57 results about "Anti estrogen" patented technology

The present invention relates to a method of treating or preventing musculoskeletal pain in a mammal receiving administration of an estrogen. suppressant selected from the group consisting of aromatase inhibitors, GnRH analogues, cyclo-oxy-genase 2 (COX-2) inhibitors, 17β-hydroxysteroid dehydrogenase type 1 inhibitors, progestogens, anti-estrogens and combinations thereof, said method comprising the administration of an effective amount of an estrogenic component, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula (1) in which formula R₁, R₂, R₃, R₄ independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors.

This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein.

This invention relates to combination therapies for the treatment of breast cancer comprising administering to a subject in need thereof a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist, or an estrogen receptor downregulator) and to compositions (e.g., pharmaceutical compositions) comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent. This invention also relates to a method of treating the side effects (e.g., vasomotor disturbances, osteoporosis and musculoskeletal complaints) associated with anti-estrogen therapy in a subject treated with one or more anti-estrogenic agents (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist or an estrogen receptor downregulator). The method comprises administering to the subject an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof.

The invention relates to an endogenous protein marking method applied to genome-wide binding spectrum analysis. The method comprises the steps of designing sgRNA for upstream and downstream 50bp regions of an encoding termination site of an NCOA1 gene; verifying cutting efficiency of sgRNA mediated Cas9 by an experiment; building an anti-estrogen therapy tolerant MCF-7 breast cancer cell model; by utilizing a CRISPR/Cas9 homologous recombination technology, selecting and using effective sgRNA and DNA donors, and introducing a Flag tag in the 3' end of the ER alpha co-transcription factor NCOA1 gene; and establishing a stable cell line with the Flag tag. Compared with the prior art, the method has the advantages that gene editing is performed by utilizing the CRISPR/Cas9 technology, so that the tag insertion efficiency of the gene editing is greatly improved; more importantly, chromatin structure parameters are introduced for designing sgRNA, so that effective cutting of Cas9 at a target site of a genome is ensured; and positive clone screening is performed by adopting DNA sequencing and RT-PCR sequencing methods, so that the positive clone identification step is simplified and the manpower and material resources for screening are reduced.

Methods and compositions containing bicifadine are provided for the treatment and prevention of hyperthermia in mammalian subjects. The methods and compositions may be used to prevent or treat fever, pyresis, menopausal hot flashes; peri menopausal hot flashes, postmenopausal hot flashes, hot flashes caused by anti-estrogen therapy, hot flashes secondary to surgical removal of estrogen producing tissue, hot flashes caused by radiation therapy, malignant hyperthermia, serotonin syndrome, heat stroke, febrile seizures, and neuroleptic malignant syndrome, among other conditions. Additional compositions and methods are provided employing bicifadine to treat pyresis and simultaneously elicit an analgesic response in mammalian subjects. Yet additional compositions and methods are provided which employ bicifadine in combination with a second antipyretic agent, a second analgesic agent, or a different therapeutic agent to yield more effective antipyretic treatment tools, and/or dual activity therapeutic methods and formulations useful to prevent or reduce hyperthermia and one or more additional symptoms (e.g., pain, or depression) in mammalian subjects.

The present invention relates to compounds of Formula (I),

methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

The present invention relates to compounds of Formula (I),

methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

The invention discloses a method for identifying excited and antagonistic actions of an organic estrogen. By utilizing the molecular dynamic method, the binding process between an organic substance and an estrogen receptor is computed and analyzed; and based on the ligand binding mode and the change of the estrogen ligand binding area conformation, particularly the change of the spiral position of H12 in the LBD structure of ER, whether the organic substance is the excitant or antagon is identified. The method has the advantages of effectively identifying the pseudo/anti-estrogen action, having simple method and low cost, saving a large amount of manpower, material resources and financial resources and providing a basic tool and a shortcut for the large-scaled implementation of the poisonous chemicals environment safety evaluation(REACH).

The present invention relates to pharmaceutically acceptable complex formulae comprising complexes of Fulvestrant, or a salt, or derivatives thereof and complexation agents and pharmaceutically acceptable excipients, process for the preparation thereof and pharmaceutical compositions containing them. The complex formulae of the present invention have improved physicochemical properties which makes the compound orally available and makes oral administration of the compound possible in the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.

A method for inducing ERα expression in cancer cells in a subject affected with cancer cells which are ERα (−) is disclosed. The method involves administering to the subject an effective amount of a PPARγ antagonist alone or in combination with anti-estrogen therapy.

The invention provides a 3-substituted acrylic acid compound as well as a preparation method and application thereof and in particular relates to a 3-substituted acrylic acid compound, a stereoisomer,a pro-drug, a hydrate or pharmaceutically acceptable salt or ester thereof, and a pharmaceutical composition thereof as well as a preparation method and application thereof. The compound provided bythe invention can inhibit activity of an estrogen receptor, regulate expression level of the estrogen receptor down or induce degradation of the estrogen receptor and can be used for preventing or treating diseases related to overactivity of the estrogen receptor, especially estrogen receptor positive (ER+) drug-resistant diseases (such as breast cancer producing drug resistance to anti-estrogen therapy).

The present invention is directed to a method of treating estrogen responsive breast cancer in an individual comprising administering to an individual a therapeutically effective estradiol inhibiting amount of interferon gamma (IFN-γ) and/for a tumor necrosis factor (TNF) antagonist and/or an interleukin-1 (IL-1) antagonists. The invention is based upon the surprising discovery that IFN-γ and/or a tumor necrosis factor (TNF) antagonist and/or an interleukin-1 (IL-1) antagonists inhibit estradiol production in human adipocytes. This discovery is not only important because it allows for the treatment and/or prevention of estrogen dependent breast cancer using IFN-γ, TNF antagonists or IL-1 antagonist each alone or in combination, but also because IFN-γ and/or TNF antagonists and/or IL-1 antagonists can be used in conjunction with standard anti-estrogen therapy, e.g., tamoxifen and/or aromatase inhibitor, to result in lower estrogen levels than seen with standard anti-estrogen therapy alone. Moreover, the ability to lower estrogen levels by means of the present invention, when combined with standard anti-estrogen therapy, provides an important therapeutic option in that it allows the dose of the anti-estrogen to be reduced, reducing the likelihood of side effects and complications commonly seen with anti-estrogen therapy.

The present invention is a kind of pessary or intrauterine medicine releasing device containing one medicine part, and features the medicine part containing anti-estrogen in 40-70 weight portions and anti-progestogen in 30-60 weight portions. The present invention also provides the application of the pessary or the intrauterine medicine releasing device in preparing medicine for treating hysteromyma or endometriosis.

An improved method and products for the hormonal treatment of breast cancer by breast implants of anti-estrogens and steroid hormones in formulations as fused with a lipoid carrier or encapsulated in microcapsules or in Silastic capsules is provided. Such breast implants renders a constant slow-release of their contents to the breast tissue for extended periods by biodegradation and diffusion. It facilitates higher breast tissue concentrations of anti-estrogen and hormonal compositions. Because of their high concentration in the breast and lower systemic distribution, tumor control is much improved and the their systemic toxicity is minimized. An added beneficial effect of these breast implants on breast cancer is mediated by the inhibition of hypothalamic-pituitary LHRH, FSH and LH secretion by these composition's systemic contents. It is also an effective prophylaxis against breast cancer. Furthermore, it reduces the cost of hormonal treatment of breast cancer. Anti-estrogen hormonal implants to the breast as concomitant hormonal treatment with conventional radiation therapy also facilitates improved tumor control and cure rates of breast cancer.

In one embodiment, the invention provides a method of treating a subject suffering from a breast cancer tumor which is non-responsive or intrinsically resistant to anti-estrogen therapy comprising administering a therapeutically effective amount of an inhibitor of alternative (ALT) non-homologous end joining (NHEJ) factor to the subject.

In another embodiment the invention provides a method of treating a subject who suffers from a pancreatic cancer which is non-responsive to chemotherapy and/or radiation comprising co-administering a therapeutically effective amount of PARP1 inhibitor and a DNA ligase IIIα inhibitor to the subject. Related diagnostic methods, nucleic acid arrays, devices and kits are also provided.

The invention relates to a pharmaceutical combined preparation of LHRH analogues and anti-oestrogens having tissue-selective oestrogen activity and also to its use for the treatment of gynaecological disorders, especially for the treatment of endometrioses and myomas.

Gene signatures, specific marker genes, and diagnostic assays for predicting progression free survival and objective response to anti-estrogen, e. g., tamoxifen therapy for recurring breast cancer patients are described.

The invention relates to dialkyltriazene-bearing estrogens and anti-estrogens that are suited for use as chemotherapeutic drugs for treating carcinomas of the sexual organs of humans and animals.

The invention discloses a compound used as an estrogen-related receptor regulator and an application of the compound. The compound is a 1-hydrogen-1, 2, 3-triazole compound with a structure as shown in formula (I) as well as pharmaceutical acceptable salt or prodrug molecule. The compound as well as pharmaceutical acceptable salt or prodrug molecule can be used for preparing drugs for adjusting activity of estrogen relevant receptor (ERR), preventing and treating breast cancer (comprising diseases which are free of influence of an anti-estrogen method), prostatic cancer or metabolic diseases. The formula (I) is as shown in the specification.

The invention provides for treatment of MUC1+/ERα+/− cancers using an anti-MUC1 therapy, optionally including an anti-ERα therapy. In particular, the invention addresses the treatment of tamoxifen-resistant cancers, using MUC1+, and optionally anti-ERα therapy.