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PE20230769A1 - Antagonistas del receptor de adenosina a2a - Google Patents

Antagonistas del receptor de adenosina a2a

Info

Publication number
PE20230769A1
PE20230769A1 PE2022002570A PE2022002570A PE20230769A1 PE 20230769 A1 PE20230769 A1 PE 20230769A1 PE 2022002570 A PE2022002570 A PE 2022002570A PE 2022002570 A PE2022002570 A PE 2022002570A PE 20230769 A1 PE20230769 A1 PE 20230769A1
Authority
PE
Peru
Prior art keywords
hydrogen
halo
heteroaryl
cyano
absent
Prior art date
Application number
PE2022002570A
Other languages
English (en)
Inventor
Clive Mccarthy
Benjamin Moulton
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 PE20230769A1 publication Critical patent/PE20230769A1/es

Links

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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

Abstract

La presente invencion se refiere a compuestos de formula I donde R0 es hidrogeno o deuterio; R1 se selecciona de arilo o heteroarilo, entre otros; R2 se selecciona de hidrogeno, ciano, halo, alquilo (C1-4), haloalquilo (C1-4), arilo, heteroarilo, alquenilo (C2-6), entre otros; R3 se selecciona de hidrogeno, halo, ciano o un grupo de formula: -L-Y-Lq-Q en donde: L esta ausente o es alquileno (C1-4) u oxo; Y esta ausente o es O, S, SO, SO2, entre otros; Lq esta ausente o es alquileno (C1-4) opcionalmente sustituido por uno o mas sustituyentes seleccionados de alcoxi (C1-2), halo, ciano, amino u oxo; y Q es hidrogeno, alquilo (C1-6), alquenilo (C2-6), alquinilo (C2-6), arilo, cicloalquilo (3-8), cicloalquenilo (C3-8), heteroarilo o heterociclilo; utiles en el tratamiento de enfermedades o afecciones en las que esta implicada la actividad del receptor de adenosina A2a, tales como, por ejemplo, el cancer.
PE2022002570A 2020-05-07 2021-05-06 Antagonistas del receptor de adenosina a2a PE20230769A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB2006823.5A GB202006823D0 (en) 2020-05-07 2020-05-07 Antagonist compounds
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 (1)

Publication Number Publication Date
PE20230769A1 true PE20230769A1 (es) 2023-05-09

Family

ID=75977772

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002570A PE20230769A1 (es) 2020-05-07 2021-05-06 Antagonistas del receptor de adenosina a2a

Country Status (17)

Country Link
US (1) US20230203041A1 (es)
EP (1) EP4146654A1 (es)
JP (2) JP7724239B2 (es)
KR (1) KR20230035236A (es)
CN (1) CN115996929B (es)
AU (1) AU2021266433A1 (es)
BR (1) BR112022022437A2 (es)
CA (1) CA3181354A1 (es)
CL (1) CL2022003055A1 (es)
CO (1) CO2022017618A2 (es)
EC (1) ECSP22091613A (es)
GB (1) GB2609879B (es)
IL (2) IL297963A (es)
MX (1) MX2022013946A (es)
PE (1) PE20230769A1 (es)
PH (1) PH12022552987A1 (es)
WO (1) WO2021224636A1 (es)

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* Cited by examiner, † Cited by third party
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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
EP4467545A4 (en) * 2022-01-18 2026-01-21 Jiangsu Yayo Biotechnology Co Ltd NEW TYPE OF COMPOUND PYRAZOLOPYRIMIDINE AND ASSOCIATED COMPOSITION, PREPARATION PROCESS AND USE
WO2023201267A1 (en) 2022-04-13 2023-10-19 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
WO2025054448A1 (en) * 2023-09-08 2025-03-13 Satellos Bioscience Inc. Ap2 associated kinase 1 inhibitors and uses thereof
TW202535406A (zh) 2023-10-30 2025-09-16 美商壯生和壯生企業創新公司 用於治療肺癌之a2a受體拮抗劑
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

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US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
JP4500055B2 (ja) * 2002-04-23 2010-07-14 塩野義製薬株式会社 ピラゾロ［１，５−ａ］ピリミジン誘導体およびそれを含有するＮＡＤ（Ｐ）Ｈオキシダーゼ阻害剤
EP2308867A3 (en) * 2005-06-01 2011-10-19 UCB Pharma S.A. 2-oxo-1-pyrrolidine deriatives, processes for preparing them and their uses
MY146924A (en) * 2007-06-21 2012-10-15 Cara Therapeutics Inc Substituted imidazoheterocycles
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
EP2402345A1 (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
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
CA2825098C (en) * 2011-01-27 2020-03-10 Universite De Montreal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
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US10174021B2 (en) * 2014-12-02 2019-01-08 Bayer Pharma Aktiengesellschaft Substituted pyrazolo[1,5-A]pyridines and their use
JP2019500893A (ja) 2015-11-03 2019-01-17 ヤンセン バイオテツク，インコーポレーテツド Ｐｄ−１及びｔｉｍ−３に特異的に結合する抗体及びそれらの使用
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JP7164203B2 (ja) * 2017-02-08 2022-11-01 中国医▲薬▼研究▲開▼▲発▼中心有限公司 ピロロ芳香族複素環化合物及びその製造方法並びに医薬用途
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Also Published As

Publication number Publication date
GB202217519D0 (en) 2023-01-04
CA3181354A1 (en) 2021-11-11
JP2025183201A (ja) 2025-12-16
US20230203041A1 (en) 2023-06-29
IL297963A (en) 2023-01-01
CN115996929A (zh) 2023-04-21
AU2021266433A1 (en) 2022-12-15
CL2022003055A1 (es) 2023-07-07
CN115996929B (zh) 2026-01-13
GB2609879A (en) 2023-02-15
WO2021224636A1 (en) 2021-11-11
IL324071A (en) 2025-12-01
BR112022022437A2 (pt) 2023-01-03
EP4146654A1 (en) 2023-03-15
JP7724239B2 (ja) 2025-08-15
JP2023525762A (ja) 2023-06-19
MX2022013946A (es) 2023-02-01
CO2022017618A2 (es) 2023-02-16
ECSP22091613A (es) 2023-03-31
KR20230035236A (ko) 2023-03-13
GB2609879B (en) 2023-08-16
PH12022552987A1 (en) 2024-02-26

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