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AR042316A1 - NEW COMPOUNDS - Google Patents

NEW COMPOUNDS

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Publication number
AR042316A1
AR042316A1 ARP030104495A ARP030104495A AR042316A1 AR 042316 A1 AR042316 A1 AR 042316A1 AR P030104495 A ARP030104495 A AR P030104495A AR P030104495 A ARP030104495 A AR P030104495A AR 042316 A1 AR042316 A1 AR 042316A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heterocycloalkyl
heterocycle
alkenyl
Prior art date
Application number
ARP030104495A
Other languages
Spanish (es)
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR042316A1 publication Critical patent/AR042316A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

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

Abstract

La presente se refiere a compuestos de biperidina, en los cuales presenta un proceso para su preparación, intermediarios usados en ellos, formulaciones farmacéuticas que contienen dichos compuestos terapéuticamente activos y al uso de dichos compuestos activos. Tratamiento de condiciones asociados con la activación de la JNK, trastornos degenerativos neurológicos centrales o periféricos. Reivindicación 1: Un compuesto de la fórmula general (1), en el cual: R1 es arilo o heteroarilo, cada uno de los cuales está sustituido en forma opcional con uno o más de R3, OR3, OCOR3, COOR3, COR3, CONR3R4, NHCOR3, NR3R4, NHSO2R3, SO2R3, SO2NR3R4, SR3, CN, halógeno y NO2; R2 es R5, R6, COR5, COR6, CONHR5, CONHR6, CON(R6)2, COOR5, COOR6, SO2R5 o SO2R6; R3 y R4 son, en forma independiente, hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, heterociclo, heterocicloalquilo C1-6, fluoralquilo C1-6, trifluoralquilo C1-6; R5 es arilo o heteroarilo, cada uno de los cuales está sustituido en forma opcional con uno o más de R7, OR7, OCOR7, COOR7, COR7, CONR7R8, CONHOR7, NHCOR7, NR7R8, NHSO2R7, SO2R7, SO2NR7R8, SR7, R7SR8, CN, halógeno, oxígeno y NO2; R6 es hidrógeno, alquilo C1-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, heterociclo, heterocicloalquilo C1-6, heteroarilalquilo C1-6, arilalquilo C1-6, alcoxilo C1-6, o alquenilo C2-6, donde cada uno de alquilo C1-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, heterociclo, heterocicloalquilo C1-6, heteroarilalquilo C1-6, arilalquilo C1-6, alcoxilo C1-6, y alquenilo C2-6 está sustituido en forma opcional con uno o más A; R7 y R8 son, en forma independiente, hidrógeno, alquilo C1-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, alquenilo C2-6, arilo, heteroarilo, heteroarilalquilo C1-6, heterociclo, heterocicloalquilo C1-6, arilo, fluoralquilo C1-6 y cloroalquilo C1-6, donde cada uno de alquilo C1-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, alquenilo C2-6, heteroarilo, heteroarilalquilo C1-6, heterociclo y heterocicloalquilo C1-6 están sustituidos en forma opcional con uno o más B; R9 y R10 son, en forma independiente, hidrógeno, alquilo C1-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, alquenilo C2-6, heterociclo, heterocicloalquilo C1-6, heteroarilo, heteroarilalquilo C1-6, arilo o arilalquilo C1-6, donde cada uno de alquilo C1-6, cicloalquilo C3-8, (cicloalquilo C3-8)alquilo C1-6, alquenilo C2-6, heterociclo, heterocicloalquilo C1-6, heteroarilo, heteroarilalquilo C1-6, arilo o arilalquilo C1-6 están sustituidos en forma opcional con uno o más B; A es R9, OR9, OCOR9, COOR9, COR9, CONR9R10, CONHOR9, NHCOR9, NR9R10, NR9SO2R10, SO2R9, SO2NR9R10, SR9, R9SR10, CN o halógeno; B es alquilo C1-6, alcoxilo C1-6, alquilamino C1-6, di(alquil C1-6)amino o halógeno; como una de las sales o base libre.This refers to biperidine compounds, in which it presents a process for its preparation, intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and the use of said active compounds. Treatment of conditions associated with the activation of JNK, central or peripheral neurological degenerative disorders. Claim 1: A compound of the general formula (1), wherein: R1 is aryl or heteroaryl, each of which is optionally substituted with one or more of R3, OR3, OCOR3, COOR3, COR3, CONR3R4, NHCOR3, NR3R4, NHSO2R3, SO2R3, SO2NR3R4, SR3, CN, halogen and NO2; R2 is R5, R6, COR5, COR6, CONHR5, CONHR6, CON (R6) 2, COOR5, COOR6, SO2R5 or SO2R6; R3 and R4 are, independently, hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, (C3-8 cycloalkyl) C1-6 alkyl, heterocycle, C1-6 heterocycloalkyl, fluoralkyl C1-6, trifluoralkyl C1-6; R5 is aryl or heteroaryl, each of which is optionally substituted with one or more of R7, OR7, OCOR7, COOR7, COR7, CONR7R8, CONHOR7, NHCOR7, NR7R8, NHSO2R7, SO2R7, SO2NR7R8, SR7, R7SR8, CN , halogen, oxygen and NO2; R 6 is hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl, (C 3-8 cycloalkyl) C 1-6 alkyl, heterocycle, C 1-6 heterocycloalkyl, C 1-6 heteroarylalkyl, C 1-6 arylalkyl, C 1-6 alkoyl, or C 2 alkenyl -6, where each of C 1-6 alkyl, C 3-8 cycloalkyl, (C 3-8 cycloalkyl) C 1-6 alkyl, heterocycle, C 1-6 heterocycloalkyl, C 1-6 heteroarylalkyl, C 1-6 arylalkyl, C 1-6 alkoxy, and C2-6 alkenyl is optionally substituted with one or more A; R7 and R8 are independently hydrogen, C1-6 alkyl, C3-8 cycloalkyl, (C3-8 cycloalkyl) C1-6 alkyl, C2-6 alkenyl, aryl, heteroaryl, C1-6 heteroarylalkyl, heterocycle, heterocycloalkyl C1 -6, aryl, C1-6 fluoralkyl and C1-6 chloroalkyl, where each of C1-6 alkyl, C3-8 cycloalkyl, (C3-8 cycloalkyl) C1-6 alkyl, C2-6 alkenyl, heteroaryl, heteroarylalkylC1- 6, heterocycle and C1-6 heterocycloalkyl are optionally substituted with one or more B; R9 and R10 are, independently, hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl, (C 3-8 cycloalkyl) C 1-6 alkyl, C 2-6 alkenyl, heterocycle, C 1-6 heterocycloalkyl, heteroaryl, C 1-6 heteroarylalkyl , aryl or C 1-6 arylalkyl, wherein each of C 1-6 alkyl, C 3-8 cycloalkyl, (C 3-8 cycloalkyl) C 1-6 alkyl, C 2-6 alkenyl, heterocycle, C 1-6 heterocycloalkyl, heteroaryl, C 1-6 heteroarylalkyl 6, aryl or C 1-6 arylalkyl are optionally substituted with one or more B; A is R9, OR9, OCOR9, COOR9, COR9, CONR9R10, CONHOR9, NHCOR9, NR9R10, NR9SO2R10, SO2R9, SO2NR9R10, SR9, R9SR10, CN or halogen; B is C1-6 alkyl, C1-6 alkoxy, C1-6 alkylamino, di (C1-6 alkyl) amino or halogen; as one of the salts or free base.

ARP030104495A 2002-12-09 2003-12-05 NEW COMPOUNDS AR042316A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0203654A SE0203654D0 (en) 2002-12-09 2002-12-09 New compounds

Publications (1)

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AR042316A1 true AR042316A1 (en) 2005-06-15

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AR (1) AR042316A1 (en)
AU (1) AU2003302919A1 (en)
SE (1) SE0203654D0 (en)
TW (1) TW200417546A (en)
WO (1) WO2004052880A1 (en)

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WO2004052880A1 (en) 2004-06-24
AU2003302919A1 (en) 2004-06-30
TW200417546A (en) 2004-09-16
SE0203654D0 (en) 2002-12-09

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