Patent classifications
C07J17/00
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and 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.
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SWEETENING COMPOSITIONS AND PROCESSES FOR PREPARING THEM
The invention relates to sweetening compositions obtained from the Luo Han Guo fruit, a member of the Cucurbitaceae family. The compositions are free of bitter-tasting impurities, have a light colour and contain about 16-75% mogroside V and about 30-95% total terpene glycosides on a dry weight basis. A filtered (0.2 μm) solution of the composition in water with a solids content of 1% w/v has an absorbance at 420 nm of about 0.55 or below. Also disclosed is a method of preparing such compositions which includes a heating step to encourage the formation of melanoidins, highly coloured impurities, thereby permitting their removal by filtration providing a lighter coloured product.
Mogrosides and use thereof
The present invention provides a process for preparation of compositions comprising novel mogrosides from fruit of Siraitia grosvenorii. The compositions have superior organoleptic properties compared to known mogroside compositions and are useful in wider range of consumables including foods and beverages.
SAPONIN DERIVATIVES FOR USE IN MEDICINE
The invention relates to a Quillaja saponaria saponin derivative based on a saponin comprising a triterpene aglycone and a first saccharide chain and/or a second saccharide chain, and comprising: an aglycone core structure comprising an aldehyde group which has been derivatised; and/or the first saccharide chain wherein the first saccharide chain comprises a carboxyl group, which has been derivatised; and/or the second saccharide chain wherein the second saccharide chain comprises at least one acetoxy group which has been derivatised. The invention also relates to a first pharmaceutical composition comprising the saponin derivative of the invention. In addition, the invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the invention and a second pharmaceutical composition comprising any one or more of an antibody-toxin conjugate, a receptor-ligand - toxin conjugate, an antibody-drug conjugate, a receptor-ligand - drug conjugate, an antibody-oligonucleotide conjugate or a receptor-ligand - oligonucleotide conjugate. The invention also relates to the first pharmaceutical composition or the pharmaceutical combination of the invention, for use as a medicament, or use in the treatment or prophylaxis of a cancer, an infectious disease, viral infection, hypercholesterolemia, primary hyperoxaluria, haemophilia A, haemophilia B, alpha-1 antitrypsin related liver disease, acute hepatic porphyria, transthyretin-mediated amyloidosis, or an autoimmune disease. Furthermore, the invention relates to an in vitro or ex vivo method for transferring a molecule from outside a cell to inside said cell, comprising contacting said cell with the molecule and with a saponin derivative of the invention.
THERAPEUTIC AGENTS AND METHODS
The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.
THERAPEUTIC AGENTS AND METHODS
The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
High-purity mogrosides and process for their purification
The present invention provides a process for preparation of highly purified mogrosides mixture from low purity mogrosides mixture. The process comprises providing a mixture of low purity mogrosides, dissolving the low purity mogrosides mixture in water or an aqueous alcohol solution to form an initial solution of mogrosides, passing the initial solution through a column system, wherein the column system comprises a plurality of columns, and each column is packed with a sorbent having different affinities to impurities and mogrosides so that one or more columns retains more mogrosides than other columns, washing the columns to remove impurities with an acidic aqueous solution, a basic aqueous solution, and an aqueous alcoholic solution successively, eluting the columns with an aqueous alcohol solution that contains higher alcohol content than the aqueous alcohol solution used in the washing step, wherein the eluate from the columns with high content of mogrosides are combined, and drying the combined eluate to obtain high purity mogrosides with the content of the total mogrosides are more than 70% (w/w). The present invention also provides a sweetener mixture and product comprising high purity mogrosides.
Raman tag
A method of forming a probe, wherein the method includes converting cholenic acid into a compound with a terminal alkyne group, wherein the converting the cholenic acid comprises using a sequence, wherein the sequence comprises synthesizing a THP-protection group, LiAlH4 reduction, Dess-Martin oxidation, and Seyferth-Gilbert-Bestmann homologation. The method additionally includes forming A-Chol by removing the THP-protection. Further, the method includes forming PhA-Chol from the compound with the terminal alkyne group via a palladiumcatalyzed Sonogashira reaction. Additionally, the method includes forming PhDY Chol from the compound with the terminal alkyne group via a coppercatalyzed Cadiot-Chodkiewicz reaction.