7 results about "Androgen receptor activity" patented technology

The present invention provides a compound represented by formula I, its racemate, stereoisomer, tautomer, solvate, crystalline polymorph, or a pharma- ceutically acceptable salt thereof. The compound has good prostate tumor cell proliferation inhibitory activity and anti-AR activity. In addition, the compound has good in vivo metabolism, and has AUC and C max The compounds of the present invention have good hair growth promoting effect and can effectively increase the number of hair follicles and the length of hair growth. [Formula 1] JPEG2025515508000061.jpg30169

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a piperazine (or similar) structure which function as antagonists of androgen receptor activity, and their use as therapeutics for the treatment of cancer (e.g., castration-resistant prostate cancer) and other conditions characterized with androgen receptor activity and / or androgen receptor expression.

The present application relates to a kind of compound with anti-androgen receptor activity and its use, the present application provides the compound shown in formula I, its racemate, stereoisomer, tautomer, solvate, polymorph or their pharmaceutically acceptable salt.The compound has good prostate tumor cell proliferation inhibitory activity and anti-AR activity.The compound has good in vivo metabolic properties, AUC and C max Both are higher, and the drug has good property, can be used for preventing and / or treating male hormone related disorder disease.The compound of the present application also has good hair production promoting effect, can effectively increase the number of hair follicle and the length of hair growth.

Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.

The application provides a compound hormone receptor activity prediction method and device, the method comprises the following steps: obtaining sample compound data with known estrogen and androgen receptor activity; drawing an IC50 value distribution map based on the IC50 value in the sample compound data, and determining a demarcation point of the strength of the estrogen and androgen receptor activity according to the IC50 value distribution map; classifying the compounds in the sample compound data into strong and weak estrogen and androgen receptor activity according to the demarcation point; converting the SMILES code of the compounds in the sample compound data into corresponding fingerprint information; describing the compounds in the sample compound data with the fingerprint information, and labeling the compounds in the sample compound data with the activity strength / weakness as a label to update the sample compound data; training a machine learning model through the updated sample compound data to obtain a compound hormone receptor activity prediction model; and predicting the hormone receptor activity of a to-be-predicted compound with the prediction model.

This invention belongs to the field of biomedical materials technology, specifically relating to an ionic liquid for improving androgenetic alopecia and its applications. The ionic liquid is prepared according to the following steps: L-L-carnitine and succinic acid are reacted under inert conditions to obtain an L-L-carnitine-succinic acid ionic liquid with an ion-hydrogen bond network structure; vanillin is added to the L-L-carnitine-succinic acid ionic liquid, and the mixture is heated and stirred to obtain the ionic liquid. This ionic liquid can function in the microenvironment of dermal papilla cells, improving the hair follicle microenvironment and enhancing the activity of dermal papilla cells, which play a key role in androgenetic alopecia. Furthermore, this drug-loaded ionic liquid can effectively inhibit androgen receptor activity, preventing the binding of androgens and androgen receptors from causing problems such as hair follicle miniaturization and hair loss. Simultaneously, it also has the effect of improving androgenetic alopecia and promoting hair growth.

The present application belongs to the technical field of pharmaceutical crystal chemistry, and specifically relates to anhydrous polymorphs of androgen receptor antagonists, and a preparation method and use thereof. Specifically, the present application provides four anhydrous polymorphs (having crystal forms A, B, C and D respectively) of a compound of formula I, a preparation method of each of the anhydrous polymorphs, a pharmaceutical composition containing the anhydrous polymorphs, and use in preventing, alleviating and / or treating diseases or disorders related to androgen receptor activity.