Chiral 3-aminopyrrolidines as a rigid diamino scaffold for organocatalysis and organometallic chemistry
摘要:
Over 20 new and easily prepared diamines were screened for the asymmetric Morita-Baylis-Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1-methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to 73% were reached with electron-deficient benzaldehyde derivatives. After a simple deprotonation, one of these diamines was transformed into a chiral mixed aggregate for the enantioselective synthesis of (R)-1-o-tolylethanol with 76% ee. (C) 2010 Elsevier Ltd. All rights reserved.
Chiral 3-aminopyrrolidines as a rigid diamino scaffold for organocatalysis and organometallic chemistry
摘要:
Over 20 new and easily prepared diamines were screened for the asymmetric Morita-Baylis-Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1-methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to 73% were reached with electron-deficient benzaldehyde derivatives. After a simple deprotonation, one of these diamines was transformed into a chiral mixed aggregate for the enantioselective synthesis of (R)-1-o-tolylethanol with 76% ee. (C) 2010 Elsevier Ltd. All rights reserved.
[EN] 5H-ISOTHIAZOLO[4,5-C]PYRIDINE-3,4-DIONE OR 5H-PYRAZOLO[4,3-C]PYRIDIN-3,4-DIONE AS ANTIBACTERIAL COMPOUNDS<br/>[FR] 5H-ISOTHIAZOLO[4,5-C]PYRIDINE-3,4-DIONE OU 5H-PYRAZOLO[4,3-C]PYRIDINE-3,4-DIONE EN TANT QUE COMPOSÉS ANTIBACTÉRIENS
申请人:REDX PHARMA PLC
公开号:WO2015114317A1
公开(公告)日:2015-08-06
This invention relates to antibacterial drug compounds of formula (I) containing a fused isothiazolinone or pyrazolone ring and related compounds. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and in methods of treating bacterial infections. Many of the antibacterial drug compounds contain a isothiazolinone or pyrazolone ring fused to a pyridone ring. The compounds have broad spectrum antibacterial activity but are particularly effective against Gram negative strains. wherein X is selected from S, SO, SO2, O and NR4;
[EN] NOVEL BIS-AMIDES AS ANTIMALARIAL AGENTS<br/>[FR] NOUVEAUX BISAMIDES EN TANT QU'AGENTS ANTIPALUDIQUES
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2010058353A1
公开(公告)日:2010-05-27
The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
NOVEL 3-AMINOALKYL-1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
申请人:FOULON Loic
公开号:US20110059955A1
公开(公告)日:2011-03-10
The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application.
The compounds of the present invention correspond to the formula (I):
in which the variables are as set forth in the specification.
These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V
1a
receptors and some compounds additionally exhibit a strong affinity for AVP V
1b
receptors.
7-(Piperazine-1-Ymethyl)-1H-Indole-2-Carboxylic Acid (Phenyl)-Amide Derivatives and Allied Compounds as P38 Map Kinase Inhibitors for the Treatment of Respiratory Diseases
申请人:Wagner Holger
公开号:US20110269737A1
公开(公告)日:2011-11-03
The present invention provides compounds according to general formula (I)
which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.