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アルキニルアリールカルボキサミド
专利权人:
メルク セローノ ソシエテ アノニム
发明人:
スウィンネン,ドミニク,ジェルベ,パトリック,ゴンザレス,ジェローム,ボンブルン,アグネス,ヨラン-ルブラン,カトリーヌ
申请号:
JP2006520835
公开号:
JP5198768B2
申请日:
2004.07.20
申请国别(地区):
JP
年份:
2013
代理人:
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 C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-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. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
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