CN115996929B - 腺苷A2a受体的拮抗剂 - Google Patents

腺苷A2a受体的拮抗剂

Info

Publication number
CN115996929B
CN115996929B CN202180047824.2A CN202180047824A CN115996929B CN 115996929 B CN115996929 B CN 115996929B CN 202180047824 A CN202180047824 A CN 202180047824A CN 115996929 B CN115996929 B CN 115996929B
Authority
CN
China
Prior art keywords
methyl
pyrazolo
pyridinyl
chloro
cyanophenyl
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
CN202180047824.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN115996929A (zh
Inventor
克莱夫·麦卡锡
本杰明·莫尔顿
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.)
Adolphus Treatment Co ltd
Original Assignee
Adolphus Treatment Co ltd
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
Priority claimed from GBGB2006823.5A external-priority patent/GB202006823D0/en
Priority claimed from GBGB2019922.0A external-priority patent/GB202019922D0/en
Application filed by Adolphus Treatment Co ltd filed Critical Adolphus Treatment Co ltd
Publication of CN115996929A publication Critical patent/CN115996929A/zh
Application granted granted Critical
Publication of CN115996929B publication Critical patent/CN115996929B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • C07D487/04—Ortho-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
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202180047824.2A 2020-05-07 2021-05-06 腺苷A2a受体的拮抗剂 Active CN115996929B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB2006823.5A GB202006823D0 (en) 2020-05-07 2020-05-07 Antagonist compounds
GB2006823.5 2020-05-07
GB2019922.0 2020-12-16
GBGB2019922.0A GB202019922D0 (en) 2020-12-16 2020-12-16 Antagonist compounds
PCT/GB2021/051106 WO2021224636A1 (en) 2020-05-07 2021-05-06 Antagonists of the adenosine a2a receptor

Publications (2)

Publication Number Publication Date
CN115996929A CN115996929A (zh) 2023-04-21
CN115996929B true CN115996929B (zh) 2026-01-13

Family

ID=75977772

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180047824.2A Active CN115996929B (zh) 2020-05-07 2021-05-06 腺苷A2a受体的拮抗剂

Country Status (16)

Country Link
EP (1) EP4146654A1 (https=)
JP (2) JP7724239B2 (https=)
KR (1) KR20230035236A (https=)
CN (1) CN115996929B (https=)
AU (1) AU2021266433A1 (https=)
BR (1) BR112022022437A2 (https=)
CA (1) CA3181354A1 (https=)
CL (1) CL2022003055A1 (https=)
CO (1) CO2022017618A2 (https=)
EC (1) ECSP22091613A (https=)
GB (1) GB2609879B (https=)
IL (2) IL297963A (https=)
MX (1) MX2022013946A (https=)
PE (1) PE20230769A1 (https=)
PH (1) PH12022552987A1 (https=)
WO (1) WO2021224636A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4447971A4 (en) * 2021-12-17 2025-12-10 Merck Sharp & Dohme Llc PYRAZOLOPYRIMIDINE DERIVATIVES AND THEIR METHODS OF USE FOR THE TREATMENT OF HERPESVIRUS
CN116283994B (zh) * 2021-12-20 2025-01-07 艾立康药业股份有限公司 作为mat2a抑制剂的杂环化合物
CN117247386B (zh) * 2022-01-18 2025-10-24 江苏亚尧生物科技有限公司 新型吡唑并嘧啶化合物及其组合物、制备方法和用途
JP2025512384A (ja) * 2022-04-13 2025-04-17 ギリアード サイエンシーズ， インコーポレイテッド Ｔｒｏｐ－２発現がんを治療するための併用療法
WO2025094087A1 (en) 2023-10-30 2025-05-08 Johnson & Johnson Enterprise Innovation Inc. Safe administration of a2a rector antagonist
WO2025123251A1 (en) 2023-12-13 2025-06-19 Johnson & Johnson Enterprise Innovation Inc. Crystalline forms of a2a receptor antagonist, preparation methods, and uses thereof
WO2025123253A1 (en) 2023-12-13 2025-06-19 Johnson & Johnson Enterprise Innovation Inc. Pharmaceutical compositions of an a2a receptor antagonist
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors
WO2025202955A1 (en) 2024-03-28 2025-10-02 Pi Industries Ltd. Fused bicyclic compounds and their use as pest control agents
CN120093763A (zh) * 2025-03-25 2025-06-06 上海天龙生物科技有限公司 治疗前列腺疾病和腺体类散结节的药物组合物及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1662537A (zh) * 2002-04-23 2005-08-31 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
EP2402345A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazole fused bicyclic compounds
EP2402337A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds

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US3910907A (en) * 1973-07-09 1975-10-07 Icn Pharmaceuticals Pyrazolo(1,5-a)-1,3,5-triazines
US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
US8178533B2 (en) * 2005-06-01 2012-05-15 Ucb Pharma, S.A. 2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
CN101686989B (zh) * 2007-06-21 2016-10-19 卡拉治疗学股份有限公司 取代的咪唑并杂环
US20100029657A1 (en) 2008-02-29 2010-02-04 Wyeth Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof
EP2402343A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazole-fused bicyclic compounds
EP2402344A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazole fused bicyclic compounds
WO2012100342A1 (en) * 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
ES2728932T3 (es) * 2014-01-09 2019-10-29 Intra Cellular Therapies Inc Compuestos orgánicos
CA2969265A1 (en) * 2014-12-02 2016-06-09 Bayer Pharma Aktiengesellschaft Substituted pyrazolo[1,5-a]pyridines and imidazo[1,2-a]pyrazines and their use
PE20181326A1 (es) 2015-11-03 2018-08-20 Janssen Biotech Inc Anticuerpos que se unen especificamente a pd-1 y sus usos
WO2017178844A1 (en) * 2016-04-15 2017-10-19 Cancer Research Technology Limited Heterocyclic compounds as ret kinase inhibitors
US11608334B2 (en) * 2017-02-08 2023-03-21 The National Institutes of Pharmaceutical R&D Co., Ltd. Pyrrolo-aromatic heterocyclic compound, preparation method therefor, and medical use thereof
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1662537A (zh) * 2002-04-23 2005-08-31 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
EP2402345A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazole fused bicyclic compounds
EP2402337A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds

Also Published As

Publication number Publication date
KR20230035236A (ko) 2023-03-13
CO2022017618A2 (es) 2023-02-16
EP4146654A1 (en) 2023-03-15
MX2022013946A (es) 2023-02-01
ECSP22091613A (es) 2023-03-31
GB2609879A (en) 2023-02-15
GB202217519D0 (en) 2023-01-04
WO2021224636A1 (en) 2021-11-11
IL297963A (en) 2023-01-01
PE20230769A1 (es) 2023-05-09
AU2021266433A1 (en) 2022-12-15
CN115996929A (zh) 2023-04-21
JP7724239B2 (ja) 2025-08-15
IL324071A (en) 2025-12-01
PH12022552987A1 (en) 2024-02-26
CL2022003055A1 (es) 2023-07-07
JP2023525762A (ja) 2023-06-19
BR112022022437A2 (pt) 2023-01-03
US20230203041A1 (en) 2023-06-29
GB2609879B (en) 2023-08-16
CA3181354A1 (en) 2021-11-11
JP2025183201A (ja) 2025-12-16

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