摘要 |
Disclosed is a compound of formula I wherein: Y is ?CH2CH2-, -CH2CH(OH)-, -CH(OH)CH2-, -CH2C(O)-, -CH=CH- or 1,2-cyclopropylene; X is arylene of C5-6heteroarylene optionally substituted by one to three substituents selected from halogen, nitro, C1-10alkyl and halogen-substituted C1-6alkyl; R1 is aryl, aryl-C2-4alkenyl, heteroaryl, or heteroaryl-C2-4alkenyl each substituted as defined; R2 is hydrogen, halogen, C1-4 alkyl optionally substituted with one or more halogens, C2-6 alkenyl, C2-6alkynyl, cycloalkyl optionally substituted by halogen, aryl optionally substituted with hydroxyl, C1-4alkyl optionally substituted on the terminal C atom by OH or a residue of formula (h) with substituents as defined; R3 and R4 are independently, H, or C1-4alkyl optionally substituted by halogen or acyl; and R5 is H, -OH, -Oacyl, -NHacyl, or a residue of formula (h) as defined. With the proviso that at least R2 comprises a terminal OH or a residue of formula (h) or R5 is OH or a residue of formula (h). Compounds of the type disclosed are useful either alone or in combination with an immunosuppressive, immunomodulating, anti-inflammatory or chemotherapeutic agent for treating disorders or diseases mediated by lymphocytes, preventing or treating acute or chronic transplant rejection or T-cell mediated inflammatory or autoimmune diseases, for inhibiting or controlling deregulated angiogenesis, or for preventing or treating diseases mediated by neo-angiogenesis.
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申请人 |
NOVARTIS AG;IRM LLC |
发明人 |
FAN, YING;GAO, WENQI;GRAY, NATHANAEL S;HINTERDING, KLAUS;LEFEBVRE, SOPHIE;NUSSBAUMER, PETER;PAN, SHIFENG;WANG, WEI;ZECRI, FREDERIC;PEREZ, LAWRENCE BLAS;LA MONTAGNE, KENNETH RICHARD;ETTMAYER, PETER;MI, YUAN |