139 results about "PR - Progesterone receptor" patented technology

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.

Compounds of formula I are provided, wherein R₁-R₉ and n are defined herein, and pharmaceutical compositions and kits containing these compounds.

Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R₃-R₅, R₁₀, and R₁₁ are defined herein.

Compounds of formula I, wherein R₁-R₉ and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided.

Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R₃-R₅, R₁₀, and R₁₁ are defined herein.

Compounds of formula I or II are provided, wherein R₁—R₈ are defined herein, and pharmaceutical compositions and kits containing these compounds.

Also provides are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III, wherein R₂—R₄ and R₉ are defined herein.

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.

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.

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.

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.

The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.

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.

The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.

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.

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.

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.

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.

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.

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.

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.

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.

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.

Disclosed herein are compositions and methods of identifying a subject at risk for preterm birth and selecting effective therapies for preventing preterm birth in the subject. The disclosed methods generally involve determining the identity of one or more nucleotides in the progesterone receptor (PR) gene of the subject.

The flavonoid family of phytochemicals, particularly those derived from soy, has received attention regarding their hormonal activity and their effects on human health and disease. The types and amounts of these compounds in soy and other plants are controlled by both constitutive expression and stress-induced biosynthesis. The health benefits of soy may therefore be dependent upon the amounts of the various hormonally active phytochemicals present. We have identified increased biosynthesis of the isoflavonoid phytoalexin compounds, Glyceollins I, II and III, in soy plants grown under stressed conditions (elicited soy), which exhibit marked anti-estrogenic effects on ER function. Here we demonstrate that specific glyceollins, isolated from elicited soy, displayed anti-estrogenic activity, suppressing basal and estrogen stimulated colony formation of ER-positive estrogen dependent breast cancer cells and inhibiting ER-dependent gene expression of progesterone receptor (PgR) and stromal derived factor-1 (SDF1/CXCL12). Examining the effects of glyceollin on in vivo tumor formation/growth we demonstrate the ability of glyceollins to significantly suppress basal and estrogen-stimulated tumor growth of ER-positive MCF-7 breast and BG-1 ovarian carcinoma cells in ovariectomized female nude mice. We further demonstrate that the effects of glyceollins on suppression of tumor growth correlate with inhibition of estrogen stimulated PgR expression. In contrast to the uterotropic activity of tamoxifen the glyceollins displayed no uterine agonist activity. The Glyceollin (I-III) compounds may represent an important component of the health effects of soy as well as represent novel anti-estrogens useful in the prevention or treatment of breast and ovarian carcinoma.