HUTCHINSON, JOHN HOWARD,SEIDERS, THOMAS JON,WANG, BOWEI,ARRUDA, JEANNIE M.,ROPPE, JEFFREY ROGER,PARR, TIMOTHY
申请号：
PE0020412011
公开号：
PE09362012A1
申请日:
2010.06.03
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to a compound of formula I, wherein R1 is - CO2H, - CN, tetrazolilo, 5-oxo - 2.5 - Oxadiazoles] - 3 - [1,2,4] ILO, among others R3 is H, c1-c4 alkyl, cycloalkyl - C3 - C4, C6, fluoroalquiloc1 R4 is nr7c (= OR) och (R8) - CY is h R7, R8 is c1-c4 alkyl h, c1-c4 alkyl, fluoroalquilo c1-c4 CY is Cycle C3 C6 alkyl substituted or unsubstituted phenyl, substituted or unsubstituted, among others, ra and RB are each F, CL, Oh,Fluoroalcoxi C1 - C4, C1 - C4 alkoxy, among others M is 0 - 2 - 4 1 n p is 0 - 2. Preferred compounds are: 1 - {4 [3-methyl-4 - ((R) - 1 - phenyl isoxazole etoximetilbonilamino) - biphenyl] - 5 - il - - 4 - - ciclopropanocarbonilo il} (R) - 1 - phenyl ethyl ester acid (5 - [4 - (1 - bencenosulfonilaminocarbonil - cyclopropyl) - biphenyl - 4-yl] - 3 - methyl isoxazole - 4-yl) - carbamic among others.These polycyclic compounds are antagonists of lysophosphatidic acid receptor useful in the treatment of Asthma, pulmonary fibrosis, renal fibrosis, Bone cancer, colon cancer, among othersREFERIDA A UN COMPUESTO DE FORMULA I, DONDE R1 ES -CO2H, -CN, TETRAZOLILO, 5-OXO-2,5-DIHIDRO[1,2,4]OXADIAZOL-3-ILO, ENTRE OTROS R3 ES H, ALQUILO C1-C4, CICLOALQUILO C3-C6, FLUOROALQUILOC1-C4 R4 ES NR7C(=O)OCH(R8)-CY R7 ES H, ALQUILO C1-C4 R8 ES H, ALQUILO C1-C4, FLUOROALQUILO C1-C4 CY ES CICLOALQUILO C3-C6 SUSTITUIDO O NO, FENILO SUSTITUIDO O NO, ENTRE OTROS RA Y RB SON CADA UNO F, Cl, OH, FLUOROALCOXI C1-C4, ALCOXI C1-C4, ENTRE OTROS m ES 0-2 n 1-4 p ES 0-2. SON COMPUESTOS PREFERIDOS: 1-{4[3-METIL-4-((R)-1-FENIL-ETOXIMETILBONILAMINO)-ISOXAZOL-5-IL]-BIFENIL-4-IL}-CICLOPROPANOCARBONILO (R)-1-FENIL-ETIL ESTER DE ACIDO {5-[4-(1-BENCENOSULFONILAMINOCARBONIL-CICLOPROPIL)-BIFENIL-4-IL]-3-METIL-ISOXAZOL-4-IL}-CARBAMICO ENTRE OTROS. DICHOS COMPUESTOS SON ANTAGONISTAS POLICICLICOS DE LOS RECEPTORES DE ACIDO LISOFOSFATIDICO UTILES EN EL TRATAMIENTO DE FIBROSIS PULMONAR, ASMA, FIBROSIS RENAL, CANCER OSEO, CANCER DE COLON, ENTRE OTROS
