252 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.

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 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.

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 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.

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).

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.

Nanoparticles and formulations for treating prostate cancer in a subject are disclosed. The nanoparticles contain a cage, such as a zeolitic imidazolate framework (“ZIF”), a surface modifying agent, a targeting ligand, and an active agent. The surface modifying ligand is attached to the outer surface of the cage and the targeting ligand is exposed to the surrounding environment. The active agent is encapsulated in the cage. The targeting ligand binds to a reproductive hormone or a receptor of a reproductive hormone. The active agents can be a ribosome inactivating protein, an apoptosis inducer, a hormone, a receptor ligand, or a nucleic acid, or a chemotherapy drug or a combination thereof, that kill and / or reduce or prevent growth or proliferation of gonadotroph cells and / or tumor cells, regulate FSH and / or LH secretion, and / or interfere with androgen production. Uses for formulations incorporating the nanoparticles for treating cancer in a subject are also disclosed.

The present invention relates to methods and compositions for the treatment of BAF-related disorders such as cancer.

The present application relates to the technical field of biological medicine, in particular to a curcumin analogue, a synthetic method and application thereof. The present application takes curcumin as a lead compound, introduces cyclopropylmethyl, n-butyl and isobutyl in acetylacetone, introduces 4-acetylamino, 3,4-dimethoxy, 2-fluoro and 3-trifluoromethyl on a benzene ring, and designs and synthesizes a series of curcumin analogues. In vitro cytotoxicity experiments show that the killing effect of the newly synthesized curcumin analogue on prostate cancer cells is stronger than that of dimethyl curcumin, and the androgen receptor inhibition effect is also stronger than that of dimethyl curcumin.

The present invention discloses an adjuvant treatment of node-positive, carly stage, hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2—) breast cancer comprising administering an effective amount of an endocrine therapy in combination with an effective amount of abemaciclib or a pharmaceutically acceptable salt thereof.

The invention provides a novel estrogen receptor protein degradation targeting chimera compound and application of the novel estrogen receptor protein degradation targeting chimera compound in medicine. The compound provided by the invention can be used as an estrogen receptor degradation agent for treating estrogen dependent diseases.

The present invention is directed to a therapeutic agent for use in the treatment of a disease associated with gain-of-function of androgen receptor (AR) and / or with overexpression of an AR coactivator, such as Kennedy disease or cancer. The therapeutic agent of the invention comprises at least one inhibitor of an androgen receptor (AR) coactivator, selected from protein arginine methyltransferase 6 (PRMT6) inhibitor, lysine specific demethylase 1 (LSD1) inhibitor, or combinations thereof.

The invention discloses an anti-prostatic cancer sulfonamide compound and application thereof, and belongs to the technical field of medicines. The structural formula of the sulfonamide compound is shown as a general formula (I), and the structure of the sulfonamide compound is different from that of traditional steroidal and non-steroidal androgen receptor antagonists. The compound has remarkable androgen receptor transcription inhibition activity, can be effectively combined with an androgen receptor ligand binding pocket in a competitive manner, blocks homologous dimerization of an androgen receptor, inhibits nuclear translocation of the androgen receptor, inhibits expression of downstream genes in an androgen receptor signal channel, and can be used for inhibiting the transcription of the androgen receptor. Further, the effects of antagonizing the transcriptional activity of an androgen receptor and inhibiting tumor cell proliferation are achieved; the compound can effectively inhibit the transcriptional activity of a mutant androgen receptor related to the clinical drug resistance of enzalutamide and the proliferation activity of drug-resistant cells, and shows better safety. The invention provides a new choice for prostatic cancer treatment and drug development.