Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
摘要:
A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.
Disclosed are compounds of general formula (I),
wherein the groups R
1
, R
2
, R
a
and R
b
have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.
[EN] NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO<br/>[FR] NOUVEAUX COMPOSÉS, COMPOSITION PHARMACEUTIQUE ET PROCÉDÉS CORRESPONDANTS
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2010149684A1
公开(公告)日:2010-12-29
New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
The invention provides novel substituted azaheterocyclic compounds compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO
申请人:DYCK Brian
公开号:US20110166116A1
公开(公告)日:2011-07-07
New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I):
wherein R
1
, R
2
, R
3
, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
Cyclophane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
申请人:Dr. Karl Thomae GmbH
公开号:EP0450429A1
公开(公告)日:1991-10-09
Die vorliegende Erfindung betrifft Cyclophane der allgemeinen Formel
in der
X₁, X₂, A, R und R₁ bis R₄ wie im Anspruch 1 definiert sind, deren Enantiomere, deren Diastereomere, deren Additionssalze, insbesondere für die pharmazeutische Anwendung deren physiologisch verträgliche Additionssalze, welche wertvolle Eigenschaften aufweisen, insbesondere wertvolle pharmakologische Eigenschaften wie eine blutdrucksenkende und coronardilatatierende sowie eine milde herzfrequenzsenkende Wirkung, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung.