Patent classifications
C07J17/00
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
PRODUCTION METHOD OF TELOMERASE ACTIVATORS AND TELOMERASE ACTIVATORS OBTAINED BY THIS METHOD
A method for producing telomerase activators which provide to obtain new/novel molecules (metabolites) from saponin group compounds by using biotransformation with endophytic fungi and telomerase activators obtained by this method. Included is the elucidation of chemical structures and investigation of the effects of telomerase enzyme activation in cells. These molecules have the potential to be used in diseases and/or conditions that can be treated/ameliorated by telomerase activation and associated with telomere shortening (For example; HIV, degenerative diseases, acute and chronic wound healing, ex vivo cell therapies and stem cell proliferation due to increment in vitro and ex-vivo replicative capacity of cells).
Mogroside Biocatalysis Methods
Monk fruit extracts containing mogrol glycosides such as mogroside V may be treated with enzymes under specific reaction conditions to shift distribution of the Siamenoside I reaction product. Modified enzymes are also employed to shift Siamenoside I distribution to increase yield of Siamenoside I and reduce reaction contaminants. Methods of purifying bioconversion reaction product are also described. Siamenoside I obtained using these methods is a useful sweetener and flavor enhancer for food and beverage compositions and the like.
System and method for diagnosis and treatment
This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.
System and method for diagnosis and treatment
This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.
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.
SERIES OF HALOGENATED TETRACYCLIC TRITERPENE DERIVATIVES AND THEIR PREPARATION AND APPLICATION
The invention provides a series of halogenated tetracyclic triterpene derivatives and their preparation and application. It is represented by the following general structural formula:
##STR00001##
R.sub.1 is halogen, R.sub.2 is H, and the halogen is selected from fluorine, chlorine, bromine or iodine; or R.sub.1 and R.sub.2 are each fluorine, and R.sub.3 is an amine, alcohol, amino acid, peptide or phosphate linked to oxygen through an acyl group.
The derivatives are relatively stable in rat whole blood through pharmacokinetic studies. The absolute bioavailability after a single intragastric administration for male and female rats was 15.6% and 28.4% respectively. The mean bioavailability was 22%. The derivatives showed better in vivo activities compared with the existing standard drugs enalapril and sacubitril valsartan sodium. Meanwhile, hydrophilic prodrugs of the tetracyclic triterpenoid derivatives in the present invention were prepared. The derivatives of the present invention can be used for preparing cardiovascular medicines.
SERIES OF HALOGENATED TETRACYCLIC TRITERPENE DERIVATIVES AND THEIR PREPARATION AND APPLICATION
The invention provides a series of halogenated tetracyclic triterpene derivatives and their preparation and application. It is represented by the following general structural formula:
##STR00001##
R.sub.1 is halogen, R.sub.2 is H, and the halogen is selected from fluorine, chlorine, bromine or iodine; or R.sub.1 and R.sub.2 are each fluorine, and R.sub.3 is an amine, alcohol, amino acid, peptide or phosphate linked to oxygen through an acyl group.
The derivatives are relatively stable in rat whole blood through pharmacokinetic studies. The absolute bioavailability after a single intragastric administration for male and female rats was 15.6% and 28.4% respectively. The mean bioavailability was 22%. The derivatives showed better in vivo activities compared with the existing standard drugs enalapril and sacubitril valsartan sodium. Meanwhile, hydrophilic prodrugs of the tetracyclic triterpenoid derivatives in the present invention were prepared. The derivatives of the present invention can be used for preparing cardiovascular medicines.
METHODS OF PRODUCING MOGROSIDES AND COMPOSITIONS COMPRISING SAME AND USES THEREOF
Isolated mogroside and mogrol biosynthetic pathway enzyme polypeptides useful in mogroside biosynthesis are provided. Mogroside biosynthetic pathway enzymes of the invention include squalene epoxidase (SE), epoxy hydratase (EH), cytochrome p450 (Cyp), cucurbitadienol synthase (CDS) and udp-glucosyl-transferase (UGT), Also provided are methods of producing a mogroside using the isolated mogroside and mogrol biosynthetic enzyme polypeptides, the methods comprising contacting a mogrol and/or a glycosylated mogrol (mogroside) with at least one UDP glucose glucosyl transferase (UGT) enzyme polypeptide of the invention catalyzing glucosylation of the mogrol and/or the glucosylated mogrol to produce a mogroside with an additional glucosyl moietie(s), thereby producing the mogroside. Alternatively or additionally provided is a method of synthesizing a mogrol, the method comprising contacting a mogrol precursor substrate with one or more mogrol biosynthetic pathway enzyme polypeptides as described herein catalyzing mogrol synthesis from the mogrol precursor substrate, thereby synthesizing the mogrol.