JP7724239B2 - アデノシンa2a受容体のアンタゴニスト - Google Patents

アデノシンa2a受容体のアンタゴニスト

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Publication number
JP7724239B2
JP7724239B2 JP2022567895A JP2022567895A JP7724239B2 JP 7724239 B2 JP7724239 B2 JP 7724239B2 JP 2022567895 A JP2022567895 A JP 2022567895A JP 2022567895 A JP2022567895 A JP 2022567895A JP 7724239 B2 JP7724239 B2 JP 7724239B2
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JP
Japan
Prior art keywords
methyl
pyrazolo
pyridyl
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
JP2022567895A
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English (en)
Japanese (ja)
Other versions
JP2023525762A5 (https=
JP2023525762A (ja
Inventor
マッカーシー,クライヴ
モールトン,ベンジャミン
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.)
AdoRx Therapeutics Ltd
Original Assignee
AdoRx Therapeutics 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 AdoRx Therapeutics Ltd filed Critical AdoRx Therapeutics Ltd
Publication of JP2023525762A publication Critical patent/JP2023525762A/ja
Publication of JP2023525762A5 publication Critical patent/JP2023525762A5/ja
Priority to JP2025130117A priority Critical patent/JP2025183201A/ja
Application granted granted Critical
Publication of JP7724239B2 publication Critical patent/JP7724239B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • C07D487/04Ortho-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
    • A61K31/495Heterocyclic 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged 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
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
JP2022567895A 2020-05-07 2021-05-06 アデノシンa2a受容体のアンタゴニスト Active JP7724239B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025130117A JP2025183201A (ja) 2020-05-07 2025-08-04 アデノシンa2a受容体のアンタゴニスト

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025130117A Division JP2025183201A (ja) 2020-05-07 2025-08-04 アデノシンa2a受容体のアンタゴニスト

Publications (3)

Publication Number Publication Date
JP2023525762A JP2023525762A (ja) 2023-06-19
JP2023525762A5 JP2023525762A5 (https=) 2024-05-17
JP7724239B2 true JP7724239B2 (ja) 2025-08-15

Family

ID=75977772

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2022567895A Active JP7724239B2 (ja) 2020-05-07 2021-05-06 アデノシンa2a受容体のアンタゴニスト
JP2025130117A Pending JP2025183201A (ja) 2020-05-07 2025-08-04 アデノシンa2a受容体のアンタゴニスト

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025130117A Pending JP2025183201A (ja) 2020-05-07 2025-08-04 アデノシンa2a受容体のアンタゴニスト

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)

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WO2003091256A1 (en) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
JP2011513334A (ja) 2008-02-29 2011-04-28 ワイス・エルエルシー ピラゾロ[1,5−a]ピリミジンの架橋二環式複素環式またはスピロ二環式複素環式誘導体、その調製方法および使用
JP2017502069A (ja) 2014-01-09 2017-01-19 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 有機化合物

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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
EP2402337A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds
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
EP2402345A1 (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
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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WO2003091256A1 (en) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
JP2011513334A (ja) 2008-02-29 2011-04-28 ワイス・エルエルシー ピラゾロ[1,5−a]ピリミジンの架橋二環式複素環式またはスピロ二環式複素環式誘導体、その調製方法および使用
JP2017502069A (ja) 2014-01-09 2017-01-19 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 有機化合物

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Dennis R. Compton, et al.,"Pyrazolo[1,5-a]pyrimidines: Estrogen Receptor Ligands Possessing Estrogen Receptor β Antagonist Activity",J. Med. Chem,2004年,Vol.47,pp.5872-5893
REGISTRY(STN)[Online],2015年,CAS登録番号:1782806-38-5, 1496301-75-7等

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
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
CN115996929B (zh) 2026-01-13
CA3181354A1 (en) 2021-11-11
JP2025183201A (ja) 2025-12-16

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