131 results about "Estrogen" patented technology

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 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.

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 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.

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 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.

This invention belongs to the field of pharmaceutical technology, specifically relating to ligand modulators targeting the estrogen-related receptor ERRγ and their uses. In a first aspect, this invention provides the use of small molecule compounds in the preparation of ligand modulators targeting the estrogen-related receptor ERRγ, said small molecule compounds being as shown in formula (I). In a second aspect, this invention also provides the use of the small molecule compounds described in the first aspect in the preparation of drugs for the prevention or treatment of ERRγ-related diseases. This invention provides a series of small molecule compounds targeting the estrogen-related receptor ERRγ as its ligand modulators, solving the problem of low drugability of ERRγ and providing more options for the development of related drugs, thus showing good prospects for development and utilization.

The application discloses a human vagina micro-ecological in-vitro model and a construction method and application thereof, and relates to the technical field of medicines.The application discloses a human vagina micro-ecological in-vitro model and a construction method and application thereof.Firstly, a mixed cell group of the vaginal epithelium containing a complete cell lineage and capable of long-term subculture is successfully established, a technical bottleneck that primary vaginal epithelial cells are difficult to expand is solved, and ideal seed cells are provided for model construction.Secondly, a highly-bionic vaginal mucosa model having a tight connection structure, rich layers and an orderly arrangement is constructed, and the physiological barrier and immune regulation functions of the vaginal mucosa are truly simulated.Finally, by introducing lactobacillus symbiosis and confirming the response to estrogen, a multi-element in-vitro research model integrating the anatomical structure of the vagina, resident flora, local immunity and endocrine regulation is constructed, and a reliable technical platform is provided for in-depth exploration of the mechanism of vaginal micro-ecological disorder and efficient screening of related drugs.

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 application discloses application of microRNA-32-5p in preparation of a medicine for preventing and treating osteoporosis, and a medicine composition taking microRNA-32-5p as an active ingredient. It is proved through experiments that knocking out the microRNA-32-5p gene significantly aggravates osteoporosis induced by estrogen deficiency; the microRNA-32-5p plays a bone protection role by promoting osteogenic differentiation of bone marrow mesenchymal stem cells. Therefore, the microRNA-32-5p can be applied to prevention and treatment of osteoporosis as a microRNA medicine.

The present application belongs to the field of pharmaceutical chemistry, and relates to the use of a compound shown in formula (I) or a solvate thereof and a pharmaceutically acceptable salt thereof for preparing a drug for treating breast cancer. The compound has the characteristics of significantly improving the stability, solubility and dissolution of the drug and the metabolizability in vivo, has ideal pharmacokinetic characteristics and a good drug development prospect.

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.

The present invention relates to compounds of formula (I) wherein A is a 3-10 membered carbocyclic ring or a 4-12 membered heterocyclic ring containing 1-4 heteroatoms selected from O, N or S; B is any one of the following groups (1), (2) or (3); C is any one of the following groups (1'), (2'), (3') or (4'); G1 is CH2, NH or O; G2 and G3 are independently of each other CH or N; Z is -C(O)-, -SO2-, -C 1‑3 alkyl- or -CH2-C(O)-; L is a bond, -C 1‑7 alkyl- or -C 1‑7 alkenyl-. The compounds of formula (I) are inhibitors of cytochrome P450 monooxygenase 11A1 (CYP11A1). The compounds are useful as medicaments for the treatment of steroid receptor, e.g. androgen receptor or estrogen receptor dependent diseases and disorders such as cancer including prostate cancer and estrogen cancer.

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 application relates to the technical field of medicine, and more particularly to the application of beta-hydroxybutyric acid in the preparation of a drug for preventing and / or treating osteoporosis, including postmenopausal osteoporosis due to estrogen deficiency and diabetic osteoporosis, wherein the concentration of the beta-hydroxybutyric acid is 150 mM, the application of beta-hydroxybutyric acid in the preparation of a drug for inhibiting the differentiation of osteoclasts or inhibiting the formation of osteoclasts, wherein the beta-hydroxybutyric acid inhibits the differentiation of osteoclast precursor cells into osteoclasts, and the concentration of the beta-hydroxybutyric acid is 10 mM; the present application proves that beta-hydroxybutyric acid improves the bone microstructure of OVX mice and db / db mice, inhibits the differentiation of osteoclasts, and reduces bone resorption, thereby providing a new target for the prevention and treatment of osteoporosis.

The invention relates to a pharmaceutical composition comprising tamoxifen-loaded mesenchymal stem cell-derived exosomes enriched with miR-342 for use in the pharmaceutical and vaccine industry, in the treatment of cancer, in the treatment of breast cancer, in overcoming tamoxifen resistance in the treatment of estrogen receptor positive breast cancer using tamoxifen.

The application discloses application of AGPG in treatment of endocrine-resistant estrogen receptor positive breast cancer, and finds that AGPG can promote in-vitro endocrine-resistant cell cycle progression and cell proliferation through stable knockout research. Finally, a small interfering RNA drug is tested in an in-vivo experiment, and it is further proved that down-regulation of AGPG mediated by the small interfering RNA can significantly inhibit growth of tamoxifen-resistant MCF7 xenografts.

This invention discloses a Polygonatum sibiricum vesicle preparation for treating premature ovarian failure, its preparation method, and its application. The preparation method includes: cleaning Polygonatum sibiricum, juicing, filtering to remove residue, and collecting the juice; subjecting the juice to gradient centrifugation to remove residual plant tissue, plant cells, and plant cell debris; then using an extraction reagent for stepwise precipitation, collecting the precipitate, and resuspending it to obtain the final product. The Polygonatum sibiricum vesicle preparation prepared by this invention can be efficiently taken up by ovarian granulosa cells. It effectively treats premature ovarian failure by activating the Nrf2 signaling pathway, upregulating antioxidant enzyme expression, scavenging reactive oxygen species, restoring mitochondrial membrane potential, inhibiting apoptosis, and restoring the expression levels of estrogen, follicle-stimulating hormone, and anti-Müllerian hormone. The preparation method of this invention is standardized, biocompatible, and safe, and has broad clinical application prospects.

Disclosed are novel compounds for use in treating a proliferative disorder such as a cancer. Further disclosed are compositions comprising the novel compounds. Methods of using the disclosed compounds and compositions are further described. The methods include administering one or more of the disclosed compounds for treatment of various proliferative disorders, including an HRAS-driven cancer, a KRAS-driven cancer, a NRAS-driven cancer, Ewing sarcoma, B-cell acute lymphoblastic leukemia, leukemia, lung cancer, non-small cell lung cancer (NSCLC), solid tumor, breast cancer, triple-negative breast cancer (TNBC), hormone-resistant triple negative breast cancer. Further described are combination therapies in which a novel compound is administered in combination with one or more of a MEK inhibitor, a KRAS G12C inhibitor, or a Selective Estrogen Receptor Degrader (SERD) to an individual in need thereof.

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

The present disclosure provides solid and salt forms of an estrogen receptor (ER) inhibitor, compositions thereof and methods of treating a ER-mediated disorder.

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 invention belongs to the field of medical detection, and particularly relates to a memristor for non-invasive dynamic ovulation monitoring and application. The memristor comprises a substrate, a bottom electrode, a functional layer and a top electrode which are sequentially arranged from top to bottom, wherein the functional layer is a hafnium oxide film. The memristor provided by the invention has the characteristic of ultrahigh sensitivity to electrical property changes of ion concentration and viscosity in biological fluids such as saliva, urine and the like, and a complex physiological state under regulation and control of hormones such as estrogen, LH and the like is converted into a quantifiable electric signal to be output, so that dynamic and accurate capture of a growth window is realized. The low power consumption and stable cycle characteristics of the device lay a solid foundation for developing wearable integrated equipment, and the device is expected to promote the development of reproduction management towards the family, real-time and intelligent directions, and finally the success rate and safety of assisted reproduction treatment are improved.

The present invention provides a plastic composition, comprising at least one plastic and at least one plasticizer. The plastic comprises polylactic acid, the plasticizer comprises an amide ester compound, and the amide ester compound has biodegradability. The weight percentage of the plastic in the plastic composition is 85% to 99.99%, and the weight percentage of the plasticizer in the plastic composition is 0.01% to 15%. Thus, the plastic composition of the present invention can reduce damage to the environment and ecology by the biodegradable polylactic acid and the plasticizer characteristics, and has excellent biodegradability and good plasticizing effect by the specific mixing ratio. Furthermore, by designing the plasticizer structure similar to the estrogen, the plasticizer can prevent affecting normal physiological functions.

Provided herein is a method of treating, preventing, or ameliorating one or more symptoms of breast cancer with a CDK4 / 6 degrader, e.g., a compound of Formula (I). Also provided herein is a method of treating, preventing, or ameliorating one or more symptoms of breast cancer with a CDK4 / 6 degrader in combination with an estrogen receptor antagonist.