306 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 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.

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 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.

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

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.

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 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.

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 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.

The invention relates to a difunctional chimera heterocyclic compound for targeted degradation of an androgen receptor and application of the difunctional chimera heterocyclic compound, and particularly provides a compound shown in a formula (I), or an isotope compound of the compound, or an optical isomer of the compound, or a tautomer of the compound, or a pharmaceutically acceptable salt of the compound, or a prodrug of the compound, or a solvate of the compound, aRB is an androgen receptor recognition / combination part, L is a linking part, and U is a ubiquitin protease recognition / combination part; the three parts are connected through chemical bonds. The compound provided by the invention can degrade androgen receptors in prostate cancer cells in a targeted manner and inhibit proliferation of the prostate cancer cells, and also shows good metabolic stability and pharmacokinetic properties. The compound provided by the invention has a good application prospect in preparation of a protein degradation targeting chimera of an androgen receptor and in preparation of drugs for treating related diseases (including prostatic cancer, breast cancer and Kenildie disease) regulated and controlled by the androgen receptor. # imgabs0 #

Described herein are growth hormone receptor antagonists and modified growth hormone receptor antagonists. The growth hormone receptor antagonists and modified growth hormone receptor antagonists are useful in treating diseases or conditions, such as cancer and acromegaly, that are responsive to human growth hormone receptor antagonists.

Provided is a bifunctional compound, or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein the bifunctional compound is represented by Formula (I) : ABM-L-CLM (I); wherein: ABM is an androgen receptor binding moiety; -L-is a linking moiety; and CLM is a cereblon E3 ubiquitin ligase binding moiety represented by Formula (II) -1: wherein one end of the -L-is covalently joined to Q3, Q4, Q5 or Q6; and the other end of the -L-is covalently joined to the ABM. Also provided are a pharmaceutical composition comprising the bifunctional compound and a method for treating an androgen receptor related disease or disorder by administering the bifunctional compound.

The present invention discloses an andrographolide compound as an estrogen receptor agonist, including the above-mentioned andrographolide compound and the application of andrographolide compound, wherein the andrographolide compound is deoxyandrographolide or 14-deoxy-11,12-didehydroandrographolide. In combination with the contents of the embodiment part of the specification, this andrographolide compound has a pro-proliferation effect on breast cancer cells MCF-7 (estrogen receptor positive cells), and in addition, in combination with Figures 1 and 2, it is verified by a molecular docking calculation method that andrographolide compounds have a strong affinity with estrogen receptors, thereby indicating that andrographolide compounds can be used as estrogen receptor agonists.

The invention relates to an estrogen receptor alpha and fibroblast activating protein dual-targeting near-infrared fluorescent probe as well as a preparation method and medical application thereof. Specifically, the probe can be used as a fluorescence probe for developing cells co-expressing the estrogen receptor alpha and the fibroblast activating protein, and can also be used as a near-infrared fluorescence imaging probe for diagnosing benign / malignant lesions such as nodules / tumors co-expressing the estrogen receptor alpha and the fibroblast activating protein. The fluorescent probe can also be applied to research on related biological events in cells for co-expressing the estrogen receptor alpha and the fibroblast activating protein, and particularly can be applied to fluorescent navigation in tumor resection operations for co-expressing the estrogen receptor alpha and the fibroblast activating protein; particularly, the composition can be applied to the synergistic treatment of an anti-estrogen therapy and a photodynamic therapy on a diseased region which co-expresses the estrogen receptor alpha and the fibroblast activating protein.

A compound represented by formula (I) or a stereoisomer, tautomer or pharmaceutical salt thereof, and its use in the preparation of a medicament to prevent and / or treat estrogen receptor (ER) related diseases or disorders.

Methods and compositions for treatment of prostate cancers, such as androgen receptor (AR) deficient and androgen receptor (AR) low cancers, are disclosed. The methods include administration of an agent that inhibits activity of eIF4F or an agent that disrupts the eIF4F translation-initiation complex (composed of eIF4E, eIF4A, and eIF4G).

Methods and compositions are provided for reversibly localizing proteins to the exterior part of the cell surface. Essentially, the protein must comprise, in addition to a transmembrane domain, also a hormone receptor like the estrogen receptor alpha or the progesterone receptor. Compositions provided herein can include nucleic acids that encode polypeptides of interest and the ligand binding domain (LBD) of a nuclear hormone receptor. Medical applications are provided, including controlling the toxicity of CAR T cells.

Described herein are radiotherapeutic agents that target tumor cells that express the follicle-stimulating hormone receptor (FSHR), and their use in the treatment and / or diagnosis of cancer.

The present invention provides radiolabeled 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-α]indol-9-yl]pyridin-2(1H)-one derivatives of general formula (I) or salts thereof, as well as precursors of the radioligands of general formulae (II) and (III), processes for their preparation, and intermediates of the processes. The radiolabeled compounds enable visualization and quantification of melanin-concentrating hormone receptor 1 (MCHR1) in various target tissues, including monitoring MCHR1 in such target tissues. The compounds exhibit high binding affinity for MCHR1 and are able to cross the blood-brain barrier, thus facilitating diagnosis of various disease states in human clinical studies.