Patent classifications
C07J71/0005
DIHYDROARTEMISININ-STEROID CONJUGATE AND PREPARATION METHOD AND APPLICATION THEREOF
Described is a dihydroartemisinin-steroid conjugate of formula (I), or a pharmaceutically acceptable salt thereof, where position 10 of dihydroartemisinin is linked to the steroid through a linker X. This application further provides a preparation method of the dihydroartemisinin-steroid conjugate and an application of the dihydroartemisinin-steroid conjugate in the preparation of a drug for treating cancer. The dihydroartemisinin-steroid conjugate of the invention exhibits potent inhibitory activity against various tumor cells and low cytotoxicity, moreover, the conjugate is capable of penetrating the blood-brain barrier, having a broad application prospect.
##STR00001##
Cyclopentanoperhydrophenanthrene framework compounds and preparation method therefor
The present invention pertains to the field of pharmaceutical chemistry, and relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures. These compounds and salts thereof are useful as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Provided herein is a compound of Formula (I)
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein ring D and the substituents are defined herein. Also provided are pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of using the compound of Formula (I) in the treatment of CNS-related disorders.
Method for producing biogas from waste liquid/residue after diosgenin extraction from <i>Dioscorea composita </i>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%.
PHENYL MALEIMIDE LINKER AGENTS
Compounds useful as linker-payload compounds are disclosed. The compounds have the following Structure (I):
##STR00001##
as a stereoisomer, enantiomer or tautomer thereof or a mixture thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, R.sup.4a, and R.sup.4b are as defined herein. Additional compounds, conjugates, methods of preparation, pharmaceutical compositions, and methods of treatment related to conjugates of compounds of Structure (I) and a targeting moiety, or binding fragment thereof, are also provided.
MODIFIED GUAYULE RESIN PRODUCT AND RELATED PROCESSES
Disclosed herein are a modified guayule resin product and related processes for preparing the modified guayule resin product. The modified guayule resin product comprises a mixture of argentatins having at least one functional group, wherein the at least one functional group is provided by a functionalizing compound selected from alkoxysilanes, mercaptosilanes and blocked mercaptosilanes. In a second embodiment, a process for preparing a modified guayule resin product is provided whereby a guayule resin component (comprising a mixture of argentatins) is mixed with a functionalizing compound selected from alkoxysilanes, mercaptosilanes and blocked mercaptosilanes to produce a modified guayule resin comprising functionalized argentatins having at least one functional group provided by the functionalizing compound.
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.
STEROID SAPONINS WITH ANTI-CANCER ACTIVITY
The present invention relates to a new class of steroid saponins that have interesting biological activity. In particular the present invention relates to a class of steroid saponins in which the sugar moiety has been selectively functionalised to introduce a moiety that contains either, (i) a hydrogen ion donor, (ii) a hydrogen ion acceptor or (iii) a combination thereof. These new, water-soluble compounds are found to not only have potent anti-cancer properties per se but also have the ability to promote the immune response in a subject and can thus act as adjuvants for T-cell activation in cancer therapy.
SUBSTITUTED STEROIDS FOR THE TREATMENT OF CANCER
A compound and pharmaceutically acceptable salts thereof for treating cancer, having a structure represented by the following formula (I) or formula (II):
##STR00001##
in which X and Y each individually represent:
##STR00002## R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 individually represents hydrogen atom, acyl having 20 or less carbon atoms, alkyl having 20 or less carbon atoms, alkanoyl having 20 or less carbon atoms, aroyl having 20 or less carbon atoms, aryl having 20 or less carbon atoms, aralkyl having 20 or less carbon atoms, sulfonyl having 20 or less carbon atoms, phosphonyl having 20 or less carbon atoms, or haloacyl having 20 or less carbon atoms.
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.