Patent classifications
C07J73/00
SMALL MOLECULES ACTIVE AGAINST GRAM-NEGATIVE BACTERIA
Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
SMALL MOLECULES ACTIVE AGAINST GRAM-NEGATIVE BACTERIA
Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
CRYSTALLINE POLYMORPH OF 15B-HYDROXY-OSATERONE ACETATE
Provided is a crystalline polymorphic form A of 15-hydroxy-osaterone acetate having an improved stability (storage stability, pulverization stability, and absorption characteristics). In a powder X-ray diffraction spectrum, characteristic diffraction peaks of the crystalline polymorphic form A of 15-hydroxy-osaterone acetate appear at diffraction angles 2 of 9.60.2, 17.10.2, and 20.20.2. The crystalline polymorphic form A has a melting point of 280 to 283 C. and is a prism crystal.
Esters of steroidal lactam and bis(2-chloroethyl) aminophenoxy propanoic acid derivatives
Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.
NOVEL INHIBITORS OF 17?-HSD7 AND USES THEREOF
Novel chemical agents are described herein. More specifically, a novel inhibitor of 17?-HSD7 for decreasing estradiol concentrations while restoring dihydrotestosterone (DHT) concentrations in breast cancer cells is disclosed herein. In a particular embodiment, the inhibitor of 17?-HSD7 has the following structure: (Formula I) A process for producing the novel inhibitors of 17?-HSD7 and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed.
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STEROID COMPOUNDS
The present application discloses derivatives of steroids, pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and processes for preparation thereof. The compounds and compositions described herein can be used in therapy.
Complex and structurally diverse compounds
The invention a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.
SIALYLTRANSFERASE INHIBITORS AND USES THEREOF
Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease.
ESTERS OF STEROIDAL LACTAM AND BIS(2-CHLOROETHYL) AMINOPHENOXY PROPANOIC ACID DERIVATIVES
Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.
Limonin extraction method
A limonin extraction method, comprising the following steps: step one, raw material extracting or juicing: directly soaking raw material in water or using a presser to directly juice the raw material to obtain the extract; step two, adding salt and adjusting pH: adding a sulfate solid material or saturated sulfate solution to the extract; adjusting pH to 3-7; step three, heating and preserving heat: heating to 20 C.-100 C. and keeping at the temperature for 10 minutes-110 minutes; step four, centrifuging: centrifuging for 10 minutes at a rotational speed of 2500g, and obtaining limonin precipitation. Compared with a traditional method, the raw material in the present invention can directly use the extract liquid or juicing liquid without drying, and recover most limonin in water using a precipitation method without complicated apparatus, and is easy to operate and has a low process cost.