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58 results about "Oestrogen receptor" patented technology
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Prognostic biomarkers to predict overall survival and metastatic disease in patients with triple negative breast cancer
Owner:VM INST OF RES
Laser microdissection and microarray analysis of breast tumors reveal estrogen receptor related genes and pathways
InactiveCN101965190APeptide/protein ingredientsMicrobiological testing/measurementPathway analysisLaser micro dissection
Owner:VERIDEX LCC
Piperazinyltriazines as estrogen receptor modulators
Triazine derivatives of formula (I), which exhibit pharmacological activity at estrogen receptors alpha (ER alpha) and beta (ER beta) are described herein. The described invention also includes compositions and medicaments containing the triazine derivatives as well as processes for the preparation and use of such compounds, compositions and medicaments.
Owner:SMITHKLINE BECKMAN CORP
Oxo-bridged bicyclo-heptylene sulfonamides compound containing different alkyl chain lengths, as well as preparation method and application thereof
The invention discloses an oxo-bridged bicyclo-heptylene sulfonamides compound containing different alkyl chain lengths, as well as a preparation method and application thereof, and belongs to the technical field of medicines. 3-(4-hydroxycyclohexyl phenyl)-4-(4-alkoxy phenyl)-furan and a phenylethylene sulfonamide derivative are adopted as raw materials, no catalyst is needed, the raw materials are reacted at 90 DEG C for 8 hours, and the oxo-bridged bicyclo-heptylene sulfonamides compound containing the different alkyl chain lengths is obtained through one-step preparation. The action mode of the oxo-bridged bicyclo-heptylene sulfonamides compound is different from the action mode of existing anti-breast cancer drug tamoxifen, and the compound not only can be used for effectively inhibiting the growth of a breast cancer cell MCF-7, but also has favorable estrogen receptor alpha down-regulation activity equivalent to fulvestrant, and shows an application prospect of the compound in breast cancer therapy.
Owner:WUHAN UNIV
Methods and compositions in breast cancer diagnosis and therapeutics
Owner:BAYLOR COLLEGE OF MEDICINE
N-substituted azetidine derivatives
The present invention relates to novel N-substituted azetidine derivatives < of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, > to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER-positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERa) antagonistic and—in certain embodiments—selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells.
Owner:MERCK SHARP & DOHME BV
Methods and compositions in breast cancer diagnosis and therapeutics
The present invention is directed to compositions regarding a specific mutation in estrogen receptor alpha and their use as diagnostic markers in breast tissue, such as premalignant lesions, for the development of breast cancer. More specifically, cells of breast cancer whose nucleic acid comprises the estrogen receptor alpha mutation identify the breast cancer to be an invasive breast cancer.
Owner:BAYLOR COLLEGE OF MEDICINE
Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
PendingUS20210060008A1Organic active ingredientsInorganic non-active ingredientsOestrogen receptorPharmaceutical medicine
The present application relates to treating and / or preventing breast cancer, including locally advanced or metastatic, ER+, HER2− breast cancer, in a subject in need of treatment, comprising administering a compound of Formula (I),or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, R4, m, and n are defined herein.
Owner:ARVINAS OPERATIONS INC
Method for screening estrogen receptor Alpha single chain antibody with phage antibody library
InactiveCN108250295AStrong specificityImmunoglobulins against cell receptors/antigens/surface-determinantsAntigenSingle-Chain Antibodies
The invention discloses a method for screening an estrogen receptor Alpha (ER Alpha) single-chain antibody with a phage antibody library. The method comprises the following steps: using an ER Alpha protein as an immunogen for immunizing a New Zealand white rabbit and extracting total RNA of spleen; amplifying VH and VL fragments by RT-PCR, and splicing an scFv gene; constructing a PCANTAB5E-ScFv recombinant plasmid, electrotransforming E. coli TG1 competent cells with the recombinant plasmid to construct a phage single-chain antibody library; using ER Alph-positive breast cancer tissue sections and ER Alpha protein as solid phase antigens for performing affinity enrichment screening on the antibody library; and identifying positive clones with a method of combining a Phage-ElLSA method with breast cancer cell smear immunochemistry. The invention establishes a method for specifically screening ER from the phage antibody library by using the ER Alpha -positive breast cancer tissue sections, and identifying the positive clones with the method of combining the Phage-ElLSA method with the breast cancer cell smear immunochemistry, and provides a new idea for a phage antibody library screening method.
Owner:FUZHOU UNIV
Anti-breast cancer application of indeno isoquinoline estrogen receptor alpha regulator
The present invention relates to an estrogen receptor regulator of a formula (I) or a pharmaceutically acceptable salt thereof. The compounds can combine with the estrogen receptor alpha to produce the anti-breast cancer function and produce regulation function in uterus and other parts at the same time. The compounds have strong function of combining with the estrogen receptor alpha in vitro, and can effectively antagonize the combination of estrogen and the estrogen receptor alpha, thus treating breast cancer caused by excessive estrogen, while playing the role of regulating in the uterus and other parts.
Owner:CHINA PHARM UNIV
Benzoselenazole compound as well as preparation method and application thereof
InactiveCN108863985AERβ agonistic activity is goodMild conditionsOrganic chemistryAntineoplastic agentsDiseaseOestrogen receptor
The invention discloses a benzoselenazole compound as well as a preparation method and application thereof and belongs to the technical field of medicines. The preparation method of the benzoselenazole compound is characterized by preparing a series of methoxy-containing benzoselenazole compounds from o-iodoaniline derivatives, benzaldehyde derivatives and selenium under catalysis of copper through a one-pot process, and finally carrying out boron tribromide demethylation to obtain a hydroxy-containing benzoselenazole compound. In-vitro experiments show that the benzoselenazole compound as a ligand of an oestrogen receptor ER beta shows excellent agonist effect; the correlation research shows that the compound as an ERb ligand has treatment effect in animal model of rheumatic arthritis andintestinal diseases caused by inflammation, so that the benzoselenazole compound has potential treatment effect in treatment of rheumatic arthritis and intestinal diseases.
Owner:WUHAN UNIV
Androgen receptor ligands
Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation. The novel class reported demonstrates full (‘true’) antagonism in AR with low micromolar potency, high selectivity over both the Estrogen Receptors alpha and beta (ERα and ERβ) and the Glucocorticoid Receptor (GR) and only micromolar partial antagonism in the Progesterone Receptor (PR). Data provide compelling evidence for such non-LBP intervention as an alternative approach to classical PCa therapy. (Formula I).
Owner:TRINITY COLLEGE DUBLIN
Methods and medical uses
PendingUS20200171032A1Antineoplastic agentsHeterocyclic compound active ingredientsOestrogen receptorEndocrine secretion
The invention described herein provides a method for the treatment of an oestrogen receptor positive breast cancer in a subject in need thereof comprising administering to said subject a therapeutically effective amount of an MPS1 inhibitor, wherein:(i) said subject has previously been treated with an endocrine therapy; and / or(ii) said breast cancer is resistant to endocrine therapy.
Owner:THE INST OF CANCER RES ROYAL CANCER HOSPITAL +1
Cyclopropane compound as well as preparation method and application thereof
ActiveCN106632144AWide variety of sourcesLow costNervous disorderOrganic chemistryOestrogen receptorOrganic solvent
The invention discloses a cyclopropane compound as well as a preparation method and application thereof. The cyclopropane compound has a structure shown as formula I. The cyclopropane compound is prepared by taking a diazo compound and unsaturated ketone as raw materials, reacting in an organic solvent in the presence of a catalyst to obtain a cyclopropane ketone compound, and taking the cyclopropane ketone compound to further react. The preparation method of the cyclopropane compound, disclosed by the invention, has the characteristics of low cost, simplicity in method operation, moderate conditions and the like. The cyclopropane compound disclosed by the invention has affinity on an ER (Oestrogen Receptor) or has selective affinity on different subtypes; the cyclopropane compound is applied to preparation of pharmaceutical preparations for preventing or treating diseases caused by excessive expression and lack or relative shortage of the oestrogen receptor. (The formula I is shown in the description.).
Owner:ZHEJIANG ACAD OF MEDICAL SCI
Skin nutrient solution component capable of improving skin microcirculation
InactiveCN107898708AGood anti-inflammatory effectPromote gastric laxative effectCosmetic preparationsToilet preparationsDiseaseOestrogen receptor
The invention discloses a skin nutrient solution component capable of improving skin microcirculation. The skin nutrient solution component capable of improving the skin microcirculation is prepared from the following components: 20 to 30 parts of radix puerariae, 22 to 28 parts of radix ginseng, 15 to 18 parts of aloe, 10 to 15 parts of water-soluble vitamin, 10 to 12 parts of ascorbyl glucoside,6 to 10 parts of creatine phosphate sodium and 4 to 8 parts of hyaluronic acid; the component radix pueraria can be combined with oestrogen receptors on surfaces of all systems and organ tissue cellsof a body to play a role; compared with other medicines for adjusting female endocrine, pueraria isoflavone has the unique feature that the pueraria isoflavone is combined with the in vivo oestrogenreceptors firstly and has a moderate effect; the wild radix ginseng is suitable for reinforcing vital energy, improving intelligence and calming nerves, tonifying and keeping health, improving the immune function and promoting the rehabilitation of diseases; the aloes have a sterilization effect, an anti-inflammation effect, a moistening and beautifying effect and an anti-ageing effect; the components including the water-soluble vitamin, the ascorbyl glucoside, the creatine phosphate sodium and the hyaluronic acid are adopted; the components are microelements which are used for keeping human body skin healthy and beautifying skin.
Owner:张明越
Primer used for performing pyrophosphoric acid detection on PvuII and XbaI polymorphism of intron 1 of estrogen receptor gene alpha
ActiveCN102703591AStrong specificityImprove accuracyMicrobiological testing/measurementDNA/RNA fragmentationHormone dependenceEstrogen receptor gene
The invention discloses a primer used for performing pyrophosphoric acid detection on PvuII and XbaI polymorphism of an intron 1 of an estrogen receptor gene alpha. The primer comprises a specific primer and a primer, wherein the specific primer is used for amplifying the PvuII and XbaI nucleic acid fragment of the estrogen receptor gene alpha from a sample nucleic acid, and the primer is used for performing pyrophosphoric acid sequencing on the obtained nucleic acid fragment. By adopting the pyrophosphoric acid sequencing technology, through the specific amplification primer and the pyrophosphoric acid sequencing primer disclosed by the invention, the PvuII and XbaI polymorphism of the intron 1 of the estrogen receptor gene alpha, which is related with hormone-dependent diseases, can be detected. The primer used for performing the pyrophosphoric acid detection on the PvuII and XbaI polymorphism of the intron 1 of the estrogen receptor gene alpha is high in specificity and accuracy, and can be clinically used as an auxiliary index and screening of early prevention and early diagnosis on agnogenic hypomenorrhea and other certain hormone-dependent related diseases.
Owner:北京艾迪康医学检验实验室有限公司
Applications of isobavachin for preparing antineoplastic, osteoporosis and senile dementia medicament
The invention relates to the use of bavachin in preparing drugs against tumors, osteoporosis and senile dementia, which belongs to the field of natural medicines. Bavachin has the structural formula shown as the figure (I). Experimental studies shows that the compound of formula (I), in low concentration, doesn't change the expressions of ERalpha66, ERalpha46 and ERalpha36, but in high concentration, inhibits the expressions thereof. Furthermore, the compound (I) can kill breast cancer cell line MCF7 that expresses ERalpha66, ERalpha46 and ERalpha36. The compound (I) can also be used as regulator of estrogen receptor ERalpha36 to treat diseases caused by abnormal expression of estrogen receptor ERalpha36, such as tumors, osteoporosis, asthma, heart diseases and senile dementia.
Owner:BEIJING SHENOGEN BIOMEDICAL
Hepatocytes
InactiveUS20080131404A1Evaluate suitabilityDetermining effectBiocideFusion with DNA-binding domainOestrogen receptorMammal
The invention relates to the production of hepatocyte cell lines useful in toxicology screens or therapy. A mammalian hepatocyte comprises, as a single polypeptide, a fusion protein comprising a c-myc protein and an oestrogen receptor, or functional fragments thereof.
Owner:JOHNSON DEBORAH +3
Methods and medical uses
ActiveUS20200138815A1Antineoplastic agentsHeterocyclic compound active ingredientsOestrogen receptorOncology
The invention described herein provides a method for the treatment of an oestrogen receptor positive breast cancer in a subject in need thereof comprising administering to said subject a therapeutically effective amount of a compound capable of inhibiting MPS1, wherein:(i) said subject has previously been treated with a CDK4 / 6 inhibitor; and / or(ii) said breast cancer is resistant to treatment with a CDK4 / 6 inhibitor.
Owner:THE INST OF CANCER RES ROYAL CANCER HOSPITAL +1
Function of 2',2'-CH3-2'H,4H-3,6'-two benzopyran-4-ketone
The invention relates to an application of 2`,2`-dimethyl-2`H, 4H-3, 6`-bis- benzopyran-4-ketone , in particular to an application of the compound 2`,2`-dimethyl-2`H, 4H-3, 6`-bis- benzopyran-4-ketone in preparing drugs for treating related diseases such as estrogen receptor ER-Alpha subtype and ER-Beta subtype, belonging to the medicine field. In the condition of low concentration, the compound does not change the expressions of ER-Alpha66, ER-Alpha46 and ER-Alpha36; while in the condition of high concentration, the compound can inhibit the expressions of the three at the same time. Meanwhile, the compound can kill breast cancer cell MCF7 that expresses the ER-Alpha66, the ER-Alpha46 and the ER-Alpha36. Therefore, the compound can be also used as the regulator of the estrogen receptor ER-Alpha36 to treat diseases caused by abnormal expression of the estrogen receptor ER-Alpha36, such as tumor, osteoporosis, asthma, heart disease or senile dementia , etc.
Owner:BEIJING SHENOGEN BIOMEDICAL
Breast cancer organoid culture solution, preparation method and culture method
ActiveCN114591887AReflect tumor drug resistanceEffective guidanceCulture processEpidermal cells/skin cellsOestrogen receptorHistiocyte
The invention discloses a breast cancer organoid culture solution as well as a preparation method and a culture method thereof. The culture solution is prepared from the following components: a basic culture medium, 1 to 5mM of L-alanyl-L-glutamine, 90 to 110U / mL of a blue chain double antibody, 0.5 to 1 percent (vol / vol) of an N2 additive, 1 to 2 percent (vol / vol) of a B27 additive, 0.06 to 0.1 mM of non-essential amino acid, 0.1 to 0.5 mu M of SB 203580, 3 to 8mM of nicotinamide, a growth factor and a system stabilizing factor. According to the culture solution disclosed by the invention, not only can very high cell and tissue activity be maintained in a culture process of breast cancer tissue cells, but also the breast cancer tissue cells can be cultured by simulating a disordered hormone environment in the body of a patient; the expression levels of the estrogen receptor PR and the progestational hormone receptor ER during preservation of the in-vitro cultured breast cancer organoid sample can better express the inherent pathological characteristics of the estrogen receptor PR and the progestational hormone receptor ER.
Owner:杭州艾名医学科技有限公司
Phoshorylation of Estrogen Receptor Alpha
Owner:UNIVERSITY OF MANITOBA
Mycer immortalized hepatocyte
InactiveCN101044236AExcellent transplantFusion with DNA-binding domainAntipyreticOestrogen receptorMammal
Owner:RENEURON LTD
Methods and medical uses
PendingCN110799183AAntineoplastic agentsHeterocyclic compound active ingredientsEndocrine therapyOestrogen receptor
Owner:THE INST OF CANCER RES ROYAL CANCER HOSPITAL +1
Application of ligustilide to prevention and treatment of breast cancer
InactiveCN105640940AReduce expressionIncrease transcriptional activityOrganic active ingredientsAntineoplastic agentsEstrogen receptorOncology
The invention discloses application of ligustilide to prevention and treatment of breast cancer. A research represents that the ligustilide has a certain inhibition effect on negative and positive breast cancer cells of an estrogen receptor alpha (ERalpha). Furthermore, existing breast-cancer-resisting drugs including tamoxifen and the like in the market mainly have effects on the positive breast cancer cells of the estrogen receptor alpha, but have very slight effects on the negative breast cancer cells of the estrogen receptor alpha; the research provided by the invention represents that the ligustilide can be used for increasing ERalpha protein expression of the breast cancer cells, and furthermore, the ligustilide and the tamoxifen are cooperated to realize the effect of preventing and treating the breast cancer.
Owner:SOUTHWEST UNIVERSITY
Methods for utilizing esr copy number changes in breast cancer treatments and prognoses
InactiveUS20080318240A1Microbiological testing/measurementAntineoplastic agentsTreatment effectEstrogen receptor
The present invention relates to methods for estimation of efficacy of therapeutic treatment of cancer patients, in particular breast cancer patients. The estimation is based on determining of the status of aberration of the estrogen receptor alpha gene (ESR1) in situ, and, optionally, the status of aberration of a gene related to ESR1. In particular, the invention relates to determining the presence or absence and, if present, the type of aberration, e.g. amplification, duplication, polyploidization, deletion or translocation of the ESR1 gene in the tumor cells of the patient. The invention further relates to a kit-in-parts comprising probes for the determining the status of aberration of ESR1 and ESR1-related genes in situ.
Owner:DAKOAS
Selective estrogen receptor degrader
Owner:SUN PHARMA INDS
RT-PCR primer and method for amplifying estrogen receptor alpha genes in female chinemys reevesii
InactiveCN107653302ARapid expansionAccurate amplificationMicrobiological testing/measurementDNA/RNA fragmentationTotal rnaGene
The invention discloses a RT-PCR primer and method for amplifying estrogen receptor alpha genes in female chinemys reevesii. The RT-PCR primer comprises a primer pairs as shown in SEQ ID No:1 and SEQID No:2. The method comprises the following steps: 1) extracting total RNA of a to-be-amplified sample; 2) reversely transcribing the extracted total RNA into cDNA; 3) amplifying the cDNA by using theRT-PCR primer; PT-PCR primer is the PT-PCR primer. According to the invention, a set of RT-PCR primers are designed, the total RNA of the to-be-amplified sample is extracted, and then reverse transcription is conducted to obtain the cDNA. The cDNA is amplified by using the RT-PCR primer. Under the premise of cost reducing, a great number of estrogen receptor alpha genes in female chinemys reevesii fallopian tubes are amplified rapidly and accurately, and large-scale and more intuitive studies of the estrogen receptor alpha genes in the female chinemys reevesii are effectively achieved.
Owner:ANHUI NORMAL UNIV
16Alpha-methyl or ethyl substituted estrogens
The invention makes a 16α-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a Δ5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor α selective treatment
Owner:NV ORGANON
Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket
![Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/1a5aa94f-5bc1-4104-8f1f-91f8f3c2df14/H2007101218530E00011.PNG "Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket")
![Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/1a5aa94f-5bc1-4104-8f1f-91f8f3c2df14/H2007101218530E00012.PNG "Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket")
![Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/1a5aa94f-5bc1-4104-8f1f-91f8f3c2df14/H2007101218530E00013.PNG "Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket")
Owner:BEIJING SHENOGEN BIOMEDICAL
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