Abstract: A pharmaceutical solution is capable of being ejected from a thermal fluid ejection device onto a substrate. The solution includes a vehicle with predetermined properties, and an active pharmaceutical ingredient with a solubility of at least about 30 mg/ml in the vehicle. The vehicle substantially evaporates from the substrate.
Abstract: The present invention provides a method for preparing a sterile suspension of a glucocorticosteroid. The glucocorticosteroids used in the invention are preferably antiinflammatory glucocorticosteroids. By making the last stage of product preparation be the sterilization process, the potential for contamination during manufacture and heat degradation of products is greatly reduced.
Type:
Application
Filed:
November 16, 2005
Publication date:
October 30, 2008
Inventors:
John Miller, Paul Ronald, Adrian Ashley, Paul Lamb, Donald MacDonald, Martin Oliver, Matthew Pollard
Abstract: The transdermal delivery system for treating infertility in a patient comprises an apparatus (10) for facilitating transdermal delivery of a drug (5a) through an area of the apparatus (10) comprises an ablator that is configured to generate a microporation in the area of the skin of the patient, and comprises a drug (5a), wherein the drug effects at least one of the biological regulation of at least one oocyte containing follicle, stimulation of follicle growth, induction of ovulation, promotion of gestational status, maintenance of conceptus, maintenance of pregnancy.
Type:
Application
Filed:
October 6, 2006
Publication date:
October 16, 2008
Applicant:
PANTEC BIOSOLUTIONS AG
Inventors:
Christof Bohler, Thomas Bragagna, Reinhard Braun, Werner Braun, Herbert Zech
Abstract: The present invention relates to the use of specific steroid derivatives in the preparation of medicaments for the treatment or prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.
Type:
Application
Filed:
June 29, 2005
Publication date:
October 16, 2008
Applicants:
JadoLabs GmbH, Max-Planck-Gesellschaft zur Forderung der Wissenschaftenhaften e.V., Technische Universitat Dresden
Inventors:
Tobias Braxmeier, Kai Simons, Marino Zerial, Teymuras Kurzchalia, Tim Friedrichson, Wolfgang Frohner, Gary Jennings, Georg Schlechtingen, Cornelia Schroeder, Hans-Joachim Knolker
Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?, 17?-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
Abstract: The compounds of the present invention can be used to inhibit formation of beta-amyloid protein. The present invention provides methods of preventing, delaying onset of, or treating diseases or conditions characterized or mediated by amyloidosis. In particular, the present invention is useful for preventing, delaying onset of, and treating Alzheimer's disease and related diseases causing dementia.
Type:
Application
Filed:
January 31, 2008
Publication date:
September 25, 2008
Inventors:
Theresa M. LaVallee, Anthony M. Treston, Todd A. Hembrough
Abstract: The present invention relates to the area of chemotherapy and more especially to the development of new galenic forms for application to the skin. It relates more particularly to a topical hormonal composition with systemic action for the correction of progesterone deficiency in premenopausal women and for hormone replacement in menopausal women, characterized in that it contains, as the active principle, a progestogen derived from 19-nor progesterone, a vehicle permitting systemic passage of the said active principle chosen from the group comprising a solubilizing agent, an absorption promoter, a film-forming agent, a gelling agent or their mixtures, combined with or mixed with suitable excipients for production of a pharmaceutical form as a gel and/or a film.
Type:
Application
Filed:
March 20, 2008
Publication date:
September 18, 2008
Inventors:
Michel Lanquetin, Jacques Paris, Jean-Louis Thomas
Abstract: Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
Abstract: The present invention relates to soft gelatin capsules characterized in that the shell includes a cyclodextrin and in that the filling material contains a liposoluble drug capable of forming a complex with said cyclodextrin for improving the solubility of the active ingredient upon disintegration of the soft gelatin capsule.
Abstract: Disclosed are sustained release compositions for vaginal or transdermal administration that contain a progesterone receptor modulator such as CDB-2914 (also referred to as VA-2914), and methods of using them for long term contraception or therapeutic purposes. Also disclosed are methods for making the compositions.
Abstract: Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17?-alkoxycarbonyloxy-11?-hydroxyandrost-4-cn-3-one-17?-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: wherein Z1 is carbonyl, ?-hydroxymethylene or methylene; R2 is H, —OH or —OCOR3 wherein R3 is C1-5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Ophthalmic administration in the treatment of dry eye is specifically targeted.
Abstract: A dosage form is disclosed comprising a semipermeable walled container that houses a capsule, which capsule comprises a drug formulation, a piston, and an osmotic composition. The dosage form delivers the drug formulation through a passageway at a controlled rate over a sustained-release period of time up to 24 hours.
Type:
Application
Filed:
April 2, 2008
Publication date:
July 31, 2008
Applicant:
ALZA CORPORATION
Inventors:
Liang-Chang Dong, Patrick S.L. Wong, Vincent Joseph Ferrari, Steven Espinal
Abstract: The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched alkyl group, a bicycloalkyl group, or a C5-C6 cycloalkyl which optionally may be substituted with a C1-C4 alkyl group; R2 represents hydrogen, a methyl group, which may be in either the ? or ? configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; represents a single or a double bond; and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.
Abstract: The present invention is directed to bi-layer tablets comprising at least one estrogen in a first layer and a therapeutic agent in a second layer, and processes for their preparation.
Type:
Application
Filed:
November 28, 2007
Publication date:
July 24, 2008
Applicant:
Wyeth
Inventors:
Xiuying Liu, John Kresevic, Nizamuddin Baksh, Robin Enever
Abstract: Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue.
Type:
Grant
Filed:
September 27, 2002
Date of Patent:
July 22, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Jiabing Wang, Mark E. Duggan, David B. Whitman
Abstract: Pharmaceutical preparations for topical or local administration of drugs directly to the skin for treatment of disorders of the subcutaneous fatty tissue, in particular in cases of cellulite, are disclosed herein. In a preferred embodiment, the drug is danazol or gastrinone. In another embodiment, the drug is danazol in combination with an aromatase inhibitor or an estrogen compound. The preferred formulations contain drugs in the form of micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or carrier. The excipient or carrier may modify the release rates or enhance absorption into the affected area. The drug formulation may be in the form of a cream, lotion, ointment, gel or emulsion, solution or foam.
Abstract: The present invention relates to the regional delivery of therapeutic agents for the treatment of vascular diseases wherein regional delivery refers to delivery of a therapeutically effective amount of the therapeutic agent to an area of the vessel that includes not only afflicted tissue but non-afflicted tissue at the periphery of the afflicted tissue as well.
Type:
Application
Filed:
December 15, 2006
Publication date:
June 19, 2008
Inventors:
Stephen D. Pacetti, Paul M. Consigny, Ronald W. Heil, Florian Niklas Ludwig, Dariush Davalian, Li Zhao, Irina Astafieva, Jinping Wan, Fozan El-Nounou, Katsuyuki Murase, Syed F.A. Hossainy, Rachel Bright, Jeffrey Ellis
Abstract: Disclosed herein are methods for regulation of fat and/or cholesterol uptake from the gastrointestinal tract and/or regulation of plasma fat and/or cholesterol levels comprising administering to a mammal in need thereof an effective amount of a regulator of pancreatic IB PLA2 functionality. Also disclosed herein are methods of regulating the function of a polypeptide of interest comprising inserting of the 62-66 loop region of a pancreatic IB PLA2 amino acid sequence into the polypeptide of interest; and administering an effective amount of a regulatory molecule that effects its regulation through said amino acid sequence. Further disclosed are novel bile salt compounds that regulate pancreatic IB PLA2. Methods for detecting altered pancreatic IB PLA2 function and methods for identifying an agent suitable for regulating pancreatic IB PLA2 enzyme functionality are also disclosed.
Type:
Application
Filed:
August 21, 2007
Publication date:
June 12, 2008
Inventors:
Mahendra K. Jain, Rafael J. Apitz-Castro, Otto G. Berg
Abstract: The present invention comprises a composition and method treating eye diseases using a composition having a therapeutically effective amount of a progestagen and a pharmaceutically acceptable carrier, wherein the composition is applied to the palpebral part of the eye and/or ocular surface.
Type:
Application
Filed:
December 5, 2006
Publication date:
June 5, 2008
Inventors:
Charles Gerald Connor, Charles L. Haine
Abstract: Certain chemical entities chosen from compounds of Formula I: and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof are described. Pharmaceutical compositions comprising at least one chemical entity chosen from compounds of Formula I and a pharmaceutically acceptable vehicle are described. Also described are methods for inhibiting ?-2,3-sialyltransferase activity in cells, and methods for treating a patient having a disease responsive to inhibition of ?-2,3-sialyltransferase activity.
Type:
Application
Filed:
July 3, 2006
Publication date:
May 22, 2008
Inventors:
Wen-Shan Li, Yi-Ching Wang, Hsueh-Fen Juan
Abstract: A method of sexual enhancement in women includes the steps of identifying a woman requesting sexual enhancement, assuring that the woman's blood includes estradiol within a first predetermined range and testosterone within a second predetermined range, and thereafter administrating a drug selected from the group consisting of vardenafil hydrochloride and tadalafil prior to sexual activity. The selected drug may be loaded into a starch strip which is then applied to the woman's tongue. Sexual enhancement in women can also be achieved by transdermal or subcutaneous application of the hormone DHEA.
Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.
Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.
Type:
Grant
Filed:
May 28, 2004
Date of Patent:
May 13, 2008
Assignee:
EntreMed, Inc.
Inventors:
Gregory E. Agoston, Theresa M. LaVallee, Victor S. Pribluda, Jamshed H. Shah, Anthony M. Treston
Abstract: Compositions containing ?2 adrenergic agonists in combination with carbonates and carbamates of the formula and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.
Type:
Application
Filed:
July 13, 2007
Publication date:
May 1, 2008
Applicant:
SEPRACOR INC.
Inventors:
Mark G. Currie, Steve Jones, Paul Grover, Chris H. Senanayake, Q. Kevin Fang
Abstract: Methods of using compounds having certain inhibitory effect to treat cancer are disclosed. More specifically, methods of using myosin light chain kinase inhibitor (MLCK) to treat cancer are disclosed. MLCK inhibitors may cause reduction in MLC-P and induce apoptosis in neoplastic cells and prevent and or inhibit the tumor growth.
Type:
Application
Filed:
March 30, 2007
Publication date:
April 3, 2008
Applicant:
The Board of Trustees of the University of Illinois
Abstract: The use of DHEA or at least one of its biological precursors or of its metabolic derivatives in or for the manufacture of a composition for topical application to the skin, as a pigmentation regulator for the skin or its superficial growths, especially as a depigmenting and/or bleaching agent for the skin, in particular in the treatment of pigmentation marks, and as a pro-pigmenting agent for superficial body growths.
Type:
Grant
Filed:
October 12, 2000
Date of Patent:
April 1, 2008
Assignee:
L'Oreal
Inventors:
Olivier De Lacharriere, Stephanie Nouveau
Abstract: The present invention generally relates to methods of suppressing estrus in breeding or competitive animals comprising parenterally administering to breeding animals an estrus suppressing amount of 17-?-Allyl-17-?-hydroxyoestra-4,9,11-trien-3-one. According to the method of the present invention, estrus can be suppressed for any of a variety of periods including 30 days or more. Furthermore, the method of the present invention includes repeated sustained release doses for an indefinite period.
Abstract: The present invention provides improving health in a woman or man comprising non-orally administering a testosterone-containing moiety to said woman or man by topically applying a liquid composition including said testosterone-containing moiety to the eye of said woman or man in an amount sufficient to provide a therapeutic effect.
Type:
Application
Filed:
August 17, 2006
Publication date:
February 21, 2008
Inventors:
Diane D.S. Tang-Liu, Zhiling Yu, Ronald Bradford
Abstract: Use of a composition comprising at least one prodrug of a steroid, preferably of a corticosteroid, for the preparation of an ophthalmic composition intended for the treatment of an ocular condition or disease of a human being or an animal.
Type:
Application
Filed:
June 1, 2007
Publication date:
December 6, 2007
Applicant:
NOVAGALI PHARMA SA
Inventors:
Laura Rabinovich-Guilatt, Gregory Lambert
Abstract: A fluticasone lotion having improved vasoconstrictor and anti-inflammatory activity and higher than expected potency. The fluticasone lotion contains 0.05 weight percent fluticasone propionate and an oil-in-water vehicle that includes excipients. The fluticasone lotion is unexpectedly efficacious while exhibiting an improved safety profile.
Type:
Grant
Filed:
March 15, 2004
Date of Patent:
November 27, 2007
Assignee:
Altana Inc.
Inventors:
Gordon J. Dow, Keith Arthur Johnson, Frances Furr Kelly, Robert William Lathrop, Rukmini Rajagopalan
Abstract: The invention features a method for treating a patient having an immunoinflammatory disorder, by administering to the patient (i) a tetra-substituted pyrimidopyrimidine, and (ii) a corticosteroid simultaneously or within 14 days of each other in amounts sufficient to reduce or inhibit immunoinflammation.
Type:
Grant
Filed:
October 4, 2002
Date of Patent:
August 7, 2007
Assignee:
CombinatoRx, Inc.
Inventors:
Curtis Keith, Alexis Borisy, Grant Zimmerman, Edward Roydon Jost-Price, Palaniyandi Manivasakam, Nicole Hurst, Michael A. Foley
Abstract: A topical composition comprising an antiinflammatory glucocorticoid and a nucleoside analogue antiviral agent in a pharmaceutical carrier characterized in that the carrier comprises about 15 to about 25 weight % propylene glycol and about 10 to about 25 weight percent isopropyl C12–C22 alkanoic ester. The compositions have utility in the treatment or prophylaxis of herpesvirus infections and exhibit superior antiviral and therapeutic efficacy and an improved shelf life.
Abstract: New 17?-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5?-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.
Type:
Grant
Filed:
April 13, 2005
Date of Patent:
April 3, 2007
Assignee:
Schering AG
Inventors:
Ulrich Bothe, Peter Droescher, Walter Elger, Gudrun Reddersen, Bernd Menzenbach, Hans-Udo Schweikert, Alexander Hillisch, Birgitt Schneider
Abstract: Modulating the metabolism of a dieting mammal by administering to the dieting mammal the metabolic modulating agent 7-oxo DHEA or a pro-drug thereof incapable of in vivo conversion to testosterone.
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.
Abstract: A stable composition of a drug comprising a carrier having a phosphatidylcholine component which entraps the drug is applied to the skin for transdermal delivery of the drug.
Abstract: A method of decreasing atherosclerosis and its complications including but not limited to myocardial infarction, stroke and peripheral vascular disease wherein the method involves administering to a human or an animal an amount of an inhibitor of the release of LHRH or GnRH.
Abstract: The present invention relates to novel steroid derivatives that ace on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex as well as methods for making the same and their applications to induce anesthesia, in the treatment of stress, anxiety, PMS, PND, and seizures such as those caused by epilepsy, to ameliorate or prevent the attacks of anxiety, muscle tension, and depression common with patients suffering from central nervous system abnormalities. The present invention comprises a compound represented by Formula (I): wherein, R, R1, R2, R3, R4, R5 are defined in the description of the invention. The present invention also includes formulations which consist of one or more of the compounds of Formula (I).
Type:
Grant
Filed:
December 21, 2001
Date of Patent:
June 20, 2006
Inventors:
Theodora Calogeropoulou, Andrew Tsotinis, Charikleia Souli, Alexandros Makriyannis
Abstract: The present invention is directed to improved formulations for dihydroergotamine in which the drug is present at a concentration of at least 2.9 mM. The invention encompasses methods for using these formulations in treating patients for migraine headaches and the packaging of formulation into prefilled syringes for self-administration by patients.
Abstract: The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.
Type:
Grant
Filed:
May 13, 1999
Date of Patent:
May 30, 2006
Assignee:
Schering AG
Inventors:
Walter Elger, Pekka Lähteenmäki, Matti Lehtinen, Gudrun Reddersen, Holger Zimmermann, Michael Oettel, Sigfrid Schwarz
Abstract: Disclosed are improved pharmaceutical formulations comprising dehydroepiandrosterone (DHEA), enriched in selected polymorphic forms, for therapeutic applications. In one embodiment, the formulation comprises, in solid form, DHEA, at least 85% of which is present as a single polymorph selected from the form I polymorph or the form II polymorph, and at least one pharmaceutical excipient. Methods for making and using such compositions are also disclosed.
Type:
Grant
Filed:
March 16, 2000
Date of Patent:
May 16, 2006
Assignee:
Genelabs Technologies, Inc.
Inventors:
Jagdish Parasrampuria, Maxine B. Yonker, Kenneth E. Schwartz, Marc J. Gurwith
Abstract: Novel methods for the medical treatment and/or inhibition of the development of hypercholesterolemia in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing precursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
Abstract: The present invention relates to methods for preventing the development of epithelial ovarian cancer by administering progestin products, either alone or in combination with other agents such as estrogen products.
Abstract: The invention pertains to a process for the preparation of a high purity composition of (7?, 17?)-17-hydroxy-7-methyl-19-nor-17-pregn-5(10)-en-20-yn-3-one. The process provides for a composition with less than 0.5% of (7?, 17?)-17-hydroxy-7-methyl-19-nor-17-pregn-4-en-20-yn-3-one. This composition can be used as a source for the preparation of stable pharmaceutical dosage units.
Type:
Grant
Filed:
October 11, 1999
Date of Patent:
November 29, 2005
Assignee:
Akzo Nobel N.V.
Inventors:
Peter H. G. M. Kirchholtes, Gerard A. J. M. T. Sas
Abstract: Disclosed are androgenic steroids of the (14?,17?)-17-(hydroxymethyl) type. The invention relates to an improvement thereof, which is based on the presence of a ?-oriented, annellated cyclopropyl group which includes carbon atoms 16 and 17 of the steroid skeleton, i.e. a 16,17?-methylene moiety. These steroids show an unexpectedly high androgenic potency.
Type:
Grant
Filed:
December 5, 2001
Date of Patent:
September 27, 2005
Assignee:
Akzo Nobel N.V.
Inventors:
Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer
Abstract: Lupus erythematosus can be treated by administering therapeutic amounts of ?5-androstene-3?-ol-7,17-dione and metabolizable precursors thereof, such as ?5-androstene-3b-acetoxy-7,17-dione, which are readily metabolized in vivo to ?5-androstene-3?-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.