CN115996923A - 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途 - Google Patents

一种作为二肽基肽酶1抑制剂的腈衍生物及其用途 Download PDF

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Publication number
CN115996923A
CN115996923A CN202180052880.5A CN202180052880A CN115996923A CN 115996923 A CN115996923 A CN 115996923A CN 202180052880 A CN202180052880 A CN 202180052880A CN 115996923 A CN115996923 A CN 115996923A
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CN
China
Prior art keywords
alkyl
cyano
halogen
hydroxy
cycloalkyl
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Pending
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CN202180052880.5A
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English (en)
Inventor
李瑶
石宗军
张国彪
陈雷
王文晶
张晓波
郑登宇
徐波
刘鑫
王亚军
叶飞
唐平明
倪佳
张晨
严庞科
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Tibet Haisike Pharmaceutical Co ltd
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Sichuan Haisco Pharmaceutical Co Ltd
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Application filed by Sichuan Haisco Pharmaceutical Co Ltd filed Critical Sichuan Haisco Pharmaceutical Co Ltd
Publication of CN115996923A publication Critical patent/CN115996923A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

提供一种式(I)所示的腈衍生物化合物，其立体异构体、氘代物、共晶、溶剂化物或药学上可接受的盐，各基团如说明书之定义。所述化合物具有二肽基肽酶1抑制活性，可用于制备治疗包括气道阻塞性疾病、支气管扩张、囊性纤维化、哮喘、肺气肿和慢性阻塞性肺病等疾病的药物。

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN202180052880.5A 2020-08-26 2021-08-25 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途 Pending CN115996923A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN202010871912 2020-08-26
CN2020108719121 2020-08-26
CN202011129809 2020-10-21
CN2020111298096 2020-10-21
CN202110167731 2021-02-07
CN2021101677315 2021-02-07
PCT/CN2021/114500 WO2022042591A1 (zh) 2020-08-26 2021-08-25 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途

Publications (1)

Publication Number Publication Date
CN115996923A true CN115996923A (zh) 2023-04-21

Family

ID=80354645

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180052880.5A Pending CN115996923A (zh) 2020-08-26 2021-08-25 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途

Country Status (13)

Country Link
US (2) US11807635B2 (zh)
EP (1) EP4129989A4 (zh)
JP (1) JP2023539101A (zh)
KR (1) KR20230084134A (zh)
CN (1) CN115996923A (zh)
AU (1) AU2021330865A1 (zh)
BR (1) BR112023003492A2 (zh)
CA (1) CA3190610A1 (zh)
CL (1) CL2023000532A1 (zh)
IL (1) IL300855A (zh)
MX (1) MX2023002371A (zh)
TW (1) TW202214616A (zh)
WO (1) WO2022042591A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114980887A (zh) 2019-12-20 2022-08-30 特纳亚治疗股份有限公司 氟代烷基-噁二唑及其用途
WO2023160542A1 (zh) * 2022-02-22 2023-08-31 四川海思科制药有限公司 二肽基肽酶抑制剂化合物的盐及晶型
WO2023160541A1 (zh) * 2022-02-22 2023-08-31 四川海思科制药有限公司 一种含氮杂环化合物的制备方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6462076B2 (en) 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
AU2002352126A1 (en) 2001-12-04 2003-06-17 F. Hoffmann-La Roche Ag Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors
WO2004110988A1 (en) 2003-06-18 2004-12-23 Prozymex A/S Protease inhibitors
KR20100098683A (ko) * 2007-12-12 2010-09-08 아스트라제네카 아베 펩티딜 니트릴, 및 디펩티딜 펩티다제 ｉ 억제제로서의 그의 용도
CN102574830A (zh) 2009-05-07 2012-07-11 阿斯利康(瑞典)有限公司 取代的1-氰基乙基杂环基甲酰胺化合物750
JP5815542B2 (ja) * 2009-10-29 2015-11-17 ヤンセン ファーマシューティカ エヌ．ベー． Ｄｐｐ−１阻害剤として有用なアルキニル誘導体
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
US8999975B2 (en) 2011-09-19 2015-04-07 Boehringer Ingelheim International Gmbh Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
WO2015032942A1 (en) * 2013-09-09 2015-03-12 Prozymex A/S N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors
NO2699580T3 (zh) * 2014-01-24 2018-02-24
EP3174879B1 (en) 2014-08-01 2018-07-18 Boehringer Ingelheim International GmbH Substituted oxetanes and their use as inhibitors of cathepsin c
WO2016139355A1 (en) * 2015-03-05 2016-09-09 Prozymex A/S N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors
EP3286172B1 (en) 2015-04-23 2019-06-12 Constellation Pharmaceuticals, Inc. Lsd1 inhibitors and uses thereof
CN107922315B (zh) 2015-08-29 2021-03-26 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途

Also Published As

Publication number Publication date
IL300855A (en) 2023-04-01
US11807635B2 (en) 2023-11-07
MX2023002371A (es) 2023-05-19
US20240059681A1 (en) 2024-02-22
CA3190610A1 (en) 2022-03-03
JP2023539101A (ja) 2023-09-13
EP4129989A1 (en) 2023-02-08
CL2023000532A1 (es) 2023-09-29
TW202214616A (zh) 2022-04-16
BR112023003492A2 (pt) 2023-05-09
US20230121807A1 (en) 2023-04-20
WO2022042591A1 (zh) 2022-03-03
EP4129989A4 (en) 2024-06-05
KR20230084134A (ko) 2023-06-12
AU2021330865A1 (en) 2023-04-27

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