CN111635408B - 三唑并-嘧啶化合物和其用途 - Google Patents

三唑并-嘧啶化合物和其用途 Download PDF

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Publication number
CN111635408B
CN111635408B CN202010656938.4A CN202010656938A CN111635408B CN 111635408 B CN111635408 B CN 111635408B CN 202010656938 A CN202010656938 A CN 202010656938A CN 111635408 B CN111635408 B CN 111635408B
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methyl
mmol
pyrimidin
triazolo
fluorophenyl
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Chinese (zh)
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CN111635408A (zh
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曾庆北
齐长河
徐汉忠
杨振帆
张小林
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Dizhe Jiangsu Pharmaceutical Co ltd
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Dizhe Jiangsu Pharmaceutical Co ltd
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202010656938.4A 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途 Active CN111635408B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CNPCT/CN2018/105220 2018-09-12
CN2018105220 2018-09-12
CN201980006436.2A CN111601809A (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途
PCT/CN2019/105591 WO2020052631A1 (en) 2018-09-12 2019-09-12 Triazolo-pyrimidine compounds and uses thereof

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CN201980006436.2A Division CN111601809A (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途

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CN111635408A CN111635408A (zh) 2020-09-08
CN111635408B true CN111635408B (zh) 2022-07-22

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CN202010657655.1A Active CN112279852B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途
CN201980006436.2A Pending CN111601809A (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途

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CN201980006436.2A Pending CN111601809A (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途

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US (2) US10858365B2 (https=)
EP (1) EP3849983A4 (https=)
JP (2) JP7572353B2 (https=)
KR (1) KR102841843B1 (https=)
CN (3) CN111635408B (https=)
AR (1) AR116315A1 (https=)
AU (1) AU2019340767B9 (https=)
BR (1) BR112021004774A2 (https=)
CA (1) CA3111869A1 (https=)
MX (1) MX2021002998A (https=)
TW (1) TWI820209B (https=)
WO (1) WO2020052631A1 (https=)

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US11066410B2 (en) * 2017-03-24 2021-07-20 3100 Central Expressway Llc Fused triazolo-pyrimidine compounds having useful pharmaceutical application
WO2019018584A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
BR122023024273A2 (pt) 2018-02-27 2024-02-20 Incyte Corporation Compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
WO2019222677A1 (en) 2018-05-18 2019-11-21 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
GEP20237548B (en) 2018-07-05 2023-10-10 Incyte Corp Fused pyrazine derivatives as a2a /a2b inhibitors
AR116315A1 (es) * 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos
EP3911324A4 (en) 2019-01-18 2022-08-17 Nuvation Bio Inc. 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES
EP3911323A4 (en) 2019-01-18 2022-11-16 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US20210061809A1 (en) * 2019-08-26 2021-03-04 Incyte Corporation Triazolopyrimidines as a2a / a2b inhibitors
WO2021156439A1 (en) 2020-02-06 2021-08-12 Astrazeneca Ab Triazole compounds as adenosine receptor antagonists
CN120022278A (zh) * 2023-11-22 2025-05-23 英诺湖医药(杭州)有限公司 用于治疗癌症的化合物
CN117865963B (zh) * 2023-12-15 2026-02-24 上海凌凯科技股份有限公司 一种嘧啶酮衍生物的合成方法及嘧啶酮衍生物

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CN1596258A (zh) * 2001-11-30 2005-03-16 先灵公司 腺A2α受体拮抗剂
EP1544200A1 (en) * 2002-09-24 2005-06-22 Kyowa Hakko Kogyo Co., Ltd. 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE

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JPWO2002079204A1 (ja) 2001-03-28 2004-07-22 協和醗酵工業株式会社 ８−チアゾリル［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体
CN110214012B (zh) * 2017-01-20 2023-05-09 艾库斯生物科学有限公司 用于治疗癌症相关疾病的唑嘧啶
CN109963854B (zh) * 2017-03-16 2022-04-12 江苏恒瑞医药股份有限公司 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用
PL3611174T3 (pl) * 2017-04-07 2022-08-08 Medshine Discovery Inc. Pochodne [1,2,4]triazolo[1,5-c]pirymidyny jako inhibitor receptora a2a
CN109535161B (zh) * 2017-09-22 2021-09-03 江苏恒瑞医药股份有限公司 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用
BR122023024273A2 (pt) * 2018-02-27 2024-02-20 Incyte Corporation Compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos
CN112105617B (zh) * 2018-04-28 2022-04-05 南京明德新药研发有限公司 一种三唑并嘧啶类化合物的晶型、盐型及其制备方法
AR116315A1 (es) * 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
CN1596258A (zh) * 2001-11-30 2005-03-16 先灵公司 腺A2α受体拮抗剂
EP1544200A1 (en) * 2002-09-24 2005-06-22 Kyowa Hakko Kogyo Co., Ltd. 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE

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BR112021004774A2 (pt) 2021-08-03
TW202024089A (zh) 2020-07-01
JP2022500402A (ja) 2022-01-04
MX2021002998A (es) 2021-05-14
CN111635408A (zh) 2020-09-08
US11629147B2 (en) 2023-04-18
TWI820209B (zh) 2023-11-01
CN111601809A (zh) 2020-08-28
AU2019340767B9 (en) 2024-12-05
JP7572353B2 (ja) 2024-10-23
CN112279852A (zh) 2021-01-29
KR20210075996A (ko) 2021-06-23
WO2020052631A1 (en) 2020-03-19
US20210009600A1 (en) 2021-01-14
US10858365B2 (en) 2020-12-08
JP2024123079A (ja) 2024-09-10
AU2019340767A1 (en) 2021-04-08
EP3849983A1 (en) 2021-07-21
CA3111869A1 (en) 2020-03-19
AU2019340767B2 (en) 2024-11-14
AR116315A1 (es) 2021-04-21
KR102841843B1 (ko) 2025-08-01
US20200331918A1 (en) 2020-10-22
CN112279852B (zh) 2023-01-17
EP3849983A4 (en) 2022-06-01

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