CN113302194A - 作为治疗剂的cGAS活性的抑制剂 - Google Patents

作为治疗剂的cGAS活性的抑制剂 Download PDF

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Publication number
CN113302194A
CN113302194A CN202080007945.XA CN202080007945A CN113302194A CN 113302194 A CN113302194 A CN 113302194A CN 202080007945 A CN202080007945 A CN 202080007945A CN 113302194 A CN113302194 A CN 113302194A
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CN
China
Prior art keywords
pyrimidin
compound
methylbenzofuro
pyrrolidine
optionally substituted
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.)
Pending
Application number
CN202080007945.XA
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English (en)
Chinese (zh)
Inventor
罗伯特·G·洛厄里
梅拉·库马尔
马修·博克瑟
大卫·马洛尼
苏珊·博伊德
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Belbrook Laboratories LLC
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Belbrook Laboratories LLC
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Filing date
Publication date
Application filed by Belbrook Laboratories LLC filed Critical Belbrook Laboratories LLC
Publication of CN113302194A publication Critical patent/CN113302194A/zh
Pending legal-status Critical Current

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202080007945.XA 2019-01-04 2020-01-03 作为治疗剂的cGAS活性的抑制剂 Pending CN113302194A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962788624P 2019-01-04 2019-01-04
US62/788,624 2019-01-04
PCT/US2020/012243 WO2020142729A1 (en) 2019-01-04 2020-01-03 Inhibitors of cgas activity as therapeutic agents

Publications (1)

Publication Number Publication Date
CN113302194A true CN113302194A (zh) 2021-08-24

Family

ID=72338800

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080007945.XA Pending CN113302194A (zh) 2019-01-04 2020-01-03 作为治疗剂的cGAS活性的抑制剂

Country Status (8)

Country Link
US (1) US20220073532A1 (https=)
EP (1) EP3906241A4 (https=)
JP (1) JP7507161B2 (https=)
KR (1) KR20210112316A (https=)
CN (1) CN113302194A (https=)
AU (1) AU2020205114A1 (https=)
CA (1) CA3125625A1 (https=)
WO (1) WO2020142729A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2021349249A1 (en) * 2020-09-24 2023-04-13 Ventus Therapeutics U.S., Inc. Pyrido(4,3-b)indole derivatives and their use as pharmaceuticals
US20240174684A1 (en) * 2021-02-11 2024-05-30 Bellbrook Labs, Llc INHIBITORS OF cGAS ACTIVITY AS THERAPEUTIC AGENTS
CN117337291A (zh) * 2021-05-12 2024-01-02 勃林格殷格翰国际有限公司 作为cGAS抑制剂的具有C-连接环状取代基的吡啶衍生物
CN119119063A (zh) 2021-05-12 2024-12-13 勃林格殷格翰国际有限公司 作为cGAS抑制剂的具有N-连接环状取代基的吡啶衍生物
WO2022238335A1 (en) 2021-05-12 2022-11-17 Boehringer Ingelheim International Gmbh Pyridine derivatives with c-linked cyclic substituents as cgas inhibitors
JP2025528113A (ja) * 2022-08-10 2025-08-26 ベルブルック ラボズ，エルエルシー 治療剤としてのｃＧＡＳ活性の阻害剤
KR20250103719A (ko) 2022-11-09 2025-07-07 베링거 인겔하임 인터내셔날 게엠베하 cGAS 억제제로서의 사이클릭 벤즈이미다졸 유도체
AU2023376006A1 (en) * 2022-11-09 2025-03-13 Boehringer Ingelheim International Gmbh Cyclic pyridine derivatives as cgas inhibitors
WO2025172882A1 (en) 2024-02-14 2025-08-21 Janssen Pharmaceutica Nv Substituted pyrrolidine-2-carboxylic acid derivatives as cgas inhibitors
WO2025233174A1 (en) 2024-05-08 2025-11-13 Boehringer Ingelheim International Gmbh Benzimidazole derivatives as cgas inhibitors

Citations (8)

* Cited by examiner, † Cited by third party
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CN1897928A (zh) * 2003-10-15 2007-01-17 Imtm股份有限公司 用于功能上影响不同类型的细胞和用于治疗免疫、炎症、神经和其他疾病的新的丙氨酰氨肽酶抑制剂
US20080261946A1 (en) * 2005-09-21 2008-10-23 Cellzome (Uk) Ltd. Pyrimidine Compounds for the Treatment of Inflammatory Disorders
US20080269239A1 (en) * 2004-11-11 2008-10-30 Argenta Discovery Ltd. Pyrimidine Compounds as Histamine Modulators
CN101511190A (zh) * 2006-07-11 2009-08-19 詹森药业有限公司 组胺h4受体的苯并呋喃并-和苯并噻吩并嘧啶调节剂
CN102209714A (zh) * 2008-11-10 2011-10-05 巴塞尔大学 三嗪、嘧啶和吡啶类似物和它们作为治疗剂和诊断探针的应用
WO2013115167A1 (ja) * 2012-01-31 2013-08-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 アムバチニブ誘導体
CN104513257A (zh) * 2013-09-26 2015-04-15 广东东阳光药业有限公司 取代脲衍生物及其在药物中的应用
WO2019084271A1 (en) * 2017-10-25 2019-05-02 Children's Medical Center Corporation PAPD5 INHIBITORS AND METHODS OF USE

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* Cited by examiner, † Cited by third party
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US3755583A (en) * 1970-06-05 1973-08-28 Chas0!nhx
WO2009086303A2 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
KR20250065420A (ko) * 2015-12-25 2025-05-12 가부시키가이샤 한도오따이 에네루기 켄큐쇼 화합물, 발광 소자, 표시 장치, 전자 기기, 및 조명 장치

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1897928A (zh) * 2003-10-15 2007-01-17 Imtm股份有限公司 用于功能上影响不同类型的细胞和用于治疗免疫、炎症、神经和其他疾病的新的丙氨酰氨肽酶抑制剂
US20080269239A1 (en) * 2004-11-11 2008-10-30 Argenta Discovery Ltd. Pyrimidine Compounds as Histamine Modulators
US20080261946A1 (en) * 2005-09-21 2008-10-23 Cellzome (Uk) Ltd. Pyrimidine Compounds for the Treatment of Inflammatory Disorders
CN101312979A (zh) * 2005-09-21 2008-11-26 塞尔佐姆（英国）有限公司 用于治疗炎性病症的嘧啶化合物
CN101511190A (zh) * 2006-07-11 2009-08-19 詹森药业有限公司 组胺h4受体的苯并呋喃并-和苯并噻吩并嘧啶调节剂
CN102209714A (zh) * 2008-11-10 2011-10-05 巴塞尔大学 三嗪、嘧啶和吡啶类似物和它们作为治疗剂和诊断探针的应用
WO2013115167A1 (ja) * 2012-01-31 2013-08-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 アムバチニブ誘導体
CN104513257A (zh) * 2013-09-26 2015-04-15 广东东阳光药业有限公司 取代脲衍生物及其在药物中的应用
WO2019084271A1 (en) * 2017-10-25 2019-05-02 Children's Medical Center Corporation PAPD5 INHIBITORS AND METHODS OF USE

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ACS: "RN:1165797-10-3 等", 《STN REGISTRY》, pages 1 - 2 *

Also Published As

Publication number Publication date
US20220073532A1 (en) 2022-03-10
EP3906241A1 (en) 2021-11-10
EP3906241A4 (en) 2022-11-02
AU2020205114A1 (en) 2021-07-22
WO2020142729A1 (en) 2020-07-09
KR20210112316A (ko) 2021-09-14
JP2022518148A (ja) 2022-03-14
CA3125625A1 (en) 2020-07-09
JP7507161B2 (ja) 2024-06-27

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Application publication date: 20210824