CN111050766A - Rho相关含卷曲螺旋蛋白激酶的抑制剂 - Google Patents

Rho相关含卷曲螺旋蛋白激酶的抑制剂 Download PDF

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CN111050766A
CN111050766A CN201880049759.5A CN201880049759A CN111050766A CN 111050766 A CN111050766 A CN 111050766A CN 201880049759 A CN201880049759 A CN 201880049759A CN 111050766 A CN111050766 A CN 111050766A
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lower alkyl
group
cycloalkyl
independently selected
alkyl
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Chinese (zh)
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E.斯库卡斯
K.G.刘
J-I.金
M.V.波于洛夫斯基
R.莫
J.张
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Kadmon Corp LLC
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Kadmon Corp LLC
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    • 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
    • C07D403/10—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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
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    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D231/14—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • 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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
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  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880049759.5A 2017-07-21 2018-07-23 Rho相关含卷曲螺旋蛋白激酶的抑制剂 Pending CN111050766A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762535611P 2017-07-21 2017-07-21
US62/535611 2017-07-21
PCT/US2018/043335 WO2019018855A1 (en) 2017-07-21 2018-07-23 ALPHA PROPELLER PROTEIN KINASE INHIBITORS ("COILED-COIL") ASSOCIATED WITH RHO

Publications (1)

Publication Number Publication Date
CN111050766A true CN111050766A (zh) 2020-04-21

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CN201880049759.5A Pending CN111050766A (zh) 2017-07-21 2018-07-23 Rho相关含卷曲螺旋蛋白激酶的抑制剂

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Country Link
US (1) US11479533B2 (https=)
EP (1) EP3654970A4 (https=)
JP (3) JP7383598B2 (https=)
CN (1) CN111050766A (https=)
CA (1) CA3070115A1 (https=)
EA (1) EA202090306A1 (https=)
WO (1) WO2019018855A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111707832A (zh) * 2020-07-16 2020-09-25 首都医科大学附属北京朝阳医院 Rock激酶活性在辅助诊断肾损害中的应用
CN111707830A (zh) * 2020-07-16 2020-09-25 首都医科大学附属北京朝阳医院 Rock激酶活性在辅助诊断肺损害中的应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019161162A1 (en) * 2018-02-16 2019-08-22 Constellation Pharmaceuticals, Inc. P300/cbp hat inhibitors
JP7531379B2 (ja) * 2019-12-31 2024-08-09 財團法人工業技術研究院 βアミノ酸誘導体、これを含むキナーゼ阻害剤および医薬組成物ならびにその使用
US20240423998A1 (en) * 2021-11-29 2024-12-26 Woolsey Pharmaceuticals, Inc. Methods of treating agitation and other dementia-associated behavioral symptoms
JPWO2024075838A1 (https=) * 2022-10-07 2024-04-11
WO2025017500A1 (en) * 2023-07-17 2025-01-23 Graviton Bioscience Bv Formulations of rock2 inhibitors for cns disorders

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101253152A (zh) * 2005-09-02 2008-08-27 安斯泰来制药株式会社 作为rock抑制剂的酰胺衍生物
WO2009079009A1 (en) * 2007-12-19 2009-06-25 Yangbo Feng Anilides and analogs as rho kinase inhibitors
WO2015070170A1 (en) * 2013-11-08 2015-05-14 The Translational Genomics Research Institute Compounds for cognitive enhancement and methods of use thereof
CN105102448A (zh) * 2013-02-28 2015-11-25 百时美施贵宝公司 作为强效rock1和rock2抑制剂的苯基吡唑衍生物
CN105517993A (zh) * 2013-07-08 2016-04-20 百时美施贵宝公司 芳基酰胺激酶抑制剂

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WO2003053941A2 (en) 2001-12-20 2003-07-03 Bristol-Myers Squibb Company Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
MXPA05003317A (es) 2002-09-25 2005-07-05 Memory Pharm Corp Indazoles, benzotiazoles y benzoisotiazoles asi como preparacion y usos de los mismos.
JP2017523214A (ja) 2014-08-05 2017-08-17 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロ環キナーゼ阻害剤
US11926596B2 (en) * 2017-07-21 2024-03-12 Kadmon Corporation, Llc Inhibitors of Rho associated coiled-coil containing protein kinase
EP3675861A4 (en) * 2017-09-01 2021-01-06 Kadmon Corporation, LLC ALPHA SUPERWINDING PROTEIN KINASE INHIBITORS ("COILED-COIL") ASSOCIATED WITH RHO

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101253152A (zh) * 2005-09-02 2008-08-27 安斯泰来制药株式会社 作为rock抑制剂的酰胺衍生物
WO2009079009A1 (en) * 2007-12-19 2009-06-25 Yangbo Feng Anilides and analogs as rho kinase inhibitors
CN105102448A (zh) * 2013-02-28 2015-11-25 百时美施贵宝公司 作为强效rock1和rock2抑制剂的苯基吡唑衍生物
CN105517993A (zh) * 2013-07-08 2016-04-20 百时美施贵宝公司 芳基酰胺激酶抑制剂
WO2015070170A1 (en) * 2013-11-08 2015-05-14 The Translational Genomics Research Institute Compounds for cognitive enhancement and methods of use thereof

Non-Patent Citations (2)

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Title
XINGANG FANG等: "Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors", 《J. MED. CHEM.》 *
贾娴主编: "《药物化学课堂笔记》", 31 January 2011, 人民军医出版社 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111707832A (zh) * 2020-07-16 2020-09-25 首都医科大学附属北京朝阳医院 Rock激酶活性在辅助诊断肾损害中的应用
CN111707830A (zh) * 2020-07-16 2020-09-25 首都医科大学附属北京朝阳医院 Rock激酶活性在辅助诊断肺损害中的应用
CN111707830B (zh) * 2020-07-16 2023-08-15 首都医科大学附属北京朝阳医院 Rock激酶活性在辅助诊断肺损害中的应用
CN111707832B (zh) * 2020-07-16 2023-08-15 首都医科大学附属北京朝阳医院 Rock激酶活性在辅助诊断肾损害中的应用

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CA3070115A1 (en) 2019-01-24
WO2019018855A1 (en) 2019-01-24
EA202090306A1 (ru) 2020-06-25
JP7383598B2 (ja) 2023-11-20
US11479533B2 (en) 2022-10-25
JP2023126245A (ja) 2023-09-07
JP2020527585A (ja) 2020-09-10
JP7778745B2 (ja) 2025-12-02
EP3654970A4 (en) 2021-03-17
JP2026020169A (ja) 2026-02-06
EP3654970A1 (en) 2020-05-27
US20200165206A1 (en) 2020-05-28

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