45 results about "Androgen receptor activity" patented technology

The present invention relates to methods and antagonist compounds for modulating androgen receptor activity. The invention includes a method for identifying molecules that bind to a coactivator binding site of a receptor in the androgen receptor family. Also included is a cocrystal of an androgen receptor ligand binding domain complexed with a ligand and a coactivator. The invention further includes a method for inhibiting androgen receptor activity in a mammal, thereby facilitating treatment of diseases such as prostate cancer.

Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.

The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R¹, R², R³, R^11a, R^11b, R^11c, R^11d, X, n¹, n², and n³ are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

The present invention discloses certain diterpenes that can be used to inhibit androgen receptor activity, induce apoptosis and block cell cycle progression of androgen receptor-dependent cells. Androgen receptor has been associated with various diseases such as prostate cancer, androgeneic alopecia, breast cancer, acne etc. Accordingly, the present invention further discloses methods of treating androgen receptor-associated diseases by administering the disclosed diterpenes.

Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R¹, R², L¹, L², L³, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided.

The invention provides a compound with androgen receptor degradation activity and particularly provides a compound shown as a formula I. Definitions of each group are as shown in the specification. The compound has excellent AR (androgen receptor) degradation activity and can be used for preparing medicines for disease treatment.

The invention relates to the field of traditional Chinese medicine extract, and particularly discloses application of tripterygium wilfordii root extract triptophenolide (CAS number:74285-86-2) as an androgen receptor antagonist and application of triptophenolide to preparation of drugs for treating androgen disorders and drugs for male contraception. A reliable androgen activity screening method is constructed, the inhibiting effect of various kinds of traditional Chinese medicine extract on androgen receptor activity is tested, and finally it is found that the tripterygium wilfordii root extract triptophenolide is a novel androgen receptor antagonist and can inhibit activity of wild type and mutability androgen receptors. Further, anti-prostrate-cancer activity of triptophenolide is tested, and it is found that triptophenolide has good activity for AR (androgen receptor) positive prostrate cancer cells such as LNCaP and 22 RV1.

The invention discloses medicinal composition, synthesis process and medical application of hydantoin derivatives. The compounds have an effect of inhibiting an androgen receptor, and can be used for treating prostatic cancer and other diseases and physiologic derangement related with androgen receptor activity.

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.

The current disclosure reveals a complex regulatory pattern between miR-31 and AR, indicating that miR-31 plays a key role in prostate cancer development and progression. Another aspect of the current disclosure shows that miR-31 directly targets and destabilizes AR mRNA through interaction with the AR mRNA coding sequence showing that miR-31, or a fragment thereof has the ability to act as a novel therapeutic agent in treating cancer. The current disclosure also shows that AR indirectly represses miR-31 expression by binding to the miR-31 promoter region and modulating methyltransferase activity. Another aspect of the current disclosure shows that miR-31 indirectly modulates AR activity by modulating regulators of cell cycle progression. The disclosure further provides an isolated nucleic acid that modulates the activity of the androgen receptor in a cell. The disclosure further provides a method of treating a prostate cancer in a subject, by administering to the subject an effective amount of an agent that modulates the activity or levels of miR-31.

In the method of determining hormonal effects of substances, a test substance is contacted with Ewing sarcoma protein (EWS) or a derivative of it and with an androgen receptor (NR) or a derivative of it; and the effect of the test substance on binding of EWS with the androgen receptor or its derivative or on ligand-induced activity of the androgen receptor is determined, preferably in a cellular system. A method for determining interference in the co-modulator mechanism between androgen receptor and EWS, which includes measurement of androgen receptor and EWS concentrations, is described. A method for identification and characterization of substances that influence the activity of a nuclear receptor, especially androgen receptor, using EWS or a derivative of it is disclosed.

The invention relates to N-aromatic amide compounds represented by general formulas (I) and (II), a preparation method thereof, a pharmaceutical composition and a pharmaceutical preparation containingthe compound represented by the general formula (I) or (II), and applications of the compounds represented by the general formulas (I) and (II) in preparation of drugs used for treating androgen-related diseases. The definitions of R1, R2, R3, R4, R5, R6, W1, W2, W3, W4 and W5 in the general formulas are the same as those in the specifications. The compounds of the general formulas (I) and (II) are capable of binding to androgen receptors, have activity against androgens and degrade androgen receptors. The compound can be used for treating various androgen-related diseases such as prostate cancer, benign prostatic hyperplasia, breast cancer, bladder cancer, ovarian cancer and the like alone or as a composition, and can also be used for treating diseases such as acnes, hirsutism, alopeciaand the like.

A pharmaceutical composition comprising an ailanthone (AIL) compound or a derivative thereof, for the treatment of diseases or conditions caused by, dependent from, or associated with excessive androgen receptor activity. Ailantone compounds have been discovered to be a potent inhibitor of both full-length AR (AR-FL) and constitutively-active truncated AR splice variants (AR-Vs), and are found to possess favorable drug-like properties such as good bioavailability, high solubility, lack of CYP inhibition, and low hepatotoxicity. Methods of treatment are also provided.

One embodiment is directed toward a method for treating an individual with a disorder affected by androgen receptor activity. This method includes administering a therapeutic amount of DL3 (6-amino-2-(2-4-tert-butyl-phenoxy)-ethylsulfanyl)-1H-pyrimidin-4-one) to the individual. In an additional embodiment, the disorder affected by androgen receptor activity includes cancer. Another embodiment is directed toward a method for treating an individual with prostate cancer. This method includes administering to the individual a therapeutic amount of an androgen receptor antagonist which reduces the production of prostate specific antigen and has only negligible androgen receptor agonist effects.