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Piperidine derivatives and their use for the treatment of metabolic disorders
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
ROTH GERALD JUERGEN,FLECK MARTIN,LEHMANN-LINTZ THORSTEN,NEUBAUER HEIKE,NOSSE BERND
申请号:
NZ60372411
公开号:
NZ603724A
申请日:
2011.06.30
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed is are N-({ 4-[1-(aryl)-piperidin-4-yl]-phenyl} -alkylene)acetamide derivatives as represented by the general formula (I), wherein Ar1 is selected from the group consisting of: phenyl, naphthyl, pyridyl, 2H-pyridin-2-onyl, pyrimidinyl, pyridazinyl, pyrazinyl, furanyl, thienyl, pyrrolyl, imidazolyl, triazolyl, oxazolyl, isoxazolyl, pyrazolyl, thiazolyl, quinolinyl, isoquinolinyl, indolyl, benzofuranyl, benzoimidazolyl, benzooxazolyl, benzotriazolyl, 2,3-dihydrobenzofuranyl, benzo[1,3]dioxolyl and 2,3-dihydro-benzo[1,4]dioxinyl, wherein all of the before mentioned mono- and bicyclic groups may be optionally substituted with one or more substituents RA Ar2 is a para substituted phenyl group which may optionally be further substituted X is a straight chain alkylene group which may be optionally substituted Y is selected from the group consisting of -C(=O)-, -C(=S)- and -S(=O)2- RN is selected from the group consisting of H and alkyl T is selected from the group consisting of: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, cycloalkyloxy, cycloalkyl-alkoxy, alkylthio, cycloalkyl-thio-, cycloalkyl-alkyl-thio-, alkyl-C(=O)-, alkyl-S(=O)2-, amino, aminoalkyl-, amido, alkyl-C(=O)-RT2N-alkyl, heterocyclyl, phenyl and heteroaryl, each of which may be further substituted, or the groups T, Y, RN and the nitrogen atom to which they are connected may form a 4-7-membered lactam ring and wherein the remaining substituents are as defined herein including any tautomers and stereoisomers thereof, or a salt thereof. Representative compounds include (S)-N-(1-{ 4-[1-(2-ethoxy-pyridin-5-yl)-piperidin-4-yI]-phenyl} -ethyl)-acetamide, (S)-1-(1-{ 4-[1-(4-ethoxy-phenyl)-piperidin-4-yl]-phenyl} -ethyl)-3,3-dimethyl-urea, (S)-N-(1-{ 4-[1-(4-cyclopropxy-phenyl)-piperidin-4-yI]-phenyl} -ethyl)-cyclopropane carboxamide, (S)-N-(1-{ 4-[1-(2-fluoro-4-cyclopropylmethyloxy-phenyl)-piperidin-4-yI]-phenyl} -ethyl)-acetamide and (S)-N-(1-{ 4-[1-(4-cyclopropylmethyloxy-phenyl)-piper
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