BISWAS, KAUSTAV,BROWN, JAMES,CHEN, JIAN J.,GORE, VIJAY KESHAV,HARRIED, SCOTT,HORNE, DANIEL B.,KALLER, MATTHEW R.,LIU, QINGYIAN,MA, VU VAN,MONENSCHEIN, HOLGER,NGUYEN, THOMAS T.,ST. JEAN, JR., DAVID J.
申请号：
PE0028692013
公开号：
PE08682014A1
申请日:
2012.06.21
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Relates to compounds of formula (i) where M is 0 to 3 n is 0 OR 1 x1 is c or N (R4) R4 is H, alkyl (C1 - C6), F, CN, among others x2 is n or CH, CF r1 is alkyl (C1 - C6) or a bicyclic Ring 7 to 11 members or monociclico 3 to 7 members R2 is H, Halo, CN, among others R3 is H, alkyl (C1 - C8), haloalquilo (c1-c4), CN, among others R5 is Halo, CH3, CF3, among others R6 F, alkyl (C1 - C6)Among others. Preferred compounds are: (S) - N - ((3 - fluoropiridin IL - 2 - (4 - (trifluoromethoxy) phenyl) methyl) - 6 - oxo - 1.6 - dihidropiridin - 3 - carboxamide (S) - 2 - oxo - (N - (4 - (trifluoromethyl) phenyl) (3 - (trifluoromethyl) pyridin-2-yl) methyl) - 1.6 - dihidropiridin - 3 - carboxamide (S) - N - (3 - (fluoropiridin IL - 2 - (4 - (trifluoromethyl) phenyl) methyl 6) - oxo - 1.6 - dihidropiridin - 3 - carboxamide among others.It also relates to a Pharmaceutical composition. These compounds are antagonists of the Transient Receptor Potential TRPM8 being useful in the treatment of Pain, Osteoarthritis, migranaSE REFIERE A COMPUESTOS DE FORMULA (I) DONDE m ES DE 0 A 3 n ES 0 O 1 X1 ES C(R4) O N R4 ES H, ALQUILO(C1-C6), F, CN, ENTRE OTROS X2 ES CH, CF O N R1 ES ALQUILO(C1-C6) O UN ANILLO BICICLICO DE 7 A 11 MIEMBROS O MONOCICLICO DE 3 A 7 MIEMBROS R2 ES H, HALO, CN, ENTRE OTROS R3 ES H, ALQUILO(C1-C8), HALOALQUILO(C1-C4), CN, ENTRE OTROS R5 ES HALO, CH3, CF3, ENTRE OTROS R6 ES F, ALQUILO(C1-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (S)-N-((3-FLUOROPIRIDIN-2-IL)(4-(TRIFLUOROMETOXI)FENIL)METIL)-6-OXO-1,6-DIHIDROPIRIDIN-3-CARBOXAMIDA (S)-6-OXO-N-((4-(TRIFLUOROMETIL)FENIL)(3-(TRIFLUOROMETIL)PIRIDIN-2-IL)METIL)-1,6-DIHIDROPIRIDIN-3-CARBOXAMIDA (S)-N-((3-FLUOROPIRIDIN-2-IL)(4-(TRIFLUOROMETIL)FENIL)METIL)-6-OXO-1,6-DIHIDROPIRIDIN-3-CARBOXAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE POTENCIAL TRANSITORIO TRPM8 SIENDO UTILES EN EL TRATAMIENTO DE DOLOR, OSTEOARTRITIS, MIGRANA
