AR037487A1 - Compuestos derivados de pirimidina, proceso para prepararlos, composicion farmaceutica y el uso de los mismos en la fabricacion de medicamentos que producen un efecto inhibidor del ciclo celular (anti-proliferacion celular) - Google Patents

Compuestos derivados de pirimidina, proceso para prepararlos, composicion farmaceutica y el uso de los mismos en la fabricacion de medicamentos que producen un efecto inhibidor del ciclo celular (anti-proliferacion celular)

Info

Publication number
AR037487A1
AR037487A1 ARP020100543A ARP020100543A AR037487A1 AR 037487 A1 AR037487 A1 AR 037487A1 AR P020100543 A ARP020100543 A AR P020100543A AR P020100543 A ARP020100543 A AR P020100543A AR 037487 A1 AR037487 A1 AR 037487A1
Authority
AR
Argentina
Prior art keywords
alkyl
carbamoyl
sulfamoyl
amino
optionally substituted
Prior art date
Application number
ARP020100543A
Other languages
English (en)
Inventor
Andrew Peter Thomas
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 AR037487A1 publication Critical patent/AR037487A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • 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
    • 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
    • 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

Abstract

Compuestos derivados de pirimidina caracterizado porque tiene la fórmula (1), donde: el anillo A es un grupo de fórmula (2) ó (3), donde uno o más de X1, X2, X3 y X4 son nitrógeno y los otros son CR5 donde los valores de R5 pueden ser iguales o diferentes; R1 es halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, (alquil C1-6)S(O)a donde a es entre 1 y 2, N-(alquil C1-6)sulfamoilo o N,N-(alquil C1-6)2sulfamoilo; donde R1 puede ser opcionalmente sustituido en un carbono por uno o más R6, R2 y R5 se seleccionan independientemente entre sí entre hidrógeno, halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, (alquil C1-6)S(O)a donde a es entre 1 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamoilo, fenilo, grupo heterocíclico, feniltio o (grupo heterocíclico)tio; donde cualquier R2 o R5 puede ser opcionalmente sustituido en un carbono por uno o más R7; y donde si dicho grupo heterocíclico contiene una porción -NH- ese nitrógeno puede ser opcionalmente sustituido por un grupo seleccionado entre R8, n es entre 1 y 2, donde los valores de R1 pueden ser iguales o diferentes; R3 es halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquenilo C2-6, o alquinilo C2-6; p es 0-4; donde los valores de R3 pueden ser iguales o diferentes; R4 es un grupo A-E-; donde A se selecciona entre alquilo C1-6, fenilo, un grupo heterocíclico, cicloalquilo C3-8, fenil alquilo C1-6, (grupo heterocíclico)alquilo C1-6 o cicloalquil C3-8 alquilo C1-6; donde A puede ser opcionalmente sustituido en un carbono por uno o más R9; y donde si dicho grupo heterocíclico contiene una porción -NH- ese nitrógeno puede ser opcionalmente sustituido por un grupo seleccionado entre R10; E es un enlace directo o -O-, -C(O)-, -OC(O)-, -C(O)O-, -N(Ra)C(O)-, -C(O)N(Ra)-, -N(Ra)-, -S(O)a-, -SO2N(Ra)- o -N(Ra)SO2-; donde Ra es hidrógeno o alquilo C1-6 opcionalmente sustituido por uno o más R11 y a es 0-2, R9 se selecciona independientemente entre oxo, halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, (alquil C1-6)S(O)a donde a es entre 1 y 2, alcoxicarbonilo C1-6, alcoxicarbonilamino C1-6, benciloxicarbonilamino, N-(alquil C1-6)sulfamoilo y N,N-(alquil C1-6)2sulfamoilo; donde R9 puede ser opcionalmente sustituido en un carbono por uno o más R12; q es 0-2; donde los valores de R4 pueden ser iguales o diferentes; y donde p + q L 5; R6, R7, R11 y R12 se seleccionan independientemente entre halo, nitro, ciano, hidroxi, trifluorometoxi, trifluorometilo, amino, carboxi, carbamoilo, mercapto, sulfamoilo, metilo, etilo, metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etialmino, acetilamino, N-metilcarbamoilo, N-etilcarbamoilo, N,N-dimetilcarbamoilo, N,N-dietilcarbamoilo, N-metil-N-etilcarbamoilo, metiltio, etiltio, metilsulfinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoilo, N-etilsulfamoilo, N,N-dimetilsulfamoilo, N,N-dietilsulfamoilo o N-metil-N-etilsulfamoilo; y R8 y R10 se seleccionan independientemente entre alquilo C1-4, alcanoilo C1-4, alquilsulfonilo C1-4, alcoxicarbonilo C1-4, carbamoilo N-(alquil C1-4)carbamoilo, N,N-(alquil C1-4)carbamoilo, bencilo, benciloxicarbonilo, benzoílo y fenilsulfonilo, o una sal aceptable para uso farmacéutico o un éster hidrolizable en vivo del mismo. También se describen composiciones farmacéuticas que los comprenden, procesos para su preparación y el uso de los mismos en la fabricación de medicamentos que producen un efecto inhibidor del ciclo celular y son útiles para el tratamiento de distintos tipos de cánceres, trastornos fibroproliferativos y de diferenciación, psoriasis, artritis, reumatoidea, sarcoma de Kaposi, hemangioma, nefropatías agudas y crónicas, ateroma, aterosclerosis, restenosis arterial, enfermedades autoinmunes, inflamación aguda y crónica, enfermedades óseas y enfermedades oculares con proliferación de los vasos retinales.
ARP020100543A 2001-02-17 2002-02-15 Compuestos derivados de pirimidina, proceso para prepararlos, composicion farmaceutica y el uso de los mismos en la fabricacion de medicamentos que producen un efecto inhibidor del ciclo celular (anti-proliferacion celular) AR037487A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0103926.2A GB0103926D0 (en) 2001-02-17 2001-02-17 Chemical compounds

Publications (1)

Publication Number Publication Date
AR037487A1 true AR037487A1 (es) 2004-11-17

Family

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ARP020100543A AR037487A1 (es) 2001-02-17 2002-02-15 Compuestos derivados de pirimidina, proceso para prepararlos, composicion farmaceutica y el uso de los mismos en la fabricacion de medicamentos que producen un efecto inhibidor del ciclo celular (anti-proliferacion celular)

Country Status (22)

Country Link
US (1) US6844341B2 (es)
EP (1) EP1362050B1 (es)
JP (1) JP4421189B2 (es)
KR (1) KR100829035B1 (es)
CN (1) CN1307179C (es)
AR (1) AR037487A1 (es)
AT (1) ATE288436T1 (es)
AU (1) AU2002231960B2 (es)
BR (1) BR0207294A (es)
CA (1) CA2438646C (es)
DE (1) DE60202844T2 (es)
DK (1) DK1362050T3 (es)
ES (1) ES2236494T3 (es)
GB (1) GB0103926D0 (es)
IL (2) IL157282A0 (es)
MX (1) MXPA03007351A (es)
MY (1) MY136643A (es)
NO (1) NO326831B1 (es)
NZ (1) NZ527367A (es)
PT (1) PT1362050E (es)
WO (1) WO2002066481A1 (es)
ZA (1) ZA200306081B (es)

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