PE20030477A1 - ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a - Google Patents

ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a

Info

Publication number
PE20030477A1
PE20030477A1 PE2002001009A PE2002001009A PE20030477A1 PE 20030477 A1 PE20030477 A1 PE 20030477A1 PE 2002001009 A PE2002001009 A PE 2002001009A PE 2002001009 A PE2002001009 A PE 2002001009A PE 20030477 A1 PE20030477 A1 PE 20030477A1
Authority
PE
Peru
Prior art keywords
alkyl
heteroaryl
phenyl
inhibitors
adenosine
Prior art date
Application number
PE2002001009A
Other languages
English (en)
Inventor
Deen Tulshian
Lisa S Silverman
Julius J Matasi
John P Caldwell
Eugenia Y Kiselgof
Original Assignee
Schering Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of PE20030477A1 publication Critical patent/PE20030477A1/es

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A 5-AMINO-IMIDAZOLO[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA SUSTITUIDO DE FORMULA I, DONDE: R ES R1-HETEROARILO, R10-FENILO, -C(=CH2)CH3, CH3, -CH=C(CH3)2, OXAZOL; X ES ALQUILENO C1-C6, COCH2, CONR2CH2; Y ES NR2CH2CH2NR3, OCH2CH2NR2, O, S, CH2S, (CH2)(2-3)-NR2, R5-HETEROARILO, GRUPO a, b, c, Z ES R5-FENILO, ALQUILO C1-C6, R5-HETEROARILO, DIFENILMETILO, R6CO, CUANDO Y ES GRUPO c, Z TAMBIEN ES R6-SO2, R7-NR8CO, R7NR8CS, R6OCO; CUANDO Q ES CH, Z ES FENILAMINO, PIRIDILAMINO; Z E Y SON GRUPOS d, e, ENTRE OTROS O Z E Y FORMAN UN ANILLO PIPERIDINILO, PIRROLIDINILO FUSIONADO A ARILO O HETEROARILO MONOCICLO O BICICLO; X ESTA UNIDO AL N DEL PIPERIDINILO, PIRROLIDINILO; R1 ES H, ALQUILO, CF3, HALOGENO, NO2, NR12R13, ALCOXI, ALQUILTIO, ENTRE OTROS; R2 Y R3 SON H, ALQUILO; m Y n SON 2-3; p Y q SON 0-2; Q Y Q1 SON N, CH, C-CN, COH, C-COCH3; POR LO MENOS UNO DE Q Y Q1 ES N, CH; R4 ES H, ALQUILO, R1-ARILO, R1-HETEROARILO; R5 ES H, HALOGENO, ALQUILO, HIDROXI, ALCOXI, CN, ENTRE OTROS; R6 ES ALQUILO C1-C6, R5-FENILO, TIENILO, ENTRE OTROS; R7 ES ALQUILO, R5-FENILO; R8 ES H, ALQUILO C1-C6, R7 Y R8 JUNTOS SON (CH2)p-A-(CH2)q; p Y q SON 2-3; A ES UN ENLACE, CH2, S, O.TAMBIEN SE REFIERE AL USO CON AGENTES L-DOPA, AGONISTAS DOPAMINERGICOS, INHIBIDORES DE MAO-B, INHIBIDORES DE DOPA DECARBOXILASA, INHIBIDORES COMT. LOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE ENFERMEDADES DEL SISTEMA NERVIOSO CENTRAL COMO PARKINSON
PE2002001009A 2001-10-15 2002-10-11 ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a PE20030477A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US32956701P 2001-10-15 2001-10-15

Publications (1)

Publication Number Publication Date
PE20030477A1 true PE20030477A1 (es) 2003-06-06

Family

ID=23286007

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001009A PE20030477A1 (es) 2001-10-15 2002-10-11 ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a

Country Status (16)

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

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ES2385702T3 (es) * 2005-06-07 2012-07-30 Kyowa Hakko Kirin Co., Ltd. Antagonistas de A2A para uso en el tratamiento de trastornos de la motricidad
ATE538123T1 (de) 2005-09-19 2012-01-15 Schering Corp 2-heteroarylpyrazoloä4,3-eü-1, 2, 4-triazolo-ä1,5-cü-pyrimidine als antagonisten des adenosin-a2a- rezeptors
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Also Published As

Publication number Publication date
JP4545437B2 (ja) 2010-09-15
ZA200402812B (en) 2005-04-25
HUP0401777A3 (en) 2008-06-30
JP2008297312A (ja) 2008-12-11
WO2003032996A1 (en) 2003-04-24
CA2463598C (en) 2009-09-08
JP2005506352A (ja) 2005-03-03
MY124864A (en) 2006-07-31
NZ531761A (en) 2005-10-28
CN100421663C (zh) 2008-10-01
CN1612736A (zh) 2005-05-04
MXPA04003474A (es) 2004-07-30
AU2002340184B2 (en) 2005-10-06
US20030171381A1 (en) 2003-09-11
CA2463598A1 (en) 2003-04-24
EP1435960B1 (en) 2014-07-30
HUP0401777A2 (hu) 2004-12-28
AR037243A1 (es) 2004-11-03
KR20050035155A (ko) 2005-04-15
EP1435960A1 (en) 2004-07-14
IL160878A0 (en) 2004-08-31
KR100687954B1 (ko) 2007-02-27
US6653315B2 (en) 2003-11-25

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