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AR048617A1 - Antagonistas del receptor a2a de la adenosina con estructura de pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina. - Google Patents

Antagonistas del receptor a2a de la adenosina con estructura de pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina.

Info

Publication number
AR048617A1
AR048617A1 ARP050101559A ARP050101559A AR048617A1 AR 048617 A1 AR048617 A1 AR 048617A1 AR P050101559 A ARP050101559 A AR P050101559A AR P050101559 A ARP050101559 A AR P050101559A AR 048617 A1 AR048617 A1 AR 048617A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
hydroxyalkyl
group
alkoxyalkyl
Prior art date
Application number
ARP050101559A
Other languages
English (en)
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34966464&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR048617(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR048617A1 publication Critical patent/AR048617A1/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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a antagonistas del receptor A2A de la adenosina con estructura de pirazolo-[4,3-E]-1,2,4-triazolo-[1,5-C]-pirimidina, y composiciones farmacéuticas que los contienen y usos. Reivindicacion 1: Un compuesto que tiene la formula estructural (1) o una sal aceptable para uso farmacéutico del mismo, donde R es R6-fenilo, R6-furanilo, R6-tienilo, R6-piridilo, R6-piridilo N-oxido, R6-oxazolilo, R6-pirrolilo o cicloalquenilo; R1, R2, R3, R4 y R5 se seleccionan independientemente del grupo integrado por H, alquilo y alcoxialquilo; R6 es 1 a 3 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, -CF3, halogeno, -NO2, -CN, -NR7R8, alcoxi, alquiltio, alquilsulfinilo y alquilsulfonilo; R7 es H o alquilo; R8 es H, alquilo, alquilC(O)- o alquil-SO2-; Z es R9, R10-arilo o R9,R10-heteroarilo; R9 es alquenilo, hidroxialquilo, alcoxialquilo, alcoxi-alcoxi-alquilo-, (di-alcoxi)-alquilo, (hidroxi)-alcoxialquilo, R15-cicloalquilo, R15- cicloalquilalquilo, cicloalquil-oxi, cicloalquil-O-alcoxi, cianoalquilo, -C(O)R13, -N(R11)(R12), N(R11)(R12)-alquilo-, -C(O)N(R13)(R16), -alquilen-C(O)-N(R11)2, -C(O)-(R15-heterocicloalquilo), R15-heterocicloalquil-alquilo, R15-heterocicloalquil- alcoxi, R19-heteroarilo, 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 o - C(=NOR17)-CF3; R10 es 1 a 3 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, alquenilo, hidroxi, alcoxi, hidroxialquilo, hidroxialcoxi, alcoxialquilo, alcoxialcoxi, alcoxi-alcoxi-alquilo-, (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), R19-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 un grupo R9 y un grupo R10 en átomos de anillos de C adyacentes juntos forman -O-(CH2)2-O-, -CH2-O-(CH2)2-O-, -O-(CH2)2-, -(CH2)3-O-, -O-(CH2)3-O-, -(CH2)3- o -CH2-CH=CH-, done el anillo formado por los sustituyentes R9 y R10 y los átomos de C del anillo al cual están unidos están sustituidos con R16; o un grupo R9 y un grupo R10 en átomos de anillos de C adyacentes juntos forman -N(R11)-C(O)-O-, -N(R11)-C(O)-S- o -N(R12)-(CH2)2-; o un grupo R9 y un grupo R10 en átomos de anillos de C adyacentes juntos forman -(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-, donde el anillo formado por los sustituyentes R9 y R10 y los átomos de C del anillo al cual están unidos está sustituido opcionalmente en un átomo de C con hidroxialquilo o alcoxialquilo; cada R11 se selecciona independientemente del grupo integrado por H y alquilo; cada R12 se selecciona independientemente del grupo integrado por H, alquilo, cicloalquilo, 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, R15 es 1 a 3 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, -OH, alcoxi, alcoxialquilo e hidroxialquilo, o dos sustituyentes R15, tomados junto con el C al cual están unidos, forman un grupo -C(=O)-, R16 es H, alquilo, alcoxialquilo, OH o hidroxialquilo; R17 es H o alquilo; R18 es H o alquilo, y R19 es 1 o 2 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, hidroxialquilo, alcoxialquilo, -C(O)N(R11)(R12) y -N(R11)2.
ARP050101559A 2004-04-21 2005-04-20 Antagonistas del receptor a2a de la adenosina con estructura de pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina. AR048617A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56391304P 2004-04-21 2004-04-21
US60996604P 2004-09-15 2004-09-15

Publications (1)

Publication Number Publication Date
AR048617A1 true AR048617A1 (es) 2006-05-10

Family

ID=34966464

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050101559A AR048617A1 (es) 2004-04-21 2005-04-20 Antagonistas del receptor a2a de la adenosina con estructura de pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina.

Country Status (16)

Country Link
US (1) US7709492B2 (es)
EP (1) EP1745047B1 (es)
JP (2) JP2007533754A (es)
KR (1) KR20060135901A (es)
AR (1) AR048617A1 (es)
AT (1) ATE461932T1 (es)
AU (1) AU2005236059B2 (es)
CA (1) CA2563635A1 (es)
DE (1) DE602005020127D1 (es)
ES (1) ES2342082T3 (es)
IL (1) IL178674A0 (es)
MX (1) MXPA06012231A (es)
NZ (1) NZ550591A (es)
PE (1) PE20060185A1 (es)
TW (1) TW200538118A (es)
WO (1) WO2005103055A1 (es)

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WO2005103055A1 (en) 2005-11-03
PE20060185A1 (es) 2006-03-20
US20050239795A1 (en) 2005-10-27
NZ550591A (en) 2010-10-29
JP2008231111A (ja) 2008-10-02
HK1095818A1 (en) 2007-05-18
AU2005236059B2 (en) 2009-01-15
KR20060135901A (ko) 2006-12-29
US7709492B2 (en) 2010-05-04
EP1745047A1 (en) 2007-01-24
DE602005020127D1 (de) 2010-05-06
JP2007533754A (ja) 2007-11-22
ATE461932T1 (de) 2010-04-15
MXPA06012231A (es) 2006-12-15
IL178674A0 (en) 2007-02-11
ES2342082T3 (es) 2010-07-01
TW200538118A (en) 2005-12-01
EP1745047B1 (en) 2010-03-24
CA2563635A1 (en) 2005-11-03
AU2005236059A1 (en) 2005-11-03

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