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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 6482. Отображено 100.
17-05-2012 дата публикации

Pharmaceutical composition for transdermal or transmucous administration

Номер: US20120122829A1
Принадлежит: BESINS Healthcare Luxembourg SARL

The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition.

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09-08-2012 дата публикации

Methods and devices for the sustained release of multiple drugs

Номер: US20120202742A1

The invention relates to an drug delivery device and a method for delivering multiple drugs over a prolonged period of time. The drug delivery device has two or more unitary segments comprising a drug-permeable polymeric substance, wherein at least one of the segments further comprises a pharmaceutically active agent. The invention also relates to a method for the treatment of a benign ovarian secretory disorder in a female mammal, a method of contraception, and a method of relieving the symptoms associated with menopausal, perimenopausal and post-menopausal periods in a woman.

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23-08-2012 дата публикации

Modified L-Nucleic Acid

Номер: US20120214868A1
Принадлежит: NOXXON PHARMA AG

A modified L-nucleic acid, containing an L-nucleic acid part conjugated to a non-L-nucleic acid part is described. The conjugate has extended retention time in and demonstrates a delayed elimination from an organism.

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01-11-2012 дата публикации

Chroman-derived anti-androgens for treatment of androgen mediated disorders

Номер: US20120277301A1
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Methods for the prevention and/or alleviation of androgen-mediated disorders treatable by administering a chroman-derived anti-androgen compound are provided by the present invention. The invention further provides pharmaceutical and nutraceutical compositions containing chroman-derived anti-androgen compounds useful in the prevention and/or alleviation of androgen-mediated disorders, particularly prostate cancer.

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01-11-2012 дата публикации

Cell surface coating with hyaluronic acid oligomer derivative

Номер: US20120277416A1
Принадлежит: Kode Biotech Ltd

A method of localising reproduction assisting hyaluronic acid to reproductive cell surfaces by covalently linking it to lipids is disclosed.

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22-11-2012 дата публикации

Sustained-release composition and process for producing the same

Номер: US20120295848A1
Принадлежит: Takeda Pharmaceutical Co Ltd

Present invention is to provide a sustained-release composition which contains a physiologically active substance in high content even when gelatin is not included, and suppresses its initial excessive release and, thus, can achieve a stable release rate over about one month. A sustained-release composition containing a lactic acid-glycolic acid polymer having a ratio or weight average molecular weight and number average molecular weight of about 1.90 or lower, or a salt thereof, and a physiologically active substance.

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24-01-2013 дата публикации

Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same

Номер: US20130022674A1
Принадлежит: Clarus Therapeutics Inc

A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

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21-02-2013 дата публикации

Steroid hormone delivery systems and methods of preparing the same

Номер: US20130045271A1
Принадлежит: MONOSOL RX LLC

The present invention is directed to steroid hormone delivery systems and methods of preparing the same. In particular, the steroid hormone delivery systems provided include a primary construct having one or more hydrophobic steroid hormone esters in the form of a liposome, a lipid particle, a micelle, an emulsion or a niosome which is then formulated into a secondary construct for administration. Exemplary secondary constructs include a film for sublingual or buccal administration.

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28-02-2013 дата публикации

Therapeutic Regimens

Номер: US20130053448A1
Принадлежит: Individual

This invention relates to clinically useful therapeutic regimens comprising the administration of (R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol.

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14-03-2013 дата публикации

Methods and compositions for treating prostate cancer

Номер: US20130064821A1
Принадлежит: Individual

A polypeptide comprising an androgen binding region, the androgen binding region capable of binding to an androgen at a sufficient affinity or avidity such that upon administration of the polypeptide to a mammalian subject the level of biologically available androgen is decreased. Specifically disclosed is an AR IgG1 Fc fusion protein, comprising the androgen binding domain of human androgen receptor and the Fc region of IgG. This fusion protein is used in the treatment of prostate cancer and testosterone flare.

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01-08-2013 дата публикации

Antagonist for mutant androgen receptor

Номер: US20130197009A1
Принадлежит: Astellas Pharma Inc

[Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation [Means for Solution] The present inventors conducted thorough research on mutant androgen-related diseases for which the traditional anti-androgen drugs become ineffective. As a result, they found that the compound, which is an active ingredient of the pharmaceutical composition of the present invention, exhibits an inhibitory action against transcriptional activation in a human mutant androgen receptor (AR), and has an excellent antitumor action in a human prostate cancer-bearing mouse, thereby completing the present invention. Accordingly, the compound, which is an active ingredient of the pharmaceutical composition of the present invention, is useful for a series of androgen receptor-related diseases including prostate cancer.

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22-08-2013 дата публикации

Novel treatment of prostate carcinoma

Номер: US20130219528A1
Автор: Per Borgstrom
Принадлежит: Pellficure Pharmaceuticals Inc

Disclosed herein are naphthoquinone analogs, such as plumbagin, pharmaceutical compositions that include naphthoquinone analogs, such as plumbagin, and methods of treating diseases and/or conditions such as cancer with naphthoquinone analogs, such as plumbagin. Also included are combination therapies wherein a naphthoquinone analog, such as plumbagin, and a hormone therapy agent are provided to a subject suffering from a condition such as cancer.

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28-11-2013 дата публикации

Transdermal delivery system for hormones and steroids

Номер: US20130317462A1
Принадлежит: Acrux DDS Pty Ltd

A transdermal delivery system comprising a composition comprising a pharmacological agent and a penetration enhancer wherein the penetration enhancer comprises polyethylene glycol (PEG) of average molecular weight no more than 300.

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26-12-2013 дата публикации

Substituted morpholines as modulators for the calcium sensing receptor

Номер: US20130345213A1
Принадлежит: Lupin Ltd

Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).

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27-02-2014 дата публикации

Anti-androgenic agent, sebum secretion blocker, hair growth stimulant, and food or beverage

Номер: US20140057840A1
Принадлежит: Lotte Corp

Provision of an anti-androgenic agent which has a strong anti-androgenic action, is free of side effects and very safe, and a sebum secretion blocker and a hair growth stimulant containing the anti-androgenic agent as an active ingredient. Provided are the anti-androgenic agent comprising lactoferrin, the sebum secretion blocker containing the anti-androgenic agent as an active ingredient, the hair growth stimulant containing the anti-androgenic agent as an active ingredient, and a food or drink product comprising the anti-androgenic agent containing lactoferrin as an active ingredient.

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06-03-2014 дата публикации

Methods and Compounds for Vitamin D Therapy

Номер: US20140066415A1
Принадлежит: Opko IP Holdings II Inc

Methods and compositions comprising 1,25-dihydroxyvitamin D 2 are disclosed. A method for lowering or maintaining lowered serum parathyroid hormone in human patients including administering to said patients an effective amount of 1,25-dihydroxyvitamin D 2 to lower or maintain lowered serum parathyroid hormone levels is disclosed. Dosage forms and dosing regimens are also disclosed.

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20-03-2014 дата публикации

Methods and compositions for increasing sex steroids and growth hormones

Номер: US20140079829A1
Принадлежит: Basic Research LLC

Embodiments of the invention generally relate to methods and supplements for increasing sex steroids and human growth hormone in a human being.

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10-04-2014 дата публикации

Natural combination hormone replacement formulations and therapies

Номер: US20140100205A1
Принадлежит: TherapeuticsMD Inc

Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.

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06-01-2022 дата публикации

Composition comprising elderberry extract as effective component for preventing, treating, or alleviating andropause syndrome

Номер: US20220000954A1
Автор: Hyun Seok Kong
Принадлежит: Kosa Bio Inc

The present invention relates to a composition comprising an elderberry extract as an effective component for preventing, treating, or alleviating andropause syndrome, wherein the elderberry extract of the present invention increases testosterone secretion in sperm cells and andropause syndrome animal models, and thus can be usefully employed as a pharmaceutical or food composition for preventing, treating or alleviating andropause syndrome.

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06-01-2022 дата публикации

COMPOSITION FOR ALLEVIATING SYMPTOMS OF ANDROPAUSE, CONTAINING EXTRACT OF FICUS AURICULATA LOUR. AS ACTIVE INGREDIENT

Номер: US20220000957A1
Принадлежит:

The present invention relates to a pharmaceutical composition, food composition, and food additive for preventing or alleviating symptoms of andropause containing extract of Lour. as an active ingredient. 1Ficus auriculata. Pharmaceutical composition for preventing or alleviating symptoms of andropause containing extract of Lour. as an active ingredient2Ficus auriculata. The pharmaceutical composition of claim 1 , wherein the extract is a fruit extract of Lour.3. The pharmaceutical composition of claim 1 , wherein the symptoms of andropause is one or more selected from the group consisting of lower urinary tract symptoms claim 1 , BPH claim 1 , prostatitis claim 1 , nervousness claim 1 , emotional anxiety claim 1 , depression claim 1 , hot flashes claim 1 , sleep disorders claim 1 , decreased vitality claim 1 , reduced work ability claim 1 , erectile dysfunction claim 1 , and alopecia.4. The pharmaceutical composition of claim 1 , wherein the extract is the hot water extract or ethanol extract5. The pharmaceutical composition of claim 1 , wherein the symptoms of andropause is caused by activation of PDE5 claim 1 , androgen receptor expression claim 1 , or PSA (Prostate specific antigen) expression.6Ficus auriculata. Food composition for alleviating symptoms of andropause containing extract of Lour. as an active ingredient7. The food composition of claim 6 , wherein the extract is a hot water extract or an ethanol extract. The present invention relates to a composition for alleviating symptoms of andropause, and more particularly, to a pharmaceutical, food and food additive composition for alleviating symptoms of andropause containing extract of Lour. as an active ingredient.As interest in the development of medical technology and health maintenance increases, the average life expectancy is gradually increasing, and the proportion of the population of the elderly is rapidly increasing for various social reasons. As society is aging, problems with the health of the ...

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13-01-2022 дата публикации

1-PHENYL-2-PHENYLETHANE DERIVATIVE

Номер: US20220009869A1
Принадлежит: KAO CORPORATION

Provided is a novel compound having a selective activating effect on ERβ. The present invention provides a compound represented by the following formula (1) wherein Rrepresents a cycloalkyl group having 3 to 8 carbon atoms, an alkenyl group having 2 to 6 carbon atoms and optionally substituted with a halogen atom, a 5-membered nitrogen-containing heteroaryl group, a 4- to 6-membered cyclic amino group, an alkanoylamino group having 2 to 6 carbon atoms and optionally substituted with a halogen atom, a 1-trifluoromethyl-1-hydroxymethyl group, or a 1-methylpropyl group; Rto Rare the same or different and each represent a hydrogen atom or a fluorine atom; and Rrepresents a hydrogen atom or an alkanoyl group having 2 to 5 carbon atoms, or a salt thereof. 2: An ERβ activating agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.3: A skin aging preventing or ameliorating agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.4: A sebum secretion inhibiting agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.5: An acne preventing or ameliorating agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.6: A hot flash preventing or ameliorating agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.7: A prostatic hyperplasia preventing or ameliorating agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.8: An androgen activation inhibiting agent comprising the compound represented by the formula (1) or the salt thereof according to as an active ingredient.932-. (canceled) The present invention relates to a compound having high selectivity for estrogen receptor 0.Estrogen, also called follicle hormone ...

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14-01-2021 дата публикации

Fixed Dose Oral Testosterone Undecanoate Compositions and Use Thereof

Номер: US20210007978A1
Принадлежит: LIPOCINE INC.

Disclosed are effective fixed dose oral testosterone undecanoate compositions for use in regimens without dose titration and methods for treatment of patients in need of testosterone replacement therapy. Also disclosed are criteria for continuation and discontinuation of such regimens, based on single serum T concentration levels measured at a steady state at predetermined times after initiation of said regimen and at a predetermined number of hours after administration of a morning dose of the regimen. 1. A Testosterone Undecanoate (TU) pharmaceutical composition for restoring an effective amount of T concentration in a hypogonadal male subject in response to a fixed dose oral administration therapy regimen thereof , wherein said composition includes a continuation criteria comprising a single serum T concentration level measured at a steady state a 3 to 4 weeks after initiation of said regimen and 8 to 9 hours after administering a morning dose of said regimen , wherein if said single serum T measured concentration level is within a range of 300 ng/dL to 1080 ng/dL , said regimen is continued , and wherein if said single serum T concentration level is not within a range of 300 ng/dL to 1080 ng/dL , said regimen is discontinued.2. The composition of claim 1 , wherein said regimen comprises a daily administration of 450 mg of TU.3. The composition of claim 3 , wherein said regimen comprises a twice daily administration of 225 mg of TU.4. The composition of claim 4 , wherein said 225 mg of TU comprises two capsules claim 4 , and wherein each capsule comprises 112.5 mg of TU.5. The composition of claim 1 , wherein said regimen comprises administration of said composition with food.6. The composition of claim 1 , wherein said subject has a testosterone concentration below at least one of 300 ng/dL claim 1 , 250 ng/dL claim 1 , 200 ng/dL claim 1 , 150 ng/dL claim 1 , and 100 ng/dL claim 1 , and wherein in response to said regimen claim 1 , a T Cof said subject is ...

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12-01-2017 дата публикации

Mammalian metabolites of steroids

Номер: US20170008920A1
Принадлежит: Tokai Pharmaceuticals Inc

Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions.

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10-01-2019 дата публикации

Trans-Clomiphene and Progesterone Receptor Antagonist Combination Therapy for Treating Hormone-Dependent Conditions

Номер: US20190008804A1
Принадлежит:

The present invention pertains to a combination for simultaneous, separate, or sequential use which comprises (a) trans-clomiphene or a salt or analogue thereof and (b) a progesterone receptor antagonist and to its use for the treatment of hormone-dependent conditions. 1. A method for treating a hormone-dependent condition in a mammal , comprising administering to a mammal in need thereof , an effective amount of a combination comprising (a) trans-clomiphene or a salt or analogue thereof and (b) a selective progesterone receptor modulator (SPRM) , wherein the hormone-dependent condition is selected from the group consisting of: adenomyosis , endometriosis or pain associated therewith , endometriomas of the ovary , dysmenorrhea , endocrine hormone-dependent tumors , uterine fibroids , endometrial hyperproliferation , menorrhagia , ovarian cancer , cervical cancer and breast cancer.2. A method of contraception comprising administering to a female mammal in need thereof , an effective amount of a combination comprising (a) trans-clomiphene or a salt or analogue thereof and (b) an SPRM.3. The method of or , wherein the SPRM is selected from telapristone (21 -methoxy-17α-acetoxy-11β-(4 N , N-dimethylaminophenyl)-19-norpregna-4 ,9-diene-3 ,20-dione) , ulipristal (17α-acetoxy-11β-(4-N ,N-dimethylaminophenyl)-19-norpregna-4 ,9-dien-3 ,20-dione) , CDB-4453 (21-methoxy-17α-acetoxy-11β-(4-N-methylaminophenyl)-19-norpregna-4 ,9-diene-3 ,20-dione) and asoprisnil (benzaldehyde , 4-[(11β ,17β)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4 ,9-dien-11-yl]-1-(E)-oxim).4. The method of claim 3 , wherein the SPRM is telapristone.5. The method of any one of - claim 3 , wherein (a) and (b) are sequentially administered.6. The method according to any one of - claim 3 , wherein (a) and (b) are co-administered to the mammal in the same formulation.7. The method according to any one of - claim 3 , wherein (a) and (b) are administered to the mammal by the same route claim 3 , preferably wherein ...

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17-01-2019 дата публикации

Filters for infusion sets

Номер: US20190015587A1
Принадлежит: NOVARTIS AG

In an acute care setting, rapid onset of the therapeutic effects of medication is highly desirable. The invention provides in-line filters suitable for rapid delivery of a positively charged protein therapeutic via intravenous administration.

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21-01-2021 дата публикации

CORTICOTROPIN RELEASING FACTOR RECEPTOR ANTAGONISTS

Номер: US20210015827A1
Принадлежит:

The present invention provides novel pharmaceutical compositions comprising -(4-Chloro-2-(morpholin-4-yl)thiazol-5-yl)-7-(1-ethylpropyl)-2,5-dimethylpyrazolo(1,5-a)pyrimidine and methods of using the same for the treatment of Congenital adrenal hyperplasia (CAH). 2. The method of claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 50 mg/day and about 1200 mg/day.3. The method of or claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 50 mg/day and about 1000 mg/day.4. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 50 mg/day and about 800 mg/day.5. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 100 mg/day and about 600 mg/day.6. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 200 mg/day and 400 mg/day.7. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose of about 200 mg/day.8. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is in the form of microparticles.9. The method of claim 8 , wherein the average size of the microparticles is between about 1 μm and about 20 μm.10. The method of or claim 8 , wherein the average size of the microparticles is between about 5 μm and about 15 μm.11. The method of any one of to claim 8 , wherein the average size of the microparticles is less than about 10 μm.12. The method of any one of ...

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25-01-2018 дата публикации

Method of Safely and Effectively Treating and Preventing Secondary Hyperparathyroidism in Chronic Kidney Disease

Номер: US20180021355A1
Принадлежит: Opko Renal Llc

A method of treating and preventing secondary hyperparathyroidism in CKD by increasing or maintaining blood concentrations of both 25-hydroxyvitamin D and 1,25-dihydroxyvitamin D in a patient by administering 25-hydroxyvitamin D 3 with or without 25-hydroxyvitamin D 2 and, as necessary, 1,25-dihydroxyvitamin D 2 as a Vitamin D hormone replacement therapy.

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24-01-2019 дата публикации

FOOD COMPOSITION FOR PREVENTING AND ALLEVIATING FEMALE MENOPAUSE SYMPTOMS CONTAINING GRAPE SEED EXTRACT, VALERIAN EXTRACT AND SAFFLOWER SEED EXTRACT

Номер: US20190022163A1
Автор: Kim Ji Hoon, SHIM Tae Jin
Принадлежит: FromBio Co., Ltd

Provided is a food composition for preventing and alleviating female menopause symptoms containing a grape seed extract, a valerian extract and a safflower seed extract. 1. A food composition for preventing and alleviating female menopause symptoms comprising , as an active ingredient , a combination of a grape seed extract , a valerian extract and a safflower seed extract.2. The food composition according to claim 1 , wherein the combination is a combination comprising 10 to 40% by weight of the grape seed extract claim 1 , 15 to 50% by weight of the valerian extract and 30 to 70% by weight of the safflower seed extract.3. The food composition according to claim 1 , wherein the grape seed extract claim 1 , the valerian extract and the safflower seed extract are each extracted with water claim 1 , a C1 to C4 lower alcohol or a mixture thereof as an extraction solvent.4. The food composition according to claim 1 , wherein the combination is present in an amount of 0.01 to 50% by weight with respect to the total weight of the food composition.5. A method of preventing or alleviating a female menopause symptom in a subject in need thereof comprising administering the composition of to the subject.6. The method of claim 5 , wherein the composition comprises 10 to 40% by weight of the grape seed extract claim 5 , 15 to 50% by weight of the valerian extract and 30 to 70% by weight of the safflower seed extract.7. The method of claim 5 , wherein the grape seed extract claim 5 , the valerian extract and the safflower seed extract are each an extract of water claim 5 , an extract of a C1 to C4 lower alcohol or an extract of the mixture thereof.8. The method of claim 5 , wherein the combination is present in an amount of 0.01 to 50% by weight with respect to the total weight of the composition. The present invention relates to a food composition for preventing and alleviating female menopause symptoms containing a grape seed extract, a valerian extract and a safflower seed ...

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28-01-2021 дата публикации

Composition for promoting increase in androgen

Номер: US20210023105A1
Принадлежит: Kobayashi Pharmaceutical Co Ltd

An object of the present invention is to provide a composition for stimulating an increase in an androgen. The composition for stimulating an increase in an androgen contains compound K. The composition for stimulating an increase in an androgen contains a fermentation product and/or enzymatically degraded product of ginseng as an active ingredient.

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28-01-2021 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20210024458A1
Принадлежит:

This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 3. The method according to claim 1 , wherein Qis CN.4. The method according to claim 1 , wherein Qand Qare joined together to form a substituted or unsubstituted C-Cnon-aromatic carbocyclic or a substituted or unsubstituted C-Cheterocyclic ring.6. The method according to claim 1 , wherein said disease or condition is hypergonadism claim 1 , hypersexuality claim 1 , sexual dysfunction claim 1 , gynecomastia claim 1 , precocious puberty in a male claim 1 , hair loss claim 1 , hyperandrogenic dermatological disorders claim 1 , pre-cancerous lesions of the prostate claim 1 , benign prostate hyperplasia claim 1 , prostate cancer and/or other androgen-dependent cancers.8. The method according to claim 7 , wherein said disease or condition is hypergonadism claim 7 , hypersexuality claim 7 , sexual dysfunction claim 7 , gynecomastia claim 7 , precocious puberty in a male claim 7 , hair loss claim 7 , hyperandrogenic dermatological disorders claim 7 , pre-cancerous lesions of the prostate claim 7 , benign prostate hyperplasia claim 7 , prostate cancer and/or other androgen-dependent cancers. This Application is a Continuation application of U.S. patent application Ser. No. 16/153,193, filed on Oct. 5, 2018, which is a Continuation-in-Part application of U.S. patent application Ser. No. 15/830,688, filed on Dec. 4, 2017, which is a Continuation-in-Part application of U.S. ...

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31-01-2019 дата публикации

AMINOAZOLE DERIVATIVE

Номер: US20190031628A1
Принадлежит: TEIJIN PHARMA LIMITED

A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (R)-A- (CRR)—(CRR); A represents aryl, heteroaryl; Rrepresents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; Rrepresents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, RRNCO—; Rand Rrepresent hydrogen, halogen, alkyl, phenyl, and cycloalkyl. 2. The compound or a medically acceptable salt thereof according to claim 1 , wherein Ris a C1-C9 alkyl group (optionally substituted with a halogen claim 1 , a hydroxyl group claim 1 , a cyano group claim 1 , a carboxyl group claim 1 , a C1-C4 alkoxycarbonyl group claim 1 , an amino group claim 1 , a C1-C6 monoalkylamino group claim 1 , a C1-C6 dialkylamino group or a C1-C6 alkylsulfonyl group) or a C1-C6 alkoxy C1-C6 alkyl group (optionally substituted with a halogen claim 1 , a hydroxyl group claim 1 , a cyano group or a C1-C4 alkoxy group).3. The compound or a medically acceptable salt thereof according to claim 1 , wherein Ris a halogen claim 1 , a C1-C6 alkyl group (optionally substituted with a halogen claim 1 , a hydroxyl group or a cyano group) claim 1 , a C3-C8 cycloalkyl group (optionally substituted with a halogen claim 1 , a hydroxyl group or a cyano group) or a phenyl group (optionally substituted with a halogen claim 1 , a hydroxyl group or a cyano group).4. The compound or a medically acceptable salt thereof according to claim 1 , wherein Ris a hydrogen atom claim 1 , a halogen claim 1 , a C1-C6 alkyl group (optionally substituted with a halogen claim 1 , a hydroxyl group or a cyano group) or a C3-C8 cycloalkyl group optionally substituted with a ...

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08-02-2018 дата публикации

Method of treating thermoregulatory dysfunction with paroxetine

Номер: US20180036299A1
Принадлежит: Sebela International Ltd

The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.

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06-02-2020 дата публикации

METHODS OF TREATING TESTOSTERONE DEFICIENCY

Номер: US20200038411A1
Принадлежит:

Methods of treating a testosterone deficiency or its symptoms with a pharmaceutical formulation of testosterone esters are provided. The methods are designed to provide optimum plasma testosterone levels over an extended period. 1. A method of treating chronic testosterone deficiency in a subject in need thereof comprising the steps of:a. administering daily to the subject a defined dose of an oral pharmaceutical composition comprising a testosterone ester solubilized in a carrier comprising at least one lipophilic surfactant and at least one hydrophilic surfactant;b. collecting said subject's blood sample in tubes containing NaF;c. measuring the NaF-containing plasma testosterone concentration in the subject; andd. increasing the dose of testosterone ester administered in step a. when the measured plasma testosterone concentration in the subject is less than about 350 ng/dL, decreasing each dose of testosterone ester administered in step a. when the measured plasma testosterone concentration in the subject is greater than about 800 ng/dL, and maintaining each dose of testosterone ester administered in step a. when the measured plasma testosterone concentration in the subject is between about 350 ng/dL and about 800 ng/dL.2. The method of claim 1 , wherein the initial defined dose of testosterone ester in the oral pharmaceutical composition is equivalent to about 150 mg of testosterone.3. The method of claim 2 , wherein the defined dose of testosterone ester in the administered oral pharmaceutical composition is increased by the equivalent of about 25-75 mg of testosterone when the plasma testosterone concentration in the subject is less than about 350 ng/dL.4. The method of claim 2 , wherein the defined dose of testosterone ester in the administered oral pharmaceutical composition is decreased by the equivalent of about 10-75 mg of testosterone when the plasma testosterone concentration in the subject is greater than about 800 ng/dL.5. The method of claim 1 , ...

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12-02-2015 дата публикации

Biphasic lipid-vesicle compositions and methods for treating cervical dysplasia by intravaginal delivery

Номер: US20150044274A1
Автор: Praveen Kumar
Принадлежит: Helix Biopharma Corp

This invention relates to biphasic lipid-vesicle compositions and methods for treating cervical displasia by intravaginal delivery.

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07-02-2019 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20190040000A1
Принадлежит:

This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 3. The method according to claim 1 , wherein Qis CN.4. The method according to claim 1 , wherein Qand Qare joined together to form a substituted or unsubstituted C-Cnon-aromatic carbocyclic or a substituted or unsubstituted C-Cheterocyclic ring.6. The method according to claim 1 , wherein said condition is hypergonadism claim 1 , hypersexuality claim 1 , sexual dysfunction claim 1 , gynecomastia claim 1 , precocious puberty in a male claim 1 , alterations in cognition and mood claim 1 , depression claim 1 , hair loss claim 1 , hyperandrogenic dermatological disorders claim 1 , pre-cancerous lesions of the prostate claim 1 , benign prostate hyperplasia claim 1 , prostate cancer and/or other androgen-dependent cancers.9. The method according to claim 7 , wherein Qis CN.10. The method according to claim 7 , wherein Qand Qare joined together to form a substituted or unsubstituted C-Cnon-aromatic carbocyclic or a substituted or unsubstituted C-Cheterocyclic ring.12. The method of claim 7 , wherein said castration-resistant prostate cancer is AR overexpressing castration-resistant prostate cancer claim 7 , F876L mutation expressing castration-resistant prostate cancer claim 7 , F876L_T877A double mutation expressing castration-resistant prostate cancer claim 7 , AR-V7 expressing castration-resistant prostate cancer claim 7 , d567ES expressing castration-resistant prostate ...

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13-02-2020 дата публикации

Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same

Номер: US20200046733A1
Принадлежит: Clarus Therapeutics Inc

A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

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21-02-2019 дата публикации

ORAL DOSAGE FORM OF BOTH CLOMIPHENE ISOMERS AND METHOD OF USING SAME TO TREAT SECONDARY HYPOGONADISM AND MINIMIZE DRUG SIDE EFFECTS IN MEN

Номер: US20190054044A1
Принадлежит: ASPEN PARK PHARMACEUTICALS, INC.

The present invention relates to a pharmaceutical oral dosage form comprising both (A) trans-clomiphene or a pharmaceutically acceptable salt thereof and (B) cis-clomiphene or a pharmaceutically acceptable salt thereof, wherein (i) the ratio of (A):(B) in the dosage form is about 70:30; (ii) the amount of (A) in the dosage form is about 12.5 mg or about 25 mg; and (iii) the amount of (B) in the dosage form is less than 15 mg. The pharmaceutical oral dosage form is useful to treat secondary hypogonadism in men and minimize certain antiestrogenic drug side effects such as impaired cognition, hot flashes and bone loss, osteoporosis, and skeletal fractures. 1. A method of treating secondary hypogonadism in a human male patient in need thereof comprising orally administering to said human male patient an effective amount therefor of both (A) trans-clomiphene or a pharmaceutically acceptable salt thereof and (B) cis-clomiphene or a pharmaceutically acceptable salt thereof , wherein (i) the ratio of (A):(B) administered is about 70:30; (ii) the effective amount of (A) is about 12.5 mg per day or about 25 mg per day; and (iii) the effective amount of (B) is less than 15 mg per day.2. The method according to claim 1 , wherein the male is administered a daily dose of about 12.5 mg of (A) and about 5.3 mg of (B).3. The method according to claim 2 , wherein the daily dose of (A) and (B) is contained in a single tablet comprising both (A) and (B).4. The method according to claim 1 , wherein the male is administered a daily dose of about 25 mg of (A) and about 10.7 mg of (B).5. The method according to claim 4 , wherein the daily dose of (A) and (B) is contained in a single tablet comprising both (A) and (B).6. The method according to claim 1 , wherein (A) is trans-clomiphene citrate and/or (B) is cis-clomiphene citrate.7. The method according to claim 1 , which is for treatment of chronic secondary hypogonadism claim 1 , and is carried out for at least 6-12 months or for the ...

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04-03-2021 дата публикации

Liquid polymer delivery system for extended administration of drugs

Номер: US20210060036A1
Принадлежит: Tolmar International Ltd

Liquid polymer pharmaceutical compositions with a biodegradable liquid polyester that has a carboxylic acid end group, a biocompatible solvent, and an active pharmaceutical agent are useful for administration into the body to provide extended long term release of the drug.

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08-03-2018 дата публикации

Ulipristal acetate tablets

Номер: US20180064651A1
Принадлежит: Laboratoire HRA Pharma SAS

The invention relates to a pharmaceutical tablet for oral administration comprising ulipristal acetate together with the following excipients: at least one diluent in an amount of 50 to 98.5 wt %, at least one binding agent in an amount of 0 to 10 wt %, at least one disintegrating agent in an amount of 0.5 to 10 wt %, and at least one lubricant in an amount of 0 to 10 wt %.

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11-03-2021 дата публикации

NOVEL PHARMACEUTICAL COMPOSITIONS AND METHODS FOR MENOPAUSE RELATED ANXIETY AND DEPRESSION

Номер: US20210069209A1
Автор: Cui Geping, Wang Jianmin
Принадлежит:

Pharmaceutical compositions comprising azelastine or a pharmaceutically acceptable salt of azelastine and alprazolam are disclosed. Methods of using the pharmaceutical compositions for treating perimenopausal or menopausal patients, such as patients suffering from, experiencing, exhibiting and/or having one or more symptoms of anxiety or depression, are also disclosed. 1. A pharmaceutical composition , comprising:up to about 8 mg azelastine or a pharmaceutically acceptable salt of azelastine;alprazolam;and one or more pharmaceutically acceptable excipients.2. The pharmaceutical composition of claim 1 , wherein the alprazolam is present in the pharmaceutical composition in an amount in the range of up to about 4 mg.3. The pharmaceutical composition of claim 1 , wherein the azelastine or the pharmaceutically acceptable salt of azelastine is present in the pharmaceutical composition in an amount 5 times that of the alprazolam present in the pharmaceutical composition.4. The pharmaceutical composition of claim 3 , wherein:the azelastine or the pharmaceutically acceptable salt of azelastine is present in the pharmaceutical composition in an amount in the range of about 2 mg; andthe alprazolam is present in the pharmaceutical composition in an amount in the range of about 0.4 mg.5. The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable salt of azelastine is azelastine hydrochloride.6. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is formulated as an oral pharmaceutical dosage form.7. A method comprising:administering a pharmaceutical composition to a perimenopausal or menopausal patient;wherein the pharmaceutical composition comprises azelastine, or a pharmaceutically acceptable salt of azelastine, and alprazolam.8. The method of claim 7 , wherein the pharmaceutical composition is administered once or twice a day claim 7 , or once every 2 or 3 or 4 days claim 7 , to the patient in an oral solid or liquid ...

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24-03-2022 дата публикации

TREATMENT METHODS OF TRIPHENYL CALCILYTIC COMPOUNDS

Номер: US20220087961A1
Принадлежит:

The present disclosure provides a method of treating an autosomal dominant hypocalcemia type 1 (ADH1) with a therapeutically effective amount of a compound of formula (I), in particular CLTX-305, wherein the therapeutically effective amount of the compound increases a blood calcium concentration (cCa) to a range of about 7.5 mg/dL to about 10.5 mg/dL, such as about 8.5 mg/dL to about 10.5 mg/dL. Also provided herein is a dosing finding method for treating an autosomal dominant hypocalcemia type 1 (ADH1) with a therapeutically effective amount of a compound of formula (I) or CLTX-305 according to one or more dosing regimens. 3. The method of or , wherein the subject has hypocalcemia , hypoparathyroidism , hypercalciuria , hyperphosphatemia , and/or hypomagnesemia.4. The method of any one of to , wherein the subject has an activating mutation of the calcium-sensing receptor (CASR) gene.5. The method of any one of to , wherein the subject has 25-hydroxy-vitamin D in blood at a level of at least about 25 nanograms per milliliter (ng/mL).6. The method of any one of to , wherein the subject is not treated with calcitriol.7. The method of any one of to , wherein the subject receives a daily calcium intake of at least about 1000 mg from diet and/or supplementation.8. The method of any one of to , wherein the therapeutically effective amount is a total daily dosage of from about 10 mg to about 1800 mg , from about 10 mg to about 1200 mg , from about 10 mg to about 900 mg , from about 10 mg to about 600 mg , or from about 10 mg to about 360 mg of CLTX-305.9. The method of claim 8 , wherein the therapeutically effective amount is a total daily dosage of about 10 mg claim 8 , 20 mg claim 8 , 30 mg claim 8 , 40 mg claim 8 , 60 mg claim 8 , 80 mg claim 8 , 120 mg claim 8 , 140 mg claim 8 , 180 mg claim 8 , 300 mg claim 8 , 360 mg claim 8 , 480 mg claim 8 , or 720 mg of CLTX-305.10. The method of any one of to claim 8 , wherein the compound of formula (I) or CLTX-305 is ...

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24-03-2022 дата публикации

METHODS OF TREATING TESTOSTERONE DEFICIENCY

Номер: US20220088034A1
Принадлежит:

Methods of treating a testosterone deficiency or its symptoms with a pharmaceutical formulation of testosterone undecanoate are provided. 1. A method of treating conditions associated with a deficiency or absence of endogenous testosterone in a subject in need thereof comprising the steps of:administering to the subject a defined dose of an oral pharmaceutical composition comprising testosterone undecanoate solubilized in a carrier comprising at least one lipophilic surfactant and at least one hydrophilic surfactant, wherein the defined dose is 198 mg administered twice daily;collecting a blood sample from the subject;measuring the serum testosterone concentration in the subject; andincreasing the dose of testosterone undecanoate to 237 mg, administered twice daily, when the measured serum testosterone concentration in the subject is less than about 425 ng/dL,decreasing the dose of testosterone undecanoate to 158 mg, administered twice daily, when the measured serum testosterone concentration in the subject is greater than about 970 ng/dL, ormaintaining the dose of testosterone undecanoate when the measured serum testosterone concentration in the subject is between about 425 ng/dL and about 970 ng/dL.2. The method of claim 1 , wherein the serum testosterone concentration is measured four to eight hours after administering the oral pharmaceutical composition.3. The method of claim 1 , wherein the oral pharmaceutical composition comprises about 19.8 percent by weight of solubilized testosterone undecanoate claim 1 , about 51.6 percent by weight of oleic acid claim 1 , and about 16.1 percent by weight of polyoxyethylene (40) hydrogenated castor oil.4. The method of claim 3 , wherein the oral pharmaceutical composition further comprises about 10 percent by weight of borage seed oil and about 2.5 percent by weight of peppermint oil.5. The method of claim 1 , wherein the testosterone concentrations are measured in serum from a blood sample collected in a plain tube drawn ...

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24-03-2022 дата публикации

Methods of treating female infertility

Номер: US20220088114A1
Принадлежит: Myovant Sciences Gmbh

Further according to the present disclosure, there are methods for promoting egg maturation in assisted reproductive technologies, such as in in vitro fertilization (IVF) or in an embryo transfer (ET) process. There are also methods for decreasing the rate of ovarian hyper-stimulation syndrome (OHSS), providing comparable or improved pregnancy rates, decreasing the time to pregnancy, and inhibiting premature ovulation. The methods include the step of administering a therapeutically effective amount of an active pharmaceutical ingredient of 2-(N-acetyl-D-tyrosyl-trans-4-hydroxy-L-prolyl-L-asparaginyl-L-threonyl-L-phenylalanyl) hydrazinocarbonyl-L-leucyl-Nω-methyl-L-arginyl-L-tryptophanamide or a pharmaceutically acceptable salt thereof.

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24-03-2022 дата публикации

COMPOSITIONS CONTAINING A PEPTIDE ABLE TO STIMULATE THE GPRC6A-DEPENDENT SIGNALING PATHWAY

Номер: US20220088121A1
Принадлежит:

Disclosed are pharmaceutical or nutraceutical compositions comprising the peptide having the sequence NMYLPPVPPP PVVPTF or extracts containing it, in admixture with suitable excipients. 1. Pharmaceutical or nutraceutical compositions comprising a peptide having sequence NMYLPPVPPPPVVPTF (SEQ ID NO:1) in isolated form or isolated proteins containing said sequence or extracts containing said sequences or isolated proteins.2Phaseolus vulgaris.. Compositions according to wherein the peptide is contained in extracts of3. Compositions according to further comprising additional active ingredients having complementary or synergic activity.4. Method of treating conditions benefiting from stimulation of the GPRC6A-dependent signalling pathway with the compositions according to in patients in need thereof claim 1 , said method comprisingadministering said compositions to said patient.5. The method according to wherein the conditions comprise male hypogonadism claim 4 , osteopenia/osteoporosis claim 4 , erectile dysfunction and metabolic syndrome. The present invention relates to pharmaceutical or nutraceutical compositions comprising the peptide having the sequence NMYLPPVPPP PVVPTF or extracts containing it, in admixture with suitable excipients. The compositions according to the invention are useful for therapeutic or adjuvant treatment of conditions that benefit from stimulation of the GPRC6A-dependent signalling pathway. Examples of such conditions include male hypogonadism, osteopenia/osteoporosis, erectile dysfunction and metabolic syndrome.The role of bone tissue as an endocrine organ is a subject that has aroused great scientific interest in the last ten years. Initial studies of animal models suggested that osteocalcin (OCN), a small protein of osteoblastic origin which is normally involved in mineralisation of extracellular bone matrix in its γ-carboxylated form, may exhibit systemic effects after decarboxylation. In particular, uncarboxylated osteocalcin (ucOCN) ...

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26-03-2015 дата публикации

Method and composition for transdermal drug delivery

Номер: US20150087623A1
Принадлежит: Acrux DDS Pty Ltd

The invention is directed to a transdermal drug delivery composition which includes at least one physiologically active agent; and at least one volatile solvent; and at least one viscosity modulating agent. The invention extends to methods of administering such a composition to a subject and treatment of subjects using the composition.

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25-03-2021 дата публикации

USE OF MIR-21 IN PREPARATION OF DRUG FOR TREATING INTRAUTERINE ADHESION AND/OR THIN ENDOMETRIUM

Номер: US20210085806A1
Принадлежит: NANJING DRUM TOWER HOSPITAL

Provided is use of miR-21 in preparation of a therapeutic drug or diagnostic reagent for intrauterine adhesion and/or thin endometrium. 1. A method for treating intrauterine adhesion and/or thin endometrium , comprising increasing an amount of miR-21 in endometrial epithelial cells and/or interstitial cells so as treat intrauterine adhesion and/or thin endometrium.2. The method according to claim 1 , wherein a therapeutically effective amount of miR-1 is provided to a subject in need of treatment for a disease caused by intrauterine adhesion and/or thin endometrium.3. The method according to claim 2 , wherein the disease is uterine infertility claim 2 , recurrent abortion claim 2 , or placenta adhesion and implantation caused by intrauterine adhesion and/or thin endometrium.4. A method comprising detecting expression of miR-21 in a subject having or suspected of having intrauterine adhesion and/or thin endometrium with a reagent specific for miR-21.5. A method for detecting intrauterine adhesion and/or thin endometrium claim 4 , comprising performing the method according to to measure whether there is underexpression of miR-21 in endometrial epithelial cells and/or interstitial cells.6. The method according to claim 4 , wherein the reagent is selected from the group consisting of PCR and qPCR primers claim 4 , Taqman probes claim 4 , dioxigenin or fluorescent dye-labeled probes claim 4 , miRNA expression profile chips claim 4 , and deep sequencing reagents.7. The method according to claim 6 , wherein the reagent comprises a digoxigenin or fluorescent dye-labeled probe that includes SEQ ID NO. 1.811-. (canceled) The invention belongs to the field of biological pharmacy, and relates to use of miR-21 in preparation of a drug for treating intrauterine adhesion and/or thin endometrium.The endometrium regeneration disorders mainly include intrauterine adhesion and thin endometrium. Intrauterine adhesion is an adhesion between uterine walls characterized by endometrial ...

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12-05-2022 дата публикации

CORTICOTROPIN RELEASING FACTOR RECEPTOR ANTAGONISTS

Номер: US20220143037A1
Принадлежит:

The present invention provides novel pharmaceutical compositions comprising -(4-Chloro-2-(morpholin-4-yl)thiazol-5-yl)-7-(1-ethylpropyl)-2,5-dimethylpyrazolo(1,5-a)pyrimidine and methods of using the same for the treatment of Congenital adrenal hyperplasia (CAH). 2. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is administered at a dose between about 50 mg/day and about 1600 mg/day.3. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is administered at a dose between about 100 mg/day and about 600 mg/day.4. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is administered at a dose of about 200 mg/day.5. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is in the form of microparticles.6. The method of claim 5 , wherein the average size of the microparticles is between about 1 μm and about 20 μm.7. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is in the form of a pharmaceutical composition.8. The method of claim 7 , wherein the pharmaceutical composition is in the form of a capsule or a tablet.9. The method of claim 1 , wherein CAH is classic CAH.10. The method of claim 1 , wherein CAH is non-classic CAH.11. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 15% from baseline.12. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 20% from baseline.13. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 25% from baseline.14. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 10% from baseline and is maintained at a reduced level post 24 hours.15. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 10% from baseline and is maintained at a reduced level post 4 weeks.16. The method of claim 1 , wherein the 17-OHP ...

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12-04-2018 дата публикации

METHODS, COMPOSITIONS, AND KITS INVOLVING ALTERATION OF THE CHAPERONE PROTEIN AXIS IN A SUBJECT

Номер: US20180099024A1
Автор: Casey Patrick J.
Принадлежит:

The present invention broadly related to compositions, treatment methods, and kits involving alteration of the chaperone protein axis of a subject. In one aspect, the invention features a method of treatment of a subject including the step of administering to the subject at least one dose of a therapeutically effective amount of a composition for altering a chaperone protein axis of the subject. The composition includes at least one essential fragment of a feto-placental unit protein. 1. A method of treatment of a subject comprising:administering to the subject at least one dose of a therapeutically effective amount of a composition for altering a chaperone protein axis of the subject;wherein the composition includes at least one essential fragment of a feto-placental unit protein.2. The method of claim 1 , wherein the essential fragment of the feto-placental unit protein comprises an essential fragment of a chaperone protein.3. The method of claim 2 , wherein the chaperone protein comprises a protein included in the HSP70 family.4. The method of claim 1 , wherein prior to the administering step claim 1 , the method comprises identifying a subject in need of alteration of the chaperone protein axis of the subject.5. The method of claim 1 , wherein altering the chaperone protein axis of the subject comprises stimulating the chaperone protein axis for at least one of manufacturing a chaperone protein claim 1 , releasing a chaperone protein from a cell claim 1 , decreasing an amount of a chaperone protein claim 1 , and increasing an amount of a chaperone protein in the subject.6. The method of claim 1 , wherein altering the chaperone protein axis of the subject comprises decreasing an amount of a chaperone protein circulating in a blood stream of the subject.7. The method of further comprising monitoring the chaperone protein axis in the subject during at least one of a selected pre-treatment time period claim 1 , a treatment time period claim 1 , and a post-treatment ...

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13-04-2017 дата публикации

Compositions based on plant extracts for inhibition of the 5-alpha reductase

Номер: US20170100447A1
Принадлежит: BIONAP Srl

The present invention refers to nutraceutical, cosmetic or pharmaceutical compositions based on a combination of vegetal extracts from flowers or fruits of Opuntia ficus and Oryza sativa (Black rice) for inhibition of the 5-alpha reductase. In particular, the preparations according to the invention are useful in prevention or treatment of benign prostatic hypertrophy or hyperplasia, of androgenic alopecia and acne.

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23-04-2015 дата публикации

Method for retarding unhealthy manifestations brought by ageing of human beings

Номер: US20150110769A1
Принадлежит: CLS Therapeutics Ltd

The present invention provides a method for retarding unhealthy manifestations brought by ageing of human beings (in particular, but not limited to the reduction of sexual activity and fertility, climax, changes in glucose tolerance, reduction of cognitive and mnestic functions, reduction of stress resistance, development of organ and tissue sclerosis). According to the invention this task is solved by administration into the blood circulation of an agent which inactivates extracellular blood plasma DNA e.g. a DNase enzyme.

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11-04-2019 дата публикации

LYMPH DIRECTING PRODRUGS

Номер: US20190105299A1
Принадлежит:

The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug. 123-. (canceled)26. The compound of claim 24 , wherein —Y— is substituted.27. The compound of claim 24 , wherein —Z— is —C(O)R—.28. The compound of claim 24 , wherein —Y— is substituted and —Z— is —C(O)R—.29. The compound of claim 24 , wherein —Y— represents a —C-Calkyl- claim 24 , —C-Calkenyl- claim 24 , or —C-Calkynyl- group optionally substituted with one or more groups selected from hydroxyl claim 24 , alkyl claim 24 , alkoxy claim 24 , alkoxycarbonyl claim 24 , alkenyl claim 24 , alkenyloxy claim 24 , alkynyl claim 24 , alkynyloxy claim 24 , amino claim 24 , aminoacyl claim 24 , thio claim 24 , arylalkyl claim 24 , arylalkoxy claim 24 , aryl claim 24 , aryloxy claim 24 , acylamino claim 24 , carboxy claim 24 , cyano claim 24 , halogen claim 24 , nitro claim 24 , sulfo claim 24 , phosphono claim 24 , phosphorylamino claim 24 , phosphinyl claim 24 , heteroaryl claim 24 , heteroaryloxy claim 24 , heterocyclyl claim 24 , heterocycloxy claim 24 , trihalomethyl claim 24 , pentafluoroethyl claim 24 , trifluoromethoxy claim 24 , difluoromethoxy claim 24 , trifluoromethanethio claim 24 , trifluoroethenyl claim 24 , mono- and di-alkylamino claim 24 , mono- and di-(substituted alkyl)amino claim 24 , mono- and di-arylamino claim 24 , mono- and di-heteroarylamino claim 24 , mono- and di-heterocyclyl claim 24 , amino claim 24 , and unsymmetric di-substituted amines having different substituents selected from alkyl claim 24 , aryl claim 24 , heteroaryl claim 24 , and heterocyclyl claim 24 , wherein one or more of the carbon atoms in the —C-Calkyl- claim 24 , —C-Calkenyl- claim 24 , or —C-Calkynyl- group of —Y— may be replaced with NH claim 24 , S claim 24 , or O.30. The compound of claim 25 , wherein —Y— represents a —C-Calkyl- claim 25 , —C- ...

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13-05-2021 дата публикации

Administration of Testosterone Compositions

Номер: US20210137944A1
Принадлежит: Antares Pharma, Inc.

The present invention provides compositions and methods for treating a subject in need of treatment with testosterone, including introducing testosterone into the subject subcutaneously, intradermally, or intramuscularly, from a needle assisted jet injection device. 1. A method of obtaining steady state average blood concentration of testosterone comprising the step of repeatedly administering a dose of testosterone over a prescribed time period such that a steady state blood plasma level of testosterone is obtained after three or more doses.2. The method of claim 1 , wherein the dose is selected from between 50 mg. claim 1 , 75 mg. and 100 mg.3. The method of claim 2 , wherein the concentration of the administered dose is 100 mg/ml claim 2 , 150 mg/ml or 200 mg/ml.4. The method of claim 1 , wherein the dose is between 50 mg and 100 mg.5. The method of claim 1 , wherein the prescribed time period is weekly dosing.6. The method of claim 1 , wherein steady state is reached after the fourth dose.7. The method of claim 1 , wherein steady state is reached after the fifth dose.8. The method of claim 1 , wherein the doses are continued after steady state is reached.9. The method of claim 8 , wherein the doses administered after steady state is reached are the same or different than the dose administered prior to reaching steady state.10. The method of claim 5 , wherein once steady state is reached claim 5 , the average blood plasma concentration obtained after administration of a subsequent dose or doses is less than + or −30% of the average plasma concentration obtained during the immediately preceding week.11. The method of claim 1 , wherein the steady state therapeutic blood levels maintained at steady state after multiple dosings is about 800 ng/dl to about 1100 ng/dl claim 1 ,12. The method of claim 1 , wherein the steady state therapeutic blood levels maintained at steady state after multiple dosings is about 500 ng/dl to about 800 ng/dl claim 1 ,13. The method of ...

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09-04-2020 дата публикации

Treatment of Fibrotic Conditions

Номер: US20200108069A1
Принадлежит:

This invention relates to the treatment of fibrotic conditions, such as Peyronie's disease, by administering a phosphodiesterase type 5 (PDE5) inhibitor, such as vardenafil, and a selective oestrogen receptor modulator (SERM), such as tamoxifen, to an individual in need thereof. 1. A method of treatment of a fibrotic condition comprising administering a phosphodiesterase type 5 (PDE5) inhibitor and a selective oestrogen receptor modulator (SERM) to an individual in need thereof.2. The method according to claim 1 , wherein the PDE5 inhibitor is selected from the group consisting of avanafil claim 1 , lodenafil claim 1 , mirodenafil claim 1 , udenafil claim 1 , benzamidenafil claim 1 , dasantafil claim 1 , sildenafil claim 1 , vardenafil and tadalafil.3. The method according to claim 1 , wherein the PDE5 inhibitor is vardenafil.4. The method according to claim 1 , wherein the SERM is selected from the group consisting of arzoxifene (LY353381) claim 1 , toremifene claim 1 , bazedoxifene (TSE-424) claim 1 , lasofoxifene (CP-336156) claim 1 , ospemifene claim 1 , raloxifene claim 1 , or tamoxifen.5. The method according to claim 1 , wherein the SERM is tamoxifen.6. The method according to claim 1 , wherein the fibrotic condition is a pulmonary claim 1 , liver claim 1 , heart claim 1 , kidney claim 1 , skin or brain fibrotic condition.7. The method according to claim 6 , wherein the pulmonary fibrotic condition is idiopathic pulmonary fibrosis or radiation induced lung injury.8. The method according to claim 6 , wherein the liver fibrotic condition is cirrhosis.9. The method according to claim 6 , wherein the heart fibrotic condition is atrial fibrosis or endomyocardial fibrosis.10. The method according to claim 6 , wherein the brain fibrotic condition is a glial scar.11. The method according to claim 1 , wherein the fibrotic condition is selected from the group consisting of arterial stiffness claim 1 , arthrofibrosis claim 1 , Crohn's disease claim 1 , Dupuytren's ...

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03-05-2018 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20180118663A1
Принадлежит:

This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 2. The method of claim 1 , wherein said cancer is a cancer associated with partial androgen insensitivity syndromes (PAIS) claim 1 , cancer of the fallopian tubes or peritoneum claim 1 , salivary gland cancer claim 1 , esophageal cancer claim 1 , bladder cancer claim 1 , melanoma claim 1 , mantle cell lymphoma claim 1 , hepatocellular carcinoma claim 1 , renal cell carcinoma claim 1 , non-small cell lung cancer (NSCLC) claim 1 , gastric cancer claim 1 , and/or colon cancer.3. The method of claim 2 , wherein the cancer associated with partial androgen insensitivity syndromes (PAIS) is gonadal tumors and/or seminoma.9. The method of claim 8 , wherein said hyperandrogenic hormonal condition in a female is precocious puberty claim 8 , early puberty claim 8 , dysmenorrhea claim 8 , amenorrhea claim 8 , multilocular uterus syndrome claim 8 , endometriosis claim 8 , hysteromyoma claim 8 , abnormal uterine bleeding claim 8 , early menarche claim 8 , fibrocystic breast disease claim 8 , fibroids of the uterus claim 8 , ovarian cysts claim 8 , polycystic ovary syndrome claim 8 , pre-eclampsia claim 8 , eclampsia of pregnancy claim 8 , preterm labor claim 8 , premenstrual syndrome claim 8 , and/or vaginal dryness.11. The topical pharmaceutical composition of claim 10 , wherein said composition is in the form of a solution claim 10 , lotion claim 10 , salve claim 10 , cream claim ...

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25-08-2022 дата публикации

COMPOSITION FOR ALLEVIATING SYMPTOMS OF ANDROPAUSE, CONTAINING EXTRACT OF FICUS AURICULATA LOUR. AS ACTIVE INGREDIENT

Номер: US20220265753A1
Принадлежит:

The present invention relates to a method of preventing or alleviating symptoms of andropause comprising administering a pharmaceutically effective amount of an extract of Lour. To a patient in need thereof. The extract of Lour. of the present invention exhibits the effect of preventing and alleviating erectile dysfunction by inhibiting the activity of PDE5, and the effect of preventing and alleviating prostatic hyperplasia by suppressing the expression of AR and PSA. 1Ficus auriculata. A method of preventing or alleviating symptoms of andropause comprising administering a pharmaceutically effective amount of an extract of Lour. to a patient in need thereof.2Ficus auriculata. The method of claim 1 , wherein the extract is a fruit extract of Lour.3. The method of claim 1 , wherein the symptoms of andropause is one or more selected from the group consisting of lower urinary tract symptoms claim 1 , BPH claim 1 , prostatitis claim 1 , nervousness claim 1 , emotional anxiety claim 1 , depression claim 1 , hot flashes claim 1 , sleep disorders claim 1 , decreased vitality claim 1 , reduced work ability claim 1 , erectile dysfunction claim 1 , and alopecia.4. The method of claim 1 , wherein the extract is a hot water extract or ethanol extract5. The method of claim 1 , wherein the symptoms of andropause is caused by activation of PDE5 claim 1 , androgen receptor expression claim 1 , or PSA (Prostate specific antigen) expression. The present invention relates to a composition for alleviating symptoms of andropause, and more particularly, to a pharmaceutical, food and food additive composition for alleviating symptoms of andropause containing extract of Lour. as an active ingredient.As interest in the development of medical technology and health maintenance increases, the average life expectancy is gradually increasing, and the proportion of the population of the elderly is rapidly increasing for various social reasons. As society is aging, problems with the health of the ...

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25-04-2019 дата публикации

Compositions based on plant extracts for inhibition of the 5-alpha reductase

Номер: US20190117723A1
Принадлежит: BIONAP Srl

The present invention refers to nutraceutical, cosmetic or pharmaceutical compositions based on a combination of vegetal extracts from flowers or fruits of Opuntia ficus and Oryza sativa (Black rice) for inhibition of the 5-alpha reductase. In particular, the preparations according to the invention are useful in prevention or treatment of benign prostatic hypertrophy or hyperplasia, of androgenic alopecia and acne.

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04-05-2017 дата публикации

Diglycidic ether derivative therapeutics and methods for their use

Номер: US20170121261A1

This invention provides compound having a structure of Formula I or Formula II. Uses of such compounds for treatment of various indications, including prostrate cancer as well as methods of treatment involving such compounds are also provided.

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25-04-2019 дата публикации

Parathyroid hormone receptor 1 antagonist and inverse agonist polypeptides and methods of their use

Номер: US20190119348A1

Parathyroid hormone receptor 1 (PTHR1) antagonist and inverse agonist polypeptides and pharmaceutically acceptable salts thereof are disclosed. The polypeptides include N-terminally truncated PTH/PTHrP hybrid peptides or their fragments. Also disclosed are pharmaceutical compositions containing the PTHR1 antagonists and inverse agonists as well as methods of their use.

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10-05-2018 дата публикации

COMPOSITION FOR TREATMENT OF INFERTILITY

Номер: US20180125942A1
Принадлежит: FERRING B.V.

Preparations including FSH, for example recombinant FSH, for use in the treatment of infertility. 119-. (canceled)20. A method of treating infertility , comprising administering a follicle stimulating hormone (FSH) composition at a dose of or equivalent to from 9 to 24 μg FSH to a patient identified prior to treatment as having variant Ser/Ser at position 680 of the FSH receptor.21. The method of claim 20 , wherein the method comprises daily administration of the composition.22. The method of claim 20 , wherein the patient also is identified prior to treatment as having a serum AMH level<15 pmol/L.23. The method of claim 20 , wherein the patient also is identified prior to treatment as having a serum AMH level of from 0.05 pmol/L to 14.9 pmol/L.24. The method of claim 20 , wherein the method further comprises claim 20 , prior to administering the composition claim 20 , identifying the patient as having variant Ser/Ser at position 680 of the FSH receptor.25. The method of claim 20 , wherein the method further comprises claim 20 , prior to administering the composition claim 20 , identifying the patient as having a serum AMH level of <15 pmol/L.26. The method of claim 20 , wherein the method further comprises claim 20 , prior to administering the composition:identifying the patient as having variant Ser/Ser at position 680 of the FSH receptor, andidentifying the patient as having a serum AMH level of <15 pmol/L.27. The method of claim 20 , wherein the FSH composition is administered at a dose of or equivalent to from greater than 12 to 24 μg FSH.28. The method of claim 20 , wherein the FSH composition is administered starting on day one of treatment and continuing for from six to sixteen days.29. The method of claim 20 , wherein the FSH is recombinant FSH.30. The method of claim 20 , wherein the FSH is recombinant FSH that includes α2 claim 20 ,3-sialylation and α2 claim 20 ,6-sialylation.31. The method of claim 20 , wherein the FSH is recombinant FSH that includes α2 ...

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01-09-2022 дата публикации

Treatment of Genital Psoriasis

Номер: US20220275078A1
Принадлежит:

Methods of treating genital psoriasis, genital pruritus and genital psoriasis sexual activity impairment with anti-IL17A antibodies, including dose regimens and pharmaceutical formulations of anti-IL17A antibodies for use in the treatment of genital psoriasis, genital pruritus and genital psoriasis sexual activity impairment. 1. A method of treating a patient having less than 10% body surface area psoriasis involvement , comprising administering to the patient a therapeutically effective amount of an anti-IL17A antibody , or a pharmaceutical formulation thereof ,wherein the anti-IL17A antibody comprises a light chain variable region (LCVR) and a heavy chain variable region (HCVR), wherein said LCVR is the amino acid sequence of SEQ ID NO: 2 and said HCVR is the amino acid sequence of SEQ ID NO: 3.2. The method of claim 1 , wherein the anti-IL17A antibody comprises a light chain (LC) and a heavy chain (HC) claim 1 , wherein the LC is the amino acid sequence of SEQ ID NO: 4 and the HC is the amino acid sequence of SEQ ID NO: 5.3. The method of claim 2 , wherein the anti-IL17A antibody is ixekizumab.4. The method of claim 1 , wherein the patient has greater than 3% body surface area psoriasis involvement.5. The method of claim 1 , wherein the patient has less-than 3% body surface area psoriasis involvement.6. The method of claim 1 , wherein said step of administering comprises(a) during a 12-week induction period, administering an initial dose subcutaneous of about 160 mg of the anti-IL17 antibody or pharmaceutical formulation thereof on day 0, followed by administering subcutaneous about 80 mg of the anti-IL17 antibody or pharmaceutical formulation thereof at each of weeks 2, 4, 6, 8, 10 and 12; and(b) following the 12-week induction period, administering subcutaneous about 80 mg of the anti-IL17 antibody or pharmaceutical formulation thereof at week 16 and at every four-week interval thereafter.7. The method of claim 1 , wherein said step of administering comprises ...

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03-06-2021 дата публикации

Crystalline Forms Of An Androgen Receptor Modulator

Номер: US20210163441A1

Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.

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08-09-2022 дата публикации

Composition for ameliorating premenstrual syndrome symptoms, including chrysanthemum zawadskii extract

Номер: US20220280583A1
Принадлежит: Genencell Co Ltd

The present invention relates to a composition which is for preventing and ameliorating or treating premenstrual syndrome symptoms, and includes: (a) a Chrysanthemum zawadskii extract; (b) a mixture of the Chrysanthemum zawadskii extract and a malt extract; or (c) a mixture of the Chrysanthemum zawadskii extract, the malt extract, and an aloe extract. Specifically, the present compositions effectively inhibit the secretion of prolactin from pituitary cells, which is a phenomenon that appears during premenstrual syndrome, thereby increasing the secretion of progesterone, which is reduced during the luteal phase of women, and can thus be advantageously used as a composition for preventing and ameliorating or treating women's premenstrual syndrome.

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30-04-2020 дата публикации

Progesterone in Bioadhesive Formulation for Buccal Delivery

Номер: US20200129422A1
Принадлежит: Viramal Ltd

A pharmaceutical mucoadhesive gel composition for delivering therapeutic agents (such as progesterone) by buccal, nasal, vaginal and rectal administration, thereby avoiding the hepatic first-pass metabolism. The gel composition comprises a vehicle with a gel-forming agent and a bioadhesive agent; and a therapeutic agent dispersed or suspended in the vehicle.

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28-05-2015 дата публикации

Progesterone formulations

Номер: US20150148323A1
Принадлежит: TherapeuticsMD Inc

Various pharmaceutical formulations are disclosed herein. For example, a pharmaceutical formulation is disclosed comprising ultra-micronized progesterone.

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15-09-2022 дата публикации

PHARMACEUTICAL COMPOSITION FOR IMPROVING OR TREATING POST-SURGICAL HYPOPARATHYROIDISM AND TREATMENT METHOD USING THE SAME

Номер: US20220288076A1
Принадлежит:

The present invention relates to a pharmaceutical composition for improving or treating hypoparathyroidism caused by damage to parathyroid tissue and vascular tissue around the parathyroid gland due to surgery around the neck, and a method for treating post-surgical hypoparathyroidism using the same, and the composition can promote secretion of parathyroid hormone by containing a calcium-sensing receptor antagonist as an active ingredient to help the restoration of damaged parathyroid tissue through neovascularization and angiogenesis, and furthermore, can alleviate hypocalcemia, hyperphosphatemia, and hypercalciuria by increasing the concentration of blood parathyroid hormone to a normal range level. Administration of the composition can improve the quality of life of patients with hypoparathyroidism. 1. A pharmaceutical composition useful for improving or treating post-surgical hypoparathyroidism , said composition comprising a calcium-sensing receptor antagonist as an active ingredient.3. The composition of claim 1 , wherein the composition further comprises a pharmaceutically acceptable carrier claim 1 , adjuvant or diluent.4. The composition of claim 1 , wherein administration of the composition to a mammal increases the secretion of parathyroid hormone.5. A method for treating post-surgical hypoparathyroidism claim 1 , the method comprising administering the composition of to a mammal in need of functional restoration of a parathyroid gland damaged by surgery.6. The method of claim 5 , wherein the composition is orally administered at a concentration of 1 to 30 mg/mL.7. The method of claim 5 , wherein the method increases the concentration of blood parathyroid hormone in the mammal. The present invention relates to a pharmaceutical composition for improving or treating hypoparathyroidism caused by damage to parathyroid tissue and vascular tissue around the parathyroid gland due to surgery around the neck, and a method for treating post-surgical ...

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15-09-2022 дата публикации

ORAL DISODIUM PYROPHOSPHATE FOR USE IN REDUCING CALCIFICATION

Номер: US20220288115A1
Принадлежит:

The current invention relates to use of oral disodium pyrophosphate for preventing and/or reducing tissue calcification, particularly soft tissue calcification, and/or diseases or disorders characterized by low plasma PPi levels, as, e.g., occurs in chronic kidney disease (CKD), end-stage renal disease (ESRD), generalized arterial calcification of infancy (GACI), Pseudoxanthoma elasticum (PXE), Arterial Calcification Due to Deficiency of CD73 (ACDC), Ehlers-Danlos syndrome, arteriosclerosis obliterans, venous calcifications, crystal deposition disorders, calcification resulting from neurological disorders, calcinosis universalis, calcinosis circumscripta, scleroderma, dermatomyositis, systemic lupus erythematosus, hyperparathyroidism, neoplasms, milk-alkali syndrome, hypervitaminosis D, tumoral calcinosis, hypophosphatemic rickets, ossification of the posterior longitudinal ligament of the spine, myocardial ischemia, joint calcification, heterotropic ossification of traumatized muscle, angioid streaks, diabetes mellitus type II, cardiovascular disorder, calciphylaxis, calciphylaxis secondary to chronic kidney disease, calcific uremic arteriolopathy or atherosclerosis. 1. Disodium pyrophosphate for use as a medicament , wherein said disodium pyrophosphate is administered in oral form.2. Disodium pyrophosphate for use in preventing and/or treating diseases or disorders characterized by calcification , particularly tissue calcification , particularly soft tissue calcification , or diseases or disorders characterized by low plasma inorganic pyrophosphate (PPi) levels , wherein said disodium pyrophosphate is administered in oral form.3. Disodium pyrophosphate for use according to claim 2 , wherein the soft tissue calcification is vascular calcification such as arterial calcification or intimal calcification.4. Disodium pyrophosphate for use according to claim 2 , wherein the tissue calcification is in a subject having ENPP1 deficiency claim 2 , chronic kidney disease ( ...

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15-09-2022 дата публикации

GNRH ANTAGONISTS FOR THE TREATMENT OF ESTROGEN-DEPENDENT DISORDERS

Номер: US20220288154A1
Принадлежит:

The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month, over the course of an extended treatment period, such as a treatment period having a duration of multiple years. Advantageously, using the compositions and methods of the present disclosure, the GnRH antagonist may be administered to a patient over a lengthy treatment period without inducing adverse side effects, such as a loss in bone mineral density, which is otherwise known to be a risk associated with GnRH antagonism. 1. A method of treating an estrogen-dependent disease in a human patient in need thereof , the method comprising periodically administering to the patient a therapeutically effective amount of a gonadotropin-releasing hormone (GnRH) antagonist over the course of a treatment period having a duration of at least 52 weeks.2. The method of claim 1 , wherein the estrogen-dependent disease is uterine fibroids.3. A method of reducing the volume of menstrual blood loss in a human patient diagnosed as having uterine fibroids claim 1 , the method comprising periodically administering to the patient a therapeutically effective amount of a GnRH antagonist over the course of a treatment period having a duration of at least 52 weeks.4. A ...

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16-05-2019 дата публикации

Natural combination hormone replacement formulations and therapies

Номер: US20190142844A1
Принадлежит: TherapeuticsMD Inc

Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.

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31-05-2018 дата публикации

Substantially Testosterone Free Compositions

Номер: US20180147246A1
Принадлежит:

1. A therapeutic composition, substantially free of testosterone, comprises 1. A therapeutic composition , in the absence of testosterone , comprising{'i': 'bulbine natalensis', '(a) at least one compound present in a therapeutically effective amount to increase testosterone levels when administered to a mammal; and'}{'i': 'bulbine natalensis', '(b) a topical transdermal pharmaceutical carrier effective for the therapeutic delivery of said'}2bulbine natalensis. The composition according to claim 1 , wherein said compound is present in an amount sufficient to compensate for a reduction in said mammal's natural testosterone production and/or said mammal's blood serum testosterone level.3. The composition according to claim 1 , wherein said mammal has low claim 1 , insufficient or deficient testosterone levels claim 1 , and wherein the topical administration of said composition to said mammal results in an increase in testosterone levels in said mammal.4. (canceled)5. The composition according to claim 3 , wherein a mammal with testosterone deficiency has a testosterone blood serum level of less than 300 ng/dl or a mammal with testosterone insufficiency has a testosterone blood serum level in the range of about 300 ng/dl to about 400 ng/dl or a mammal with low testosterone which is a testosterone blood serum level lower than normal for said mammal.6bulbine natalensis. The composition according to claim 1 , wherein said topical transdermal pharmaceutical carrier results in transdermal delivery of the in therapeutic amounts into the skin in the absence of irritating penetration enhancers such as alcohols claim 1 , glycols claim 1 , DMSO (dimethyl sulfoxides) claim 1 , or terpenes.7bulbine natalensisbulbine natalensis, anthericum latifoliumbulbine natalensisbulbine natalensisbulbine. The composition according to claim 1 , wherein said compound is selected from the group consisting of L.f. claim 1 , baker claim 1 , baker stem extract claim 1 , broad-leaved claim 1 , ...

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16-05-2019 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20190144387A1

This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 4. The compound of claim 1 , wherein W claim 1 , W claim 1 , W claim 1 , W claim 1 , W claim 1 , and Ware CH.5. The compound of claim 1 , wherein Wis N and W claim 1 , W claim 1 , W claim 1 , W claim 1 , and Ware CH.6. The compound of claim 1 , wherein Wis N and W claim 1 , W claim 1 , W claim 1 , W claim 1 , and Ware CH.7. The compound of claim 1 , wherein Wis N and W claim 1 , W claim 1 , W claim 1 , W claim 1 , Ware CH.8. The compound of claim 1 , wherein only one of X claim 1 , X claim 1 , X claim 1 , X claim 1 , and Xare N.9. The compound of claim 1 , wherein Xor Xis N.10. The compound of claim 1 , wherein Xor Xis N.11. The compound of claim 1 , wherein Xis N.12. The compound of claim 1 , wherein Xis N and X claim 1 , X claim 1 , X claim 1 , and Xare CH.14. The compound of claim 1 , wherein Q is H claim 1 , NO claim 1 , COR claim 1 , alkyl claim 1 , alkoxy claim 1 , aryl claim 1 , CN claim 1 , CF claim 1 , F claim 1 , Cl claim 1 , Br or I.15. The compound of claim 1 , wherein Z is CN.16. The compound of claim 1 , wherein Y is Cl or CF.18. ...

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16-05-2019 дата публикации

METHOD FOR TREATING OR/AND PREVENTING CALCIUM DEFICIENCY-RELATED DISEASES

Номер: US20190144502A1
Принадлежит:

The present invention discloses a method for treating or/and preventing calcium deficiency-related diseases, which comprises administering a composition containing an effective amount of a peptide to a subject, wherein the peptide has an amino acid sequence as shown in SEQ ID NO. 3. The calcium ions are allowed to bind to the peptide and enter the cells of the patient, to achieve the effect of treating or/and preventing calcium deficiency-related diseases. 1. A method for treating or/and preventing calcium deficiency-related diseases , comprising administering a composition containing an effective amount of a peptide to a subject , wherein the peptide has an amino acid sequence as shown in SEQ ID NO. 3.2. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the peptide is selected from the group consisting of SEQ ID NO.1 claim 1 , SEQ ID NO.2 claim 1 , and SEQ ID NO.3.3. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the composition is a pharmaceutical product.4. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the composition is a nutritional supplement.5. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the composition is a bone loss inhibitor.6. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the composition is a bone growth promoter.7. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the composition is a functional food.8. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the calcium deficiency-related diseases is osteoporosis.9. The method for treating or/and preventing calcium deficiency-related diseases according to claim 1 , wherein the subject ...

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07-05-2020 дата публикации

Treatment of Genital Psoriasis

Номер: US20200140537A1
Принадлежит:

Methods of treating genital psoriasis, genital pruritus and genital psoriasis sexual activity impairment with anti-IL17A antibodies, including dose regimens and pharmaceutical formulations of anti-IL17A antibodies for use in the treatment of genital psoriasis, genital pruritus and genital psoriasis sexual activity impairment. 1. A method of treating a patient in need of treatment for genital psoriasis (GenPs) comprising administering to said patient a therapeutically effective amount of an anti-IL17A antibody , or a pharmaceutical formulation thereof ,wherein the anti-IL17A antibody comprises a light chain variable region (LCVR) and a heavy chain variable region (HCVR), wherein said LCVR is the amino acid sequence of SEQ ID NO: 2 and said HCVR is the amino acid sequence of SEQ ID NO: 3.2. The method of claim 1 , wherein the anti-IL17A antibody comprises a light chain (LC) and a heavy chain (HC) claim 1 , wherein said LC is the amino acid sequence of SEQ ID NO: 4 and said HC is the amino acid sequence of SEQ ID NO: 5.3. The method of claim 2 , wherein the anti-IL17A antibody is ixekizumab.4. The method of claim 1 , wherein the patient possesses a static physician's global assessment of genitalia (sPGA-G) of greater than sPGA-G 1.5. The method of claim 4 , wherein the patient possesses a sPGA-G of greater-than-or-equal-to sPGA-G 3.6. The method of claim 1 , wherein the patient does not need treatment for psoriasis at other body regions.7. The method of claim 1 , wherein the patient has less than 10% body-surface area (BSA) psoriasis involvement.8. The method of claim 7 , wherein the patient has less-than-or-equal to 3% BSA psoriasis involvement.9. The method of claim 1 , wherein the patient has at least one of genital fissure and genital erosion.10. The method of claim 1 , wherein administering comprises administering a pharmaceutical formulation of the anti-IL17A antibody claim 1 , said pharmaceutical formulation comprising the anti-IL17A antibody at a concentration ...

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21-08-2014 дата публикации

Method of treating thermoregulatory disfunction with paroxetine

Номер: US20140235674A1
Принадлежит: Noven Therapeutics LLC

The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.

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09-06-2016 дата публикации

Therapeutic agents for reducing parathyroid hormone levels

Номер: US20160159860A1
Принадлежит: Kai Pharmaceuticals Inc

Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X 1 -X 2 -X 3 -X 4 -X 5 -X 6 -X 7 , wherein the X 1 subunit comprises a thiol-containing moiety and the distribution of charge on the X 2 -X 7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

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07-06-2018 дата публикации

ORODISPERSIBLE TABLET CONTAINING ESTETROL

Номер: US20180153801A1
Принадлежит: Mithra Pharmaceuticals S.A.

The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit containing at least 100 μg of an estetrol component selected from estetrol, estetrol esters and combinations thereof; wherein the solid dosage unit can be obtained by a process comprising: ⋅providing an aqueous liquid comprising water, estetrol component and optionally one or more other pharmaceutically acceptable ingredients; ⋅mixing 1 part by weight of the aqueous liquid with 0.5-20 parts by weight of the carrier particles to produce wet particles; ⋅removing water from the wet particles to produce loaded particles; ⋅optionally mixing the loaded particles with one or more tabletting excipients; and ⋅forming the loaded particles or the mixture of loaded particles and the one or more tabletting excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration. 125-. (canceled)26. A process of making an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1 ,000 mg and containing at least 100 μg of an estetrol component selected from one or more of estetrol and estetrol esters , comprising:providing carrier particles having a volume median diameter of from 10 μm to 400 μm;providing an aqueous liquid comprising water in an amount of at least 60 wt. %, the estetrol component in an amount of 1-40 wt. %, and, optionally, one or more other pharmaceutically acceptable ingredients in an amount of 0-40 wt. %;mixing 1 part by weight of the aqueous liquid with 0.5-20 parts by weight of the carrier particles to produce wet particles;removing water from the wet particles to produce loaded particles;optionally, mixing the loaded particles with one or more tabletting excipients to produce a mixture; andforming the loaded particles or the mixture into a solid dosage unit having a weight between 30 and 1,000 mg and containing at least 100 μg ...

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07-06-2018 дата публикации

ORAL TESTOSTERONE TRIDECANOATE THERAPY

Номер: US20180153905A1
Принадлежит: LIPOCINE INC.

The present disclosure provides methods and compositions for testosterone replacement therapy. The methods and compositions employ a fixed dose dosing regimen that does not require titration or dose adjustments and that can provide a therapeutically effective amount of a testosterone ester while avoiding unacceptably high testosterone levels. 1. A method of restoring serum testosterone levels to a normal eugonadal range in a male having a condition associated with a deficiency or absence of endogenous testosterone , comprising orally administering a pharmaceutical composition comprising a therapeutically effective amount of testosterone tridecanoate (T13) in a fixed dose administration regimen with food.2. The method of claim 1 , wherein the composition further comprises an additive.3. The method of claim 1 , wherein the fixed dose administration regimen provides a total daily dose of T13 of from 750-1150 mg.4. The method of claim 1 , wherein the fixed dose administration regimen comprises administering said composition once or twice daily.5. The method of claim 1 , wherein said composition is in the form of a hard or soft capsule.6. The method of claim 1 , wherein a unit dosage form of the composition comprises about 100-500 mg T13.7. The method of claim 1 , further comprising measuring a therapy discontinuation criterion that indicates an advised discontinuation of therapy where serum testosterone (T) levels are consistently >2500 ng/dl.8. A method of restoring daily average serum testosterone (C) to a normal eugonadal range in at least 75% of males in a population having a condition associated with a deficiency or absence of endogenous testosterone claim 1 , comprising oral administration of an oral dosage form comprising a therapeutically effective amount of testosterone tridecanoate (T13) in a fixed dose administration regimen with food.9. The method of claim 8 , wherein the oral dosage form further comprises an additive.10. The method of claim 8 , wherein the ...

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08-06-2017 дата публикации

Nk3 receptor antagonist compound (nk3ra) for use in a method for the treatment of polycystic ovary syndrome (pcos)

Номер: US20170157109A1
Принадлежит: AstraZeneca AB

A method for treating polycystic ovarian syndrome and related conditions with a compound (I): or a pharmaceutically acceptable salt thereof.

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07-06-2018 дата публикации

Azasteroidal Mimics

Номер: US20180155299A1
Принадлежит: Florida International University FIU

An azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic is formed via an oxocycloalkenyl isoxazolium anhydrobase and its dimer. The dimer can be used to form mono- and dihydrazones, which can be an azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic. A method of preparation of the dimer and the azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic occurs with hydrazonation and, optionally, a subsequent dehydrazonation. The dimer can be converted by inserting a nitrogen atom into the six membered ring of to a C-17 position cyclohexenone moiety of the dimer to yield a reduced tetrazolo[1,5-a]azepin-8-yl group. A subsequent hydrozone formation at a benzylic ketone can be carried out to generate an azasteroid mimic with a (triazol-4-yl)imino substituent. Monohydrazones can be converted to their thione equivalents.

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23-05-2019 дата публикации

NOVEL COMPOUND PROMOTING OSTEOBLAST DIFFERENTIATION AND INHIBITING ADIPOCYTE DIFFERENTIATION, PREPARATION METHOD THEREOF AND APPLICATION THEREOF

Номер: US20190152935A1
Принадлежит: SUNG KYUN BIOTECH CO., LTD.

The present disclosure relates to a compound having the activity of promoting osteoblast differentiation and inhibiting adipocyte differentiation and a preparation method thereof. The novel compound of the present disclosure increases the expression of the gene ALP involved in the differentiation of osteoblasts, regulates expression of the genes PPARγ, aP2 and CD36 involved in the differentiation of adipocytes, increases bone mineral density (BMD) in an ovariectomized osteoporosis animal model and decreases adipocytes in the bone marrow. Therefore, it can be used as an active ingredient of a medication or a health functional food useful for metabolic bone disease or obesity. 2. The composition for preventing or treating metabolic bone disease according to claim 1 , wherein each of R claim 1 , R claim 1 , Rand R claim 1 , which may be identical or different from each other claim 1 , is independently selected from a group consisting of C-Calkyl and C-Calkoxy claim 1 , and{'sub': 2', '5, 'each of Rand R, which may be identical or different from each other, is independently selected from a group consisting of hydrogen, hydroxy, halogen and trifluoromethyl.'}4. The composition for preventing or treating metabolic bone disease according to claim 1 , which promotes osteoblast differentiation and inhibits adipocyte differentiation.5. The composition for preventing or treating metabolic bone disease according to claim 4 , which prevents or treats obesity and metabolic bone disease at the same time.7. The health functional food for improving or preventing metabolic bone disease according to claim 6 , wherein each of R claim 6 , R claim 6 , Rand R claim 6 , which may be identical or different from each other claim 6 , is independently selected from a group consisting of C-Calkyl and C-Calkoxy claim 6 , and{'sub': 2', '5, 'each of Rand R, which may be identical or different from each other, is independently selected from a group consisting of hydrogen, hydroxy, halogen and ...

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21-05-2020 дата публикации

MATERIAL FOR IMPROVING ENDOMETRIOSIS AND METHOD FOR PRODUCING THE SAME

Номер: US20200155499A1
Принадлежит:

A material using an aglycone type isoflavone which has the effect of improving the endometriosis is provided. Also, a method of producing an endometriosis improving material includes: inoculating legumes with aspergillus oryzae and koji treating them, and hydrolyzing the proteins in the products by hydrolyzing the products of the koji treatment and decomposing glycosides of the isoflavone compounds in the legumes, then producing isoflavone compounds containing a large amount of aglycone, and producing a material for improving endometriosis containing aglycone type isoflavone from the legumes. 1. A material for improving endometriosis comprising ,an aglycon type isoflavone having an action of improving endometriosis.2. The material for improving endometriosis according to claim 1 , wherein the action to improve the endometriosis comprising at least one of the following actions;To suppress proliferation of endometriotic stromal cells,Reducing gene expression of IL-6, IL-8, aromatase and COX-2 in endometriosis cells,Decrease the protein level of PGE2 in endometriosis cells,Reducing aromatase enzyme activity of endometriosis cells,In endometriosis cells, suppressing the phosphorylation IκB promoted by TNF-α,Inhibiting nuclear uptake of p65 by fluorescence immunostaining of endometriosis cells,PHTPP as ERβantagonist suppresses the growth inhibitory effect of aglycone type isoflavone against endometriosis cells,ERβ knockdown cells counteract the effect of aglycone type isoflavones on endometriosis cells,MPP as ERαantagonist does not counteract the effect of AglyMax on endometriosis cells to improve endometriosis,Reducing gene expression of SGK1 in endometriosis cells,Inhibit cyst formation in endometriosis model mice,Reducing Ki67 staining rate in endometriosis cells.3. A method for producing the material for improving endometriosis characterized in that claim 1 ,inoculating legumes with aspergillus oryzae and koji treating them, and hydrolyzing the proteins in the ...

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29-09-2022 дата публикации

Use of an Anti-P-selectin Antibody

Номер: US20220306749A1
Принадлежит: NOVARTIS AG

The invention relates to a method of treating priapism in a patient in need of such treatment, comprising administering a pharmaceutically effective amount of an anti-P-selectin antibody or a binding fragment thereof to said patient, especially wherein the patient is suffering from Sickle Cell Disease (SCD), and related invention embodiments (uses, methods, pharmaceutical preparations and use in the preparation of pharmaceutical preparations).

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22-06-2017 дата публикации

Treatment of androgen deprivation therapy associated symptoms

Номер: US20170172992A1
Автор: Charles Thomas Benson
Принадлежит: Eli Lilly and Co

The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I: [Formula should be inserted here] or a pharmaceutically acceptable salt thereof.

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06-06-2019 дата публикации

NUTRITIONAL SUPPLEMENTS FOR INCREASING MALE TESTOSTERONE LEVELS

Номер: US20190167750A1
Автор: Damaj Bassam
Принадлежит:

The invention provides compositions and methods that are effective to boost testosterone levels in a mammal. 1. A composition comprising:Vitamin B6MagnesiumZinc{'i': 'Piper Nigrum', '(Black Pepper or Bioperine)'}{'i': Rhodiola', 'Rhodiola Rosea, '()'}DIM (Diindolymethane){'i': 'Eurycorna Longifolia', 'TongkatAli ()'}Fenugreek Seed Extract and{'i': 'Cordyceps Sinesis', 'Mushroom.'}2. A composition comprising:Vitamin B6MagnesiumZinc{'i': 'Piper Nigrum', '(Black Pepper or Bioperine)'}{'i': Rhodiola', 'Rhodiola Rosea, '()'}DIM (Diindolymethane){'i': 'Eurycorna Longifolia', 'TongkatAli ()'}Fenugreek Seed Extract andAshwagandha Root Extract3. A composition comprising:Vitamin B6MagnesiumZinc{'i': 'Piper Nigrum', '(Black Pepper or Bioperine)'}{'i': Rhodiola', 'Rhodiola Rosea, '()'}DIM (Diindolymethane){'i': 'Eurycorna Longifolia', 'TongkatAli ()'}Fenugreek Seed Extract{'i': 'Cordyceps Sinesis', 'Mushroom and'}Ashwagandha Root Extract4Piper Nigrum,. A unit dosage form comprising at least about 18 mgVitamin B6MagnesiumZinc{'i': Rhodiola', 'Rhodiola Rosea, '()'}DIM (Diindolymethane){'i': 'Eurycorna Longifolia', 'TongkatAli ()'}Fenugreek Seed Extract{'i': 'Cordyceps Sinesis', 'Mushroom and'}Ashwagandha Root Extract.5Piper Nigrum.. The unit dosage form of that comprises at least about 19 mg6Piper Nigrum.. The unit dosage form of that comprises at least about 20 mg7Cordyceps Sinesis. The unit dosage form of that comprises about 500 mg Mushroom.8. The unit dosage form of that comprises about 100 mg Ashwagandha Root Extract.10Cordyceps Sinesis. The unit dosage form of that further comprises about 500 mg Mushroom.11. The unit dosage form of that further comprises about 100 mg Ashwagandha Root Extract.12. The unit dosage form of that further comprises about 100 mg Ashwagandha Root Extract.13. The unit dosage form of wherein the term about claim 12 , at each occurrence claim 12 , means ±5% of the associated value.15. The unit dosage form of that further comprises microcrystalline ...

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06-06-2019 дата публикации

COMPOSITION FOR PROPHYLAXIS OR TREATMENT OF IL-8 RELATED DISEASES

Номер: US20190169286A1
Принадлежит:

For example, therapeutic methods and the like for novel IL-8-related diseases using an IL-8 signal inhibitor are provided. Alternatively, for example, therapeutic methods and the like for known or novel IL-8-related diseases using a novel anti-IL-8 antibody are provided. 1. A composition for treating or preventing an IL-8-related disease , which comprises as an active ingredient an isolated anti-IL-8 antibody that binds to human IL-8 , wherein the IL-8-related disease is selected from the group consisting of:endometriosis; adenomyosis; dysmenorrhea; adhesion; fibrotic diseases; pain in endometriosis, adenomyosis, or dysmenorrhea; infertility; and pain resulting from adhesion, fibrosis, or inflammation; [ (a) HVR-H1 comprising the amino acid sequence of SEQ ID NO: 23,', '(b) HVR-H2 comprising the amino acid sequence of SEQ ID NO: 24,', '(c) HVR-H3 comprising the amino acid sequence of SEQ ID NO: 25,', '(d) HVR-L1 comprising the amino acid sequence of SEQ ID NO: 26,', '(e) HVR-L2 comprising the amino acid sequence of SEQ ID NO: 27, and', '(f) HVR-L3 comprising the amino acid sequence of SEQ ID NO: 28;, '(1) an anti-IL-8 antibody which binds to IL-8 in a pH-dependent manner, and comprises at least one amino acid substitution in at least one of, (a) HVR-H1 comprising the amino acid sequence of SEQ ID NO: 23,', '(b) HVR-H2 comprising the amino acid sequence of SEQ ID NO: 24,', '(c) HVR-H3 comprising the amino acid sequence of SEQ ID NO: 25,', '(d) HVR-L1 comprising the amino acid sequence of SEQ ID NO: 26,', '(e) HVR-L2 comprising the amino acid sequence of SEQ ID NO: 27, and', '(f) HVR-L3 comprising the amino acid sequence of SEQ ID NO: 28,, '(2) an anti-IL-8 antibody which binds to IL-8 in a pH-dependent manner, and comprises at least one amino acid substitution in at least one of, 'wherein the anti-IL-8 antibody at least comprises amino acid substitutions of:', 'tyrosine at position 3 in the amino acid sequence of SEQ ID NO: 25, asparagine at position 1 and leucine at ...

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18-09-2014 дата публикации

Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same

Номер: US20140274986A1
Принадлежит: Clarus Therapeutics Inc

A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

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16-07-2015 дата публикации

Novel benzopyran compounds, compositions and uses thereof

Номер: US20150197506A1
Принадлежит: Olema Pharmaceuticals Inc

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.

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06-07-2017 дата публикации

Method for preparing amg 416

Номер: US20170190739A1
Принадлежит: AMGEN INC

A method for preparing AMG 416, or a pharmaceutically acceptable salt thereof, is provided. AMG 416 is a synthetic, eight amino-acid selective peptide agonist of the calcium sensing receptor. It is being developed as an intravenous treatment of secondary hyperparathyroidism (SHPT) in hemodialysis patients with chronic kidney disease—mineral and bone disorder (CKD-MBD).

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14-07-2016 дата публикации

Process for Preparing Cinacalcet and Pharmaceutically Acceptable Salts Thereof

Номер: US20160200664A1

The present patent application relates to a process for preparing cinacalcet or a pharmaceutically acceptable salt thereof, which comprises reacting 3-trifluoromethylbenzaldehyde having the following formula (II) with the phosphorus-comprising derivative having the following formula (III) in which R 1 and R 2 , which may be identical or different, are each a (C 1 -C 6 )alkyl group. The present invention also relates to the phosphorus-comprising derivative having the formula (III), to the use thereof and to the process for preparing same. The present invention also relates to the phosphate salt of cinacalcet and to uses thereof.

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25-09-2014 дата публикации

Abiraterone Acetate Formulation

Номер: US20140287039A1
Принадлежит: Iceutica Inc

Pharmaceutical compositions, including unit dosage forms, comprising fine particle abiraterone acetate with or without an antioxidant and or a sequestering agent as well as methods for producing and using such compositions are described.

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30-07-2015 дата публикации

Progesterone Receptor Modulators for Use in Preventing or Treating Androgen Mediated Diseases

Номер: US20150209373A1
Принадлежит: PregLem SA

The present invention relates generally to a progesterone receptor modulator, or any metabolite thereof for use in the prevention or treatment of androgen mediated diseases characterized in that said progesterone receptor modulator, or any metabolite thereof, is administered to a subject in need thereof.

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21-07-2016 дата публикации

Method of preparing microspheres

Номер: US20160206563A1
Автор: Shalabh Jain
Принадлежит: Hyalo Technologies LLC

Methods of preparing particles using a sonication device are disclosed. The methods include directing a particle forming solution containing a particle forming liquid and a particle forming agent as a stream into contact with a sonicating tip of a sonication device under conditions sufficient to transform the stream containing the particle forming solution into a plurality of droplets having a substantially uniform size. The plurality of droplets are contacted with a hardening solution under conditions sufficient to solidify the droplets into particles having a substantially uniform particle size which are then recovered. Particles made in accordance with the methods can be solid or semi-solid and range in size from sub-micron to over 100 microns in diameter.

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18-06-2020 дата публикации

Active ester derivatives of testosterone, compositions and uses thereof

Номер: US20200188412A1
Принадлежит: Acerus Biopharma Inc

The present invention relates to new compounds and compositions comprising active ingredient derivatives of testosterone, and novel testosterone derivatives, novel testosterone methods, novel testosterone compositions, novel testosterone articles of manufacture of pharmaceutical preparations and novel testosterone therapeutic uses thereof.32

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18-06-2020 дата публикации

Development of a standardized and effect-optimized herbal extract of wedelia chinensis and its use for treating disease

Номер: US20200188463A1
Принадлежит: Academia Sinica

A composition including a standardized Wedelia chinensis extract and a method of treating an androgen-stimulated disorder with such a composition. Also provided are a method for qualifying a standardized preparation of a Wedelia chinensis extract for treating an androgen-stimulated disorder and a method for treating said disorder with a thus qualified preparation.

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20-07-2017 дата публикации

Solid preparation

Номер: US20170202777A1
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a solid preparation wherein variation in weight is suppressed, a solid preparation wherein the active ingredient is stabilized, and a stabilization method thereof. A solid preparation containing (1) an active ingredient, (2) D-mannitol and (3) an alkaline earth metal salt selected from magnesium aluminometasilicate and calcium silicate. A method of stabilizing the active ingredient, including adding an alkaline earth metal salt selected from magnesium aluminometasilicate and calcium silicate.

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06-08-2015 дата публикации

Prodrug of Green Tea Epigallocatechin-3-Gallate (Pro-EGCG) for Use in the Treatment of Endometriosis

Номер: US20150216841A1

Method of treating endometriosis and related indications, comprising the administration of Pro-EGCG, a synthetic and derivative product of epigallocatechin-3-gallate [(−)-EGCG]. Use of Pro-EGCG in the manufacture of a medicament for treating endometriosis and related indications. Pro-EGCG for use in the treatment of endometriosis and related indications.

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25-06-2020 дата публикации

METHODS OF TREATING TESTOSTERONE DEFICIENCY

Номер: US20200197412A1
Принадлежит:

Methods of treating a testosterone deficiency or its symptoms with a pharmaceutical formulation of testosterone undecanoate are provided. 1. A method of treating conditions associated with a deficiency or absence of endogenous testosterone in a subject in need thereof comprising the steps of:administering to the subject a defined dose of an oral pharmaceutical composition comprising testosterone undecanoate solubilized in a carrier comprising at least one lipophilic surfactant and at least one hydrophilic surfactant, wherein the defined dose is 237 mg administered twice daily;collecting a blood sample from the subject;measuring the serum testosterone concentration in the subject; andincreasing the dose of testosterone undecanoate to 316 mg, administered twice daily, when the measured serum testosterone concentration in the subject is less than about 425 ng/dL,decreasing the dose of testosterone undecanoate to 198 mg, administered twice daily, when the measured serum testosterone concentration in the subject is greater than about 970 ng/dL, ormaintaining the dose of testosterone undecanoate when the measured serum testosterone concentration in the subject is between about 425 ng/dL and about 970 ng/dL.2. The method of claim 1 , wherein the serum testosterone concentration is measured four to eight hours after administering the oral pharmaceutical composition.3. The method of claim 1 , wherein the oral pharmaceutical composition comprises about 19.8 percent by weight of solubilized testosterone undecanoate claim 1 , about 51.6 percent by weight of oleic acid claim 1 , and about 16.1 percent by weight of polyoxyethylene (40) hydrogenated castor oil.4. The method of claim 3 , wherein the oral pharmaceutical composition further comprises about 10 percent by weight of borage seed oil and about 2.5 percent by weight of peppermint oil.5. The method of claim 1 , wherein the testosterone concentrations are measured in serum from a blood sample collected in a plain tube drawn ...

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25-06-2020 дата публикации

METHODS OF TREATING TESTOSTERONE DEFICIENCY

Номер: US20200197413A1
Принадлежит:

Methods of treating a testosterone deficiency or its symptoms with a pharmaceutical formulation of testosterone undecanoate are provided. 1. A method of treating conditions associated with a deficiency or absence of endogenous testosterone in a subject in need thereof comprising the steps of:administering to the subject a defined dose of an oral pharmaceutical composition comprising testosterone undecanoate solubilized in a carrier comprising at least one lipophilic surfactant and at least one hydrophilic surfactant, wherein the defined dose is 198 mg administered twice daily;collecting a blood sample from the subject;measuring the serum testosterone concentration in the subject; andincreasing the dose of testosterone undecanoate to 237 mg, administered twice daily, when the measured serum testosterone concentration in the subject is less than about 425 ng/dL,decreasing the dose of testosterone undecanoate to 158 mg, administered twice daily, when the measured serum testosterone concentration in the subject is greater than about 970 ng/dL, ormaintaining the dose of testosterone undecanoate when the measured serum testosterone concentration in the subject is between about 425 ng/dL and about 970 ng/dL.2. The method of claim 1 , wherein the serum testosterone concentration is measured four to eight hours after administering the oral pharmaceutical composition.3. The method of claim 1 , wherein the oral pharmaceutical composition comprises about 19.8 percent by weight of solubilized testosterone undecanoate claim 1 , about 51.6 percent by weight of oleic acid claim 1 , and about 16.1 percent by weight of polyoxyethylene (40) hydrogenated castor oil.4. The method of claim 3 , wherein the oral pharmaceutical composition further comprises about 10 percent by weight of borage seed oil and about 2.5 percent by weight of peppermint oil.5. The method of claim 1 , wherein the testosterone concentrations are measured in serum from a blood sample collected in a plain tube drawn ...

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05-08-2021 дата публикации

NOVEL USES

Номер: US20210236506A1
Автор: Trower Mike
Принадлежит: KaNDy Therapeutics Limited

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. 110-. (canceled)11. A method of treating vasomotor symptoms in a human in need thereof , comprising administering to the human an effective amount of 2-[3 ,5-bis(trifluoromethyl)phenyl]-N-{-(4-fluoro-2-methylphenyl)-6-[(7S ,9aS)-7-(hydroxymethyl)hexahydropyrazino[2 ,1-c][1 ,4]oxazin-8(1H)-yl]-3-pyridinyl}-N ,2-dimethylpropanamide.12. The method of claim 11 , wherein the 2-[3 claim 11 ,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S claim 11 ,9aS)-7-(hydroxymethyl)hexahydropyrazino[2 claim 11 ,1-c][1 claim 11 ,4]oxazin-8(1H)-yl]-3-pyridinyl}-N claim 11 ,2-dimethylpropanamide is in crystalline anhydrate form.13. The method of claim 11 , wherein the 2-[3 claim 11 ,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S claim 11 ,9aS)-7-(hydroxymethyl)hexahydropyrazino[2 claim 11 ,1-c][1 claim 11 ,4]oxazin-8(1H)-yl]-3-pyridinyl}-N claim 11 ,2-dimethylpropanamide is in crystalline anhydrate Form 1 and has characteristic 2 theta angles occurring at 4.3±0.1 claim 11 , 7.9±0.1 claim 11 , 9.8±0.1 claim 11 , 10.7±0.1 claim 11 , 10.8±0.1 claim 11 , 13.3±0.1 claim 11 , 14.0±0.1 claim 11 , and 15.1±0.1 degrees.14. The method of claim 11 , wherein the 2-[3 claim 11 ,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S claim 11 ,9aS)-7-(hydroxymethyl)hexahydropyrazino[2 claim 11 ,1-c][1 claim 11 ,4]oxazin-8(1H)-yl]-3-pyridinyl}-N claim 11 ,2-dimethylpropanamide is in crystalline anhydrate Form 1 and has d-spacing at 20.4 claim 11 , 11.1 claim 11 , 9.0 claim 11 , 8.3 claim 11 , 8.2 claim 11 , 6.6 claim 11 , 6.3 claim 11 , and 5.9 Angstroms.15. The method of claim 11 , wherein the 2-[3 claim 11 ,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S claim 11 ,9aS)-7-(hydroxymethyl)hexahydropyrazino[2 claim 11 ,1-c][1 claim 11 ,4]oxazin-8(1H)-yl]-3- ...

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05-08-2021 дата публикации

SYNERGISTIC HERBAL COMPOSITIONS FOR TESTOSTERONE BOOSTING

Номер: US20210236572A1
Принадлежит:

Synergistic herbal compositions comprising combination of a first ingredient selected from the extract(s), fraction(s), active compound(s) and phytochemicals or mixtures thereof derived from the plant parts of and a second ingredient selected from the extract(s), fraction(s), active compound(s) and phytochemicals or mixtures thereof derived from the plant parts of for improving testosterone levels. The invention further provides the method of obtaining at least one health benefit tin related to enhanced anabolic and androgenic activities in the body selected from improving testosterone levels, energy levels, sustained energy, vigor, stamina, healthy aging, cellular longevity, muscle mass, muscle strength sexual function (libido and erectile function) and psychological well-being (mood and focus); and reducing stress in humans and alleviating the symptoms associated with the low levels of testosterone in humans such as loss of libido, loss of erectile function, abdominal obesity, decreased muscle mass and strength, fatigue, mood swing, decreased bone density, decreased motivation, and decreased memory and concentration. 114-. (canceled)15. A synergistic herbal composition comprising a combination of:{'i': 'Punica granatum', 'from 10% to 90% of a first ingredient comprising an extract of ; and'}{'i': 'Theobroma cacao;', 'from 10% to 90% of a second ingredient comprising an extract of'}based on the combined weight of the first ingredient and the second ingredient;wherein the herbal composition contains the combination in an amount effective for obtaining at least one health benefit related to enhanced anabolic and androgenic activities in a patient in need thereof.16. The synergistic herbal composition as claimed in claim 15 , wherein the herbal composition contains punicalagins in the concentration range of 0.1% to 20% by weight of the composition and theobromine in the concentration range of 0.1% to 10% by weight of the composition.17. The synergistic herbal ...

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09-10-2014 дата публикации

Methods of treating testosterone deficiency

Номер: US20140303129A1
Принадлежит: Clarus Therapeutics Inc

Methods of treating a testosterone deficiency or its symptoms with a pharmaceutical formulation of testosterone esters are provided. The methods are designed toprovide optimum serum testosterone levels over an extended period.

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