AR059187A1 - Derivados de imidazo[1,5a]pirazina inhibidores de quinasas mtor, utiles para el tratamiento del cancer, y composiciones farmaceuticas que los contienen. - Google Patents

Derivados de imidazo[1,5a]pirazina inhibidores de quinasas mtor, utiles para el tratamiento del cancer, y composiciones farmaceuticas que los contienen.

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Publication number
AR059187A1
AR059187A1 ARP070100329A ARP070100329A AR059187A1 AR 059187 A1 AR059187 A1 AR 059187A1 AR P070100329 A ARP070100329 A AR P070100329A AR P070100329 A ARP070100329 A AR P070100329A AR 059187 A1 AR059187 A1 AR 059187A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
aryl
nr31c
nr31r32
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ARP070100329A
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English (en)
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Osi Pharm Inc
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Publication of AR059187A1 publication Critical patent/AR059187A1/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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • 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
    • 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
    • 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
    • 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

Abstract

Reivindicacion 1: Un compuesto representado por la formula (1) o una sal farmacéuticamente aceptable del mismo, donde: X1 y X2 son cada uno independientemente N o C-(E1)aa; X5 es N, C-(E1)aa, o N-(E1)aa; X3, X4, X6, y X7 son cada uno independientemente N o C; donde por lo menos uno de X3, X4, X5, X6, y X7 es independientemente N o N-(E1)aa, R3 es aIquiIo C0-10, cicloalquilo C3-10, aminometilcicloalquilo C3-10, bicicIoalquilo C5-10, arilo, heteroarilo, aralquilo, heteroaralquilo, heterociclilo o heterobicicloalquilo C5-10 cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes G11 independientes; Q1 es -A-(K)m; A es vinilo o acetilenilo; K es independientemente, hidrogeno, -N(alquil C0-8)(alquil C0- 8), hidroxilo, halogeno, oxo, arilo (opcionalmente sustituido con uno o más grupos R31), hetarilo (opcionalmente sustituido con uno o más grupos R31), alquilo C0-6, -alquil C0-8-cicloalquilo C3-8, -aIquil C0-8-NR311S(O)0-2R321, -alquil C0-8- NR311S(O)0-2NR321R331, -alquil C0-8-NR311CO2R321, -alquil C0-8-CON(R311)S(O)0-2R321, -alquil C0-8-S(O)0-2NR311R321, -alquil C0-8-NR311COR321, -alquil C0-8-NR311CONR321R331, -alquil C0-8-CONR311R321, -alquil C0-8-CO2R311, -alquil C0-8-COR311, -alquil C0-8-S(O)0-2R311, -aIquil C0-8-O-alquilo C1-8, -alquil C0-8-O-alquil C0-8-cicloalquilo C3-8, -alquil C0-8-O-alquil C0-8-heterocicloalquilo, -alquil C0-8-O-alquil C0-8-arilo, -alquil C0-8-O-alquil C0-8-hetarilo, -alquil C0-8-arilo, -alquil C0-8- hetarilo, -alquil C0-8-heterociclilo, -alquil C0-8-S-alquilo C0-8, alquil C0-8-S-alquil C0-8-cicloalquilo C3-8, -alquil C0-8-S-alquil C0-8-heterocicloalquilo, -alquil C0-8-S-aIquil C0-8-arilo, -alquil C0-8-S-alquil C0-8-hetarilo, - alquil C0-8- N(R311)-alquilo C0-8, -alquil C0-8-N(R311)-alquil C0-8-cicloalquilo C3-8, - alquil C0-8-N(R311)-alquil C0-8-heterocicloalquilo, -alquil C0-8-N(R311)-alquil C0-8-arilo, - alquil C0-8-N(R311 )-alquil C0-8-hetarilo, -alquil C0-8-NR311R321, -alquenilo C2-8, - alquinilo C2-8, NO2, CN, CF3, OCF3, OCHF2; R31, R32, R33, R311, R321, R331, R312, R322, R332, R341, R313, R323, R333, y R342 en cada caso, es independientemente alquilo C0-8 opcionalmente sustituido con 1-6 sustituyentes independientes arilo, ciclilo, heterociclilo, hetarilo, halo, -CON(alquil C0-8)(alquil C0-8), -CO(alquil C0-8), -O-alquilo C0-8, -Oarilo, -Ohetarilo, -Oheterociclilo, -S(O)0-2arilo, -S(O)0-2hetarilo, -S(O)0-2heterociclilo, -S(O)2-alquilo C0-8, -N(alquil C0- 8)(alquil C0-8), -N(alquil C0-8)CON(alquil C0-8)(alquil C0-8), -N(alquil C0-8)CO(alquil 0-8), -N(alquil C0-8)CO(cicloalquil C3-8), -N(alquil C0-8)CO2(alquil C0-8), -S(O)1-2N(alquil C0-8)(alquil C0-8),-NR11S(O)1-2(alquil C0-8), -CON(cicloalquil C3- 8)(cicloalquil C3-8), -CON(alquil C0-8)(cicloalquil C3-8), -N(cicloalquil C3-8)CON(alquil 0-8)(alquil C0-8), -N(cicloalquil C3-8)CON(cicloalquil C3-8)(alquil C0-8), -N(aIquil C0-8)CON(cicloalquil C3-8)(alquil C0-8), -N(alquil C0-8)CO2(cicloalquil C3- 8), -N(cicloalquil C3-8)CO2(cicloalquil C3-8), S(O)1-2N(alquil C0-8)(cicloalquil C0-8), -NR11S(O)1-2(cicloalquil C3-8), alquenilo C2-8, alquinilo C2-8, CN, CF3, OH, o sustituyentes arilo opcionalmente sustituidos; de modo tal que cada uno de los anteriores grupos arilo, heterociclilo, hetarilo, alquilo o cicloalquilo puede estar opcional, independientemente sustituido con -N(alquil C0-8)(alquil C0-8), hidroxilo, halogeno, oxo, arilo, hetarilo, alquilo C0-6, aIquil C0-8-cicIilo, -alquil C0-8- N(alquiI C0-8)-S(O)0-2-(alquil C0-8), alquil C0-8-S(O)0-2- N(alquiI C0-8)(alquiI C0-8), alquil C0-8-N(alquil C0-8)CO(aIquil C0-8), aIquil C0-8-N(alquiI C0-8)CO-N(alquil C0-8)(aIquil C0-8), -alquil C0-8-CO-N(alquil C0-8)(alquil C0-8), -aIquil C1-8- CO2-(alquil C0-8), -alquiI C0-8-S(O)0-2-(alquil C0-8), -aIquil C0-8-O-aIquiIo C1-8, -alquil C0-8-O-alquil C0-8-ciclilo, -alquil C0-8-O-alquil C0-8-heterociclilo, -alquil C0-8-O-alquil C0-8-arilo, -alquil C0-8-O-alquil C0-8-hetarilo, -alquil C0-8-S- alquiIo C0-8, -alquiI C0-8-S-alquil C0-8-ciclilo, -alquiI C0-8-S-alquiI C0-8-heterociclilo, -alquil C0-8-S-alquiI C0-8-arilo,-alquil C0-8-S-alquil C0-8-hetarilo, -alquiI C0-8-N(alquil C0-8)-alquilo C0-8, - alquiI C0-8-N(alquiI C0-8)-alquil C0-8- ciclilo, -alquil C0-8-N(aIquil C0-8)-alquiI C0-8-heterociclilo, -alquil C0-8-N(alquiI C0-8)-alquil C0-8-arilo, -aIquil C0-8-N(alquil C0-8)-alquil C0-8-hetarilo, alquenilo C2-8, alquinilo C2-8, NO2, CN, CF3, OCF3, OCHF2, aIquil C0-8-cicloalquilo C3- 8, -alquiI C0-8-O-alquilo C0-8, -alquil C0-8-N(alquiI C0-8)(aIquil C0-8), -alquil C0-8-S(O)0-2-alquilo C0-8, o heterociclilo opcionalmente sustituido con 1-4 sustituyentes independientes alquilo C0-8, ciclilo, o ciclilo sustituido; E1 en cada caso es independientemente halo, -CF3, -OCF3, -OR2, -NR31R32, -C(=O)R31, -CO2R31, -CONR31R32, -NO2, -CN, -S(O)0-2R31, -S(O)0-2NR31R32, -NR31C(=O)R32, -NR31C(=O)OR32, -NR31C(=O)NR32R33, -NR31S(O)0-2R32, -C(=S)OR31,-C(=O)SR31, -NR31C(=NR32)NR33R31, - NR31C(=NR32)OR33, -NR31C(=NR31)SR31, -OC(=O)OR31, -OC(=O)NR31R32, -OC(=O)SR31, -SC(=O)OR31, -SC(=O)NR31R32, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, - alcoxi C1-10-alquilo C1-10, -alcoxi C1-10-alquenilo C2-10, -alcoxi C1-10-alquinilo C2-10, - alquiltio 1-10-alquilo 1-10, -alquiltio C1-10-alquenilo C2-10, -alquiltio C1-10-alquinilo C2-10, cicloalquilo C3-8, -cicloalquenilo C3-8, -cicloalquil C3-8-alquilo C1-10, -cicloalquenil C3-8-aIquilo C1-10, -cicloalquil C3-8-alquenilo C2-10, - cicloalquenil C3-8-alquenilo C2-10, -cicloalquil C3-8-alquinilo C2-10, -cicloalquenil C3-8-alquinilo C2-10, -heterociclilalquilo C0-10, -heterociclilalquenilo C2-10, o -heterociclilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes halo, oxo, -CF3, -OCF3, -OR31,-NR31R32, -C(=O)R31, -CO2R31, -C(=O)NR31R32, -NO2, -CN, -S(=O)0-2R31, -SO2NR31, -NR31C(=O)R32, -NR31C(=O)OR31, -NR31 C(=O)NR32R33, -NR31S(O)0-2R31, -C(=S)OR31, - NR31C(=NR32)NR33R31, -NR31C(=NR32)OR33, -NR31C(=NR32)SR33, -OC(=O)OR31, -OC(=O)NR31R32, -OC(=O)SR31, -SC(=O)OR31, o -SC(=O)NR31R32; o E1 en cada caso es independientemente aril-alquilo C0-10, aril-alquenilo C2-10, aril-alquinilo C2-10, hetaril- alquilo C0-10, hetaril-alquenilo C2-10, o hetaril-alquinilo C2-10, donde el punto de enlace está a la izquierda o bien a la derecha segun se indica, donde cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes halo, -CF3, -OCF3, -OR31,-NR31R32, -C(O)R31, -CO2R31, -C(=O)NR31R32, -NO2, -CN, -S(O)0-2R31, -S(O)0-2NR31R32, -NR31C(=O)R32, -NR31C(=O)OR32, -NR31 C(=O)NR32R33, -NR31S(O)0-2R32, -C(=S)OR31, -C(=O)SR31, -NR31C(=NR32)NR33R31, - NR31C(=NR32)OR33, -NR31C(=NR32)SR33, -OC(=O)OR31, -OC(=O)NR31R32, -OC(=O)SR31, -SC(=O)OR31, o -SC(=O)NR31R32; en los casos de -NR31R32, -NR311R321, -NR312R322, -NR332R341, -NR313R323, y -NR323R333, los respectivos R31 y R32, R311 y R321, R312 y R322, R331 y R341, R313 y R323, y R323 y R333 se toman opcionalmente junto con el átomo de nitrogeno al cual están ligados para formar un anillo saturado o insaturado de 3 a 10 miembros; donde dicho anillo en cada caso está opcional, independientemente sustituido con uno o más sustituyentes independientes -N(alquil C0-8)(alquil C0-8), hidroxilo, halogeno, oxo, arilo, hetarilo, alquilo C0-6, -alquil C0-8-cicloalquilo C3-8, -alquil C0-8-N(alquiI C0-8)-S(O)0-2-(alquil C0-8), alquil C0-8-N(alquiI C0-8)S(O)0-2N(alquiI C0-8)(alquil C0-8), -(alquil C0-8)-N-(alquil C0-8)CO2(aIquil C0-8), -aIquil C0-8-CON((alquiI C0-8))S(O)0-2-(alquil C0-8), -(aIquil C0-8)-S(O)0-2-N(alquil C0-8)(aIquil C0-8), -alquiI C0-8N(alquil C0-8-)CO(alquil C0- 8), -alquil C0-8-N(alquil C0-8)CON(alquil C0-8)(alquil C0-8), -alquiI C0-8-CON(alquiI C0-8)(alquil C0-8), -alquil C0-8-CO2(aIquil C0-8), -alquiI C0-8-S(O)0-2(alquil C0-8), -alquil C0-8-O-alquiI C0-8, -alquil C0-8-O-aIquil C0-8-ciclilo, -alquil C0-8- O-alquil C0-8-heterocicloalquilo, -alquil C0-8-O-alquil C0-8-arilo, Oarilo, -alquil C0-8-O-alquil C0-8-hetarilo, -alquil C0-8-S-alquilo C0-8, -alquil C0-8-S-alquil C0-8-cicloalquilo C3-8, -alquil C0-8-S-alquil C0-8-heterocicloalquilo, -alquil C0-8-S- alquil C0-8-arilo, -alquiI C0-8-S-aIquil C0-8-hetarilo, -alquil C0-8-N(aIquil C0-8)-alquiIo C0-8, -alquil C0-8-N(alquil C0-8)-alquil C0-8-cicloalquilo C3-8, -alquil C0-8-N(alquil C0-8)-alquil C0-8-heterocicloalquilo, - aIquil C0-8-N(aIquil C0-8)- alquiI C0-8-arilo, -aIquil C0-8-N(alquiI C0-8)-alquil C0-8-hetarilo, - alquiI C0-8-N(alquil C0-8)(aIquil C0-8), alquenilo C2-8, alquinilo C2-8, NO2, CN, CF3, OCF3, o OCHF2; donde dicho anillo en cada caso incluye opcional, independientemente uno o más heteroátomos distintos de nitrogeno; m es 0, 1, 2,o 3; aa es 0 o 1; y siempre y cuando el compuesto no sea 3-ciclobutil-1-[(4-fenoxifenil)etinil]imidazo[1,5-a]pirazin-8-amina, 3-ciclobutil-1-[(1-metil-1H-imidazol-5-il)etinil]imidazo[1,5- a]pirazin-8-amina, N-{3-[(8-amino-3-ciclobutilimidazo[1,5-a]pirazin-1-iI)etinil]fenil)-4-clorobenzamida o 3-ciclobutil-1-(piridin-4-iletinil)imidazo[1,5-a]pirazin-8-amina.
ARP070100329A 2006-01-25 2007-01-25 Derivados de imidazo[1,5a]pirazina inhibidores de quinasas mtor, utiles para el tratamiento del cancer, y composiciones farmaceuticas que los contienen. AR059187A1 (es)

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US (1) US7659274B2 (es)
EP (1) EP1981890A2 (es)
JP (1) JP5156644B2 (es)
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TW (1) TW200738725A (es)
WO (1) WO2007087395A2 (es)

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