | Redx Pharma Plc | Compounds |
| WO2023182856A1 (ko) * | 2022-03-24 | 2023-09-28 | 서울대학교산학협력단 | 로-키나제 억제제를 포함하는 켈로이드 등 피부 섬유화 질환의 예방 또는 치료용 약학적 조성물 및 그의 용도 |
| DK4514782T3 (da) | 2022-05-19 | 2025-12-15 | Astrazeneca Ab | Heteroaromatiske amidoforbindelser, der er nyttige ved behandling af leversygdomme |
| CN115124558B (zh) * | 2022-07-08 | 2024-08-13 | 闽都创新实验室 | 一种芳基硼酸酯类化合物的制备方法及其应用 |
| WO2024123129A1 (ko) * | 2022-12-08 | 2024-06-13 | 한국과학기술원 | 파브리병의 예방 또는 치료용 조성물 |
| CN116891460A (zh) * | 2023-07-12 | 2023-10-17 | 浙江大学 | 一种吲唑类衍生物或其药用盐及应用 |
| WO2025017499A1 (en) | 2023-07-17 | 2025-01-23 | Graviton Bioscience Bv | Formulations and uses of rock2 inhibitors for als |
| GB202311061D0 (en) * | 2023-07-19 | 2023-08-30 | Redx Pharma Plc | Modulators of rho-associated protein kinase |
| GB202311062D0 (en) * | 2023-07-19 | 2023-08-30 | Redx Pharma Plc | Modulators of rho-associated protein kinase |
| WO2025069008A1 (en) | 2023-09-28 | 2025-04-03 | Graviton Bioscience Bv | Therapy for treating type 1 diabetes using rock2 and dyrk1 inhibitors |
| WO2025069009A1 (en) | 2023-09-29 | 2025-04-03 | Graviton Bioscience Bv | Rock2 inhibitors in the treatment of obesity |
| TW202542129A (zh) * | 2023-12-22 | 2025-11-01 | 美商美國禮來大藥廠 | Rho相關蛋白激酶抑制劑 |
| IT202400002560A1 (it) * | 2024-02-07 | 2025-08-07 | Univ Pisa | Inibitori della proteina rock per uso nel trattamento della fibrosi polmonare |
| WO2025256614A1 (zh) * | 2024-06-14 | 2025-12-18 | 北京普祺医药科技股份有限公司 | 一种促进胶原蛋白表达的抑制剂 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006135383A2 (en) * | 2004-08-04 | 2006-12-21 | Myriad Genetics, Inc. | Indazoles |
| CN103429585A (zh) * | 2010-12-20 | 2013-12-04 | 默克雪兰诺股份有限公司 | 作为白细胞介素-1受体相关激酶抑制剂的吲唑基三唑衍生物 |
| WO2016138335A1 (en) * | 2015-02-27 | 2016-09-01 | Lycera Corporation | Indazolyl thiadiazolamines and related compounds for inhibition of rho-associated protein kinase and the treatment of disease |
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| GB9207396D0 (en) | 1992-04-03 | 1992-05-13 | Merck Sharp & Dohme | Therapeutic agents |
| EP1317450B1 (en) * | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CL2003002353A1 (es) * | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| WO2004052280A2 (en) * | 2002-12-10 | 2004-06-24 | Imclone Systems Incorporated | Anti-angiogenic compounds and their use in cancer treatment |
| WO2005013982A1 (en) * | 2003-08-06 | 2005-02-17 | Vertex Pharmaceuticals Incorporated | Aminotriazole compounds useful as inhibitors of protein kinases |
| WO2005097758A1 (en) * | 2004-03-26 | 2005-10-20 | Amphora Discovery Corporation | Certain triazole-based compounds, compositions, and uses thereof |
| EP2035396B1 (en) * | 2006-05-25 | 2014-05-14 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| DE102007022565A1 (de) * | 2007-05-14 | 2008-11-20 | Merck Patent Gmbh | Heterocyclische Indazolderivate |
| WO2009155156A1 (en) * | 2008-06-18 | 2009-12-23 | Merck & Co., Inc. | Inhibitors of janus kinases |
| ES2677356T3 (es) * | 2010-03-24 | 2018-08-01 | Amitech Therapeutics Solutions, Inc. | Compuestos heterocíclicos útiles para la inhibición de quinasas |
| US9061966B2 (en) | 2010-10-08 | 2015-06-23 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2013133367A1 (ja) * | 2012-03-09 | 2013-09-12 | カルナバイオサイエンス株式会社 | 新規トリアジン誘導体 |
| EP3055301B1 (en) | 2013-10-07 | 2019-11-20 | Kadmon Corporation, LLC | (2-(5-isoindolin-2-yl)pyrimidin-4-yl)-amine derivatives as rho kinase inhibitors for treating autoimmune diseases |
| WO2016138336A1 (en) | 2015-02-27 | 2016-09-01 | Purdue Research Foundation | Perimeter fill syringe |
| WO2017103611A1 (en) | 2015-12-16 | 2017-06-22 | Redx Pharma Plc | Compounds useful as kinase inhibitors |
| US10323023B2 (en) * | 2017-06-30 | 2019-06-18 | Beijing Tide Pharmaceutical Co., Ltd. | Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof |
| WO2019000682A1 (zh) | 2017-06-30 | 2019-01-03 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
| CN110582489B (zh) | 2017-06-30 | 2023-10-27 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
| GB201801226D0 (en) * | 2018-01-25 | 2018-03-14 | Redx Pharma Plc | Modulators of Rho-associated protein kinase |
| JP7490569B2 (ja) | 2018-04-24 | 2024-05-27 | トランスレイショナル・ドラッグ・ディベロップメント・エルエルシー | キナーゼ阻害剤としてのアミド化合物、組成物および処置方法 |
| US20240131029A1 (en) | 2021-02-04 | 2024-04-25 | President And Fellows Of Harvard College | Selective rock2 inhibition for treatment of edema and associated conditions |
| GB202200735D0 (en) | 2022-01-20 | 2022-03-09 | Redx Pharma Plc | Compounds |
-
2018
- 2018-01-25 GB GBGB1801226.0A patent/GB201801226D0/en not_active Ceased
-
2019
- 2019-01-25 CN CN201980010083.3A patent/CN111655681B/zh active Active
- 2019-01-25 LT LTEPPCT/GB2019/050215T patent/LT3743420T/lt unknown
- 2019-01-25 EP EP21214072.7A patent/EP4026834A1/en active Pending
- 2019-01-25 CA CA3088330A patent/CA3088330A1/en active Pending
- 2019-01-25 HR HRP20220269TT patent/HRP20220269T8/hr unknown
- 2019-01-25 SM SM20220099T patent/SMT202200099T1/it unknown
- 2019-01-25 MX MX2020007898A patent/MX2020007898A/es unknown
- 2019-01-25 EP EP19702694.1A patent/EP3743420B1/en active Active
- 2019-01-25 WO PCT/GB2019/050215 patent/WO2019145729A1/en not_active Ceased
- 2019-01-25 AU AU2019213214A patent/AU2019213214B2/en active Active
- 2019-01-25 JP JP2020561950A patent/JP7518324B2/ja active Active
- 2019-01-25 EA EA202091711A patent/EA202091711A1/ru unknown
- 2019-01-25 PT PT197026941T patent/PT3743420T/pt unknown
- 2019-01-25 PL PL19702694T patent/PL3743420T3/pl unknown
- 2019-01-25 KR KR1020207022578A patent/KR102737926B1/ko active Active
- 2019-01-25 SG SG11202006087UA patent/SG11202006087UA/en unknown
- 2019-01-25 ES ES19702694T patent/ES2907833T3/es active Active
- 2019-01-25 US US16/964,904 patent/US11497751B2/en active Active
- 2019-01-25 DK DK19702694.1T patent/DK3743420T3/da active
- 2019-01-25 HU HUE19702694A patent/HUE058940T2/hu unknown
- 2019-01-25 SI SI201930178T patent/SI3743420T1/sl unknown
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2020
- 2020-06-25 PH PH12020550986A patent/PH12020550986A1/en unknown
- 2020-06-30 ZA ZA2020/03983A patent/ZA202003983B/en unknown
- 2020-07-12 IL IL275988A patent/IL275988B2/en unknown
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2022
- 2022-02-16 CY CY20221100132T patent/CY1125017T1/el unknown
- 2022-08-26 US US17/896,626 patent/US11878020B2/en active Active
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2023
- 2023-11-28 JP JP2023200631A patent/JP2024026193A/ja active Pending
- 2023-12-08 US US18/534,285 patent/US12453734B2/en active Active
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2025
- 2025-10-02 US US19/348,406 patent/US20260034140A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006135383A2 (en) * | 2004-08-04 | 2006-12-21 | Myriad Genetics, Inc. | Indazoles |
| CN103429585A (zh) * | 2010-12-20 | 2013-12-04 | 默克雪兰诺股份有限公司 | 作为白细胞介素-1受体相关激酶抑制剂的吲唑基三唑衍生物 |
| WO2016138335A1 (en) * | 2015-02-27 | 2016-09-01 | Lycera Corporation | Indazolyl thiadiazolamines and related compounds for inhibition of rho-associated protein kinase and the treatment of disease |
Non-Patent Citations (1)
| Title |
|---|
| 李仁利.环内等价电子等排.《药物构效关系》.2003,第182页. * |
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