GB2609879B - Antagonists of the adenosine A2a receptor - Google Patents

Antagonists of the adenosine A2a receptor Download PDF

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Publication number
GB2609879B
GB2609879B GB2217519.4A GB202217519A GB2609879B GB 2609879 B GB2609879 B GB 2609879B GB 202217519 A GB202217519 A GB 202217519A GB 2609879 B GB2609879 B GB 2609879B
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United Kingdom
Prior art keywords
adenosine
antagonists
receptor
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
GB2217519.4A
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English (en)
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GB202217519D0 (en
GB2609879A (en
Inventor
Mccarthy Clive
Moulton Benjamin
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
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AdoRx Therapeutics Ltd
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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 GB202217519D0 publication Critical patent/GB202217519D0/en
Publication of GB2609879A publication Critical patent/GB2609879A/en
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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)
  • 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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
GB2217519.4A 2020-05-07 2021-05-06 Antagonists of the adenosine A2a receptor Active GB2609879B (en)

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 (3)

Publication Number Publication Date
GB202217519D0 GB202217519D0 (en) 2023-01-04
GB2609879A GB2609879A (en) 2023-02-15
GB2609879B true GB2609879B (en) 2023-08-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
GB2217519.4A Active GB2609879B (en) 2020-05-07 2021-05-06 Antagonists of the adenosine A2a receptor

Country Status (17)

Country Link
US (1) US12617796B2 (enExample)
EP (1) EP4146654A1 (enExample)
JP (2) JP7724239B2 (enExample)
KR (1) KR20230035236A (enExample)
CN (2) CN115996929B (enExample)
AU (1) AU2021266433A1 (enExample)
BR (1) BR112022022437A2 (enExample)
CA (1) CA3181354A1 (enExample)
CL (1) CL2022003055A1 (enExample)
CO (1) CO2022017618A2 (enExample)
EC (1) ECSP22091613A (enExample)
GB (1) GB2609879B (enExample)
IL (2) IL297963A (enExample)
MX (1) MX2022013946A (enExample)
PE (1) PE20230769A1 (enExample)
PH (1) PH12022552987A1 (enExample)
WO (1) WO2021224636A1 (enExample)

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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
KR20250004779A (ko) 2022-04-13 2025-01-08 길리애드 사이언시즈, 인코포레이티드 Trop-2 발현 암을 치료하기 위한 병용 요법
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
WO2025123253A1 (en) 2023-12-13 2025-06-19 Johnson & Johnson Enterprise Innovation Inc. Pharmaceutical compositions of an a2a receptor 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
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DATABASE REGISTRY[Online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US,Anonymous,"Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 2-(2-pyridinyl)-"(20120413), Database accession no.1367863-71-5, 1367833-85-9, 1367824-67-6, Abstract.Further database acession no's 1367817-15-9, 1367753-06-7 *
DE LERA RUIZ ET AL., "Adenosine A 2A Receptor as a Drug Discovery Target", J. MED. CHEM.(20131115), vol. 57, no. 9, pages 3623 - 3650 doi:10.1021/jm4011669. The whole doc. For instance: page 362, figure 2 and page 3630, fig 5: ZM241385; page 3634, fig 8: bicyclic core; page 3635, fig 9: compound 32 *
NEUSTADT ET AL., "Potent and selective adenosine A"2"A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines", BIORG. MED. CHEM. LETT., vol. 19, no. 3, (20090201) pages 967 - 971 doi:10.1016/J.BMCL.2008.11.075 [retrieved 24.11.2008], Title; abstract; page 968, table 1;page 970, table 3. *
NORMAN ET AL."N,N-Dialkyl-N'-Chlorosulfonyl Chloroformamidines in Heterocyclic Synthesis. Part XIII. Cleavage and Rearrangement Reactions of Pyrazolo[1,5-b][1,2,4,6]thiatriazine...", AUSTRALIAN JRNL OF CHEM, (20151015), vol. 69, no.1, pp.61-75, p.65, scheme 11 and table 3: compound 5 with R=H *

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