1-(P-THIENYLBENZYL)-IMIDAZOLE ALS AGONISTEN VON ANGIOTENSIN-(1-7)-REZEPTOREN, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE
    1.
    发明公开
    1-(P-THIENYLBENZYL)-IMIDAZOLE ALS AGONISTEN VON ANGIOTENSIN-(1-7)-REZEPTOREN, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权
    1-(P-thienylbenzyl)咪唑类含有它们的血管紧张素 - (1-7)受体激动剂,PROCESS FOR THEIR,它们的用途和药物制剂

    公开(公告)号:EP1185527A1

    公开(公告)日:2002-03-13

    申请号:EP00929466.1

    申请日:2000-04-29

    IPC分类号: C07D409/10 A61K31/415

    CPC分类号: C07D409/10

    摘要: The invention relates to novel 1-(p-thienylbenzyl)-imidazoles of formula (I), wherein radicals R(1)-R(6), X and Y have the meaning cited in the description. Said compounds are potent agonists of angiotensin-(1-7) receptors. As a result of the production and release of vasodilating, antithrombotic and cardioprotective messengers such as cyclic 3',5'-guanosine monophosphate (cGMP) and nitrogen monoxide (NO) associated with the stimulation of said receptors in the endothelial cells, said compounds represent valuable medicaments in the treatment and prophylaxis of hypertension, heart hypertrophy, heart failure, coronary heart diseases such as Angina Pectoris, myocardial infarct, vascular restenosis following angioplasty, cardiomyopathy, endothelial dysfunction or endothelial lesions, e.g. as a result of atherosclerotic processes or in case of Diabetis mellitus and arterial or venous thrombosis.

    CINNAMOYLAMINOALKYL-SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES
    3.
    发明公开
    CINNAMOYLAMINOALKYL-SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES 有权
    肉桂酰氨基取代的苯磺酰胺衍生物

    公开(公告)号:EP1183236A1

    公开(公告)日:2002-03-06

    申请号:EP00938626.9

    申请日:2000-05-06

    摘要: The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula (I) in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y and Z have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death or for improving decreased contractility of the heart. The invention further more relates to processes for the preparation of the compounds of formula (I), their use and pharmaceutical preparations comprising them.

    摘要翻译: 本发明涉及式(I)的肉桂酰氨基烷基取代的苯磺酰胺衍生物,其中A(1),A(2),A(3),R(1),R(2),R(3),R(4) ),X,Y和Z具有权利要求中所示的含义。 式(I)化合物是有价值的药物活性化合物,其表现出例如对心肌和/或心脏神经中对ATP敏感的钾通道的抑制作用,并且适用于例如治疗疾病 心血管系统如冠心病,心律失常,心功能不全或心肌病,或用于预防心脏性猝死或改善心脏收缩性下降。 本发明进一步涉及制备式(I)化合物的方法,其用途以及包含它们的药物制剂。

    ACYLAMINOALKYL-SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES
    7.
    发明公开
    ACYLAMINOALKYL-SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES 有权
    酰氨基 - 取代苯磺酰胺

    公开(公告)号:EP1345892A2

    公开(公告)日:2003-09-24

    申请号:EP01992696.3

    申请日:2001-10-20

    摘要: The present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of formula (I), in which A, R(1), R(2), X, Y and Z have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmaceutical active compounds which have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use and pharmaceutical preparations comprising them.

    P-THIENYLBENZYL-AMIDE ALS AGONISTEN VON ANGIOTENSIN-(1-7)-REZEPTOREN, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE
    9.
    发明公开
    P-THIENYLBENZYL-AMIDE ALS AGONISTEN VON ANGIOTENSIN-(1-7)-REZEPTOREN, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权
    P-thienylbenzyl酰胺含有它们的血管紧张素 - (1-7)受体激动剂,制造,使用方法和药物制剂

    公开(公告)号:EP1370548A1

    公开(公告)日:2003-12-17

    申请号:EP02722180.3

    申请日:2002-03-06

    发明人: HEITSCH, Holger

    CPC分类号: C07D409/12 C07D333/34

    摘要: The invention relates to p-thienylbenzyl-amides of formula (I), in which R(1), R(2), R(3), R(4), R(5), R(6) and X have the meanings as cited in the description. The compounds of formula (I) constitute potent agonists of angiotensin-(1-7)-receptors. Due to the stimulation of these receptors caused by the compounds of formula (I), and to the production and release, on endothelial cells, of the vaso-relaxing and cardioprotective messengers cyclic guanosine monophosphate (cGMP) and nitrogen monoxide (NO), said production and release being associated with the stimulation of said receptors, the compounds of formula (I) are suitable for use as valuable medicament active substances for treating and preventing hypertension, cardiac hypertrophy, cardiac power failure, coronary heart diseases such as angina pectoris and endothelial dysfunction or endothelial damages, e.g. as a consequence of arteriosclerotic processes or in the case of diabetes mellitus.