Oxygen Double Bonded To A Ring Carbon Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 514/177)
Oxygen single bonded to a ring carbon of the cyclopentanohydrophenanthrene ring system (Class 514/178)
  • Method of increasing the sensitivity of mammography
    Publication number: 20040028610
    Abstract: Methods of improving detection of cancerous lesions in the breast through breast examination are provided. Such methods comprise administering to a patient in need of a breast examination, an androgen, preferably testosterone or a derivative thereof, in an amount sufficient to reduce the palpable breast tissue density or radiographic breast tissue density of the patient. Methods of treating conditions associated with dense breasts in a patient are also provided. Such methods comprise administering, a biologically effective amount of an androgen to a patient in need of the same. In accordance with the present invention, it has been found that administration of testosterone to pre- and post-menopausal women with fibrous or dense breasts results in a decrease in palpable breast density, radiographic density, and the number or size of fibrous breast lesions in these women.
    Type: Application
    Filed: September 22, 2003
    Publication date: February 12, 2004
    Inventor: Stephen E. Zimberg
  • Compounds useful for treating hypertriglyceridemia
    Publication number: 20040019026
    Abstract: The present invention is directed to a method for treating a patient having hypertriglyceridemia comprising administering thereto a compound of the formula: 1
    Type: Application
    Filed: April 7, 2003
    Publication date: January 29, 2004
    Inventor: Arthur G. Schwartz
  • Initiation of oestrus
    Patent number: 6683071
    Abstract: This invention relates to a method for the initiation of oestrus and ovulation early postpartum, especially but not exclusively, in dairy cows which comprises supplying a prostaglandin post partum and subsequently treating with a progesterone.
    Type: Grant
    Filed: July 17, 2002
    Date of Patent: January 27, 2004
    Assignees: The University of Nottingham, Milk Development Council
    Inventor: George Eric Lamming
  • Use of dhea and some of its derivatives in a cosmetic composition for preventing or treating dermal atrophy
    Publication number: 20040009196
    Abstract: The present invention relates to the use of DHEA and/or of its chemical and/or biological precursors and derivatives, in a cosmetic composition or for the manufacture of a dermatological composition for topical application to the skin, for preventing atrophy of the epidermis which is one of the characteristic signs of intrinsic and/or photoinduced skin ageing.
    Type: Application
    Filed: June 30, 2003
    Publication date: January 15, 2004
    Inventors: Corrine Ferraris, Isabelle Castiel, Olivia Zobiri
  • Pharmaceutical composition with tumor necrosis factor A and 2-methoxyestrone-3-0-sulphamate for inhibition of estrone sulphatase
    Patent number: 6676934
    Abstract: A composition is described. The composition comprises i) a compound comprising a sulphamate group (“a sulphamate compound”); and ii) a biological response modifier.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: January 13, 2004
    Assignee: Sterix Limited
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Methods and compositions for treating diseases due to androgen deficiency with glucocorticoid receptor antagonist compounds and new compounds
    Patent number: 6670493
    Abstract: The method of treating or preventing a disease in a human male or a male animal caused by a decreased production of androgens, such as testosterone, in the human male or male animal includes administering an effective amount of a glucocorticoid receptor antagonist to the human male or the male animal in order to increase production of the androgens. These diseases include male sexual dysfunction, infertility and hypogonadism. Novel androgen receptor antagonist compounds and methods of synthesis are also described.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: December 30, 2003
    Assignee: Jenapharm GmbH & Co. KG
    Inventors: Vladimir Patchev, Lothar Sobek, Gerd Schubert
  • Method of administering dienogest in high dosages to reduce the body of the breast and pharmaceutical composition for same
    Patent number: 6670350
    Abstract: A method of administering dienogest to a women in high dosages for reducing the body of the breast is described. The dosage should be at least ten times the effective dosage for inhibiting ovulation in the women. A pharmaceutical composition for use in the method is also described. Furthermore, retrogression of mastopathic changes in the body of the breast can be brought about. Dienogest is also outstandingly suitable for the prophylaxis of mastopathies. In high dosages, dienogest prevents the formation of mastopathic changes in the body of the breast.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: December 30, 2003
    Assignee: JenaPharm GmbH & Co. KG
    Inventors: Michael Oettel, Claudia Moore, Adolf Eduard Schindler, Bernd Christensen
  • PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING HYPOGONADISM
    Publication number: 20030232072
    Abstract: A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition.
    Type: Application
    Filed: January 3, 2003
    Publication date: December 18, 2003
    Inventors: Robert E. Dudley , S. George Kottayil , Olivier Palatchi
  • Treatments for age-related macular degeneration (AMD)
    Publication number: 20030229062
    Abstract: The present invention addresses the treatment of age-related macular degeneration using regulation of pathogenic mechanisms similar to atherosclerosis. In further specific embodiments, reverse cholesterol transport components, such as transporters and HDL fractions, are utilized as diagnostic and therapeutic targets for age-related macular degeneration. In a specific embodiment, the lipid content of the retinal pigment epithelium, and/or Bruch's membrane is reduced.
    Type: Application
    Filed: May 2, 2003
    Publication date: December 11, 2003
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Daniel M. Schwartz, Keith G. Duncan, Kathy R. Bailey, John P. Kane, Brian Y. Ishida
  • Method and compositions for solubilization of pentacyclic triterpenes
    Patent number: 6656970
    Abstract: The present invention provides compositions and methods for the solubilization of poorly soluble drugs such as triterpenes like betulinic acid and/its derivatives in pharmaceutically acceptable liquid vehicles that avoid use of potentially toxic solvents that are often used for the solubilization of poorly soluble drugs. In the compositions of this invention the drugs remain physically and chemically stable and can be administered intravascularly without undue toxicity from undissolved drug and/or from the solvent vehicles at a drug dose meant to be effective to exhibit clinically significant anticancer activity.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: December 2, 2003
    Assignee: Dabur Research Foundation
    Inventors: Anand C. Burman, Rama Mukherjee, Honey Bala, Dhiraj Khattar
  • Matrix-type device for the transdermal delivery of testosterone applied to the non-scrotal skin
    Publication number: 20030215487
    Abstract: The present invention relates to a matrix-type device for the transdermal delivery of testosterone comprising (i) a matrix layer containing a) a therapeutically effective amount of testosterone or the salt thereof, b) an adhesive polymer, and c) a penetration enhancer comprising N-methylpyrrolidone and oleoylsarcosine, and, (ii) a backing layer of polyurethane. The device of the present invention is applicable to a non-scrotal skin as compared with a known matrix-type device for the transdermal delivery and has an excellent skin-adhesion and has less tendencies of crystallizing testosterone.
    Type: Application
    Filed: May 17, 2002
    Publication date: November 20, 2003
    Applicant: IL YANG PHARM CO., LTD. Republic of Korea
    Inventors: Dong-Yeun Kim, Dong-Woo Park, Sookyun Kim
  • Immediate release eplerenone compositions
    Publication number: 20030215518
    Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.
    Type: Application
    Filed: November 6, 2002
    Publication date: November 20, 2003
    Inventors: Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
  • Dry powder for inhalation
    Patent number: 6645466
    Abstract: The aim of the invention is to improve the moisture resistance of dry powder formulations for inhalation which contain a pharmaceutically ineffective carrier of not-inhalable particle size and a finely divided pharmaceutically active compound of inhalable particle size and to also improve the storage stability of said formulations. To this end, magnesium stearate is used in said formulations. One of the features of the inventive dry powder is that a high fine particle dosage or fine particle fraction can be maintained also under relatively extreme temperature and humidity conditions.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: November 11, 2003
    Assignee: Jago Research AG
    Inventors: Manfred Keller, Rudi Müller-Walz
  • Compositions comprising ethisterone or its derivatives
    Patent number: 6645954
    Abstract: Treatment of androgen deficiency using a pharmaceutically effective dose of ethisterone or an ethisterone derivative such as Danazol. In particular, androgen deficiency in the aging male, also known as the male climacteric andropause or the male menopause, can be treated by ethisterone or ethisterone derivatives. Treatment of hypogonadism using ethisterone or ethisterone derivative in combination with testosterone is also effective.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: November 11, 2003
    Assignee: Multimed Limited
    Inventor: Malcolm Carruthers
  • Meiosis regulating compounds
    Patent number: 6645953
    Abstract: Sterol derivative compounds, structurally related to natural compounds which can be extracted from bull testes and from human follicular fluid, useful for regulating meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: November 11, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Frederik Christian Gronvald, Peter Faarup, Erling Guddal
  • Pressurized aerosol compositions comprising powdered medicament dispersed in hydrofluoroalkane
    Patent number: 6641800
    Abstract: Pressurized aerosol composition for administration by inhalation comprising a liquefied hydrofluoroalkane, a powdered medicament dispersed therein, and a suspending agent comprising a polymer soluble in the liquefied hydrofluoroalkane which is selected from polymers including recurring amide containing structural units, copolymers of amide containing units and carboxylic acid ester units, polyvinylacetate and acrylic acid/methacrylic acid ester copolymers.
    Type: Grant
    Filed: July 13, 2000
    Date of Patent: November 4, 2003
    Assignee: Fisons Ltd.
    Inventors: Suresh N Mistry, Mark Gibson
  • Progestogen-antiprogestogen regimens
    Patent number: 6642219
    Abstract: 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: Grant
    Filed: June 26, 2000
    Date of Patent: November 4, 2003
    Assignee: Akzo Nobel N.V.
    Inventor: Herman Jan Tijmen Coelingh Bennink
  • Novel composition for transdermal and/or transmucosal administration of active compounds that ensures adequate therapeutic levels
    Publication number: 20030199426
    Abstract: The present invention refers to a pharmaceutical composition suitable for the transdermal or transmucosal administration of one or more active agents, in form of a gel or a solution, comprising as a permeation enhancers a combination of: a) saturated fatty alcohol of formula CH3—(CH2)n—CH2OH or saturated fatty acid CH3—(CH2)n—CH2COOH wherein n is an integer number 8÷22, preferably 8÷12, most preferably 10, or unsaturated fatty alcohol or fatty acid of formula: CH3(CnH2(n−1))—OH or CH3(CnH2(n−1))—COOH wherein n is an integer number 8÷22, b) a ternary vehicle or carrier consisting of a C1÷C4 alkanol, a polyalcohol in particular propylenglycol and water, c) optionally also a monoalkylether of diethylenglycol.
    Type: Application
    Filed: May 19, 2003
    Publication date: October 23, 2003
    Inventors: Dario Carrara, Gabriel Porto, Jorge Rodriguez
  • Estrogenic compounds as anti-mitotic agents
    Publication number: 20030195180
    Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
    Type: Application
    Filed: March 3, 2003
    Publication date: October 16, 2003
    Inventors: Robert John D'Amato, Moses Judah Folkman
  • Methods for the treatment or prophylaxis of aldosterone-mediated pathogenic effects in a subject
    Publication number: 20030191100
    Abstract: The present invention provides methods for the treatment or prophylaxis of one or more aldosterone-mediated pathogenic effects in a subject suffering from or susceptible to the pathogenic effect or effects wherein the subject has one or more conditions selected from the group consisting of a sub-normal endogenous aldosterone level, salt sensitivity and an elevated dietary sodium intake. The methods comprise administering to the subject a therapeutically-effective amount of one or more aldosterone antagonists.
    Type: Application
    Filed: September 13, 2002
    Publication date: October 9, 2003
    Applicant: Pharmacia Corporation, Corporate Patent Department
    Inventors: Gordon H. Williams, John W. Funder, Susan M. Garthwaite, Barbara Roniker, Kenton N. Fedde, Ricardo Rocha
  • Enone cancer therapeutics
    Publication number: 20030191066
    Abstract: New enone derivatives and conjugates are described. These compounds can be used as cancer therapeutics.
    Type: Application
    Filed: March 15, 2002
    Publication date: October 9, 2003
    Applicant: Cornell Research Foundation, Inc.
    Inventors: Bruce Ganem, Donald J. Creighton, Diana S. Hamilton, Zhebo Ding
  • Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors
    Publication number: 20030186952
    Abstract: A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.
    Type: Application
    Filed: February 1, 2002
    Publication date: October 2, 2003
    Inventors: Marshall D. Crew, William J. Curatolo, Dwayne T. Friesen, Michael Jon Gumkowski, Douglas A. Lorenz, James A. S. Nightingale, Roger B. Ruggeri, Ravi M. Shanker
  • AlphaAED and betaAED regulation of nuclear transcription, gene regulation, and/or gene expression
    Publication number: 20030181434
    Abstract: The present invention provides a means to regulate nuclear transcription and/or gene expression. The present invention also provides a means to regulate the levels of PPAR-&ggr;, COX-2 and/or NF&kgr;B in a patient. The method of the present invention involves administering &agr;AED (or an analogue thereof) or &bgr;AED (or an analogue thereof) or both to a patient in need of regulation of nuclear transcription and/or gene expression and/or levels of PPAR-&ggr;, COX-2, and/or NF&kgr;B. The methods of the present invention can be used to control adipogenesis (i.e. to treat obesity), angiogenesis, atherosclerosis, mesenteric fat hypertrophy, inflammatory bowel disease, colitis, Alzheimer's disease, and inflammatory glial responses in the brain. The methods of the present invention can also be used for treating diabetes, for regulating the immune response, and for regulating inflammation in a patient.
    Type: Application
    Filed: March 21, 2003
    Publication date: September 25, 2003
    Inventor: Roger M. Loria
  • Novel topical oestroprogestational compositions with a systemic effect
    Publication number: 20030181430
    Abstract: 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: Application
    Filed: June 26, 2002
    Publication date: September 25, 2003
    Inventors: Georges Gray, Bertrand Villet, Jacques ` Paris, Jean-Louis Thomas
  • Semisolid topical hormonal compositions and methods for treatment
    Publication number: 20030175329
    Abstract: Semisolid topical pharmaceutical compositions comprising a therapeutically effective amount of a mammalian hormone and an effective amount of a penetration enhancer and methods for their use are provided. The pharmaceutical compositions and methods for their use can provide blood or plasma levels of the administered hormone within a predetermined or normal range of hormone values. In particular embodiments, the hormone is testosterone or estrogen and the amount to be applied to the skin of the subject is determined according to the weight or body mass index of the subject. The topical composition can be formulated in solutions, creams, lotions, ointments, and gels.
    Type: Application
    Filed: October 4, 2002
    Publication date: September 18, 2003
    Applicant: Cellegy Pharmaceuticals, Inc.
    Inventors: Daniel L. Azarnoff, Vivien H.W. Mak
  • Polycaprolactone-b-poly (ethylene oxide) copolymer non-cross-linked micelles as a delivery vehicle for steroid
    Publication number: 20030176406
    Abstract: The present invention relates to non-cross-linked micelles as delivery vehicles for steroid compounds and more particularly to a polycaprolactone-b-poly(ethylene oxide) copolymer micelle as a delivery vehicle for steroids. The delivery system comprises a population of diblock copolymer non-cross-linked micelles, each micelle defining a non-cross-linked core for containing the steroid compound. The delivery system of the present invention maintains the release of the steroid compound in a patient having a deficient steroid level.
    Type: Application
    Filed: December 10, 2002
    Publication date: September 18, 2003
    Applicant: McGill University
    Inventors: Christine Allen, Adi Eisenberg, Dusica Maysinger
  • Diagnosis of pre-eclampsia
    Patent number: 6620590
    Abstract: A method for diagnosis of pre-eclampsia is disclosed, which comprises measuring the hormone inhibin A in a biological sample such as maternal serum. The method allows non-invasive, early diagnosis and can be used to predict the onset of secondary symptoms.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: September 16, 2003
    Assignees: Isis Innovation Limited, The University of Reading, Oxford Brookes University
    Inventors: Nigel Patrick Groome, Philip Gerald Knight, William Leigh Ledger, Christopher Willard George Redman, Shanthi Muttukrishna
  • Dermal cytochrome P450 1A inhibitors and enhancers
    Publication number: 20030166583
    Abstract: The present invention provides dermal cytochrome P450 1A (CYP1A) inhibitors, which include free base or pharmacologically acceptable salt of (−)-epicatechin, (+)-epicatechin, (+)-limonene, 3-phenylpropyl acetate, &agr;-naphthoflavone, apigenin, baicalein, baicalin, &bgr;-myrcene, catechin, &bgr;-naphthoflavone, cineole, daidzein, daidzin, diosmin, ergosterol, formononetin, gallic acid, genistein, glycyrrhizin, glycyrrhizic acid, hesperetin, hesperidin, isoquercitrin, kaempferol, lauryl alcohol, luteolin, luteolin-7-glycoside, narigenin, narigin, nordihydroguaiaretic acid, oleanolic acid, paeoniflorin, quercetin, quercitrin, rutin, swertiamarin, terpineol, trans-cinnamaldehyde, trans-cinnamic acid, umbelliferone, genkwanin, homoorientin, isovitexin, neohesperidin, wongonin, capillarisin, liquiritin, ethyl myristate, poncirin, and ursolic acid.
    Type: Application
    Filed: February 22, 2002
    Publication date: September 4, 2003
    Inventors: Oliver Yoa-Pu Hu, Cheng-Huei Hsiong, Chao-Jih Wang, Li-Heng Pao
  • Penetration enhancing and irritation reducing systems
    Publication number: 20030166625
    Abstract: This invention lies in the technology of transdermal and topical drug delivery. In particular, the present invention relates to enhancement of the penetration of transdermally or topically applied drugs and with the reduction of skin irritation that often accompanies transdermal and topical drug delivery.
    Type: Application
    Filed: March 12, 2003
    Publication date: September 4, 2003
    Applicant: CELLEGY PHARMACEUTICALS INC.
    Inventors: Vivien H.W. Mak, Stephen Grayson
  • Method of treating inflammatory conditions with progesterone analogs
    Patent number: 6610674
    Abstract: The present invention provides methods for treating inflammatory conditions, including but not limited to, inflammatory bowel disease (ulcerative colitis, Crohn's disease, and proctitis), other noninfectious, inflammatory conditions of the GI tract (microscopic colitis, allergic eosinophilic gastroenteritis, food allergies, pill induced esophagitis, celiac disease, recurrent polyps, and hemorrhoids), and psoriasis, using progesterone or progesterone analogs such as medroxyprogesterone acetate.
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: August 26, 2003
    Assignee: University of Pennsylvania
    Inventor: Alan D. Schreiber
  • Administration of non-oral androgenic steroids to women
    Publication number: 20030153540
    Abstract: 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: Application
    Filed: October 22, 2002
    Publication date: August 14, 2003
    Inventors: Theresa Rosario-Jansen, Norman A. Mazer
  • Estrogenic substances combined with cruciferous indole compounds
    Patent number: 6605605
    Abstract: Provided herein are medicinal compositions of matter that comprise an estrogenic medication component and a cruciferous indole component (indole 3-carbinol, diindolylmethane, or any derivative thereof. Through use of the compositions of the invention a heretofore unobserved synergy is observed in the treatment of perimenopause, menopause or any other cause of ovarian failure. The invention also provides procedures for administering the composition to a patient who is afflicted with perimenopause, menopause or any other cause of ovarian failure.
    Type: Grant
    Filed: November 10, 2001
    Date of Patent: August 12, 2003
    Inventor: Milton Hammerly
  • Selective 11beta-HSD inhibitors and methods of use thereof
    Publication number: 20030148987
    Abstract: Methods for treating glucocorticoid associated states using selective 11&bgr;-HSD1-dehydrogenase, 11&bgr;-HSD1-reductase and 11&bgr;-HSD2 dehydrogenase modulating compounds are described.
    Type: Application
    Filed: December 20, 2002
    Publication date: August 7, 2003
    Inventors: David J. Morris, Andrew S. Brem
  • Methods and tests for producing and for inhibiting coronary artery vasospasms
    Patent number: 6602487
    Abstract: Methods for producing coronary vasospasms and for inhibiting coronary vasospasms are disclosed. Both in vivo and in vitro methods are disclosed. The methods are useful as tests for determining the ability of a chemical compound to inhibit or reduce coronary vasospasms.
    Type: Grant
    Filed: August 16, 2000
    Date of Patent: August 5, 2003
    Assignee: Dimera Incorporated
    Inventor: R. Kent Hermsmeyer
  • Breast cancer hormonal therapy
    Publication number: 20030144259
    Abstract: Exemestane is disclosed for use in the first-line treatment of metastatic, advanced hormone-dependent breast cancer, particularly in post-menopausal woman.
    Type: Application
    Filed: January 28, 2003
    Publication date: July 31, 2003
    Inventors: Giorgio Massimini, Robert Paridaens, Jean-Pierre Lobelle, Gabriella Piscitelli
  • Method for treating erectile dysfunction and increasing libido in men
    Publication number: 20030139384
    Abstract: The present invention relates to a transdermal hydroalcoholic testosterone gel formulation that overcomes the problems associated with other testosterone delivery mechanisms by providing, among other things, a desirable pharmacokinetic hormone profile with little or no skin irritation. In addition, the gel is used in conjunction with pharmaceuticals aimed at treating erectile dysfunction, such as VIAGRA®, to enhance their effectiveness.
    Type: Application
    Filed: October 18, 2002
    Publication date: July 24, 2003
    Inventor: Robert E. Dudley
  • Methods of treating cognitive decline disease conditions with androgens
    Publication number: 20030139362
    Abstract: Methods for treating a host, particularly a female host, for a cognitive decline disease condition are provided. Also provided are methods for improving the cognitive function of a host. In the subject methods, an effective amount of androgenic agent, e.g., a male sex hormone such as testosterone or analogue thereof, is administered to the host, resulting in at least an improvement in cognitive function of the host. The subject methods find use in a variety of different applications, and are particularly suited for use in treating female hosts for neurodegenerative disease conditions, e.g., Alzheimer's disease. Also provided are kits for use in practicing the subject methods.
    Type: Application
    Filed: September 27, 2002
    Publication date: July 24, 2003
    Inventors: Jacob Raber, Lennart Mucke
  • 19-Nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, their use as medicaments and compositions
    Patent number: 6596885
    Abstract: Novel compounds having a formula selected from the group consisting of wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-proliferative activity.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: July 22, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Andre Claussner, Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
  • Halogenated sulphamate-, phosphonate-, thiophosphonate-, sulphonate- and sulphonamide- compounds as inhibitors of steroid sulphatase
    Publication number: 20030134829
    Abstract: A compound is described. The compound has the formula (Ia) as presented in the FIG. 1; wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at least one of Rh1 and Rh2 is present; Rs is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group. The compound is capable of inhibiting steroid sulphatase (STS) activity.
    Type: Application
    Filed: June 7, 2002
    Publication date: July 17, 2003
    Inventors: Michael John Reed, Barry Victor Lloyd Potter, Hatem Hejaz, Atul Purohit
  • Progestin therapy for maintaining amenorrhea
    Patent number: 6593317
    Abstract: The present invention teaches that daily, cyclical vaginal delivery of progestin may be used to provide regular, predictable withdrawal bleeding during hormone replacement therapy. The present invention also teaches that constant administration of progestin in a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer may be used to maintain amenorrhea. Either regimen is accompanied by a significant decrease in adverse side effects.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: July 15, 2003
    Assignee: Columbia Laboratories, Inc.
    Inventors: Dominique de Ziegler, William J. Bologna, Howard L. Levine
  • Use of &Dgr;5-androstene-3&bgr;ol-7,17-dione in the treatment of lupus erythematosus
    Patent number: 6593316
    Abstract: Lupus erythematosus can be treated by administering therapeutic amounts of &Dgr;5-androstene-3&bgr;-ol-7,17-dione and metabolizable precursors thereof, such as &Dgr;5-androstene-3&bgr;-acetoxy-7,17-dione, which are readily metabolized in vivo to &Dgr;5-androstene-3&bgr;-ol-7,17-dione but are not appreciably metabolizable in vivo to androgens, estrogens or dehydroepiandrosterone. Such treatment can be prophylactic, ameliorative or curative in nature.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: July 15, 2003
    Inventors: Henry A. Lardy, Charles E. Weeks
  • Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
    Publication number: 20030130246
    Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
    Type: Application
    Filed: August 28, 2002
    Publication date: July 10, 2003
    Inventors: Laxminarayan Bhat, Mark A. Gallop, Bernd Jandeleit
  • Use of an immediate-release powder in pharmaceutical and nutraceutical compositions
    Publication number: 20030124191
    Abstract: The present invention relates to the use of a powder comprising at least one active substance, at least one surfactant, at least one wetting agent and at least one diluent, for preparing a pharmaceutical or nutraceutical composition, this composition allowing rapid and immediate release of the active substance.
    Type: Application
    Filed: March 25, 2002
    Publication date: July 3, 2003
    Inventors: Jerome Besse, Laurence Besse
  • Methods of treatment using an epithelial sodium channel blocker and an inhibitor of the mineralocorticoid receptor
    Patent number: 6586416
    Abstract: Co-administration of a channel blocking epithelial sodium channel (ENaC) blocker in conjunction with a mineralocorticoid receptor inhibitor makes it possible to achieve desired lowering of blood pressure with use in the range of 20% to 75% or less of the presently used dosage of the mineralocorticoid receptor inhibitor (MRI), thus avoiding many of the deleterious side effects usually associated with administration of an MRI. As little as 10% of the usual dosage of MRI may, in some cases, be efficacious. The most commonly used ENaC blocker now in use is amiloride. The most commonly used inhibitors of the mineralocorticoid receptor are precursors of canrenone.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: July 1, 2003
    Inventor: James K. Bubien
  • Method for reducing coronary artery reactivity
    Publication number: 20030119799
    Abstract: A method for treating myocardial ischemia and angina pectoris comprising administering to a subject in need thereof an effective amount of progesterone with or without estrogen.
    Type: Application
    Filed: October 7, 2002
    Publication date: June 26, 2003
    Inventor: R. Kent Hermsmeyer
  • Administration of non-oral androgenic steroids to women
    Patent number: 6583129
    Abstract: 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: Grant
    Filed: June 9, 2000
    Date of Patent: June 24, 2003
    Assignee: Watson Pharmaceuticals, Inc.
    Inventors: Norman A. Mazer, Theresa Rosario-Jansen
  • Stabilized injectable suspension of a steroidal drug
    Publication number: 20030114430
    Abstract: A parenterally deliverable composition is provided, comprising an aqueous medium having dispersed therein, in solid particulate form, a steroidal drug in a therapeutically effective amount. The aqueous medium comprises one or more wetting and/or suspending agents in an amount effective to provide controlled flocculation of the drug, at least one of the wetting and/or suspending agents being susceptible to oxidative degradation. The composition further comprises, as a component thereof or as an adjunct thereto, means for protecting the oxidative degradation susceptible agent from oxidative degradation.
    Type: Application
    Filed: August 21, 2002
    Publication date: June 19, 2003
    Inventors: Steven K. MacLeod, Lloyd E. Fox, Neal S. Adams, David J. Salvat
  • Methods for treating pulmonary fibrosis
    Publication number: 20030113330
    Abstract: The present invention relates to uses of non-thiol ACE inhibitors, angiotensin II antagonists, angiotensin II receptor antagonists, endonuclease inhibitors, and caspase-inhibitors to treat pulmonary fibrosis and/or inhibit pulmonary epithelial cell apoptosis, including pulmonary fibrosis associated with amiodarone product toxicity.
    Type: Application
    Filed: January 6, 2003
    Publication date: June 19, 2003
    Inventor: Bruce D. Uhal
  • 3-methylene steroid derivatives
    Patent number: 6579864
    Abstract: The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a &bgr;-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C1-C5) alkyl or CF3; R3 is &bgr;H, &bgr;CH3 or together with R1 forms a &bgr;-epoxide or R3 is absent if there is a 5-10 double bond; R4 is H, lower alkyl; Y is [H, H], [OH, H], ═O, [OH, lower alkyl], [OH, (C2-C5)alkenyl], [OH, (C2-C5)alkynyl] or (C1-C6) alkylidene, whereby said alkyl, alkenyl, alkynyl and alkylidene is optionally halogenated; ═NOR5, whereby R5 is H, lower alkyl; dotted lines represent an optional double bond, or prodrugs thereof for the treatment of arthritic diseases and/or autoimmune diseases.
    Type: Grant
    Filed: May 29, 2002
    Date of Patent: June 17, 2003
    Assignee: Akzo Nobel NV
    Inventors: Ralf Plate, Wilhelmina Maria Bagchus
  • Novel androgens
    Publication number: 20030100543
    Abstract: The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14&bgr;,15&bgr;-cyclopropane ring and a 17&agr; hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.
    Type: Application
    Filed: September 11, 2002
    Publication date: May 29, 2003
    Inventors: Dirk Leysen, Jaap Van der Louw, Roberta Buma Bursi, Marcel Evert De Gooyer