Neurosteroid derivatives and uses thereof
AssigneeAcerus Pharmaceuticals SRL
InventorsNathan Bryson, Avinash Chander Sharma
Life of this patent
Estimating the term…
Abstract
The present invention contemplates novel neurosteroid derivative compounds, such as derivatives of ganaxolone and allopregnanolone, having improved solubility and bioavailability. The novel neurosteroid derivative compounds are characterized by the following formulas: wherein R1 is methyl or hydrogen, R2 is an ester function (R—C(O)O—), R3 is hydrogen, R4 is alpha or beta hydrogen, R5 is R—CO— or any hydrocarbon structure (R—), and wherein R (in R2 or R5) is independently selected from any structure comprising 10 carbon atoms or fewer, which is linear or branched, saturated or unsaturated, may comprise cyclic or aromatic functions within the structure, and wherein R contains no more than 1 OH or NR2, or 2 ether or thioether functions.
Claims67
A neurosteroid compound having a formula comprising:
- wherein R1 is methyl or hydrogen, R2 is an ester function (R—C(O)O—), R3 is hydrogen, R4 is alpha or beta hydrogen, R5 is R—CO— or any hydrocarbon structure (R—), and wherein R (in R2 or R5) is independently selected from any structure comprising 10 carbon atoms or fewer, which is linear or branched, saturated or unsaturated, may comprise cyclic or aromatic functions within the structure, and wherein R contains no more than 1 OH or NR2, or 2 ether or thioether functions.
A neurosteroid compound having a formula comprising:
- wherein R1 is methyl or hydrogen, R2 is an ester function (R—C(O)O—), R3 is hydrogen, R4 is alpha or beta hydrogen, R5 is R—CO— or any hydrocarbon structure (R—), and wherein R (in R2 or R5) is independently selected from any structure comprising 10 carbon atoms or fewer, which is linear or branched, saturated or unsaturated, may comprise cyclic or aromatic functions within the structure, and wherein R contains no more than 1 OH or NR2, or 2 ether or thioether functions.
A pharmaceutical composition comprising:
- (1) an esterified ganaxalone derivative;
- (2) an oily vehicle;
- and (3) a wetting agent or mixture of wetting agents and/or a pharmaceutically acceptable surfactant or mixture of surfactants.
A pharmaceutical composition comprising:
- (1) an esterified ganaxalone derivative;
- (2) an oily vehicle;
- (3) a wetting agent or mixture of wetting agents and/or a pharmaceutically acceptable surfactant or mixture of surfactants;
- and (5) a thickening agent.
A pharmaceutical composition comprising:
- (1) an esterified ganaxalone derivative;
- (2) an oily vehicle;
- (3) a wetting agent or mixture of wetting agents and/or a pharmaceutically acceptable surfactant or mixture of surfactants;
- (4) a thickening agent;
- and (5) optionally water.
A thixotropic pharmaceutical composition comprising:
- (1) an esterified ganaxalone derivative;
- (2) an oily vehicle;
- (3) a wetting agent or mixture of wetting agents and/or a pharmaceutically acceptable surfactant or mixture of surfactants;
- (4) and a thickening agent;
- and (5) optionally water.
A pharmaceutical composition for treating a subject, e.g., an animal or human, for a medical condition, wherein the subject is in need of treatment for the medical condition, said method composition comprising:
- (a) a neurosteroid selected from a group of neurosteroids consisting of ganaxolone proprionate, ganaxolone enanthate, ganaxolone cypionate, ganaxolone undecanoate, and combinations or mixtures thereof;
- and
- (b) a pharmaceutically acceptable excipient.
Dependencies are inferred from the claim text.