AR034137A1 - Un compuesto de biciclo-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, y una biblioteca quimica combinatoria - Google Patents

Un compuesto de biciclo-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, y una biblioteca quimica combinatoria

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Publication number
AR034137A1
AR034137A1 ARP010103806A ARP010103806A AR034137A1 AR 034137 A1 AR034137 A1 AR 034137A1 AR P010103806 A ARP010103806 A AR P010103806A AR P010103806 A ARP010103806 A AR P010103806A AR 034137 A1 AR034137 A1 AR 034137A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
optionally
different
same
Prior art date
Application number
ARP010103806A
Other languages
English (en)
Inventor
Valeria Pittala
Daniele Fancelli
Mario Varasi
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.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=24549630&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR034137(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmacia & Upjohn Spa filed Critical Pharmacia & Upjohn Spa
Publication of AR034137A1 publication Critical patent/AR034137A1/es

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    • 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
    • C07D487/02—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 two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Un compuesto de biciclo-pirazol de fórmula (1), en la cual: R y R1, iguales o diferentes, son independientemente un átomo de hidrógeno o un grupo opcionalmente sustituido seleccionado entre R', -COR', -COOR', -CONHR', -CONR'R'', -NH-C(=NH)NHR', -C(=NH)NHR'. -SO2R', -SO2NHR', o -SO2NR'R''; en donde R' y R'', iguales o diferentes, son seleccionados independientemente entre hidrógeno o arilo alquilo C1-6, cicloalquilo C3-6, arilo o alquilo C1-6, rectos o ramificados, opcional y adicionalmente sustituido, o R' y R'' tomados juntos forman una cadena alquileno C4-6; Ra, Rb, Rc y Rd, iguales o diferentes, son seleccionados independientemente entre hidrógeno, grupos -CH2OR', aril- alquilo C1-6, aril- alquilo C1-6, rectos o ramificados, opcional- y adicionalmente sustituidos, en donde R' es como se definió más arriba o Ra y Rb y/o Rc y Rd, tomados junto con el átomo de carbono al cual está unidos, forman un grupo cicloalquilo C3-6 opcionalmente sustituido; m y n, cada uno independientemente, representa 0 o un número entero de 1 a 2, con la condición de que m + n sea menor que, o igual a, 2 (m + n </= 2); y la sal farmacéuticamente aceptable del mismo. Su uso, un procedimiento para prepararlo, una composición farmacéutica que lo comprende, y una biblioteca química combinatoria que comprende una pluralidad de miembros de fórmula (2) en donde: R y R1, iguales o diferentes, son independientemente un átomo de hidrógeno o un grupo sustituido opcionalmente seleccionado entre R', -COR', -COOR', -CONHR', -CONR'R'', NH-C(=NH)NHR', -C(=NH)NHR', -SO2R', -SO2NHR', o -SO2NR'R'', iguales o diferentes, son seleccionados independientemente entre hidrógeno o arilo alquilo C1-6, cicloalquilo C3-6, arilo o alquilo C1-6, rectos o ramificados, opcional y adicionalmente sustituidos, o R' y R'' tomados juntos forman una cadena alquileno C4-6; Ra, Rb, Rc y Rd, iguales o diferentes, son seleccionados entre hidrógeno, grupos -CH2OR', arilo alquilo C1-6, o alquilo C1-6, rectos o ramificados, opcional y adicionalmente sustituidos, en donde R es como se definió más arriba o Ra y Rb y/o Rc y Rd, tomados junto con el átomos de carbono al cual está unidos, forman un grupo cicloalquilo C3-6 opcionalmente sustituido; m y n, cada uno independientemente, representa 0 o un número entero de 1 a 2, con la condición de que m + n sea menor que, o igual a, 2 (m + n </= 2). Los compuestos de fórmula (1) son útiles para el tratamiento de enfermedades ligadas a las proteínas quinasas desreguladas.
ARP010103806A 2000-08-10 2001-08-09 Un compuesto de biciclo-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, y una biblioteca quimica combinatoria AR034137A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US63591400A 2000-08-10 2000-08-10

Publications (1)

Publication Number Publication Date
AR034137A1 true AR034137A1 (es) 2004-02-04

Family

ID=24549630

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010103806A AR034137A1 (es) 2000-08-10 2001-08-09 Un compuesto de biciclo-pirazol, su uso, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende, y una biblioteca quimica combinatoria

Country Status (29)

Country Link
US (3) US7541354B2 (es)
EP (1) EP1320531B1 (es)
JP (2) JP4555547B2 (es)
KR (1) KR100904157B1 (es)
CN (2) CN102060857A (es)
AR (1) AR034137A1 (es)
AT (1) ATE480539T1 (es)
AU (2) AU8765401A (es)
BR (1) BR0113176A (es)
CA (1) CA2416527C (es)
CY (1) CY1110914T1 (es)
CZ (1) CZ2003591A3 (es)
DE (1) DE60143041D1 (es)
DK (1) DK1320531T3 (es)
EA (1) EA006381B1 (es)
EE (1) EE05405B1 (es)
ES (1) ES2349762T3 (es)
HU (1) HU229824B1 (es)
IL (2) IL153997A0 (es)
MX (1) MXPA03001169A (es)
MY (1) MY148632A (es)
NO (1) NO325530B1 (es)
NZ (1) NZ524475A (es)
PE (1) PE20020274A1 (es)
PL (1) PL213199B1 (es)
PT (1) PT1320531E (es)
SK (1) SK1882003A3 (es)
WO (1) WO2002012242A2 (es)
ZA (1) ZA200301813B (es)

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