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4- (5-Isoxazolyl or 5-pyrrazolyl-1,2,4-oxadiazol-3-yl) -mandelic acid amides as sphingosine-1-phosphate receptor agonists 1
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
CHERNEY, ROBERT J.,ZHANG, YANLEI
申请号:
ES11717430
公开号:
ES2548683T3
申请日:
2011.04.21
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of Formula (I): ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: Q is ** Formula ** R1 is: (i) C3-6 alkyl; (ii) C3-7 cycloalkyl substituted with zero to 3 substituents independently selected from halogen, - CN, C1-4 alkyl, C1-4 alkoxy, C1-3 fluoroalkyl, C1-3 chloroalkyl and / or C1-2 fluoroalkoxy; (iii) phenyl substituted with zero to 3 substituents independently selected from halogen, -CN, C1-4 alkyl, C3-6 cycloalkyl, C1-4 alkoxy, C1-3 fluoroalkyl, C1-3 chloroalkyl and / or C1-2 fluoroalkoxy ; or (iv) pyridinyl substituted with zero to 3 substituents independently selected from halogen, -CN, C1-4 alkyl, C3-6 cycloalkyl, C1-4 alkoxy, C1-3 fluoroalkyl, C1-3 chloroalkyl and / or C1- fluoroalkoxy 2; R2 is CF3; n is zero, 1, or 2; each R3 is independently C1-3 alkyl, F, Cl, C1-3 fluoroalkyl, C1-3 chloroalkyl, -CN, C1-3 alkoxy and / or C1-3 fluoroalkoxy; R4 is H or -CH3; R5 is H or -CH3; and G is: (i) H, C1-6 alkyl or C3-6 cycloalkyl; (ii) C1-6 alkyl substituted with -NH2, C1-6 alkoxy, -C (O) OH, -C (O) O (C1-6 alkyl) or -S (O) 2 C1-6 alkyl; (iii) C1-6 alkyl substituted with one or more substituents selected from -OH, -CN and / or cyclopropyl; (iv) - (CH2) 0-3-Ra, wherein Ra is C3-6 cycloalkyl substituted with zero to 2 substituents independently selected from -OH, -CN and / or -CH2OH; (v) - (CH2) 0-3-Rb, wherein Rb is phenyl substituted with zero to 2 substituents independently selected from -OH, C1-3 hydroxyalkyl and / or -S (O) 2NH2; (vi) - (CH2) 1-3C (O) NRcRd, wherein Rc is H or -CH3; and Rd is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 hydroxyalkyl, - (CH2) 0-2 (heteroaryl) or - (CH2) 0-2 (heterocyclyl); (vii) -CH (CN) Re, wherein Re is phenyl, benzyl, -C (O) NH2 or -C (O) NH (C1-3 alkyl); (viii) -CHRfC (O) NH (CH3), wherein Rf is C1-6 alkyl, -CN, phenyl, benzyl or -CH2CH2-phenyl; (ix) - (CH2) 1-3NHC (O) Rg, wherein Rg is C1-6 alkyl or -O (C1-6 alkyl); (x) -CHRh- (CH2) 0-3-Ri, wherein Rh is H or -CH3 and Ri is heteroaryl; (xi) - (CH2) 0-3-
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