CN111511745A - 吡唑并[1,5-a][1,3,5]三嗪-2-胺类衍生物、其制备方法及其在医药上的应用 - Google Patents

吡唑并[1,5-a][1,3,5]三嗪-2-胺类衍生物、其制备方法及其在医药上的应用 Download PDF

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CN111511745A
CN111511745A CN201980006595.2A CN201980006595A CN111511745A CN 111511745 A CN111511745 A CN 111511745A CN 201980006595 A CN201980006595 A CN 201980006595A CN 111511745 A CN111511745 A CN 111511745A
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compound
alkyl
cycloalkyl
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CN111511745B (zh
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陆标
桂斌
张俊珍
贺峰
陶维康
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Shandong Shengdi Pharmaceutical Co ltd
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

一种通式(I)所示的吡唑并[1,5‑a][1,3,5]三嗪‑2‑胺类衍生物、其制备方法及含有该衍生物的药物组合物以及其作为治疗剂的用途，特别是作为A2a受体拮抗剂的用途和在制备用于治疗通过对A2a受体的抑制而改善的病况或病症的药物中的用途。

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN201980006595.2A 2018-02-06 2019-02-01 吡唑并[1，5-a][1，3，5]三嗪-2-胺类衍生物、其制备方法及其应用 Active CN111511745B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810118455 2018-02-06
CN2018101184551 2018-02-06
PCT/CN2019/074324 WO2019154294A1 (zh) 2018-02-06 2019-02-01 吡唑并[1,5-a][1,3,5]三嗪-2-胺类衍生物、其制备方法及其在医药上的应用

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CN111511745A true CN111511745A (zh) 2020-08-07
CN111511745B CN111511745B (zh) 2022-05-27

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US (1) US20210032253A1 (zh)
EP (1) EP3750891A4 (zh)
JP (1) JP2021512959A (zh)
CN (1) CN111511745B (zh)
CA (1) CA3089159A1 (zh)
TW (1) TWI701251B (zh)
WO (1) WO2019154294A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112028891A (zh) * 2019-07-30 2020-12-04 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3070273A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2019018583A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC 1,8-NAPHTHYRIDINONE COMPOUNDS AND USES THEREOF
AU2020207951A1 (en) 2019-01-18 2021-08-26 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
CA3126702A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5356894A (en) * 1990-05-29 1994-10-18 Rodney Peter W Morpholinyl substituted [1,2,4]-triazolo[1,5-a]triazine as antagonist
WO2000059907A2 (en) * 1999-04-06 2000-10-12 Du Pont Pharmaceuticals Company Pyrazolotriazines as crf antagonists
CN1278819A (zh) * 1997-09-02 2001-01-03 杜邦药品公司 作为促肾上腺皮质素释放激素拮抗剂、可用于治疗cns障碍和紧张相关性疾病的杂环基取代的环稠合吡啶和嘧啶
WO2004110454A1 (ja) * 2003-06-13 2004-12-23 Ishihara Sangyo Kaisha, Ltd. アデノシンＡ2ａ受容体アゴニストの投与が必要な疾患を治療又は予防するための組成物
US20060106019A1 (en) * 2002-07-26 2006-05-18 Greenpharma Novel substituted pyrazolo[1,5 a]-1,3,5-triazine derivatives and their analogues, pharmaceutical compositions containing same, use thereof as medicine and methods for preparing same
WO2017055305A1 (en) * 2015-09-30 2017-04-06 Ucb Biopharma Sprl Fused pyrazole derivatives as kinase inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0459702A1 (en) * 1990-05-29 1991-12-04 Zeneca Limited Azole Derivatives
EP0915880B1 (en) * 1996-07-24 2007-10-10 Bristol-Myers Squibb Pharma Company Azolo triazines and pyrimidines
US7329658B2 (en) * 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
EP1780205A1 (en) 2004-06-14 2007-05-02 Mitsui Chemicals, Inc. Method for producing 3-aminomethyltetrahydrofuran derivative
WO2007116106A1 (es) 2006-04-12 2007-10-18 Palobiofarma, S.L. Nuevos compuestos como antagonistas de los receptores a1 de adenosina
DE102007061763A1 (de) 2007-12-20 2009-06-25 Bayer Healthcare Ag Substituierte azabicyclische Verbindungen und ihre Verwendung
GB0906579D0 (en) * 2009-04-16 2009-05-20 Vernalis R&D Ltd Pharmaceuticals, compositions and methods of making and using the same
SI2531492T1 (sl) 2010-02-05 2016-08-31 Heptares Therapeutics Limited Derivati 1,2,4-triazin-4-amina
WO2011159302A1 (en) 2010-06-17 2011-12-22 Janssen Pharmaceutica Nv Arylindenopyrimidines for treating neurodegenerative and movement disorders while minimizing cardiac toxicity
AU2011340721A1 (en) 2010-12-07 2013-06-20 Bayer Intellectual Property Gmbh Substituted 1-benzylcycloalkylcarboxlic acids and use thereof
TWI577671B (zh) 2011-11-14 2017-04-11 Sunshine Lake Pharma Co Ltd Aminoquinazoline derivatives and salts thereof and methods of use thereof
WO2014101120A1 (en) 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
WO2015027431A1 (en) 2013-08-29 2015-03-05 Merck Sharp & Dohme Corp. 2,2-difluorodioxolo a2a receptor antagonists
US11066413B2 (en) * 2017-03-07 2021-07-20 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5356894A (en) * 1990-05-29 1994-10-18 Rodney Peter W Morpholinyl substituted [1,2,4]-triazolo[1,5-a]triazine as antagonist
CN1278819A (zh) * 1997-09-02 2001-01-03 杜邦药品公司 作为促肾上腺皮质素释放激素拮抗剂、可用于治疗cns障碍和紧张相关性疾病的杂环基取代的环稠合吡啶和嘧啶
WO2000059907A2 (en) * 1999-04-06 2000-10-12 Du Pont Pharmaceuticals Company Pyrazolotriazines as crf antagonists
US20060106019A1 (en) * 2002-07-26 2006-05-18 Greenpharma Novel substituted pyrazolo[1,5 a]-1,3,5-triazine derivatives and their analogues, pharmaceutical compositions containing same, use thereof as medicine and methods for preparing same
WO2004110454A1 (ja) * 2003-06-13 2004-12-23 Ishihara Sangyo Kaisha, Ltd. アデノシンＡ2ａ受容体アゴニストの投与が必要な疾患を治療又は予防するための組成物
WO2017055305A1 (en) * 2015-09-30 2017-04-06 Ucb Biopharma Sprl Fused pyrazole derivatives as kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PAUL JGILLIGAN，等: "Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-Releasing factor (CRF) receptor ligands", 《BIOORGANIC & MEDICINAL CHEMISTRY》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112028891A (zh) * 2019-07-30 2020-12-04 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂
CN112608316A (zh) * 2019-07-30 2021-04-06 杭州阿诺生物医药科技有限公司 一种吡唑并三嗪类腺苷受体拮抗剂

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TW201934554A (zh) 2019-09-01
WO2019154294A1 (zh) 2019-08-15
US20210032253A1 (en) 2021-02-04
TWI701251B (zh) 2020-08-11
EP3750891A1 (en) 2020-12-16
JP2021512959A (ja) 2021-05-20
CN111511745B (zh) 2022-05-27
EP3750891A4 (en) 2021-08-11
CA3089159A1 (en) 2019-08-15

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Effective date of registration: 20230518

Address after: 222047 No. 7 Kunlun Shan Road, Lianyungang economic and Technological Development Zone, Jiangsu

Patentee after: JIANGSU HENGRUI MEDICINE Co.,Ltd.

Patentee after: Shandong Shengdi Pharmaceutical Co.,Ltd.

Patentee after: SHANGHAI HENGRUI PHARMACEUTICAL Co.,Ltd.

Address before: 222047 No. 7 Kunlun Shan Road, Lianyungang economic and Technological Development Zone, Jiangsu

Patentee before: JIANGSU HENGRUI MEDICINE Co.,Ltd.

Patentee before: SHANGHAI HENGRUI PHARMACEUTICAL Co.,Ltd.

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