C07J31/00

Combinations Of Lanosterol Or 25-Hydroxycholesterol Including Derivatives Thereof Useful In The Treatment Of Lens Disorders
20200281944 · 2020-09-10 ·

Novel lanosterol derivatives and novel 25-hydroxycholesterol derivatives including their pharmaceutically acceptable salts as well as methods of treatment and pharmaceutical compositions and formulations of lanosterol and derivatives thereof and 25-hydroxycholesterol and derivatives thereof useful in treating ophthalmic disorders including cataracts and presbyopia.

Neuroactive steroids, compositions, and uses thereof

Compounds are provided according to Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v): ##STR00002##
and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.

Cytotoxic agents that preferentially target leukemia inhibitory factor (LIF) for the treatment of malignancies and as new contraceptive agents
10738075 · 2020-08-11 · ·

Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.

METHODS AND INTERMEDIATES FOR THE PREPARATION BILE ACID DERIVATIVES
20200239515 · 2020-07-30 ·

The present invention relates to methods and novel intermediates useful in the preparation of a compound or a pharmaceutically acceptable salt thereof. An objective of the present invention is to provide methods of preparing bile acid derivatives and novel intermediates. A use of the methods and intermediates described relates to the synthesis of bile acid derivatives which activate both FXR and TGR5.

3,3 DISUBSTITUTED 19-NOR PREGNANE COMPOUNDS, COMPOSITIONS, AND USES THEREOF

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III):

##STR00001##

where R, R.sup.2, R.sup.3, R.sup.3, R.sup.4, R.sup.6a, R.sup.6a, R.sup.11a, and R.sup.11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.

Oxysterols and methods of use thereof

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. ##STR00001##

PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF OBETICHOLIC ACID AND DERIVATIVES THEREOF

A process for the preparation of obeticholic acid and derivatives thereof by: (a) hydrogenation of the double bond and reductive opening of the epoxide of a compound of formula (II) or a salt or solvate thereof

##STR00001## to obtain a compound of formula (IIIa) and/or (IIIb), or salts or solvates thereof

##STR00002## and (b) conversion of a compound of formula (IIIa) and/or a compound of formula (IIIb), or a salt or solvate thereof, into a compound of formula (I), or a salt or solvate thereof

##STR00003##

NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3BETA-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVERS DISEASES AND ATHEROSCLEROSIS
20200157140 · 2020-05-21 ·

5-cholesten, 3, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR.sub. agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.

TASTE-MODIFIED CREATINE SALTS, COMPOUNDS, COMPOSITIONS AND USES THEREOF
20200148632 · 2020-05-14 ·

Provided are embodiments of creatine and creatine ethyl ester (CEE) salts where the anion is an artificial (non-saccharide) taste-modifier. These compounds represent stable white non-hygroscopic solids or semisolids that can readily dissolve in water and buffer solutions. Synthesis of novel creatine salts using environmentally safe solvents such as ethanol resulted in the formation of products in quantitative yields with sodium or potassium chloride as a byproduct. The creatine and creatine alkyl eater derivative salts are stable sweet-tasting compounds that are more palatable to a consumer than creatine or derivatives thereof.

Methods for preparation of bile acids and derivatives thereof
10604544 · 2020-03-31 · ·

The present application relates to a method of preparing compounds of Formula (A) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof. ##STR00001##