37 results about "Estrogenic Compounds" patented technology

Novel estrogenic compounds of Formula I are provided.wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an α or a β orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

Novel estrogenic compounds of Formula I are provided.wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower allyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an α or a β orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

Novel estrogenic compounds of Formula I are provided.wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an α or a β orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

The present invention relates to an improvement in a method of contraception, in treatment of benign gynecological disorders, and in hormone replacement. The improved method includes administering intranasally an estrogenic compound and an androgenic compound, and in some embodiments an optional progestin compound, in a once-daily bolus formulation comprised of the two or three steroids complexed with a cyclodextrin. An intranasal delivery system for administration of the formulation is also described.

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 hormone replacement therapy formulation and method comprising selective estrogenic compounds which preferentially stimulate the estrogen receptor alpha over the estrogen receptor beta.

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.

An improvement in a method of treating benign gynecological disorders is described. In the method, treatment of a benign gynecological disorder with a composition comprised of a gonadotropin releasing hormone (GnRH) compound and an estrogenic compound, and optionally, an androgenic compound, is extended to premenopausal women who are not receiving an exogenously supplied progestin on a regular or periodic basis. Treatment in accord with the invention does not increase significantly the risk of endometrial hyperplasia. The method is also suitable for contraception.

Methods are provided for detecting the amount of one or more HRT panel analytes (i.e., estrone (E1), estrone sulfate (E1s), 17α-estradiol (E2a), 17β-estradiol (E2b), estradiol sulfate (E2s), estriol (E3), equilin (EQ), 17α-dihydroequilin (EQa), 17β-dihydroequilin (EQb), Equilenin (EN), 17α-dihydroequilenin (ENa), 17β-dihydroequilenin (ENb), and Δ8,9-dehydroestrone (dE1)) in a sample by mass spectrometry. The methods generally involve ionizing one or more HRT panel analytes in a sample and quantifying the generated ions to determine the amount of one or more HRT panel analytes in the sample. In methods where amounts of multiple HRT panel analytes are detected, the amounts of multiple analytes are detected in the same sample injection.

The present disclosure describes a study of estrogenic activity present in various plant species, selectively inducing some but not all estrogenic responses in the uterus. Prepubertal female rats were treated sequentially with various extracts or decoctions of different plant species or its vehicle, followed 1 h later by treatment with estradiol-17β (E) or its solvent. Uteri were excised under anesthesia and histologically processed for eosinophil quantification and morphometric evaluation of various uterine responses to estrogen, at 6 or 24 h after hormone or vehicle treatment. Besides extracts or decoctions, pure phytoestrogens were also used. Additionally, human mammary cancer cells MCF-7 or MDAMB-231 were cultured in presence of the extract (or decoction), E, both or solvent and cell proliferation was evaluated. Various extracts or decoction displayed selective estrogenic and / or antiestrogenic action for some but not all parameters of estrogen stimulation in the uterus and inhibited growth of human mammary cells in culture or antagonized the estrogen-induced increase in their growth. Present results reveal, for the first time, a dissociation of responses to estrogen by phytoestrogens, suggesting its possible therapeutic application as estrogenic compounds not inducing cell proliferation and reveal the anticancerous effect of some of the extracts with possible therapeutic relevance. The dissociation of responses to estrogen additionally suggest therapeutic applications in estrogen-related diseases (for instance, premenstrual syndrome, endometriosis, etc.); the inhibition of eosinophil degranulation suggest an application in diseases related to eosinophils (hypereosinophilic syndrome, allergic and hypersensitivity diseases).

The invention belongs to the technical field of hormone detection, and relates to a kit and a method for determining various estrogens in dried blood spots. Aiming at the technical problems that in the prior art, estrogen exists at a trace level in a biological sample and a human body, the content of estrogen in a dried blood spot sample is extremely low, the polarity of estrogen compounds is relatively small, the ionization efficiency in ESI and APCI sources in a mass spectrum is not high, and the direct detection sensitivity is not high, the invention provides a kit for determining various estrogens in a dried blood spot. Comprising a derivatization reagent, a first extraction agent and a second extraction agent, and the trace estrogen in the dried blood spot can be rapidly, simply and accurately detected by combining extraction and derivatization pretreatment with ultra-high performance liquid chromatography-tandem mass spectrometry. The invention further provides a method for determining the multiple estrogens in the dried blood spot, the estrogens are extracted from the dried blood spot by using the first extraction agent and then derivatized, and the derived estrogens are extracted again by using the second extraction agent, so that the flux is increased, and the analysis efficiency is improved.

A method for the prevention or treatment of postmenopausal osteoporosis by initiating the treatment with a low close of an estrogenic compound and increasing the dose of the estrogenic compound after the initiation period.

A method for the prevention or treatment of postmenopausal osteoporosis by initiating the treatment with a low dose of an estrogenic compound and increasing the dose of the estrogenic compound after the initiation period.

The invention relates to a method for brewing a health wine, in particular to a grape medicated wine which is brewed by using a natural plant and contains plant estrogen. When a female becomes middle-aged or old, the secretory volume of internal estrogen reduces year by year, the glossiness and elasticity of skin decreases, osteoporosis, adiposis and vessel wall incrassation appear, and the vascular permeability reduces, so the organism starts to age gradually. If artificial estrogen is supplemented, the estrogen is accumulated in the human body and causes other malignant diseases. The natural plant estrogen has double functions of xenoestrogen and estrogenic activity resistance on the human body, quantitative supplementation of the natural plant estrogen everyday can play a role in balancing the internal estrogen; when the internal estrogen content is too low, the natural plant estrogen can increase the internal estrogen; and when the estrogen content is too high, the natural plant estrogen is discharged to reduce the estrogen to achieve the balance of the internal estrogen level and achieve the functions of delaying senility and eliminating diseases to prolong life.