175 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 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.

A method for treatment of benign prostate hyperplasia, prostate cancer, estrogen-dependent breast cancer, endometrial cancer, ovarian cancer, endometriosis and precocious puberty, or for use for contraceptive purposes or in an in vitro fertilization programme, or for treatment of sex offenders is provided. The method comprises the administration by subcutaneous or intramuscular injection of a therapeutically effective amount of an injectable pharmaceutical composition comprising a solution of a GnRH antagonist peptide according to general formula 1 or a pharmaceutically acceptable salt thereof in a concentration of 0.3-120 mg / ml. Also a pharmaceutical composition and a pharmaceutical kit of parts are provided.

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.

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.

To provide a compound useful as a prophylactic or therapeutic agent for a sex hormone-dependent disease or the like. [MEANS FOR SOLVING PROBLEMS] Disclosed are: a nitrogenated fused ring derivative represented by the general formula (I), or a prodrug, salt or the like thereof, which has a GnRH antagonistic activity; a pharmaceutical composition comprising the derivative or the prodrug, salt or the like thereof; use of the the derivative or the prodrug, salt or the like thereof for medical purposes; and others. In the general formula (I), the rings A and B independently represent an aryl or a heteroaryl; R and R independently represent a halogen, a cyano, an alkyl, an alkylsulfonyl, -OW<1>, -SW<1>, -COW<2>, -NW<3>W<4>, -SO2NW<3>W<4>, an aryl or the like; R<C> represents H or an alkyl; Erepresents an oxygen atom or the like; U represetns a single bond or an alkylene; and X represents Y, -CO-Y, -SO2-Y, -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y or the like [wherein Y represents Z, an amino or the like; and Z represents a cycloalkyl, a heterocycloalkyl, an aryl, a heteroaryl or the like].

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.

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.