Patent classifications
C07J71/00
Terpenoid derivatives
It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway. The present invention provides terpenoid derivative A represented by the following formula (I): ##STR00001##
ESTRA-1,3,5(10)-TRIENE COMPOUNDS CONDENSED IN POSITION 16(17) WITH A PYRAZOLE RING AS INHIBITORS OF 17-HSD1
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof
##STR00001##
wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
NOVEL SALTS AND POLYMORPHS OF SCY-078
SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.
COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:
##STR00001##
wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.
Nanoemulsions and methods for cancer therapy
An oxysterol or oxysterol-like compound is provided, which finds use in treating and/or targeting cancer.
METHOD FOR PRODUCING BIOGAS FROM WASTE LIQUID/RESIDUE AFTER DIOSGENIN EXTRACTION FROM DIOSCOREA COMPOSITA BY ALUMINUM CHLORIDE
Disclosed is a method for producing biogas from a waste liquid/residue after diosgenin extraction by aluminum chloride. Specifically, in a fermentation vessel, an anaerobic sludge and a waste residue from diosgenin extraction by aluminum chloride are added at a volatile solids ratio of (1-3):(1-2), or a seeding sludge and a diosgenin waste liquid are added with an organic loading having a VS:COD ratio of (1-2):(1-2); and then the above components are fermented at 35-37° C. for 5-25 d such that biogas is produced. According to the method of the present invention, the maximum cumulative biogas production rates are 255.4 mL/g VS for waste residue and 326.9 mL/g COD for waste liquid, and throughout the fermentation period, ammoniacal nitrogen values are below 1500 mg/L and pH variation is within the normal range, and the COD removal rate for the fermentation broth is 91.11%.
Certain chemical entities, compositions, and methods
Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.
Timosaponin compounds
Provided herein are timosaponin compounds of Formula I, II, III, I′, II′ and III′, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.
C4-MODIFIED OLEANOLIC ACID DERIVATIVES FOR INHIBITION OF IL-17 AND OTHER USES
Disclosed herein are C4 modified oleanolic acid derivatives of the formula:
##STR00001##
as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.
Steroids and protein-conjugates thereof
Described herein are protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.