CN111601809A - 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
CN111601809A
CN111601809A CN201980006436.2A CN201980006436A CN111601809A CN 111601809 A CN111601809 A CN 111601809A CN 201980006436 A CN201980006436 A CN 201980006436A CN 111601809 A CN111601809 A CN 111601809A
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Prior art keywords
pyrimidin
methyl
triazolo
amino
amine
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CN201980006436.2A
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English (en)
Chinese (zh)
Inventor
曾庆北
齐长河
徐汉忠
杨振帆
张小林
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Dizal Jiangsu Pharmaceutical Co Ltd
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Dizal Jiangsu Pharmaceutical Co Ltd
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Priority to CN202010657655.1A priority Critical patent/CN112279852B/zh
Priority to CN202010656938.4A priority patent/CN111635408B/zh
Publication of CN111601809A publication Critical patent/CN111601809A/zh
Pending legal-status Critical Current

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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
    • 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
    • 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

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

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN202010657655.1A CN112279852B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途
CN202010656938.4A CN111635408B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018105220 2018-09-12
CNPCT/CN2018/105220 2018-09-12
PCT/CN2019/105591 WO2020052631A1 (en) 2018-09-12 2019-09-12 Triazolo-pyrimidine compounds and uses thereof

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CN202010656938.4A Division CN111635408B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途
CN202010657655.1A Division CN112279852B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途

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CN111601809A true CN111601809A (zh) 2020-08-28

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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
CN202010657655.1A Active CN112279852B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途
CN202010656938.4A Active CN111635408B (zh) 2018-09-12 2019-09-12 三唑并-嘧啶化合物和其用途

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CN202010656938.4A Active CN111635408B (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 (enExample)
EP (1) EP3849983A4 (enExample)
JP (2) JP7572353B2 (enExample)
KR (1) KR102841843B1 (enExample)
CN (3) CN111601809A (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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112384515A (zh) * 2018-02-27 2021-02-19 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
CN117865963A (zh) * 2023-12-15 2024-04-12 上海凌凯医药科技有限公司 一种嘧啶酮衍生物的合成方法及嘧啶酮衍生物
WO2025108116A1 (zh) * 2023-11-22 2025-05-30 英诺湖医药(杭州)有限公司 用于治疗癌症的化合物

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EP3600328A4 (en) * 2017-03-24 2021-01-06 3100 Central Expressway LLC MERGED TRIAZOLO-PYRIMIDINE COMPOUNDS WITH USEFUL PHARMACEUTICAL APPLICATION
JP2020527588A (ja) 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． アデノシンアンタゴニストとしてのヘテロ環式化合物
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
CN117304191A (zh) 2018-07-05 2023-12-29 因赛特公司 作为a2a/a2b抑制剂的稠合吡嗪衍生物
AR116315A1 (es) * 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos
WO2020150674A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
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
PH12022550470A1 (en) * 2019-08-26 2023-02-27 Incyte Corp Triazolopyrimidines as a2a / a2b inhibitors
WO2021156439A1 (en) 2020-02-06 2021-08-12 Astrazeneca Ab Triazole compounds as adenosine receptor antagonists

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CN109535161A (zh) * 2017-09-22 2019-03-29 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
CN110446712A (zh) * 2017-04-07 2019-11-12 南京明德新药研发有限公司 作为A2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物
CN112105617A (zh) * 2018-04-28 2020-12-18 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
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KR20190129851A (ko) * 2017-03-16 2019-11-20 지앙수 헨그루이 메디슨 컴퍼니 리미티드 헤테로아릴[4,3-c]피리미딘-5-아민 유도체, 이의 제조 방법 및 이의 의학적 용도
AR116315A1 (es) * 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos

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CN110446712A (zh) * 2017-04-07 2019-11-12 南京明德新药研发有限公司 作为A2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物
CN109535161A (zh) * 2017-09-22 2019-03-29 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
CN112384515A (zh) * 2018-02-27 2021-02-19 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
CN112105617A (zh) * 2018-04-28 2020-12-18 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

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JULIUS J. MATASI ET AL.: ""2-(2-Furanyl)-7-phenyl[1, 2, 4]triazolo[1, 5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1"", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 15, 22 June 2005 (2005-06-22), pages 3670 - 3674 *
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112384515A (zh) * 2018-02-27 2021-02-19 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
CN112384515B (zh) * 2018-02-27 2024-12-10 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
WO2025108116A1 (zh) * 2023-11-22 2025-05-30 英诺湖医药(杭州)有限公司 用于治疗癌症的化合物
CN117865963A (zh) * 2023-12-15 2024-04-12 上海凌凯医药科技有限公司 一种嘧啶酮衍生物的合成方法及嘧啶酮衍生物

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US11629147B2 (en) 2023-04-18
MX2021002998A (es) 2021-05-14
JP2022500402A (ja) 2022-01-04
AU2019340767B9 (en) 2024-12-05
TW202024089A (zh) 2020-07-01
CA3111869A1 (en) 2020-03-19
US10858365B2 (en) 2020-12-08
KR102841843B1 (ko) 2025-08-01
AR116315A1 (es) 2021-04-21
CN112279852B (zh) 2023-01-17
EP3849983A4 (en) 2022-06-01
CN111635408B (zh) 2022-07-22
WO2020052631A1 (en) 2020-03-19
AU2019340767A1 (en) 2021-04-08
KR20210075996A (ko) 2021-06-23
CN112279852A (zh) 2021-01-29
JP7572353B2 (ja) 2024-10-23
AU2019340767B2 (en) 2024-11-14
JP2024123079A (ja) 2024-09-10
TWI820209B (zh) 2023-11-01
BR112021004774A2 (pt) 2021-08-03
CN111635408A (zh) 2020-09-08
US20200331918A1 (en) 2020-10-22
EP3849983A1 (en) 2021-07-21
US20210009600A1 (en) 2021-01-14

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