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Neuroactive enantiomeric 15-, 16- and 17-substituted steroids as modulators for gaba type-a receptors

a gaba type-a receptor and neuroactive enantiomeric technology, which is applied in the direction of retrosteroids, drug compositions, organic chemistry, etc., can solve the problems of neuronal inhibition, membrane hyperpolarization, and inhibition of neurotransmitter releas

Active Publication Date: 2016-09-01
WASHINGTON UNIV IN SAINT LOUIS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Activation of the GABAB receptor by GABA causes hyperpolarization and a resultant inhibition of neurotransmitter release.
GABAA receptors are chloride ion channels; as a result, activation of the receptor induces increased inward chloride ion flux, resulting in membrane hyperpolarization and neuronal inhibition.

Method used

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  • Neuroactive enantiomeric 15-, 16- and 17-substituted steroids as modulators for gaba type-a receptors
  • Neuroactive enantiomeric 15-, 16- and 17-substituted steroids as modulators for gaba type-a receptors
  • Neuroactive enantiomeric 15-, 16- and 17-substituted steroids as modulators for gaba type-a receptors

Examples

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examples

[0127]The following Examples describe or illustrate various embodiments of the present disclosure. Other embodiments within the scope of the appended claims will be apparent to a skilled artisan considering the specification or practice of the disclosure as described herein. It is intended that the specification, together with the Examples, be considered exemplary only, with the scope and spirit of the disclosure being indicated by the claims, which follow the Examples.*

Compound Chemistry

[0128]In accordance with the following methods and Examples, the following compounds were prepared for purposes of illustration.

[0129]General Methods.

[0130]Solvents were either used as purchased or dried and purified by standard methodology. Extraction solvents were dried with anhydrous Na2SO4 and after filtration, removed under reduced pressure on a rotary evaporator. Flash column chromatography was performed using silica gel (32-63 μm) purchased from Scientific Adsorbents (Atlanta, Ga.). Melting p...

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Abstract

The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application claims priority benefit of U.S. Provisional Patent Application Ser. No. 61 / 765,228, filed on Feb. 15, 2013, the entire content of which is incorporated herein by reference.GOVERNMENT SUPPORT[0002]The claimed subject matter was developed with Government support under NIH Grant #GM47969, awarded by the National Institute of Health. Accordingly, the Government has certain rights in the claimed subject matter.BACKGROUND OF THE DISCLOSURE[0003]The present disclosure is generally directed to novel compounds having utility as an anesthetic and / or in the treatment of disorders relating to GABA function and activity. More specifically, the present disclosure is directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids, and more specifically ent-steroids, with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof for use as, for example, an anesthetic, as wel...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07J1/00
CPCC07J1/00C07J21/00C07C35/42C07J13/002C07J15/005C07J21/008C07J31/006C07J41/0094C07J51/00C07J61/00C07J63/008C07J71/001C07J75/005C07C43/307C07C2603/26C07C2603/40A61P25/00
Inventor COVEY, DOUGLAS
Owner WASHINGTON UNIV IN SAINT LOUIS