21-position Substituted Patents (Class 514/181)
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Publication number: 20090169587Abstract: A chronotherapeutic pharmaceutical formulation comprising a core containing an active agent (e.g., a drug) and a surfactant and a delayed release compression coating comprising a natural or synthetic gum applied onto the surface of the core.Type: ApplicationFiled: March 2, 2009Publication date: July 2, 2009Applicant: Penwest Pharmaceuticals Co.Inventors: Anand R. Baichwal, Paul Woodcock, Steve Labudzinski
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Patent number: 7553829Abstract: Chronic fatigue syndrome (CFS) and fibromyalgia syndrome (FMS) can be treated by the administration of ?5-androstene-3?-ol-7,17 dione and metabolizable precursors thereof.Type: GrantFiled: October 31, 2001Date of Patent: June 30, 2009Assignee: Humanetics CorporationInventors: Ronald J. Zenk, John L. Zenk
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Publication number: 20090143328Abstract: The present invention provides for methods of treating cancer comprising administering a topical active corticosteroid in conjunction with a form of non-myeloablative conditioning, wherein the above regimen results in a reduction or elimination of cancer cells in an individual.Type: ApplicationFiled: August 5, 2008Publication date: June 4, 2009Inventor: George McDonald
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Publication number: 20090117203Abstract: To provide a kit for cancer treatment and a pharmaceutical composition for cancer treatment that can inhibit the growth of tumors and cancers in mammals more than ever. The kit for cancer treatment includes a combination of two different drugs in a kit formulation. The first drug contains a synthetic retinoid or a pharmaceutically acceptable organic or inorganic acid addition salt thereof, and the second drug contains a chemotherapeutic agent for cancer treatment. A synthetic retinoid that can be suitably used is a benzoic acid derivative represented by the following formula (I): or a pharmaceutically acceptable organic or inorganic acid addition salt thereof.Type: ApplicationFiled: February 22, 2007Publication date: May 7, 2009Applicant: TMRC Co., Ltd.Inventor: Hisao Ekimoto
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Patent number: 7528123Abstract: Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11?-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor ? and estrogen receptor ?.Type: GrantFiled: November 18, 1999Date of Patent: May 5, 2009Assignee: N.V. OrganonInventors: Hubert Jan Jozef Loozen, Wilhelmus Gerardus Eduardus Joseph Schoonen
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Publication number: 20090111784Abstract: The present invention relates to novel uses of a steroid compound, which specifically binds to the androgen receptor (AR) but which is not metabolized by aromatase to a process for their preparation, to pharmaceutical compositions containing them, and to the use of said compounds for the prophylaxis and/or treatment of hormone-dependent or hormone receptor regulated cancers in mammals.Type: ApplicationFiled: May 11, 2007Publication date: April 30, 2009Inventor: Alexander Tobias Teichmann
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Publication number: 20090093449Abstract: The present invention relates to formulations of concentrated azalide antibiotics and methods for making and using them. Specifically, the invention relates to a method of treating an infection comprising administering to a patient in need thereof, an effective amount of a concentrated aqueous azalide antibiotic formulation made according to the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. The invention also relates to methods for making concentrated aqueous azalide antibiotic formulations for use in pulmonary infection, a nasopharyngeal infection, an otic infection, an ocular infection, a dermal or a vaginal infection. The invention also relates to concentrated aqueous azalide antibiotic formulations made by dissolving an azalide antibiotic in an aqueous solution comprising a strong acid.Type: ApplicationFiled: October 4, 2007Publication date: April 9, 2009Inventors: Lyle Bowman, S. Kumar Chandrasekaran, Roy Duane Archibald, Stephen Pham, David Mufson
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Publication number: 20090088413Abstract: A topical composition for treatment of contact dermatitis comprising a corticosteroid, one or more drying agents, such as zinc oxide and talc, an alcohol solvent, a humectant and a viscosity agent, such as bentonite. The humectant may be glycerin, and the carrier is water.Type: ApplicationFiled: September 27, 2007Publication date: April 2, 2009Inventor: Bruce Burkenstock, SR.
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Publication number: 20090075960Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicants: THE HOSPITAL FOR SICK CHILDREN, McMASTER UNIVERSITYInventors: Don J. Mahuran, Michael B. Tropak, Justin D. Buttner, Jan E. Blanchard, Eric D. Brown
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Publication number: 20090035375Abstract: The present invention relates to glucocorticoid-containing pharmaceutical compositions or kits for use in acute emergency situations where acute glucocorticoid therapy is required. Notably, the invention relates to pharmaceutical compositions and kits that are designed to be administered by non-medically trained persons outside a hospital or another medical or clinical setting.Type: ApplicationFiled: April 21, 2005Publication date: February 5, 2009Inventors: Stanko Skrtic, Jorgen Johnsson, Hans Lennernas, Thomas Hedner, Gudmundur Johannsson
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Patent number: 7479486Abstract: The present invention is related to novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues, their use as antiglucocorticoids for the treatment and/or prophylaxis of disease associated to an excess of glucocorticoids. In particular, the invention relates to the use of novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues for treating Cushing's syndrome, iatrogenic hypercortisolism or depression. Also the present invention is related to methods of preparing the novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues.Type: GrantFiled: May 6, 2005Date of Patent: January 20, 2009Assignee: Laboratoires Serono SAInventors: Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
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Publication number: 20090004232Abstract: Physically stable pharmaceutical/cosmetic compositions contain at least one hydrophilic phase, at least one lipophilic phase and at least one active principle, e.g., at least one steroidal anti-inflammatory agent, anti-fungal agent, anti-parasitic agent, nuclear receptor modulator and/or sex steroid, said at least one active principle being present in dissolved state in each of these phases; these are formulated via characteristic multi-step methodology.Type: ApplicationFiled: May 12, 2008Publication date: January 1, 2009Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: ALAIN BRZOKEWICZ
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Patent number: 7456161Abstract: A method for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.Type: GrantFiled: June 3, 2003Date of Patent: November 25, 2008Assignee: Epigenesis Pharmaceuticals, LLCInventor: Jonathan W. Nyce
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Publication number: 20080269875Abstract: Methods for making comb-type antithrombotic conjugate wherein substantially all side chains of water soluble poly(vinyl alcohol) (PVA) are extended by ring-opening polymerization to form a copolymer wherein substantially all terminals are conjugated to an antithrombotic molecule. In addition, a method is provided for applying a coating comprising a comb-type anti-thrombotic conjugate to at least a portion of an implantable device to prevent or reduce the formation of thrombosis on the surface of the device. A first or sub-layer of the coating is prepared by mixing a polymeric material and a biologically active agent with a solvent, thereby forming a homogeneous solution. A second or outer layer comprising a comb-type anti-thrombotic conjugate may be applied over the inner drug-containing layers using, for example, a dip coating or spray coating process.Type: ApplicationFiled: April 30, 2007Publication date: October 30, 2008Inventor: Jonathon Z. Zhao
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Patent number: 7442386Abstract: The invention relates to compositions and methods for a one-step synthetic technique for making cationic steroid or cationic drug molecules for use as delivery vehicles. The invention further relates to methods for using cationic steroid molecules in lipofection or transfection, delivery of drugs, and for treatment of inflammation and other diseases and disorders. The invention also relates to cationic steroid prodrugs and cationic prodrugs and to methods of modifying drugs.Type: GrantFiled: February 12, 2004Date of Patent: October 28, 2008Assignee: The Trustees of the University of PennsylvaniaInventors: Scott L. Diamond, Jeffrey Alan Gruneich
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Publication number: 20080221072Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.Type: ApplicationFiled: May 15, 2008Publication date: September 11, 2008Applicant: SEPRACOR INC.Inventors: Mark G. Currie, Steven Jones, Charles M. Zepp
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Publication number: 20080207570Abstract: Novel topically applicable oil-in-water emulsions, with a high proportion of oily phase in the inner phase, combine the occlusive and emollient properties of an ointment without having the drawbacks of a greasy feel, while at the same time promoting the therapeutic properties of a biologically active agent contained therein; such emulsions are especially useful for the treatment of dermatological diseases, conditions or afflictions, notably psoriasis.Type: ApplicationFiled: February 8, 2008Publication date: August 28, 2008Applicant: L'OREALInventor: Sandrine Segura-Orsoni
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Publication number: 20080139522Abstract: The present invention relates to the use of xanthan gum as re-epithelializing agent and, in particular, to a pharmaceutical formulation comprising xanthan gum as a re-epithelializing active principle eventually mixed with hyaluronic acid. Said use and composition speed up and improve advantageously the formation of newly grown epithelium.Type: ApplicationFiled: February 14, 2008Publication date: June 12, 2008Applicant: SIFI S.p.A..Inventors: Maria Grazia Mazzone, Grazia Paladino, Clara Marino, Ornella Peri, Vincenzo Enea
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Patent number: 7378405Abstract: Stabilized 17-substituted hydrocortisone containing compositions and methods of manufacture. Isomerization of the hydrocortisone component of topical steroid compositions is markedly reduced by introducing an omega-6. acid in the form of linoleic acid into the skin preparation. Preferably, the linoleic acid is added as a component of refined safflower oil. The omega-6 acid has been found to be an effective way of preventing the isomerization of hydrocortisone 17-butyrate into the undesirable isomer HC21-B.Type: GrantFiled: January 22, 2004Date of Patent: May 27, 2008Assignee: Triax Pharmaceuticals, LLCInventor: Pravin M. Patel
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Patent number: 7345035Abstract: The invention provides methods of downregulating mRNA encoding osteopontin comprising administering to a cell or mammal an amount of astrogorgiadiol effective to downregulate production of mRNA encoding osteopontin. The invention also provides methods of treating osteoporosis and autoimmune disease comprising administering to a patient in need of such treatment a therapeutically effective amount of astrogorgiadiol. Pharmaceutical compositions comprising astrogorgiadiol and a pharmaceutically acceptable carrier or diluent are also provided.Type: GrantFiled: May 28, 2003Date of Patent: March 18, 2008Assignee: University of DelawareInventors: Douglass F. Taber, Mary C. Farach-Carson, Scott C. Malcolm, Yihuan Xu
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Patent number: 7335650Abstract: There is provided a pharmaceutical composition comprising (i) a compound of the formula wherein: X is a hydrocarbyl ring having at least 4 atoms in the ring; K is a hydrocarbyl group; Rs is a sulphamate group; (ii) optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant, wherein the compound is present in an amount to provide a dosage of no greater than 200 ?g/day.Type: GrantFiled: April 10, 2002Date of Patent: February 26, 2008Assignees: Sterix Limited, Schering AktiengesellschaftInventors: Barry Victor Lloyd Potter, Michael John Reed, Walter Elger, Gudrun Roddersen, Heinrich-Thomas Proske
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Publication number: 20080026014Abstract: A stick for the topical or transmucosal application of a skin care or active agent onto and via the nasal mucosa, respectively, is provided, wherein the stick material contains a composition of at least one carrier substance and at least one skin care or active agent, which is capable of acting on the nasal mucosa and/or being resorbed by it or which contains at least one volatile substance that acts on the deeper respiratory tract and/or is being resorbed by the deeper respiratory tract. Furthermore, the use of a medical skin care or cosmetical stick or of a stick material or of a refill cartridge containing said material for the topical or transmucosal application is described.Type: ApplicationFiled: October 31, 2003Publication date: January 31, 2008Inventor: Olaf Michel
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Patent number: 7192941Abstract: Methods are provided for the treatment of pulmonary hypertension and other conditions associated therewith. In particular, the methods include treatment of pulmonary hypertension with estradiol metabolite or estradiol metabolite associated with biodegradable microparticles or nanoparticles alone or in combination with another therapeutic agent. Preferred estradiol metabolites include 2-methoxyestradiol, 4-methoxyestradiol, 2-hydroxyestradiol, and 4-hydroxyestradiol, and/or to synthetic derivatives and analogues thereof or prodrugs thereof. The compositions may also be in the form of a controlled release formulation.Type: GrantFiled: February 20, 2004Date of Patent: March 20, 2007Assignee: University of PittsburghInventors: Stevan P. Tofovic, Edwin K. Jackson
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Patent number: 7163934Abstract: This invention generally pertains to the field of psychiatry. In particular, this invention pertains to the discovery that agents which inhibit the binding of cortisol to its receptors can be used in methods for treating delirium. Mifepristone, a potent specific glucocorticoid receptor antagonist, can be used in these methods. The invention also provides a kit for treating delirium in a human including a glucocorticoid receptor antagonist and instructional material teaching the indications, dosage and schedule of administration of the glucocorticoid receptor antagonist.Type: GrantFiled: May 6, 2002Date of Patent: January 16, 2007Assignee: Corcept Therapeutics, Inc.Inventor: Joseph K. Belanoff
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Patent number: 7148213Abstract: This invention describes the new 17?-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.Type: GrantFiled: September 24, 2004Date of Patent: December 12, 2006Assignee: Schering AGInventors: Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp
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Patent number: 7071328Abstract: The present invention relates to a novel method for preparing 21-hydroxy-6,19-oxidopro-gesterone (21OH-6OP) and/or its 21-acetate, 21-propionate, 21-hemisuccinate, 21-phosphate, 21-oleate derivatives. 21OH-6OP and its ester derivatives are antiglucocorticoids for the treatment or prophyl axis of diseases associated to an excess of glucocorticoids, in particular for treating Cushing's syndrome, iatrogenic hypercortisolism or depression.Type: GrantFiled: September 17, 2001Date of Patent: July 4, 2006Assignee: Applied Research System ARS Holding N.V.Inventors: Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
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Patent number: 7067502Abstract: A medicament containing, separately or together, (A) formoterol or a pharmaceutically acceptable salt thereof or a solvate of formoterol or a solvate of the salt and (B) mometasone furoate, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.Type: GrantFiled: November 20, 2003Date of Patent: June 27, 2006Assignee: Novartis AGInventors: Ian Francis Hassan, Jeremy Guy Clarke, Henry Luke Danahay
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Patent number: 7053074Abstract: The present invention relates to methods for preventing the development of epithelial ovarian cancer by administering a Vitamin D compound in an amount capable of increasing apoptosis in non-neoplastic ovarian epithelial cells of the female subject.Type: GrantFiled: January 18, 2002Date of Patent: May 30, 2006Assignee: New Life Pharmaceuticals, Inc.Inventors: Gustavo C. Rodriguez, Regina Salas Whitaker
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Contraceptive process and kit for female mammals, comprising a combination of gestagen and oestrogen
Patent number: 6995149Abstract: The present invention relates to a female mammal contraceptive process consisting of the sequential administration for at least 28 days of (a) a gestagen in an ovulation-preventing dose for at least 28 days in combination with (b) a natural oestrogen for 5 to 10 days at the end of the sequential dosage of at least 28 days, and a contraception kit.Type: GrantFiled: December 20, 1996Date of Patent: February 7, 2006Assignee: Schering AGInventors: Jan Endrikat, Bernd Düsterberg, Pia Reilhac -
Patent number: 6844320Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI2-mimetic, a thromboxane (TXA2) inhibitor, a compound possessing TXA2-agonistic and TXA2-inhibiting properties, a compound possessing TXA2-antagonistic and PGI2-memetic activities, and a TXA2 antagonist.Type: GrantFiled: July 24, 1998Date of Patent: January 18, 2005Assignees: Board of Regents, The University of Texas System, Schering AktiengesellschaftInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 6835724Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I: are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II: in which R(5) is OH, with an activated carboxylic acid of the formula III: R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1) III. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.Type: GrantFiled: July 22, 1997Date of Patent: December 28, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Ulrich Stache, Hans-Georg Alpermann, Walter Dürckheimer, Manfred Bohn
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Patent number: 6806263Abstract: 17&agr;-fluoroalkyl steroids of formula I as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well their physiologically compatible salts with bases, have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.Type: GrantFiled: November 27, 2002Date of Patent: October 19, 2004Assignee: Schering AGInventors: Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp
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Patent number: 6803060Abstract: There is provided a natural composition for boosting the libido of an individual, the composition including an effective amount of an aphrodisiac and a compound to increase blood flow to the pelvic area in a pharmaceutically acceptable carrier. A natural composition for boosting the libido of an individual, including an effective amount of a compound for driving blood flow to the penis and an aphrodisiac in a pharmaceutically acceptable carrier is also provided. Also provided is a method of increasing the libido by administering an effective amount of composition including an aphrodisiac and a compound to increase blood flow to the pelvic area in a pharmaceutically acceptable carrier.Type: GrantFiled: August 10, 2001Date of Patent: October 12, 2004Inventor: Joe Reyes
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Patent number: 6762175Abstract: The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.Type: GrantFiled: April 5, 2002Date of Patent: July 13, 2004Assignee: Norsk Hydro ASAInventors: Finn Myhren, Bernt Børretzen, Are Dalen, Marit Liland Sandvold
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Patent number: 6656970Abstract: 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: GrantFiled: March 8, 2001Date of Patent: December 2, 2003Assignee: Dabur Research FoundationInventors: Anand C. Burman, Rama Mukherjee, Honey Bala, Dhiraj Khattar
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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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Patent number: 6610674Abstract: 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: GrantFiled: September 8, 2000Date of Patent: August 26, 2003Assignee: University of PennsylvaniaInventor: Alan D. Schreiber
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Patent number: 6579862Abstract: The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I): containing at least one olefinic bond in or on their D-ring for the treatment of hyperlipidemic and hyperglycemic conditions in mammals wherein X═OH or O and the olefinic bonds are at 4(5); 5(6); 16(17); or 17(20) or various combinations, and wherein the compounds contain at lest one olefinic bond in or on their D-ring. The method comprises administering an effective amount of said compounds to recipient mammals.Type: GrantFiled: March 30, 1999Date of Patent: June 17, 2003Assignee: Council of Scientific & Industrial ResearchInventors: Ram Pratap, Ram Chandra Gupta, Ramesh Chander, Ashok Kumar Khanna, Arvind Kumar Srivastava, Deepak Raina, Satyavan Singh, Savita Srivastava, Anil Kumar Rastogi, Omkar Prasad Asthana, Swarn Nityanand, Nitya Anand, Ashim Ghatak, Narinder Kumar Kapoor, Sukh Dev
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Patent number: 6514516Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.Type: GrantFiled: June 29, 1999Date of Patent: February 4, 2003Assignee: Euro-Celtique, S.A.Inventors: Mark Chasin, Richard Sackler, Ronald M. Burch, Paul Goldenheim, Joseph Tigner
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Patent number: 6511970Abstract: The present invention relates to compositions and methods for preventing the development of epithelial ovarian cancer by administering compounds in an amount capable of increasing TGF-&bgr; expression in the ovarian epithelium. HRT and OCP regimens comprising such compositions and methods are disclosed.Type: GrantFiled: September 28, 2000Date of Patent: January 28, 2003Assignee: New Life Pharmaceuticals Inc.Inventor: Gustavo C. Rodriguez
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Patent number: 6479475Abstract: This invention provides a method of contraception which comprises administering to a female of child bearing age for 23-25 consecutive days, a first phase combination of a progestin at a daily dosage of 40-500 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol for 3-8 days beginning on day 1 of the menstrual cycle, wherein the same dosage of the progestin and estrogen combination is administered in each of the 3-8 days, a second phase combination of a progeslin at a daily dosage of 40-500 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol, for 4-15 days beginning on the day immediately following the last day of administration of the first phase combination, wherein the same dosage of the progestin and estrogen combination is administered in each ofType: GrantFiled: July 2, 1997Date of Patent: November 12, 2002Assignee: WyethInventor: Michael J. Gast
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Patent number: 6468994Abstract: The invention provides finely divided, substantially crystalline particles of budesonide characterized in that they are substantially smooth and having a BET value of from 1 to 4.5 m2/g, a process for their preparation, a pharmaceutical composition comprising said particles, the use of said particles in the treatment of and in the manufacture of a medicament for use in the treatment of respiratory disorder, and a method of treatment of respiratory disorders by administration of said particles to a host in need of such treatment.Type: GrantFiled: November 6, 2001Date of Patent: October 22, 2002Assignee: AstraZeneca ABInventors: Mikael Bisrat, Saeed Moshashaee
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Patent number: 6395746Abstract: Methods of treating or preventing ophthalmic, otic, and nasal infections and attendant inflammation are described. The methods utilize ophthalmic, otic, and nasal compositions containing a new class of antibiotics (e.g. trovafloxacin). The compositions also contain one or more anti-inflammatory agents (e.g. dexamethasone). The compositions are utilized to treat ophthalmic, otic, and nasal conditions by topically applying the compositions to the affected tissues.Type: GrantFiled: September 22, 2000Date of Patent: May 28, 2002Assignee: Alcon Manufacturing, Ltd.Inventors: Gerald Cagle, Robert L. Abshire, David W. Stroman, John M. Yanni
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Patent number: 6369115Abstract: A dry powder formulation for treatment of pulmonary conditions, via inhalation, includes an effective amount of formoterol or a salt or solvate thereof, in a dry powder form, an effective amount of fluticasone, in a dry powder form, and an excipient. A method for preparing a physically stable dry powder formulation for inhalation includes the steps of micronizing a first active polar drug, a second active non-polar drug, and a polar excipient. The second non-polar active drug is first blended with the excipient to form an intermediate mixture. The intermediate mixture is then blended with the first active polar drug. The increased separation of the polar drug and polar excipient stabilizes the formulation.Type: GrantFiled: March 20, 2000Date of Patent: April 9, 2002Assignee: Dura Pharmaceuticals, Inc.Inventor: Gary Ward
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Patent number: 6350739Abstract: The present invention in various embodiments provides methods of treating stroke and conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the delivery of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing hormones that are non-sex hormones is also provided. A method of treating stroke with ent-17&bgr;-estradiol, and a method of synthesis, and compounds produced from the synthesis are provided.Type: GrantFiled: August 11, 1999Date of Patent: February 26, 2002Assignees: University of Florida Resarch Foundation, Inc., Washington UniversityInventors: James W. Simpkins, Douglas F. Covey
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Patent number: 6346523Abstract: The invention provides finely divided, substantially crystalline particles of budesonide characterized in that they are substantially smooth and having a BET value from 1 to 4.5 m2/g, process for their preparation, a pharmaceutical composition comprising said particles, the use of said particles in the treatment of and in the manufacture of a medicament for use in the treatment of a respiratory disorder, and a method of treatment of respiratory disorders by administration of said particles to a host in need of such treatment.Type: GrantFiled: June 18, 1998Date of Patent: February 12, 2002Assignee: AstraZeneca ABInventors: Mikael Bisrat, Saeed Moshashaee
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Patent number: 6339078Abstract: The present invention provides methods of conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the delivery of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing non-sex hormones is also provided.Type: GrantFiled: July 20, 1999Date of Patent: January 15, 2002Assignee: University of Florida Research Foundation, Inc.Inventors: James W. Simpkins, Katherine D. Gordon, Robert J. Leonard
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Patent number: 6326365Abstract: The present invention provides methods of conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the intravenous administration of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing non-sex hormones is also provided.Type: GrantFiled: July 20, 1999Date of Patent: December 4, 2001Assignees: Apollo BioPharmaceutics, Inc., University of Florida Research Foundation, Inc.Inventors: James W. Simpkins, Katherine D. Gordon, Robert J. Leonard
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Patent number: 6319914Abstract: The invention comprises methods for conferring a cytoprotective effect on a population of cells, such as providing a polycyclic phenolic compound in a physiologically acceptable formulation, and administering the formulation in an effective dose to the population of cells.Type: GrantFiled: July 12, 1999Date of Patent: November 20, 2001Assignees: Apollo BioPharmaceuticals, Inc., University of Florida Research Foundation, Inc.Inventors: James W. Simpkins, Katherine D. Gordon, Pattie S. Green
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Patent number: 6316432Abstract: This invention describes the new 17&agr;-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with acids, and for —CO2R9 radicals with R9 meaning hydrogen as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.Type: GrantFiled: March 1, 2000Date of Patent: November 13, 2001Assignee: Schering AktiengesellschaftInventors: Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp