CN116157154B - 血浆激肽释放酶抑制剂 - Google Patents

血浆激肽释放酶抑制剂

Info

Publication number
CN116157154B
CN116157154B CN202180055135.6A CN202180055135A CN116157154B CN 116157154 B CN116157154 B CN 116157154B CN 202180055135 A CN202180055135 A CN 202180055135A CN 116157154 B CN116157154 B CN 116157154B
Authority
CN
China
Prior art keywords
mmol
mixture
stirred
chloro
added
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
CN202180055135.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN116157154A (zh
Inventor
J·D·希克斯
邝荣泽
C·J·辛兹
M·J·隆巴尔多
J·A·洛佩兹
R·玛钱特
P·P·夏普
吴志才
赵志强
A·C·郑
S·杨
包奖明
M·天
G·P·谢兰-南斯
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.)
Merck Sharp & Dohme BV
Original Assignee
Merck Sharp & Dohme BV
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 Merck Sharp & Dohme BV filed Critical Merck Sharp & Dohme BV
Publication of CN116157154A publication Critical patent/CN116157154A/zh
Application granted granted Critical
Publication of CN116157154B publication Critical patent/CN116157154B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CN202180055135.6A 2020-07-10 2021-07-06 血浆激肽释放酶抑制剂 Active CN116157154B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063050220P 2020-07-10 2020-07-10
US63/050220 2020-07-10
PCT/US2021/040420 WO2022010828A1 (en) 2020-07-10 2021-07-06 Plasma kallikrein inhibitors

Publications (2)

Publication Number Publication Date
CN116157154A CN116157154A (zh) 2023-05-23
CN116157154B true CN116157154B (zh) 2026-05-01

Family

ID=79552050

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180055135.6A Active CN116157154B (zh) 2020-07-10 2021-07-06 血浆激肽释放酶抑制剂

Country Status (9)

Country Link
US (1) US12528786B2 (enExample)
EP (1) EP4178620B1 (enExample)
JP (1) JP7773522B2 (enExample)
KR (1) KR20230038526A (enExample)
CN (1) CN116157154B (enExample)
AU (1) AU2021306250A1 (enExample)
CA (1) CA3185597A1 (enExample)
MX (1) MX2023000507A (enExample)
WO (1) WO2022010828A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4210694B1 (en) * 2020-09-10 2025-10-15 Merck Sharp & Dohme LLC Plasma kallikrein inhibitors
WO2024173196A1 (en) * 2023-02-17 2024-08-22 Merck Sharp & Dohme Llc Plasma kallikrein inhibitors
WO2026096331A1 (en) * 2024-10-30 2026-05-07 Merck Sharp & Dohme Llc Plasma kallikrein inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102762203A (zh) * 2009-12-18 2012-10-31 艾克提弗赛特制药股份有限公司 血浆激肽释放酶抑制剂的前药
CN106257976A (zh) * 2014-03-07 2016-12-28 拜奥克里斯特制药公司 人类血浆激肽释放酶抑制剂

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9290485B2 (en) * 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
GB201300304D0 (en) 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
RU2712621C2 (ru) 2013-05-23 2020-01-30 Калвиста Фармасьютикалз Лимитед Азотсодержащие гетероциклические производные, полезные в качестве ингибитора калликреина плазмы
KR102286305B1 (ko) 2014-07-16 2021-08-09 라이프에스씨아이 파마슈티컬스, 인크. 치료적 억제 화합물
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
WO2017001926A2 (en) 2015-07-01 2017-01-05 Lifesci Pharmaceuticals, Inc Therapeutic inhibitory compounds
WO2017072020A1 (en) * 2015-10-27 2017-05-04 Boehringer Ingelheim International Gmbh Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
US10640486B2 (en) * 2015-10-27 2020-05-05 Boehringer Ingelheim International Gmbh Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
BR112018008506B8 (pt) 2015-10-29 2023-12-05 Merck Sharp & Dohme Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos
EP3612523B1 (en) 2017-04-21 2021-06-09 Boehringer Ingelheim International GmbH Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
GB201719882D0 (en) * 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of a plasma kallikrein inhibitor and salts thereof
CN113039181B (zh) * 2018-08-16 2024-08-13 勃林格殷格翰国际有限公司 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物
KR102931248B1 (ko) * 2020-06-16 2026-03-03 머크 샤프 앤드 돔 엘엘씨 혈장 칼리크레인 억제제

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102762203A (zh) * 2009-12-18 2012-10-31 艾克提弗赛特制药股份有限公司 血浆激肽释放酶抑制剂的前药
CN106257976A (zh) * 2014-03-07 2016-12-28 拜奥克里斯特制药公司 人类血浆激肽释放酶抑制剂

Also Published As

Publication number Publication date
CN116157154A (zh) 2023-05-23
US12528786B2 (en) 2026-01-20
KR20230038526A (ko) 2023-03-20
WO2022010828A1 (en) 2022-01-13
EP4178620A1 (en) 2023-05-17
CA3185597A1 (en) 2022-01-13
AU2021306250A1 (en) 2023-02-16
EP4178620A4 (en) 2024-08-07
JP7773522B2 (ja) 2025-11-19
US20230348428A1 (en) 2023-11-02
EP4178620B1 (en) 2026-04-01
JP2023533519A (ja) 2023-08-03
MX2023000507A (es) 2023-02-09

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