5 results about "Anti-Androgen" 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

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.

Herein is reported a class of chiral compounds with paradoxical effects on the androgen receptor (AR). The (R)-enantiomers behave like classical anti-androgens while the (S)-enantiomers activate AR signaling. In castration-resistant prostate cancer, the change during the course of therapy to growth in the presence of AR targeted therapeutics, a harbinger of progression to lethal disease, is commonly attributed to acquired mutations of the AR-ligand binding domain. This is the first report of an antagonist-agonist duality solely due to structural enantiomerism, without any modification to the AR binding site.

Embodiments of the invention are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and / or activity.

A method of treating prostate cancer in a patient comprising administering to the patient a pharmaceutical composition including a first therapeutic including a TLK1B inhibitor, or a pharmaceutically acceptable salt, solvate, ester, amide, clathrate, stereoisomer, enantiomer, prodrug or analog thereof, and a second therapeutic including an antiandrogen or a pharmaceutically acceptable salt, solvate, ester, amide, clathrate, stereoisomer, enantiomer, prodrug or analog thereof.