Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and 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.

##STR00001##

Disclosed herein are functionalized 3,4-alkylenedioxythiophene (ADOT+) monomers represented by a chemical formula (CR.sup.1R.sup.2)(CR.sup.3R.sup.4)(CR.sup.4R.sup.6).sub.xO.sub.2H.sub.2S, wherein x=0 or 1; wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is independently selected from hydrogen, a hydrocarbyl moiety, and a heteroatom-containing functional group; and wherein at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 comprises the heteroatom-containing functional group selected from an aldehyde, a maleimide, and their derivatives thereof. Also, disclosed herein are aldehyde derivatives represented by (ADOT-CH.sub.2—NH).sub.pY and a maleimide derivative represented by (ADOT-(CH.sub.2).sub.q—N).sub.pZ where p=1-2 and each of Y and Z is a hydrocarbyl moiety or a biofunctional hydrocarbyl moiety. In an embodiment of the ADOT+ monomers, one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is replaced by a direct bond to an amide group, an azide group, or an ester group of a biofunctional hydrocarbyl moiety. Also, disclosed herein are polymers and copolymers made therefrom.

Compounds of general formula (1):

##STR00001##

wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein;
are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.

Compounds having the formula

##STR00001##

or solvates of the compounds can be used as intermediates in the preparation of the synthetic steroids, Etonogestrel and Desogestrel, as well as other pharmaceutically active agents.

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI formula XII, formula XIII, formula XIV, formula XV, formula XVI, or formula XVII and the methods for the treatment of eye diseases may be formulated for topical eye drop, topical paste, ocular solution, device-drug delivery, oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of glaucoma, presbyopia, IOP, cataract, dry eye and oGVHD.

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):

##STR00001##

wherein: , R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein.

The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

A process for the preparation of 11-methylene steroids from di-keto steroids involves selective olefination of the ketone at position 11 of the di-keto steroids. The resulting 11-methylene steroid products can be used as intermediates in the preparation of the synthetic steroids, Etonogestrel and Desogestrel, as well as other pharmaceutically active agents.

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): ##STR00001##
wherein:
, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.

##STR00001##