50 results about "Oestrogen deficiency" patented technology

The present invention relates to compositions containing unconjugated estrogens and methods of their use in the treatment of conditions associated with hypoestrogenism or reduced estrogen levels in females.

One aspect of the present invention relates to a method of hormone replacement in mammals, which method comprises the oral administration of an estrogenic component and a progestogenic component to a mammal in an effective amount to prevent or treat symptoms of hypoestrogenism, wherein the estrogenic component is selected from the group consisting of substances represented by the above formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and / or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and a progestogenic component as well as an androgenic component.

A nasal spray formulation for use in female contraception or in the treatment of benign gynecological disorders is described. The nasal preparation is comprised of a GnRH compound and an estrogenic compound in the form of a water-soluble complex with a water-soluble cyclodextrin. The preparation effectively suppresses ovarian estrogen and progesterone production, and prevents signs and symptoms of estrogen deficiency, without a significant increase in the risk of endometrial hyperplasia.

A dipsacus root total saponin is disclosed in the present invention, its weight percent accounts for 60 percent to 95 percent of dipsacus root medicinal materials extraction gross, and in dipsacus root total saponin 3-O-alpha-L-arabinopyranosyl-hederagenin-28-O-beta-D-glucopyranosyl(1-6)-beta-D-glucopyranoside accounts for 30 percent to 90 percent of dipsacus root medicinal materials extraction. A dipsacus root extracting method and its application in preparing medicine for treating cervical vertebra, arthritis, hyperosteogeny or osteoporosis are also disclosed in the present invention. By researching pharmacologic effect of the dipsacus root total saponin, finding that the dipsacus root total saponin prepared by the present invention has obvious anti-inflammation, pain-relieving, increasing carotid blood flow and decreasing blood viscosity, treating oestrogen deficiency type osteoporosis function, and has obvious prevention and cure for experimental cervical spondylosis, arthritis, hyperosteogeny or osteoporosis.

The use of a lignan, which is a plant lignan, a metabolite thereof or a combination of both, for the manufacture of a composition for preventing or alleviating of symptoms relating to estrogen deficiency in an individual. Also disclosed is the use of a plant lignan capable of being a precursor for enterolactone or another metabolite of the plant lignan, for the manufacture of a composition useful for increasing the level of enterolactone or another metabolite of a plant lignan in an individual's serum, where the individual suffers from or is at risk of estrogen deficiency.

A pharmaceutical composition comprises at least one estrogenic compound, the composition being adapted for application in a unit dose amount to a vulvovaginal surface and having at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to the vulvovaginal surface, wherein the at least one estrogenic compound is present in an amount of about 5 to about 1000 μg estradiol equivalent per unit dose of the composition, and upon application of the composition to the vulvovaginal surface the at least one estrogenic compound is released over a period of about 3 hours to about 30 days. The composition is useful for vulvovaginal administration to treat atrophic vaginitis or a disorder associated therewith, for example in a menopausal or postmenopausal woman. A method for treating a hypoestrogenism-related condition of the urogenital system of a female patient comprises intravaginal administration of at least one estrogenic compound according to a treatment regimen wherein a series of compositions releasing a progressively increasing daily amount of the at least one estrogenic compound is administered over a period of at least about 1 month.

The present invention relates to a method of treating or preventing estrogen-sensitive tumours in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consisting of:substances represented by the following formulain which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and / or precursors.The estrogenic component according to the invention does not have undesirable proliferative effects on breast and / or endometrial tissue and displays sufficient estrogenicity to prevent that its administration will lead to hypoestrogenism and / or climacteric complaints.Other aspects of the invention relate to pharmaceutical compositions, drug delivery systems and kits comprising the aforementioned estrogenic component in combination with an estrogen suppressant.

The present invention relates to a method of treating or preventing estrogen-sensitive tumours in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and / or precursors. The estrogenic component according to the invention does not have undesirable proliferative effects on breast and / or endometrial tissue and displays sufficient estrogenicity to prevent that its administration will lead to hypoestrogenism and / or climacteric complaints.

A general benzifuran is extracted from the Styrax plant and can be used to prepared injection, tablet, capsule, etc for preventing and treating early failure of ovary function, climacteric syndrome, osteoporosis, polycystic overy syndrome, acyesis, etc. Its preparing process is also disclosed.

The subject invention provides a use of tibolone and a SERM for the manufacture of a medicine for the treatment of an estrogen-deficiency related complaint and for the prevention of a recurrence of breast cancer in females suffering from, or at risk for breast cancer that exhibit the estrogen-deficiency related complaint.

The invention belongs to the technical field of medicines, and relates to a phenylindole derivative and application thereof.The phenylindole derivative comprises stereisomer and pharmaceutically-applicable salt of a phenylindole compound and has the structural formula (please see the formula in the description).The phenylindole derivative and the acid-added pharmaceutically-applicable salt of the phenylindole compound can be used in cooperation with existing medicines or used independently as an estrogen receptor regulator for treating or preventing various diseases related to estrogen functions such as bone loss, fractures, bone rarefaction, hectic fever, LDL cholesterol level rise, cardiovascular diseases, cognitive deficits, brain degeneration diseases, anxiety, depression caused by estrogen deficiency, sexual dysfunction, hypertension, retinal degeneration, cancers and especially osteoporosis.

The invention belongs to the technical field of medicine and relates to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and application thereof used as an estrogen receptor, in particular to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and a pharmaceutically acceptable salt, or a stereoisomer thereof and a prodrug as well as a pharmaceutically acceptable vector in compatibility or a diluent used as an estrogen receptor. The structural general formula of the derivative is disclosed in the specification, and in the structural formula, n R1 can be independently selected from a substituted or unsubstituted amido group, and R2 can be independently selected from H or an acetyl group. The derivative can be used for treating and preventing various diseases related to estrogen functions, such as diseases related to estrogen deficiency, estrogen sensitive cancer and hyperplasia, endometriosis, uterus myoma and osteoarthritis. Compounds or compositions of the derivative can also be independently used or combined with progestogen or a hormoneantagonist as a contraceptive.

The present invention relates to compounds having estrogenic activity selected from the group consisting of Loliolide, (4S,6S)-4-Hydroxy-6-nonadecyl-tetrahydro-pyran-2-one, (4R,6S)-4-Hydroxy-6-nonadecyl-tetrahydro-pyran-2-one and analogues thereof. The compounds of the present invention are selective estrogen receptor modulator, which can selectively activate ERβ and simultaneously express high estrogenic activity, and also can be applied as medical or food compositions to improve estrogen deficiency-related symptoms.

The invention relates to a traditional Chinese medicine for preventing estrogen deficiency from causing bone loss. The traditional Chinese medicine is prepared by the following original medicinal materials in parts by weight: 6-12 parts of rehmannia glutinosa, 4-6 parts of rhizoma dioscoreae, 4-6 parts of fructus lycii, 4-6 parts of semen cuscutae, 4-6 parts of colla corni cervi, 4-6 parts of colla plastri testudinis, 4-6 parts of fructus psoraleae, 4-6 parts of rhizoma drynariae, 2-4 parts of cortex eucommiae and 2-3 parts of liquorice. At the same time, the invention provides a preparation method of the traditional Chinese medicine with water extraction and alcohol precipitation. The traditional Chinese medicine takes into account symptoms and root causes all-around and applies tonification and purgation, and has an efficacy of nourishing kidney and strengthening essence and enriching marrow and strengthening bone altogether, so that the purpose of preventing estrogen deficiency from causing bone loss is achieved. The water extraction and alcohol precipitation is adopted by the preparation method of the traditional Chinese medicine to extract active ingredients and removing inactive ingredients in the original medicinal materials, and furthermore, the efficacy of the medicines is increased. The medicine has no obvious toxic and side effects and no obvious taboo when administrating.

The present invention is directed to an aromatase activating agent containing a plant selected from among mulberry bark, ginseng, cucumber, and phellodendron bark; or chlorella; or an extract of any of these ingredients. The aromatase activating agent of the present invention is highly safe to the human body, and useful as a drug or cosmetic composition for prevention, amelioration, or treatment of various lesions caused by estrogen deficiency.

The invention belongs to the technical field of medicine, and relates to piperazinyl-containing indole derivatives and medical application thereof. The phenyl indole derivatives comprise stereomers and pharmaceutically applicable salts of the compounds, and the structural general formula is disclosed in the specification. The piperazinyl-containing indole derivatives and pharmaceutically applicable acid-added salts of the compounds can be mixed with the existing drug or independently used as an estrogen receptor regulator for treating or preventing various estrogen-function-related diseases, such as bone loss, fracture, osteoporosis, hectic fever, LDL cholesterol level increase, cardiovascular diseases, cognitive impairment, brain degeneration diseases, anxiety, depression caused by deficiency of estrogen, sexual disorder, hypertension, retinosis and cancer, and especially osteoporosis.

The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC—OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl)or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC═H—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

The invention discloses an application of oltipraz in preparation of a product for preventing and treating osteoporosis. The application comprises any one of the following items: 1) preparing a product for preventing and treating osteoporosis caused by lack of active vitamin D; 2) preparing a product for preventing and treating osteoporosis caused by estrogen deficiency; and 3) preparing a product for preventing and treating osteoporosis caused by vitamin D receptor deficiency. According to the invention, through a test of supplementing an Nrf2 agonistoltiprazto a mouse model, the effect and related mechanism of oltipraz in preventing and treating osteoporosis caused by lack of active vitamin D are disclosed, and meanwhile, experimental and theoretical bases are provided for the application of oltipraz in preventing and treating osteoporosis caused by estrogen deficiency.

The invention discloses a new use of Eryngiolide A for curing rarefaction of bone. The rarefaction of bone is an important disease damaging human health, with aging of population, rarefaction of bone patients gradually increase, the rarefaction of bone causes huge burden on society, medical treatment and economy. Although relative experts and scholars at home and abroad attach great importance to prevent and cure the rarefaction of bone, the rarefaction of bone still lacks effective curing medicines. The fact that the Eryngiolide A has evident rarefaction of bone resisting function is discovered through in vivo test. Experiment results show that the Eryngiolide A can inhibit strengthening of bone conversion rate caused by ovariectomizing, reduce bone destruction, meanwhile can improve blood calcium concentration, and is benefit for deposition of bones. The Eryngiolide A has therapeutic effect on the deposition of rarefaction of bone caused by lack of the antiestrogen, and has no estrogen side effect.

The invention discloses application of punicalagin in preparing the medicine for preventing and curing postmenopausal osteoporosis, and further discloses a pharmaceutic preparation for preventing andcuring postmenopausal osteoporosis. The therapeutic action of punicalagin (PUN) on osteoporosis of ovariectomized mice is observed by applying the ovariectomized mouse osteoporosis model, the changesof the key indicators, including RANKL and CTSK, of osteoclast activation are evaluated, various indexes of osteoporosis are analyzed, and then therapeutic action mechanism of PUN on estrogen deficiency osteoporosis can be explained. According to the therapeutic action mechanism, after menopause, because of estrogen deficiency, the expression of RANKL can be up-regulated by bone resorption factors, the RANKL path is activated, osteoclasts are activated as a result, and at present, the mechanism is the important one of causing postmenopausal osteoporosis; and the application of PUN is a new wayfor preventing and curing postmenopausal osteoporosis because PUN can inhibit the path and thereby inhibiting osteoclast activation.

The invention belongs to the technical field of medicine and relates to 1-ethyl-4-[4-[5-hydroxy-2-(4-hydroxyphenyl)-3-methyl-1H-indole-1-yl]butyl]piperazine-2,3-dione as well as a medical application, a stereoisomer and pharmaceutically acceptable salt thereof. The structural formula of 1-ethyl-4-[4-[5-hydroxy-2-(4-hydroxyphenyl)-3-methyl-1H-indole-1-yl] butyl]piperazine-2,3-dione is represented in the specification; 1-ethyl-4-[4-[5-hydroxy-2-(4-hydroxyphenyl)-3-methyl-1H-indole-1-yl]butyl]piperazine-2,3-dione and pharmaceutically acceptable acid addition salt of the compound can be combined with existing drugs or can be independently used as an estrogen receptor modulator for treating or preventing various estrogen function related diseases such as bone loss, fracture, osteoporosis, hectic fever, LDL cholesterol level rise, cardiovascular disease, cognitive impairment, brain degeneration disease and anxiety, as well as depression, sexual dysfunction, hypertension, retinal degeneration and cancer caused by estrogen deficiency, especially osteoporosis.

The present invention relates to treating one or more estrogen related diseases while preventing or reducing the likelihood of developing estrogen deficiency related side effects, wherein said composition comprises administering a therapeutically effective amount of a Gn RH antagonist to a patient in need of said treatment, and wherein said amount of Gn RH antagonist is sufficient for providing a mean endogenous serum estradiol level of between about 20 pg / ml and 60 pg / ml, preferably between 30 pg / ml and 50 pg / m, in said patient in a treatment period of at least four weeks, without relying on “add-back” therapy. Said composition and method is simple, effective and will accordingly both increase patient acceptance and compliance of therapy.

The present invention relates to a composition for accelerating secretion of estrogen and regenerating tissue cells of female sexual organs, more particularly; to a composition for accelerating secretion of estrogen and regenerating tissue cells of female sexual organs in postmenopausal women comprising one or more of Platycodi Radix and Cynanchum wilfordii extract and / or Phlomis umbrosa extract. The present invention provides a composition, a pharmaceutical composition and a food composition capable of replacing estrogen, which comprise one or more selected from the group consisting of Platycodi Radix extract and Cynanchum wilfordii extract and / or Phlomis umbrosa extract. The composition of this invention comprised of the extracts of natural source shows little or no adverse effects such as cancer occurrence compared with estrogen-replacing agent used for conventional hormone replacement therapy; in addition, it has excellent effect on the regeneration and proliferation of tissue cells of female sexual organs, so that it is applicable to treatment of various disorders and diseases developed in postmenopausal women who are deficient in estrogen. Moreover, the composition of this invention has little impurities and high amount of active ingredients.

An application of oleanolic benzifuran and its heteroside in preparing the medicine for treating estrin deficiency, ovarian function sanilism, polycystic ovarian syndrome, climacteric syndrome, osteoporosis, ovarian hypofunction, etc, and the medicine in the form of tablet, capsule, etc are disclosed.

The present invention relates to treating one or more estrogen related diseases while preventing or reducing the likelihood of developing estrogen deficiency related side effects, wherein the composition comprises administering a therapeutically effective amount of a Gn RH antagonist to a patient in need of the treatment, and wherein the amount of Gn RH antagonist is sufficient for providing a mean endogenous serum estradiol level of between about 20 pg / ml and 60 pg / ml, preferably between 30 pg / ml and 50 pg / m, in the patient in a treatment period of at least four weeks, without relying on “add-back” therapy. The composition and method are simple, effective and will accordingly both increase patient acceptance and compliance of therapy.

This invention describes the new 9alpha-substituted estratrienes of general formula (I) in which R3, R7, R7', R13, R16 as well as R17 and R17' have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.

The invention discloses application of tormentic acid in preparation of medicine for treating or preventing the Alzheimer disease caused by estrogen lack, and belongs to the technical field of tormentic acid medicine new application. According to the technical scheme, the application is characterized in that the molecular formula of the tormentic acid is C30H48O5, and the structural formula is as shown in specifications; the tormentic acid can improve the cognition impairment of an AD patient and increase the number of in-brain cholinergic neurons and has a neuron protection effect on CNS, wherein the protection effect can be achieved through ERalpha, and the result provides experimental bases for using the tormentic acid as a medicine select for treating menopause women in combination with AD.

This invention describes the new 18-nor steroids (gonatrienes) of general formula (I), in which R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R15, R16, R17 and R17′ have the meanings that are indicated in the description, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo a preferential action on bone in comparison to the uterus, and / or pronounced action relative to the stimulation of the expression of 5HT2a-receptors and transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention further describes the use of steroids, on which the gonatriene skeleton is based, for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of the gonatriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bone in comparison to the uterus.

The invention relates to the field of medicine preparation, in particular to application of a radix angelicae dahuricae extract in the aspect of regulating climacteric dyslipidemia. Through exploration, the inventor finds that the angelica dahurica extract can be used for regulating climacteric dyslipidemia, and a new medicament is provided for lipid metabolism disorder caused by estrogen deficiency. Specifically, the radix angelicae dahuricae extract can significantly up-regulate gene expression of HMG-CoA reductase (HMGCR) and cytochrome P450 7A1(CYP7A1) in intestinal liver circulation, and regulate gene expression of related receptors and proteins. The radix angelicae dahuricae extract can reduce the levels of total cholesterol (TC) and triglyceride (TG) of serum and liver, and can relieve fatty degeneration and inflammation of the liver. The radix angelicae dahuricae extract can remarkably regulate the composition of OVX intestinal microorganisms, remarkably improve the activity of bile salt hydrolase (BSH) and reconstruct an SCFA spectrum and a cholic acid metabolic spectrum.

The invention belongs to the technical field of medicine, and relates to piperazinyl-containing indole derivatives and medical application thereof. The phenyl indole derivatives comprise stereomers and pharmaceutically applicable salts of the compounds, and the structural general formula is disclosed in the specification. The piperazinyl-containing indole derivatives and pharmaceutically applicable acid-added salts of the compounds can be mixed with the existing drug or independently used as an estrogen receptor regulator for treating or preventing various estrogen-function-related diseases, such as bone loss, fracture, osteoporosis, hectic fever, LDL cholesterol level increase, cardiovascular diseases, cognitive impairment, brain degeneration diseases, anxiety, depression caused by deficiency of estrogen, sexual disorder, hypertension, retinosis and cancer, and especially osteoporosis.