TWI820209B - 三唑并-嘧啶化合物及其用途 - Google Patents

三唑并-嘧啶化合物及其用途 Download PDF

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TWI820209B
TWI820209B TW108132759A TW108132759A TWI820209B TW I820209 B TWI820209 B TW I820209B TW 108132759 A TW108132759 A TW 108132759A TW 108132759 A TW108132759 A TW 108132759A TW I820209 B TWI820209 B TW I820209B
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Taiwan
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methyl
triazolo
pyrimidin
amino
amine
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TW108132759A
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Chinese (zh)
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TW202024089A (zh
Inventor
慶北 曾
長河 齊
漢忠 徐
振帆 楊
小林 張
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大陸商迪哲(江蘇)醫藥股份有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/243Platinum; Compounds thereof

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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)
TW108132759A 2018-09-12 2019-09-11 三唑并-嘧啶化合物及其用途 TWI820209B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
WOPCT/CN2018/105220 2018-09-12
CN2018105220 2018-09-12

Publications (2)

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TW202024089A TW202024089A (zh) 2020-07-01
TWI820209B true TWI820209B (zh) 2023-11-01

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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=)

Families Citing this family (14)

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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

Citations (3)

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WO2002079204A1 (en) 2001-03-28 2002-10-10 Kyowa Hakko Kogyo Co., Ltd. 8-thiazolyl[1,2,4]triazolo[1,5-c]pyrimidine derivative
CN1596258A (zh) * 2001-11-30 2005-03-16 先灵公司 腺A2α受体拮抗剂
TW202000666A (zh) * 2018-02-27 2020-01-01 美商英塞特公司 作為a2a/a2b抑制劑之咪唑并嘧啶及三唑并嘧啶

Family Cites Families (8)

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JP4195729B2 (ja) * 1997-03-24 2008-12-10 協和醗酵工業株式会社 [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体
EP1544200A1 (en) 2002-09-24 2005-06-22 Kyowa Hakko Kogyo Co., Ltd. 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE
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
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 (3)

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Publication number Priority date Publication date Assignee Title
WO2002079204A1 (en) 2001-03-28 2002-10-10 Kyowa Hakko Kogyo Co., Ltd. 8-thiazolyl[1,2,4]triazolo[1,5-c]pyrimidine derivative
CN1596258A (zh) * 2001-11-30 2005-03-16 先灵公司 腺A2α受体拮抗剂
TW202000666A (zh) * 2018-02-27 2020-01-01 美商英塞特公司 作為a2a/a2b抑制劑之咪唑并嘧啶及三唑并嘧啶

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BR112021004774A2 (pt) 2021-08-03
TW202024089A (zh) 2020-07-01
JP2022500402A (ja) 2022-01-04
CN111635408B (zh) 2022-07-22
MX2021002998A (es) 2021-05-14
CN111635408A (zh) 2020-09-08
US11629147B2 (en) 2023-04-18
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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