Cocensys Inc.

Euro-celtique S.a.

Warner-lambert Company

Ravindra B Upasani

Derk J Hogenkamp

Nancy C Lan

Haiji Xia

Phong X Nguyen

David B Fick

Suzanne Ross Kesten

Jonathan L Wright

Neuroactive steroids of the androstane and pregnane series

Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof

Aryl substituted pyrazoles, and pyrroles, and the use thereof

Novel 4-Benzyl piperidine alkylsulfoxide heterocycles are disclosed and their use as subtype selective NMDA receptor antagonists, particularly for the treatment of Parkinson's disease, most preferably in combination with L-DOPA.

4-Benzyl piperidine alkylsulfoxide heterocycles and their use as subtype-selective NMDA receptor antagonists

Methods, compositions, and compounds for modulating the GABA,receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.

Methods for allosteric modulation of the GABA receptor by members of the androstane and pregnane series

Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.

Methods, compositions, and compounds for allosteric modulation of the

Method, compositions, and compounds for allosteric modulation of the

The invention relates to 3.alpha.-hydroxy, 17-(un)substituted derivatives of the androstane series and 3.alpha.-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R.sub.4 =methyl), 19-norandrostanes, and norpregnanes (R.sub.4 =H).

A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.

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Foothill Ranch, CA, United States of America

Ravindra B Upasani