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34 results about "Androgen Receptor Antagonists" patented technology
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Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.
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
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
Diaryl hydantoin compound as androgen receptor antagonist and applications of diaryl hydantoin compound
InactiveCN104341352AOrganic active ingredientsOrganic chemistryHormone refractory prostate cancerNK1 receptor antagonist
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.
Owner:NANJING HENGJIE BIOTECH
Nano composition containing diaminopyrimidine oxide and pyrrolidinyl diaminopyrimidine oxide and preparation method and application of nano composition
ActiveCN109528725AImprove securityImprove stabilityOrganic active ingredientsCosmetic preparations5 Alpha-Reductase InhibitorAntioxidant
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.
Owner:WUHAN BEST CARRIER NANO TECH
Thiohydantoin ternary fused cyclic androgen receptor antagonist and application thereof
ActiveCN106810552AEnhanced inhibitory effectQuite inhibitory activityOrganic active ingredientsOrganic chemistryMedicineAntiandrogen
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.
Owner:CHINA PHARM UNIV
Imidazoline derivatives, preparation methods thereof, and their applications in medicine
ActiveUS9586947B2Optimize dataImproved pharmacokinetic propertiesOrganic active ingredientsOrganic chemistryDiseasePharmaceutical drug
Owner:SHANGHAI HENGRUI PHARM CO LTD +1
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
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
Imidazoline derivatives, preparation methods thereof, and their applications in medicine
ActiveUS20150225381A1Optimize dataImproved pharmacokinetic propertiesBiocideOrganic chemistryDiseasePharmaceutical drug
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.
Owner:SHANGHAI HENGRUI PHARM CO LTD +1
Imidazolidinedione compounds and their uses
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.
Owner:HINOVA PHARM INC
Use of monoamine oxidase inhibitors to improve epithelial biology
Owner:PROCTER & GAMBLE CO
Substituted thiohydantoin derivatives as androgen receptor antagonists
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.
Owner:JANSSEN PHARMA NV
Method for preparing novel androgen receptor antagonist
InactiveCN108218908ARaw materials are easy to getAtom utilization is highGroup 4/14 element organic compoundsOrganic chemistry methodsSingle isomerUtilization rate
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.
Owner:LIANYUNGANG RUNZHONG PHARMA CO LTD +1
Tetrahydrocarbazole structure type androgen receptor antagonist and application thereof
ActiveCN109700804AHigh antagonistic activityOrganic active ingredientsAntineoplastic agentsProstate cancer cellCarbazole
Owner:ZHEJIANG UNIV
Aromatic ring and cyclic lactone thiohydantoin compound as well as preparation method and application thereof
PendingCN114315805AOrganic active ingredientsOrganic chemistryAndrogen Receptor GeneMedicinal chemistry
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.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Androgen receptor antagonists
ActiveUS20170101384A1Inhibitory activityReceptors for hormonesAndrogen Receptor AntagonistsImmunology
Owner:RGT UNIV OF CALIFORNIA
Nuclear receptor modulators and their use for the treatment and prevention of cancer
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.
Owner:UNITED STATES OF AMERICA
Method for treatment of castration-resistant prostate cancer
InactiveUS9205102B2Slow onsetReduce expressionOrganic active ingredientsSugar derivativesCastration resistantCancer research
Owner:THE UNIV OF BRITISH COLUMBIA
Cancer treatment pharmaceutical composition containing cdk inhibitor
PendingUS20220071978A1Effective preventionEffective treatmentOrganic active ingredientsDisease diagnosisPhosphorylationPharmaceutical medicine
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.
Owner:SUMITOMO DAINIPPON PHARMA CO LTD
3,4,6-triaryl-(1,3)-oxazine-2-ketone compound as well as preparation method and application thereof
The invention belongs to the field of pharmaceutical chemistry and relates to a 3,4,6-triaryl-(1,3)-oxazine-2-ketone compound, a preparation method thereof and also a drug composition containing the compound in a formula (I). The 3,4,6-triaryl-(1,3)-oxazine-2-ketone compound and the drug composition are used as an androgen receptor antagonist and can be used for preparing a non-steroidal drug for preventing and / or treating prostatic hyperplasia, prostate cancers, hirsutism, severe androgen-dependent alopecia or acne symptoms or diseases, associated with androgen receptors.
Owner:SICHUAN UNIV
Methods for treating androgen receptor related disorders
InactiveUS20080015207A1Reduce productionNo measurable androgen receptor agonist effectOrganic active ingredientsBiocideAndrogen Receptor AgonistsProstate-specific antigen
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.
Owner:CINCINNATI UNIV OF
New application for imidazo(1,2-A)pyridine compound capable of serving as androgen receptor antagonist
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.
Owner:LANZHOU UNIVERSITY
Thiohydantoin ternary and cyclic androgen receptor antagonists and uses thereof
ActiveCN106810552BEnhanced inhibitory effectQuite inhibitory activityOrganic active ingredientsOrganic chemistryMedicineAntiandrogen
Owner:CHINA PHARM UNIV
Benzo[f]cyclopenta[c]quinoline derivatives and their application
ActiveCN111170943BHigh antagonistic activityOrganic active ingredientsOrganic chemistryDiseasePharmacology
![Benzo[f]cyclopenta[c]quinoline derivatives and their application](https://images-eureka.patsnap.com/patent_img/3f71a077-b7bd-4a88-af04-ff3e61eb3c20/HDA0002378345220000011.png "Benzo[f]cyclopenta[c]quinoline derivatives and their application")
![Benzo[f]cyclopenta[c]quinoline derivatives and their application](https://images-eureka.patsnap.com/patent_img/3f71a077-b7bd-4a88-af04-ff3e61eb3c20/HDA0002378345220000012.png "Benzo[f]cyclopenta[c]quinoline derivatives and their application")
![Benzo[f]cyclopenta[c]quinoline derivatives and their application](https://images-eureka.patsnap.com/patent_img/3f71a077-b7bd-4a88-af04-ff3e61eb3c20/HDA0002378345220000021.png "Benzo[f]cyclopenta[c]quinoline derivatives and their application")
Owner:ZHEJIANG UNIV
Androgen receptor antagonist, its preparation method and application
ActiveCN109593061BNovel structureGood effectOrganic chemistryUrinary disorderPharmaceutical medicineMedicinal chemistry
Owner:KUNMING JIDA PHARMA
Combinations with a c-19 steroid for treating cancers
PendingUS20210346398A1Antineoplastic agentsNitrile/isonitrile active ingredientsAnticarcinogenCancer cell
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.
Owner:CURADIS GMBH
Hydrazone structural type androgen receptor antagonist and application thereof
ActiveCN109700794AHigh antagonistic activityOrganic active ingredientsAntineoplastic agentsProstate cancer cellHydrazone
The application of the invention discloses a hydrazone structural type androgen receptor antagonist and an application thereof, and belongs to the technical field of a biochemical technique. The compound provided by the invention has obvious antagonistic activity to an androgen receptor. Therefore, the compound can be applied to preparation of the androgen receptor antagonist, a prostate cancer cell proliferation inhibitor and a prostate tumor resisting medicine. The compound provided by the invention is used as the medical composition of effective components, and provides a new choice for medicine research on treatment of prostatic cancer.
Owner:ZHEJIANG UNIV
A nano composition containing diaminopyrimidine oxide and pyrrolidinyl diaminopyrimidine oxide, its preparation method and application
ActiveCN109528725BImprove securityImprove stabilityCosmetic preparationsOrganic active ingredientsEnzyme Inhibitor AgentAntiseptic Agent
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.
Owner:WUHAN BEST CARRIER NANO TECH
Use of a mek inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors
The invention relates to the use of a MEK inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors. Specifically, MEK inhibitors are selected from compounds represented by formula (I) or pharmaceutically acceptable salts thereof, and androgen receptor antagonists are selected from compounds represented by formula (II) or pharmaceutically acceptable salts thereof.
Owner:JIANGSU HENGRUI MEDICINE CO LTD
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