31 results about "Anti estrogenic" patented technology

Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.

Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.

The present invention provides methods for treating and preventing gynecomastia by administering 4-hydroxy tamoxifen to a patient. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with gynecomastia, this reduces the effective estrogen-androgen ratio in the breast tissue, thereby reducing ductal proliferation, epithelial and stromal hyperplasia, and pain. In patients at risk for developing gynecomastia, 4-hydroxy tamoxifen's anti-estrogenic effect prevents tissue proliferation and its accompanying pain.

Pharmaceutical compositions of 4-hydroxy tamoxifen, particularly compositions suitable for percutaneous administration, are useful in methods for treating and preventing breast cancer. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with breast cancer, this effect reduces tumor tissue proliferation. In patients at risk for developing breast cancer, the anti-estrogenic effect prevents breast tumor formation.

The present disclosure provides a compound of Formula I:or a pharmaceutically acceptable salt wherein X, R1-R8, Y1-Y5, m, n, p, and q are defined herein. The novel 2H-chromene compounds are useful for the modulation of disorders mediated by estrogen, and other disorders, as described herein. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions.

The present invention relates to a transgenic fish having at least one genomically integrated expression cassette containing a 5′-regulatory nucleotide sequence responsive to hormones, particularly estrogenic hormones, connected in a functional manner upstream of a nucleotide sequence encoding a reporter protein. The present invention further relates to methods of using the transgenic fish for various purposes, including, for example: (1) identifying estrogenic endocrine disruptors; (2) monitoring estrogen-like activity of test samples; (3) identifying anti-estrogenic endocrine disruptors; and (4) investigating the effects of endocrine disruptors on liver regeneration. Expression cassettes, host cells, and transgenic cells of aquatic animals are also disclosed.

The present invention relates to the treatment of a woman for endometriosis comprising the administration of IFN-gamma, a cytokine antagonist and / or an anti-estrogenic agent.

Syntheses of steroids such as 3-hydroxy-7α-methyl-21-[2′-methoxy-4′-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.

The invention discloses novel application of Gypensapogenin B in medicament for treating osteoporosis. Osteoporosis is one of vital diseases which are harmful to human health, and the number of patients with osteoporosis is increased progressively along with aging of population, which brings huge social, medical and economical burden to the whole world. Although home and abroad related experts and scholars pay attention to prevention and treatment of osteoporosis, an effective treatment medicament to the disease does not exist. In vivo tests discover that the Gypensapogenin B has remarkable effect in resisting osteoporosis. Experiment results indicate that the Gypensapogenin B can inhibit strengthening of bone conversion caused by ovariectomized, so that bone is less destroyed, the blood calcium concentration can be improved, and bone deposition are favored. The Gypensapogenin B has treatment effect on osteoporosis caused by anti-estrogenic deficiency, and does not have estrogen-like side effect.

The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and / or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.

The invention relates to application of clomifene citrate to anti-mycobacterium tuberculosis medicines. Clomifene citrate has estrogenic and antiestrogenic properties that appear to prevent the release of gonadotropins, follicle-stimulating hormone and luteinizing hormone, thus leading to follicular development and maturation, ovulation and subsequent corpus luteum development and function and then resulting in pregnancy. It is found through researches that the clomifene citrate has an antitubercular effect and has good development value. The application of the clomifene citrate to anti-mycobacterium tuberculosis medicines and the obvious anti-mycobacterium tuberculosis effect of the clomifene citrate are disclosed for the first time.

The present invention provides methods for treating and preventing benign breast disease by administering 4-hydroxy tamoxifen to a patient. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with benign breast disease, this effect induces disease regression. In patients at risk for developing breast cancer, the anti-estrogenic effect prevents formation of benign breast conditions that can lead to cancer.

The invention discloses a new use of Gypensapogenin A in preventing and curing osteoporosis. The osteoporosis is one of important diseases harming human health. With the ageing of population, patients suffering from the osteoporosis are increasingly, and thus, huge social, medical and economic burdens are brought to the whole world. Although related experts and scholars at home and abroad attach high importance to the prevention and cure of the osteoporosis, effective therapeutic drugs for treating the osteoporosis are lacking. Discovered by in vivo tests, the Gypensapogenin A disclosed by the invention is remarkable in effect of resisting the osteoporosis. Shown by test results, the Gypensapogenin A is capable of remarkably inhibiting bone transformation rate enhancement caused by ovariectomy, reducing bone destruction, and meanwhile, is capable of improving blood calcium concentration, and thereby, the improvement of the blood calcium concentration is in favor of bone deposition. The Gypensapogenin A has a therapeutic effect on the osteoporosis caused by the estrogen deficiency, and has no estrogen-like side effects.

The invention discloses a medicine for treating hysteromyoma and a preparation method thereof. The medicine is characterized in that the effective component of the medicine composition is glycyrrhetinic acid. The invention relates to the medicine for treating hysteromyoma and the preparation method thereof. It is creatively found that glycyrrhetinic acid can effectively inhibit hysteromyoma, and specifically, treatment is achieved through the anti-estrogenic function of glycyrrhetinic acid. Other normal tissue and cells are protected to the largest extent while hysteromyoma is inhibited, and side effects of glycyrrhetinic acid are small.

The invention discloses an oral medication for treating diseases including hysteromyoma, its preparation process and application, the medicament is prepared from traditional Chinese medicinal raw materials including rhubarb horsetails, wood louse, leeches, peach kernels, cattail pollen. The preparation comprises the steps of refining through stepwise grilling, then charging different pharmaceutically acceptable excipients. The medicament has the actions of resisting estrogenic hormones, anti-inflammatory and haemostasis, it also has function of immunological enhancement and improvement.

Anti-hormonal (anti-estrogenic steroid) therapy and immunotherapy are used in combination to treat breast cancer. The preferred immunotherapeutic agent is an immunogen, preferably comprising sialyl-Tn, and more preferably is a sialyl-Tn / KLH conjugate.

The invention relates to an application of prawnella in treatment or prevention of osteoporosis. The P.histicola bacteria are used as symbiotic bacteria in normal human intestinal tracts and have excellent safety, animal experiments on estrogen-deficient mice find that the P.histacola can be used for preventing bone mass loss of the mice; the imbalance of intestinal flora caused by estrogen deficiency is regulated, the expression of inflammatory factors is inhibited, the intestinal permeability increase caused by estrogen deficiency is reduced, then inflammatory factors in the intestinal tractwall are reduced, differentiation, maturation and activation of osteoclasts guided by RANKL are inhibited; the P.histacola bacteria have effects of osteoporosis resistance, bone absorption reducing,bone mass loss inhibition and estrogen deficiency osteoporosis resistance, and can meet the requirements of long-term taking, economy, safety and no side effect required by osteoporosis prevention andtreatment as the micro-ecological preparation.

The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1):in whichR1 represents a hydrogen atom, etc.,R2 represents a C1–C7 halogenoalkyl group, etc.,m represents an integer of 2 to 14, andn represents an integer of 2 to 7,or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

The present invention primarily relates to specific uses of a composition containing a roasted extract and xanthohumol for health-promoting purposes. In particular, the invention relates to a composition, preferably pharmaceutical composition, comprising xanthohumol (XN), preferably in a therapeutically effective amount, for (i) use in the treatment and / or prevention of cancer, and / or (ii) use in the treatment and / or prevention of osteoporosis, and / or (iii) use in the treatment and / or prevention of metabolic syndrome, and / or (iv) use in the treatment and / or prevention of diabetes, and / or (v) use in the treatment and / or prevention of cardiovascular disease(s), and / or (vi) use as anti-oxidant, and / or (vii) use as detoxifying agent, and / or (viii) inhibiting metabolic activation of procarcinogens, and / or (ix) use as anti-mutagenic and / or anti-genotoxic agent, and / or (x) use as anti-estrogenic and / or estrogenic agent, and / or (xi) inducing apoptosis, and / or (xii) use as anti-angiogenetic agent, and / or (xiii) use as anti-inflammatory agent, and / or (xiv) inhibiting NF-κB, and / or (xv) use in the treatment and / or prevention of infection(s), in particular, use as antimicrobial agent, wherein the composition comprises or consists of (a) a roasted extract and (b) XN, preferably a hop extract comprising XN, and / or wherein the composition is obtainable or obtained by mixing (a) a roasted extract and (b) XN or, preferably, a hop extract comprising XN.

The present invention primarily relates to specific uses of a composition containing a roasted extract and xanthohumol for health-promoting purposes. In particular, the invention relates to a composition, preferably pharmaceutical composition, comprising xanthohumol (XN), preferably in a therapeutically effective amount, for (i) use in the treatment and / or prevention of cancer, and / or (ii) use in the treatment and / or prevention of osteoporosis, and / or (iii) use in the treatment and / or prevention of metabolic syndrome, and / or (iv) use in the treatment and / or prevention of diabetes, and / or (v) use in the treatment and / or prevention of cardiovascular disease(s), and / or (vi) use as anti-oxidant, and / or (vii) use as detoxifying agent, and / or (viii) inhibiting metabolic activation of procarcinogenes, and / or (ix) use as anti-mutagenic and / or anti-genotoxic agent, and / or (x) use as anti-estrogenic and / or estrogenic agent, and / or (xi) inducing apoptosis, and / or (xii) use as anti-angiogenetic agent, and / or (xiii) use as anti-inflammatory agent, and / or (xiv) inhibiting NF-kappaBeta, and / or (xv) use in the treatment and / or prevention of infection(s), in particular, use as antimicrobial agent, wherein the composition comprises or consists of (a) a roasted extract and (b) XN, preferably a hop extract comprising XN, and / or wherein the composition is obtainable or obtained by mixing (a) a roasted extract and (b) XN or, preferably, a hop extract comprising XN.