63 results about "Estrogen receptor" patented technology

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.

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

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.

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.

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.

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).

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.

This invention discloses an S-estrol composition for delaying ovarian aging and its uses, relating to the fields of biomedicine and health products. The S-estrol composition for delaying ovarian aging comprises, by weight, the following components: 1-5 parts S-estrol, 2-8 parts soy isoflavones, 3-10 parts coenzyme Q10, 2-6 parts vitamin E, 4-12 parts vitamin C, 0.01-0.05 parts folic acid, 0.1-0.3 parts zinc source, 0.5-1.5 parts anti-aging protective agent, 50-80 parts carrier, and 10-15 parts purified water. This invention uses high-purity S-estrol as the core, combined with soy isoflavones, coenzyme Q10 and a variety of antioxidant nutrients in a scientific formulation to form a synergistic system for estrogen receptor signal regulation and antioxidant defense. By constructing a complex antioxidant network and introducing novel anti-aging protectants for synergistic effect, the activity of antioxidant enzymes tends to increase and the level of lipid peroxidation tends to decrease, thereby improving the oxidative stress state in ovarian cells as a whole.

Provided are novel crystalline forms of Elacestrant (Referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline form, and uses of the crystalline form for preparing estrogen receptor depressant drugs and drugs for treating breast cancer with ER+, HER2−, ESR1 mutations.

Disclosed are a pyrrolidine compound as represented by formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and the use of the pharmaceutical composition as a selective estrogen receptor degrader (SERD) in the prevention or treatment of estrogen receptor-related diseases.

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).

Compounds of formula (I):wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH) 2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group;and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

The present invention relates to the technical field of molecular imaging probes, and more specifically to a fluorescent probe targeting the estrogen receptor, a preparation method, and applications thereof. The fluorescent probe targeting the estrogen receptor is composed of a fluorescein ester, an estrogen receptor recognition group, raloxifene, and an alkane chain. The preparation method comprises the following steps: Step S1, hydrolyzing or hydrogenolyzing the carbamate of raw material I to synthesize an amino intermediate II; Step S2, condensing the amino intermediate II with FITC to obtain a fluorescent probe targeting the estrogen receptor III. The fluorescent probe targeting the estrogen receptor in the present invention can avoid the effects of short emission wavelength and low signal-to-noise ratio during probe application, and can be better used to promote the clinical application of the fluorescent probe targeting the estrogen receptor.

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

The application discloses a traditional Chinese medicine composition, a medicine preparation and application thereof, and belongs to the technical field of traditional Chinese medicine compositions. The traditional Chinese medicine composition comprises herba rhizomatosi and herba rhizomatosi, and the mass ratio of the herba rhizomatosi and the herba rhizomatosi is 1:1. The traditional Chinese medicine composition, the medicine preparation and the application thereof are based on the compatibility of the kidney-nourishing and heart-nourishing theory of traditional Chinese medicine, utilize the herba rhizomatosi and the herba rhizomatosi to form a kidney-yang tonifying traditional Chinese medicine pair, and are consistent with the core pathogenesis of MIRI. The corresponding traditional Chinese medicine composition of the traditional Chinese medicine pair can inhibit cell apoptosis, reduce the level of inflammatory factors in cells, relieve calcium ion overload and improve cell survival rate, so as to improve the hypoxia / reoxygenation-induced H9C2 myocardial cell damage state in multiple dimensions. The traditional Chinese medicine composition can activate estrogen receptors to inhibit the expression of related proteins in the endoplasmic reticulum stress signal pathway, and simultaneously regulate the expression of apoptosis-related proteins, thereby laying a foundation for the application of phytoestrogen therapy in the field of cardiovascular diseases and having significant clinical transformation value and market potential.

Provided herein are methods of treating somatostatin receptor-positive, estrogen receptor-positive, human epidermal growth factor receptor 2-negative breast cancer using 225Ac-DOTA-TATE or a pharmaceutically acceptable salt thereof.

Disclosed herein is a compound, or a pharmaceutically acceptable salt thereof, in particular hydrochloride salt thereof, characterized in that said compound is selected from the following compounds: -4-(4-((1-(3-fluoropropyl)azetidin-3-yl)oxy)benzoyl)-3-(4-(trifluoromethyl)phenyl)quinoline-7-carboxylic acid (1), -3-(2-fluoro-4-(trifluoromethyl)phenyl)-4-(4-(2-(3-(fluoromethyl)azetidin-1-yl)ethoxy)benzoyl)quinoline-7-carboxylic acid (2), and -(R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid (3). 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.

A combined drug of an estrogen receptor degrader and an AKT inhibitor and use thereof. The present invention pertains to the field of pharmaceuticals. The combined drug comprises an estrogen receptor degrader and an AKT inhibitor of the same specification or different specifications that are administered simultaneously or separately and a pharmaceutically acceptable carrier, can degrade estrogen receptors, inhibit cancer cell growth, exert a synergistic inhibitory effect, and significantly improve the effect of treating estrogen receptor-related diseases, and has good application prospects.