34 results about "Androgen Receptor Antagonists" patented technology

The invention relates to tanshinone compounds in the technical field of medicine and applications thereof. The tanshinone compounds contain tanshinone I, tanshinone IIA, cryptotanshinone and dihydrotanshinone I and the structural formulas are shown as below. The method of the invention uses the tanshinone compounds as the active ingredients of the androgen receptor antagonist; the compounds are used alone or used along with the excipient to prepare oral agents or non-oral agents for curing the diseases related to androgen.

The invention relates to diaryl hydantoin compounds of general formula (I), and derivatives, pharmaceutically acceptable salts and solvates of the diaryl hydantoin compounds, as well as applications thereof in treatment of hormone refractory prostate cancer and breast cancer. The structural formula is as shown in the description, wherein R1-R5, G and X are as defined in the description.

The invention provides a nano composition containing diaminopyrimidine oxide and pyrrolidinyl diaminopyrimidine oxide and a preparation method and application of the nano composition, and belongs to the technical field of cosmetics with special functions. The provided nano composition comprises the following components in percentages by mass: 5-20% of diaminopyrimidine oxide, 2.5-10% of pyrrolidinyl diaminopyrimidine oxide, 0.1-10% of 5 alpha-reductase inhibitor, 0.1-10% of an androgen receptor antagonist, 0.1-5% of a vasodilator agent, 0.1-10% of an anti-inflammation bacteriostatic agent, 0.1-5% of an antioxidant, 0.5-10% of phospholipid, 0.1-40% of a softening agent, 0.1-5% of a stabilizer, 0.01-1% of a preservative and the balance of water. By the nano composition, transdermal co-transportation of multi-target hair loss prevention active components is realized, and the nano composition deepens into hair follicles, is synergistic, has double effects of preventing hair loss and promoting hair growing, and can be widely applied to cosmetics for preventing hair loss and promoting hair growing.

The invention discloses a sulfo-imidazole diketone compound represented by the formula (I). The sulfo-imidazole diketone compound can be used as an androgen receptor and can be used to prepare drugs for treating diseases or disorders related with androgen receptors such as cancer, and the like.

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.

New imidazoline derivatives represented by formula (I):

preparation methods thereof, pharmaceutical compositions comprising such derivatives, and applications of such derivatives in preparing androgen receptor antagonists and medicaments for treating diseases such as prostate cancer are described.

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I) as follows:

wherein R₁ and G are defined herein.

The invention relates to a method for preparing a novel androgen receptor antagonist. The method mainly comprising the following step: performing a cyclization reaction on a compound of formula V as shown in the description, thereby obtaining a compound of formula VI as shown in the description. The method has the characteristics of being easy in raw material obtaining, high in atom utilization rate, mild in reaction condition and simple and convenient in aftertreatment; in addition, by controlling stereo-chemical configuration of initial raw materials, ODM-201 and single isomer thereof can bedirectionally synthesized, and the method is simple and controllable in process and applicable to industrial production.

The invention discloses an aromatic ring and cyclic lactone thiohydantoin compound as well as a preparation method and application thereof, the structure is as shown in formula I. In the formula, the definition of each substituent group is as described in the specification and claims. The compound provided by the invention has excellent antagonistic activity on androgen receptors, and can be used as an androgen receptor antagonist for treating prostate cancer patients.

Disclosed herein are compositions and methods for modulating the androgen receptor.

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R₁ to R₅ and X₁ to X₅ are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

Provided is a cancer treatment pharmaceutical composition that contains a CDK inhibitor. A pharmaceutical composition that includes a CDK inhibitor and is for treating cancers that demonstrate resistance to androgen removal therapy. The CDK inhibitor includes alvocidib or a pharmaceutically acceptable salt thereof. The cancers are cancers that demonstrate treatment resistance to androgen receptor antagonists and/or androgen synthesis inhibitors. A cancer treatment composition that includes alvocidib or a pharmaceutically acceptable salt thereof as an active ingredient and is to be administered to subjects that have enhanced androgen receptor phosphorylation.

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.

The invention relates to the technical field of medicines, and provides application of an imidazo(1,2-A)pyridine compound capable of serving as an androgen receptor antagonist in preparing anti-tumor medicines. Through a cell experiment, the imidazo(1,2-A)pyridine compound disclosed by the invention has a function of inhibiting the growth of tumor cells in vitro, can be used for preparing medicines capable of preventing or/and treating benign prostatic hyperplasia, prostatic cancer, woman hirsutism, severe androgen-dependent alopecia or acne symptoms or diseases related to androgen receptors, and has a potential prospect.

The present invention relates to the field of medicine, particularly to novel uses of C-19 steroid compounds, more particularly to C-19 steroids having an androsten-3-one structure with specific structural configurations, in particular at the 4- and/or 17-position, for inhibition of cancer cell growth in combination with another anticancer agent or as second or third line treatment. The present invention particularly relates to selected C-19 steroids inhibiting the proliferation of tumor cells expressing an androgen receptor and show only limited sensitivity to other cancer agents such as aromatase inhibitors, androgen receptor antagonists, androgen synthesis inhibitors, chemotherapeutics as well as CDK4/CDK6 inhibitors.