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73 results about "Androgen receptor antagonist" patented technology
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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
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
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
Thyroid receptor antagonists for the treatment of cardiac and metabolic disorders
InactiveUS7005538B1Organic chemistryOrganic compound preparationNK1 receptor antagonistCCR5 receptor antagonist
Owner:KARO BIO AB
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
Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
InactiveUS20150374721A1Organic active ingredientsMicrobiological testing/measurementLyase inhibitorMolecular Targeted Therapies
Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.
Owner:UNIV OF MARYLAND +2
Application of triptophenolide as androgen receptor antagonist
ActiveCN105497045AAchieve contraceptive effectPrevent proliferationOrganic active ingredientsUrinary disorderProstate cancer cellDisease
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
Imidazolidinedione compounds and their uses
Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said 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.
Owner:HINOVA PHARM INC
Combination of Anti-clusterin oligonucleotide with androgen receptor antagonist for the treatment of prostate cancer
InactiveUS20140088178A1Reduce expressionOrganic active ingredientsGenetic material ingredientsProstate cancerPharmaceutical medicine
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
ActiveCN106902112AEnhanced inhibitory effectHigh activityUrinary disorderDermatological disorderDiseaseProstate cancer cell
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
Tanshinone compounds, preparation method and use thereof
The invention provides tanshinone compounds, a preparation method and use thereof, and relates to the technical field of pharmaceutical chemistry. The tanshinone compounds possess a structure formula I or II as shown in the specification. The use of the tanshinone compounds includes but not limited to anticancer drugs, particularly the treatment of prostate cancer and bladder cancer, and induction of androgen receptor antagonist activity when patients have androgen-related diseases, wherein the androgen-related diseases include but not limited to multi-disease, acne, and spermatogenesis without inhibition in need of suppressing spermatogenesis.
Owner:利川市常大产业技术研究院有限公司
Combination therapy for neoplasia treatment
InactiveUS20140255413A1Improve the level ofOrganic active ingredientsImmunoglobulins against growth factorsInsulin-like growth factorPROSTATE NEOPLASIA
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
Androgen receptor antagonists
InactiveUS20050085467A1Decrease and inhibit activationReduce activationBiocideOrganic chemistryNK1 receptor antagonistBiological activation
Owner:WARNER-LAMBERT CO
Method for Treatment of Castration-Resistant Prostate Cancer
InactiveUS20150157656A1Slow onsetReduce expressionBiocideAmide active ingredientsMedicineCastration resistant
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
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
Combination therapy for neoplasia treatment
ActiveUS20160199488A1Organic active ingredientsImmunoglobulins against growth factorsInsulin-like growth factorPROSTATE NEOPLASIA
Owner:BOEHRINGER INGELHEIM INT GMBH
Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
InactiveUS20160038511A1Organic active ingredientsMicrobiological testing/measurementMolecular Targeted TherapiesLyase inhibitor
Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.
Owner:UNIV OF WASHINGTON +2
Androgen receptor antagonists and uses thereof
ActiveUS8809550B2Reducing and preventing progressionReduce incidenceBiocideOrganic active ingredientsEccentric hypertrophyMuscle loss
Owner:SUZHOU KINTOR PHARMA
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
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
Use of imb-a6 as an androgen receptor antagonist
ActiveCN106902112BEnhanced inhibitory effectHigh activityUrinary disorderDermatological disorderProstate cancer cellDisease
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
Androgen receptor antagonists and uses thereof
ActiveUS9216957B2Reducing and preventing progressionPreventing and counteracting masculinisationOrganic chemistryUrinary disorderEccentric hypertrophyNK1 receptor antagonist
Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.
Owner:SUZHOU KINTOR PHARMA
Application of stachyose in preparation of medicine for treating castration-resistant prostate cancer
ActiveCN113440533AShorten the timeAchieve reuseOrganic active ingredientsAntineoplastic agentsOncologyAdvanced stage
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
Imidazole diketone compound and use thereof
Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess 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.
Owner:HINOVA PHARM INC
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