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

Info

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
Authority
JP
Japan
Prior art keywords
substituted
alkyl
heterocyclyl
chr
cycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2020524791A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021501782A5 (enExample
JP2021501782A (ja
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of JP2021501782A publication Critical patent/JP2021501782A/ja
Publication of JP2021501782A5 publication Critical patent/JP2021501782A5/ja
Application granted granted Critical
Publication of JP7163385B2 publication Critical patent/JP7163385B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (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 (enExample) 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 (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)

Families Citing this family (18)

* 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
ES2829400T3 (es) 2016-11-30 2021-05-31 Bristol Myers Squibb Co Inhibidores tricíclicos de Rho cinasa
EP3652164B1 (en) 2017-07-12 2023-06-21 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
ES2894128T3 (es) 2017-07-12 2022-02-11 Bristol Myers Squibb Co Inhibidores aminoheterocíclicos de cinco miembros y aminoheterocíclicos bicíclicos de 5,6 o 6,6 miembros de ROCK para el tratamiento de la insuficiencia cardíaca
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
WO2019014304A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company SPIROHEPTANYL HYDANTOIDS AS ROCK INHIBITORS
EP3704121B1 (en) 2017-11-03 2022-12-21 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
KR20210083286A (ko) * 2018-10-24 2021-07-06 아락세스 파마 엘엘씨 종양 전이를 억제하기 위한 g12c 돌연변이 kras 단백질의 억제제로서 2-(2-아크릴로일-2,6-디아자스피로[3.4]옥탄-6-일)-6-(1h-인다졸-4-일)-벤조니트릴 유도체 및 관련 화합물
EP4431596A1 (en) 2021-11-11 2024-09-18 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
CN116615417B (zh) * 2022-03-31 2024-05-14 广州必贝特医药股份有限公司 1,4-二杂环基取代芳环或芳杂环类化合物及其应用
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
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 (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
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
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
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
TW201443023A (zh) 2013-01-18 2014-11-16 必治妥美雅史谷比公司 作爲ｒｏｃｋ抑制劑之酞□酮及異喹啉酮
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 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
TW201506024A (zh) 2013-07-02 2015-02-16 必治妥美雅史谷比公司 作為有效ｒｏｃｋ抑制劑的三環甲醯胺衍生物
WO2015002926A1 (en) 2013-07-02 2015-01-08 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
JP6633618B2 (ja) 2014-08-21 2020-01-22 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ｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体
EP3268360B1 (en) 2015-03-09 2019-04-24 Bristol-Myers Squibb Company Lactams as inhibitors of rock
UY37073A (es) 2016-01-13 2017-07-31 Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock, y las composiciones que los contienen
US10562887B2 (en) 2016-05-27 2020-02-18 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
ES2829400T3 (es) 2016-11-30 2021-05-31 Bristol Myers Squibb Co Inhibidores tricíclicos de Rho cinasa
EP3652164B1 (en) 2017-07-12 2023-06-21 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
WO2019014304A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company SPIROHEPTANYL HYDANTOIDS AS ROCK INHIBITORS
ES2894128T3 (es) 2017-07-12 2022-02-11 Bristol Myers Squibb Co Inhibidores aminoheterocíclicos de cinco miembros y aminoheterocíclicos bicíclicos de 5,6 o 6,6 miembros de ROCK para el tratamiento de la insuficiencia cardíaca
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
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
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
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
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
ES2937039T3 (es) 2023-03-23
CN111278825B (zh) 2023-05-02
WO2019089868A1 (en) 2019-05-09
KR20200083543A (ko) 2020-07-08
EP3704121B1 (en) 2022-12-21
CN111278825A (zh) 2020-06-12
US11192891B2 (en) 2021-12-07
US20210188848A1 (en) 2021-06-24
KR102716960B1 (ko) 2024-10-11
EP3704121A1 (en) 2020-09-09
JP2021501782A (ja) 2021-01-21

Similar Documents

Publication Publication Date Title
JP7163385B2 (ja) ジアザスピロｒｏｃｋ阻害剤
JP7268116B2 (ja) Ｒｏｃｋ阻害剤としてのスピロヘプタンサリチルアミドおよび関連性化合物
JP7225317B2 (ja) 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
JP6721741B2 (ja) Ｒｏｃｋの阻害剤としてのスピロシクロヘプタン
JP6770053B2 (ja) Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン
US11673886B2 (en) 5-membered and bicyclic heterocyclic amides as inhibitors of ROCK
US11306081B2 (en) Phenylacetamides as inhibitors of rock
JP7155102B2 (ja) Ｒｏｃｋ阻害剤としてのスピロ縮合環尿素

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211027

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20211027

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220901

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20220920

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20221019

R150 Certificate of patent or registration of utility model

Ref document number: 7163385

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250