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46 results about "Androgen receptor activity" patented technology
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The simplified mechanism of action for how it can increase androgen receptors naturally is as follows: Carnitine transports lipids (fat) into the cellular mitochondria to be used as energy -> androgen receptor (AR) activity within those same cells is increased.
Inhibitors for androgen antagonist refractory prostate cancer
InactiveUS20050202440A1Modulating activity of receptorModulate androgen receptor activityCompound screeningApoptosis detectionBinding siteMammal
The present invention relates to methods and antagonist compounds for modulating androgen receptor activity. The invention includes a method for identifying molecules that bind to a coactivator binding site of a receptor in the androgen receptor family. Also included is a cocrystal of an androgen receptor ligand binding domain complexed with a ligand and a coactivator. The invention further includes a method for inhibiting androgen receptor activity in a mammal, thereby facilitating treatment of diseases such as prostate cancer.
Owner:KARO BIO AB +1
Androgen Receptor Modulators
Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.
Owner:KARO BIO AB
Methods for treating androgen receptor dependent disorders including cancers
InactiveUS8450290B2Reduce expressionEffectively decreasedOrganic active ingredientsSugar derivativesMedical disorderIsrapafant
The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers.
Owner:ROCHE INNOVATION CENT COPENHAGEN
Methods for treating androgen receptor dependent disorders including cancers
InactiveUS20110152348A1Reduce expressionEffectively decreasedOrganic active ingredientsSugar derivativesMedical disorderIsrapafant
The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers.
Owner:ROCHE INNOVATION CENT COPENHAGEN
Bisphenol derivatives and their use as androgen receptor activity modulators
Compounds having a structure of Formula I:or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Owner:THE UNIV OF BRITISH COLUMBIA +1
Androgen receptor modulators and methods for their use
InactiveUS20200123117A1Organic chemistryAntineoplastic agentsAndrogen Receptor GenePharmaceutical medicine
The present invention relates to compounds of formula (I)-(VI) and / or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.
Owner:ESSA PHARMA INC
Inhibitors for androgen antagonist refractory prostate cancer
InactiveUS20070087352A9Modulating activity of receptorModulate androgen receptor activityCompound screeningApoptosis detectionBinding siteAndrogen Receptor Gene
The present invention relates to methods and antagonist compounds for modulating androgen receptor activity. The invention includes a method for identifying molecules that bind to a coactivator binding site of a receptor in the androgen receptor family. Also included is a cocrystal of an androgen receptor ligand binding domain complexed with a ligand and a coactivator. The invention further includes a method for inhibiting androgen receptor activity in a mammal, thereby facilitating treatment of diseases such as prostate cancer.
Owner:KARO BIO AB +1
Heterocyclic compounds for cancer imaging and treatment and methods for their use
ActiveUS20180327368A1Organic active ingredientsIsotope introduction to heterocyclic compoundsProstate cancerPharmaceutical medicine
Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, X, n1, n2, and n3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Owner:THE UNIV OF BRITISH COLUMBIA +1
Use certain diterpene compounds in the treatment of androgen receptor-associated diseases
ActiveUS20100022632A1Reduce AR activityInhibitory activityBiocideHydroxy compound active ingredientsAndrogen Receptor GeneApoptosis
The present invention discloses certain diterpenes that can be used to inhibit androgen receptor activity, induce apoptosis and block cell cycle progression of androgen receptor-dependent cells. Androgen receptor has been associated with various diseases such as prostate cancer, androgeneic alopecia, breast cancer, acne etc. Accordingly, the present invention further discloses methods of treating androgen receptor-associated diseases by administering the disclosed diterpenes.
Owner:ACAD SINIC
Androgen receptor modulators and methods for their use
ActiveUS20200247763A1Organic chemistryAntineoplastic agentsAndrogen Receptor GenePharmaceutical medicine
The present invention relates to compounds of formula (I)-(VI) and / or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.
Owner:PROVINCIAL HEALTH SERVICES AUTHORITY +2
Bisphenol ether derivatives and methods for using the same
Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, L1, L2, L3, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Owner:THE UNIV OF BRITISH COLUMBIA +1
Compound with androgen receptor degradation activity
The invention provides a compound with androgen receptor degradation activity and particularly provides a compound shown as a formula I. Definitions of each group are as shown in the specification. The compound has excellent AR (androgen receptor) degradation activity and can be used for preparing medicines for disease treatment.
Owner:SHANGHAI MEIZER PHARM CO LTD
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
Composition, synthesis and application of hydantoin derivatives
The invention discloses medicinal composition, synthesis process and medical application of hydantoin derivatives. The compounds have an effect of inhibiting an androgen receptor, and can be used for treating prostatic cancer and other diseases and physiologic derangement related with androgen receptor activity.
Owner:陈德桂
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
Androgen receptor modulators and methods for their use
ActiveUS20210198213A1Organic chemistrySulfur/selenium/tellurium active ingredientsDiseaseAndrogen Receptor Gene
Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.
Owner:PROVINCIAL HEALTH SERVICES AUTHORTY +2
MiRNA-31 AS A DIAGNOSTIC, PROGNOSTIC AND THERAPEUTIC AGENT IN CANCER
InactiveUS20150104440A1Lower Level RequirementsInhibitory activitySugar derivativesPeptide/protein ingredientsAndrogenMethyltransferase
The current disclosure reveals a complex regulatory pattern between miR-31 and AR, indicating that miR-31 plays a key role in prostate cancer development and progression. Another aspect of the current disclosure shows that miR-31 directly targets and destabilizes AR mRNA through interaction with the AR mRNA coding sequence showing that miR-31, or a fragment thereof has the ability to act as a novel therapeutic agent in treating cancer. The current disclosure also shows that AR indirectly represses miR-31 expression by binding to the miR-31 promoter region and modulating methyltransferase activity. Another aspect of the current disclosure shows that miR-31 indirectly modulates AR activity by modulating regulators of cell cycle progression. The disclosure further provides an isolated nucleic acid that modulates the activity of the androgen receptor in a cell. The disclosure further provides a method of treating a prostate cancer in a subject, by administering to the subject an effective amount of an agent that modulates the activity or levels of miR-31.
Owner:CORNELL UNIVERSITY
Bisphenol ether derivatives and methods for using the same
Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, L1, L2, L3, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Owner:THE UNIV OF BRITISH COLUMBIA +1
Compound with androgen receptor (AR) degradation activity
The invention provides a type of compound with androgen receptor (AR) degradation activity, and specifically provides a compound as shown in the following formula I: (please see the specification forthe formula), wherein all groups are as defined in the specification. The compound has the great AR degradation activity, and can be used for preparing drugs for treatment of AR expression-related diseases.
Owner:SHANGHAI MEIZER PHARM CO LTD
Aromatic amide compound and preparation method and application thereof
ActiveCN108558760AOrganic compound preparationOrganic chemistry methodsDiseaseAndrogen receptor activity
The invention relates to an aromatic amide compound as shown in general formula I, a preparation method of the aromatic amide compound, a pharmaceutical composition containing the compound as shown ingeneral formula I, a pharmaceutic preparation containing the compound as shown in general formula I, and application of the compound as shown in general formula I in preparation of drugs for treatingdiseases related to androgen. In general formula, definitions of R1, R2, R3, R4, R5, R6, X, Y, Q and n are the same as definitions in specification. The compound as shown in general formula I can becombined to an androgen receptor, and has activities of resisting androgen and degrading the androgen receptor. The compound can be independently used as a composition for treating various diseases related to the androgen such as prostate cancer, benign prostate hyperplasia, breast cancer and bladder cancer, and can further be used for treating diseases such as acnes, hirsutism and alopecia.
Owner:杨国宏 +2
Methods for determining hormonal effects of substances using Ewing sarcoma protein and androgen receptor
InactiveUS7208283B2Reliable and sensitive and simple and economic and rapidImprove economyOrganic active ingredientsPeptide/protein ingredientsSubstance useHormones regulation
In the method of determining hormonal effects of substances, a test substance is contacted with Ewing sarcoma protein (EWS) or a derivative of it and with an androgen receptor (NR) or a derivative of it; and the effect of the test substance on binding of EWS with the androgen receptor or its derivative or on ligand-induced activity of the androgen receptor is determined, preferably in a cellular system. A method for determining interference in the co-modulator mechanism between androgen receptor and EWS, which includes measurement of androgen receptor and EWS concentrations, is described. A method for identification and characterization of substances that influence the activity of a nuclear receptor, especially androgen receptor, using EWS or a derivative of it is disclosed.
Owner:SCHERING AG
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
Selective androgen receptor modulators (SARMs) and uses thereof
ActiveUS9139520B2Organic active ingredientsNervous disorderSelective androgen receptor modulatorMedicinal chemistry
Owner:LIGAND PHARMA INC
N-aromatic amide compound and preparation method and application thereof
The invention relates to N-aromatic amide compounds represented by general formulas (I) and (II), a preparation method thereof, a pharmaceutical composition and a pharmaceutical preparation containingthe compound represented by the general formula (I) or (II), and applications of the compounds represented by the general formulas (I) and (II) in preparation of drugs used for treating androgen-related diseases. The definitions of R1, R2, R3, R4, R5, R6, W1, W2, W3, W4 and W5 in the general formulas are the same as those in the specifications. The compounds of the general formulas (I) and (II) are capable of binding to androgen receptors, have activity against androgens and degrade androgen receptors. The compound can be used for treating various androgen-related diseases such as prostate cancer, benign prostatic hyperplasia, breast cancer, bladder cancer, ovarian cancer and the like alone or as a composition, and can also be used for treating diseases such as acnes, hirsutism, alopeciaand the like.
Owner:SHENZHEN EDK PHARM TECH CO LTD
Method for assessing or selecting sebaceous-gland- or hair-follicle-selective androgen receptor activity controlling agent
Owner:KAO CORP
N-Aromatic amide compound and its preparation method and application
The present invention relates to general formula (I) and (II) N-aromatic amide compound and preparation method thereof, the pharmaceutical composition and pharmaceutical preparation containing described general formula (I) or (II) compound and described general formula (I) and (II) the application of the compound in the preparation of medicines for the treatment of androgen-related diseases, R in the general formula 1 , R 2 , R 3 , R 4 , R 5 , R 6 , W 1 , W 2 , W 3 , W 4 and W 5 The definition of is the same as in the specification. The compounds of the general formulas (I) and (II) can bind to the androgen receptor, and have the activity of resisting androgen and degrading the androgen receptor. The compound can be used alone or as a composition for the treatment of various androgen-related diseases, such as prostate cancer, benign prostatic hyperplasia, breast cancer, bladder cancer, ovarian cancer, etc., and can also be used for acne, hirsutism, hair loss and other diseases treat.
Owner:SHENZHEN EDK PHARM TECH CO LTD
Antagonist for mutated androgen receptor
InactiveCN103180309AStrong antagonistic effectImprove anti-tumor effectOrganic active ingredientsOrganic chemistryProstate cancer cellDisease
To provide a novel anticancer drug which is useful for treating prostatic cancer associated with an androgen receptor mutation. [Solution] As the results of intensive studies on mutated androgen-associated diseases for which the conventional anti-androgen drugs are inefficacious, the present inventors found that a compound, said compound being the active ingredient of a medicinal composition according to the present invention, exhibits an effect of inhibiting the transcriptional activation in a human mutated androgen receptor (AR) and has an excellent antitumor effect on a mouse carrying human prostatic cancer cells, thereby completing the present invention. The compound that is the active ingredient of the medicinal composition according to the present invention is useful for treating diseases such as prostatic cancer in which a series of androgen receptors participate.
Owner:ASTELLAS PHARMA INC
Compositions and methods for using androgen signaling inhibitors
PendingUS20220233551A1Amide active ingredientsAntineoplastic agentsPharmaceutical drugAndrogen receptor activity
The present invention relates to the use of compositions for treating or preventing a condition in a subject by inhibiting androgen signaling. The use of composition comprises methods of treating or preventing cancer with agents that inhibit androgen signaling. The pharmaceutical composition will further comprise agents that inhibit Androgen receptor activity, transcription, or expression in a subject.
Owner:GLAX HEALTH LLC
Methods for the evaluation or selection of sebaceous gland or hair follicle selective androgen receptor activity controllers
ActiveCN107429284BOrganic active ingredientsMicrobiological testing/measurementAndrogen Receptor GeneHair follicle
Owner:KAO CORP
Cancer treatment method using ailanthone compounds
ActiveUS20180125814A1Favorable drug-like propertyImprove bioavailabilityOrganic active ingredientsSolubilityDisease
A pharmaceutical composition comprising an ailanthone (AIL) compound or a derivative thereof, for the treatment of diseases or conditions caused by, dependent from, or associated with excessive androgen receptor activity. Ailantone compounds have been discovered to be a potent inhibitor of both full-length AR (AR-FL) and constitutively-active truncated AR splice variants (AR-Vs), and are found to possess favorable drug-like properties such as good bioavailability, high solubility, lack of CYP inhibition, and low hepatotoxicity. Methods of treatment are also provided.
Owner:EAST CHINA NORMAL UNIV
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