发明名称 1a, 5a-TETRAHYDRO-S-THIACYCLOPROPA[a]PENTALENES: TRICYCLIC DERIVATIVES OF THIOPHENE AS S1P1/EDG1 RECEPTOR AGONISTS
摘要 FIELD: chemistry. ^ SUBSTANCE: described are novel thiophene derivatives of formula (1) and pharmaceutically acceptable salts thereof, where A is -CH2CH2-, -NH-CH2-, -CH2-O or -CH2NH-, R1 is hydrogen or alkyl, when X is C-R4, R1 additionally represents halogen, and when A is -CH2-CH2- or -CH2NH, R1 additionally represents alkoxy, R2 is hydrogen, alkoxy, fluoralkoxy, hydroxyalkoxy, hydroxyalkyl, di-(hydroxy)alkoxy, pyridinyl-3-methoxy, pyridinyl-4-methoxy, R3 is hydrogen, alkyl, trifluoromethyl, and when X is C-R4, R3 additionally represents halogen, and when A is -CH2-CH2-, R3 additionally represents alkoxy, X is N or C-R4, R4 is hydrogen, alkyl, alkoxy or halogen, R5 is methyl or ethyl. Also described are isomers of the said compounds, an initial compound for synthesis of formula (1) compound, which has agonistic effect on S1P1/EDG1 receptors, as well as a pharmaceutical composition based on formula (1) compound and use of formula (1) compound. ^ EFFECT: obtaining a pharmaceutical composition for preventing or treating diseases or disorders associated with activated immune system. ^ 19 cl, 2 tbl, 167 ex
申请公布号 RU2386626(C2) 申请公布日期 2010.04.20
申请号 RU20070107164 申请日期 2005.07.20
申请人 AKTELION FARMAS'JUTIKLZ LTD 发明人 BOLLI MARTIN;BUR DANIEL';KLOZEL' MARTINA;FISHLI VAL'TER;LEMANN DAVID;MATIS BORIS;MJULLER KLAUS;NAJLER OLIVER;SHERTS MIKHAEHL';VELLER TOMAS
分类号 A61K31/38;A61K31/4436;A61P37/00;C07D333/78;C07D409/12 主分类号 A61K31/38
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