CN107108581B - 作为强效rock抑制剂的回接苯甲酰胺衍生物 - Google Patents
作为强效rock抑制剂的回接苯甲酰胺衍生物 Download PDFInfo
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- CN107108581B CN107108581B CN201580044710.7A CN201580044710A CN107108581B CN 107108581 B CN107108581 B CN 107108581B CN 201580044710 A CN201580044710 A CN 201580044710A CN 107108581 B CN107108581 B CN 107108581B
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P27/00—Drugs for disorders of the senses
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A61P37/00—Drugs for immunological or allergic disorders
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/08—Vasodilators for multiple indications
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- A—HUMAN NECESSITIES
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D401/02—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 two hetero rings
- C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
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- 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
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- 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
- C07D403/10—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 carbon chain containing aromatic rings
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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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- 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
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- 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
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- 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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- C07—ORGANIC CHEMISTRY
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Gynecology & Obstetrics (AREA)
- Pain & Pain Management (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462040044P | 2014-08-21 | 2014-08-21 | |
| US62/040044 | 2014-08-21 | ||
| PCT/US2015/046032 WO2016028971A1 (en) | 2014-08-21 | 2015-08-20 | Tied-back benzamide derivatives as potent rock inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107108581A CN107108581A (zh) | 2017-08-29 |
| CN107108581B true CN107108581B (zh) | 2020-06-23 |
Family
ID=54011128
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580044710.7A Active CN107108581B (zh) | 2014-08-21 | 2015-08-20 | 作为强效rock抑制剂的回接苯甲酰胺衍生物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10112939B2 (OSRAM) |
| EP (1) | EP3183248B1 (OSRAM) |
| JP (1) | JP6633618B2 (OSRAM) |
| CN (1) | CN107108581B (OSRAM) |
| ES (1) | ES2838573T3 (OSRAM) |
| WO (1) | WO2016028971A1 (OSRAM) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016112236A1 (en) | 2015-01-09 | 2016-07-14 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| US10112929B2 (en) | 2015-03-09 | 2018-10-30 | Bristol-Myers Squibb Company | Lactams as inhibitors of rock |
| CN106924254A (zh) * | 2015-12-31 | 2017-07-07 | 中国医学科学院药物研究所 | 黄连碱在制备预防和/或治疗系统性红斑狼疮及其并发症药物中的应用 |
| AR107354A1 (es) | 2016-01-13 | 2018-04-18 | Bristol Myers Squibb Co | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock |
| WO2017205709A1 (en) | 2016-05-27 | 2017-11-30 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of rock |
| WO2018009625A1 (en) | 2016-07-07 | 2018-01-11 | Bristol-Myers Squibb Company | Spirolactams as inhibitors of rock |
| JP7155102B2 (ja) | 2016-07-07 | 2022-10-18 | ブリストル-マイヤーズ スクイブ カンパニー | Rock阻害剤としてのスピロ縮合環尿素 |
| CN110049977B (zh) | 2016-07-07 | 2022-01-18 | 百时美施贵宝公司 | 作为强效和选择性rock抑制剂的内酰胺、环状脲和氨基甲酸酯及三唑酮衍生物 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| CN108203433B (zh) * | 2016-12-16 | 2020-07-03 | 成都先导药物开发股份有限公司 | 一种rock抑制剂及其应用 |
| CA3063616A1 (en) * | 2017-06-30 | 2019-12-06 | Beijing Tide Pharmaceutical Co., Ltd. | Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof |
| TW201908293A (zh) | 2017-07-12 | 2019-03-01 | 美商必治妥美雅史谷比公司 | 作為rock抑制劑之5員及雙環雜環醯胺 |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
| KR102680160B1 (ko) | 2017-07-12 | 2024-06-28 | 브리스톨-마이어스 스큅 컴퍼니 | 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제 |
| WO2019014300A1 (en) | 2017-07-12 | 2019-01-17 | Bristol-Myers Squibb Company | PHENYLACETAMIDES AS ROCK INHIBITORS |
| CN110914257B (zh) | 2017-07-12 | 2023-05-26 | 百时美施贵宝公司 | 作为rock抑制剂的螺庚基乙内酰脲 |
| CN111278825B (zh) | 2017-11-03 | 2023-05-02 | 百时美施贵宝公司 | 二氮杂螺rock抑制剂 |
| EP3782987B1 (en) | 2018-04-18 | 2025-04-02 | Medshine Discovery Inc. | Benzopyrazole compound used as rho kinase inhibitor |
| CN114555561B (zh) * | 2019-10-18 | 2023-08-11 | 南京明德新药研发有限公司 | 作为rho激酶抑制剂的苯并吡唑类化合物的盐型、晶型及其制备方法 |
| CN114262322A (zh) * | 2020-09-16 | 2022-04-01 | 中国科学院上海有机化学研究所 | 一类细胞程序性坏死抑制剂及其制备方法和用途 |
| WO2022100614A1 (zh) * | 2020-11-11 | 2022-05-19 | 南京明德新药研发有限公司 | 苯并脲环衍生物及其制备方法和应用 |
| US20250000083A1 (en) | 2021-11-11 | 2025-01-02 | The Doshisha | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010080357A1 (en) * | 2008-12-18 | 2010-07-15 | Boehringer Ingelheim International Gmbh | Serotonin 5-ht2b receptor inhibitors |
| WO2011073376A1 (en) * | 2009-12-18 | 2011-06-23 | Euroscreen S.A. | Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disordersas as agonists of g- protein coupled receptor 43 (gpr43) |
Family Cites Families (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0259559A (ja) | 1988-08-23 | 1990-02-28 | Mitsubishi Kasei Corp | ピリドン誘導体又はその塩類 |
| GB9119932D0 (en) * | 1991-09-18 | 1991-10-30 | Glaxo Group Ltd | Chemical compounds |
| US5696122A (en) * | 1993-09-03 | 1997-12-09 | Smithkline Beecham P.L.C. | Indole and indoline derivatives as 5HT1D receptor antagonists |
| JPH09503773A (ja) | 1993-10-19 | 1997-04-15 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | 5ht−1dレセプター拮抗剤用のベンズアニリド誘導体 |
| CA2338697A1 (en) * | 1998-07-28 | 2000-02-10 | Smithkline Beecham Corporation | Compounds and methods |
| CA2340100A1 (en) | 1998-08-11 | 2000-02-24 | Daiichi Pharmaceutical Co., Ltd. | Novel sulfonyl derivatives |
| ES2244437T3 (es) | 1999-05-04 | 2005-12-16 | Schering Corporation | Derivados de piperazina utiles como antagonistas de ccr5. |
| HUP0300850A2 (hu) | 2000-03-17 | 2003-07-28 | Bristol-Myers Squibb Pharma Company | Gyűrűs béta-aminosav-származékok mint mátrix metalloproteázok és a TNF-alfa inhibitorok és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk |
| GB2361003A (en) | 2000-04-07 | 2001-10-10 | Astrazeneca Ab | Novel compounds |
| US20020045613A1 (en) | 2000-04-27 | 2002-04-18 | Heinz Pauls | 1-aroyl-piperidinyl benzamidines |
| TWI243164B (en) * | 2001-02-13 | 2005-11-11 | Aventis Pharma Gmbh | Acylated indanyl amines and their use as pharmaceuticals |
| CN1596253A (zh) | 2001-10-01 | 2005-03-16 | 布里斯托尔-迈尔斯斯奎布公司 | 用作抗炎药的螺-乙内酰脲化合物 |
| ES2316777T3 (es) * | 2002-02-15 | 2009-04-16 | Glaxo Group Limited | Moduladores de receptores vainilloides. |
| TWI319387B (en) * | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| US7541477B2 (en) * | 2002-07-30 | 2009-06-02 | Banyu Pharmaceutical Co., Ltd. | Antagonists to melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient |
| CA2509711A1 (en) | 2002-12-13 | 2004-07-01 | Smithkline Beecham Corporation | Piperidine derivatives as ccr5 antagonists |
| EP1575918A2 (en) * | 2002-12-19 | 2005-09-21 | Neurogen Corporation | Substituted biaryl-4-carboxylic acid arylamide analogues as capsaicin receptor modulators |
| DE10306250A1 (de) * | 2003-02-14 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO2004076412A2 (en) | 2003-02-26 | 2004-09-10 | Sugen, Inc. | Aminoheteroaryl compounds as protein kinase inhibitors |
| US7432375B2 (en) | 2003-03-06 | 2008-10-07 | Eisai R & D Management Co., Ltd. | JNK inhibitors |
| EP1713775A4 (en) * | 2004-01-30 | 2009-08-12 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
| ATE454372T1 (de) * | 2004-04-01 | 2010-01-15 | Lilly Co Eli | Am histamin-h3-rezeptor wirksame mittel, herstellung und therapeutische anwendungen |
| PL1882684T3 (pl) | 2005-05-19 | 2015-08-31 | Astellas Pharma Inc | Pochodna pirolidyny albo jej sól |
| US8921376B2 (en) | 2005-05-20 | 2014-12-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| WO2007002559A1 (en) | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Pyrazole based lxr modulators |
| GB0514812D0 (en) | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| WO2007084667A2 (en) * | 2006-01-19 | 2007-07-26 | Osi Pharmaceutical, Inc. | Fused heterobicyclic kinase inhibitors |
| TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
| US7601716B2 (en) | 2006-05-01 | 2009-10-13 | Cephalon, Inc. | Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors |
| TWI386405B (zh) | 2006-09-05 | 2013-02-21 | 咪唑衍生物 | |
| ES2729424T3 (es) | 2006-09-20 | 2019-11-04 | Aerie Pharmaceuticals Inc | Inhibidores de Rho cinasa |
| CL2007003874A1 (es) | 2007-01-03 | 2008-05-16 | Boehringer Ingelheim Int | Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio |
| JP2010525062A (ja) | 2007-04-25 | 2010-07-22 | エグゼリクシス, インコーポレイテッド | Pimモジュレーターとしてのピリミジノン類 |
| JP2010535733A (ja) | 2007-08-07 | 2010-11-25 | エフ.ホフマン−ラ ロシュ アーゲー | Nk3受容体アンタゴニストとしてのピロリジンアリールエーテル |
| ES2453950T3 (es) * | 2007-08-27 | 2014-04-09 | AbbVie Deutschland GmbH & Co. KG | 4-(4-Piridinil)-benzamidas y su uso como moduladores de la actividad de ROCK |
| JP2011518109A (ja) | 2007-11-30 | 2011-06-23 | ビオタ サイエンティフィック マネージメント ピーティーワイ リミテッド | 抗菌剤としてのテトラヒドロ−イソキノリンppat阻害剤 |
| AR069526A1 (es) * | 2007-12-03 | 2010-01-27 | Takeda Pharmaceutical | Compuesto heterociclico que contiene nitrogeno y su uso |
| WO2009153179A1 (en) | 2008-06-16 | 2009-12-23 | F. Hoffmann-La Roche Ag | Pyrrolidine derivatives as nk2 receptor antagonists |
| EP2321274A1 (en) | 2008-07-08 | 2011-05-18 | Boehringer Ingelheim International GmbH | Pyrrolidinyl and piperidinyl compounds useful as nhe-1 inhibitors |
| EP2318403B1 (en) | 2008-08-25 | 2015-12-23 | Boehringer Ingelheim International GmbH | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| WO2010040663A1 (en) | 2008-10-09 | 2010-04-15 | F. Hoffmann-La Roche Ag | Pyrrolidine n-benzyl derivatives |
| US8367679B2 (en) | 2008-12-09 | 2013-02-05 | Merck Sharp & Dohme Corp. | Biaryl carboxamides |
| AU2010209825A1 (en) | 2009-01-30 | 2011-08-11 | F. Hoffmann-La Roche Ag | Piperidine derivatives as NK3 receptor antagonists |
| US8324250B2 (en) | 2009-03-19 | 2012-12-04 | Hoffmann-La Roche Inc. | Piperidine derivatives as NK3 receptor antagonists |
| AR076332A1 (es) | 2009-04-21 | 2011-06-01 | Boehringer Ingelheim Int | Derivados heterociclicos de 5-alquinil-piridinas, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento y/o prevencion del cancer, procesos inflamatorios, autoinmunes, y/o infecciones. |
| US9206173B2 (en) * | 2009-05-28 | 2015-12-08 | Otsuka Pharmaceutical Co., Ltd. | Heterocyclic compounds for the treatment of stress-related conditions |
| TW201103904A (en) * | 2009-06-11 | 2011-02-01 | Hoffmann La Roche | Janus kinase inhibitor compounds and methods |
| WO2011047319A2 (en) | 2009-10-16 | 2011-04-21 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compounds and methods of making and using the same |
| US8633183B2 (en) | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US9079880B2 (en) | 2010-07-07 | 2015-07-14 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| US8507535B2 (en) | 2010-07-07 | 2013-08-13 | Hoffmann-La Roche Inc. | Methyl-pyrrolidine ether derivatives |
| PE20140913A1 (es) | 2010-11-15 | 2014-08-22 | Abbvie Inc | Inhibidores de nampt y rock |
| JP6111195B2 (ja) * | 2011-08-09 | 2017-04-05 | 武田薬品工業株式会社 | シクロプロパンアミン化合物 |
| CA2873701A1 (en) | 2012-04-12 | 2013-10-17 | Auckland Uniservices Limited | Substituted benzamides and their uses |
| WO2013153539A1 (en) * | 2012-04-13 | 2013-10-17 | Glenmark Pharmaceuticals S.A. | Tricyclic compounds as tec kinase inhibitors |
| JP6272846B2 (ja) | 2012-06-27 | 2018-01-31 | 4エスツェー ディスカバリー ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌、自己免疫性炎症及びcns疾患の処置のためのビフルオロジオキサラン−アミノ−ベンゾイミダゾールキナーゼ阻害剤 |
| BR112015000106B1 (pt) * | 2012-07-03 | 2022-02-22 | Sagimet Biosciences Inc | Moduladores heterocíclicos de síntese de lipídio, composição farmacêutica e uso dos referidos moduladores |
| EP2687528A1 (en) * | 2012-07-17 | 2014-01-22 | Ares Trading S.A. | Fused triazole derivatives as gamma secretase modulators |
| CN103664878A (zh) | 2012-09-12 | 2014-03-26 | 山东亨利医药科技有限责任公司 | 杂芳环及其衍生物类酪氨酸激酶抑制剂 |
| CA2926478C (en) | 2012-10-05 | 2022-05-24 | Kadmon Corporation, Llc | Rho kinase inhibitors |
| TR201807740T4 (tr) * | 2012-12-07 | 2018-06-21 | Vertex Pharma | ATR kinaz inhibitörü olarak 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid. |
| US9926282B2 (en) | 2013-01-18 | 2018-03-27 | Bristol-Myers Squibb Company | Phthalazinones and isoquinolinones as rock inhibitors |
| TW201444798A (zh) | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物 |
| US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
-
2015
- 2015-08-20 CN CN201580044710.7A patent/CN107108581B/zh active Active
- 2015-08-20 ES ES15756322T patent/ES2838573T3/es active Active
- 2015-08-20 EP EP15756322.2A patent/EP3183248B1/en active Active
- 2015-08-20 US US15/503,419 patent/US10112939B2/en active Active
- 2015-08-20 WO PCT/US2015/046032 patent/WO2016028971A1/en not_active Ceased
- 2015-08-20 JP JP2017510314A patent/JP6633618B2/ja active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010080357A1 (en) * | 2008-12-18 | 2010-07-15 | Boehringer Ingelheim International Gmbh | Serotonin 5-ht2b receptor inhibitors |
| WO2011073376A1 (en) * | 2009-12-18 | 2011-06-23 | Euroscreen S.A. | Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disordersas as agonists of g- protein coupled receptor 43 (gpr43) |
Non-Patent Citations (1)
| Title |
|---|
| REGISTRY[Online];Columbus,Ohio,US;《REGISTRY》;20120130;1354720-58-3,1354719-49-5 * |
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| JP6633618B2 (ja) | 2020-01-22 |
| US20170226105A1 (en) | 2017-08-10 |
| EP3183248A1 (en) | 2017-06-28 |
| ES2838573T3 (es) | 2021-07-02 |
| CN107108581A (zh) | 2017-08-29 |
| EP3183248B1 (en) | 2020-11-11 |
| WO2016028971A1 (en) | 2016-02-25 |
| JP2017524026A (ja) | 2017-08-24 |
| US10112939B2 (en) | 2018-10-30 |
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