C07J9/00

High intensity sweeteners

Disclosed herein are compounds having structural Formula (I), or salts thereof. These compounds are useful as sweet tasting agents and/or sweetness enhancers. Also disclosed are compositions comprising the present compounds and methods of increasing the sweet taste of ingestible compositions. Furthermore, methods for preparing the compounds are also disclosed.

High intensity sweeteners

Disclosed herein are compounds having structural Formula (I), or salts thereof. These compounds are useful as sweet tasting agents and/or sweetness enhancers. Also disclosed are compositions comprising the present compounds and methods of increasing the sweet taste of ingestible compositions. Furthermore, methods for preparing the compounds are also disclosed.

19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein custom character, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein custom character, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

TGR5 modulators and methods of use thereof

The application relates to compounds of formula A: ##STR00001##
or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

TGR5 modulators and methods of use thereof

The application relates to compounds of formula A: ##STR00001##
or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

PROCESS FOR PREPARING HIGH PURITY ALLOPREGNANOLONE AND INTERMEDIATES THEREOF

The invention relates to an efficient and industrially applicable process for the preparation and purification of allopregnanolone and intermediates thereof without the assistance of column chromatography.

METHOD FOR PREPARING CHENODEOXYCHOLIC ACID DERIVATIVE
20220162256 · 2022-05-26 ·

The present invention relates to a method for preparing a chenodeoxycholic acid derivative. Particularly, disclosed is a method for carrying out one-pot reduction on a compound represented by Formula (VI), i.e., 3α-hydroxyl-ethidene-7-ketone-5β-chole-24-alkamide, to obtain a compound represented by Formula (V), i.e., 3α,7α-dyhydroxyl-6α-ethyl-5β-cholanic acid, and then carrying out salt formation crystallization to obtain a high-purity obeticholic acid sodium salt, a potassium salt, a magnesium salt, and a calcium salt.

Functionalized bile acids for therapeutic and material applications

The subject disclosure is directed to functionalized bile acids, preparation thereof, and usage thereof for therapeutic and material applications. In one embodiment, a method of generating functionalized bile acid materials can comprise directly activating a carboxylic acid of a bile acid compound using a coupling agent comprising an amide or ester compound, thereby generating an intermediate bile acid derivative material. The method can further comprise attaching a functional group material to the intermediate bile acid derivative material by reacting the functional group material and the intermediate bile acid derivative material, thereby generating a functionalized bile acid material.

Functionalized bile acids for therapeutic and material applications

The subject disclosure is directed to functionalized bile acids, preparation thereof, and usage thereof for therapeutic and material applications. In one embodiment, a method of generating functionalized bile acid materials can comprise directly activating a carboxylic acid of a bile acid compound using a coupling agent comprising an amide or ester compound, thereby generating an intermediate bile acid derivative material. The method can further comprise attaching a functional group material to the intermediate bile acid derivative material by reacting the functional group material and the intermediate bile acid derivative material, thereby generating a functionalized bile acid material.