AR040513A1 - Inhibidores de quinasas - Google Patents

Inhibidores de quinasas

Info

Publication number
AR040513A1
AR040513A1 AR20030102643A ARP030102643A AR040513A1 AR 040513 A1 AR040513 A1 AR 040513A1 AR 20030102643 A AR20030102643 A AR 20030102643A AR P030102643 A ARP030102643 A AR P030102643A AR 040513 A1 AR040513 A1 AR 040513A1
Authority
AR
Argentina
Prior art keywords
alkyl
3alkyl
group
cooh
formula
Prior art date
Application number
AR20030102643A
Other languages
English (en)
Original Assignee
Warner Lambert Co
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
Application filed by Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR040513A1 publication Critical patent/AR040513A1/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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • 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

Landscapes

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

Abstract

Se proporcionan pirimidopirimidinas, dihidropirimidopirimidinas, piridopirimidinas, naftiridinas y piridopirazinas fenil sustituidas, que inhiben las enzimas quinasa y tirosinaquinasa dependientes de la ciclina, los procedimientos y compuestos intermedios para su síntesis, así como composiciones farmacéuticas y procedimientos para su uso en tratamiento, inhibición o prevención de enfermedades asociadas con trastornos de proliferación celular, que incluyen angiogénesis, aterosclerosis, reestenosis y cáncer. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque: A es O, NH2, NH-alquilo (C1-6), N-(alquilo (C1-6))2 o -NHC(O)-NHR12; R12 es alquilo (C1-6) de cadena lineal o ramificada, o -(CH2)n-anillo cicloalquilo (C3-8), n es un número entero entre 1 y 3; B, C y D se seleccionan independientemente de CH o N con la condición de que C y D no sean ambos N; R1 se selecciona del grupo de alquilo (C1-6) de cadena lineal o ramificada, opcionalmente sustituido con -COOH o ; a) un fenilo, bencilo, o anillo cicloalquilo (C3-8) o -CH2-anillo cicloalquilo (C3-8), con los anillos del fenilo, bencilo o cicloalquilo estando sustituidos opcionalmente con 1 ó 2 grupos COOH o -CH2-COOH; o b) un resto de piperidina o piperazina seleccionado del grupo de fórmula (2) en donde los anillos de los restos de piperidina o piperazina estando sustituidos opcionalmente con 1 ó 2 grupos COOH o -CH2-COOH; o c) un resto de tetrahidropirano o morfolina de fórmula (3); R2 es H, Cl o F; R3 es H, Cl o F, con la condición de que al menos uno de R2 o R3 es F; R4 es H, OH, -OCH3, o -OCH2CH3, con la condición de que si R4 es H, R2 y R3 no son H; R5 es -OCH3, o -OCH2CH3; R6 se selecciona del grupo H, -alquil(C1-5)-NH2, -alquil(C1-5)-NH-alquil(C1-3)-R11, -alquil(C1-5)-N-(alquil(C1-3)-R11)2, O-alquil(C1-5)-NH2, -O-alquil(C1-5)-NH-alquil(C1-3)-R11, -O-alquil(C1-5)-N-(alquil(C1-3)-R11)2, -CH(CH2OH)2, -alquil(C1-3)-(CH2OH)2, -alquil(C1-3)-O-alquil(C1-3)-R11, -alquil(C1-3)-O-alquil(C1-3)-NH2, -alquil(C1-3)-O-alquil(C1-3)-NH-alquil(C1-3)-R11,-alquil(C1-3)-O-alquil(C1-3)-N-(alquilC1-3)-R11)2, fenilo sustituido con 1 ó 2 grupos seleccionados de NH2, -N-alquilo(C1-3), -N(alquilo(C1-3))2, CN o alquil(C1-3)-tetrazol, o alquilo(C1-6), o un grupo de resto de fórmula (4), con cada una de las cadenas alquilo de cualquier grupo en esta definición de R4 estando opcionalmente sustituida con de 1 a 4 grupos OH; R7 en cada caso se selecciona independientemente de H, NH2, NH-alquilo(C1-3), N-(alquilo(C1-3))2 o alquilo (C1-3); R8 es H, OH o alquilo (C1-3); R9 es H, OH, -NH2, NH-alquilo (C1-3), o N-(alquilo(C1-3))2; R10 es H o alquilo(C1-3); R11 es H, CN, OH, NH2, F o CF3; o una forma de sal o éster farmacéuticamente aceptable del mismo.
AR20030102643A 2002-07-25 2003-07-23 Inhibidores de quinasas AR040513A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US39863802P 2002-07-25 2002-07-25

Publications (1)

Publication Number Publication Date
AR040513A1 true AR040513A1 (es) 2005-04-06

Family

ID=31188438

Family Applications (1)

Application Number Title Priority Date Filing Date
AR20030102643A AR040513A1 (es) 2002-07-25 2003-07-23 Inhibidores de quinasas

Country Status (18)

Country Link
US (1) US7196090B2 (es)
EP (1) EP1549651B1 (es)
JP (1) JP2005538992A (es)
AR (1) AR040513A1 (es)
AT (1) ATE452891T1 (es)
AU (1) AU2003249442A1 (es)
BR (1) BR0312867A (es)
CA (1) CA2493633C (es)
DE (1) DE60330694D1 (es)
ES (1) ES2335659T3 (es)
GT (1) GT200300150A (es)
HN (1) HN2003000227A (es)
MX (1) MXPA05000814A (es)
PA (1) PA8577501A1 (es)
PE (1) PE20040688A1 (es)
TW (1) TW200413375A (es)
UY (1) UY27906A1 (es)
WO (1) WO2004011465A1 (es)

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CA2493633A1 (en) 2004-02-05
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PA8577501A1 (es) 2004-02-07
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AU2003249442A1 (en) 2004-02-16
US20040019210A1 (en) 2004-01-29
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MXPA05000814A (es) 2005-04-19
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US7196090B2 (en) 2007-03-27
ATE452891T1 (de) 2010-01-15
CA2493633C (en) 2009-04-07
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