108 results about "Estrogen 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.

Described herein are compounds of Formula I and pharmaceutically acceptable salts, solvates, or stereoisomers thereof, and their uses (e.g., as estrogen receptor degrading agents).

The invention relates to the field of antibacterial gels, in particular to an ovary maintenance antibacterial gel as well as a preparation method and application thereof. The invention relates to an ovary maintenance antibacterial gel, which comprises a component A, a component B and a component C, the component A is prepared from 64 to 84 parts of deionized water, 0.05 to 0.15 part of preservative synergist, 0.6 to 0.9 part of carbomer U-30, 0.06 to 0.12 part of ultra-high molecular weight hyaluronic acid, 3 to 7 parts of hydrogel, 3 to 6 parts of glycerol and 3 to 6 parts of propylene glycol; the component B is prepared from 3 to 7 parts of selective estrogen receptor regulator and 0.5 to 2.5 parts of flos lonicerae extract; the component C is prepared from the following components in parts by weight: 0.1 to 0.3 part of silver ion solution, 0.3 to 0.6 part of preservative, 0.05 to 0.15 part of tween-20 and 0.05 to 0.25 part of triethanolamine. The gel obtained in the invention is applied to ovaries, can play a role in bacteriostasis, and can also effectively improve premature ovarian failure.

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%.

Disclosed herein are methods for treating cancer comprising administering to a subject a daily dose of Compound A or a pharmaceutically acceptable salt thereof in combination with an Akt inhibitor.

The present disclosure relates to novel chroman derivatives having estrogen receptor degrading activity and uses thereof. In particular, the present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in the prevention and treatment of cancer and related diseases and conditions.

Novel mutant ESR1 molecules and uses are disclosed.

The invention relates to the technical field of medicines, in particular to application of osthole in preparation of a medicine for protecting cognitive function impairment caused by down-regulation of an estrogen receptor. The OST has an improvement effect on the learning and memory ability and pathological damage of 6-month-old female peripheral ERs down-regulated mice and ER alpha- / -mouse models. The mechanism of the OST for improving learning and memory may be related to improvement of neuroplasticity, inhibition of nerve apoptosis and enhancement of neurotransmitter by regulating and controlling an estrogen-cholinergic system by the OST. The OST has a better intervention effect on a 6-month-old female ER alpha- / -mouse model, and possibly is a kidney-tonifying medicine which acts on a related target spot of a peripheral target organ so as to participate in regulation of a cognitive function of a central system.

Novel selective estrogen receptor degraders (SERDs) according to the following formula and pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof: wherein R is selected from the group consisting of

The present invention relates to the technical field of medicine. Provided are an estrogen receptor modulator and a use thereof, particularly a compound as represented by general formula (i) or an isomer or pharmaceutically acceptable salt thereof and a use thereof, particularly a use thereof as an estrogen receptor degrading agent, a use thereof in the preparation of a medicament for treating and / or preventing an estrogen receptor-mediated or dependent disease or condition, and a use thereof in the preparation of a medicament for treating and / or preventing a disease or condition by degrading a target protein.

Compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and other related diseases and conditions are disclosed. In an embodiment, the disclosed compounds have the following Formula (I) and pharmaceutically acceptable salts thereof:

Disclosed herein are methods of treating breast cancer in a subject. Preferably, these methods include presenting a plurality of mammograms from one or more breasts of a subject over a time period, performing an algorithm-based analysis of the mammograms, the algorithm predicting a risk of interval or occult mammographic cancers, and administering an estrogen receptor modulating pharmaceutical to the subject based on a breast cancer risk score generated from the algorithm-based analysis.

Disclosed herein are compounds of the formula (I), or pharmaceutically acceptable salts thereof wherein R1 and R2 represent a hydrogen atom or a deuterium atom; R3 represents a hydrogen atom, a —COOH group or a —OH group; R3′ and R3″ represent a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom, or a cyano group; R4 and R5 represent a hydrogen atom, a halogen atom, a —IMH2 group, a (C1-C3)alkyl group, a (C1-C3)alkoxy group, or a —OH group; or R4 and R5 together form an oxo group or R4 and R5 together form a ═NOCH3 group or a (C3-C5)cycloalkyl group; R7 represents a hydrogen atom, a methyl group, a —OH group or a fluorine atom; R6 represents a phenyl group, a fused phenyl group, a bicyclic group comprising 5 to 12 carbon atoms, a heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, a cycloalkyl group comprising 3 to 7 carbon atoms, a (C3-C6) cycloalkyl (C1-C3) alkyl group, a 3 to 8 membered-heterocycloalkyl group, a (C1-C6)alkyl group or a phenyl (C1-C2) alkyl group; X represents —CH2—, —O— or —S—; Y represents —CH═, —N═ or —CR″═; R8 represents a (C1-C3) alkyl group, a halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; R9 represents a hydrogen atom or a fluorine atom; RIO and RIO′ represent a hydrogen atom or a fluorine atom; R11 represents a hydrogen atom a (C1-C3)alkyl group or a cyclopropyl group; n is 0, 1 or 2, and m is 0 or 1. Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.

The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

In one aspect, the disclosure relates to relates to substituted benzothiophene analogs which are useful as selective degraders of estrogen receptor, methods of making same, pharmaceutical compositions comprising same, and methods of treating one or more clinical conditions associated with estrogen receptor, such as a cancer, including breast cancer, or osteoporosis. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Disclosed herein is a method of treating breast cancer by administering 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile, alone or in combination with a second agent such as aromatase inhibitor or a selective estrogen receptor degrader. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile and second agent such as aromatase inhibitor or a selective estrogen receptor degrader.

To provide a selective estrogen receptor decomposer (SERD) as well as an intermediate thereof and a salt thereof including pharmaceutically acceptable salt, and a method for making a pharmaceutical composition thereof.SOLUTION: Disclosed is a method for producing a compound of formula A [in the formula, either R1 or R2 is independently Cl, F, -CF3 or -CH3 and the other is H, R7 is H or PG, and PG is an alcohol protecting group.] having an enantiomeric excess percentage of at least about 92%.SELECTED DRAWING: None

Tetrahydropyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulating activity or function are described, having the structure of Formula I (see Formula), and pharmaceutically acceptable stereoisomers, tautomers, or salts thereof, with the substituents and structural features described herein. Pharmaceutical compositions and medicinal products comprising the compounds of Formula I are also described, as well as methods of using such estrogen receptor modulators, alone or in combination with other therapeutic agents, to treat diseases or pathological conditions that are mediated by or dependent on estrogen receptors.

Provided is a method of regulating the expression of a target gene in a cell. Aspects of the method include contacting 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 protein; (ii) the second moiety exhibits specific binding to a second endogenous protein different from the first endogenous protein; (iii) upon contact with the cell, the first endogenous protein and the second endogenous protein spatially complex with each other via the compound to effect a gain of function in the cell, whereby a process that is not normally regulated by either the first endogenous protein or the second endogenous protein is activated. Here, the first moiety targets BCL-6; the second moiety targets any one of an estrogen receptor, an androgen receptor, BRD4 or a cyclin-dependent kinase. TIFF2025517099000355.tif106159

To provide methods and compounds for use in treating and / or preventing breast cancer, including locally advanced or metastatic, ER+, HER2- breast cancer, in a subject in need of treatment.SOLUTION: Treating and / or preventing methods are provided which comprise administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof.SELECTED DRAWING: Figure 8

To provide new SERDs to treat cancers as well as mutations due to emerging resistance.SOLUTION: The present invention provides a novel selective estrogen receptor degrader (SERD) of the following formula (where either R1 or R2 is independently selected from Cl, F, -CF3, or -CH3, and the other is hydrogen), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and methods for use thereof.SELECTED DRAWING: None

This document provides pharmaceutical combinations, compositions, and methods using compounds with estrogen receptor (ER) degradation activity and cyclin-dependent kinase (CDK) inhibitors, wherein the compounds are such as compounds of formula (I) or their tautomers, stereoisomers, or mixtures of stereoisomers, or pharmaceutically acceptable salts or hydrates, wherein R1, Y, R 22 R 33 R2, p, X3, X4 and Z are defined in this paper.

The present specification relates to a method for treating a patient suffering from hormone receptor positive (HR +), human epidermal growth factor receptor 2 negative (HER2-), breast cancer, comprising administering to the patient in need thereof an oral selective estrogen receptor degrading agent (SERD) in combination with an AKT inhibitor or an mTOR inhibitor and / or a cyclin dependent kinase 4 / 6 inhibitor (CDK4 / 6i).

Provided is a preparation method for a selective estrogen receptor degrader. Specifically provided is a preparation method for a compound as represented by formula (I) and a pharmaceutically acceptable salt thereof. The method reduces the reaction steps, improves the reaction yield, and is suitable for industrial production.

Described herein are compounds of Formula (I) and pharmaceutically acceptable salts, solvates, or stereoisomers thereof, as well as their uses (e.g., as estrogen receptor degraders).

Provided herein are methods related to measuring clonal fraction of one or more estrogen receptor 1 (ESRI) mutations in a liquid biopsy sample from an individual having cancer, as well as uses, systems, and computer readable storage media related thereto. In some embodiments, the methods comprise measuring a variant allele frequency of one or more ESRI mutations in a liquid biopsy sample obtained from the individual, measuring a tumor fraction of tumor nucleic acid molecules in the liquid biopsy sample, and calculating a ratio of the variant allele frequency of the one or more ESRI mutations to the tumor fraction of tumor nucleic acid molecules in the liquid biopsy sample.

The invention discloses application of alpha spiral polypeptide combined with tamoxifen to preparation of an anti-breast cancer pharmaceutical composition, and belongs to the technical field of biological medicine. A large number of experimental studies show that the alpha spiral polypeptide 6w and tamoxifen are combined for medication, the killing ability of the ERalpha high-expression breast cancer cell line can be obviously improved, the phenomena of apoptosis, cell cycle arrest in the G0 / G1 phase and the like of the ERalpha high-expression breast cancer cell line can be obviously improved, an estrogen receptor signal channel can be inhibited, and the ERalpha high-expression breast cancer cell line can be used for treating the ERalpha high-expression breast cancer cell line. The expression level of related genes such as pS2 at the downstream of a signal is obviously reduced, and the proliferation of tamoxifen drug-resistant cells can be better inhibited.