Abstract: The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, &agr;-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.
Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
Type:
Application
Filed:
July 8, 2002
Publication date:
December 9, 2004
Applicant:
Pharmacia Corporation
Inventors:
John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers charcterized by over-activity or inappropriate activity HER2 or EGFR.
Type:
Application
Filed:
June 25, 2003
Publication date:
December 2, 2004
Applicants:
Yissum Research Development Company of the Hebrew University of Jerusalem, SUGEN, Inc.
Inventors:
Hui Chen, Aviv Gazit, Alexander Levitzki, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
March 30, 2004
Publication date:
November 18, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops.
A carbamate derivative represented by the general formula [I]
{wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.
Type:
Grant
Filed:
February 5, 2002
Date of Patent:
November 2, 2004
Assignees:
Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
Abstract: This invention relates to treating pulmonary diseases such as chronic obstructive pulmonary disease or asthma by administering a phosphodiesterase 4 inhibitor in combination with anti-inflammatory corticosteriod.
Type:
Application
Filed:
May 17, 2004
Publication date:
October 28, 2004
Applicant:
SmithKline Beecham Corporation
Inventors:
Peter N. Goodfellow, Richard Nieman, Theodore J. Torphy
Abstract: The invention compounds and methods for the treatment of motor disorders. In particular, the invention provides eicosanoid analogs which are effective in ameliorating motor disorders such as spasticity caused by multiple sclerosis (MS).
Type:
Grant
Filed:
January 17, 2003
Date of Patent:
October 5, 2004
Assignee:
Virginia Commonwealth University
Inventors:
Billy Martin, Raj K. Razdan, Anu Mahadevan, David Baker
Abstract: A method of inducing the viral resistance of plants comprises treating the plants, the soil or seeds with an effective amount of the compound of the formula I 1
Abstract: A process is described for producing 2-cyano-3-hydroxy-N-(phenyl)but-2-enamide, in which a phenyl-substituted 2-cyano-N-(phenyl)acetamide is reacted in the presence of a base, acetic anhydride and at least one solvent, and the resultant 2-cyano-3-hydroxy-N-(phenyl-derivative)but-2-enamide is crystallized by acidification.
Type:
Application
Filed:
March 17, 2004
Publication date:
September 23, 2004
Applicant:
Aventis Pharma Deutschland GmbH
Inventors:
Jochen Hachtel, Bernd Neises, Wilfried Schwab, Roland Utz, Martin Zahn
Abstract: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.
Type:
Application
Filed:
March 23, 2004
Publication date:
September 16, 2004
Applicant:
Sepracor Inc.
Inventors:
Thomas P. Jerussi, Chrisantha H. Senanayake, Nandkumar N. Bhongle
Abstract: This invention relates to treating pulmonary diseases such as chronic obstructive pulmonary disease or asthma by administering a phosphodiesterase 4 inhibitor in combination with an H1-receptor antagonist.
Type:
Application
Filed:
December 8, 2003
Publication date:
September 9, 2004
Inventors:
Richard Graham Knowles, Peter Ward, Anthony Terence Nials
Abstract: The invention relates to a method for controlling the application of an insecticide on a surface, which comprises the use of an insecticide composition including a pH indicator colorant in an aqueous medium changing the colourless after drying in the air on said surface, and the recoloration of the insecticide composition by remoistering selected areas of the surface to be checked.
Type:
Application
Filed:
December 19, 2003
Publication date:
September 9, 2004
Inventors:
Hisham Mohamed Mahgoub, Amina Ahmed Mahmoud Fahmy
Abstract: In one aspect, the present invention provides a method of inhibiting an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with an amount of an Edg-3 receptor inhibitor sufficient to inhibit the Edg-3 receptor mediated biological activity. Preferably, the inhibitor is not a phospholipid.
Type:
Application
Filed:
January 16, 2004
Publication date:
August 26, 2004
Inventors:
David Solow-Cordero, Geetha Shankar, Juliet V. Spencer, Charles Gluchowski
Abstract: Provided is a group of active substances capable of inhibiting the proliferation of cancer cells and inhibiting inflammation, as well as suppressing bodily defense reactions to control autoimmune diseases, transplant rejections, and acute and chronic inflammatory reactions.
Type:
Application
Filed:
March 15, 2004
Publication date:
August 5, 2004
Inventors:
Erich Eigenbrodt, Stefan Muellner, Sybille Mazurek, Hugo Fasold
Abstract: The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.
Type:
Application
Filed:
October 14, 2003
Publication date:
July 22, 2004
Inventors:
Darlene Coleman Deecher, Istvan Jozsef Merchenthaler, Liza Leventhal, Kimberly Jean Sipe, Lawrence Thomas O'Connor
Abstract: The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (−)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient.
Type:
Application
Filed:
October 22, 2003
Publication date:
July 22, 2004
Inventors:
Roman V. Rariy, Michael Heffernan, Stephen L. Buchwald, Timothy M. Swager
Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4′-cyano-&agr;′,&agr;′,&agr;′-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide in a solid dispersion with PVP. In one embodiment, >50% of the drug is provided in the form of the R-enantiomer. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of PVP in solid dispersion with the drug (in one embodiment wherein >50% of the 4′-cyano-&agr;′,&agr;′,&agr;′-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide is provided in the form of the R-enantiomer) for increasing the bioavailability of the drug; for reducing inter-patient variability in plasma concentrations of the drug; for enhancing the storage stability of the drug; or for treating and/or reducing the risk of prostate cancer in a patient.
Abstract: This invention relates to N-acylamino aryl derivatives of the formula
where
R1, R21, R22, R23, R24, R3, R4, R5 R6, R7, R8, R, and
n are as defined herein and where
X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—.
The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.
Type:
Grant
Filed:
May 27, 2003
Date of Patent:
July 13, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
Abstract: Methods and products for inhibiting growth of fungus and fungal disease on a plant. Methods comprise contacting at least a portion of a plant or plant seed together with a fungicidal composition comprising a fungicidal carboxamide. Products comprise any of leaves, crowns, roots, stolons, seed, seedlings, sod, and any combination thereof, treated with a fungicidal carboxamide. Preferred pathogens are of the genus Colletotrichum, preferred disease is anthracnose, preferred fungicides are carboxamides, and preferred plants are turfgrass.
Abstract: Analogs of andandamide and arvanil have been found to act preferential at CB1 and AR1 receptors, and at receptors other than CB1 and AR1. The analogs provide analgesic effects in vivo, and are useful in pain management. In addition, the analogs may be used as anti-proliferative/anti-tumor agents, vasodilators, and in other applications. Several of the anandamide and arvanil analogs are more potent than anandamide and arvanil.
Type:
Application
Filed:
February 13, 2003
Publication date:
June 24, 2004
Inventors:
Billy R. Martin, Raj K. Razdan, Vincenzo Di Marzo
Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors, including allergy treatments.
Abstract: N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization).
Type:
Application
Filed:
October 28, 2003
Publication date:
June 10, 2004
Inventors:
Eva Altmann, Claudia Betschart, Keigo Gohda, Miyuki Horiuchi, Rene Lattmann, Martin Missbach, Junichi Sakaki, Michihiro Takai, Naoki Teno, Scott Douglas Cowen, Paul David Greenspan, Lesile Wighton McQuire, Ruben Alberto Tommasi, John Henry van Duzer
Abstract: Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.
Type:
Application
Filed:
November 25, 2003
Publication date:
June 3, 2004
Applicant:
Sepracor Inc.
Inventors:
Thomas P. Jerussi, Chrisantha H. Senanayake, Nandkumar N. Bhongle
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 6, 2000
Date of Patent:
June 1, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: Material of electronics component and electronics components using the same material are provided. The material includes repellent that can withstand severe solder-mounting conditions, and the electronics components such as printed wiring boards can lasts repelling effect for a long period. The material is used in electronics components requiring a soldering process, and includes at least curable resin, filler and the repellent. The repellent has vapor pressure of less than 10,000 nPa at room temperature. Film is formed using the material at a given place of an electronics component such as a printed wiring board.
Abstract: The invention relates to the use of aminoacetonitrile compounds of formula (I), wherein R1, R2, R3, R4, R8, R9, A, m and n have the significances given in claim 1, in the control of endoparasites, especially helminths, in warm-blooded productie livestock and domestic animals.
Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient. In the formula, A, B and C independently represents a hydrogen atom or a monovalent substituent; and X and X′ independently represents a hydrogen atom or a monovalent substituent.
Inventors:
Karl Eicken, Ingo Rose, Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Maria Scherer, Klaus Schelberger, Egon Haden
Abstract: A method of preventing damage to the shoots and foliage of a plant by a pest includes treating the seed from which the plant grows with a composition that includes at one pyrethrin or synthetic pyrethroid. In another embodiment, the seed is a transgenic seed having at least one heterologous gene encoding for the expression of a protein having pesticidal activity against a first pest and the pyrethrin or synthetic pyrethroid has activity against at least one second pest. Treated seeds are also provided.
Abstract: The present invention is directed to compounds that are analogues of lipid mediators derived from a fish oil-derived fatty acid, eicosapentaenoic acid [C20:5 &ohgr;-3; EPA], but with a longer tissue half-life and enhanced bioactivity. These analogues may be used to treat inflammatory, angioproliferative, cardiovascular, thrombophlebotic, vascular, ocular, dermatologic, neurodegenerative, pulmonary, endocrine, reproductive, rheumatologic and gastrointestinal diseases.
Type:
Application
Filed:
June 13, 2003
Publication date:
March 4, 2004
Inventors:
Daniel W. Goodman, Michael R. Hanley, Stuart L. Bursten
Abstract: The invention relates to the use of aminoacetonitrile compounds of formula wherein Ar1, Ar2, R3, R4, R5, R6, R7, R8, Q, W, a, b and d have the significances given in claim 1, in the control of endoparasites, especially helminths, in warm-blooded productive livestock and domestic animals.
Abstract: This invention provides a means for preparing a monohydrate of the lithium salt of cis 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylate which is a novel composition of matter.
Abstract: The invention relates to 3-phenyl-propionamido, 3-phenyl-acrylamido and 3-phenyl-propynamido derivatives, for example, deriviatives of the formula 1
Type:
Application
Filed:
July 3, 2003
Publication date:
February 19, 2004
Inventors:
Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
Abstract: The invention relates to the formulation of deltamethrin as water-dispersible granules which comprise wetting agents, dispersants, solid inert substances and one or more acids in an amount sufficient to adjust the pH of the mixture to a value in the range from 1 to 7. The granules are particularly useful for controlling animal pests.
Type:
Grant
Filed:
September 24, 2001
Date of Patent:
February 17, 2004
Assignee:
Aventis CropScience GmbH
Inventors:
Gunnar Noeding, Agnes Nied, Andrew Adams, Heiko Diehlmann, Manfred Wagenbach
Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
Type:
Application
Filed:
September 27, 2002
Publication date:
January 22, 2004
Applicant:
AXYS PHARMACEUTICALS, INC.
Inventors:
Michael Graupe, John O. Link, John W. Patterson, Sheila Zipfel
Abstract: The invention compounds and methods for the treatment of motor disorders. In particular, the invention provides eicosanoid analogs which are effective in ameliorating motor disorders such as spasticity caused by multiple sclerosis (MS).
Type:
Application
Filed:
January 17, 2003
Publication date:
January 1, 2004
Inventors:
Billy Martin, Raj K. Razdan, Anu Mahadevan, David Baker
Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
December 10, 2002
Publication date:
January 1, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: This invention relates to a method for the prophylaxis of or for treating COPD by administering a PDE4 inhibitor which has a defined therapeutic ratio.
Type:
Grant
Filed:
August 31, 2001
Date of Patent:
December 30, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Mary S. Barnette, Theodore J. Torphy