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34 results about "Androgen Receptor Antagonists" patented technology

Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.

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

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

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

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

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

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

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

Imidazoline derivatives, preparation methods thereof, and their applications in medicine

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

Use of monoamine oxidase inhibitors to improve epithelial biology

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.
Owner:PROCTER & GAMBLE CO

Method for preparing novel androgen receptor antagonist

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

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.
Owner:ZHEJIANG UNIV

Aromatic ring and cyclic lactone thiohydantoin compound as well as preparation method and application thereof

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

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

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

Cancer treatment pharmaceutical composition containing cdk inhibitor

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

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

Benzo[f]cyclopenta[c]quinoline derivatives and their application

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.
Owner:ZHEJIANG UNIV

Androgen receptor antagonist, its preparation method and application

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).
Owner:KUNMING JIDA PHARMA

Combinations with a c-19 steroid for treating cancers

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

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

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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