Plural Compounds Containing Cyclopentanohydrophenanthrene Ring Systems Patents (Class 514/170)
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Patent number: 6759408Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.Type: GrantFiled: May 9, 2002Date of Patent: July 6, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6759399Abstract: The method of treating narcotic withdrawal symptoms in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound having anti-mineralocorticoid activity sufficient to treat narcotic withdrawal symptoms.Type: GrantFiled: March 27, 2000Date of Patent: July 6, 2004Assignee: Aventis Pharma S.A.Inventors: Francis Petit, Daniel Philibert, Nick Goeders
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Publication number: 20040121992Abstract: Methods of reducing the cholesterol accumulation in a subject, including methods of reducing cholesterol synthesis and methods of increasing cholesterol degradation. Cholesterol synthesis is inhibited by administering a compound capable of increasing 27-hydroxy-7-dehydrocholesterol and/or 27-hydroxy-8-dehydrocholesterol levels, wherein an increase in 27-hydroxy-7-dehydrocholesterol and/or 27-hydroxy-8-dehydrocholesterol levels results in an inhibition of cholesterol synthesis. Cholesterol degradation is increased by increasing the level of 7&agr;-hydroxylase in extrahepatic tissue and cells.Type: ApplicationFiled: September 10, 2003Publication date: June 24, 2004Inventor: Norman B. Javitt
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Publication number: 20040110732Abstract: The present invention relates to a novel pharmaceutical composition for transdermal or transmucosal administration, comprisingType: ApplicationFiled: March 20, 2003Publication date: June 10, 2004Applicant: BESINS INTERNATIONAL BELGIQUEInventors: Valerie Masini-Eteve, Brigitte Taravella
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Patent number: 6747019Abstract: A hormone replacement therapy, comprising a plurality of daily doses of a pharmaceutical preparation, the doses being administered continuously and consecutively in alternating phases of three daily doses, a relatively dominant estrogenic activity phase comprising three daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17&bgr;-estradiol per day, and a relatively dominant progestagenic activity phase of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17&bgr;-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 &mgr;g per day of norgestimate.Type: GrantFiled: April 30, 2002Date of Patent: June 8, 2004Assignees: Jencap Research, Ltd., Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert F. Casper, Gary A. Shangold, Militza K. Ausmanas
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Publication number: 20040106587Abstract: The present invention relates to compositions and methods for preventing the development of epithelial ovarian cancer by administering compounds in an amount capable of regulating TGF-&bgr; expression in the ovarian epithelium and/or capable of optimally altering expression of other surrogate biomarkers identified by microarray technology. HRT and OCP regimens comprising such compositions and methods are disclosed.Type: ApplicationFiled: July 7, 2003Publication date: June 3, 2004Inventor: Gustavo C. Rodriguez
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Publication number: 20040106586Abstract: Method for hormone replacement therapy, in which at least in the established postmenopause a daily unit with at least one hormonal component, namely with at least estrogen (E) and/or at least one gestagen (G) is administered permanently and continuously every day, characterized in that in at least one ingestion period preceding the permanent administration of hormone daily units is provided an ingestion pause (P), in which either no daily units or placebos or daily units with a much lower estrogen and/or gestagen content than during the permanent administration of hormone daily units in the established postmenopause and during the ingestion phase(s) of the preceding, ingestion period are administered, as well as administration form for hormone therapy.Type: ApplicationFiled: January 14, 2004Publication date: June 3, 2004Inventor: Hermann Kulmann
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Publication number: 20040102422Abstract: Use of a steroid hormone or steroid hormone analogue and at least a portion of HPV E2 protein in the preparation of a pharmaceutical composition for the treatment of cervical cancer.Type: ApplicationFiled: October 31, 2002Publication date: May 27, 2004Applicant: The University of BristolInventor: Kevin Gaston
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Publication number: 20040072808Abstract: The present invention includes methods for preventing endometrial hyperplasia associated with estrogen therapy through the administration of a progestin agent. The methods presented may include starting the administration of a progestin agent at a high dose, and then lowering the dose.Type: ApplicationFiled: October 3, 2003Publication date: April 15, 2004Inventor: Thomas W. Leonard
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Publication number: 20040067922Abstract: This invention addresses the pharmaceutical composition for topical corticosteroid use in association with diffusing enzyme for treatment of phimosis. A pharmaceutical composition for treatment of phimosis using topical corticosteroid characterized by including around 0.025 to 5 percent in weight in relation to the total weight of the mixture composition of one or more corticosteroids and/or hormone steroids, whether or not associated with non-hormonal anti-inflammatory agents and around 25 UTR to 4000 UTR/g of one or more proteolytic diffusing enzymes in proper medium, in different pharmaceutical forms, accompanied with additives known to the technical man. Topical corticosteroid application in association with diffusing enzyme for treatment of phimosis in which 90 percent of the patients had improvements over their clinical complaints, with the prepuce being easily retracted.Type: ApplicationFiled: October 31, 2003Publication date: April 8, 2004Inventor: Paulo Cesar Rodrigues Palma
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Patent number: 6716437Abstract: The present invention relates to topical compositions useful in enhancing lipid synthesis in skin comprising an effective amount of cafestol or kahweol, or derivative thereof, in combination with a pharmaceutically or cosmetically acceptable carrier. Such compositions are useful in treatment or prevention of dry skin and conditions in which the skin's lipid barrier is defective or damaged.Type: GrantFiled: April 2, 2001Date of Patent: April 6, 2004Assignee: E-L Management CorporationInventors: Edward Pelle, Jon Anderson
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Publication number: 20040062794Abstract: The present invention relates to a method for reducing triglyceride levels in a patient and effecting hormone replacement therapy comprising continuously and transdermally administering an essentially constant therapeutically effective amount of a composition comprising an estradiol (17&bgr;-estradiol) and a progestin (levonorgestrel (LNG)) in a pharmaceutically acceptable carrier.Type: ApplicationFiled: September 30, 2002Publication date: April 1, 2004Inventors: Lee Shulman, Kerstin Uhl, Vladimir Yankov
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Publication number: 20040053898Abstract: A novel medicament for the treatment of estrogen-deficient disease states is disclosed. Said medicament is a combination preparation comprising an ER&bgr;-selective estrogen and an ER&agr;-selective antiestrogen or SERM (Selective Estrogen Receptor Modulator). The antiestrogen or SERM which is a component of the combination preparation is preferably selective for the periphery. The preparation is suitable for an organ-specific estrogen therapy and has clear advantages over conventional therapies. Due to the combination of ER&agr;-selective SERM and ER&bgr;-estrogen the preparation permits a complete protection against bone loss caused by estrogen deficiency. The components of the medicament also have a synergistic effect with respect to the inhibition of inflammation inducing genes, in particular in inflammatory disorders such as atherosclerosis and arthritis, or neurodegenerative diseases such as Alzheimers and multiple sclerosis. Furthermore, positive effects on cognition and mood may be expected.Type: ApplicationFiled: September 26, 2003Publication date: March 18, 2004Inventors: Karl-Heinrich Fritzemeier, Uwe Kollenkirchen, Christa Hegele-Hartung
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Publication number: 20040038950Abstract: The present invention relates to a pharmaceutical composition for treating (IL-1)-related disease or disorder, which comprises: (a) a therapeutically effective dose of dehyroepiandrosterone or its derivative represented by the formula (I); and (b) a pharmaceutically acceptable carrier: 1Type: ApplicationFiled: February 5, 2003Publication date: February 26, 2004Inventors: Sang-Cheol Seong, Myung-Chul Lee, Hyun-Chul Jo, Jung-Sun Park, Mi-Young Jeong
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Patent number: 6696432Abstract: The present invention concerns the combination of dehydroepiandrosterone (DHEA) and at least one aromatase inhibitor and the use of such a combination to produce a medicament for treating relative and/or absolute androgen deficiency in men. Selective aromatase inhibitors such as atamestan, formestan, pentrozol, aramidex, fadrozol, CGS 20267 and/or vorozol, are preferred for producing the medicament according to the invention.Type: GrantFiled: November 3, 1998Date of Patent: February 24, 2004Assignee: Schering AktiengesellschaftInventors: Jörg Elliesen, Albert Radlmaier, Ursula Habenicht, Friedmund Neumann
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Publication number: 20040033999Abstract: The invention is the novel androgen (7&agr;,17&bgr;)-7-methyl-17-[(1-oxoundecyl)oxy]estr-4en-3one (MENT undecanoate). This compound distinguishes favourably from other testosterone derivatives in that it has a good solubility in oily media. It particularly exhibits a good dissolved potency relative to testosterone. The compound is particularly suitable for administration by means of injection.Type: ApplicationFiled: June 21, 2002Publication date: February 19, 2004Inventors: Dirk D. Leysen, Hendrikus Adrianus Antonius Van Der Voort H.A.A.
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Publication number: 20040022738Abstract: 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.Type: ApplicationFiled: November 15, 2002Publication date: February 5, 2004Inventors: Malcolm C. Pike, Darcy V. Spicer, AnnaMarie Daniels, John R. Daniels
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Publication number: 20040022739Abstract: 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.Type: ApplicationFiled: November 15, 2002Publication date: February 5, 2004Inventors: John R. Daniels, Malcolm C. Pike, Darcy V. Spicer, AnnaMarie Daniels
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Publication number: 20040018991Abstract: A composition for medicinal treatment by means of topical administration is described, which contains an aromatase inhibitor, in addition to conventional constituents of topical forms of administration. The active ingredient or the composition containing this active ingredient is especially suitable for the prophylaxis and for the treatment of mastalgia.Type: ApplicationFiled: May 2, 2003Publication date: January 29, 2004Inventors: Alfred Schmidt, Heinrich Wieland
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Publication number: 20040009960Abstract: A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6&bgr;,7&bgr;;15&bgr;;16&bgr;-dimethylene-3-oxo-17&agr;-preg-4-ene-21, 17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form.Type: ApplicationFiled: February 6, 2003Publication date: January 15, 2004Applicant: Schering AktiengesellschaftInventors: Wolfgang Heil, Juergen Hilmann, Ralph Lipp, Rolf Schuermann
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Patent number: 6677327Abstract: The present invention relates to an edible phytosterol or phytostanol composition useful in the food industry and to methods of preparing such an edible composition. The edible composition comprises a phytosterol or phytostanol, an isolated water soluble protein, and optionally an emulsifier, wherein the weight ratio of the protein to the phytosterol or phytostanol is from about 0.2:1 to about 10:1, and the weight ratio of the emulsifier to the phytosterol or phytostanol is from about 0.2:1 to about 5:1. The invention also relates to edible products containing such a composition and to methods for the production of the edible products.Type: GrantFiled: November 24, 1999Date of Patent: January 13, 2004Assignee: Archer-Daniels-Midland CompanyInventor: Thomas V. Gottemoller
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Patent number: 6677324Abstract: The invention describes a combination preparation of an oestrogen and an antioestrogen, characterized in that the oestrogen is selected from the group consisting of 17-&bgr;-oestradiol, 17-&agr;-ethynyloestradiol, oestriol, oestrone, oestrone sulphate, oestrogen sulphamates, 17&agr;-oestradiol, mestranol, stilboestrol and naturally conjugated oestrogens and in that the antioestrogen is a substituted 7&agr;-(&xgr;-aminoalkyl)oestratriene of the general formula I The combination preparation according to the invention can be used for hormone substitution therapy.Type: GrantFiled: August 21, 2000Date of Patent: January 13, 2004Assignee: Schering AktiengesellschaftInventors: Rudolf Knauthe, Christa Hegele-Hartung
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Publication number: 20040006053Abstract: A method for long-term therapy using corticosteriods to treat tissue damage associated with graft-versus-host disease in a patient having undergone hematopoietic cell transplantation, and host-versus-graft disease in a patient having undergone organ allograft transplantation. The method includes orally administering to the patient a therapeutically effective amount of a topically active corticosteroid, such as beclomethasone dipropionate, from the 29th day until the 56th day following hematopoietic cell or organ allograft transplantation. Representative tissues includes tissue of the intestine and liver, while representative tissue damage includes inflammation thereof.Type: ApplicationFiled: July 3, 2003Publication date: January 8, 2004Applicant: Enteron Pharmaceuticals, Inc.Inventor: George B. McDonald
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Publication number: 20030229057Abstract: A method of hormone replacement therapy is disclosed comprising the step of administering continuously to a post-menopausal or estrogen deficient female in need of such therapy a combination of estrogen in an effective hormone replacement amount and a progestogen which is a potent sulfatase inhibiting progestogen in an amount which is both an effective endometrium protective amount and an effective breast protective amount.Type: ApplicationFiled: March 11, 2003Publication date: December 11, 2003Inventors: Patrick Michel Caubel, Andrew Joseph Friedman
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Publication number: 20030228375Abstract: This invention provides compositions and methods related to the administration of deer antler, one or more nor-testosterone precursors, and one or more testosterone precursors, to increase testosterone levels, treat sexual dysfunction, improve sexual function, improve energy, enhance feelings of well-being and increase muscle mass in males. This invention also provides for inhibitors of the enzymes aromatase and/or 5-alpha reductase, to support testosterone levels and avoid undesirable metabolites.Type: ApplicationFiled: April 25, 2002Publication date: December 11, 2003Applicant: A. Glenn BraswellInventor: Inna Yegorova
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Publication number: 20030225048Abstract: A method of contraception is described comprising the step of administering to a menstruating female a cycle of contraceptive therapy, said cycle of therapy including, for at most 35 successive days, the administration of a combination of an estrogen and a progestogen in a contraceptively effective daily dosage wherein said progestogen is a potent sulfatase inhibiting progestogen and said cycle of therapy including 4-8 days in which said progestogen is administered in the absence of estrogen administration following said at most 35 successive days.Type: ApplicationFiled: March 11, 2003Publication date: December 4, 2003Inventors: Patrick Michel Caubel, Andrew Joseph Friedman
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Publication number: 20030225047Abstract: A method of contraception is disclosed comprising the step of administering to a menstruating female a cycle of contraceptive therapy, said cycle of therapy including the continuous administration for the length of the cycle of a potent sulfatase inhibiting progestogen in a contraceptively effective and breast protecting dose, in the absence of the administration of an estrogen.Type: ApplicationFiled: March 11, 2003Publication date: December 4, 2003Inventors: Patrick Michel Caubel, Andrew Joseph Friedman
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Patent number: 6656929Abstract: The object of this invention is a pharmaceutical composition with a synthetic natural progesterone and oestradiol base coming in the form of a tablet, characterised by the fact that it has a disintegration time of less than 15 minutes, preferably less than 10 minutes, and more preferably still less than 5 minutes.Type: GrantFiled: March 16, 1999Date of Patent: December 2, 2003Assignee: Laboratoires Besins IscovescoInventors: Benoît Agnus, Antoine Besins
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Publication number: 20030220308Abstract: Methods for enhancing the ability of an individual, exposed to sunlight, to produce vitamin D via the skin. Pharmaceutical compositions comprising provitamin D and at least one of lumisterol and tachysterol and analogs and derivatives thereof are also disclosed.Type: ApplicationFiled: May 22, 2003Publication date: November 27, 2003Inventor: Michael F. Holick
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Publication number: 20030216359Abstract: This invention relates to combination chemotherapy, particularly involving vitamin D or a derivative thereof. In one aspect, the invention provides a method of killing a cell by first administering to the cell vitamin D (or a derivative) and subsequently administering to the cell a cytotoxic agent. Where this strategy is applied to an intact tumor, the present invention provides a method of retarding the growth of the tumor by first administering vitamin D (or a derivative) to the tumor and subsequently administering the cytotoxic agent. A further aspect of the invention concerns a method of treating prostate cancer within a patient by co-administration of vitamin D (or a derivative) and a glucocorticoid to the patient. In yet a further aspect, the invention provides an improved method of treating a patient with vitamin-D involving the adjunctive administration of zoledronate.Type: ApplicationFiled: May 5, 2003Publication date: November 20, 2003Applicant: University of Pittsburgh of the Commonwealth System of Higher EducationInventors: Candace S. Johnson, Donald L. Trump
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Publication number: 20030207850Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.Type: ApplicationFiled: April 28, 2003Publication date: November 6, 2003Applicant: WyethInventor: James H. Pickar
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Patent number: 6642219Abstract: An estrogen-free contraceptive is provided which does not have the bleeding-related drawbacks of conventional progestogen-only pills. Thus the invention is a contraceptive kit comprising a combined means for the simultaneous daily administration of a progestogen as the sole contraceptively effective ingredient and an anti-progestogen. Said combined means preferably is in the form of tablets having a normal contraceptive dose of the progestogen and low dose of the anti-progestogen.Type: GrantFiled: June 26, 2000Date of Patent: November 4, 2003Assignee: Akzo Nobel N.V.Inventor: Herman Jan Tijmen Coelingh Bennink
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Publication number: 20030203043Abstract: This invention provides compositions and methods related to the administration of deer antler, one or more nor-testosterone precursors, and one or more testosterone precursors, to increase testosterone levels, treat sexual dysfunction, improve sexual function, improve energy, enhance feelings of well-being and increase muscle mass in males. This invention also provides for inhibitors of the enzymes aromatase and/or 5-alpha reductase, to support testosterone levels and avoid undesirable metabolites.Type: ApplicationFiled: April 25, 2002Publication date: October 30, 2003Inventor: Inna Yegorova
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Publication number: 20030203047Abstract: This invention provides compositions and methods related to the administration of deer antler, one or more nor-testosterone precursors, and one or more testosterone precursors, to increase testosterone levels, treat sexual dysfunction, improve sexual function, improve energy, enhance feelings of well-being and increase muscle mass in males. This invention also provides for inhibitors of the enzymes aromatase and/or 5-alpha reductase, to support testosterone levels and avoid undesirable metabolites.Type: ApplicationFiled: April 25, 2002Publication date: October 30, 2003Applicant: A. Glenn BraswellInventor: Inna Yegorova
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Patent number: 6638547Abstract: A prepared food product for ingestion by mammals is described and methods for preparing such products. The food product includes an oxidation-resistant fat-based composition substantially free of exogenous solubilizing and dispersing agents for phytosterols. The fat-based composition includes between 75% and 98% by weight of at least one triglyceride-based edible oil or fat, and between 2% and 25% by weight of non-esterified phytosterols. Typically, approximately 1.5% by weight of phytosterols remain soluble at room temperature, and between 0.5% and 23.5% by weight are converted to triglyceride-recrystallized phytosterols (TRPs). The fat-based composition which has been partially oxidized in the prepared food by exposure to air (and typically heat), contains a reduced amount of oxidative by-products compared to a similar fat-based composition lacking these non-esterified phytosterols.Type: GrantFiled: November 14, 2002Date of Patent: October 28, 2003Assignee: Brandeis UniversityInventors: Daniel Perlman, Kenneth Hayes, Andrzej Pronczuk
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Publication number: 20030195177Abstract: The present invention combines the administration of estrogens with the administration of non-aromatizing androgens to treat hormonal deficiencies in women undergoing estrogen replacement therapy.Type: ApplicationFiled: April 29, 2003Publication date: October 16, 2003Inventors: Thomas W. Leonard, R. Forrest Waldon
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Publication number: 20030191096Abstract: The present invention combines the administration of estrogens with the administration of non-aromatizing androgens to treat frailty in women undergoing estrogen replacement therapy.Type: ApplicationFiled: October 9, 2002Publication date: October 9, 2003Inventors: Thomas W. Leonard, R. Forrest Waldon
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Publication number: 20030191097Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.Type: ApplicationFiled: April 1, 2003Publication date: October 9, 2003Applicant: WyethInventors: Gary S. Grubb, James H. Pickar, Ginger D. Constantine, Michael S. Dey
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Publication number: 20030181430Abstract: The present invention relates to the field of therapeutic chemistry and more especially to the realization of new galenic forms intended to be applied on the skin.Type: ApplicationFiled: June 26, 2002Publication date: September 25, 2003Inventors: Georges Gray, Bertrand Villet, Jacques ` Paris, Jean-Louis Thomas
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Publication number: 20030176404Abstract: An estrogen-free contraceptive is disclosed which does not have the bleeding-related drawbacks of conventional progestogen-only pills. The invention includes a contraceptive kit comprising a combined means for the simultaneous daily administration of a progestogen and an anti-progestogen. The combined means may be in the form of tablets having a normal contraceptive dose of the progestogen and a low dose of the anti-progestogen.Type: ApplicationFiled: March 14, 2003Publication date: September 18, 2003Inventor: Herman Jan Tijmen Coelingh Bennink
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Patent number: 6617319Abstract: The invention provides a process for the isolation of 2-deoxy ecdysterone from Zoanthus sp process comprising the steps (a) preparing crude methanol extract of Zoanthus sp., (b) subjecting the crude methanol extract to fractionation using petroleum ether, ethyl acetate, chloroform, n-butanol and mixtures thereof to yield a fraction, (c) subjecting the active fraction to flash chromatography over silica gel to obtain partially purified active compound, and (d) subjecting the active subfraction obtained from step (c) above to gel permeation chromatography to obtain the active pure compound.Type: GrantFiled: January 16, 2002Date of Patent: September 9, 2003Assignee: Council of Science and Industrial ResearchInventors: Cynthia Olimpia Lydia Gonsalves, Perunninakulath Parameswaran Subrayan, Chandrakant Govind Naik, Chittur Thelakkat Achuthankutty
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Publication number: 20030158159Abstract: A method of treating an individual to increase the individual's bone mineral density (BMD) is disclosed. The method includes co-administering a calcitonin-like agent and a DHEA-like agent. Also disclosed are methods for potentiating the effect of treatment with a calcitonin-like agent on BMD and for increasing BMD in an individual being treated with DHEA, e.g., for treatment of systemic lupus erythematosus (SLE).Type: ApplicationFiled: February 13, 2003Publication date: August 21, 2003Applicant: Genelabs Technologies, Inc.Inventor: Kenneth E. Schwartz
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Publication number: 20030153540Abstract: The present invention provides compositions, methods, and kits for improving health in a woman having elevated SHBG levels, or who is receiving oral estrogen supplementation, by non-orally administering an effective amount of an androgenic steroid. Further, the present invention provides compositions, methods, and kits for coadministering an effective amount of an orally administered estrogen and an effective amount of a non-orally administered androgenic steroid for women in need of estrogen supplementation.Type: ApplicationFiled: October 22, 2002Publication date: August 14, 2003Inventors: Theresa Rosario-Jansen, Norman A. Mazer
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Publication number: 20030152615Abstract: A composition for transdermal administration resulting from an admixture includes: a therapeutically effective amount of a pharmaceutically active agent that includes a corresponding steroid and a steroid derivative; and a carrier for the pharmaceutically active agent. The steroid and the corresponding steroid derivative are present in a weight ratio of 10:1 to 1:10 steroid: corresponding steroid derivative. In a preferred embodiment ratio is 6:1 to 1:6. In a preferred embodiment, the corresponding steroid derivative is a steroid ester. In another preferred embodiment, the carrier is a polymer that includes a pressure-sensitive adhesive.Type: ApplicationFiled: December 30, 2002Publication date: August 14, 2003Applicant: Noven Pharmaceuticals, Inc.Inventor: David Houze
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Publication number: 20030153539Abstract: The use of estramustine phosphate and its metabolites estramusfine and estromustine allow to potentiate the therapeutic efficacy of taxanes by both improving their pharmacokinetic and pharmacodynamidc profile through the inhibition of (CYP)2C8 and (CYP)3A4 enzymes, both responsible for the metabolism of the taxanes; formulations of estramustine phosphate and metabolites, combinations of these latter with taxanes and therapeutic methods of treatment comprising them as a combined therapy are also disclosed.Type: ApplicationFiled: December 12, 2002Publication date: August 14, 2003Inventors: Marius Monshouwer, Robert Ings, Maurizio Rocchetti
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Publication number: 20030149009Abstract: The subject invention concerns a unit dose formulation comprising less than 2.5 mg of prednisolone or an equivalent, equipotent amount of another corticosteroid. One embodiment of a method of the invention concerns once daily administration of the unit dose formulation between midnight and 6 a.m. for the treatment of rheumatoid arthritis.Type: ApplicationFiled: October 1, 2002Publication date: August 7, 2003Inventors: Hazel Judith Bardsley, Robin Mark Bannister, Julian Clive Gilbert
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Publication number: 20030147936Abstract: An improved method and products for the primary hormonal treatment of early stage, low and intermediate risk prostate cancers by prostatic implants of androgen suppressive drugs formulated as fused with a lipoid carrier or encapsulated in microcapsules or in Silastic capsules is provided. Such prostatic implants renders a constant slow-release of their contents to the prostate for extended periods by biodegradation and diffusion. It facilitates higher prostatic and lower systemic concentrations of androgen suppressive hormones. Because of their high prostatic and lower systemic concentrations, tumor control is much improved and the their systemic toxicity is minimized. Tumor control after such primary hormonal implant treatment is followed by clinical examinations and the biochemical tumor control is followed by periodic estimations of serum levels of PSA and acid phosphatase.Type: ApplicationFiled: February 7, 2002Publication date: August 7, 2003Inventor: Velayudhan Sahadevan
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Publication number: 20030149008Abstract: An improved method and products for the hormonal treatment of breast cancer by breast implants of anti-estrogens and steroid hormones in formulations as fused with a lipoid carrier or encapsulated in microcapsules or in Silastic capsules is provided. Such breast implants renders a constant slow-release of their contents to the breast tissue for extended periods by biodegradation and diffusion. It facilitates higher breast tissue concentrations of anti-estrogen and hormonal compositions. Because of their high concentration in the breast and lower systemic distribution, tumor control is much improved and the their systemic toxicity is minimized. An added beneficial effect of these breast implants on breast cancer is mediated by the inhibition of hypothalamic-pituitary LHRH, FSH and LH secretion by these composition's systemic contents. It is also an effective prophylaxis against breast cancer. Furthermore, it reduces the cost of hormonal treatment of breast cancer.Type: ApplicationFiled: February 27, 2002Publication date: August 7, 2003Inventor: Velayudhan Sahadevan
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Publication number: 20030144258Abstract: A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6&bgr;,7&bgr;; 15&bgr;; 16&bgr;-dimethylene-3-oxo-17&agr;-preg-4-ene-21,17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form.Type: ApplicationFiled: February 6, 2003Publication date: July 31, 2003Applicant: Schering AktiengesellschaftInventors: Wolfgang Heil, Juergen Hilmann, Ralph Lipp, Rolf Schuermann
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Patent number: RE38253Abstract: A combination product for oral contraception is disclosed comprising an estrogen selected from 2.0 to 6.0 mg of 17&bgr;-estradiol and 0.020 mg of ethinylestradiol; and a gestagen selected from 0.25 to 0.30 2.5 to 3.0 mg of drospirenone and 0.1 to 0.2 1 to 2 mg of cyproterone acetate, followed by 5 or 4 pill-free or sugar pill days.Type: GrantFiled: February 25, 2002Date of Patent: September 16, 2003Assignee: Schering AktiengesellschaftInventors: Jürgen Spona, Bernd Düsterberg, Frank Lüdicke