发明名称 Alkynyl aryl carboxamides
摘要 The present invention is related to alkynyl aryl carboxamides of Formula (I') and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I') to modulate, notably to inhibit the activity of PTPs. (I') A is a C<SUB>2</SUB>-C<SUB>15 </SUB>alkynyl, C<SUB>2</SUB>-C<SUB>6</SUB>-alkynyl aryl, C<SUB>2</SUB>-C<SUP>6</SUP>-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy' is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R<SUP>1 </SUP>and R<SUP>2 </SUP>are independently from each other is selected from the group consisting of hydrogen or (C<SUB>1</SUB>-C<SUB>6</SUB>)alkyl. R<SUP>4</SUP>and R<SUP>5 </SUP>are each independently from each other selected from the group consisting of H, hydroxy. C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl, carboxy, C<SUB>1</SUB>-C<SUB>6 </SUB>alkoxy, C<SUB>1</SUB>-C<SUB>3 </SUB>alkyl carboxy, C<SUB>2</SUB>-C<SUB>3 </SUB>alkenyl carboxy, C<SUB>2</SUB>-C<SUB>3 </SUB>alkynyl carboxy, amino or R<SUP>4 </SUP>and R<SUP>5 </SUP>may form an unsaturated or saturated heterocyclic ring, whereby at least one of R<SUP>4 </SUP>or R<SUP>5 </SUP>is not a hydrogen or C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl.
申请公布号 US2007105913(A1) 申请公布日期 2007.05.10
申请号 US20040565538 申请日期 2004.07.20
申请人 APPLIED RESEARCH SYSTEMS ARS HOLDINGS N.V. 发明人 SWINNEN DOMINIQUE;GERBER PATRICK;GONZALEZ JEROME;BOMBRUN AGNES;JORAND-LEBRUN CATHERINE
分类号 A61K31/44;A61K31/16;A61K31/192;A61K31/194;A61K31/195;A61K31/24;A61K31/381;A61K31/40;A61K31/4402;A61K31/4406;A61K38/28;A61K45/06;A61P3/00;A61P29/00;C07C233/18;C07C233/20;C07C233/51;C07C233/52;C07C233/54;C07C233/55;C07C233/63;C07C233/81;C07C235/08;C07C235/16;C07C255/19;C07D213/40;C07D213/48;C07D213/81;C07D213/82;C07D231/14;C07D231/56;C07D261/18;C07D307/79;C07D317/68;C07D319/08;C07D333/24;C07D333/70;C07D405/12;C07D407/12;C07D409/12;C07D413/12 主分类号 A61K31/44
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