C07J7/0005

BASE-CATALYZED SILYLATION OF TERMINAL ALKYNE C-H BONDS

The present invention is directed to a mild, efficient, and general direct C(sp)-H bond silylation. Various embodiments includes methods, each method comprising or consisting essentially of contacting at least one organic substrate comprising a terminal alkynyl CH bond, with a mixture of at least one organosilane and an alkali metal hydroxide, alkali metal alkoxide, or alkali metal hydride under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the presence or substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.

NEUROACTIVE 13, 17-SUBSTITUTED STEROIDS AS MODULATORS FOR GABA TYPE-A RECEPTORS
20170037079 · 2017-02-09 ·

The present disclosure is generally directed to neuroactive 13, 17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Compositions and methods for inhibiting norovirus infection

A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia is disclosed. The composition may contain a therapeutically effective amount of a binding-inhibiting compound and a carrier and/or excipient. The compounds may competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions may be administered to a human prior to or after infection by a Norovirus, to prevent, ameliorate, or reduce the effects of an infection.

Crystalline anhydrate forms of a pharmaceutical

The invention provides and describes solid state 17-ethynyl-androst-5-ene-3,7,17-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17-ethynyl-androst-5-ene-3,7,17-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17-ethynyl-androst-5-ene-3,7,17-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17-ethynyl-androst-5-ene-3,7,17-triol and uses of such formulations in treating the described conditions.

Base-catalyzed silylation of terminal alkyne C—H bonds

The present invention is directed to a mild, efficient, and general direct C(sp)-H bond silylation. Various embodiments includes methods, each method comprising or consisting essentially of contacting at least one organic substrate comprising a terminal alkynyl CH bond, with a mixture of at least one organosilane and an alkali metal hydroxide, under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.

DHCR24 INHIBITORY COMPOUNDS

The present disclosure relates to compounds suitable for the inhibition of 424-dehydrocholesterol reductase (DHCR24), particularly the selective inhibition of DHCR24. These compounds are for use as therapeutic agents, in particular, agents for use in the treatment and/or prevention of a DHCR24-mediated disorder, such as non-alcoholic steatohepatitis (NASH), atherosclerotic cardiovascular disease (asCVD) or multiple sclerosis (MS).