375 results about "Estrogen" 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.

Embodiments of the present invention provide a pharmaceutical intervention in the neonatal pig that inhibits and delays development and activation of the HPG axis, growth of the boar testis and inhibits testicular production of testosterone and androstenone, which prevents the development of aggressive behavior in the maturing boars and the presence of boar taint in the meat. The invention comprises treatment with a combination of an androgen and an estrogen in the newborn male piglet using extended drug delivery methods, with a defined duration of no more than 12 weeks, for the purpose of inhibiting the production of testosterone and androstenone and the accumulation of the boar taint-inducing molecules androstenone and skatole in the fat.

The invention discloses application of PGRN in preparation of products for preventing and treating neuropsychiatric disorder related diseases caused by estrogen deficiency. The invention provides an application of a PGRN protein or a coding gene thereof or a virus expressing the coding gene thereof in preparation of a product with any one of the following functions: 1) preventing or treating or saving neuropsychiatric disorder related diseases caused by estrogen deficiency; 2) preventing or treating perimenopausal anxiety and / or depression symptoms; and 3) relieving anxiety-like behaviors and / or depression-like behaviors caused by estrogen deficiency. The application proves that the PGRN can play a role in protecting neuron damage caused by estrogen deficiency by rescuing CTSD enzyme activity and an autophagy pathway, and prompts that related medicines and measures influencing secretion and content of the PGRN can treat perimenopausal anxiety and depressive symptoms; and a new target and a new idea are provided for clinical treatment and drug development of anxiety and depression symptoms of climacteric women.

The invention relates to the technical field of medicine, in particular to application of beta-hydroxybutyric acid in preparation of medicine for preventing and / or treating osteoporosis, the osteoporosis comprises postmenopausal osteoporosis and diabetic osteoporosis due to estrogen deficiency, the administration concentration of the beta-hydroxybutyric acid is 150mM, and the administration concentration of the beta-hydroxybutyric acid is 10mM. According to the application of the beta-hydroxybutyric acid in preparing the medicine for inhibiting osteoclast differentiation or osteoclast formation, the beta-hydroxybutyric acid inhibits osteoclast precursor cells from being differentiated into osteoclasts, and the administration concentration of the beta-hydroxybutyric acid is 10 mM; the invention proves that the beta-hydroxybutyric acid improves bone microstructures of OVX mice and db / db mice, inhibits osteoclast differentiation and reduces bone resorption, and provides a new target for prevention and treatment of osteoporosis.

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 provides a method for breeding all-male hybrid pelteobagrus fulvidraco through hybridization of double super-male populations, which comprises the following steps: S1, respectively constructing super-male maintenance lines of pelteobagrus fulvidraco and pelteobagrus vachelli by utilizing a sex reversal technology and a sex molecular marker; s2, carrying out artificial propagation on the maintenance line, and propagating the super male fish in batches; s3, partially replacing estrogen with an androgen antagonist for the propagated supermale fish, and synergistically inducing the supermale fish to obtain superfemale fish; s4, performing specific nutrient enrichment cultivation on the super female fish and the super male parent fish; and S5, carrying out reciprocal cross artificial propagation on the super-female fish and the super-male fish between the two super-male groups to obtain a heterozygous super-male group, namely commercial fry of the all-male hybrid pelteobagrus fulvidraco. According to the technical scheme, super-female fishes can be efficiently induced in batches, high-density breeding of parent fishes is achieved, and the effect and efficiency of artificial breeding are remarkably improved; the bred hybrid all-realgar catfish is high in individual uniformity, the growth speed is increased by 20%, and the male rate reaches 100%.

The invention discloses a bifidobacterium animalis subsp. Lactis BA-C53 and an application of the bifidobacterium animalis subsp. Lactis BA-C53 in products for improving bone health. The bifidobacterium animalis subsp. Lactis BA-C53 is classified and named as bifidobacterium animalis subsp. Lactis Bifidobacterium animalis subsp. Lactis BA-C53, the preservation number is CCTCC NO: M 2024460, the preservation unit is China Center for Type Culture Collection, and the preservation time is March 11, 2024. The bifidobacterium animalis subsp. Lactis BA-C53 can effectively improve the steady state of intestinal flora of a mouse with osteoporosis induced by estrogen deficiency, so that the relative abundance of phylum firmicalis and phylum actinomycetes is increased, the relative abundance of phylum bacteroides is reduced, and then short-chain fatty acid is generated to activate intestinal immunity and maintain the integrity of an intestinal barrier, so that the osteoporosis caused by estrogen deficiency is inhibited. Meanwhile, osteoclast differentiation can be inhibited by regulating NFATC1, RANKL and OPG pathways, then osteoporosis is relieved, and the compound can be widely applied to preparation of food and drugs.

The invention provides a multi-walled carbon nanotube paste electrode based on gold nanoparticles and C60 modification as well as a preparation method and application thereof, and belongs to the technical field of electrochemical sensors. The preparation method comprises the following steps: firstly, modifying fullerene C60 on the surface of a carbon nanotube paste electrode (MWCNTPE) to form C60 / MWCNTPE, then loading gold nanoparticles on the surface of the C60 / MWCNTPE, and finally constructing the AuNPs / C60 / MWCNTPE composite electrode. The prepared composite electrode is used for environmental estrogen detection, especially for simultaneous detection of hydroquinone, catechol and bisphenol A. The method has the advantages of high sensitivity and low detection limit, can solve the problem that hydroquinone and catechol isomeride are difficult to separate through the detection capability, has the advantages of simplicity and convenience in operation and low cost, and has good practical applicability, stability and reproducibility.

Disclosed are devices and methods for providing local administration of a sex hormone composition in a mammalian body to promote bone remodeling. The device includes an implantable structure configured for placement at a target intraosseous and / or periosteal site in the mammalian body and an effective amount of a sex hormone composition associated with the implantable structure. The sex hormone composition comprises both an estrogen and an androgen.

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.

The invention relates to the technical field of medical informatics, in particular to an intelligent endometrial receptivity evaluation system based on multi-modal fusion. The system comprises a memory and a processor, and the processor executes a computer program stored in the memory so as to realize the following steps: acquiring endometrial thickness, estrogen content, luteal hormone content and pulse index of a reference person and a person to be evaluated; determining the intimal change stability according to the endometrial thickness increase characteristics of the reference person; according to the fluctuation condition of the estrogen content of the reference personnel, the decrease condition of the estrogen content detected in two adjacent times and the change condition of the luteal hormone content, determining the category of the to-be-evaluated personnel; and determining the creep over-frequency expression degree by combining the decreasing condition of the pulse index of the to-be-evaluated person and the uterine contraction condition so as to obtain a comprehensive index. According to the method, the data of different dimensions of the endometrium of the to-be-evaluated person is synthesized to obtain the comprehensive index, and reference data is provided for subsequent evaluation of a doctor.

The invention relates to a breast cancer dynamic risk assessment method based on an adaptive model, and aims to improve the accuracy of early screening and risk prediction of breast cancer. The method comprises the following steps that firstly, clinical data of the unresected side mammary gland of an estrogen receptor positive breast cancer patient are obtained, and the data comprise the estrogen receptor state, the hormone treatment duration and mammary gland density classification; selecting an imaging detection mode according to the mammary gland density grading and the estrogen receptor state, and obtaining a calcification focus image of the target mammary gland; performing multi-parameter quantitative analysis on the image, and extracting parameters such as hydroxyapatite crystal proportion, calcification edge sharpness index and the like; and carrying out risk value calculation by using the trained adaptive risk assessment model, comparing the risk value with a preset risk grading threshold, and finally generating an assessment report based on a risk grade. According to the method, accurate dynamic risk assessment can be provided for the breast cancer patient, and personalized health management and intervention decision are supported.

Disclosed herein are compounds of Formula (I) or pharmaceutically acceptable salts thereof: wherein R1 and R2 independently represent a hydrogen atom or a deuterium atom; r3 represents a hydrogen atom or a-COOH group; r3'represents a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom, a cyano group, or a-COOH group; r3 ''represents a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom, or a cyano group; with the proviso that one but not both of R3 and R3'represents a-COOH group, and R3 and R3 'do not represent a hydrogen atom at the same time; r4 represents a hydrogen atom or a fluorine atom; r5 and R5'independently represent a hydrogen atom or a fluorine atom; y represents-CH2-,-CH =,-CR9 =,-O-or-NH-wherein R9 represents a fluorine atom or a (C1-C3) alkyl group; represents a single bond or a double bond; p is 0 or 1; x represents-CH =,-N = or-CR ''= wherein R'' represents a (C1-C3) alkyl or halogen atom such as fluorine or chlorine atom, cyano, or a (C1-C3) fluoroalkyl group such as trifluoromethyl; r7 independently represents a (C1-C3) alkyl group such as a methyl group, a halogen atom such as a fluorine atom, a cyano group, or a (C1-C3) fluoroalkyl group such as a trifluoromethyl group; n is 0, 1 or 2; and R6 represents an optionally substituted (C1-C9) alkyl group, and R8 in particular represents a (C1-C6) alkyl group. Further disclosed are processes for their preparation, pharmaceutical compositions comprising them and the compounds of formula (I) for use as inhibitors and degradation agents of estrogen receptors, in particular in the treatment of ovulation dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hyperplasia or inflammation. # imgabs0 #

Described herein are pinoxifene compositions comprising novel compounds and methods of use thereof. Methods of synthesizing the compositions are described herein. The odoxifene compositions described herein may exhibit aromatase inhibitory activity or estrogen receptor activity. The odoxifene compositions described herein can be used to treat a condition, such as cancer, in a subject.

The invention relates to the field of biological medicine, and discloses application of ergothioneine in preparation of a medicine for preventing and / or treating osteoporosis. The invention discloses a new mechanism of the ergothioneine for improving the osteoporosis by regulating and controlling the NF-kB / NFATc1 signal channel and reducing oxidative stress and inflammatory response for the first time, and provides a brand new thought for developing safe and effective anti-osteoporosis medicines. The discovery that the ergothioneine improves bone mass loss related to estrogen decline provides a new solution for lack of osteoporosis treatment means at present, and opens up a new way for application of natural products in bone metabolic diseases.

The invention belongs to the technical field of medical supplies, and particularly relates to a composition for improving perimenopausal symptoms. The feed consists of the following components in parts by weight: 400-700 parts of protein substances, 30-50 parts of fat substances, 120-170 parts of carbohydrate substances, 40-90 parts of dietary fiber substances, 30-80 parts of medicinal and edible substances, 2-6 parts of compound trace minerals, 50-95 parts of compound macro minerals, 3-5 parts of compound vitamins and 5-10 parts of blueberry powder. Wherein the protein substance is composed of whey protein, soybean protein and collagen peptide in a mass ratio of (7-12): (6.1-8.5): 1. According to the composition disclosed by the invention, the perimenopausal symptoms such as hectic fever, insomnia, osteoporosis, decrease of estrogen level, uterine atrophy and the like can be remarkably improved by accurately controlling the proportion of soybean protein and collagen peptide in protein.

The invention provides a preparation method and application of an engineered exosome derived from placenta mesenchymal stem cells, and belongs to the field of biological medicine. According to the invention, the placenta mesenchymal stem cells transfected with the miRNA virus vector are constructed, the engineered exosome is prepared in a culture system under an anoxic condition and stimulated by estrogen, and the invention also provides application of the placenta mesenchymal stem cells and the exosome in preparation of medicines for treating ovarian insufficiency, female climacteric syndrome and the like. The miRNA transfected placenta mesenchymal stem cells and exosomes provided by the invention have good effects in the aspects of treating ovarian insufficiency, female climacteric syndrome and the like.

The invention relates to a pharmaceutical composition for treating uterine adhesion and application thereof. The kidney reinforcing and miscarriage preventing pills are used for improving endometrial blood perfusion and increasing the endometrial thickness, the kidney reinforcing and miscarriage preventing pills, aspirin and estrogen play a synergistic treatment role, the postoperative re-adhesion rate is remarkably reduced through combined treatment, and the fertility prognosis of a patient is improved; and the molecular mechanism of a TGF-beta1 pathway and EMT is deeply researched, and by inhibiting excessive activation of the TGF-beta1 signaling pathway, reducing endometrial fibrosis, regulating an epithelial-mesenchymal transition (EMT) process and promoting regeneration of endometrial epithelial cells, endometrial repair is further promoted, multi-target treatment is realized, and the treatment effect is remarkable. A brand-new and efficient treatment scheme is provided for treatment of intrauterine adhesion, an individualized treatment scheme can be formulated according to the specific conditions of patients, the treatment accuracy and effectiveness are improved, and important clinical significance and application value are achieved.

The present invention relates to a compound of the formula (i) wherein Ar represents a phenyl or a 6-membered heteroaryl group, R1 and R2 represent independently a hydrogen atom or a deuterium atom, R3 represents (1) a —COR4 group, (2) a —BOR5OR6 group, (3) a —X—Z group, (4) a (C1-C6)alkyl group or a (C1-C6)alkenyl group, (5) a —X—S(O)n(R7)p(R8)q group, (6) a halogen atom, a —NH2 group or a —CN group, (7) a —O—R11 group, (8) a —NH—COR9 group, (9) a —C(═NH)NHOH group, (10) a —NH—C(NH)—R9′ group, or (11) a —NHCOCOOR12 group or a —NHCOCONR12′R12″ group, X represents a bond, a —NH— group, a —CONH— group or a —CO— group, Z represents a 4 or 5-membered cycloalkyl, a 4 or 5-membered heterocylcloalkyl group, a 4 or 5-membered heteroaryl group or a phenyl group or a pharmaceutically acceptable salt thereof. The present invention further relates to a medicament comprising said compound of formula (I) and to said compound of formula (I) for use as an inhibitor and degrader of estrogen receptors.

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%.

The invention provides a novel application of a raspberry extract. It is found through tests that any one of isoquercitrin, ellagic acid, vanillic acid, oleanolic acid, kaempferol-3-O-rutinoside, kaempferol-3-O-sophoroside, tiliroside, tormentic acid and raspberry extract can remarkably improve the activity of the human ovarian granular cells or remarkably improve the oxidative stress level, and the activity of the human ovarian granular cells can be remarkably improved. According to the present invention, the ovarian function can be effectively protected by the eight components, the ovarian function can be effectively protected by the eight components, or the mitochondrial membrane potential level can be significantly regulated and controlled, or the estrogen level in the microenvironment can be effectively maintained, such that the ovarian function can be effectively protected by the eight components, and the raspberry extract containing the eight components. The invention provides a new choice for ovarian function protection products, and also provides a new application for the substances.

The invention discloses a medicine for treating or relieving heart failure, the medicine comprises an estrogen compound, and the estrogen compound is preferably mestraanol. According to the invention, verapamil hydrochloride is used for inducing and establishing the chronic heart failure model of zebrafish, and direct exposure of the estrogen compound MESTRANOL is carried out on a zebrafish embryo with heart failure, so that the heart failure of zebrafish is relieved. The phenotype of zebrafish is observed and analyzed, and physiological data, gene expression quantity related to heart failure and key events causing heart failure in rat H9c2 myocardial cells, such as ROS level and cell apoptosis, are counted; the estrogen compound MESTRANOL is innovatively found and proved to be capable of relieving heart rate decline, venous sinus extravasated blood, pericardial cavity enlargement and heart cyclization abnormity caused by heart failure, and has more excellent drug effects compared with positive drugs E2 and G1, so that a foundation is laid for developing new drugs for treating heart failure.

This invention discloses a yam oxylipoic acid compound with aromatase inhibitory activity, its application, and analytical identification methods, belonging to the field of medicinal chemistry. The yam oxylipoic acid compound is (Z)-9-ethoxy-6,10-dihydroxyoctadec-7-enoic acid, a novel compound. This compound can significantly inhibit aromatase activity and possesses the ability to inhibit excessive estrogen production, thus showing promising application prospects and value in diseases related to estrogen imbalance regulation.

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.

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 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.

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 application provides an application of Lipofermata in preparation of a product for preventing and treating osteoporosis. The pharmacological experiment of the application shows that Lipofermata can significantly prevent and treat and improve the reduction of bone mass caused by estrogen reduction, and shows that Lipofermata has the effect of preventing and treating osteoporosis, and therefore can be used for preventing and treating osteoporosis. The application not only provides a new therapeutic use of Lipofermata, but also provides a new drug for preventing and treating osteoporosis.