Abstract: Compositions, methods, combinations, and kits for treating a disorder related to elevated serum cholesterol concentration, for example, atherosclerosis, elevated LDL plasma levels, low HDL plasma levels, hypertriglyceridemia, hyperlipidemia, hypertension, hypercholesterolemia, cholesterol gallstones, lipid storage diseases, obesity, and diabetes. The compositions, methods, combinations, and kits of the present invention are pharmaceutical compositions comprising at least two of an LXR receptor modulator, a therapeutically effective amount of a catechin, and/or a therapeutically effective amount of a lipid regulating agent, such as a HMG-CoA reductase inhibitor, a fibric acid derivative, niacin, a bile-acid sequestrant, an absorption inhibitor, probucol, raloxifene and its derivatives, an azetidinone compound, and an unsaturated omega-3 fatty acid.
Type:
Application
Filed:
June 19, 2002
Publication date:
August 14, 2003
Inventors:
Robert Dudley, Shutsung Liao, Ching Song
Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) 1
Type:
Application
Filed:
February 4, 2002
Publication date:
August 14, 2003
Inventors:
Keith Biggadike, Steven John Coote, Andrew S. Craig, Victor W. Jacewicz, Michael J. Millan, Rosalyn K. Nice, Brian M. Noga, John F. Seager, Andrew L. Theophilus, David M. Crowe
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
Type:
Application
Filed:
December 19, 2002
Publication date:
August 14, 2003
Inventors:
Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Ling Jong
Abstract: 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—, RCH 2 O—, RCH 2 NH—, —COOCH 2 R, —CONHCH 2 R and —SCH 2 R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.
Type:
Application
Filed:
April 5, 2002
Publication date:
August 14, 2003
Inventors:
Finn Myhren, Bernt Borretzen, Are Dalen, Marit Liland Sandvold
Abstract: The present invention provides methods of making 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives according to the following general reaction scheme: 1
Abstract: The invention relates to a method of treating a diabetic condition by administering a therapeutically effective amount of a histamine-3 receptor antagonist, including benzofuran and benzopyran derivatives of formula (I), aminoalkoxybiphenylcarboxamide compounds of formula (III), and aminoetherbiphenyl compounds of formula (IV) as described herein.
Type:
Application
Filed:
December 23, 2002
Publication date:
August 14, 2003
Inventors:
Arthur A. Hancock, Eugene N. Bush, Marlon D. Cowart, Peer B. Jacobson, Terry J. Opgenorth, Youssef Bennani
Abstract: The invention relates to compounds of formula (I) wherein each of X, Y and Z, which may be the same or different, represents hydrogen or an unsubstituted or substituted hydrocarbon radical, typically an alkyl, aryl, including heterocyclic aryl, or non-aromatic heterocyclic radical and Y additionally may represent —COWR wherein W represents O, S or NRiv wherein Riv represents hydrogen or a radical R, and R represents hydrogen or an unsubstituted or substituted hydrocarbon radical for use as protease inhibitors, X, Y and Z being chosen so that they do not react covalently prior to reaction of the &bgr;-lactam ring with the target protease.
Type:
Application
Filed:
January 21, 2003
Publication date:
August 14, 2003
Inventors:
Christopher Joseph Schofield, Rupert Charles Wilmouth
Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Type:
Application
Filed:
October 7, 2002
Publication date:
August 14, 2003
Inventors:
James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
Abstract: The invention provides a method for causing regression of ocular neovascularization in a subject by administering an effective amount of a staurosporine derivative to the subject.
Abstract: The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Abstract: The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Type:
Application
Filed:
November 14, 2002
Publication date:
August 14, 2003
Applicant:
Aventis Pharma Deutschland GmbH and Genentech, Inc.
Inventors:
Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
Abstract: The present invention relates to 4-pyridyl- und 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1 1
Type:
Application
Filed:
November 5, 2002
Publication date:
August 14, 2003
Inventors:
Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
Type:
Application
Filed:
November 20, 2002
Publication date:
August 14, 2003
Inventors:
Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
October 23, 2001
Publication date:
August 14, 2003
Inventors:
Francesco G. Salituro, Guy W. Bemis, Susanne Wilke, Jeremy Green, Jingrong Cao, Huai Gao, Edmund Martin Harrington
Abstract: The present invention provides a compound of formula I 1
Type:
Application
Filed:
November 5, 2002
Publication date:
August 14, 2003
Inventors:
Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach
Abstract: A class of substituted imadazolo[2,1-a]phthalazine derivatives as ligands for GABAA receptors which are partial or full inverse agonists of an &agr;5 receptor subunit while being relatively free of activity at &agr;1 and/or &agr;2 and/or &agr;3 receptor subunit binding sites; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.
Type:
Application
Filed:
January 16, 2003
Publication date:
August 14, 2003
Inventors:
William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke.
Type:
Application
Filed:
November 14, 2002
Publication date:
August 14, 2003
Applicant:
Neurocrine Biosciences, Inc.
Inventors:
Mustapha Haddach, John Patrick Williams, Michael K. Schwaebe
Abstract: There is provided compounds of formula I, 1
Type:
Application
Filed:
December 12, 2002
Publication date:
August 14, 2003
Applicant:
AstraZeneca AB
Inventors:
Annika Bjore, Magnus Bjorsne, David Cladingboel, Kurt-Jurgen Hoffmann, John Pavey, Fritiof Ponten, Gert Strandlund, Peder Svensson, Colin Thomson, Michael Wilsterman
Abstract: Compounds of the formula (1), in which the substituents have the meanings mentioned in the description, are valuable intermediates for preparing active compounds for the prevention and treatment of gastrointestinal diseases.
Type:
Application
Filed:
September 19, 2002
Publication date:
August 14, 2003
Inventors:
Jorg Senn-Bilfinger, Wilm Buhr, Peter Zimmermann
Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Type:
Application
Filed:
January 29, 2003
Publication date:
August 14, 2003
Applicant:
SmithKline Beecham Corporation
Inventors:
John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
Abstract: The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.
Type:
Application
Filed:
October 30, 2002
Publication date:
August 14, 2003
Applicant:
Cell Therapeutics, Inc.
Inventors:
Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Anil M. Kumar, John Tulinsky
Abstract: A method for the treatment of pain is disclosed comprising administration of a pain-ameliorating effective amount of any compound according to structural diagram I; 1
Type:
Application
Filed:
December 17, 2002
Publication date:
August 14, 2003
Inventors:
Dean Gordon Brown, Thomas Michael Bare, Megan Murphy, Rebecca Ann Urbanek, Wenhua Xiao, Marie Frances McLaren, Carey Lynn Horchler
Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.
Type:
Application
Filed:
December 11, 2002
Publication date:
August 14, 2003
Inventors:
Norman Kong, Emily Aijun Liu, Binh Thanh Vu
Abstract: An antibacterial formulation suitable for injection into animals containing approximately 2-10% w/v difloxacin HCI, L-arginine base, propylene glycol, ethanol and/or benzyl alcohol, and water. The formulation is a solution having a pH of form 9 to 10. The formulation produces little or no tissue damage or irritation at the injection site.
Abstract: A method and composition for treating irritable bowel syndrome in a subject in need of such treatment, utilizing an amount of a polyamine having the formula:
Abstract: Crystalline forms of the p38 kinase inhibitor N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole are provided. These crystalline forms include (a) a first anhydrous crystalline form possessing improved physical stability relative to other solid-state forms of the compound; (b) a second anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; (c) a third anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; and (d) solvated crystalline forms, hydrated crystalline forms, and crystalline salt forms of the compound that are useful, for example, as intermediate solid-state forms in the preparation of other crystalline forms of the compound.
Type:
Application
Filed:
September 25, 2002
Publication date:
August 14, 2003
Inventors:
Kimberley C. Allen, Jerry D. Clark, Thomas P. Fraher, Jason A. Hanko, Kimberly L. Kolbert, Clay R. Little, Michael K. Mao, Patricia S. Miyake, Jodi L. Moe, Partha S. Mudipalli, Tobin C. Schilke, Christine B. Seymour, Ahmad Y. Sheikh, Gopichand Yalamanchili
Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described.
Type:
Application
Filed:
April 11, 2002
Publication date:
August 14, 2003
Applicant:
Queen's University
Inventors:
Donald F. Weaver, Buhendwa Musole Guillain, John R. Carran, Kathryn Jones
Abstract: Compounds of formula (I) wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6-alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, heterocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except for hydrogen may be optionally substituted; R2 and R3 independently represent optionally substituted C1-6-alkyl, or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted C3-7cycloalkyl or C3-7cycloalkenyl ring; or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted 5 to 7-membered heterocyclyl ring containing up to 3 heteroatoms selected from N, O, S.
Type:
Application
Filed:
January 7, 2003
Publication date:
August 14, 2003
Inventors:
Jon Graham Steadman, Andrew Kenneth Takle
Abstract: Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs.
Type:
Application
Filed:
January 27, 2003
Publication date:
August 14, 2003
Inventors:
Daniel A Moros, Barrie Levitt, Avraham Yacobi
Abstract: The present invention relates to a method of treating alcoholism or alcohol abuse by administering to a subject a pharmaceutically effective amount of an opioid antagonist before imminent drinking. Particularly, the present invention relates to a method of treating alcoholism or alcohol abuse by administering transmucosally to a subject a pharmaceutically effective amount of an opioid antagonist before imminent drinking. Preferably, the opioid antagonist used in the method is nalmefene or a pharmaceutically acceptable salt thereof. The invention also relates to a method of treating alcoholism or alcohol abuse by administering to a subject before imminent drinking a transmucosal preparation comprising a pharmaceutically effective amount of an opioid antagonist, wherein the transmucosal preparation has rapid onset of action. Advantageously, a FAH+ subject is treated.
Type:
Application
Filed:
August 13, 2002
Publication date:
August 14, 2003
Applicant:
OY CONTRAL PHARMA LTD
Inventors:
Kauko O.A. Kurkela, Olli Puhakka, Tuuli I. Sonck, Sakari Karhuvaara