46 results about "Androgen receptor activity" patented technology

The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers.

The invention relates to the field of medicine primers, and particularly discloses an application of IMB-A6 serving as an androgen receptor antagonist and an application of the IMB-A6 to preparation of androgen imbalance disease treating medicines and male contraception pills. By building a reliable androgen activity screening method, the inhibiting effect of a plurality of medicine primers on androgen receptor activity is tested to finally find that the IMB-A6 is a novel androgen receptor antagonist, and activity of wild and mutagenic androgen receptors can be inhibited. Further, activity of the prostate cancer resistance of the IMB-A6 is tested to find that the IMB-A6 has good activity for AR positive prostate cancer cells such as LNCaP and has no activity for AR negative prostate cancer cells, the expression activity of the androgen receptors can be inhibited, and the IMB-A6 is similar to positive medicines such as enzalutamide.

Provided herein are compounds, such as compounds of Formula I, that bind to androgen receptors and / or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

Provided is a method for searching for a substance capable of controlling the activity of an androgen receptor rapidly, with high accuracy and in a sebaceous-gland- and hair-follicle-selective manner, particularly a method for assessing or selecting a sebaceous-gland- or hair-follicle-selective androgen receptor activity controlling agent. The method comprises (A) applying a substance of interest to a sebaceous gland-originated cell or a hair follicle-originated cell under low-oxygen conditions; (B) measuring the activity of HIF1[alpha] in the cell; (C) comparing the activity measured in step (B) with the activity of HIF1[alpha] in a control group; and (D) assessing the HIF1[alpha] activity-controlling effect of the substance on the basis of the result obtained in step (C).

The present invention relates to general formula (I) and (II) N-aromatic amide compound and preparation method thereof, the pharmaceutical composition and pharmaceutical preparation containing described general formula (I) or (II) compound and described general formula (I) and (II) the application of the compound in the preparation of medicines for the treatment of androgen-related diseases, R in the general formula 1 , R 2 , R 3 , R 4 , R 5 , R 6 , W 1 , W 2 , W 3 , W 4 and W 5 The definition of is the same as in the specification. The compounds of the general formulas (I) and (II) can bind to the androgen receptor, and have the activity of resisting androgen and degrading the androgen receptor. The compound can be used alone or as a composition for the treatment of various androgen-related diseases, such as prostate cancer, benign prostatic hyperplasia, breast cancer, bladder cancer, ovarian cancer, etc., and can also be used for acne, hirsutism, hair loss and other diseases treat.

To provide a novel anticancer drug which is useful for treating prostatic cancer associated with an androgen receptor mutation. [Solution] As the results of intensive studies on mutated androgen-associated diseases for which the conventional anti-androgen drugs are inefficacious, the present inventors found that a compound, said compound being the active ingredient of a medicinal composition according to the present invention, exhibits an effect of inhibiting the transcriptional activation in a human mutated androgen receptor (AR) and has an excellent antitumor effect on a mouse carrying human prostatic cancer cells, thereby completing the present invention. The compound that is the active ingredient of the medicinal composition according to the present invention is useful for treating diseases such as prostatic cancer in which a series of androgen receptors participate.

The present invention provides a method for searching for a substance for rapidly, accurately, and selectively controlling the activity of androgen receptors in sebaceous glands and hair follicles. A method for evaluating or selecting a sebaceous gland or hair follicle selective androgen receptor activity controller, comprising: (A) applying a substance to be tested to cells derived from sebaceous glands or cells derived from hair follicles under hypoxic conditions; B) measuring the activity of HIF1α in the cell; (C) comparing the activity determined in (B) with the activity of HIF1α in the control group; and (D) evaluating the substance to be tested based on the result of (C) The effect of controlling the activity of HIF1α.