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2-Amino-(oxadiazol-3-yl)-benzofuran derivatives and their use as S1P receptor modulators
专利权人:
AKAAL PHARMA PTY LTD
发明人:
GILL, GURMIT, S,GROBELNY, DAMIAN W
申请号:
NZ59274809
公开号:
NZ592748A
申请日:
2009.10.19
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Disclosed are 2-amino-(oxadiazol-3-yl)-benzofuran derivatives as represented by the general formula (I), wherein each of the dotted lines ---- independently is a bond or absent a, b and c are independently selected from C, O, N and S to provide a five membered heterocyclic ring, G represents an amine containing organic substituent A represents one or more ring atoms selected from C and N X is a monocyclic or bicyclic aryl or heteroaryl ring and wherein J, m and D separately, or in any combination, are selected from hydrogen, deuterium, alkoxy, alkylamino, halogen, amino, hydroxy, oxo (=O), imino (=NR), cyano, aryl, heterocycle, carbocycle, or an alkyl chain said alkyl chain optionally containing carbon-carbon multiple bond, carbon-hetero atom multiple bond and wherein one or more carbon atoms of said alkyl chain can be independently replaced with oxygen, sulphur, SO, SO2, NR (wherein R is selected from alkyl, cycloalkyl, aryl, heterocycle), carbocycle and heterocycle or J, m and D are linked together to form a ring with X or the group m is a substituent attached to either one of J or D. Representative compounds include 2-amino-2-(5-(5-(3-chloro-4-propoxyphenyl)-1,2,4-oxadiazol-3-yl)benzofuran-2-yl)propane-1,3-diol, 2-amino-2-(5-(5-(4-bromo-3-chlorophenyl)-1,2,4-oxadiazol-3-yl)benzofuran-2-yl)propane-1,3-diol, 2-amino-2-(5-(5-(3-chloro-4-(thiophen-3-yl)phenyl)-1,2,4-oxadiazol-3-yl)benzofuran-2-yl)propane-1,3-diol, 2-amino-2-(6-chloro-5-(5-(4-propylphenyl)-1,2,4-oxad iazol-3-yl)benzofuran-2-yl)propane-1,3-diol and 5-(3-(2-(2-amino-1,3-dihydroxypropan-2-yl)benzofuran-5-yl)-1,2,4-oxadiazol-5-yl)-2-propoxybenzonitrile. Further disclosed is a pharmaceutical preparation, which comprises at least one compound as defined above in any of its stereoisomeric and/or isotopic forms and/or physiologically tolerable and/or therapeutically effective salts or mixtures thereof in any ratio together with a pharmaceutically acceptable carrier( s) or excipient( s), for the treatment and/
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