197900-77-9Relevant academic research and scientific papers
PIPERAZINE AMIDE DERIVATIVES
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Page/Page column 24, (2009/03/07)
The invention is concerned with novel piperazine amide derivatives of formula (I) wherein R1 to R11, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
Process for the preparation of enantiomerically enriched cyclic beta-aryl or heteroaryl carbocyclic acids
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Page/Page column 18; 19, (2008/06/13)
The present invention relates to a process for the preparation of cis substituted cyclic β-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme w
Selective α-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity
Patane, Michael A.,DiPardo, Robert M.,Price, RoseAnn P.,Chang, Raymond S. L.,Ransom, Richard W.,O'Malley, Stacey S.,Di Salvo, Jerry,Bock, Mark G.
, p. 2495 - 2500 (2007/10/03)
The anti-anxiety agent ipsapirone has been shown to have modest affinity for α-1 receptors. We disclose the discovery of potent α-1a receptor subtype selective antagonists based on the ipsapiwne structure which possess selectivity versus the 5-HT receptors tested. These antagonists were obtained by tethering a saccharin ring to 4-phenyl-3-carboxyethyl piperidines. The design principles which led to this structural motif are discussed. The synthesis of key analogs, their SAR, as well as results of selected in vitro and in vivo studies are described.
