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AGONISTAS DEL RECEPTOR DE ESFINGOSINA-1-FOSFATO
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
GILMORE, JOHN L.,SHEPPECK, JAMES E.
申请号:
PE0001742012
公开号:
PE07322012A1
申请日:
2010.08.06
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Relates to Heterocyclic compounds of formula (i) wherein R1 is - (crdrd - (AOH), crdrd acooh, among others), where Rd is H, Oh, alkyl (c1-c4), alkoxy (c1-c4), among others is 0 to 3 R2 is Halo - Oh, alkyl (c1-c4), among Others R3 and R4 are each h, alkyl (C1 - C6) or along the C atom of the Q EU are United to form a Ring of 3 to 6 members R5 is H or alkyl (c1-c4 alkyl (r6) C1 - C3)Halo, haloalquilo (C1 - C3), among others M and N are each 1 or 2 X is 0 to 2 t is 0 to 4 W is CH2 or NH or, is a compound of formula (i), (ii), (iii) or (iv)), where Q is monociclico heteroaryl 5 members.Preferred compounds are: acid, 1 - (2 - hydroxy - 2 - (4 - (5 - (5 - 4 - phenyl - 3 - propilisoxazol - yl) 1,2,4 - Oxadiazoles - 3 - il) phenyl) ethyl) - 3 - acetidina carboxylic acid (S) - 1 - ((R) - 2 - hydroxy - 2 - (4 - (5 - (4 - (trifluoromethyl) phenyl isoxazole - 5 - il) - 1,2,4 - Oxadiazoles - 3 - il) phenyl) ethyl) - 4 - piperidine carboxylic acid 2 - (3 - (hydroxymethyl) PI Peridin - 1 - il) - 1 - (4 - (5 - (4 - (trifluoromethyl) phenyl isoxazole - il - 1.2, - 5)Oxadiazoles - 4 - 3 - il) phenyl) ethanol among others. It also relates to a Pharmaceutical composition. These compounds are agonists of sphingosine-1-phosphate receptor (%) being useful in the treatment of systemic lupus erythematosus, rheumatoid arthritis, multiple sclerosisSE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE R1 ES -(CRdRd)aOH, -(CRdRd)aCOOH, ENTRE OTROS, EN DONDE Rd ES H, OH, ALQUILO(C1-C4), ALCOXI(C1-C4), ENTRE OTROS a ES DE 0 A 3 R2 ES HALO, -OH, ALQUILO(C1-C4), ENTRE OTROS R3 Y R4 SON CADA UNO H, ALQUILO(C1-C6) O JUNTO AL ATOMO DE C AL QUE ESTAN UNIDOS FORMAN UN ANILLO DE 3 A 6 MIEMBROS R5 ES H O ALQUILO(C1-C4) R6 ES ALQUILO(C1-C3), HALO, HALOALQUILO(C1-C3), ENTRE OTROS m Y n SON CADA UNO 1 O 2 x ES DE 0 A 2 t ES DE 0 A 4 W ES O, CH2 O NH A ES UN COMPUESTO DE FORMULA (i), (ii), (iii) O (iv), EN DONDE Q ES HETEROARILO MONOCICLICO DE 5 MIEMBROS. SON COMPUESTOS PREFERIDOS: ACIDO 1-(2-HIDROXI-2-
来源网站:
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