AR035374A1 - Un derivado de fenilacetamido-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, un kit que comprende dicho derivado o composicion, un metodo para tratar desordenes proliferativos celularaes asociados con una actividad quinasa dependiente de ciclo c - Google Patents

Un derivado de fenilacetamido-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, un kit que comprende dicho derivado o composicion, un metodo para tratar desordenes proliferativos celularaes asociados con una actividad quinasa dependiente de ciclo c

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Publication number
AR035374A1
AR035374A1 ARP010105476A ARP010105476A AR035374A1 AR 035374 A1 AR035374 A1 AR 035374A1 AR P010105476 A ARP010105476 A AR P010105476A AR P010105476 A ARP010105476 A AR P010105476A AR 035374 A1 AR035374 A1 AR 035374A1
Authority
AR
Argentina
Prior art keywords
derivative
alkyl
straight
branched
formula
Prior art date
Application number
ARP010105476A
Other languages
English (en)
Inventor
Paolo Pevarello
Paolo Orsini
Gabriella Traquandi
Maria Gabriella Brasca
Raffaella Amici
Manuela Villa
Claudia Piutti
Mario Varasi
Antonio Longo
Original Assignee
Pharmacia & Upjohn Spa
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
Priority claimed from US09/907,943 external-priority patent/US6455559B1/en
Application filed by Pharmacia & Upjohn Spa filed Critical Pharmacia & Upjohn Spa
Publication of AR035374A1 publication Critical patent/AR035374A1/es

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Classifications

    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Un derivado de fenilacetamido-pirazol representado por la fórmula (1) donde R es un grupo cicloalquilo C3-C5 opcionalmente sustituido; R1 y R2 iguales o diferentes, representan hidrógeno, halógeno, amino, hidroxi o un grupo seleccionado entre alquilo C1-5 recto o ramificado opcionalmente sustituido por amino o hidroxi, alquilo C1-5 perfluorado recto o ramificado o alcoxi C1-5 recto o ramificado o tomados junto con el átomo de carbono al cual están unidos, R1 y R2 forman un grupo exometileno (>C=CH2) o un grupo cicloalquilo C3-4; R3, en posición 3 o 4 del anillo fenilo, es un grupo de la fórmula (2) representando un heterociclo que contiene nitrógeno saturado o insaturado con 5 o 6 miembros; que, opcionalmente, contiene entre 1 y 2 heteroátomos adicionales, iguales o diferentes, seleccionados entre nitrógeno, oxígeno o azufre; opcionalmente sustituido en cualquiera de las posiciones libres por uno o más grupos seleccionados entre halógeno, hidroxi, aminocarbonilo, alquilamino carbonilo C1-4; grupos oxo (>C = O, >S = O, >SO2); exometileno (>C=CH2); grupos alquiloC1-4 recto o ramificado, alquilo perfluorado, hidroxialquilo o alcoxi; grupos arilo o alquenilo C2-4; opcionalmente condensados con anillos carbocíclicos o heterocíclicos, saturados o insaturados, monocíclicos o bicíclicos, cada un de los cuales se encuentra opcional o adicionalmente sustituido como se define previamente; m es 0 o un entero de 1 a 4; de estar presente, cada R4 es el mismo o diferente, halógeno, hidroxi o un grupo seleccionado entre alquilo C1-4 recto o ramificado, alcoxi o alquilo perfluorado; o una sal farmacéuticamente aceptable del mismo; siempre que: a) cuando R es ciclopropilo y R1 y R2 son ambos átomos de hidrógeno, entonces el heterociclo que contiene nitrógeno de fórmula (2) es distinto a 1-pirrolidinilo, 2-oxo-1-pirrolidinilo o 1,2, 3-triazol-1-ilo; y b) cuando R es ciclopropilo, uno de R1 y R2 es un átomo de hidrógeno y el otro es metilo, etilo, n-propilo o n-butilo, entonces el heterociclo que contiene nitrógeno de fórmula (2) es distinto a los 1,3-dihidro-2H-isoindol-2-il o 1-oxo-1,3-dihidro-2H-isoindol-2-ilo. Su uso en la elaboración de un medicamento, métodos para la preparación de un compuesto, una composición farmacéutica que lo comprende y un kit que comprende el derivado o la composición. El derivado de fórmula (1) es útil en el tratamiento de desórdenes proliferativos celulares asociados con una actividad de quinasa con dependencia del ciclo celular alterado. Más específicamente, es útil en el tratamiento de cáncer, hiperplasia benigna de la próstata, adenomatosis familiar, poliposis, neurofibromatosis, psoriasis, proliferación de célula lisa vascular asociada con la atrosclerosis, fibrosis pulmonar, artritis, glomerulonefritis, estenosis y reestenosis post-quirúrgica, enfermedad de Alzheimer, infecciones virales, enfermedades autoinmunes , desordenes neurodegenerativos, en la prevención del desarrollo de SIDA en personas infectadas con HIV y en la inhibición de la angiogénesis y metástasis de tumores. También es útil en el tratamiento y prevención de la alopecia inducida por radioterapia o quimioterapia.
ARP010105476A 2000-11-27 2001-11-26 Un derivado de fenilacetamido-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, un kit que comprende dicho derivado o composicion, un metodo para tratar desordenes proliferativos celularaes asociados con una actividad quinasa dependiente de ciclo c AR035374A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25291100P 2000-11-27 2000-11-27
US09/907,943 US6455559B1 (en) 2001-07-19 2001-07-19 Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents

Publications (1)

Publication Number Publication Date
AR035374A1 true AR035374A1 (es) 2004-05-12

Family

ID=26942786

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010105476A AR035374A1 (es) 2000-11-27 2001-11-26 Un derivado de fenilacetamido-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, un kit que comprende dicho derivado o composicion, un metodo para tratar desordenes proliferativos celularaes asociados con una actividad quinasa dependiente de ciclo c

Country Status (10)

Country Link
US (1) US20040019046A1 (es)
EP (1) EP1345909A1 (es)
JP (1) JP2004517840A (es)
AR (1) AR035374A1 (es)
AU (1) AU2002215053A1 (es)
CA (1) CA2430151A1 (es)
MX (1) MXPA03004644A (es)
NZ (1) NZ525892A (es)
PE (1) PE20020566A1 (es)
WO (1) WO2002048114A1 (es)

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US7244757B2 (en) 2004-04-01 2007-07-17 Pfizer Inc Pyrazole-amine compounds for the treatment of neurodegenerative disorders
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GB0507575D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds
JP5303271B2 (ja) 2005-07-19 2013-10-02 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として有用な１Ｈ−チエノ［２，３−ｃ］ピラゾール化合物
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Also Published As

Publication number Publication date
PE20020566A1 (es) 2002-06-22
US20040019046A1 (en) 2004-01-29
JP2004517840A (ja) 2004-06-17
MXPA03004644A (es) 2003-09-05
EP1345909A1 (en) 2003-09-24
WO2002048114A1 (en) 2002-06-20
CA2430151A1 (en) 2002-06-20
NZ525892A (en) 2004-11-26
AU2002215053A1 (en) 2002-06-24

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