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73 results about "Androgen receptor antagonist" patented technology

Androgen receptor antagonists are compounds that block androgen receptors and antagonize the effect of androgens such as testosterone. Several conditions such as hirsutism, acne, and prostate cancer are known to be dependent on androgens and antiandrogens can help alleviate the symptoms of this condition...

Androgen receptor antagonist for resisting prostate cancer

ActiveCN101817787AOrganic active ingredientsOrganic chemistryDiseaseSex hormone receptor
The invention provides an androgen receptor antagonist for resisting the prostate cancer, relates to a sulfoimidazoledione with substituted groups on two nitrogen atoms, and relates to a use of such the compounds as a medicament for treating the diseases or disorders related to the androgen receptor, such as prostate cancer, alopecia or whelk.
Owner:SUZHOU KINTOR PHARMA

Androgen receptor antagonists

The present invention provides an androgen receptor antagonistic agent and a superior prophylactic or therapeutic agent for hormone-sensitive cancer, which contain a compound of the formula: wherein, R1 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R2 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R3 is a hydrogen atom, a hydrocarbon group which may have substituent(s), an acyl group or a heterocyclic group which may have substituent(s), R4 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, and R5 is a cyclic group which may have substituent(s); or a salt thereof, or its prodrug.
Owner:TAKEDA PHARMA CO LTD

Novel curcumin analogues and uses thereof

The present invention relates to compounds capable of acting as androgen receptor, antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.
Owner:THE UNIV OF NORTH CAROLINA AT CHAPEL HILL +2

Tanshinone compounds and applications thereof

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.
Owner:SHANGHAI JIAO TONG UNIV

Sulfo-imidazole diketone androgen receptor antagonist and applications thereof

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.
Owner:刘秀云

Application of triptophenolide as androgen receptor antagonist

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.
Owner:MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI

Combination of Anti-clusterin oligonucleotide with androgen receptor antagonist for the treatment of prostate cancer

A method for treating a mammalian subject afflicted with prostate cancer comprising i) an oligonucleotide which reduces clusterin expression and ii) an androgen receptor antagonist having the structureor a pharmaceutically acceptable salt thereof, each in an amount that when in combination with the other is effective to treat the mammalian subject.
Owner:THE UNIV OF BRITISH COLUMBIA

Application of IMB-A6 serving as androgen receptor antagonist

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.
Owner:MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI

Combination therapy for neoplasia treatment

The present invention relates to an insulin-like growth factor (IGF) receptor antagonist for use in the treatment of prostate neoplasia, including benign prostatic hyperplasia (BPH), prostate cancer, and particularly CRPC, wherein the antagonist is used in combination with an androgen receptor antagonist. An embodiment of the invention is where the androgen receptor antagonist is enzalutamide.
Owner:BOEHRINGER INGELHEIM INT GMBH

Method for Treatment of Castration-Resistant Prostate Cancer

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.
Owner:THE UNIV OF BRITISH COLUMBIA

(Heteroarylmethyl) Thiohydantoins as anticancer drugs

InactiveUS20120238533A1BiocideAmide active ingredientsFlutamideHydroxyflutamide
The invention refers to the use of androgen receptor antagonists for the treatment and / or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.
Owner:BAYER INTELLECTUAL PROPERTY GMBH

Thiohydantoin androgen receptor antagonists for the treatment of cancer

Disclosed are compounds, compositions and methods for treating and / or ameliorating diseases, syndromes, disorders, or conditions associated with AR mutant receptors linked to castration-resistant prostate cancer, in a subject, including a mammal and / or human, in need thereof, who has demonstrated resistance to a first or second generation AR antagonist, comprising, consisting of, and / or consisting essentially of, administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula (I)wherein R1, G, R10, and R11 are defined herein.
Owner:JANSSEN PHARMA NV

Constrained compounds as CGRP-receptor antagonists

The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
Owner:BRISTOL MYERS SQUIBB CO

Application of stachyose in preparation of medicine for treating castration-resistant prostate cancer

The invention discloses application of stachyose in preparation of a medicine for treating castration-resistant prostate cancer, and belongs to the technical field of biological medicine. The application of stachyose provides a new strategy for preparing the medicine for treating the CRPC by combining the stachyose with an androgen receptor antagonist for the first time, and multi-angle and multi-level verification research is carried out. A stachyose and androgen receptor combined pharmaceutical composition can be used for treating the castration-resistant prostate cancer, the effect of enzalutamide on inhibiting the castration-resistant prostate cancer is remarkably improved, a natural compound is applied to the advanced stage of the cancer, and the pharmaceutical composition has important clinical treatment significance.
Owner:JIANGNAN UNIV
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