183 results about "Sexual hormones" patented technology

GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

A sustained release formulation by using dimeticone as the dispersion medium, which includes active ingredient (e.g., drugs against parasites, insecticides, NSAIDs, antibiotics, sex hormone like agents or oily soluble vitamins) and dimeticone as the medium. Suitable stabilizer, antioxidant, local analgesics and material for sustained release may be added. The formulation is bio-compatible, stable and injectable.

An improved method and products for the primary hormonal treatment of early stage, low and intermediate risk prostate cancers by prostatic implants of androgen suppressive drugs formulated as fused with a lipoid carrier or encapsulated in microcapsules or in Silastic capsules is provided. Such prostatic implants renders a constant slow-release of their contents to the prostate for extended periods by biodegradation and diffusion. It facilitates higher prostatic and lower systemic concentrations of androgen suppressive hormones. Because of their high prostatic and lower systemic concentrations, tumor control is much improved and the their systemic toxicity is minimized. Tumor control after such primary hormonal implant treatment is followed by clinical examinations and the biochemical tumor control is followed by periodic estimations of serum levels of PSA and acid phosphatase. More complex and expensive surgery or radiation therapy for this group of good prognostic early stage prostate cancer is reserved for those patients failing to this primary hormonal treatment. It will preserve potency more than by surgery or radiation therapy. Furthermore, it would reduce the cost of treatment for early stage prostate cancer significantly. Androgen suppressive hormonal implants to the prostate before, during or after lower dose conventional radiation therapy would also facilitate equal or better cure rates of localized prostate cancer as compared to the more complex and toxic higher dose radiation therapy.

The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.

This invention relates to a pernasally administrable preparation for the controlled release of sexual hormones to the systemic circulation, in particular to a formulation which enables its active ingredient to be absorbed in a sustained manner providing a better bioavailability at very low doses and longer duration of action.

A compound of the formula:wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula:wherein R5 is hydrogen or R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.

The present compounds are intermediates for the preparation of quinoline derivatives and compositions having gonadotropin-releasing hormone antagonistic activity useful as propylactics or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, uterine or cervical cancer, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; are effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a male or female contraceptive, as an ovulation-inducing agent; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; and are useful for modulating estrous cycles in animals in the field of animal husbandry, as agents for improving the quality of edible meat or promoting the growth of animals, and as agents for promoting spawning in fish.

The present invention provides a protein capable of binding to a female sex hormone, which protein is supplemented with useful properties for measuring, quantifying and concentrating female sex hormones, such as high sensitivity, low cross-reactivity, unlikelihood of being influenced by interfering substances, and unlikelihood of being influenced by solvents. Specifically, the present invention provides a recombinant protein prepared by obtaining various genes for various antibodies against female sex hormones, and modifying, by gene recombination technology, various properties of the original antibody, such as affinity, avidity, cross-reactivity, resistance for interfering substance on antigen-antibody reaction, resistance for interfering substance on enzymatic color developing reaction, resistance for solvent and the like.

The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O— (alkylene)-Y, —O-Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.

A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a contraceptive of male or female, as an ovulation-inducing agent of female; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; is useful as modulating estrous cycles in animals in the field of animal husbandry, as an agent fro improving the quality of edible meat or promoting the growth of animals; is useful as an agent of spawning promotion in fish.

The present invention relates to a compound medicine for preventing and curing angiocardiopathy and cerebrovascular disease, belonging to the field of chemical medicine. It is characterized by that said compound medicine includes sexual hormones medicine, lipid-reducing medicine, hypotenser, hypoglycemic medicine and anticoagulant medicine. Said compound medicine can be made into various dosage forms. Besides, said compound medicine also can be used for curing the diseases of climacteric syndrome, osteoporosis, endometrial carcinoma, diabetes and metabolic syndrome, etc.

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

The invention is directed to analogs of LHRH-II and, more generally, to analogs of the LHRH family in which modifications have been made that confer enhanced binding affinity for LHRH receptors and / or improved metabolic stability.The invention is further directed to methods of targeted therapy and targeted imaging in patients with sex-hormone-related cancers or other LHRH-mediated diseases.

[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like.[Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

The medicine for preventing and treating osteoporosis is prepared with the natural plants drynaria rhizome, desert cistanche, malaytea scurfpea fruit, epimedium, American ginseng, etc. and through drying, crushing, decoction and solvent extraction, mixing, disinfection and other steps of prepare medicine powder or table. The said preparation process can maintain the biological activity of the medicine components, and the medicine can raise the sexual hormone level of the body, stimulate the osteoplast to secret collagenase, release grorth factor and cell factor, raise the activity of the osteoplast to promote the production of bone matrix, speed the bone formation process, inhibit the dynamic balance of osteoclast and thus prevent and treating osteoporosis radically.

Disclosed are methods of inhibiting bone resorption and / or promoting bone formation using GLP-2 and related Compounds. The invention has a wide spectrum of important uses including hyperparathyroidism, Paget's disease, hypercalcemia of malignancy, osteolytic lesions produced by bone metastasis, bone loss due to immobilisation or sex hormone deficiency, osteomalacia, hyperostosis and osteopetrosis.

The invention relates to a traditional Chinese medicinal wine with functions of nourishing yin, strengthening yang and prolonging life span, and a preparation method thereof, The traditional Chinese medicinal wine is characterized in that pallas pit viper, dog penis, deer penis, hippocampus, gecko, pilose antler and Cordyceps sinensis are respectively soaked in wines to obtain a pallas pit viper wine, dog penis, deer penis wine, hippocampus wine are soaked in wine by adding Ganoderma lucidum, cynomorium songaricum, morinda officinalis, epimeddium, cistanche, wolfberry and Radix Polygoni Multiflori Preparata to obtain the traditional Chinese medicinal wine, the traditional Chinese medicine is taken out and extracted by adding water, filtered to obtain a traditional Chinese medicine water decoction agent, five ingredients are mixed to prepare. The traditional Chinese medicinal wine is capable of promoting the growth of sexual glands and sexual organs of male and female, raising the sex hormone content secreted by the human bodies, increasing the immunity of human bodies and inhibiting the cell mutation to cause carcinogenesis, and has the functions of nourishing yin and reinforcing kidney, invigorating yang and producing sperm, keeping young and blackening hair, as well as prolonging life span.

A compound medicine for preventing and treating the cardiovascular and cerebrovascular diseases of climacteric woman and adult man, climacteric syndrome, osteoporosis, endometrial carcinoma, senile dementia, diabetes and metabolism syndrome contains sexual hormones, hypolipemic component, antihypertensive component and anticoagulating component. It features that the ratio of its components is adjustable according to actual disease.

The invention provides a compound. The compound is characterized by comprising a structure shown in the description. The novel small-molecule compound can be used for promoting regrowth of hair when applied for external use, and can be used for treating androgen genotype alopecia, seborrheic alopecia or alopecia caused by chemotherapy and other various factors.

The invention relates to a Chinese medicinal composition for a kidney-yang deficiency and phlegm-retention type polycystic ovary syndrome. The Chinese medicinal composition comprises the following medicinal materials of epimedium, caladium, semen psoraleae, sliced deerhorn, sea horse, tortoise plastron and the like, does not contain rhubarb and Chinese angelica. The Chinese medicinal composition can reduce the level of androgens and androgen receptors of polycystic ovanian syndrome (PCOS) patients, improve the level of sex hormone binding globulin, reduce the level of free testosterone, improve the level of in-vivo estrogens, improve the growth and development of follicles and improve the ovulation rate and pregnancy rate of patients.

A method of birth control and hormone regulation comprises utilizing a vaginal ring worn continuously during each menstrual cycle. A vaginal ring delivers predetermined doses of progesterone and beta-estradiol. Beta-estradiol does not cause an increase in sex hormone binding globulin and thereby does not decrease a woman's levels of free testosterone and libido.

The invention relates to the field of immunology, endocrinology and oncology and, in particular, the generation of a combined immune response to determined growth factors and hormones. A synergic effect, outlined herein, between growth regulating factors (EGF, TGF and VEGF) and hormones involved in the sexual hormones release cascade or reproduction (GnRH, LH, FSH) stimulates the anti-tumor response which is expressed as a reduction in the tumor mass and an increase in the survival time.

The inventors have proposed a novel panel of human plasma protein biomarkers for diagnosing hepatic fibrosis and cirrhosis. Presently there is no reliable non-invasive way of assessing liver fibrosis. A 2D-PAGE based proteomics study was used to identify potential fibrosis biomarkers. Plasma from patients with hepatic cirrhosis induced by infection with the hepatitis C virus (HCV) were analysed. Several proteins associated with liver scarring and potentially also related to viral infection were identified. These proteins include 14-3-3 protein zeta / delta, adiponectin, afamin, alpha-1-antitrypsin, alpha-2-HS-glycoprotein, apolipoprotein C-III, apolipoprotein E, C4b-binding protein beta chain, intact / cleaved complement C3dg, corticosteroid-binding globulin, fibrinogen gamma chain, beta haptoglobin at pH 5.46-5.49, haptoglobin-related protein, hemopexin, immunoglobulin J chain, leucine-rich alpha-2-glycoprotein, lipid transfer inhibitor protein, retinol-binding protein 4, serum paraoxonase / arylesterase 1, sex hormone-binding globulin and zinc-alpha-2-glycoprotein. These biomarkers can be used in conjunction with polypeptides in WO / 2008 / 031051. The concentrations of these novel biomarkers can be determined using an immunoassay where the concentrations would reflect the extent of fibrosis. A fibrosis scoring scale for each of the novel biomarkers is proposed. The additive result from the scores of all the novel biomarkers would give a more reliable indication of the degree of fibrosis rather than examining individual biomarkers.

The invention discloses a polypeptide carrier used for improving targeting ability and transfection efficiency of a medicine / gene. The polypeptide carrier has a structure represented by a formula (I): TATp-Cys-LHRHp (I), wherein TATp is a TAT fragment of HIV, Cys is Cysteine, LHRHp is an analogue of luteinizing hormone releasing hormone LHRH. The polypeptide carrier provided by the invention carries a large amount of positive charges. The polypeptide carrier has good water-solubility and high targeting ability aiming at sexual hormone dependent tumor and liver cancer. The carrier can directlycarry negatively charged nucleic acid or medicine, and mediate the nucleic acid or medicine into cells. Also, the carrier can be used for modifying other gene or medicine carriers, such that tumor targeting abilities and transfection efficiency of the gene or medicine carriers can be improved. Therefore, a novel carrier is provided for gene / medicine delivering.

The life prolonging Chinese medicine wine is prepared through soaking palls pit viper, cobra and 11 kinds of Chinese medicinal materials including glossy ganoderma, fleeceflower root, wolfberry fruit, desert cistanche, pilose antler, etc. in Kaoliang wine of 50% alcohol content. It has the functions of prolonging life, nourishing Yin, strengthening Yang, preventing and treating cancer, promoting sexual organ growth and raising sexual hormone secreting level, etc.

The invention belongs to the technical field of medicine, and particularly relates to an application of tetracyclic-triterpene-like compound-like cucurbitacine B separated and extracted from cucurbitaceous plants as a cancerous inhibitor of protein phosphatase 2A. Cucurbitacine B is taken as a main component in the cancerous inhibitor of protein phosphatase 2A, so that the expression of the cancerous inhibitor of protein phosphatase 2A can be inhibited remarkably. The cucurbitacine B can be applied to independent administration or combined treatment, including combined applications with radiotherapy, chemotherapy, surgical treatment, other growth factor inhibitors and sexual hormone inhibitors, any tumor treatment medicament and method.