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Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
专利权人:
NOVARTIS AG;NOVARTIS PHARMA GMBH
发明人:
EHRHARDT, CLAUS,HINTERDING, KLAUS
申请号:
ES04739810
公开号:
ES2384324T3
申请日:
2004.06.11
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula I in which R1 is C1-6 alkyl; C1-6 alkyl substituted with hydroxy, C1-2 alkoxy or 1 to 6 fluorine atoms; C2-6 alkenyl; or C2-6 alkynyl; R2 is C1-10 alkyl; C1-10 haloalkyl; C1-9 alkoxy; C1-9 haloalkoxy; each optionally substituted on the terminal carbon atom with phenyl, phenoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, heteroaryl, heteroaryloxy, a heterocyclic moiety, wherein phenyl, phenoxy, C3-6 cycloalkyl, C3 cycloalkoxy -6, heteroaryl, heteroaryloxy, a heterocyclic moiety may each be annularly substituted with 1 to 5 substituents selected from hydroxy, halogen, C1-4 alkyl, C1-4 haloalkyl, C3-6 cycloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C3-6 cycloalkoxy, C3-6 cycloalkyl-C1-2 alkyl, cyano, phenyl, and phenylsubstituted with hydroxy, halogen, C1-4 alkyl, C1-4 haloalkyl, C1- alkoxy 4, or cyano; or a moiety of formula (b) in which R 10 is C 1-6 alkyl and R 11 is C 1-6 alkyl; C1-10 haloalkyl; each optionally substituted on the terminal carbon atom with a phenyl, phenoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, heteroaryl, heteroaryloxy, a heterocyclic moiety, wherein phenyl, phenoxy, C3-6 cycloalkyl, cycloalkoxy C3-6, heteroaryl, heteroaryloxy, a heterocyclic moiety can each be annularly substituted with 1 to 5 substituents selected from hydroxy, halogen, C1-4 alkyl, C1-4 haloalkyl, C3-6 cycloalkyl, C1-4 alkoxy , C3-6 cycloalkoxy, C3-6 cycloalkyl-C1-2 alkyl, cyano, phenyl and phenyl substituted with hydroxy, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or cyano; R3 is Z-X2, where Z is CH2, CHF, CHMe or CF2, and X2 is OH or a remainder of formula (a) in which Z1 is a direct bond, CH2, CHF, CF2 or O, and each R8 and R9, independently, is H or C1-4alkyl optionally substituted with 1, 2 or 3 halogen atoms; each one of R4 and R5, independently, is H; C1-4 alkyl optionally substituted with 1, 2 or 3 halogen atoms; or acyl; and ring A is substituted with R2 and with two additional substituents; in free form or in salt form.Un compuesto de fórmula Ien la queR1 es
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