CN113939520B - 作为腺苷受体拮抗剂的噻唑并吡啶衍生物 - Google Patents

作为腺苷受体拮抗剂的噻唑并吡啶衍生物 Download PDF

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Publication number
CN113939520B
CN113939520B CN202080010474.8A CN202080010474A CN113939520B CN 113939520 B CN113939520 B CN 113939520B CN 202080010474 A CN202080010474 A CN 202080010474A CN 113939520 B CN113939520 B CN 113939520B
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cancer
compounds
adenosine
compound
receptor
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CN113939520A (zh
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E-M·坦策尔克劳埃尔
K·席曼
A·克雷斯波
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Merck Patent GmbH
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Merck Patent GmbH
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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

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  • 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)
CN202080010474.8A 2019-01-22 2020-01-21 作为腺苷受体拮抗剂的噻唑并吡啶衍生物 Active CN113939520B (zh)

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
CN113939520A CN113939520A (zh) 2022-01-14
CN113939520B true CN113939520B (zh) 2024-11-22

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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=)

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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

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CN1791600A (zh) * 2003-05-19 2006-06-21 弗·哈夫曼-拉罗切有限公司 用作腺苷受体的配体的苯并噻唑衍生物
CN1871244A (zh) * 2003-09-19 2006-11-29 弗·哈夫曼-拉罗切有限公司 作为腺苷受体配体的噻唑并吡啶衍生物
WO2019025099A1 (en) * 2017-08-01 2019-02-07 Merck Patent Gmbh THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

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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
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
AU2020211697B2 (en) 2025-08-14
PT3914600T (pt) 2024-10-04
BR112021014406A2 (pt) 2021-12-07
AR117844A1 (es) 2021-09-01
HRP20241385T1 (hr) 2024-12-20

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