JP7383598B2 - Ｒｈｏ関連コイルドコイル含有プロテインキナーゼの阻害剤 - Google Patents

Ｒｈｏ関連コイルドコイル含有プロテインキナーゼの阻害剤 Download PDF

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JP7383598B2
JP7383598B2 JP2020502709A JP2020502709A JP7383598B2 JP 7383598 B2 JP7383598 B2 JP 7383598B2 JP 2020502709 A JP2020502709 A JP 2020502709A JP 2020502709 A JP2020502709 A JP 2020502709A JP 7383598 B2 JP7383598 B2 JP 7383598B2
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phenyl
pyrazol
acetamide
methoxyphenyl
amino
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JP2020527585A (ja
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スキューカス エデュアーダス
ジー．リウ ケビン
キム チ－イン
ブイ．ポユロフスキー マシャ
モ リゲン
チャン チンヤー
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カドモン コーポレイション，リミティド ライアビリティ カンパニー
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    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • 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)
JP2020502709A 2017-07-21 2018-07-23 Ｒｈｏ関連コイルドコイル含有プロテインキナーゼの阻害剤 Active JP7383598B2 (ja)

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JP2023101681A JP7778745B2 (ja) 2017-07-21 2023-06-21 Ｒｈｏ関連コイルドコイル含有プロテインキナーゼの阻害剤

Applications Claiming Priority (3)

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US201762535611P 2017-07-21 2017-07-21
US62/535,611 2017-07-21
PCT/US2018/043335 WO2019018855A1 (en) 2017-07-21 2018-07-23 ALPHA PROPELLER PROTEIN KINASE INHIBITORS ("COILED-COIL") ASSOCIATED WITH RHO

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JP2020527585A JP2020527585A (ja) 2020-09-10
JP7383598B2 true JP7383598B2 (ja) 2023-11-20

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JP2023101681A Active JP7778745B2 (ja) 2017-07-21 2023-06-21 Ｒｈｏ関連コイルドコイル含有プロテインキナーゼの阻害剤

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US (1) US11479533B2 (enExample)
EP (1) EP3654970A4 (enExample)
JP (2) JP7383598B2 (enExample)
CN (1) CN111050766A (enExample)
CA (1) CA3070115A1 (enExample)
EA (1) EA202090306A1 (enExample)
WO (1) WO2019018855A1 (enExample)

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HRP20241225T1 (hr) * 2018-02-16 2024-12-06 Constellation Pharmaceuticals, Inc. Inhibitori p300/cbp hat
EP3845276B1 (en) * 2019-12-31 2025-01-29 Industrial Technology Research Institute Beta-amino acid derivative, kinase inhibitor and pharmaceutical composition containing the same, and use of the same
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
US20240423998A1 (en) * 2021-11-29 2024-12-26 Woolsey Pharmaceuticals, Inc. Methods of treating agitation and other dementia-associated behavioral symptoms
JPWO2024075838A1 (enExample) * 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 (8)

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Publication number Priority date Publication date Assignee Title
JP2005524631A (ja) 2002-01-25 2005-08-18 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なインダゾール化合物
JP2006503851A (ja) 2002-09-25 2006-02-02 メモリー・ファーマシューティカルズ・コーポレイション インダゾール、ベンゾチアゾール、及びベンゾイソチアゾール、並びにそれらの調製及び使用
JP2009506979A (ja) 2005-09-02 2009-02-19 アステラス製薬株式会社 新規化合物
JP2011507850A (ja) 2007-12-21 2011-03-10 ザ スクリプス リサーチ インスティチュート Ｒｈｏキナーゼインヒビターとしてのアニリドおよびアナログ
WO2015070170A1 (en) 2013-11-08 2015-05-14 The Translational Genomics Research Institute Compounds for cognitive enhancement and methods of use thereof
WO2016022312A1 (en) 2014-08-05 2016-02-11 Bristol-Myers Squibb Company Heterocyclic kinase inhibitors
JP2016510033A (ja) 2013-02-28 2016-04-04 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体
JP2016523963A (ja) 2013-07-08 2016-08-12 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリールアミドキナーゼ阻害剤

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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
CA3070112A1 (en) * 2017-07-21 2019-01-24 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 (8)

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Publication number Priority date Publication date Assignee Title
JP2005524631A (ja) 2002-01-25 2005-08-18 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なインダゾール化合物
JP2006503851A (ja) 2002-09-25 2006-02-02 メモリー・ファーマシューティカルズ・コーポレイション インダゾール、ベンゾチアゾール、及びベンゾイソチアゾール、並びにそれらの調製及び使用
JP2009506979A (ja) 2005-09-02 2009-02-19 アステラス製薬株式会社 新規化合物
JP2011507850A (ja) 2007-12-21 2011-03-10 ザ スクリプス リサーチ インスティチュート Ｒｈｏキナーゼインヒビターとしてのアニリドおよびアナログ
JP2016510033A (ja) 2013-02-28 2016-04-04 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体
JP2016523963A (ja) 2013-07-08 2016-08-12 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリールアミドキナーゼ阻害剤
WO2015070170A1 (en) 2013-11-08 2015-05-14 The Translational Genomics Research Institute Compounds for cognitive enhancement and methods of use thereof
WO2016022312A1 (en) 2014-08-05 2016-02-11 Bristol-Myers Squibb Company Heterocyclic kinase inhibitors

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J. Med. Chem.，2010年，53(15)，5727-5737

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Publication number Publication date
CA3070115A1 (en) 2019-01-24
EP3654970A4 (en) 2021-03-17
EA202090306A1 (ru) 2020-06-25
JP2020527585A (ja) 2020-09-10
US20200165206A1 (en) 2020-05-28
WO2019018855A1 (en) 2019-01-24
JP2023126245A (ja) 2023-09-07
EP3654970A1 (en) 2020-05-27
CN111050766A (zh) 2020-04-21
US11479533B2 (en) 2022-10-25
JP7778745B2 (ja) 2025-12-02

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