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COMPUESTOS POLICICLICOS COMO ANTAGONISTAS DEL RECEPTOR DE ACIDO LISOFOSFATIDICO
专利权人:
AMIRA PHARMACEUTICALS; INC.
发明人:
CLARK, RYAN,STEARNS, BRIAN ANDREW,ZHAO, LUCY,SEIDERS, THOMAS JON,VOLKOTS, DEBORAH,ARRUDA, JEANNIE M.,ZALATAN, DAVID NATHAN
申请号:
PE0004102012
公开号:
PE09972012A1
申请日:
2010.09.29
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Relates to polycyclic compounds of formula (i) wherein R1 is co2rd -, - C (= o) n (RD) 2, NS, tetrazolilo, among others, where Rd is H or alkyl (C1 - C6) L2 is absent or - C (= o) - (C1, alquileno - C4), among others it is heteroarileno optionally substituted phenyl or with R14, where R14 is Halogen, Oh, CN, alkoxy (c1-c4),Among others, L4 is absent or alquileno (c1-c4) R5 is H or alkyl (c1-c4) ra, RB and RC are each CN, Oh, halogen, alkyl (c1-c4), fluoroalcoxi (c1-c4), among others, M, N and P are each one of 0 to 2 R is 1 to 4.Preferred compounds are: acid 1 {- 4 - [3 - methyl - 4 - (3-phenyl pyrazole - 1 - methyl - 5 - isoxazole) - yl] - Diphenyl - 4 - il} - {1 ciclopropanocarboxilico acid - 4 - [3 - (4 - methyl - 4 - phenyl - [1,2,3] triazole - 1 - methyl - 5 - isoxazole) - yl] - Diphenyl - 4 - il} - {1 ciclopropanocarboxilico acid - 4 - [3 - (5 - methyl - 4 - phenyl - 2 -] [1,3,4 Oxadiazoles ILME Isoxazole til) - biphenyl] - il - 5 - 4 - il} - ciclopropanocarboxilico among others.It also relates to a Pharmaceutical composition. These compounds are being lysophosphatidic acid Receptor Antagonists useful in the treatment of Asthma, pulmonary fibrosis, scleroderma, atherosclerosisSE REFIERE A COMPUESTOS POLICICLICOS DE FORMULA (I) DONDE R1 ES -CO2RD, -C(=O)N(RD)2, CN, TETRAZOLILO, ENTRE OTROS, EN DONDE RD ES H O ALQUILO(C1-C6) L2 ESTA AUSENTE O ES -C(=O)-, ALQUILENO(C1-C4), ENTRE OTROS A ES FENILO O HETEROARILENO OPCIONALMENTE SUSTITUIDO CON R14, EN DONDE R14 ES HALOGENO, CN, OH, ALCOXI(C1-C4), ENTRE OTROS L4 ESTA AUSENTE O ES ALQUILENO(C1-C4) R5 ES H O ALQUILO(C1-C4) RA, RB Y RC SON CADA UNO HALOGENO, CN, OH, ALQUILO(C1-C4), FLUOROALCOXI(C1-C4), ENTRE OTROS m, n Y p SON CADA UNO DE 0 A 2 r ES DE 1 A 4. SON COMPUESTOS PREFERIDOS: ACIDO 1-{4-[3-METIL-4-(3-FENIL-PIRAZOL-1-ILMETIL)-ISOXAZOL-5-IL]-BIFENIL-4-IL}-CICLOPROPANOCARBOXILICO ACIDO 1-{4-[3-METIL-4-(4-FENIL-[1,2,3]TRIAZOL-1-ILMETIL)-ISOXAZOL-5-IL]-BIFENIL-4-IL}-CICLOPROPANOCARBOXILICO ACIDO 1-{4-[3-METIL-4-(5-
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