C07J17/00

Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

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 custom-character 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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20(R)-GINSENOSIDE RG3 POLYACYLATED DERIVATIVES, PREPARATION AND APPLICATION THEREOF
20170327529 · 2017-11-16 ·

The present invention provides 20(R)-ginsenoside Rg3 polyacylated derivatives of the formula (I) and preparation method and anti-tumor application thereof:

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wherein, R═CH.sub.3(CH.sub.2)nCO, n=0˜5.

20(R)-GINSENOSIDE RG3 POLYACYLATED DERIVATIVES, PREPARATION AND APPLICATION THEREOF
20170327529 · 2017-11-16 ·

The present invention provides 20(R)-ginsenoside Rg3 polyacylated derivatives of the formula (I) and preparation method and anti-tumor application thereof:

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wherein, R═CH.sub.3(CH.sub.2)nCO, n=0˜5.

SUCROSE ESTER BASED CATIONIC GENE VECTOR AND PREPARATION METHOD THEREOF
20170326255 · 2017-11-16 ·

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
20220346411 · 2022-11-03 ·

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.

Steroid derivative FXR agonist

The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases. ##STR00001##

METHOD FOR SCREENING ACTIVATOR OF MITOCHONDRIAL ACTIVITY
20170292945 · 2017-10-12 ·

The present invention relates to a method for screening an activator of mitochondrial activity by using gypenoside-treated cells, to a composition for screening an activator of mitochondrial activity, comprising the gypenoside, and to a kit comprising the composition. By using the method for screening an activator of mitochondrial activity of the present invention, it is possible to effectively discover a preparation which can substantially promote the mitochondrial activity, and thus the method is expected to be widely used in developing a therapeutic agent for diseases caused by mitochondrial activity inhibition.

OXYSTEROLS AND METHODS OF USE THEREOF

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

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