50 results about "Hormone sensitivity" patented technology

Anthranilic acid drivatives, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.

Fused tricyclic compounds, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.

Fused heterotricyclic compounds, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.

It has now been determined that antisense therapy which reduces the expression of TRPM-2 provides therapeutic benefits in the treatment of cancer. In particular, such antisense therapy can be applied in treatment of prostate cancer and renal cell cancer. Addition of antisense TRPM-2 ODN to prostatic tumor cells in vivo is effective for delaying the onset of androgen independence. Thus, prostate cancer can be treated in an individual suffering from prostate cancer by initiating androgen-withdrawal to induce apoptotic cell death of prostatic tumor cells in the individual, and administering to the individual a composition effective to inhibit expression of TRPM-2 by the tumor cells, thereby delaying the progression of prostatic tumor cells to an androgen-independent state in an individual Combined use of antisense TRPM-2 and taxanes synergistically enhances cytotoxic chemosensitivity of androgen-independent prostate cancer. In addition, it has also been found that antisense TRPM-2 has beneficial effect for other cancer types. Specifically, antisense TRPM-2 ODN enhances chemosensitivity in human Renal cell cancer, a normally chemoresistant disease with no active chemotherapeutic agent having an objective response rate higher than 10%. Radiation sensitivity is also enhanced when cells expressing TRPM-2 are treated with antisense TRPM-2 ODN. Thus, the antisense TRPM-2 ODNs can be used to enhance hormone sensitivity, chemosensitivity and radiation sensitivity of a variety of cancer types in which expression of TRPM-2 has been observed.

The present invention provides an androgen receptor antagonistic agent and a superior prophylactic or therapeutic agent for hormone-sensitive cancer, which contain a compound of the formula: wherein, R1 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R2 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R3 is a hydrogen atom, a hydrocarbon group which may have substituent(s), an acyl group or a heterocyclic group which may have substituent(s), R4 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, and R5 is a cyclic group which may have substituent(s); or a salt thereof, or its prodrug.

The invention provides novel compounds having the general formula (I)wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compounds inhibit hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, and obesity.

Use of compounds to inhibit hormone-sensitive lipase, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, method of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and / or prevention of a range of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Novel substituted piperidine carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and / or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and / or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

The present invention relates to novel 11-beta estradiol ester compounds and their use as locally active estrogens in the treatment of the symptomology of menopause and to treat estrogen sensitive cancers, including breast cancer.

A method of producing a phytomedicinal therapeutic for the prevention and control of a disease selected from the group consisting of obesity, cardiovascular disease, and diabetes, and conditions related thereto is provided which comprises extracting peanut shells with a solvent, removing a substantial portion of the solvent to produce a concentrated extract. Phytomedicinal compositions are provided that comprise an effective amount of at least one coumarin compound or one coumarin derivative derived from plant material that modulates a biological activity of at least one enzyme selected from the group consisting of Pancreatic Lipase (PL), Lipoprotein Lipase (LPL), and Hormone-Sensitive Lipase (HSL). Phytomedicinal compositions are provided that comprise at least an effective amount of coumarin derivatives (6,7-dihydroxycoumarin-esculetin, and esculetin-like compounds). A method for the prevention and / or treatment of treatment of a condition selected from the group consisting of obesity, cardiovascular disease, and diabetes, is provided which comprises administering a composition comprising an effective amount of at least one coumarin derivative, including 6,7-dihydroxycoumarin (esculetin), derived from plant material that modulates a biological activity of at least one enzyme selected from the group consisting of Pancreatic Lipase (PL), Lipoprotein Lipase (LPL), and Hormone-Sensitive Lipase (HSL).

The invention belongs to the field of medicine preparation, and in particular relates to an application of berberine in preparing medicines for treating obesity and type-2 diabetes, medicines for suppressing fat cell differentiation and medicines for prompting phosphodiesterase activity. According to the application, a 3T3-L1 fat cell is taken as a research target, the experiment result shows that the berberine can suppress 3T3-L1 fat cell differentiation, and particularly when the berberine concentration is 10micon mol / L, the fat cell differentiation can be completely suppressed; the berberine can reduce expression of fat cell transcription factors such as C / EBPalpha, PPARgamma and the like by activating AMPK (Adenosine Monophosphate Activated Protein Kinase), and suppress the differentiation of the fat cell; and the berberine can increase the degradation of cAMP in cells and reduce the phosphorylation level of HSL (Hormone Sensitive Lipase) by reducing the suppression to PED activity so as to achieve the function of steatolysis prevention. The preparation provides experimental data and theoretic basis for treating of type-2 diabetes and obesity patients by using the berberine more reasonably in clinic.

It has now been determined that antisense therapy which reduces the expression of TRPM-2 provides therapeutic benefits in the treatment of cancer. In particular, such antisense therapy can be applied in treatment of prostate cancer and renal cell cancer. Addition of antisense TRPM-2 ODN to prostatic tumor cells in vivo is effective for delaying the onset of androgen independence. Thus, prostate cancer can be treated in an individual suffering from prostate cancer by initiating androgen-withdrawal to induce apoptotic cell death of prostatic tumor cells in the individual, and administering to the individual a composition effective to inhibit expression of TRPM-2 by the tumor cells, thereby delaying the progression of prostatic tumor cells to an androgen-independent state in an individual Combined use of antisense TRPM-2 and taxanes synergistically enhances cytotoxic chemosensitivity of androgen-independent prostate cancer. In addition, it has also been found that antisense TRPM-2 has beneficial effect for other cancer types. Specifically, antisense TRPM-2 ODN enhances chemosensitivity in human Renal cell cancer, a normally chemoresistant disease with no active chemotherapeutic agent having an objective response rate higher than 10%. Radiation sensitivity is also enhanced when cells expressing TRPM-2 are treated with antisense TRPM-2 ODN. Thus, the antisense TRPM-2 ODNs can be used to enhance hormone sensitivity, chemosensitivity and radiation sensitivity of a variety of cancer types in which expression of TRPM-2 has been observed.

The invention provides a method for controlling anaerobic ammonia oxidized granular sludge in a high-load reactor to float, and belongs to the field of waste water treatment. In the days from 0 to 20days, namely the early stage of a high-load operation state, a mixed solution, with a certain concentration, of two kinds of AHLs (N-acyl-homoserinelactones) signal molecules is added into the external source of feed water of the reactor everyday, and the AHLs signal molecules are not added any longer after the early stage; and the AHLs signal molecules are C8-HSL (hormone-sensitive lipase) and C6-HSL. The method can control running off caused by floating of granular sludge in the high-load anaerobic ammonia oxidation reactor as well as improve the activity of the granular sludge, so that thehigh-load reactor can maintain stable and higher denitrification efficiency.

The present invention relates to a method of treating or preventing estrogen-sensitive tumours in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula 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. The estrogenic component according to the invention does not have undesirable proliferative effects on breast and / or endometrial tissue and displays sufficient estrogenicity to prevent that its administration will lead to hypoestrogenism and / or climacteric complaints.

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and / or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and / or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

The invention provides novel compounds having the general formula (I)wherein R1, R2 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) for the treatment of diabetes, metabolic syndrome and obesity.

The invention discloses an application of dibutyacyladenosine cyclophosphate salts in the preparation of fat-reducing diet drugs for external use. Dibutyacyladenosine cyclophosphate salts can directly enter fat cells and activate PKA proteins, and thus hormone sensitive lipase (HSL) is activated to catalyze fat decomposition to generate free fatty acid and glycerin. At the same time, the destructive effect of phosphodiesterase is prevented, and compared with those of cAMP, the action time is longer, and the effect is quicker.

The present invention discloses compounds that are inhibitors of hormone-sensitive lipase. The present invention also discloses the use of the compounds and derivatives to inhibit hormone-sensitive lipase, various pharmaceutical compositions including the compounds, and methods of treatment using these compounds and compositions.

A Salacia composition described herein significantly reduces appetite, activates Hormone Sensitive Lipase, and manages a healthy lipid profile through inhibition of HMG-CoA Reductase enzyme. Salacia compositions described herein include of at least 12% of polyphenols, 2% of mangiferin and 1% of 25, 26-oxidofriedelane-l, 3-dione by weight of the composition in the form of extract. The composition is obtained by continuous solvent extraction, employing non-aqueous food grade solvents. Salacia compositions herein reduce appetite by about 18% of routine diet, when effective amounts are administered to a subject in need thereof. Effective management of a healthy lipid profile is thus possible with synergistic combination of reduction in energy intake, activation of Hormone Sensitive Lipase, and inhibition of HMG-CoA Reductase enzyme responsible for cholesterol metabolism.

Disclosed are fused tricyclic compounds of the following formula I,or an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof. The disclosed compounds are useful as inhibitors of 17β-hydroxysteriod dehydrogenase 3 (17βHSD3). Also disclosed are methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer and pharmaceutical compositions comprising such compounds.

The invention provides novel compounds having the general formula (I)wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compounds inhibit hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, and obesity.

The invention discloses a weight-reducing health-care product, which is composed of the following raw materials in parts by weight: 2-4 parts of broadleaf holly leaf, 2-4 parts of hawthorn, 5-7 parts of lotus leaf, 1-3 parts of Chinese wolfberry, 2-4 parts of mango and 1-5 parts of betel palm. In the weight-reducing health-care product disclosed by the invention, the medicine and food homologous pure natural plants of broadleaf holly leaf, hawthorn, lotus leaf, Chinese wolfberry, mango and betel palm are adopted, and the active ingredients in the pure natural plants are utilized, thus the activity of metabolizing enzyme in a human body is adjusted, the induction of noradrenalin to the decomposition of fat in lipocyte is enhanced, the activity of hormone-sensitive lipase is promoted, and oxidative decomposition of in-vivo fat tissues can be accelerated. Therefore, the weight-reducing health-care product has a good weight-reducing curative effect, durable and stable action and no adverse effect, is beneficial for health of the human body after long-term administration, and is a very perfect weight-reducing health-care product.

The present invention relates to the intron and exon structure of the gene encoding .beta.3 adrenergic receptor polypeptides of mouse and human origin, which polypeptides are useful in a procedure for studying the effects of various chemical agents on the .beta.3 adrenergic receptor coupled to adenylate cyclase and hormone-sensitive lipases.

Novel substituted p-phenyl carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and / or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and / or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

The invention relates to the use of cell free nucleosome bound nuclear hormone receptor variant adducts for detecting the progression of hormone dependent disease to hormone therapy resistant disease or the effectiveness of a drug treatment in a patient. The invention also relates to methods for detecting said cell free nucleosome bound nuclear hormone receptor variant adducts.

The invention provides novel compounds having the general formula (I)wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.

The invention provides a new energy material for motor vehicles, and applications thereof. The preparation method comprises: weighing 800-1000 g of animal leaf fat, chopping, dissolving in 3000-5000 mL of a buffer solution, adding 3-5 g of hormone-sensitive lipase of the animal, carrying out a hydrolysis reaction for 12-24 h at a temperature of 35-38 DEG C to obtain a reaction product containing fatty acids and glycerol, carrying out centrifugation, removing the water phase, and cooling to a room temperature so as to obtain the product. According to the present invention, during the use, the new energy material can be matched with a certain catalyst or an igniter so as to be used as the energy of motor vehicles such as automobiles, tractors and the like; by using the animal leaf fat as theraw material, such that the source of the raw material is wide; the new energy material has advantages complete combustion, cleaning and environment protection; and the preparation method is simple and easy to perform, and the cost is greatly reduced.