Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
[EN] DUAL-ACTING ANTIHYPERTENSIVE AGENTS<br/>[FR] AGENTS ANTIHYPERTENSIFS À DOUBLE ACTION
申请人:THERAVANCE INC
公开号:WO2009035543A1
公开(公告)日:2009-03-19
The invention relates to compounds having the formula: (I) wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
[EN] QUINAZOLINE DERIVATIVES FOR USE AGAINST CANCER<br/>[FR] DERIVES DE QUINAZOLINE A UTILISER CONTRE LE CANCER
申请人:ASTRAZENECA AB
公开号:WO2006040526A1
公开(公告)日:2006-04-20
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, X1, R6, r and R7 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
In one aspect, the invention relates to compounds having the formula XII:
where R
a
, R
b
, R
2
, R
7
, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
在一方面,本发明涉及具有公式XII的化合物:
其中R
a
,R
b
,R
2
,R
7
和X如说明书中所定义,或其药用可接受的盐。所述的化合物是具有中性粒细胞弹性蛋白酶抑制活性的化合物的前药。在另一方面,本发明涉及包含这些化合物的药物组合物;使用这些化合物的方法;以及制备这些化合物的过程和中间体。
[EN] NEPRILYSIN INHIBITORS<br/>[FR] INHIBITEURS DE LA NÉPRILYSINE
申请人:THERAVANCE BIOPHARMA R & D IP LLC
公开号:WO2015116786A1
公开(公告)日:2015-08-06
In one aspect, the invention relates to compounds having the formula (I): where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.