[EN] BIS-ARYL ETHERS CONTAINING N-ACYL AZETIDINE AS EGFR/HER2 INHIBITORS [FR] BIS-ARYL ÉTHERS CONTENANT DE LA N-ACYL AZÉTIDINE EN TANT QU'INHIBITEURS DE L'EGFR/HER2
New oxybenzamide derivatives useful for inhibiting factor Xa or VIIa
申请人:——
公开号:US20020198195A1
公开(公告)日:2002-12-26
The present invention relates to compounds comprising the following formula:
R
0
—Q—X—Q′—W—U—V—G—M (I)
These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.
本发明涉及包含以下公式的化合物:
R
0
—Q—X—Q′—W—U—V—G—M (I)
这些化合物作为药物活性化合物是有用的。它们展现出抗血栓作用,并适用于例如治疗和预防心血管疾病,如血栓栓塞性疾病或再狭窄。这些化合物是血液凝固酶因子Xa(FXa)和/或因子VIIa(FVIIa)的可逆性抑制剂,通常可用于治疗、预防或治愈存在因子Xa和/或因子VIIa不期望活性的情况,或旨在抑制因子Xa和/或因子VIIa的情况。本发明还涉及制备这些化合物的方法、它们的使用方法(例如,作为药品中的活性成分)以及包含它们的药物制剂。
[EN] ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] DÉRIVÉS FUSIONNÉS D'ACIDE CYCLOPENTANE-CARBOXYLIQUE À SUBSTITUTION ACYLAMINO, ET LEUR UTILISATION COMME PRODUITS PHARMACEUTIQUES
申请人:SANOFI AVENTIS
公开号:WO2009135590A1
公开(公告)日:2009-11-12
The present invention relates to compounds of the formula (I), wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use and pharmaceutical compositions comprising them.
The present invention relates to compounds of the formula I,
R0-Q-X-Q'-W-U-V-G-M (I)
in which Q; X; Q', U, V, G and M have the meanings indicated in the claims; R0 is aryl or heteroaryl; and W is selected from aryl, heteroaryl, carbocyclic and heterocyclic groups. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa(FXa) and/or factor VIIa(FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Oxybenzamide derivatives useful for inhibiting factor Xa or Vlla
申请人:Nazare Marc
公开号:US20050165058A1
公开(公告)日:2005-07-28
The present invention relates to compounds comprising the following formula:
R
0
-Q-X-Q′-W—U—V-G-M (I)
These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.
Oxybenzamide derivatives useful for inhibiting factor Xa or viia
申请人:Nazaré Marc
公开号:US06953857B2
公开(公告)日:2005-10-11
The present invention relates to compounds comprising the following formula:
R
0
—Q—X—Q′—W—U—V—G—M (I)
These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.