172 results about "Selective estrogen receptor modulator" patented technology

The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

A mixture of a pomegranate seed oil product and a pomegranate juice product and a pharmaceutical composition containing same. The mixture, which is a cancer chemopreventive, includes a pomegranate seed oil product and pomegranate juice product. The pharmaceutical composition includes physiologically active amounts of pomegranate seed oil product, a pomegranate juice product and a pharmaceutically acceptable carrier. According to some disclosed embodiments, a pomegranate peel product is further included. Further disclosed is a selective estrogen receptor modulator and other biologically active compounds derived from pomegranates as well as methods of use thereof.

Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance , in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure:

is specifically disclosed for the medical treatment and/or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is:

and wherein R¹–R⁵ and Q¹ are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.

The invention relates to the use of one or more cannabinoids, particularly THC and/or CBD in combination with a non-cannabinoid chemotherapeutic agent in the manufacture of a medicament for use in the treatment of cancer. In particular the cancer to be treated is a brain tumour, more particularly a glioma, more particularly still a glioblastoma multiforme (GBM). The non-cannabinoid chemotherapeutic agent may be a selective estrogen receptor modulator or an alkylating agent.

The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.

The invention relates to a novel benzothiophene derivative and application thereof in preventive and/or treatment medicine for breast cancer and osteoporosis. The benzothiophene derivative is an ideal selective estrogen receptor modulator, can be used for treating or preventing various indications related to estrogen functions, and is particularly applicable to treating post-menopause breast cancer and osteoporosis. The compound has the advantages that oxidative metabolism is lowered, effective bioavailability is higher, and accordingly, dosage of the compound is little, tolerance of the compound is fine, and side effects are low.

Methods for treating or reducing the likelihood of acquiring estrogen-related (e.g. estrogen-exacerbated) diseases including endometriosis include administering to a patient a selective estrogen receptor modulator (SERM), in combination with inhibiting ovarian secretions, e.g., by administering an LHRH agonist or antagonist. In some embodiments, a precursor of sex steroids, said precursor being selected from the group consisting of dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate (DHEA-S), androst-5-ene-3β,17β-diol (5-diol), and androstenedione or a compound transformed into one of these, is also administered

This invention relates to a method for the treatment or prevention of osteoporosis in an individual suffering from increased bone turnover, said method comprising administering to said individual an effective amount of a therapeutically active compound, which is a selective estrogen receptor modulator of the triphenylalkene or triphenylalkane structure.

The present invention provides methods for boosting mucosal immunity in the female reproductive tract of pre- and post-menopausal women using a TGF-beta inhibitor, a Selective Estrogen Receptor Modulator, and/or a recombinant commensal bacterium that expresses endogenous microbicides into the intestinal tract or reproductive tract of a subject. It also provides methods for boosting innate and adaptive immunity by providing a glucocorticoid. Methods for preventing sexually transmitted infections including HIV infection are also provided.

The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Methods for treating breast cancer, comprising administering to the subject an effective amount of a selective estrogen receptor modulator and an effective amount of a compound represented by the following structural formula: (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.

A new method for the preparation of a selective estrogen receptor modulator and its isomers. Also disclosed is the preparation of new intermediates and their use in the preparation of the selective estrogen receptor modulator.