Abstract: Pharmaceutical compositions comprising, as a first anti-neoplastic drug, cyanoguanidine IKK inhibitors, and in particular compounds of formula I 1
Type:
Application
Filed:
May 21, 2002
Publication date:
March 6, 2003
Inventors:
Lise Binderup, Erik Bramm, Pernille-Julia Vig Hjarnaa, Karin Jexner Hamberg
Abstract: Disclosed are novel compounds of the formula 1
Type:
Application
Filed:
October 15, 2001
Publication date:
March 6, 2003
Inventors:
Robert G. Aslanian, Neng-Yang Shih, Pauline C. Ting, Michael Y. Berlin, Stuart B. Rosenblum, Kevin D. McCormick, Wing C. Tom, Christopher W. Boyce, Pietro Mangiaracina, Mwangi W. Mutahi, John J. Piwinski
Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action.
Abstract: The present invention relates to a novel sustained-release oral galenical form of molsidomine for the treatment of all forms of angina attack (angina of effort, spastic angina, mixed angina). According to the invention, this novel galenical form contains a therapeutically effective amount of molsidomine or one of its active metabolites and has an in vitro dissolution rate [measured spectrophotometrically at 286 or 311 nm by the method described in the European Pharmacopoeia, 3rd edition (or USP XXIV), at 50 rpm, in 500 ml of a 0.1 N HCl medium, at 37° C.] of: 15 to 25% of molsidomine released after 1 hour, 20 to 35% of molsidomine released after 2 hours, 50 to 65% of molsidomine released after 6 hours, 75 to 95% of molsidomine released after 12 hours, >85% of molsidomine released after 18 hours and >90% of molsidomine released after 24 hours, the plasma peak of molsidomine obtained in vivo occurring 2.
Abstract: Pharmaceutical compositions include aryl substituted amine compounds, and in particular, carbon-linked aromatic azabicyclo compounds, and in particular, aromatic alkylene azabicyclo compounds and aromatic alkyl azabicyclo compounds.
Type:
Application
Filed:
June 4, 2002
Publication date:
March 6, 2003
Inventors:
Jeffrey Daniel Schmitt, Peter Anthony Crooks, Gary Maurice Dull
Abstract: Compositions comprising an alpha-2-adrenergic agonist component and a fatty acid component, that enhances the pharmacokinetic disposition of the therapeutic component, are disclosed. The fatty acid component may include linolenic acid and/or other fatty acids. In a one embodiment, the alpha-2-adrenergic agonist component and the fatty acid component form a complex.
Abstract: The present invention provides a method of specifically potentiating an N-type Ca2+ channel activity, which includes administering, to a subject, a compound of the following formula (I): 1
Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or ◯subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
Type:
Application
Filed:
June 14, 2002
Publication date:
March 6, 2003
Inventors:
Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
Abstract: In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of viral infections comprising a at least one antiviral active compound of formula (1) 1
Abstract: The invention relates to 6- or 7-bicyclic-substituted 4-amino-subsituted pyridopyrimidines and to pharmaceutically acceptable salts, prodrugs and hydrates thereof. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating hyperproliferative disorders abnormal cell growth in a mammal by administering the compounds.
Type:
Application
Filed:
April 12, 2002
Publication date:
March 6, 2003
Applicant:
Pfizer Inc.
Inventors:
Joel Morris, Samit K. Bhattacharya, John C. Kath
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
Type:
Application
Filed:
November 30, 2001
Publication date:
March 6, 2003
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: The present invention relates to 4-(phenylamino)-[1,4]dioxano[2,3-g]quinazoline derivatives which inhibit tyrosine kinase of epidermal growth factor receptor (EGFR), and pharmaceutically acceptable salts, hydrates and solvates thereof, and a process for preparing the same. Since 4-(phenylamino)-[1,4]dioxano[2,3-g]quinazoline derivatives of the invention have a high solubility in water and inhibit the activity of EGFR tyrosine kinase and the growth of cancer cells, they can be practically applied in the treatment of overproliferation-associated diseases such as cancer.
Type:
Application
Filed:
March 11, 2002
Publication date:
March 6, 2003
Inventors:
Yong-Sup Lee, Ho-Koon Park, Jae-Yeol Lee, Beom-Seok Yang, Seon-Hee Seo
Abstract: The present invention provides a series of novel bifunctional molecules based on viologen linked acridine, bisacridine and bisacridinium salts of the general formula 1 (1a, 1b, 1c and 1d) and or pharmaceutically acceptable derivatives thereof, which can be used as phototherapeutic and catalytic photoactivated DNA cleaving agents. These molecules are very stable and exhibit high solubility in buffer at physiological conditions. They undergo strong binding with DNA through intercalation and groove binding interactions and show remarkably high affinity for poly(dA).poly(dT) sequences. Upon photoactivation, they cleave DNA catalytically and selectively at guanine (G) sites in duplex DNA exclusively through cosensitization mechanism with a preference for 5′-G over 3′-G. They induce unusally high specificity of cleavage at G site of the AG two base bulge sequences.
Type:
Application
Filed:
February 28, 2001
Publication date:
March 6, 2003
Applicant:
COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH of India
Inventors:
Ramaiah Danaboyina, Varghese Eldho Nadukkudy, Joseph Joshy
Abstract: This invention discloses new uses and treatments involving cabergoline, pramipexole and new combinations of cabergoline plus pramipexole used to treat patients. Here we disclose the use of cabergoline or pramipexole to treat PSP and MSA. Also disclosed is a combination treatment of cabergoline and pramipexole provided concurrently to a patient in need thereof for the treatment of various central nervous system diseases and in particular for the treatment of Parkinson's Disease (PD), but also for PSP and MSA.
Abstract: The use of GABAA-receptor modulators with NMDA-antagonistic activity for the production of a pharmaceutical agent for neuroprotection and the combination of GABAA-receptor modulators with NMDA-antagonistic action and &agr;-lipoic acid or dihydro-&agr;-lipoic acid is described.
Type:
Application
Filed:
July 19, 2002
Publication date:
March 6, 2003
Inventors:
Christopher Bruckner, Rainer Dorow, Roland Neuhaus
Abstract: A system for treating a condition associated with a mucosal surface, the system comprising an immune response modifier (IRM) compound chosen from imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines, 1,2-bridged imidazoquinoline amines, and pharmaceutically acceptable salts thereof and an applicator device for applying the IRM compound to the mucosal surface. This system of IRM compounds and applicator may be used to treat conditions associated with mucosal surfaces such as cervical dysphasia and cervical intraepithelial neoplasia.
Type:
Application
Filed:
September 10, 2002
Publication date:
March 6, 2003
Applicant:
3M Innovative Properties Company
Inventors:
John C. Hedenstrom, Michael J. Jozwiakowski, Mark Martinez, Kenneth R. Phares, Kenneth Trofatter
Abstract: The invention relates to the use of chemotherapeutic agents for the production of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Application
Filed:
September 12, 2002
Publication date:
March 6, 2003
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: 1
Type:
Application
Filed:
June 10, 2002
Publication date:
March 6, 2003
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, John A. Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Kristin P. Ollis
Abstract: The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.
Abstract: Polymorphs Form B, Form C, and amorphous of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, commonly known as cilostazol, have been identified. These polymorphs may be formed in pure form, in combination with each other, in combination with other polymorphs of cilostazol, or together with other pharmaceutical agents. Processes for preparing these polymorphs, and combinations of these polymorphs, as well as methods of use and unit dosages of these polymorphic forms, and their combinations, are described.
Type:
Application
Filed:
June 29, 2001
Publication date:
March 6, 2003
Inventors:
Grayson Walker Stowell, Robert R. Whittle
Abstract: Polymorphs Form B, Form C, and amorphous of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, commonly known as cilostazol, have been identified. These polymorphs may be formed in pure form, in combination with each other, in combination with other polymorphs of cilostazol, or together with other pharmaceutical agents. Processes for preparing these polymorphs, and combinations of these polymorphs, as well as methods of use and unit dosages of these polymorphic forms, and their combinations, are described.
Type:
Application
Filed:
June 29, 2001
Publication date:
March 6, 2003
Inventors:
Grayson Walker Stowell, Robert R. Whittle
Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as naphthoic acid derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be stromal cell-derived factor (SDF)-1, and the relevant chemokine receptors may for example be corresponding chemokine receptor (CXCR-4). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of 3-Hydroxy-2-naphthoic acid in the treatment of disease.
Type:
Application
Filed:
November 13, 2001
Publication date:
March 6, 2003
Inventors:
Geeta Saxena, Christopher R. Tudan, Ahmed Merzouk, Hassan Salari
Abstract: The present invention comprises a pseudopolymorph of (−)-cis-2-(2-chlorophenyl)-5,7-dihydroxy-8[4R-(3S-hydroxy-1-methyl)piperidinyl]-4H-1-benzopyran-4-one hydrochloride, a method of making same, a pharmaceutical composition and methods of using the pseudopolymorph.
Type:
Application
Filed:
January 16, 2001
Publication date:
March 6, 2003
Inventors:
Gary L. Bafus, Christine M. Harrison-Bowman, Gary Lee Silvey
Abstract: The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-&agr; in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.
Type:
Application
Filed:
October 5, 2001
Publication date:
March 6, 2003
Inventors:
Michael J. Robarge, Roger Shen-Chu Chen, George W. Muller, Hon-Wah Man
Abstract: Combination therapy comprising PPAR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.
Type:
Application
Filed:
April 3, 2002
Publication date:
March 6, 2003
Inventors:
Jacqueline C. Bussolari, Xiaoli Chen, Bruce R. Conway, Keith T. Demarest, Hamish N.M. Ross, Rafael Severino
Abstract: The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists.
Type:
Application
Filed:
July 17, 2002
Publication date:
March 6, 2003
Inventors:
Nelo R. Rivera, Christopher J. Welch, Yi Xiao, Nobuyoshi Yasuda
Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes.
Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: 1
Type:
Application
Filed:
April 11, 2002
Publication date:
March 6, 2003
Applicant:
Eli Lilly & Company Lily Corporate Center
Inventors:
Dawn A. Brooks, Christopher J. Rito, Anthony J. Shuker, Samuel J. Dominianni, Alan M. Warshawsky, Lynn S. Gossett, Donald P. Matthews, David A. Hay, Robert J. Ardecky, Pierre-Yves Michellys, John S. Tyhonas
Abstract: The invention is directed to small organic molecules having the ability to mimic or agonize hepatocyte growth factor/scatter factor (HGF/SF) activity, or inhibit or antagonize HGF/SF activity, the former useful for promoting, for example, vascularization of tissues or organs for promoting wound or tissue healing, or augmenting or restoring blood flow to ischemic tissues such as the heart following myocardial infarction. Inhibition of cellular growth or proliferation is beneficial in the treatment, for example, of inflammatory diseases such as inflammatory joint and skin diseases, and dysproliferative diseases such as cancer.
Type:
Application
Filed:
June 29, 2001
Publication date:
March 6, 2003
Inventors:
Sivaram Pillarisetti, Itzhak D. Goldberg
Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: 1
Type:
Application
Filed:
June 13, 2002
Publication date:
March 6, 2003
Applicant:
Wyeth
Inventors:
Thomas Joseph Commons, Susan Christman Croce, Richard Page Woodworth, Eugene John Trybulski, Hassan Mohmoud Elokdah, David LeRoy Crandall
Abstract: This invention provides for the treatment of inflammatory, cancer and thrombotic disorders through the administration, in combination, of a COX2 inhibitor, low dose aspirin, and antioxidant flavanoids, flavonoids or isoflavones and at least one of these combinations will be given in a subtherapeutic amount for improved anti-inflammatory, anti-cancer, and anti-thrombotic efficacy and safety.
Abstract: An orally deliverable pharmaceutical composition is provided comprising a drug of low water solubility, a solvent liquid that comprises at least one pharmaceutically acceptable solvent, and a turbidity-decreasing polymer, wherein (a) a substantial portion, for example at least about 15% by weight, of the drug is in dissolved or solubilized form in the solvent liquid, and (b) the polymer is present in an amount sufficient to substantially inhibit crystallization and/or precipitation of the drug in simulated gastric fluid.
Type:
Application
Filed:
January 15, 2002
Publication date:
March 6, 2003
Inventors:
Ping Gao, Michael J. Hageman, Walter Morozowich, Robert J. Dalga, Kevin J. Stefanski, Tiehua Huang, Aziz Karim, Fred Hassan, James C. Forbes
Abstract: The present invention relates to Saururus chinensis extract for prevention and treatment of neurodegenerative disease and pharmaceutical preparations containing Saururs chinensis extract or an aristolactam alkaloid derivative separated therefrom.
Type:
Application
Filed:
June 19, 2002
Publication date:
March 6, 2003
Inventors:
Young-Joong Kim, Sang-Hyun Sung, So-Ra Kim