Patent classifications
C07J17/005
SUCROSE ESTER BASED CATIONIC GENE VECTOR AND PREPARATION METHOD THEREOF
The invention provides a class of sucrose ester based cationic lipids and preparation method thereof. The vector prepared using the cationic lipid can be used to deliver nucleic acid. The sucrose ester based cationic lipid is prepared by using a chemical synthesis method in the invention, wherein the synthesis method is simple, and has a relatively high product yield. A composition, including suspension, emulsion, micelle and liposome and the like, can be prepared by mixing the sucrose ester based cationic lipid compound of the invention with a co-lipid. Sucrose ester based cationic lipid complex can be prepared by using the said composition and nucleic acid, which has advantages such as simple preparation, low toxicity and high transfection efficiency, and is a novel and highly efficient gene vector.
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.
OSW-1 analogs and conjugates, and uses thereof
Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.
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), expoxy 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.
GLUCOCORTICOID RECEPTOR AGONISTS
The present invention provides a compound of Formula I:
##STR00001##
wherein R is hydrogen, —P(═O)(OH).sub.2,
##STR00002##
or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, systemic lupus erythematosus, lupus nephritis, and inflammatory bowel disease.
Preparation method of vascular leakage blockers with a high yield
The present invention relates to a preparation method of a novel vascular leakage blocker with a high yield. The preparation method is easy to react and more productive and economical than the conventional method by using an intermediate that can easily remove impurities generated during the reaction. In addition, the preparation method can produce a novel vascular leakage blocker with a high yield by using a new reagent that has not been previously used in the step of generating an isomer, and is very advantageous in producing a high-quality active pharmaceutical ingredient.
Preparation Method of Vascular Leakage Blockers With a High Yield
The present invention relates to a preparation method of a novel vascular leakage blocker with a high yield. The preparation method is easy to react and more productive and economical than the conventional method by using an intermediate that can easily remove impurities generated during the reaction. In addition, the preparation method can produce a novel vascular leakage blocker with a high yield by using a new reagent that has not been previously used in the step of generating an isomer, and is very advantageous in producing a high-quality active pharmaceutical ingredient.
POLYPODOSIDE SWEET FLAVOR MODIFIER
The present invention includes compounds having structural formula (I), wherein R1-R9 are as defined herein, or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
##STR00001##
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.
XYLOGLUCAN-CONTAINING PRODRUGS AND METHODS OF MANUFACTURE AND USE THEREOF
The present application provides compounds, compositions and methods to reduce, alleviate or treat various enteric diseases and disorders, such as inflammatory bowel disease. The compounds are xyloglucan-containing prodrugs, referred to herein as glyco-caged prodrugs, of formula (I) or (II), xyloglucan-β-O—R.sup.D (I), xyloglucan-β-O-L.sup.SI-R.sup.D (II).