| Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women -> Monitor Keywords |
|
|
 
Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in womenRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Ether Doai, Benzene Ring Containing, Plural Oxygens, Acyclic Carbon To Carbon UnsaturationMethods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20050272825, Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001] The present application is a continuation of U.S. patent application Ser. No. 10/162,708 filed 6 Jun., 2002, which is a continuation-in-part of International Application No. PCT/FI01/00414 filed 2 May 2001 designating the U.S., which was published under PCT Article 21(2) in English as International Publication No. WO 02/07718, and which is a continuation of U.S. patent application Ser. No. 09/625,199, filed 21 Jul. 2000, now U.S. Pat. No. 6,245,819, each application being incorporated by reference herein in its entirety. FIELD OF THE INVENTION [0002] This invention relates to a method for the inhibition of skin atrophy, epithelial or mucosal atrophy in women, especially women during or after the menopause. The invention also concerns prevention or treatment of atrophy-related symptoms in women, especially women during or after menopause. BACKGROUND OF THE INVENTION [0003] The publications and other materials used herein to illuminate the background of the invention, and in particular, cases to provide additional details respecting the practice, are incorporated by reference and listed in the Bibliography. [0004] During and after menopause, elderly women commonly develop symptoms which are due to estrogen deficiency. These symptoms include hot flashes, sweating, insomnia, depression, vaginal dryness, urinary incontinence, nausea, pain, osteoporosis, coronary heart disease, breast tenderness, oedema, fatigue, decreased sexual activity, as well as subsequent psychosocial problems (Payer, 1990; Rekers, 1990). In addition, estrogens are suggested to have neuroprotective effects. Thus, declining estrogen concentrations may negatively affect the mental activities of aging women (Schneider & Finch, 1997; Wickelgren, 1997). Estradiol is known to be excellent in the treatment of climacteric symptoms, and its use in the treatment of these symptoms is rapidly increasing. However, estrogens cause an increased risk of endometrial and breast cancers. It is possible to decrease the carcinogenicity of endometrial cancer by sequential progestin administration, but the risk of breast cancer is not diminished by progestins. The carcinogenicity risk limits the length of estrogen replacement therapy, although it would be very useful to continue the therapy long term, due to the protective effects of estrogens in the bone, in the cardiovascular system, in the central nervous system, and for urinary symptoms. [0005] "SERM"s (selective estrogen receptor modulators) have both estrogen-like and antiestrogenic properties (Kauffman & Bryant, 1995). The effects may be tissue-specific as in the case of tamoxifen and toremifene which have estrogen-like effects in the bone, partial estrogen-like effect in the uterus and liver, and pure antiestrogenic effect in breast cancer. Raloxifene and droloxifen are similar to tamoxifen and toremifene, except that their antiestrogenic properties dominate. Based on the published information, all SERMs are more likely to cause menopausal symptoms than to prevent them. They have, however, other important benefits in elderly women: they decrease total and LDL cholesterol, thus deminishing the risk of cardiovascular diseases, and they may prevent osteoporosis and inhibit breast cancer growth in postmenopausal women. There are also almost pure antiestrogens under development. They are mainly aimed at the treatment of breast cancer (Wakeling & Bowler, 1988). [0006] The compound (deaminohydroxy)toremifene, which also is known under the code FC-1271a or the generic name ospemifene, has relatively weak estrogenic and antiestrogenic effects in the classical hormonal tests (Kangas, 1990). It has antiosteoporosis actions and it decreases total and LDL cholesterol levels in both experimental models and in human volunteers (International patent publications WO 96/07402 and WO 97/32574). It also has antitumor activity in an early stage of breast cancer development in an animal breast cancer model. Ospemifene is the first SERM which has been shown to have beneficial effects in climacteric syndromes in healthy women. [0007] The European patent application EP 664124 A1 suggests the use of raloxifene or related compounds for the inhibition of skin atrophy or vaginal atrophy, especially in postmenopausal women. SUMMARY OF THE INVENTION [0008] According to one aspect, this invention concerns a method for inhibition of skin atrophy, or epithelial or mucosal atrophy in women, said method comprising administering to the woman an effective amount of the compound of formula (I) 2 [0009] or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof. [0010] According to another aspect, this invention concerns a method for treatment or prevention of symptoms related to skin atrophy, or to epithelial or mucosal atrophy in women, said method comprising administering to the woman an effective amount of the compound of formula (I) 3 [0011] or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof. BRIEF DESCRIPTION OF THE DRAWINGS [0012] FIGS. 1A to 1D show changes (from start to 12 weeks' treatment) in the karyopyknosis index for superficial cells of the vaginal epitelium for the individuals treated daily with 30 mg ospemifene, i.e. FC-1271a (1A), 60 mg FC-1271a (1B), 90 mg FC-1271a (1C), and 60 mg raloxifene (1D). [0013] FIG. 2 shows the effect of 30 mg, 60 mg and 90 mg daily doses of FC-1271a and raloxifene (daily dose 60 mg) on vaginal dryness, assessed as the individuals' subjective estimates. DETAILED DESCRIPTION OF THE INVENTION [0014] The methods according to this invention are particularly useful for women during or after the menopause. However, the methods according to this invention is not restricted to women in this age group. [0015] This invention relates particularly to the use of the estrogen receptor modulator ospemifene in women during or after the menopause. Ospemifene is the Z-isomer of the compound of formula (I) and it is one of the main metabolites of toremifene, is known to be an estrogen agonist and antagonist (Kangas, 1990; International patent publications WO 96/07402 and WO 97/32574). [0016] The term "metabolite" shall be understood to cover any (deaminohydroxy)toremifene metabolite already discovered or to be discovered. As examples of such metabolites can be mentioned the oxidation metabolites mentioned in Kangas (1990) on page 9 (TORE VI, TORE VII, TORE XVIII, TORE VIII, TORE XIII), especially TORE VI and TORE XVIII, and other metabolites of the compound. [0017] The use of mixtures of isomers of compound (I) shall also be included in this invention. [0018] A particular form of atrophy to be inhibited is urogenital atrophy. Symptoms related to urogenital atrophy can be divided in two subgroups: urinary symptoms and vaginal symptoms. Continue reading about Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women... Full patent description for Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. Start now! - Receive info on patent apps like Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women or other areas of interest. ### Previous Patent Application: Methods for monitoring combretastatin resistance Next Patent Application: Dispersion of sintered materials Industry Class: Drug, bio-affecting and body treating compositions ### FreshPatents.com Support Thank you for viewing the Methods for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women patent info. IP-related news and info Results in 0.1395 seconds Other interesting Feshpatents.com categories: Daimler Chrysler , DirecTV , Exxonmobil Chemical Company , Goodyear , Intel , Kyocera Wireless , |
PATENT INFO |
|
