Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
Type:
Grant
Filed:
August 19, 2002
Date of Patent:
July 19, 2005
Assignee:
Genentech, Inc.
Inventors:
Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.
Type:
Grant
Filed:
October 25, 2001
Date of Patent:
June 21, 2005
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
Abstract: The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
Type:
Grant
Filed:
June 25, 2003
Date of Patent:
June 14, 2005
Assignee:
Warner-Lambert Company
Inventors:
Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic, Andrew David White
Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
Type:
Grant
Filed:
October 6, 2003
Date of Patent:
May 10, 2005
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Ian Churcher, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Andrew Pate Owens, Duncan Edward Shaw, Joanne Thomson, Susannah Williams
Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.
Type:
Grant
Filed:
October 14, 1999
Date of Patent:
May 3, 2005
Assignee:
Dompe S.p.A.
Inventors:
Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
August 12, 2003
Date of Patent:
March 1, 2005
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.
Type:
Grant
Filed:
March 19, 2003
Date of Patent:
February 22, 2005
Assignee:
Icagen, Inc.
Inventors:
Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
Type:
Grant
Filed:
December 7, 2001
Date of Patent:
February 1, 2005
Assignee:
ICAgen
Inventors:
Serge Beaudoin, Aimee D. Reed, Michael F. Gross
Abstract: The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
January 4, 2005
Assignee:
University of Tennessee Research Foundation
Inventors:
Mitchell S. Steiner, Karen A. Veverka, James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
Abstract: The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.
Type:
Application
Filed:
June 30, 2004
Publication date:
December 9, 2004
Inventors:
Arthur A. Aykanian, Steve Billingsley, Philip M. Hodge, Kevin L. Simpson, John Spisak, Jim Strahan
Abstract: Compounds having the general formula I are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties. These compounds may be used in methods of preventing and/or treating clotting disorders.
Abstract: Novel formulations containing a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol, and methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease.
Type:
Application
Filed:
May 28, 2004
Publication date:
December 2, 2004
Applicant:
SCHERING-PLOUGH ANIMAL HEALTH CORPORATION
Inventors:
Keith A. Freehauf, Allan Weingarten, Robert D. Simmons, Kanwal Jit Varma
Abstract: The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for the treatment of epilepsy, affective illness, cognitive disorders, neurodegenerative disease, neuropathic pain syndrome, migraine, stroke, brain ischemia, or head trauma injury.
Type:
Application
Filed:
July 14, 2004
Publication date:
December 2, 2004
Inventors:
Meir Bialer, Boris Yagen, Nina Isoherranen
Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory drug of low water solubility, for example celecoxib, in an immediate-release fraction and a controlled-release, slow-release, programmed-release, timed-release, pulse-release, sustained-release or extended-release fraction. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.
Type:
Application
Filed:
February 23, 2004
Publication date:
December 2, 2004
Inventors:
Subhash Desai, Sreekant R. Nadkarni, Randy J. Wald, Gary A. DeBrincat
Abstract: The present invention provides a method of treating Bipolar I Disorder, Single Manic Episode; Bipolar I Disorder, Most Recent Episode Hypomanic; Bipolar I Disorder, Most Recent Episode Manic; Bipolar I Disorder, Most Recent Episode Mixed; Bipolar I Disorder, Most Recent Episode Depressed; Bipolar I Disorder, Most Recent Episode Unspecified; Bipolar II Disorder; or Bipolar Disorder NOS, in a patient, comprising administering to said patient an effective amount of a compound selected from the group consisting of: A) 2-[4-(4-{2-[(methylsulfonyl)amino]ethyl}phenyl)phenyl]propyl}[(methylethyl)sulfonyl]amine; B) {(2R)-2-[4-(4-{2-[(methylsulfonyl)amino]ethyl}phenyl)phenyl]propyl}[(methylethyl)sulfonyl]amine; D) N-2-(4-N-(3,5-Difluorobenzamido)phenyl)propyl-2-propanesulfonamide; and E) N-[4-((1R)-1-methyl-2-{[(methylethyl)sulfonyl]amino}ethyl)phenyl](3,5-difluorophenyl)carboxamide; and the phar
Abstract: Disclosed are compounds of the formula: 1
Type:
Application
Filed:
June 16, 2004
Publication date:
November 25, 2004
Applicant:
Schering Corporation
Inventors:
Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.
Type:
Grant
Filed:
November 2, 2001
Date of Patent:
November 23, 2004
Assignee:
Tularik Inc.
Inventors:
Susan Schwendner, Pieter Timmermans, Jacqueline Walling
Abstract: The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of a sodium ion channel blocker in combination with a cyclooxygenase-2 selective inhibitor.
Abstract: The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
Type:
Grant
Filed:
November 26, 2002
Date of Patent:
October 26, 2004
Assignee:
Warner-Lambert Company LLC
Inventors:
Lain-Yen Hu, Suzanne Ross Kesten, Huangshu Lei, Todd Robert Ryder, David Juergen Wustrow
Abstract: A topical composition and method for treating seborrehic dermatitis designed specifically to allow for short duration skin contact time. It is a water rinseable sulfacetamide composition free of elemental sulfur, preferably dosed in a regimen of at least two daily treatments.
Type:
Application
Filed:
April 3, 2003
Publication date:
October 14, 2004
Applicant:
Healthpoint, Ltd.
Inventors:
Braham Shroot, Robert Espinoza, Jimmy Joe Willis
Abstract: A compound of formula (I) is provided which is able to interact with &bgr;-catenin/TCF-4 binding site, having a structure essentially equivalent to a pharmacophore (IA), as herein described.
Type:
Application
Filed:
May 24, 2004
Publication date:
October 14, 2004
Inventors:
Juergen Moll, Stefan Knapp, Claudio Dalvit, Jean-Yves Trosset, Michael Sundstrom, Sergio Mantegani
Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.
Type:
Application
Filed:
April 10, 2003
Publication date:
October 14, 2004
Applicant:
Schering AG
Inventors:
Thorsten Blume, Roland Neuhaus, Detlev Suelzle, Iris Pribilla, Gisbert Depke, Joseph S. Beckman
Abstract: The present invention encompasses a method for treating or preventing migraines in a mammalian patient in need of such treatment or prevention comprising administering to said patient an NR2B receptor antagonist in an amount that is effective to treat or prevent migraines. The invention also encompasses the combination of an NR2B antagonist with a cyclooxygenase-2 selective inhibitor, a calcitonin gene-related peptide receptor (CGRP) ligand, a leukotriene receptor antagonist or a 5HT1B/1D agonist for the treatment or prevention of migraines.
Type:
Application
Filed:
December 5, 2003
Publication date:
October 14, 2004
Inventors:
Christopher Allen, Ken S. Koblan, Timothy Sleeth
Abstract: The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders.
Abstract: Inhibitors of the alpha carbonic anhydrase inhibitors are administered to treat H. pylori infection in the mammalian, including human, stomach. The inhibitors are administered to mammals, including humans, in an amount that results in 4×10−4 to 4×10−9 Molar concentration of the drug in the stomach because this concentration range is lethal to the H. pylori bacteria.
Type:
Application
Filed:
April 2, 2004
Publication date:
October 14, 2004
Inventors:
David R. Scott, Elizabeth A. Marcus, George Sachs
Abstract: The present invention provides compounds of formula (I), useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
Type:
Application
Filed:
January 30, 2003
Publication date:
October 7, 2004
Inventors:
David Michael Bender, Scott Louis Forman, Winton Dennis Jones, Daryl Lynn Smith, Dennis Michael Zimmermann
Abstract: Compounds having quinone and quinone analogs useful for pharmaceutical preparations have now been found which inhibit cysteine proteases, in particular, caspases and 3C-cysteine proteases. The cysteine protease inhibitors of the present invention can be identified by their mode of action in disrupting the ability of cysteine proteases and, in particular, caspases to cleave a peptide chain. These compounds are useful in inhibiting cysteine protease or cysteine protease-like proteins and for treating infections diseases or physiopathological diseases or disorders attributed to the presence of excessive or insufficient levels of cysteine proteases.
Type:
Application
Filed:
May 17, 2004
Publication date:
October 7, 2004
Inventors:
Dorit Arad, Arthur P Bollon, David C Young, Bradley W Poland, Andrew S Peek, Balin Shaw, Jyothi Vallurupalli
Abstract: Disclosed are compounds of Formula I, their N-oxides and agricultually suitable salts (I) wherein J is a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is substituted with from one to four substituents independently selected from R5; and A, B, G, R1, R2, R3, R4, R5, R6 and n are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the pests or their environment with a biologically effective amount of a compound of Formula (I) and compositions containing the compounds of Formula (I).
Type:
Application
Filed:
January 7, 2004
Publication date:
September 30, 2004
Inventors:
Bruce Lawrence Finkelstein, George Philip Lahm, Tom Paul Selby, Thomas Martin Stevenson
Abstract: The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of a disorder ameliorated by a gastroprokinetic.
Abstract: In one aspect, the present invention provides a method for modulating an Edg-2 receptor mediated biological activity in a cell. A cell expressing the Edg-2 receptor is contacted with an modulator of the Edg-2 receptor, which modulates the Edg-2 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating Edg-2 receptor mediated biological activity in a subject. A therapeutically effective amount of an modulator of the Edg-2 receptor is administered to the subject.
Type:
Application
Filed:
January 16, 2004
Publication date:
September 30, 2004
Inventors:
David Solow-Cordero, Geetha Shankar, Juliet V. Spencer, Charles Gluchowski
Abstract: The present invention provides matriptase inhibitors and compositions thereof useful for treating cancer. Martripase is a trypsin-like serine protease active in the development of cancerous conditions, such as tumors and metastasis of cancer.
Type:
Application
Filed:
December 18, 2003
Publication date:
September 23, 2004
Applicant:
Dendreon Corporation
Inventors:
David F. Duncan, L. Josue Alfaro-Lopez, Mallareddy Komandla, Odile Esther Levy, Ofir Moreno, Joseph E. Semple, Amir P. Tamiz
Abstract: An orally deliverable pharmaceutical composition comprises a drug of low water solubility and a pregelatinized starch having low viscosity and/or exhibiting a multimodal particle size distribution. A process for preparing such a composition comprises a step of selecting a pregelatinized starch having low viscosity and/or exhibiting a multimodal particle size profile, and a step of admixing the selected pregelatinized starch with a drug of low water solubility.
Type:
Application
Filed:
August 25, 2003
Publication date:
September 23, 2004
Inventors:
Carl T. Allenspach, Sreekant R. Nadkarni, Daryl A. Roston, Brian R. Rohrs, Roxana F. Schlam
Abstract: There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the &bgr;-amyloid precursor protein, and hence are useful in the treatment of Alzheimer's Disease.
Type:
Application
Filed:
January 20, 2004
Publication date:
September 23, 2004
Inventors:
Jonne Clare Hannam, Timothy Harrison, Andrew Madin, Timothy Jason Sparey
Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): 1
Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): 1
Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
Type:
Application
Filed:
August 29, 2003
Publication date:
September 9, 2004
Applicant:
Pfizer Inc
Inventors:
Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Type:
Application
Filed:
November 26, 2003
Publication date:
September 9, 2004
Inventors:
Jonas Fagerhad, Lanna Li, Lindstedt Alstermark Eva-Lotte
Abstract: The present invention provides compositions and methods for the treatment of reduced blood flow to the central nervous system in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition comprising the administration to a subject of an amphetamine in combination with a cyclooxygenase-2 selective inhibitor.
Abstract: The invention relates to compounds of formula (I), to salts and stereoisomers thereof, to their production and to their use for producing medicaments used for treating cardiovascular diseases.
Type:
Application
Filed:
April 12, 2004
Publication date:
September 9, 2004
Inventors:
Cristina Alonso-Alija, Michael Harter, Michael Hahn, Josef Pernerstorfer, Stefan Weigand, Johannes-Peter Stasch, Frank Wunder
Abstract: The present invention provides compositions and methods for the treatment of a vaso-occlusive event. More particularly, the invention provides a combination therapy for the treatment of a vaso-occlusive event comprising the administration to a subject of a selective serotonin reuptake inhibitor in combination with a cyclooxygenase-2 selective inhibitor.
Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Type:
Application
Filed:
November 17, 2003
Publication date:
September 2, 2004
Inventors:
Solomon Ugashe, Zheng Wei, J. J. Wright, Andrew Pennell