461 results about "Hormone receptor" patented technology

The present application discloses combinations for treating estrogen receptor-positive and HER2-positive breast cancer patients. The combinations comprise pertuzumab and trastuzumab (e.g. a fixed dose combination of pertuzumab and trastuzumab, PH FDC) plus giredestrant. In one embodiment, the combination further includes a CDK4 / 6 inhibitor, such as abemaciclib or palbociclib.

The invention discloses a novel compound as well as a pharmaceutical composition and application thereof, the novel compound is represented by formula I or pharmaceutically acceptable salt, tautomer, isotope substitute or solvate, the definition of substituent groups is detailed in the specification, and the novel compound can prevent and / or treat thyroid hormone receptor related diseases. # imgabs0 #

The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has an antagonistic activity against thyroid-stimulating hormone receptors and is therefore useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.

Provided herein are oral abiraterone prodrug formulations, related methods and kits, for example, for oral administration to a subject having a sex hormone-dependent benign or malignant disorder such as prostate cancer, an androgen receptor driven cancer, a syndrome due to androgen excess, and / or a syndrome due to glucocorticoid excess such as hypercortisolemia.

Methods of modulating expression of a target gene in a cell are provided. Aspects of the methods contact the cell with a compound having a first moiety covalently linked to a second moiety wherein: (i) the first moiety exhibits specific binding to a first endogenous 10 protein; (ii) the second moiety exhibits specific binding to a second endogenous protein, the second endogenous protein being different from the first endogenous protein; and (iii) upon contact with the cell, the first endogenous protein and the second endogenous protein are spatially complexed with each other by the compound, thereby producing a function in the cell and thereby activating a process that is generally not controlled by any of the first endogenous protein and the second endogenous protein. Wherein the first moiety is targeted to BCL-6; and the second moiety targets any one of an estrogen receptor, an androgen receptor, BRD4, or a cyclin dependent kinase.

The invention discloses application of a reagent for detecting GPR174 gene expression level in CD4 + T cells and / or B cells in preparation of a product for detecting toxic diffuse goiter. The invention provides a detection marker for a toxic diffuse goiter (Graves disease). The detection marker is GPR174 expressed in a CD4 + T cell or a B cell. Experiments prove that compared with healthy people, the expression of GPR174 in CD4 + T cells or B cells in the body of a Graves disease patient is remarkably up-regulated, and the expression level of GPR174 in the CD4 + T cells and the B cells is in positive correlation with the levels of Graves disease thyroid functions FT3 (free triiodothyronine), FT4 (free tetraiodothyronine) and an autoantibody TSAb (thyroid stimulating hormone receptor stimulating antibody). The expression level of the GPR174 in the CD4 + T cell and the B cell is highly related to the occurrence of the Graves disease, and the expression level of the GPR174 in the CD4 + T cell and the B cell can be used as a detection indication of the Graves disease, so that a new thought is provided for detection and treatment of the Graves disease.

The invention belongs to the field of gene engineering, and particularly relates to an ecdysone receptor gene LvECR and application thereof. The base sequence of the ecdysone receptor gene LvECR is as shown in SEQ ID NO: 1. The amino acid sequence of the protein encoded by the LvECR gene is as shown in SEQ ID NO: 2. The invention also discloses an application of the ecdysone receptor gene LvECR in inhibition of pathogenic vibrio infection. It is verified for the first time that the prawn ecdysone receptor gene LvECR plays an important role in prawn acute hepatopancreatic necrosis, disease occurrence can be aggravated by inhibiting expression of the coding gene of the prawn ecdysone receptor gene LvECR, disease symptoms can be reduced by injecting in-vitro recombinant protein of the factor, and the huge application potential of the prawn ecdysone receptor gene LvECR in disease prevention and control is shown.

The invention discloses application of atypical retinoid A-7 in preparation of androgen receptor inhibitors and antitumor drugs, and belongs to the technical field of medicines. It is proved for the first time that AR can be degraded through a CMA pathway, and the atypical retinoid A-7 serving as an AR inhibitor can obviously reduce the AR protein level in prostate cancer cells; in addition, the Atypic retinoids 7 can be used for inhibiting the growth and proliferation capacity of the prostate cancer cells LNCaP; in addition, the invention further provides an anti-tumor medicine composition, the anti-tumor medicine composition comprises the Atypic retinoid-7 and Enzalutamide, and the anti-tumor medicine composition can be used for treating the prostatic cancer and has important clinical significance.

To provide a pharmaceutical composition comprising a novel compound which has a thyroid-stimulating hormone receptor antagonist activity and is useful for the treatment of thyroid-related diseases.SOLUTION: There is provided a pharmaceutical composition comprising a 3,4-dihydroquinolin-2(1H)-one compound represented by a formula (I) or a pharmacologically acceptable salt thereof. A pharmaceutical composition comprising the compound or the pharmacologically acceptable salt thereof has an antagonist activity against thyroid-stimulating hormone receptors and is useful as a therapeutic agent or the like for thyroid-related diseases (for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer).SELECTED DRAWING: None

The invention relates to siRNA for treating androgenetic alopecia, a nano preparation and a preparation method of the siRNA. The siRNA comprises a positive-sense strand and an antisense strand, the positive-sense strand is as shown in SEQ ID NO. 1, and the antisense strand is as shown in SEQ ID NO. 2. The siRNA disclosed by the invention can be used for efficiently and quickly inhibiting the expression of an androgen receptor in vivo and in vitro. When the medicine containing the siRNA is applied to the surface of the alopecia skin, the treatment effect can be quickly achieved, the hair growth speed is increased, and the hair regeneration time of the alopecia part is shorter.

Described herein are heterobifunctional small molecules, methods of making, pharmaceutical compositions and medicaments comprising such heterobifunctional small molecules, and methods of using such heterobifunctional small molecules are described herein, in the treatment of diseases and conditions, such as cancer, autoimmune diseases, and inflammatory diseases.

Disclosed herein are androgen receptor modulators, bifunctional compounds comprising these compounds, pharmaceutical compositions thereof and method for the treatment of androgen receptor-mediated disorders or diseases, wherein the bifunctional compounds are useful for modifying the ubiquitination and subsequent degradation of target polypeptides and proteins, in particular, androgen receptor.

The present disclosure relates to methods of treating prostate cancer in a subject, comprising administering to the subject (a) an androgen receptor inhibitor, and (b) an embryonic ectoderm development (EED) inhibitor, including those methods wherein the prostate cancer has been determined to be resistant to one or more androgen receptor signaling inhibitors (ARSI), including abiraterone.

The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to an N-substituted cyclic amide compound represented by the formula or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has a thyroid-stimulating hormone receptor antagonistic activity and is useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.

An object of the present invention is to provide a novel compound which has thyroid-stimulating hormone receptor antagonist activity and is useful for treating thyroid-related diseases. The present invention relates to a 3,4-dihydroquinolin-2(1H)-one compound represented by the following Formula (I) or a pharmacologically acceptable salt thereof. The compound of the present invention or a pharmacologically acceptable salt thereof have antagonist activity against a thyroid-stimulating hormone receptor and is useful as a therapeutic agent for thyroid-related diseases (for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer).

The purpose of the present invention is to provide a novel compound which has thyroid stimulating hormone receptor antagonist activity and is useful in the treatment of thyroid-related diseases. The present invention relates to a 3, 4-dihydroquinoline-2 (1H)-one compound represented by formula (I) or a pharmacologically acceptable salt thereof. The compound or a pharmacologically acceptable salt thereof according to the present invention has an antagonist activity against a thyroid stimulating hormone receptor, and is useful as a therapeutic agent or the like for thyroid-related diseases such as hyperthyroidism, Graves's disease, thyroid eye disease, and thyroid cancer. # imgabs0 #

The invention discloses an application of rhein in a medicine for inhibiting the activity of a glucocorticoid receptor, the rhein is associated with the glucocorticoid for the first time, and it is found that the rhein achieves the effect of inhibiting the activity of the glucocorticoid receptor by regulating and controlling the glucocorticoid receptor to convert co-activated molecules arginine and glutamic acid rich protein 1 (ARGLU1). Therefore, a basis can be provided for applying the rhein to the preparation of the medicine for inhibiting the activity of the glucocorticoid receptor, and the rhein can achieve an obvious improvement effect on anxiety caused by high-glucocorticoid including corticosterone. Rheinic acid can increase the browning degree of brown fat of mice and UCP1 expression and can induce fat browning, and in combination with mouse experiment results, it is shown that the rheinic acid increases energy consumption of organisms and reduces the body fat content, so that application of the rheinic acid in resisting obesity and improving metabolic syndromes caused by obesity has a prospect, and the rheinic acid can be used for preparing medicines for resisting obesity and improving metabolic syndromes caused by obesity. And more directions are provided for further development and application of the rhein.

The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation / inhibition of Androgen Receptor.

Provided are a combination therapy comprising inavolisib, palbociclib and fulvestrant and methods of treating PIC3CA-mutant, hormone receptor positive (HR+) and HER2 negative (HER2-) locally advanced or metastatic breast cancer comprising administering a therapeutically effective amount of inavolisib, palbociclib and fulvestrant. The combination therapy produces a statistically significant and clinically meaningful improvement to the patient as compared to administering palbociclib and fulvestrant alone to a comparable patient.

The invention relates to a quinoxalinone derivative targeting poly ADP ribose polymerase and an androgen receptor as well as a preparation method and application of the quinoxalinone derivative. The structural formula of the quinoxalinone derivative is as follows: # imgabs0 #, R1 is one of hydrogen, methoxyl, methyl and halogen, the substituent position of R1 is at least one of 5, 6, 7 and 8 sites of a quinoxalinone ring, and X is a carbon atom or a nitrogen atom. The quinoxalinone derivative provided by the invention can be used as an active photosensitizer, a PARP inhibitor and an androgen receptor antagonist and can induce cell synthesis and death, and the process can improve the oxidation state and oxygen concentration in cells and improve the hypoxic microenvironment in tumors, so that the photodynamic therapy effect is further enhanced, namely, the effect of the quinoxalinone derivative is improved. The PDT therapy and the PARP inhibitor have a synergistic effect.

The present disclosure provides a method of treating estrogen receptor-positive (ER+) breast cancer, comprising the combined administration of therapeutically effective amounts of a KAT6A / B inhibitor and a Menin inhibitor to a patient in need thereof.

Disclosed are methods for reducing T cell exhaustion and / or treating male sex biased cancers through the administration of agents that inhibit androgen receptor. In some aspects the methods further comprise the detection of a male sex biased cancer and / or T cell exhaustion via detection of TOX+ and / or T cell factor 1 (TCF1)+ T cells in the tumor microenvironment.

The invention provides a regeneration seedling raising method and system for crop seedlings, and the method comprises the steps: extracting a balance value of growth hormone of an explant in a regeneration culture process from the combination information of a hormone receptor in the regeneration culture process of the explant, and determining a light compensation point of a target crop; performing stepped compensation on the illumination period of the target crop through the light compensation points to obtain compensation characteristics of the illumination period in the regeneration culture process; determining the adjustment interval of the seedling raising temperature of the target crop in each culture stage, and performing light-temperature coupling on the illumination intensity of the target crop according to the adjustment interval of each seedling raising temperature and the compensation characteristic of the illumination period to obtain the coupling characteristic of radiation illumination of the explant of the target crop in each culture stage; and performing staged adjustment on radiation illumination in the regeneration culture process based on each coupling characteristic. Based on the scheme, staged coupling adjustment of radiation illumination in the crop seedling culture process can be achieved.

Provided are methods for administering to a disease or condition afflicted with sex hormone dependence or androgen receptor actuation, sustained release abiraterone prodrug formulations, methods, and kits for parenteral administration in human subjects, such as sex hormone dependent benign or malignant conditions such as prostate cancer, androgen receptor driven cancer, and / or syndromes caused by hyperandrogen.

Provided herein are methods, kits and compositions for the treatment and / or prevention of ovarian cancer through the induction of an immune response against Anti-Mullerian Hormone Receptor, Type II (AMHR2).

Methods for treating a cancer patient with a neutrophil-to-lymphocyte ratio (NLR) greater than 3 are disclosed, comprising administering a nonsteroidal glucocorticoid receptor antagonist (GRA) to such a cancer patient, effective to reduce the patient's NLR. The methods include administering a nonsteroidal GRA and a cancer treatment to such a cancer patient, effective to reduce the patient's NLR and enhance the treatment of the cancer patient. The GRA may be orally administered. The nonsteroidal GRA may be a nonsteroidal compound comprising a heteroaryl ketone fused azadecalin structure (e.g., relacorilant) or an octahydro fused azadecalin structure (e.g., exicorilant). The cancer treatment may include chemotherapy, immunotherapy, radiation therapy, administration of an anti-angiogenic agent, administration of a growth factor inhibitor, and surgery. The methods may enhance the cancer treatment, improve the prognosis of the cancer patient, improve the survival of the cancer patient, and provide beneficial clinical effects and advantages to the patient.

The invention belongs to the technical field of biological medicine, and particularly relates to a reagent for improving ovarian development and a preparation method and application thereof. The reagent for improving ovarian development is prepared by mixing the following raw materials in parts by weight: 20-30 parts of N-acetylcysteine; 5 to 10 parts of tranexamic acid; 3 to 8 parts of creatine; and 3000 parts of water. According to the reagent, the mRNA expression of PKD1P6 and follicle stimulating hormone receptors (FSHR) in ovarian tissues is up-regulated, the activity and functions of cumulus granular cells are enhanced, and apoptosis of the cumulus granular cells is inhibited, so that the effects of effectively promoting follicle development and inhibiting the apoptosis of the cumulus granular cells are achieved.

Provided herein is a compound of formula (I, II, IIA, III), a tautomer or stereoisomer thereof, or a pharmaceutically acceptable salt thereof, which can be used as an Androgen Receptor protein degrader and / or inhibitor. More particularly, the present disclosure concerns the use of the compound of formula (I, II, IIA, III), in the treatment of a disorder or disease in which aberrant androgen receptor (AR) signaling is implicated (e.g., prostate cancer).

The invention relates to the technical field of functional drinks, in particular to a polypeptide synergistically strengthened cubilose collagen composite drink with a breast enlarging function and a preparation method of the polypeptide synergistically strengthened cubilose collagen composite drink. The drink contains fish collagen tripeptide, elastin peptide, cubilose peptide, pueraria mirifica isoflavone, red clover isoflavone and saffron crocus extract. A lipidosome delivery system is adopted to entrap polypeptide to form a nano-scale compound, nano-emulsion entraps phytoestrogen, and berry polyphenol and lipidosome-polypeptide form a stable ternary compound. Through the multi-way synergistic effect that phytoestrogen activates a mammary gland estrogen receptor, polypeptide promotes connective tissue collagen synthesis and cubilose peptide activates a growth factor signal, mammary gland development is remarkably promoted, the breast enlarging effect is achieved, the bioavailability reaches 85% or above, and the retention rate of active ingredients stored at normal temperature for 24 months is larger than 90%.

Sustained-release abiraterone prodrug formulations, methods, and kits for parenteral administration to a human subject having a sex hormone-dependent or androgen receptor driven disease or disorder, such as a sex hormone-dependent benign or malignant disorder such as prostate cancer, an androgen receptor driven cancer, and / or a syndrome due to androgen excess.