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ANTAGONISTAS DEL RECEPTOR DE ACIDO LISOFOSFATIDICO PARA EL TRATAMIENTO DE FIBROSIS
专利权人:
AMIRA PHARMACEUTICALS; INC.
发明人:
SEIDERS, THOMAS JON,WANG, BOWEI,HUTCHINSON, JOHN HOWARD,STOCK, NICHOLAS SIMON,VOLOTS, DEBORAH
申请号:
PE0013662013
公开号:
PE08792014A1
申请日:
2011.12.06
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Relates to compounds of formula (i) wherein: R1 is CO2H, NH - C (= o) Oh, P (= o) (OH) 2, NS, among others L1 is absent or is alquileno cicloalquileno C1 - C6 C3, C6, among others The phenyl ring is, naphthyl, monociclico bicyclic heteroaryl heteroaryl, or, if that is not an isoxazole Ring Ra and RB is independently NS, Oh, alkoxy c1-c4, among others L2 is a alquileno C1 - C6Fluoroalquileno C1 - C6 substituted or unsubstituted, among others R2 is C1 - C6 fluoro alkyl, cycloalkyl C1 - C6 C3 - C10 substituted or unsubstituted, among others R3 is c1-c4 alkyl, cycloalkyl fluoroalquilo C1 - C3 - C4 or C6 M is an integer from 0 to 2 n is an integer from 0 to 2.Preferred compounds are: acid (4th - 1 - (4 - [1 - (2 - chloro phenyl) - etoxicarbonilamino] pyridin-3-yl) - biphenyl - 4-yl) - ciclopropancarboxilico acid 4th - [1 - (1 - methyl - 5 - (4 - phenyl - 2 - pyridin - ilamino) - 1h-pyrazol-4-yl] - diphenyl - 4 - il} - ciclopropancarboxilico among others. Also referred to pharmaceutical compositions.These compounds are useful for the treatment of cancer, organ fibrosis, Liver DiseasesSE REFIERE A COMPUESTOS DE FORMULA (I) DONDE: R1 ES CO2H, C(=O)NH-OH, P(=O)(OH)2, CN, ENTRE OTROS L1 ESTA AUSENTE, O ES ALQUILENO C1-C6, CICLOALQUILENO C3-C6, ENTRE OTROS EL ANILLO A ES FENILO, NAFTILO, HETEROARILO MONOCICLICO, O HETEROARILO BICICLICO, SIEMPRE QUE EL ANILLO A NO SEA UN ISOXAZOL Ra Y Rb ES INDEPENDIENTEMENTE CN, OH, ALCOXI C1-C4, ENTRE OTROS L2 ES UN ALQUILENO C1-C6, FLUOROALQUILENO C1-C6 SUSTITUIDOS O NO SUSTITUIDOS, ENTRE OTROS R2 ES ALQUILO C1-C6, FLUORO C1-C6, CICLOALQUILO C3-C10 SUSTITUIDO O NO SUSTITUIDO, ENTRE OTROS R3 ES ALQUILO C1-C4, FLUOROALQUILO C1-C4 O CICLOALQUILO C3-C6 m ES UN ENTERO DE 0 A 2 n ES UN ENTERO DE 0 A 2. SON COMPUESTOS PREFERIDOS: ACIDO 1-(4�-{4-[1-(2-CLORO-FENIL)-ETOXICARBONILAMINO]-PIRIDIN-3-IL}-BIFENIL-4-IL)-CICLOPROPANCARBOXILICO ACIDO 1-{4�-[1-METIL-5-(6-FENIL-PIRIDIN-2-ILAMINO)-1H-PIRAZOL-4-IL]-BIFENIL-4-IL}-CICLOPROPANCARBOXILICO ENTRE OTROS.
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