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AR036106A1 - Compuestos azaindoles inhibidores de quinasa selectivos, composiciones farmaceuticas y el uso de dicha composicion para la fabricacion de un medicamento - Google Patents

Compuestos azaindoles inhibidores de quinasa selectivos, composiciones farmaceuticas y el uso de dicha composicion para la fabricacion de un medicamento

Info

Publication number
AR036106A1
AR036106A1 ARP020102348A ARP020102348A AR036106A1 AR 036106 A1 AR036106 A1 AR 036106A1 AR P020102348 A ARP020102348 A AR P020102348A AR P020102348 A ARP020102348 A AR P020102348A AR 036106 A1 AR036106 A1 AR 036106A1
Authority
AR
Argentina
Prior art keywords
ny3y4
ny1y2
heteroaryl
aryl
heterocycloalkyl
Prior art date
Application number
ARP020102348A
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English (en)
Original Assignee
Aventis Pharma Ltd
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 Aventis Pharma Ltd filed Critical Aventis Pharma Ltd
Publication of AR036106A1 publication Critical patent/AR036106A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Una composición farmacéutica que comprende una cantidad de un inhibidor quinasa selectivo de compuestos azaindol de fórmula general (1), en la cual: R1 representa arilo o heteroarilo, cada uno opcionalmente sustituido por uno o más grupos seleccionados entre alquilendioxi, alquenilo, alqueniloxi, alquinilo, arilo, ciano, halo, hidroxi, heteroarilo, heterocicloalquilo, nitro, R4, -C(=O)-R, -C(=O)-OR5, -C(=O)-NY1Y2, -NY1Y2, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-C(=O)-OR7, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -N(R6)-SO2-R7, -SO2-NY1Y2 y -Z2R; R2 representa hidrógeno, acilo, ciano, halo, alquenilo inferior, -Z2R4, -SO2-NY3Y4, -NY1Y2 o alquilo inferior opcionalmente sustituido por un sustituyente seleccionado entre arilo, ciano, heteroarilo, heterocicloalquilo, hidroxi, -Z2R4, -C(=O)-NY1Y2, -C(=O)-R, -CO2OR8, -NY3Y4, -N(R6)-C(=O)-R, -N(R6)-C(=O)-NY1Y2, -N(R6)-C(=O)-OR7, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -SO2-NY1Y2, y uno o más átomos de halógeno; R3 representa a hidrógeno, arilo, ciano, halo, heteroarilo, alquilo inferior, -Z2R4, -C(=O)-OR5 o -C(=O)-NY3Y4; R4 representa a alquilo, cicloalquilo, heterocicloalquilo o heterocicloalquilalquilo, cada uno opcionalmente sustituido por un sustituyente seleccionado entre arilo, cicloalquilo, ciano, halo, heteroarilo, heterocicloalquilo, -CHO (o un acetal cíclico de 5, 6 o 7 elementos derivado del mismo), -C(=O)-NY1Y2, -C(=O)-OR5, -NY1Y2, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -Z3R7 y uno o más grupos seleccionados entre hidroxi, alcoxi y carboxi; R5 representa hidrógeno, alquilo, alquenilo, arilo, arilalquilo, heteroarilo o heteroarilalquilo; R6 representa hidrógeno o alquilo inferior; R7 representa a alquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo; R8 representa a hidrógeno o alquilo inferior; R representa arilo, heteroarilo, alquenilo o alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, o heterocicloalquilalquilo, cada uno opcionalmente sustituido por un sustituyente seleccionado entre arilo, cicloalquilo, ciano, halo, heteroarilo, heterocicloalquilo, -CHO (o un acetal cíclico de 5, 6 o 7 elementos derivado del mismo), -C(=O)-NY1Y2, -C(=O)-OR5, -NY1Y2, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -Z3R7 y uno o más grupos seleccionados entre hidroxi, alcoxi y carboxi; X1 representa a N, CH, C-arilo, C-heteroarilo, C-heterocicloalquilo, C-heterocicloalquenilo, C-halo, C-CN, -C-R4, C-NY1Y2, C-OH, C-Z2R, C-C(=O)-R, C-C(=O)-OR5, C-C(=O)NY1Y2, C-N(R8)-C(=O)-R, C-N(R6)-C(=O)-OR7, C-N(R6)-C(=O)-NY3Y4, C-N(R6)-SO2-NY3Y4, C-N(R6)-SO2-R, C-SO2-NY3Y4, C-NO2, o C-alquenilo o C-alquinilo opcionalmente sustituido por arilo, ciano, halo, hidroxi, heteroarilo, heterocicloalquilo, nitro, -C(=O)-NY1Y2, -C(=O)-OR5, -NY1Y2, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-C(=O)-OR7, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -SO2-NY1Y2 y Z2R4; Y1 e Y2 son independientemente hidrógeno, alquenilo, arilo, cicloalquilo, heteroarilo o alquilo opcionalmente sustituido por uno o más grupos seleccionados entre arilo, halo, heteroarilo, heterocicloalquilo, hidroxi, -C(=O)-NY3Y4, -C(=O)-OR5, -NY3Y4, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, y -OR7; o el grupo NY1Y2 puede formar una amina cíclica; Y3 e Y4 son independientemente hidrógeno, alquenilo, alquilo, arilo, arilalquilo, cicloalquilo, heteroarilo o heteroarilalquilo; o el grupo -NY3Y4 puede formar una amina cíclica, Z1 representa a O o S; Z2 representa a O o S(O)n; Z3 representa a O, S(O)n, NR6; n es cero o el número entero 1 o 2; y un N-óxido, prodroga, bioisósteros de ácidos y la sal y solvato farmacéuticamente aceptables de dicho compuesto y sus N-óxidos y sus prodrogas, o sus bioisósteros de ácidos; conjuntamente con uno o más vehículos o excipientes farmacéuticamente aceptables; compuestos azaindoles, y sus prodrogas, y sales o solvatos aceptables farmacéuticamente de dichos compuestos y sus prodrogas, dentro del alcance de la fórmula (1). Dichos compuestos y composiciones tienen propiedades farmacéuticas valiosas, en particular la capacidad de inhibir las quinasas, y el uso de dichas composiciones para la fabricación de un medicamento.
ARP020102348A 2001-06-21 2002-06-21 Compuestos azaindoles inhibidores de quinasa selectivos, composiciones farmaceuticas y el uso de dicha composicion para la fabricacion de un medicamento AR036106A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0115109.1A GB0115109D0 (en) 2001-06-21 2001-06-21 Chemical compounds

Publications (1)

Publication Number Publication Date
AR036106A1 true AR036106A1 (es) 2004-08-11

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ARP020102348A AR036106A1 (es) 2001-06-21 2002-06-21 Compuestos azaindoles inhibidores de quinasa selectivos, composiciones farmaceuticas y el uso de dicha composicion para la fabricacion de un medicamento

Country Status (37)

Country Link
US (2) US6897207B2 (es)
EP (2) EP1397360A1 (es)
JP (1) JP4409938B2 (es)
KR (2) KR100977344B1 (es)
CN (1) CN100509811C (es)
AP (1) AP1739A (es)
AR (1) AR036106A1 (es)
BG (1) BG108481A (es)
BR (1) BR0210507A (es)
CA (1) CA2451678C (es)
CZ (1) CZ20033444A3 (es)
EC (1) ECSP034914A (es)
EE (1) EE200400015A (es)
GB (1) GB0115109D0 (es)
HN (1) HN2002000154A (es)
HR (1) HRP20031069A2 (es)
HU (1) HUP0400247A2 (es)
IL (1) IL159445A0 (es)
JO (1) JO2327B1 (es)
MA (1) MA27043A1 (es)
MY (1) MY137099A (es)
NO (1) NO20035476D0 (es)
NZ (2) NZ529205A (es)
OA (1) OA12637A (es)
PA (1) PA8548701A1 (es)
PE (1) PE20030155A1 (es)
PL (1) PL365067A1 (es)
RU (1) RU2326880C2 (es)
SI (1) SI21462A (es)
SK (1) SK15902003A3 (es)
TN (1) TNSN03110A1 (es)
TW (1) TWI334417B (es)
UA (1) UA85660C2 (es)
UY (1) UY27350A1 (es)
WO (1) WO2003000688A1 (es)
YU (1) YU96903A (es)
ZA (1) ZA200309648B (es)

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