发明名称 SUBSTITUTED ARYL 1 ,2,4-OXADIAZOLES DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS
摘要 The present invention relates to substituted aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
申请公布号 US2014274963(A1) 申请公布日期 2014.09.18
申请号 US201414218596 申请日期 2014.03.18
申请人 Allergan, Inc. 发明人 Takeuchi Janet A.;Li Ling;Im Wha Bin;Chow Ken
分类号 C07F9/6503 主分类号 C07F9/6503
代理机构 代理人
主权项 1. A method of treating an immunosuppressant disorder associated with the sphingosine-1-phosphate receptor modulation, wherein the immunosuppressant disorder is selected from: rheumatoid arthritis, psoriasis, atherosclerosis, autoimmune uveitis, dry eye, inflammatory bowel diseases, atopic allergy, atopic dermatitis, contact dermatitis, multiple sclerosis, Sjogren's syndrome and organ transplant rejection, in a mammal in need thereof, which comprises administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of at least one compound represented by Formula I or a pharmaceutically acceptable salt thereof: wherein: R1 is substituted or unsubstituted C6-10 aryl, substituted or unsubstituted heterocycle, substituted or unsubstituted C5-8 cycloalkyl, substituted or unsubstituted C5-8 cycloalkenyl; R2 is hydrogen, —OC1-3 alkyl or substituted or unsubstituted C1-3 alkyl; R3 is hydrogen, halogen, substituted or unsubstituted C1-3 alkyl, C(O)R10 or hydroxyl; R4 is hydrogen, halogen, substituted or unsubstituted C1-3 alkyl, C(O)R10 or hydroxyl; R5 is hydrogen, halogen, substituted or unsubstituted C1-3 alkyl, C(O)R10 or hydroxyl or substituted or unsubstituted heterocycle; R6 is hydrogen, halogen, substituted or unsubstituted C1-3 alkyl, C(O)R10 or hydroxyl or substituted or unsubstituted heterocycle; R7 is hydrogen, —OC1-3 alkyl or substituted or unsubstituted C1-3 alkyl; R8 is H or C1-3 alkyl; R9 is PO3H2, —P(O)MeOH, or —P(O)(H)OH; R10 is H or C1-3 alkyl; a is 2 or 3; b is 1, 2 or 3; c is 1, 2, 3, 4, 5 or 6; with the proviso that the compound of Formula I is not of structure
地址 Irvine CA US