219 results about "Hormone dependence" patented technology

Selective androgen receptor modulators (SARMs) having antagonist activity in hormone-dependent tumors while exhibiting no activity or agonist activity against other nontumor tissues containing the androgen receptor as well as methods for identifying, designing and using SARMs are provided.

The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

A progesterone receptor modulator of the structure is provided. Use of compositions containing this compound for contraception, hormone replacement therapy, treating hormone-dependent disease, synchronizing estrus, treating dysmenorrhea, treating dysfunctional uterine bleeding, inducing amenorrhea, or treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder in a mammal are described.

A pharmaceutical composition for the treatment of an estrogen-dependent disease or condition comprises: (1) at least one polysaccharide selected from the group consisting of an alginate and a fucoidan in a quantity effective to treat an estrogen-dependent disease or condition; and (2) a pharmaceutically acceptable carrier. The composition can include both an alginate and a fucoidan. The composition can include other ingredients such as at least one compound selected from the group consisting of diindolylmethane and indole-3-carbinol in a quantity sufficient to inhibit the activity of estrogen. Methods for use of the composition for the treatment of an estrogen-dependent disease or condition, especially endometriosis, are described.

A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.

A food product containing an effective amount of an active agent which is hydroxymatairesinol, a geometric isomer or stereoisomer thereof, or an acceptable salt thereof, or a mixture thereof, where the food product is selected from the group consisting of a nutritional supplement and a nutrient. The food product can increase the level of enterolactone or another metabolite of hydroxymatairesinol in a person's serum thereby causing prevention of a cancer or a certain non-cancer, hormone dependent disease in a person, based on the administration of hydroxymatairesinol to the person.

The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

The invention relates to a gel composition containing tacrolimus, which contains the tacrolimus and ingredients of a matrix, wherein, the ingredients of the matrix contain one or more of liquid polyethylene glycol, glycerin and propylene glycol, the content of the tacrolimus in the gel is 0.01 percent to 0.5 percent, and the weight ratio of the tacrolimus to one or more of the liquid polyethylene glycol, the glycerin and the propylene glycol is 1: (50 to 3000). The invention further relates to a preparation method of the gel composition of the tacrolimus and the application of the gel composition in the preparation of drugs for the treatment of atopic dermatitis, vitiligo, psoriasis, hormone-dependent dermatitis, intractable neurodermatitis, lupus erythematosus, alopecia areata and other diseases.

LHRH analogues and LHRH antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and / or advanced prostate carcinoma, by administering an initial dose of an LHRH analogue over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an LHRH antagonist over a second period, the dose being insufficient to achieve and / or maintain hormonal castration.

Androgens and their derivates and analogs, such as anabolic agents, are characterized by at least one substituent or substituent grouping with radical trapping properties. These compounds are used as androgen or anabolic agent substitutes or therapeutical agents for treating androgen defficiency; for treating benign prostate hypertrophy and prostate carcinome, in particular with a testosterone-based compound; for treating osteoporosis, in particular post-menopausal osteoporosis in women, preferably associated with estrogen and / or gestagens; for treating brain oedema induced by vasculary or ischemic troubles, subarachnoidal bleeding, ischemic shock and cerebral insult; for treating asthma in its various forms, for treating Alzheimer's disease, Parkinson's disease; for organ transplants; and for treating androgen-dependent and non androgen-dependent malign neoplasia

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 novel class of gonane type and D-homo-gonane type steroids having sulfatase-inhibiting and / or estrogenic activity is presented for application in the pharmaceutical industry. The number and location of sulfamoyloxy groups on the steroids provides for sulfatase inhibiting and estrogenic activities that independently vary over a wide range, allowing the customization of the pharmaceutical for specific purposes, including treatment and diagnosis of estrogen-dependent tumors.

Compositions, preferably pharmaceutical compositions, containing micronized tanaproget, or pharmaceutically acceptable salt thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, butylated hydroxyanisole, povidone, and magnesium stearate, are provided. The compositions are useful in contraception and hormone replacement therapy and in the treatment and / or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.

The invention provides methods and dosing regimens for safely and effectively treating androgen-dependent prostate cancer with a gonadotrophin releasing hormone (GnRH) antagonist without causing a testosterone spike and / or other side effect of GnRH agonist therapy such as a urinary tract infection, or an arthralgia-related or cardiovascular side effect. The present disclosure also provides for methods for treating prostate cancer in a patient with a history of at least one cardiovascular event, wherein administration of degarelix to the subject decreases the likelihood of developing or experiencing an additional cardiovascular event compared to treatment with a gonadotrophin releasing hormone (GnRH) agonist.

The invention discloses a Prinsepia utilis Royle oil-containing functional skin care product and a preparation method thereof. The Prinsepia utilis Royle oil-containing functional skin care product is prepared from the following raw materials in part by weight: 1 to 2 parts of Prinsepia utilis Royle oil, 10 to 25 parts of purslane extracting solution, 5 parts of glycerol, 2 to 3 parts of 1,2-pentanediol, 5 to 7 parts of caprylic / caprictriglycerides, 2 parts of synthetic squalane, 1 to 5 parts of tocopheryl acetate, 1 to 3 parts of cetearyl alcohol, 0.1 to 0.2 part of allantoin, 0.6 to 0.9 part of coconut oil-base glucoside, 0.5 to 1 part of coconut oil alcohol, 0.5 to 2 parts of glyceryl stearate, 0.1 to 1 part of sodium hyaluronate and the balance of water. The functional skin care product has mild property and high safety without toxic or side reaction and anaphylactic reaction, can repair the destructed skin barrier, resists inflammation and skin ageing, and has a good effect and high safety of assisting in treating skin diseases related with skin barrier destruction, such as facial dermatitis (hormone dependence dermatitis, allergic dermatitis and acne), atopic dermatitis and the like.

The invention is a functional skin care product containing purslane extractive. Raw materials of the functional skin care product include, by weight, 10 parts of purslane extractive, 1-2 parts of Prinsepia utilis rogle oil, 2-5 parts of glycerol, 0.3-0.5 parts of crylic acid (ester) / C10-30 alkanol acrylate cross-linked polymer, 2-3 parts of 1,2-pentanediol, 1-5 parts of synthesized squalane, 1-2 parts of tocopheryl acetate, 2-3 parts of cetostearyl alcohol, 0.1-0.2 part of allantoin, 0.3-0.8 part of sodium hyaluronate, 3-5 parts of Butyrospermum parkii butter, and 100 parts of deionized water. Or the Prinsepia utilis rogle oil and the Butyrospermum parkii butter are not added. By the aid of animal experiments, namely, mouse auricle swelling models due to dimethlbenzene, the functional skin care product containing purslane extractive is fine in anti-inflammation and anti-allergy effects, mild in nature and fine in safety, and is free of toxic reaction and anaphylaxis. The functional skin care product has an adjuvant therapy function to skin barrier recovery of common discosmetic dermatosis such as hormone dependent dermatitis and acne, and is fine in curative effect and safety.

A compound of formula (I) 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 (A) wherein R5 is hydrogen of 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 invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and / or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.

The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, and magnesium stearate; or can contain microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, povidone, and magnesium stearate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and / or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefore Additional uses include stimulation of food intake.

The present invention relates to a method of treating prostate cancer with androgen deprivation therapy and an insulin-like growth factor receptor (IGF-IR) antagonist. Although the response rate of prostate cancer to androgen deprivation therapy (ADT) is high, surviving cancer cells invariably become androgen independent (AI) and tumor growth follows. The invention inhibits or delays transition of androgen dependent cancer to androgen independent cancer, significantly decreases risk of recurrence, and improves treatment outcome.

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 the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor, an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estrogen levels. This results in enhanced clinical efficacy and reduced side effects.

This invention relates to new use of dual NK-1 / NK-3 receptor antagonists or a pharmaceutically acceptable salt thereof in the treatment of sex-hormone dependent diseases.

The present invention relates to the field of cancer, and in particular hormone dependent cancers including, but not limited to prostate, breast, endometrial, ovarian, thyroid, bone, and testis. The present invention also relates to the use of steroid analogues, and in particular analogues of Δ5-androstene-3-β, 17α-diol, and its epimer Δ5-androstene-3-β, 17β-diol for the treatment and prevention of cancer.

The present invention is preparation process and antitumor effect of N(1)-alkyl-3'-oximino indirubin derivative (I, JN-2528). The new synthesis process uses indirubin as initial material, and under the action of alkaline compound as promoter, indirubin is reacted directly with halohydrocarbon or other halide to obtain N(1)-alkyl indirubin derivative, which is then reacted with hydroxylamine to obtain N(1)-alkyl-3'-oximino indirubin derivative. The MTT and SRB process and transplanting C57 mouse Lewis lung cancer mold test proves the antitumor activity of N(1)-alkyl-3'-oximino indirubin. The compound shows extracorporeal and intracorporeal cancer inhibiting effect.

The invention provides a method of treating and / or preventing a toxicity associated with epidermal growth factor receptor (EGFR) inhibitor therapy in a subject, the method comprising administering to the subject an effective amount of a steroid sulfatase (STS) inhibitor. The toxicity may be ocular toxicity; or dermatologic toxicity, such as papulopustular rash. The EGFR inhibitor may be selected from the group consisting of: a small molecule; an antibody or derivative or fragment thereof; another agent that targets the extracellular or intracellular domain of the EGFR, such as a tyrosine kinase inhibitor selected from the group consisting of: erlotinib; gefitinib; lapatinib; and any combination thereof. The EGFR inhibitor may also be antibody selected from the group consisting of: cetuximab; panitumumab; and any combination thereof.Preferably the STS inhibitor is selected from the group consisting of: alternative STS substrates; reversible STS inhibitors; and irreversible STS inhibitors; and any combination thereof. A preferred STS inhibitor is the irreversible nonsteroidal STS inhibitor STX64.In some embodiments, the subject receiving EGFRI therapy has a cancer comprising cells that express wildtype k-ras and / or wildtype b-raf. In other embodiments, the cancer may be hormone-dependent. Cancers that may be treated with EGFRI therapy include colorectal cancer and non-small cell lung cancer.

A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.

A method of inhibiting the growth of hormone dependent tumor cells in a mammal comprises administering to said mammal an insulin-like growth factor receptor (IGF-IR) recombinant antibody, wherein said antibody can be a single-chain recombinant antibody, which can be humanized, capable of blocking agonist interaction with the IGF-IR.