AU2020211697B2 - Thiazolopyridine derivatives as adenosine receptor antagonists - Google Patents

Thiazolopyridine derivatives as adenosine receptor antagonists

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Publication number
AU2020211697B2
AU2020211697B2 AU2020211697A AU2020211697A AU2020211697B2 AU 2020211697 B2 AU2020211697 B2 AU 2020211697B2 AU 2020211697 A AU2020211697 A AU 2020211697A AU 2020211697 A AU2020211697 A AU 2020211697A AU 2020211697 B2 AU2020211697 B2 AU 2020211697B2
Authority
AU
Australia
Prior art keywords
pyridin
methoxy
thiazolo
amide
oxa
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Active
Application number
AU2020211697A
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English (en)
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AU2020211697A1 (en
Inventor
Alejandro CRESPO
Kai Schiemann
Eva-Maria TANZER
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Domain Therapeutics SA
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Domain Therapeutics SA
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Publication of AU2020211697A1 publication Critical patent/AU2020211697A1/en
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Publication of AU2020211697B2 publication Critical patent/AU2020211697B2/en
Assigned to DOMAIN THERAPEUTICS reassignment DOMAIN THERAPEUTICS Request for Assignment Assignors: MERCK PATENT GMBH
Active legal-status Critical Current
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2020211697A 2019-01-22 2020-01-21 Thiazolopyridine derivatives as adenosine receptor antagonists Active AU2020211697B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19152961 2019-01-22
EP19152961.9 2019-01-22
PCT/EP2020/051347 WO2020152132A1 (en) 2019-01-22 2020-01-21 Thiazolopyridine derivatives as adenosine receptor antagonists

Publications (2)

Publication Number Publication Date
AU2020211697A1 AU2020211697A1 (en) 2021-09-09
AU2020211697B2 true AU2020211697B2 (en) 2025-08-14

Family

ID=65199346

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020211697A Active AU2020211697B2 (en) 2019-01-22 2020-01-21 Thiazolopyridine derivatives as adenosine receptor antagonists

Country Status (23)

Country Link
US (1) US12344623B2 (https=)
EP (1) EP3914600B1 (https=)
JP (1) JP7600119B2 (https=)
KR (1) KR102891741B1 (https=)
CN (1) CN113939520B (https=)
AR (1) AR117844A1 (https=)
AU (1) AU2020211697B2 (https=)
BR (1) BR112021014406A2 (https=)
CA (1) CA3127284A1 (https=)
DK (1) DK3914600T3 (https=)
ES (1) ES2992081T3 (https=)
FI (1) FI3914600T3 (https=)
HR (1) HRP20241385T1 (https=)
HU (1) HUE068968T2 (https=)
IL (1) IL285024A (https=)
LT (1) LT3914600T (https=)
MX (1) MX2021008510A (https=)
PL (1) PL3914600T3 (https=)
PT (1) PT3914600T (https=)
RS (1) RS66038B1 (https=)
SG (1) SG11202107858WA (https=)
SI (1) SI3914600T1 (https=)
WO (1) WO2020152132A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022258622A1 (en) 2021-06-07 2022-12-15 Ares Trading S.A. Combination treatment of cancer
CN119173276A (zh) 2022-04-13 2024-12-20 吉利德科学公司 用于治疗表达Trop-2的癌症的组合疗法
KR20250048043A (ko) 2022-08-02 2025-04-07 메르크 파텐트 게엠베하 (S)-7-옥사-2-아자-스피로[4.5]데칸-2-카르복실산 [7-(3,6-디히드로-2H-피란-4-일)-4-메톡시-티아졸로[4,5-c]피리딘-2-일]-아미드의 신규의 결정질 형태 및 이의 공-결정 형태
CN116217511B (zh) * 2023-03-22 2024-04-19 沈阳药科大学 一种双靶点化合物及其制备方法和在制备sEH抑制剂与PPARs激动剂中的应用
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors

Citations (3)

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WO2005000842A1 (en) * 2003-05-19 2005-01-06 F. Hoffman-La Roche Ag Benzothiazole derivatives as adenosine receptor ligands
WO2005028484A1 (en) * 2003-09-19 2005-03-31 F. Hoffmann-La Roche Ag Thiazolopyridine derivatives as adenosine receptor ligands
WO2019025099A1 (en) * 2017-08-01 2019-02-07 Merck Patent Gmbh THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

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GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
BR9707495A (pt) 1996-02-13 1999-07-27 Zeneca Ltd Derivado de quinazolina processo para a preparação do mesmo composição farmacêutica e processo para a produç o de um efeito antiangiogênico e/ou de redução de permeabilidade vascular em um animal de sangue quente
US6291455B1 (en) 1996-03-05 2001-09-18 Zeneca Limited 4-anilinoquinazoline derivatives
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
AU1688599A (en) 1998-01-05 1999-07-26 Eisai Co. Ltd. Purine derivatives and adenosine a2 receptor antagonists serving as preventives/remedies for diabetes
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
US6841549B1 (en) 1999-07-02 2005-01-11 Eisai Co., Ltd. Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
NZ522074A (en) 2000-05-31 2004-06-25 Astrazeneca Ab Indole derivatives with vascular damaging activity
AU8181701A (en) * 2000-06-21 2002-01-02 Hoffmann La Roche Benzothiazole derivatives
IL153484A0 (en) 2000-07-07 2003-07-06 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors
CN1255392C (zh) 2000-07-07 2006-05-10 安吉奥金尼药品有限公司 作为血管生成抑制剂的秋水仙醇衍生物
WO2004089942A2 (en) 2001-10-02 2004-10-21 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
US6734179B2 (en) * 2001-12-12 2004-05-11 Hoffmann-La Roche Inc. Benzothiazoles
EP1465634B1 (en) 2001-12-12 2014-10-22 The Government of the United States of America, as represented by the Secretary Department of Health and Human Services Methods for using adenosine receptor inhibitors to enhance immune response and inflammation
EP1618108A2 (en) 2003-04-09 2006-01-25 Biogen Idec MA Inc. Triazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]pyrimidines useful as a2a adenosine receptor antagonists
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WO2014101120A1 (en) 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
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WO2005000842A1 (en) * 2003-05-19 2005-01-06 F. Hoffman-La Roche Ag Benzothiazole derivatives as adenosine receptor ligands
WO2005028484A1 (en) * 2003-09-19 2005-03-31 F. Hoffmann-La Roche Ag Thiazolopyridine derivatives as adenosine receptor ligands
WO2019025099A1 (en) * 2017-08-01 2019-02-07 Merck Patent Gmbh THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

Also Published As

Publication number Publication date
DK3914600T3 (da) 2024-10-07
KR20210116572A (ko) 2021-09-27
IL285024A (en) 2021-09-30
SI3914600T1 (sl) 2025-03-31
ES2992081T3 (es) 2024-12-09
LT3914600T (lt) 2024-12-27
RS66038B1 (sr) 2024-11-29
CA3127284A1 (en) 2020-07-30
CN113939520A (zh) 2022-01-14
MX2021008510A (es) 2021-09-21
US20220119412A1 (en) 2022-04-21
JP7600119B2 (ja) 2024-12-16
CN113939520B (zh) 2024-11-22
AU2020211697A1 (en) 2021-09-09
KR102891741B1 (ko) 2025-11-26
WO2020152132A1 (en) 2020-07-30
HUE068968T2 (hu) 2025-02-28
EP3914600B1 (en) 2024-08-07
PL3914600T3 (pl) 2024-12-23
EP3914600A1 (en) 2021-12-01
JP2022524914A (ja) 2022-05-11
FI3914600T3 (fi) 2024-10-31
SG11202107858WA (en) 2021-08-30
US12344623B2 (en) 2025-07-01
PT3914600T (pt) 2024-10-04
BR112021014406A2 (pt) 2021-12-07
AR117844A1 (es) 2021-09-01
HRP20241385T1 (hr) 2024-12-20

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