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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Publication number
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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (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)
  • Virology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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)

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

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Family Applications (1)

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

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US (2) US10858365B2 (enExample)
EP (1) EP3849983A4 (enExample)
JP (2) JP7572353B2 (enExample)
KR (1) KR102841843B1 (enExample)
CN (3) CN112279852B (enExample)
AR (1) AR116315A1 (enExample)
AU (1) AU2019340767B9 (enExample)
BR (1) BR112021004774A2 (enExample)
CA (1) CA3111869A1 (enExample)
MX (1) MX2021002998A (enExample)
TW (1) TWI820209B (enExample)
WO (1) WO2020052631A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018237598B2 (en) * 2017-03-24 2023-12-14 Piksci Inc. Fused triazolo-pyrimidine compounds having useful pharmaceutical application
CN111163780A (zh) 2017-07-18 2020-05-15 诺维逊生物股份有限公司 作为腺苷拮抗剂的杂环化合物
TWI877770B (zh) 2018-02-27 2025-03-21 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
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
EP3810610A1 (en) 2018-05-18 2021-04-28 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
WO2020010197A1 (en) 2018-07-05 2020-01-09 Incyte Corporation 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
WO2020150676A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
AU2020208644A1 (en) 2019-01-18 2021-08-26 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
PE20230372A1 (es) * 2019-08-26 2023-03-06 Incyte Corp Triazolopirimidinas como inhibidores de a2a/a2b
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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69820866T2 (de) * 1997-03-24 2004-12-30 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-DERIVATE
WO2004029056A1 (ja) * 2002-09-24 2004-04-08 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体
HUE064141T2 (hu) * 2017-01-20 2024-02-28 Arcus Biosciences Inc Azolopirimidin rákkal összefüggõ rendellenességek kezelésére
AU2018233367B2 (en) * 2017-03-16 2021-08-12 Jiangsu Hengrui Medicine Co., Ltd. Heteroaryl[4,3-c]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
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
PL3766884T3 (pl) * 2018-04-28 2022-07-18 Medshine Discovery Inc. Postać krystaliczna i rodzaj soli związku triazolopirymidynowego oraz sposób jej wytwarzania
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)

* Cited by examiner, † Cited by third party
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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Publication number Publication date
AR116315A1 (es) 2021-04-21
US20200331918A1 (en) 2020-10-22
AU2019340767B9 (en) 2024-12-05
AU2019340767B2 (en) 2024-11-14
EP3849983A1 (en) 2021-07-21
TW202024089A (zh) 2020-07-01
CA3111869A1 (en) 2020-03-19
US10858365B2 (en) 2020-12-08
JP2022500402A (ja) 2022-01-04
KR20210075996A (ko) 2021-06-23
CN112279852A (zh) 2021-01-29
WO2020052631A1 (en) 2020-03-19
EP3849983A4 (en) 2022-06-01
US11629147B2 (en) 2023-04-18
KR102841843B1 (ko) 2025-08-01
AU2019340767A1 (en) 2021-04-08
CN112279852B (zh) 2023-01-17
JP7572353B2 (ja) 2024-10-23
BR112021004774A2 (pt) 2021-08-03
JP2024123079A (ja) 2024-09-10
MX2021002998A (es) 2021-05-14
CN111635408B (zh) 2022-07-22
CN111635408A (zh) 2020-09-08
CN111601809A (zh) 2020-08-28
US20210009600A1 (en) 2021-01-14

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