CN100421663C - 咪唑并(4,3-E),1,2,4-三唑并(1,5-C)嘧啶类化合物作为腺苷A2a受体拮抗剂 - Google Patents

咪唑并(4,3-E),1,2,4-三唑并(1,5-C)嘧啶类化合物作为腺苷A2a受体拮抗剂 Download PDF

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Publication number
CN100421663C
CN100421663C CNB028203283A CN02820328A CN100421663C CN 100421663 C CN100421663 C CN 100421663C CN B028203283 A CNB028203283 A CN B028203283A CN 02820328 A CN02820328 A CN 02820328A CN 100421663 C CN100421663 C CN 100421663C
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China
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alkoxyl
alkyl
heteroaryl
chemical compound
formula
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Expired - Fee Related
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CNB028203283A
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English (en)
Chinese (zh)
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CN1612736A (zh
Inventor
D·图尔施安
L·S·西尔弗曼
J·J·马塔西
E·Y·基谢戈夫
J·P·卡德维尔
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Merck Sharp & Dohme LLC
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Schering Corp
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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
    • C07D487/12—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 three hetero rings
    • C07D487/14—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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • 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
    • 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
    • A61P25/14—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/10—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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CNB028203283A 2001-10-15 2002-10-11 咪唑并(4,3-E),1,2,4-三唑并(1,5-C)嘧啶类化合物作为腺苷A2a受体拮抗剂 Expired - Fee Related CN100421663C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32956701P 2001-10-15 2001-10-15
US60/329,567 2001-10-15

Publications (2)

Publication Number Publication Date
CN1612736A CN1612736A (zh) 2005-05-04
CN100421663C true CN100421663C (zh) 2008-10-01

Family

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Family Applications (1)

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CNB028203283A Expired - Fee Related CN100421663C (zh) 2001-10-15 2002-10-11 咪唑并(4,3-E),1,2,4-三唑并(1,5-C)嘧啶类化合物作为腺苷A2a受体拮抗剂

Country Status (16)

Country Link
US (1) US6653315B2 (enExample)
EP (1) EP1435960B1 (enExample)
JP (2) JP4545437B2 (enExample)
KR (1) KR100687954B1 (enExample)
CN (1) CN100421663C (enExample)
AR (1) AR037243A1 (enExample)
AU (1) AU2002340184B2 (enExample)
CA (1) CA2463598C (enExample)
HU (1) HUP0401777A3 (enExample)
IL (1) IL160878A0 (enExample)
MX (1) MXPA04003474A (enExample)
MY (1) MY124864A (enExample)
NZ (1) NZ531761A (enExample)
PE (1) PE20030477A1 (enExample)
WO (1) WO2003032996A1 (enExample)
ZA (1) ZA200402812B (enExample)

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MXPA05006790A (es) 2002-12-19 2005-09-08 Schering Corp Usos de antagonistas del receptor adenosina a2a.
EP1622912B1 (en) 2003-04-23 2009-05-27 Schering Corporation 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists
EA200501924A1 (ru) * 2003-06-10 2006-06-30 Киова Хакко Когио Ко., Лтд. Способ лечения тревожного расстройства
CA2550071A1 (en) * 2003-12-19 2005-07-07 Schering Corporation Pharmaceutical compositions
ATE461932T1 (de) 2004-04-21 2010-04-15 Schering Corp Pyrazoloä4,3-eü-1,2,4-triazoloä1,5-cüpyrimidine als antagonisten des adenosin-a2a-rezeptors
JPWO2006132275A1 (ja) 2005-06-07 2009-01-08 協和醗酵工業株式会社 運動障害の予防および/または治療剤
AR057817A1 (es) * 2005-09-19 2007-12-19 Schering Corp Antagonistas del receptor a2a de 2-heteroaril-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidin adenosina. composiciones farmaceuticas
AR056080A1 (es) * 2005-09-23 2007-09-19 Schering Corp 7-[2-[4-(6-fluoro-3-metil-1,2-benciosoxazol-5-il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c] -pirimidin-5-amine
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
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US8835426B2 (en) * 2007-02-26 2014-09-16 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1
US7691869B2 (en) 2007-03-30 2010-04-06 King Pharmaceuticals Research And Development, Inc. Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity
JP5451611B2 (ja) * 2007-07-26 2014-03-26 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1のサイクリックインヒビター
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JP2011513417A (ja) 2008-03-04 2011-04-28 シェーリング コーポレイション アデノシンA2a受容体アンタゴニストとして使用するための1,2,4−トリアゾロ[4,3−c]ピリミジン−3−オンおよびピラゾロ[4,3−e]−1,2,4−トリアゾロ[4,3−c]ピリミジン−3−オン化合物
CA2718264A1 (en) * 2008-03-18 2009-09-24 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
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MXPA04003474A (es) 2004-07-30
CN1612736A (zh) 2005-05-04
PE20030477A1 (es) 2003-06-06
JP2005506352A (ja) 2005-03-03
KR100687954B1 (ko) 2007-02-27
US20030171381A1 (en) 2003-09-11
HUP0401777A3 (en) 2008-06-30
NZ531761A (en) 2005-10-28
IL160878A0 (en) 2004-08-31
AR037243A1 (es) 2004-11-03
CA2463598C (en) 2009-09-08
ZA200402812B (en) 2005-04-25
AU2002340184B2 (en) 2005-10-06
MY124864A (en) 2006-07-31
WO2003032996A1 (en) 2003-04-24
US6653315B2 (en) 2003-11-25
HUP0401777A2 (hu) 2004-12-28
CA2463598A1 (en) 2003-04-24
EP1435960A1 (en) 2004-07-14
EP1435960B1 (en) 2014-07-30
JP2008297312A (ja) 2008-12-11
JP4545437B2 (ja) 2010-09-15
KR20050035155A (ko) 2005-04-15

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