Patent classifications
C07J9/00
Pharmaceutical compositions and methods
This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.
Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds of Formula I: ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds of Formula I: ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
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.
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.
PURIFICATION METHOD OF PROGESTERONE
The present disclosure provides a purification method of progesterone. In this method, aldehyde impurities in a progesterone crude product react with a sulfurated nucleophile to yield highly polar hydroxysulfonates and progesterone to realize solubility differentiation, and highly pure progesterone with a content higher than 99.5% and a total aldehyde impurities content lower than 0.2% is obtained through elutriation, filtration, washing a filter cake with water, and drying. The purification method provided by the present disclosure avoids the technical bottleneck of progesterone purification in the prior art, and all reagents and raw materials used during the reaction are inexpensive and easily available, with low equipment requirement and cost input; the purification process is mild and safe, conditions are easy to control, and the purification and recovery rate of the product is high; reagents used cause little environmental pollution, and particularly highly polluting chromium-containing reagents are not used.
Crystalline forms of beta-sitosterol
The present invention relates to a cocrystal of beta-sitosterol or a pharmaceutically acceptable ester thereof or an edible acceptable ester thereof and an organic carboxylic acid coformer, an hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol and a combination that comprises a cocrystal of beta-sitosterol and an organic carboxylic acid; and the hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol. It also relates to processes for their preparation, and compositions containing them, as well as their use as a medicament or dietary supplement or functional food, and in particular in the prophylaxis and/or treatment of a disease or conditions that involves an alteration of lipid metabolism, circulating levels of lipids in the blood and/or lipid composition in tissues and organs.
Crystalline forms of beta-sitosterol
The present invention relates to a cocrystal of beta-sitosterol or a pharmaceutically acceptable ester thereof or an edible acceptable ester thereof and an organic carboxylic acid coformer, an hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol and a combination that comprises a cocrystal of beta-sitosterol and an organic carboxylic acid; and the hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol. It also relates to processes for their preparation, and compositions containing them, as well as their use as a medicament or dietary supplement or functional food, and in particular in the prophylaxis and/or treatment of a disease or conditions that involves an alteration of lipid metabolism, circulating levels of lipids in the blood and/or lipid composition in tissues and organs.
FARNESOID X RECEPTOR MODULATORS
The present invention provides a compound of formula (I):
##STR00001##
or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.
COCRYSTALS OF STEROID AND SECOSTEROID COMPOUNDS AND COMPOSITIONS COMPRISING THEM
It is provided a cocrystal of a compound of formula (I) or of a compound formula (II) wherein X and Y are independently selected from —CH.sub.2— and —C(CH.sub.2)—, provided that al least one of X or Y is —CH.sub.2—; R.sup.1 is —CHCH.sub.3—Z.sub.m—W.sub.n—(CH.sub.2).sub.o-T.sub.p-S, wherein Z is O, and m is 0 or 1; W is R.sup.4CH CHR.sup.5, wherein either R.sup.4 and R.sup.5 are H and the dashed line indicates that there is a single bond, or R.sup.4 and R.sup.5 together are forming a bond and the dashed line indicates that there is a double bond, and n is 0 or 1; o is 0, 1 or 3; T is selected from the group consisting of —CHR.sup.6—, —C(O), wherein R.sup.6 is —OH or —CH.sub.3, and p is 0 or 1; S is selected from the group consisting of H, (C.sub.1-C.sub.3) alkyl optionally substituted by —OH, (C.sub.1-C.sub.3) haloalkyl optionally substituted by —OH, cyclopropyl, or; and R.sup.2 is —H or —OH; R.sup.3 is H or CH.sub.3; and the dashed line in formula (II) indicates a single or a double bond; and a hydrogen bond donor coformer which is a phenolic compound. It is also provided a composition comprising the cocrystal and a personal care product comprising the composition.
##STR00001##