CN111278825B - 二氮杂螺rock抑制剂 - Google Patents

二氮杂螺rock抑制剂 Download PDF

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Publication number
CN111278825B
CN111278825B CN201880069865.XA CN201880069865A CN111278825B CN 111278825 B CN111278825 B CN 111278825B CN 201880069865 A CN201880069865 A CN 201880069865A CN 111278825 B CN111278825 B CN 111278825B
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CN111278825A (zh
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朱晔恒
S·V·德瓦尼
W·R·尤因
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/10—Spiro-condensed 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
    • A61K31/435—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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201880069865.XA 2017-11-03 2018-11-01 二氮杂螺rock抑制剂 Active CN111278825B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762581116P 2017-11-03 2017-11-03
US62/581,116 2017-11-03
PCT/US2018/058611 WO2019089868A1 (en) 2017-11-03 2018-11-01 Diazaspiro rock inhibitors

Publications (2)

Publication Number Publication Date
CN111278825A CN111278825A (zh) 2020-06-12
CN111278825B true CN111278825B (zh) 2023-05-02

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880069865.XA Active CN111278825B (zh) 2017-11-03 2018-11-01 二氮杂螺rock抑制剂

Country Status (7)

Country Link
US (1) US11192891B2 (enExample)
EP (1) EP3704121B1 (enExample)
JP (1) JP7163385B2 (enExample)
KR (1) KR102716960B1 (enExample)
CN (1) CN111278825B (enExample)
ES (1) ES2937039T3 (enExample)
WO (1) WO2019089868A1 (enExample)

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WO2018009625A1 (en) 2016-07-07 2018-01-11 Bristol-Myers Squibb Company Spirolactams as inhibitors of rock
ES2829400T3 (es) 2016-11-30 2021-05-31 Bristol Myers Squibb Co Inhibidores tricíclicos de Rho cinasa
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
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
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
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
CN111278825B (zh) 2017-11-03 2023-05-02 百时美施贵宝公司 二氮杂螺rock抑制剂
EP3870585A1 (en) * 2018-10-24 2021-09-01 Araxes Pharma LLC 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis
US20250000083A1 (en) 2021-11-11 2025-01-02 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
JP2025511097A (ja) * 2022-03-31 2025-04-15 廣州必貝特醫藥股▲ふん▼有限公司 １，４－ジヘテロシクリル置換芳香環若しくは芳香族複素環系化合物及びその使用
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
CN120271573A (zh) * 2024-04-08 2025-07-08 北京双鹤润创科技有限公司 杂环芳基或杂芳基-杂芳基衍生物及其用途
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (1)

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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

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AR074466A1 (es) * 2008-12-05 2011-01-19 Sanofi Aventis Piperidina espiro pirrolidinona y piperidinona sustituidas y su uso terapeutico en enfermedades mediadas por la modulacion de los receptores h3.
TW201202251A (en) * 2010-05-11 2012-01-16 Sanofi Aventis Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
JP5968307B2 (ja) * 2010-05-11 2016-08-10 サノフイ 置換フェニルシクロアルキルピロリジン（ピペリジン）スピロラクタム類及びアミド類、それらの製造及び治療的使用
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
CN105518005B (zh) 2013-07-02 2018-07-20 百时美施贵宝公司 作为rock抑制剂的三环吡啶-甲酰胺衍生物
CN105492444B (zh) 2013-07-02 2018-09-07 百时美施贵宝公司 作为rock抑制剂的三环吡啶-甲酰胺衍生物
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
CN107108581B (zh) 2014-08-21 2020-06-23 百时美施贵宝公司 作为强效rock抑制剂的回接苯甲酰胺衍生物
US10112929B2 (en) 2015-03-09 2018-10-30 Bristol-Myers Squibb Company Lactams as inhibitors of rock
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
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
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
WO2018009625A1 (en) * 2016-07-07 2018-01-11 Bristol-Myers Squibb Company Spirolactams as inhibitors of rock
ES2829400T3 (es) 2016-11-30 2021-05-31 Bristol Myers Squibb Co Inhibidores tricíclicos de Rho cinasa
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
WO2019014300A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company PHENYLACETAMIDES 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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
KR102716960B1 (ko) 2024-10-11
KR20200083543A (ko) 2020-07-08
ES2937039T3 (es) 2023-03-23
EP3704121B1 (en) 2022-12-21
EP3704121A1 (en) 2020-09-09
JP7163385B2 (ja) 2022-10-31
WO2019089868A1 (en) 2019-05-09
US20210188848A1 (en) 2021-06-24
JP2021501782A (ja) 2021-01-21
CN111278825A (zh) 2020-06-12
US11192891B2 (en) 2021-12-07

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