CORTEZ, ALEX,LI, YONGKAI,WU, TOM YAO-HSIANG,YUE, KATHY,ZHANG, XIAOYUE,SINGH, MANMOHAN,SKIBINSKI, DAVID
申请号：
PE0002852012
公开号：
PE11562012A1
申请日:
2010.09.01
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a naftiridilo Derivative of formula (i), wherein R1 is c1-c4 alkyl, C (R5) 2OH, l1r5, l2r5, among others is C (or L1 or L2 is alquileno C1 - C6, alquenileno C2 - C6, among other alkyl R2 is H, or C1 - C4 R3 is l3r5, l1r5, ol3r5, among others R5 is P (o) (OH) 2.Preferred compounds are: acid, 4 - (4 - (2 - (3 - amino - 4 - methyl - benzo [f] [1,7] - naftiridin - 2 - il) - ethyl) - 3 - methyl - phenoxy) - 1.1 - difluoro - butyl phosphonic acid, 3 - (5 - amino - 2 - (4 - (4,4 - difluoro - 4 - phosphono - Butoxy) - 2-methyl - Phenethyl) - benzo [f] [1,7] - naftiridin - 8 - yl) - propanoic acid, 3 - (5 - (2 - amino - 4 - (2 - (3,3 - difluoro - 3 - phosphono - propoxy) - ethoxy - 2 - Methyl Phenethyl) - benzo [f] [1,7] - naftiridin - 8 - yl) - propanoic acid, among others.These compounds are modulators of Toll like receptors (TLRs) and are useful in the treatment of Asthma, ulcerative colitis, Crohns disease, bronchitis, psoriasis, among othersREFERIDA A UN DERIVADO DE NAFTIRIDILO DE FORMULA (I), DONDE R1 ES ALQUILO C1-C4, C(R5)2OH, L1R5, L2R5, ENTRE OTROS L1 ES C(O) U O L2 ES ALQUILENO C1-C6, ALQUENILENO C2-C6, ENTRE OTROS R2 ES H O ALQUILO C1-C4 R3 ES L3R5, L1R5, OL3R5, ENTRE OTROS R5 ES P(O)(OH)2. SON COMPUESTOS PREFERIDOS: ACIDO 4-(4-(2-(5-AMINO-8-METIL-BENZO-[f][1,7]-NAFTIRIDIN-2-IL)-ETIL)-3-METIL-FENOXI)-1,1-DIFLUORO-BUTIL-FOSFONICO, ACIDO 3-(5-AMINO-2-(4-(4,4-DIFLUORO-4-FOSFONO-BUTOXI)-2-METIL-FENETIL)-BENZO-[f][1,7]-NAFTIRIDIN-8-IL)-PROPANOICO, 3-(5-AMINO-2-(4-(2-(3,3-DIFLUORO-3-FOSFONO-PROPOXI)-ETOXI-2-METIL-FENETIL)-BENZO-[f][1,7]-NAFTIRIDIN-8-IL)-PROPANOICO, ENTRE OTROS. DICHOS COMPUESTOS SON MODULADORES DE LOS RECEPTORES TIPO TOLL (TLRs) Y SON UTILES EN EL TRATAMIENTO DE ASMA, COLITIS ULCERATIVA, ENFERMEDAD DE CROHN, BRONQUITIS, SORIASIS, ENTRE OTRAS
