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145 results about "PR - Progesterone receptor" patented technology

The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found inside cells. It is activated by the steroid hormone progesterone.

6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators

Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.
Owner:WYETH LLC

Breast cancer therapy based on hormone receptor status with nanoparticles comprising taxane

The present invention relates to methods and kits for the treatment of breast cancer based on hormone receptor status of progesterone receptor and estrogen receptor comprising the administration of a taxane alone, in combination with at least one other and other therapeutic agents, as well as other treatment modalities useful in the treatment of breast cancer. In particular, the invention relates to the use of nanoparticles comprising paclitaxel and albumin (such as Abraxane®) either alone or in combination with other chemotherapeutic agents or radiation, which may be used for the treatment of breast cancer which does not express estrogen receptor and / or progesterone receptor.
Owner:ABRAXIS BIOSCI LLC

Thio-oxindole derivatives

This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, with estrogen, an estrone, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.
Owner:WYETH LLC

Neuroprotection and myelin repair using nestorone®

ActiveUS20120231052A1Neurodegeneration is prevented and reducedGood effectBiocideOrganic active ingredientsPR - Progesterone receptorAndrogen
Methods for treating neurodegeneration and / or myelination in patients are disclosed comprising treating the patient with a progestin compound which exerts binding to progesterone receptors and elicits progesterone-receptor-induced biological responses without interacting with the androgen receptor and without inducing androgen or glucocorticoid biological responses at a dosage sufficient to prevent or reduce neurodegeneration. The progestin compound preferably comprises 16-methylene-17α-acetoxy-19-norpregn-4-ene-3,20-dione, and the methods include combining the progestin compound with an estrogen compound to provide both contraception and treatment for myelin repair and neurodegeneration.
Owner:THE POPULATION COUNCIL INC

Non-steroidal progesting

The present invention relates to non-steroidal progestins of the general formula (I)whereinR1 and R2 are independently of each other —H or —F,R3 is —CH3 or —CF3, andAr isor a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.
Owner:BAYER SCHERING PHARMA AG

Prognostic biomarkers to predict overall survival and metastatic disease in patients with triple negative breast cancer

The present invention relates to a method for prognosing cancer in a subject with triple negative (TN) breast cancer, whose tumors lack expression of the estrogen receptor (ER), the progesterone receptor (PR) and normal (not amplified) levels of the human epidermal growth factor receptor 2 (HER2). Methods and biomarkers are disclosed that are useful for predicting the overall survival (OS) potential of cancer in a subject with triple negative breast cancer or for predicting metastatic disease in a subject with triple negative breast cancer. For example, the method comprises detecting in a sample from a subject one or more biomarkers selected from the group consisting of ANK3, CD24, EIF1, KLF6, KRAS, KRT1, MAP2K4, SDC4, SLC2A3, STK3, TFAP2C, and WRN. An increase or decrease in one or more biomarkers as compared to a standard is prognostic of OS of TN breast cancer. Likewise, in another example, the method comprises detecting in a sample from a subject one or more biomarkers selected from the group consisting of ANG, DICER1, EIF1, and MSH6. An increase or decrease in one or more biomarkers as compared to a standard is prognostic of metastasis of TN breast cancer.
Owner:VM INST OF RES

Chemical compounds

This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
Owner:SMITHKLINE BECKMAN CORP

Thio-oxindole derivatives

This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein:R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
Owner:WYETH LLC

Cyclothiocarbamate derivatives as progesterone receptor modulators and methods of treating skin disorders

The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is:and wherein R1-R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and conditioning the skin are described. Also provided are novel PR modulators of formula II.
Owner:WYETH LLC

Cyclothiocarbamate derivatives as progesterone receptor modulators

InactiveUS20060142280A1Organic active ingredientsOrganic chemistryProgestin AntagonistDisease
Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.
Owner:WYETH

Benzonitryl and nitrobenzyl derivatives that modulate androgen receptors

This invention relates to benzonitryl and nitrobenzyl derivatives that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds. These compounds are useful, for example, in the treatment or prophylaxis of conditions or disorders that respond to selective androgen receptor modulation.
Owner:SMITHKLINE BECKMAN CORP

Sustained Release Compositions Containing Progesterone Receptor Modulators

Disclosed are sustained release compositions for vaginal or transdermal administration that contain a progesterone receptor modulator such as CDB-2914 (also referred to as VA-2914), and methods of using them for long term contraception or therapeutic purposes. Also disclosed are methods for making the compositions.
Owner:LAB HRA PHARMA SA

Chemical Compounds

This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
Owner:SMITHKLINE BECKMAN CORP

Structure of a glucocorticoid receptor ligand binding domain comprising an expanded binding pocket and methods employing same

A solved three-dimensional crystal structure of a glucocorticord receptor (GR) α ligand binding domain polypeptide is disclosed, in the form of a crystalline glucocorticord receptor α ligand binding domain polypeptide in complex with the ligand fluticasone propionate (FP) and a peptide derived from the co-activator TIF2. The GR / FP / TIF2 structure includes an expanded binding pocket not seen in other GR structures. Methods of designing steroid and non-steroid modulators of the biological activity of GR and other nuclear receptors (NRs) are also disclosed. In another aspect of the present invention homology models of androgen receptor (AR), progesterone receptor (PR) and mineralcorticoid receptor (MR) are disclosed, as well as methods of forming homology models for other NRs. Methods of forming a soluble GR / FP / TIF2 complex are also disclosed.
Owner:SMITHKLINE BECKMAN CORP

Chemical compounds

This invention relates to non-steroidal compounds that are or are believed to be modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
Owner:SMITHKLINE BECKMAN CORP

Synthesis method of progesterone receptor regulating agent ulipristal

The invention provides a new synthesis method of a progesterone receptor regulating agent ulipristal acetate. The method has simple and short steps and mild conditions and is easy to operate, the obtained product has low cost, high yield and high purity, and the method is easy to amplify and is suitable for industrial production.
Owner:杭州容立医药科技有限公司

Multiplex assays for hormonal and growth factor receptors, and uses thereof

The present invention provides compositions and methods for simultaneously detecting mRNA expression levels of hormonal receptors, particularly both estrogen receptor (ER) and progesterone receptor (PR), optionally in combination with growth factor receptors, particularly epidermal growth factor receptor ERBB2 (Her-2), and further optionally in combination with control genes, such as the housekeeping genes NUP214 and / or PPIG. Exemplary embodiments of the invention are useful for determining hormonal receptor and / or growth factor receptor status, particular both ER and PR status and optionally also ERBB2 status, such as for assessing or treating breast cancer.
Owner:CELERA CORPORATION

6-Amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators

Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.
Owner:WYETH LLC

Novel diagnostic and therapeutic methods and reagents therefor

This invention provides novel methods of detecting or treating aberrant cell cycle regulation associated with expression of a nuclear protein encoded by a gene that is linked to map position 8q22.3 of the human genome, and to novel reagents that are useful therefor. More particularly, the invention provides novel nucleic acid and proteinaceous probes, for detecting a gene that is linked to map position 8q22.3 of the human genome or the expression products thereof, wherein expression or elevated expression of said gene is associated with the appearance or occurrence of tumors associated with cancer, DNA damage and progesterone-receptor-mediated effects on cells. The invention also provides reagents and methods for detecting or modulating the expression products of the gene, such as, for example, in the diagnosis or treatment of cancer, cellular proliferation, DNA damage or progesterone receptor-mediated effects on cells.
Owner:GARVAN INST OF MEDICAL RES

Method for purifying ulipristal serving as synthetic progesterone receptor regulator

The invention provides a method for purifying ulipristal serving as a synthetic progesterone receptor regulator. By adopting the method, high-purity ulipristal acetate can be obtained by quickly removing various impurities. The method is easy and convenient to operate, high in yield and suitable for industrial production.
Owner:杭州容立医药科技有限公司

Preventive or remedy for er-negative and her2-negative breast cancer and method of screening the same

The present invention provides (1) an agent for the prevention or treatment of an estrogen receptor-negative and HER2-negative breast cancer comprising an Akt inhibitor, (2) an agent for the prevention or treatment of an estrogen receptor-negative, progesterone receptor-negative and HER2-negative breast cancer comprising an Akt inhibitor, (3) a method of screening an agent for the prevention or treatment of a breast cancer which is negative for hormone receptors such as an estrogen receptor, a progesterone receptor, etc. and is negative for HER2, which comprises using an Akt inhibitory activity as an indicator; and so on.
Owner:TOKAI UNIV +1
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