17 results about "Anti-Androgen" patented technology

The invention discloses 7-aminobenzopyrone or 7-aminoquinolinone compounds and application thereof, the structural general formula of the compounds is as shown in formula (I), and the compounds are compounds with androgen receptor antagonistic activity. The compound provided by the invention has relatively high activity of antagonizing androgen receptor transcription, shows relatively good biological activity at molecular level, cellular level and animal level, and has relatively good safety. Therefore, the compound can be used as an androgen receptor antagonist in preparation of drugs for treating androgen receptor mediated diseases, including but not limited to prostate cancer, metastatic prostate cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, androgen-derived alopecia and acne. The side effect of systemic androgen antagonism caused by systemic distribution can be avoided, and a safer and more targeted treatment choice is provided for patients.

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

A method for treating prostate cancer by administering a first dose of a polyamine inhibitor for a first interval at a beginning of a first treatment cycle; a second dose of the polyamine inhibitor in combination with a dose of an androgen, or a derivative thereof, at a second interval during the first treatment cycle; and a dose of an antiandrogen at a third interval during the first treatment cycle is disclosed.

The invention provides a polymorphic form of a compound shown in a formula (I). The polymorphic form comprises a crystal form 1, a crystal form 2, a crystal form 3 and an amorphous form. The crystal form 1 has good stability, the preparation method is simple and easy to operate, the crystal form 1 is more suitable for large-scale production, and the crystal form 1 has good industrial application value and can be used for preparing drugs for preventing or treating symptoms or diseases related to male hormone disorder, such as androgenetic alopecia, acne and the like. # imgabs0 #

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.

The present invention relates to a method for treating prostate cancer with a combination of an antiandrogen compound and a T-cell engaging molecule that specifically binds to human prostate specific membrane antigen (PSMA) and human CD3. In particular, the present invention relates to a method for treating prostate cancer, including metastatic castration-resistant prostate cancer, in a patient in need thereof, comprising administering to the patient one or more cycles of an antiandrogen compound in combination with a PSMA-targeted T-cell engaging molecule, wherein administration of a first dose of the antiandrogen compound is delayed relative to administration of a first therapeutic dose of the PSMA-targeted T-cell engaging molecule during the first cycle.

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.

The present invention relates to a hair oil composition comprising natural oils only, wherein the natural oils are selected from the group comprising seed oils, fruit oils, nut oils, and plant leaf oils, the composition comprising: a mixture of Kakadu plum oil, pumpkin seed oil, avocado fruit oil, caiaue oil, and rosemary oil, and at least one natural anti-androgen. Furthermore, the invention relates to use of said composition and to a method for treating hair loss diseases.

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.

Provided in the present disclosure are a compound represented by formula I, and a racemate, stereoisomer, tautomer, solvate, polymorph, or pharmaceutically acceptable salts thereof. The compound has good prostate tumor cell proliferation inhibitory activity and anti-AR activity. The compound has good in-vivo metabolic properties, has high AUC and Cmax, is good in druggability, and can be used for preventing and / or treating androgen-related disorders. The compound provided by the invention also has a good hair growth promoting effect, and can effectively increase the number of hair follicles and the growth length of hair.

Pharmaceutical compositions including an effective amount of an antiandrogen or androgen antagonist in combination with a Plk inhibitor and methods of use thereof for treating cancer are disclosed. Administration of the combination of the active agents can be effective to reduce cancer cell proliferation or viability in a subject with cancer to the same degree, or a greater degree than administering to the subject the same amount of either active agent alone. The active agents can be administered together or separately. Methods of selecting and treating subjects with cancers, particular prostate cancers including castration resistant prostate cancer, breast cancers, particularly androgen receptor positive breast cancers, and pancreatic cancers are also provided.

The invention discloses an application of bakuchiol in resisting androgen alopecia. According to the research result of the invention, the bakuchiol is proved to be capable of improving the expression of VEGF (vascular endothelial cell factor) of hair papilla cells, improving the signal expression of beta-catenin (catenin), inhibiting the expression of AR (androgen receptor), inhibiting the expression of TGF-beta2 and inhibiting the expression of NOX4 (nicotinamide adenine dinucleotide phosphate oxidase); the traditional Chinese medicine composition has a good anti-alopecia effect.

The present text describes a method for treating metastatic castration-sensitive prostate cancer with an anti-androgen, which anti-androgen includes but is not limited to 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thia-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide.

A compound represented by formula I, and a racemate, stereoisomer, tautomer, solvate, polymorph, or pharmaceutically acceptable salts thereof are provided. The compound has good prostate tumor cell proliferation inhibitory activity and anti-AR activity. The compound has good in-vivo metabolic properties, has high AUC and Cmax, is good in druggability, and can be used for preventing and / or treating androgen-related disorders. The compound also has a good hair growth promoting effect, and can effectively increase the number of hair follicles and the growth length of hair.

The present invention relates to treatment methods for prostate cancer using a combination of an anti-androgen compound and a T-cell engaging molecule that specifically binds to human prostate-specific membrane antigen (PSMA) and human CD3. In particular, the present invention relates to methods for treating prostate cancer, including metastatic castration-resistant prostate cancer, in a patient in need thereof comprising administering to the patient one or more cycles of an anti-androgen compound in combination with a PSMA-targeted T-cell engaging molecule, wherein administration of the first dose of the anti-androgen compound is delayed relative to administration of the first therapeutic dose of the PSMA-targeted T-cell engaging molecule in the first cycle.