Asymmetric N-(3,3-diphenylpropyl)aminoalkyl esters of 4-aryl-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acids with antihypertensive activity
摘要:
A series of asymmetric 4-aryl-1,4-dihydropyridine-3,5-dicarboxylates characterized by the presence of a 3,3-diphenyl-propylamino moiety in one of the ester groups were synthesized. They exhibited remarkable antihypertensive activity in spontaneously hypertensive rats as well as affinity for the 1,4-dihydropyridines binding site labelled by H-3-nitrendipine in the calcium channel. Introduction of this bulky and lipophilic amine confers to the whole series an elevated level of antihypertensive activity and a long duration of action, a structure-dependent modulation of the activity being found only in the subset characterized by the presence of a branched propylene bridge between the ester and the amino groups. The presence of the amino group is essential for oral activity. Out of this series, compound 9u (Rec 15/2375-lercanidipine) was selected for clinical development and obtained marketing authorization as an antihypertensive in several countries. (C) Elsevier, Paris.
MOLECULAR PRECURSOR COMPOUNDS FOR ZINC-GROUP 13 MIXED OXIDE MATERIALS
申请人:Precursor Energetics, Inc.
公开号:US20150218190A1
公开(公告)日:2015-08-06
Molecular precursor compounds, processes and compositions for making Zn-Group 13 mixed oxide materials including IZO, GZO, AZO and BZO, by providing inks comprising a molecular precursor compound having the formula M
A
a
Zn(OROR)
3a+2
, and printing or depositing the inks on a substrate. The printed or deposited ink films can be treated to convert the molecular precursor compounds to a material.
EFFICIENT CATALYSIS OF HETEROPOLY ACID FOR ALCOHOLYSIS OF EPOXIDE
作者:Yusuke Izumi、Kyoji Hayashi
DOI:10.1246/cl.1980.787
日期:1980.7.5
Heteropoly acid (HPA) was found to catalyze the alcoholysis of epoxide more efficiently than the conventional acid catalysts such as sulfuric acid, perchloric acid and p-toluenesulfonic acid, at 45°C in the homogeneous liquid phase. The reason for the high catalytic activity of HPA is also discussed.
THIADIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
申请人:Chen Li
公开号:US20100152203A1
公开(公告)日:2010-06-17
Compounds of the formula I:
or a pharmaceutically acceptable salt thereof, wherein, R
1
is optionally substituted thiadiazolyl, and R
2
, R
3
, R
4
, R
5
, R
6
, R
7
and R
8
are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X
3
and/or a P2X
2/3
receptor antagonists and methods of making the compounds.
Compounds of the formula (III):
or salts or acyl derivatives thereof, for use as antifungal and antiprotozoal agents are disclosed. Compositions containing the compounds are also disclosed as are method for the preparation of the compounds and intermediates in their preparation.
METHOD FOR PREPARING ORGANIC FLUORIDE-ALIPHATIC COMPOUND AND METHOD FOR PURIFYING ORGANIC FLUORIDE-ALIPHATIC COMPOUND
申请人:The Asan Foundation
公开号:EP3216780A1
公开(公告)日:2017-09-13
The present disclosure relates to a method for preparing a radiopharmaceutical and, specifically, to a method for preparing an organic fluoride-aliphatic compound usable as a radiopharmaceutical, to a method for purifying the prepared organic fluoride-aliphatic compound, and to a method for preparing a radiopharmaceutical by using a cassette comprising a backdraft preventing reaction container. According to the present disclosure, the organic fluoride-aliphatic compound can be prepared and purified through even a simple process at high yield, high efficiency, and high purity, and the radiopharmaceutical can be safely prepared without damage to a synthetic apparatus.