CALDERWOOD, DAVID J.,BREINLINGER, ERIC C.,SWANN, STEVEN L.,MUKHERJEE, SUBHENDU,CHITTY, VENKATA SRIKANTH,THUNUGUNTLA, SIVA SANJEEVA RAO,HOSAHALLI, SUBRAMANYAH SEETHARAMA SHASTRY
申请号：
PE0024282013
公开号：
PE11902014A1
申请日:
2012.04.30
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Isoxazolinas refers to compounds of formula (i) where a is a compound of formula (a), (b), among others, where R1 is H, F, BR, among others Z is - C (o) OCH3 (C1 - C6), alkyl, aryl, among others. And q are each X is 0 to 3 phenyl, naphthyl, benzofuranilo is heter, among others and Oarilo ra is H, optionally substitutedAlkyl or cycloalkyl (C1 - C3 (C3 C6) optionally substituted RB CF3, is H, alkyl or cycloalkyl (C1 - C3 (C3 C6) M is 0 to 2.Preferred compounds are: 6 - (5 - (1 - acetilpiperidin - 4-yl) - 4.5 - dihidroisoxazol - 3 - yl) - N - (4-fluoro-3 - metoxibencil) - 2 - metilpirimidin - 4 - carboxamide n - (4 - fluoro - 3 - methyl - 2 - metoxibencil) 6 - (5 - (1 - (methylsulfonyl) piperidin-4-yl il) - 4.5 - dihidroisoxazol IL - 3 - 4 - pyrimidin-2-yl) - carboxamide among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of matrix metalloproteinase MMP - 13 being useful in the treatment of traumatic Osteoarthritis, Joint Injury, arthritisSE REFIERE A COMPUESTOS DERIVADOS DE ISOXAZOLINAS DE FORMULA (I) DONDE A ES UN COMPUESTO DE FORMULA (a), (b), ENTRE OTROS, DONDE R1 ES H, Br, F, ENTRE OTROS Z ES -C(O)OCH3, ALQUILO(C1-C6), ARILO, ENTRE OTROS n Y p SON CADA UNO DE 0 A 3 X ES NAFTILO, FENILO, BENZOFURANILO, ENTRE OTROS Y ES HETEROARILO OPCIONALMENTE SUSTITUIDO Ra ES H, ALQUILO(C1-C3) O CICLOALQUILO(C3-C6) OPCIONALMENTE SUSTITUIDOS Rb ES H, CF3, ALQUILO(C1-C3) O CICLOALQUILO(C3-C6) m ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 6-(5-(1-ACETILPIPERIDIN-4-IL)-4,5-DIHIDROISOXAZOL-3-IL)-N-(4-FLUORO-3-METOXIBENCIL)-2-METILPIRIMIDIN-4-CARBOXAMIDA N-(4-FLUORO-3-METOXIBENCIL)-2-METIL-6-(5-(1-(METILSULFONIL)PIPERIDIN-4-IL)-4,5-DIHIDROISOXAZOL-3-IL)PIRIMIDIN-4-CARBOXAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA METALOPROTEINASA DE MATRIZ MMP-13 SIENDO UTILES EN EL TRATAMIENTO DE OSTEOARTRITIS, LESION ARTICULAR TRAUMATICA, ARTRITIS REUMATOIDE
