- NEUROSTEROID COMPOUNDS AND METHODS FOR THEIR PREPARATION AND USE IN TREATING CENTRAL NERVOUS SYSTEM DISORDERS
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Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.
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- COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
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Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
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Page/Page column 146
(2016/05/24)
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- COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
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Described herein are deuterium-enriched neuroactive steroids of the Formula (II) or a pharmaceutically acceptable salt thereof; wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b
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Paragraph 306
(2016/12/12)
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- METHOD FOR MAKING 3α-HYDROXY, 3β- METHYL-5α-PREGNAN-20-ONE (GANAXOLONE)
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Applicants have discovered a method for the stereoselective and regioselective synthesis of 3α-hydroxy, 3β-methyl-5α- pregnan-20-one (ganaxolone) comprising reacting 5α-pregnane-3,20-dione; with an organometallic methylating agent in an inert solvent to provide a compound of the formula.
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Page/Page column 11
(2011/02/24)
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- Use of neurosteroids to treat neuropathic pain
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Ganaxolone (3α-hydroxy-3β-methyl-5β-pregnan-20-one) and 3α-hydroxy-3β-methyl-5β-pregnan-20-one and their physiologically cleavable esters are useful for treating neuropathic pain. Compositions comprising a pharmaceutically acceptable excipient and an appropriate compound, along with methods for preparing the compositions are disclosed. Also disclosed are articles of manufacture wherein the composition is combine with labeling instructions for treating neuropathic pain.
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Page/Page column 4
(2008/06/13)
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- Synthesis and in vitro activity of 3β-substituted-3α-hydroxypregnan- 20-ones: Allosteric modulators of the GABA(A) receptor
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Two naturally occurring metabolites of progesterone, 3α-hydroxy-5α- and 5β-pregnan-20-one (1 and 2), are potent allosteric modulators of the GABA(A) receptor. Their therapeutic potential as anxiolytics, anticonvulsants, and sedative/hypnotics is limited b
- Hogenkamp, Derk J.,Tahir, S. Hasan,Hawkinson, Jon E.,Upasani, Ravi B.,Alauddin, Mian,Kimbrough, Catherine L.,Acosta-Burruel, Manuel,Whittemore,Woodward,Lan, Nancy C.,Gee, Kelvin W.,Bolger, Michael B.
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- Method for making 3α-hydroxy, 3β-substituted-pregnanes
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This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3α-hydroxy,3β-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3α-hydroxy,3β-substituted-20-one form, which can be further modified at the 20-keto position. Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.
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- METHODS, COMPOSITIONS, AND COMPOUNDS FOR ALLOSTERIC MODULATION OF THE GABA RECEPTOR BY MEMBERS OF THE ANDROSTANE AND PREGNANE SERIES
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Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
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