AR044041A1 - Antagonistas del receptor a2a de 2-alquinil- y 2-alquenil-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina adenosina - Google Patents

Antagonistas del receptor a2a de 2-alquinil- y 2-alquenil-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina adenosina

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Publication number
AR044041A1
AR044041A1 ARP040101344A ARP040101344A AR044041A1 AR 044041 A1 AR044041 A1 AR 044041A1 AR P040101344 A ARP040101344 A AR P040101344A AR P040101344 A ARP040101344 A AR P040101344A AR 044041 A1 AR044041 A1 AR 044041A1
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AR
Argentina
Prior art keywords
alkyl
alkoxy
alkoxyalkyl
hydroxyalkyl
group
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ARP040101344A
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English (en)
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Schering Corp
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Publication of AR044041A1 publication Critical patent/AR044041A1/es

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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
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/26Psychostimulants, e.g. nicotine, ***e
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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

Abstract

La presente describe el uso de los compuestos de fórmula (1) en el tratamiento de enfermedades del SNC, en particular la enfermedad de Parkinson, solos o en combinación con otros agentes para el tratamiento de la enfermedad de Parkinson, y composiciones farmacéuticas que los comprenden. Reivindicación 1: Un compuesto que tiene la fórmula estructural (1) o su sal farmacéuticamente aceptable, en donde R es como se muestra en los restos de fórmulas (2); R1, R2, R3, R4 y R5 se seleccionan independientemente entre el grupo que consiste en H, alquilo y alcoxialquilo; R6 es H, alquilo, hidroxialquilo o -CH2F; R7, R8 y R9 se seleccionan independientemente entre el grupo que consiste en H, alquilo alcoxi, alquiltio, alcoxialquilo, halo y -CF3; Z es R10-arilo, R10-heteroarilo o como se muestra resto de fórmula (3); R10 es 1 a 5 sustituyentes seleccionados independientemente entre el grupo que consiste en H, alquilo, alquenilo, hidroxi, alcoxi, hidroxialquilo, hidroxialcoxi, alcoxialquilo, alcoxialcoxi, alcoxi-alcoxi-alquil-, (di-alcoxi)-alquilo, (hidroxi)-alcoxialquilo, R15-cicloalquilo, R15-cicloalquilalquilo, cicloalquil-oxi, cicloalquil-O-alcoxi, alquil-SO2-, alquil-SO-, halo, -CN, cianoalquilo, -CHF2, -CF3, -OCHF2, -OCF3, -C(O)R13, -O-alquilen-C(O)OR13, -C(O)O-alquilo, -N(R11)(R12), N(R11)(R12)-alquilo, -N(R11)(R12)-alcoxi, -C(O)N(R13)(R16), R11-heteroarilo, R15-heterocicloalquilo, R15-heterocicloalquil-alquilo, R15-heterocicloalquil-alcoxi, R15-heterocicloalquil-oxi, CF3-alquilen-O-alquilo, CF3-hidroxialquilo, (CF3)(hidroxi)alcoxi, ciano-alcoxi, -alquilen-C(O)-O-alquilo, -SO2-N(alquilo)2, (cicloalquil)hidroxialquilo, (hidroxialquil)alcoxi, (dihidroxi)alquilo, (dihidroxi)alcoxi, -C(=NOR17)-alquilo y -C(=NOR17)-CF3; o dos grupos R10 en átomos del anillo de C adyacentes juntos forman -O-CH2O-, -O-(CH2)2-O-, -CH2-O-(CH2)2-O-, -O-(CH2)2-, -(CH2)3-O-, -O-(CH2)3-O-, -(CH2)3-, en donde el anillo formado por los dos sustituyentes R10 y los átomos de C en el anillo al cual están unidos es sustituido con R16; o dos grupos R10 en átomos en el anillo de C adyacentes forman en forma conjunta -N(R11)-C(O)-O-, -N(R11)-C(O)-S-, -(CH2)2CH(OR18)-,-CH2CH(OR18)CH2-, -(CH2)3CH(OR18)-, -(CH2)2CH(OR18)CH2-, -(CH2)2C(O)-,-CH2C(O)CH2-, -(CH2)3C(O)-, -(CH2)2C(O)CH2-, -O(CH2)2CH(OR18)- o -OCH2CH(OR18)CH2-, en donde el anillo formado por dos sustituyentes R10 y los átomos de C en el anillo al cual están unidos es opcionalmente sustituido en un átomo de C por hidroxialquilo o alcoxialquilo; cada R11 se selecciona independientemente entre el grupo que consiste en H y alquilo; cada R12 se selecciona independientemente entre el grupo que consiste en H, alquilo, hidroxialquilo, alcoxialquilo, -C(O)-alquilo, -C(O)O-alquilo, (alcoxi)hidroxialquilo, alcoxialquil-C(O)-, -SO2alquilo, -alquilen-C(O)alquilo y -alquilen-C(O)O-alquilo; R13 es H, alquilo o -CF3; R14 es H, alquilo, alcoxialquilo, alquil-C(O)- o alcoxi-C(O)-; R15 es de 1 a 3 sustituyentes seleccionados independientemente entre el grupo que consiste en H, alquilo, -OH, alcoxi, alcoxialquilo e hidroxialquilo; o dos sustituyentes R15, tomados en forma conjunta con el C al cual ambos están unidos, forman un grupo -C(=O)-; R16 es H, alquilo, alcoxialquilo, OH o hidroxialquilo; R17 es H o alquilo; y R18 es H o alquilo.
ARP040101344A 2003-04-23 2004-04-21 Antagonistas del receptor a2a de 2-alquinil- y 2-alquenil-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina adenosina AR044041A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US46484003P 2003-04-23 2003-04-23

Publications (1)

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AR044041A1 true AR044041A1 (es) 2005-08-24

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Application Number Title Priority Date Filing Date
ARP040101344A AR044041A1 (es) 2003-04-23 2004-04-21 Antagonistas del receptor a2a de 2-alquinil- y 2-alquenil-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina adenosina

Country Status (32)

Country Link
US (2) US6897217B2 (es)
EP (1) EP1622912B1 (es)
JP (2) JP4527712B2 (es)
KR (1) KR100831107B1 (es)
CN (1) CN100503609C (es)
AR (1) AR044041A1 (es)
AT (1) ATE432282T1 (es)
AU (1) AU2004233334B2 (es)
BR (1) BRPI0409787B8 (es)
CA (1) CA2522813C (es)
CL (1) CL2004000847A1 (es)
CO (1) CO5700766A2 (es)
CY (1) CY1109263T1 (es)
DE (1) DE602004021250D1 (es)
DK (1) DK1622912T3 (es)
EC (1) ECSP056115A (es)
ES (1) ES2326270T3 (es)
HK (1) HK1085466A1 (es)
HR (1) HRP20090394T1 (es)
IL (1) IL171567A (es)
MX (1) MXPA05011366A (es)
MY (1) MY139344A (es)
NO (1) NO332182B1 (es)
NZ (1) NZ542823A (es)
PE (1) PE20050141A1 (es)
PL (2) PL378867A1 (es)
PT (1) PT1622912E (es)
RU (1) RU2373210C2 (es)
SI (1) SI1622912T1 (es)
TW (2) TWI355381B (es)
WO (1) WO2004094431A2 (es)
ZA (1) ZA200508489B (es)

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ATE490775T1 (de) * 2002-12-19 2010-12-15 Schering Corp Verwendung von a2a rezeptor-antagonisten zur behandlung des extrapyramidalen syndroms
US20060128694A1 (en) * 2002-12-19 2006-06-15 Michael Grzelak Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
TWI355381B (en) * 2003-04-23 2012-01-01 Schering Corp 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-tri
TW200538118A (en) * 2004-04-21 2005-12-01 Schering Corp Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
ATE556712T1 (de) 2005-06-07 2012-05-15 Kyowa Hakko Kirin Co Ltd A2a antagonisten zur behandlung von motorischen störungen
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AU2004233334B2 (en) 2010-08-12
EP1622912B1 (en) 2009-05-27
ES2326270T3 (es) 2009-10-06
US20040220194A1 (en) 2004-11-04
JP4527712B2 (ja) 2010-08-18
CN1777609A (zh) 2006-05-24
TWI375677B (en) 2012-11-01
EP1622912A2 (en) 2006-02-08
NO332182B1 (no) 2012-07-23
RU2373210C2 (ru) 2009-11-20
RU2005136166A (ru) 2006-06-10
PE20050141A1 (es) 2005-04-01
US20050222164A1 (en) 2005-10-06
JP2010059178A (ja) 2010-03-18
JP2006523619A (ja) 2006-10-19
CY1109263T1 (el) 2014-07-02
CA2522813A1 (en) 2004-11-04
NZ542823A (en) 2009-03-31
ATE432282T1 (de) 2009-06-15
ZA200508489B (en) 2007-04-25
PT1622912E (pt) 2009-08-17
MXPA05011366A (es) 2005-11-28
TWI355381B (en) 2012-01-01
TW201144317A (en) 2011-12-16
TW200427689A (en) 2004-12-16
CA2522813C (en) 2009-09-08
ECSP056115A (es) 2006-03-01
CL2004000847A1 (es) 2005-03-11
CN100503609C (zh) 2009-06-24
KR100831107B1 (ko) 2008-05-20
IL171567A (en) 2013-01-31
NO20055510D0 (no) 2005-11-22
HK1085466A1 (en) 2006-08-25
BRPI0409787A (pt) 2006-05-30
HRP20090394T1 (en) 2009-08-31
DE602004021250D1 (de) 2009-07-09
AU2004233334A1 (en) 2004-11-04
SI1622912T1 (sl) 2009-10-31
WO2004094431A3 (en) 2004-12-02
BRPI0409787B1 (pt) 2018-08-21
US7368449B2 (en) 2008-05-06
MY139344A (en) 2009-09-30
US6897217B2 (en) 2005-05-24
PL378867A1 (pl) 2006-05-29
KR20060005379A (ko) 2006-01-17
PL1622912T3 (pl) 2009-11-30
WO2004094431A2 (en) 2004-11-04
NO20055510L (no) 2006-01-20
CO5700766A2 (es) 2006-11-30
DK1622912T3 (da) 2009-09-07
BRPI0409787B8 (pt) 2021-05-25

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