New thiophene derivatives as S1P1 / EDG1 receptor agonists

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专利权人:

ACTELION PHARMACEUTICALS LTD.

发明人:

BOLLI, Martin,LEHMANN, David,MATHYS, Boris,MUELLER, Claus,NAYLER, Oliver,STEINER, Beat,VELKER, Jörg

申请号：

ES07700562

公开号：

ES2553345T3

申请日:

2007.01.10

申请国别(地区):

ES

年份:

2015

代理人:

摘要：

A compound selected from the group consisting of thiophene compounds of Formula (I), ** Formula ** in which A represents * -CO-CH>； = CH-, * -CO-CH2CH2-, * -CO-CH2 -NH -, ** Formula ** in which asterisks indicate the bond that is attached to the thiophene group of Formula (I)； R1 represents hydrogen, methyl, or trifluoromethyl； R2 represents n-propyl, isobutyl, or cyclopropylmethyl； R3 represents hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, isopropyl, or isobutyl； R4 represents hydrogen, C1-4 alkyl, methoxy, or halogen； R5 represents hydrogen, C1-4 alkyl, C1-4 alkoxy, or halogen； R6 represents di- (hydroxy-C1-4 alkyl-) - C1-4 alkyl, 2,3-dihydroxypropyl, -CH2- (CH2) n-NHCOR64, -CH2- (CH2) n- NHSO2R63, - (CH2) k - (CHR65) p-CHR66-CONR61R62, - (CH2) nCH (OH) -CH2-NR61R62, - (CH2) nCH (OH) -CH2-NHCOR64, - (CH2) nCH (OH) -CH2-NHSO2R63, - CO-NHR61, hydroxy, C2-4 hydroxy-alkoxy, di- (hydroxyC 1-4 alkyl) -C 1-4 alkoxy, 1- glyceryl, 2,3-dihydroxypropoxy, 2-hydroxy-3-methoxy-propoxy, - OCH2- (CH2) m-NR61R62, -OCH2- (CH2) m-NHCOR64, -OCH2- (CH2) m-NHSO2R63, -OCH2-CH (OH) -CH2-NR61R62, -OCH2-CH (OH) -CH2 -NHCOR64, -OCH2-CH (OH) - CH2-NHSO2R63, -NR61R62, -NHCO-R64, or -SO2NH-R61； R61 represents hydrogen, methyl, ethyl, 2-hydroxyethyl, 2-hydroxy-1-hydroxymethyl-ethyl, 2,3-dihydroxy-propyl, 2- C1-4 alkoxyethyl, 3-hydroxypropyl, 3-C1-4 alkoxypropyl, 2- aminoethyl, 2- (C1-4 alkylamino) ethyl, 2- (di- (C1-4 alkyl) amino) ethyl, carboxymethyl, C1-4 alkylcarboxymethyl, 2-carboxy ethyl, or 2- (C1-4 alkylcarboxy) ethyl； R62 represents hydrogen, or methyl； R63 represents methyl, ethyl, 2-hydroxyethyl, 2-methoxyethyl, methylamino, ethylamino, or dimethylamino； R64 represents hydroxymethyl, aminomethyl, methylaminomethyl, dimethylaminomethyl, 2-aminoethyl, or 2-methylaminoethyl； R65 represents hydrogen； R66 represents hydrogen or hydroxy； and in the case that R66 represents hydroxy, R65 may also represent hydroxy； m represents the integer 1 or 2； n represents 0, 1, or 2； k represen

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