JP7163385B2 - ジアザスピロrock阻害剤 - Google Patents

ジアザスピロrock阻害剤 Download PDF

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Publication number
JP7163385B2
JP7163385B2 JP2020524791A JP2020524791A JP7163385B2 JP 7163385 B2 JP7163385 B2 JP 7163385B2 JP 2020524791 A JP2020524791 A JP 2020524791A JP 2020524791 A JP2020524791 A JP 2020524791A JP 7163385 B2 JP7163385 B2 JP 7163385B2
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substituted
alkyl
heterocyclyl
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cycloalkyl
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Japanese (ja)
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JP2021501782A (ja
JP2021501782A5 (https=
Inventor
イェヘン・ジュー
スニタ・ブイ・デブナニ
ウィリアム・アール・ユーイング
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2020524791A 2017-11-03 2018-11-01 ジアザスピロrock阻害剤 Active JP7163385B2 (ja)

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 (3)

Publication Number Publication Date
JP2021501782A JP2021501782A (ja) 2021-01-21
JP2021501782A5 JP2021501782A5 (https=) 2021-12-09
JP7163385B2 true JP7163385B2 (ja) 2022-10-31

Family

ID=64604702

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020524791A Active JP7163385B2 (ja) 2017-11-03 2018-11-01 ジアザスピロrock阻害剤

Country Status (7)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7113810B2 (ja) 2016-07-07 2022-08-05 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ラクタム
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
US11447487B2 (en) 2017-07-12 2022-09-20 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as rock inhibitors
JP7234201B2 (ja) 2017-07-12 2023-03-07 ブリストル-マイヤーズ スクイブ カンパニー 心不全の治療のためのrockの5員アミノヘテロ環および5,6-または6,6員二環式アミノヘテロ環の阻害剤
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
US11306081B2 (en) 2017-07-12 2022-04-19 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
EP3704121B1 (en) 2017-11-03 2022-12-21 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
WO2020086739A1 (en) * 2018-10-24 2020-04-30 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
EP4431596A4 (en) 2021-11-11 2026-01-14 The Doshisha CRYOCONSERVATION PREPARATION FOR CORNIAL ENDOTHELIAL CELLS AND PROCESS FOR PRODUCING SAID CRYOCONSERVATION PREPARATION
AU2023247609A1 (en) * 2022-03-31 2024-10-17 Bebetter Med Inc. 1,4-diheterocyclic substituted aromatic ring or aromatic heterocyclic compound and use thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
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
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012511012A (ja) 2008-12-05 2012-05-17 サノフイ H3モジュレーターとして使用される置換されたピペリジンスピロピロリジノン及びピペリジノン
JP2013526527A (ja) 2010-05-11 2013-06-24 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
JP2013526526A (ja) 2010-05-11 2013-06-24 サノフイ 置換n−ヘテロアリールスピロラクタムビピロリジン類、その製造及び治療的使用
WO2016112236A1 (en) 2015-01-09 2016-07-14 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
JP2019520398A (ja) 2016-07-07 2019-07-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのスピロラクタム
JP2019520396A (ja) 2016-07-07 2019-07-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのスピロ縮合環尿素

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6488239B2 (ja) 2013-01-18 2019-03-20 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのフタラジノンおよびイソキノリノン
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
US9914740B2 (en) 2013-07-02 2018-03-13 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
EP3016950B1 (en) 2013-07-02 2017-06-07 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
WO2016028971A1 (en) 2014-08-21 2016-02-25 Bristol-Myers Squibb Company Tied-back benzamide derivatives as potent rock inhibitors
ES2730112T3 (es) 2015-03-09 2019-11-08 Bristol Myers Squibb Co Lactamas como inhibidores de ROCK
TWI730032B (zh) 2016-01-13 2021-06-11 美商必治妥美雅史谷比公司 作為rock抑制劑之螺庚烷水楊酸醯胺及相關化合物
WO2017205709A1 (en) 2016-05-27 2017-11-30 Bristol-Myers Squibb Company Triazolones and tetrazolones as inhibitors of rock
JP6903731B2 (ja) 2016-07-07 2021-07-14 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 強力で選択的なrock阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
US11306081B2 (en) 2017-07-12 2022-04-19 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
JP7234201B2 (ja) 2017-07-12 2023-03-07 ブリストル-マイヤーズ スクイブ カンパニー 心不全の治療のためのrockの5員アミノヘテロ環および5,6-または6,6員二環式アミノヘテロ環の阻害剤
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
US11447487B2 (en) 2017-07-12 2022-09-20 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as rock inhibitors
EP3704121B1 (en) 2017-11-03 2022-12-21 Bristol-Myers Squibb Company Diazaspiro rock inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012511012A (ja) 2008-12-05 2012-05-17 サノフイ H3モジュレーターとして使用される置換されたピペリジンスピロピロリジノン及びピペリジノン
JP2013526527A (ja) 2010-05-11 2013-06-24 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
JP2013526526A (ja) 2010-05-11 2013-06-24 サノフイ 置換n−ヘテロアリールスピロラクタムビピロリジン類、その製造及び治療的使用
WO2016112236A1 (en) 2015-01-09 2016-07-14 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
JP2019520398A (ja) 2016-07-07 2019-07-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのスピロラクタム
JP2019520396A (ja) 2016-07-07 2019-07-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのスピロ縮合環尿素

Also Published As

Publication number Publication date
KR20200083543A (ko) 2020-07-08
WO2019089868A1 (en) 2019-05-09
CN111278825A (zh) 2020-06-12
CN111278825B (zh) 2023-05-02
EP3704121A1 (en) 2020-09-09
EP3704121B1 (en) 2022-12-21
ES2937039T3 (es) 2023-03-23
KR102716960B1 (ko) 2024-10-11
US11192891B2 (en) 2021-12-07
JP2021501782A (ja) 2021-01-21
US20210188848A1 (en) 2021-06-24

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