Patent classifications
C07J21/00
METHOD FOR SYNTHESIZING URSODEOXYCHOLIC ACID USING BA AS RAW MATERIAL
The present invention discloses a synthesis method of ursodeoxycholic acid by using the plant-derived compound BA as a raw material to synthesize ursodeoxycholic acid through the steps of ethylene glycol or neopentyl glycol protection, oxidation, Wittig reaction, deprotection, reduction and hydrolysis, etc. The raw materials used for the synthesis of ursodeoxycholic acid in the present invention are cheap and easy to get, the synthesis steps are easy to operate, the yield is high, the reaction is environmentally friendly, and the industrial production is convenient.
Neurosteroid compounds and methods for their preparation and use in treating central nervous system disorders
Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.
STEROL ANALOGS AND USES THEREOF
The invention relates to compositions and methods for the preparation, manufacture, and therapeutic use of compositions comprising mRNA and a lipid nanoparticle comprising a compound of the invention and an ionizable lipid.
STEROL ANALOGS AND USES THEREOF
The invention relates to compositions and methods for the preparation, manufacture, and therapeutic use of compositions comprising mRNA and a lipid nanoparticle comprising a compound of the invention and an ionizable lipid.
3.ALPHA.-HYDROXY-17.BETA.-AMIDE NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
Provided herein is a compound of Formula (I) or pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.16, R.sup.17, R.sup.3, R.sup.5, R.sup.19 and R.sup.X are defined herein and wherein R.sup.Y represents optionally substituted heteroaryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
##STR00001##
Neuroactive steroids, compositions, and uses thereof
Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R.sup.1, R.sup.2, R.sup.5, A and L 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##
Methods for onapristone synthesis dehydration and deprotection
Methods and systems for making onapristone (ONA) using acidic hydrolysis and dehydration with sulfuric acid in an alcoholic solution are provided.
Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
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.
Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders
Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein n, R.sup.19, R.sup.5, R.sup.3a, R.sup.6a, R.sup.6b, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.17b, R.sup.15a, R.sup.15b, R.sup.16a and R.sup.16b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders. ##STR00001##
PROCESS FOR THE PREPARATION OF CORTEXOLONE 17alpha-PROPIONATE AND NEW HYDRATED CRYSTALLINE FORM THEREOF
The present invention is directed to a process for the preparation of cortexolone 17α-propionate, comprising a hydrolysis reaction of an ortho-ester of formula (III)
##STR00001## in which R is a hydrogen atom or a methyl group, in the presence of a dilute solution of acetic acid.
The present invention is also directed to a hydrated crystalline form of cortexolone 17α-propionate obtained by such process.