34 results about "Androgen Receptor Antagonists" patented technology

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.

Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. The imidazolidinedione compounds posses androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.

The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analog, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

The invention discloses a tetrahydrocarbazole structure type androgen receptor antagonist and an application thereof and belongs to the technical field of biochemistry. Two compounds have obvious antagonistic activity on an androgen receptor, so that the compounds can be applied to preparation of the androgen receptor antagonist, a prostate cancer cell proliferation inhibitor and a prostate tumorresisting drug. The invention also provide a pharmaceutical composition containing the compounds as effective components, and a new choice is provided for drug research for treating prostatic cancer at present.

Castrate resistant prostate cancer cell lines exhibiting resistance to the androgen-receptor antagonist enzaluatamide overexpress one or both of IGFBP-2 or IGFBP-5 when compared to non-resistant cell lines. Oligonucleotides that target IGFBP-2 and IGFBP-5 can be used to overcome this resistance or as part of a treatment program when administered concurrently with the administration of androgen-receptor antagonist treatments.

The invention relates to the field of medicinal chemistry, in particular to prostatic cancer resisting compounds (I) and (II) with thiohydantoin diindyl as skeletons and a preparation method of the compounds. The compounds are capable of molecularly antagonizing androgen receptors and excellent in prostatic cancer resisting effect in cellular level and animal level and can be used for preparation of antitumor medicines.

The invention discloses a benzo[f]cyclopenta[c]quinoline derivative and application thereof in preparation of a medicine for treating prostatic cancer, and belongs to the field of medicines. The benzo[f]cyclopenta[c]quinoline compound with the structural formula as shown in the formula (I) has obvious antagonistic activity on an androgen receptor, can be used as an androgen receptor antagonist tobe applied to treatment of androgen receptor related diseases, and provides a new choice for development of drugs for treating prostatic cancer at present.

The present invention relates to a kind of androgen receptor antagonist, its preparation method and application thereof, and the androgen receptor antagonist is a compound represented by general formula (1) and a pharmaceutically acceptable salt thereof (R in the general formula 1 , R 2 , R 3 and R 4 The definition is as shown in the manual).