JP7155102B2 - Rock阻害剤としてのスピロ縮合環尿素 - Google Patents

Rock阻害剤としてのスピロ縮合環尿素 Download PDF

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Publication number
JP7155102B2
JP7155102B2 JP2019500372A JP2019500372A JP7155102B2 JP 7155102 B2 JP7155102 B2 JP 7155102B2 JP 2019500372 A JP2019500372 A JP 2019500372A JP 2019500372 A JP2019500372 A JP 2019500372A JP 7155102 B2 JP7155102 B2 JP 7155102B2
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pyrazol
substituted
triazaspiro
decan
methoxybenzyl
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JP2019520396A (ja
JP2019520396A5 (enExample
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ラジーブ・エス・ビデ
マンダル・シュリクリシュナ・ボダス
プラビン・スダカール・シルデ
シャラナバサッパ・パティル
タルン・クマール・マイシャル
カマルラジ・ティヤガラジャン
クマレサン・チナコティ
ピーター・ダブリュー・グランツ
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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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2019500372A 2016-07-07 2017-07-06 Rock阻害剤としてのスピロ縮合環尿素 Active JP7155102B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662359363P 2016-07-07 2016-07-07
US62/359,363 2016-07-07
PCT/US2017/040852 WO2018009627A1 (en) 2016-07-07 2017-07-06 Spiro-fused cyclic ureas as inhibitors of rock

Publications (3)

Publication Number Publication Date
JP2019520396A JP2019520396A (ja) 2019-07-18
JP2019520396A5 JP2019520396A5 (enExample) 2020-08-13
JP7155102B2 true JP7155102B2 (ja) 2022-10-18

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JP2019500372A Active JP7155102B2 (ja) 2016-07-07 2017-07-06 Rock阻害剤としてのスピロ縮合環尿素

Country Status (7)

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US (1) US10787450B2 (enExample)
EP (1) EP3481828B1 (enExample)
JP (1) JP7155102B2 (enExample)
KR (1) KR102449652B1 (enExample)
CN (1) CN109661396B (enExample)
ES (1) ES2829550T3 (enExample)
WO (1) WO2018009627A1 (enExample)

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AR107354A1 (es) 2016-01-13 2018-04-18 Bristol Myers Squibb Co Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock
JP6987792B2 (ja) 2016-05-27 2022-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのトリアゾロンおよびテトラゾロン
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de ROCK
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de 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
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
EP3634412A1 (en) * 2017-06-09 2020-04-15 Bristol-Myers Squibb Company Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
JP7206253B2 (ja) 2017-07-12 2023-01-17 ブリストル-マイヤーズ スクイブ カンパニー Rock阻害剤としてのフェニルアセトアミド
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
JP7313331B2 (ja) 2017-07-12 2023-07-24 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ヘプタニルヒダントイン
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
WO2019089868A1 (en) * 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
AU2019377087B2 (en) 2018-11-06 2025-03-06 Cervello Therapeutics, Llc Rock kinase inhibitors
US11248004B2 (en) 2018-11-06 2022-02-15 Cervello Therapeutics, Llc. Substituted isoquinolines as rock kinase inhibitors
WO2023085369A1 (ja) 2021-11-11 2023-05-19 学校法人同志社 角膜内皮細胞の凍結保存製剤およびその製造法
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
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
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

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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

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WO2016144936A1 (en) 2015-03-09 2016-09-15 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
JP6987792B2 (ja) 2016-05-27 2022-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのトリアゾロンおよびテトラゾロン
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de ROCK
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de 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
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
JP2006509015A (ja) 2002-12-04 2006-03-16 メルク エンド カムパニー インコーポレーテッド スピロ環尿素、そのような化合物を含有する組成物、及び使用方法
WO2012081665A1 (ja) 2010-12-15 2012-06-21 大正製薬株式会社 グリシントランスポーター阻害物質
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

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Publication number Publication date
WO2018009627A1 (en) 2018-01-11
KR102449652B1 (ko) 2022-09-29
CN109661396B (zh) 2022-07-01
KR20190025683A (ko) 2019-03-11
ES2829550T3 (es) 2021-06-01
EP3481828A1 (en) 2019-05-15
US20190300528A1 (en) 2019-10-03
JP2019520396A (ja) 2019-07-18
US10787450B2 (en) 2020-09-29
EP3481828B1 (en) 2020-09-16
CN109661396A (zh) 2019-04-19

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