公开(公告)号：US08586612B2

公开(公告)日：2013-11-19

申请号：US11761565

申请日：2007-06-12

申请人： Stephanie Hachtel ,  Heinrich Christian Englert ,  Uwe Gerlach ,  Heinz Goegelein ,  Holger Heitsch ,  Karl-Heinz Lehr ,  Stefania Pfeiffer-Marek

发明人： Stephanie Hachtel ,  Heinrich Christian Englert ,  Uwe Gerlach ,  Heinz Goegelein ,  Holger Heitsch ,  Karl-Heinz Lehr ,  Stefania Pfeiffer-Marek

IPC分类号： A61K31/445

CPC分类号： C07D211/96

摘要： The present invention relates to piperidinesulfonylureas and piperidinesulfonylthioureas of formula I, in which A, X, R(1), R(2) and R(3) have the meanings indicated in the claims. The compounds of formula I are valuable active pharmaceutical ingredients which show in particular an inhibiting effect on ATP-sensitive potassium channels of the cardiac muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies or reduced contractility of the heart or for the prevention of sudden cardiac death. The invention further relates to processes for preparing the compounds of formula I, their use and pharmaceutical compositions comprising them.

摘要翻译： 本发明涉及式I的哌啶磺酰脲和哌啶磺酰硫脲，其中A，X，R（1），R（2）和R（3）具有权利要求中所示的含义。 式I的化合物是有价值的活性药物成分，其特别表现出对心肌的ATP敏感性钾通道的抑制作用，并且适用于例如治疗心血管系统疾病如冠心病，心律失常 ，心脏功能不全，心肌病或心脏收缩力降低或预防心源性猝死。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。