Substituted oxygenated heterocycles and thio-analogues: synthesis and biological evaluation as melatonin ligands
摘要:
A new series of substituted oxygenated heterocycles and thio-analogues were synthesized and evaluated as melatonin receptor ligands. The replacement of the indolic moiety of melatonin by heterocyclic skeleton such as 1,4-benzodioxin, 2,3-dihydro-1,4-benzodioxin, chroman, 2,3-dihydro-1,4-benzoxathiin, thiochroman, carrying the amidic chain on the aromatic ring, leads to compounds showing a weak affinity for melatonin receptors, except for the compounds 1cb and 1hb. (C) 2000 Elsevier Science Ltd, All rights reserved.
A series of dihydrobenzopyranyloxypropanolamines and dihydrobenzopyranylethanolamines containing a nitroxy moiety was synthesized. The cardiovascular effects of these compounds were investigated in anesthetized dogs. Some of the compounds exhibited hypotensive activity in combination with β-adrenergic blocking and vasodilating action. The structure-activity relationships are discussed.
The invention relates to compound of general formula (I): ##STR1## wherein: Z represents O or CH.sub.2 n is from 0 to 4 R, X and Y are as defined in the description, and A represents ##STR2## wherein R.sup.1, R.sup.2, R.sup.6, R.sup.7 and T' are as defined in the description, and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
Nouveaux composés alkylaminoindanes, leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent
申请人:ADIR ET COMPAGNIE
公开号:EP0671397A1
公开(公告)日:1995-09-13
L'invention concerne les composés de formule (I):
dans laquelle R₁, R₂, R₂', R₂'', R₂''', R₃ et n sont tels que définis dans la description,
leur isomères optiques,
et leurs sels d'addition à un acide ou une base pharmaceutiquement acceptable.
Médicaments.
Nouveaux composés hétérocycliques, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
申请人:ADIR ET COMPAGNIE
公开号:EP0873993A1
公开(公告)日:1998-10-28
L'invention concerne les composés de formule (I) :
dans laquelle :
Z représente O ou CH2
n vaut 0 à 4
R, X, Y sont tels que définis dans la description
A représente un groupement
dans lesquels R1, R2, R6, R7 et T' sont tels que définis dans la description.
Médicaments.
本发明涉及式 (I) 的化合物:
其中:
Z 代表 O 或 CH2
n 代表 0 至 4
R、X 和 Y 如描述中所定义
A 代表一个基团
其中 R1、R2、R6、R7 和 T' 如说明中所定义。
药物。
Vasopressin antagonist and oxytocin antagonist
申请人:Otsuka Pharmaceutical Company, Limited
公开号:EP1902717A2
公开(公告)日:2008-03-26
An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist.
The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1):
(wherein R1, R2, R3, R4, R5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in Claims 1 and 2) or salt thereof.