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Oxazole derivatives useful as AHAG inhibitors
专利权人:
MERCK & CO., INC.;MERCK SHARP & DOHME CORP.
发明人:
CHOBANIAN, HARRY,LIN, LINUS S.,LIU, PING,CHIODA, MARC D.,DEVITA, ROBERT J.,NARGUND, RAVI P.,GUO, YAN
申请号:
ES09790960
公开号:
ES2463765T3
申请日:
2009.07.30
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A pharmaceutical composition comprising an inert carrier and a compound of the formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: X is S or SO; R1 is selected from the group consisting of: (1) aryl, and (2) HET1. wherein R1 is optionally mono or di-substituted with substituents R4 and R5; and wherein R4 and R5 are independently selected from the group consisting of: (a) halo, (b) -CN, (c) mono, di or tri-halo C1-4 alkyl, (d) mono, di or tri -halo O-C1-4alkyl, (d) -O-C1-4alkyl, optionally substituted with hydroxyl, halo or amino, (e) -C1-4alkyl optionally substituted with one or two substituents selected from hydroxyl, CN, - CHF2 and -CF3, (f) -C1-2 alkyl-C3-6 cycloalkyl optionally substituted with hydroxy, halo or CN, (g) -S (O) C1-4 alkyl, (h) -S (O) nNR6R7 , (i) -C (O) -NH-NR8R9, (j) -C (O) -OH, (k) -C (O) -O-C 1-4 alkyl, optionally substituted with halo or hydroxy, (l ) -C (O) -NR10R11, (m) -C (O) -C1-4alkyl optionally mono, di or tri substituted with halo, (o) -C (NR12) -NR13R14, (p) HET4, (q ) aryl, (r) -C (O) -NH-NH-C (O) H, (s) -CH2-C (O) -O-C1-4alkyl, while CH2 may be optionally substituted with alkyl C1-4 or OH (t) -CH2-C (O) NR15R16, while CH2 may be optionally substituted with C1-4 alkyl or OH, and (u) -NR17R18,Una composición farmacéutica que comprende un vehículo inerte y un compuesto de la fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que: X es S o SO; R1 se selecciona entre el grupo que consiste en: (1) arilo, y (2) HET1. en la que R1 está opcionalmente mono o di-sustituido con sustituyentes R4 y R5; y en donde R4 y R5 se seleccionan independientemente entre el grupo que consiste en: (a) halo, (b) -CN, (c) mono, di o tri-halo alquilo C1-4, (d) mono, di o tri-halo O-alquilo C1-4, (d) -O-alquilo C1-4, opcionalmente sustituido con hidroxilo, halo o amino, (e) -alquilo C1-4 opcionalmente sustituido con uno o dos sustituyentes seleccionados entre hidroxilo, CN, - CHF2 y -CF3, (f) -alquil C1-2-cic
来源网站:
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