Abstract: This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments. These compounds are poly(ADP-ribose) polymerase (PARP) inhibitors.
Type:
Grant
Filed:
December 6, 2006
Date of Patent:
September 14, 2010
Assignee:
sanofi-aventis Deutschland GmbH
Inventors:
Stefan Peukert, Stefan Guessregen, Armin Hofmeister, Herman Schreuder, Uwe Schwahn
Abstract: The present invention relates to the besylate salt of 7-(2-(4-(3-(trifluoromethyl)phenyl)-1,2,3,6-tetrahydropyrid-1-yl)ethyl)isoquinoline, to its preparation and to its use in therapeutics. The salt may be represented by the formula (II) below.
Abstract: The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds of the structure of formula I and pharmaceutical compositions comprising them wherein the R groups are herein defined. These are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke.
Type:
Grant
Filed:
March 1, 2007
Date of Patent:
September 7, 2010
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Hans-Jochen Lang, Uwe Heinelt, Klaus Wirth, Thomas Licher, Armin Hofmeister
Abstract: The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
Type:
Grant
Filed:
April 20, 2006
Date of Patent:
September 7, 2010
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Mark R. Player, Nand Baindur, Benjamin Brandt, Naresh Chadha, Raymond J. Patch, Davoud Asgari, Taxiarchis M. Georgiadis
Abstract: The invention concerns a compound of the Formula I wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl;or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
Type:
Grant
Filed:
December 22, 2005
Date of Patent:
August 31, 2010
Assignee:
AstraZeneca AB
Inventors:
Ian Alun Nash, Kenneth Mark Page, Paul Allen Bethel
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
August 28, 2006
Date of Patent:
August 31, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Guy Brenchley, Ronald Knegtel, Michael Mortimore
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
August 25, 2006
Date of Patent:
August 31, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian M. C. Golec, Michael Mortimore
Abstract: The present invention relates to compounds having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 22, 2004
Date of Patent:
August 24, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Isaacs, Christopher J. Dinsmore, Charles J. McIntyre, Linda S. Payne, David A. Claremon
Abstract: The invention provides compounds of formula I blocking phosphorylcholine biosynthesis by means of the selective blocking of the choline kinase enzyme in tumor cells or in cells affected by parasitic infection and therefore being applicable in the treatment of tumors and parasitic diseases or diseases produced by viruses and fungi in animals, including human beings; as well as to a method for preparing the compounds of the invention and certain intermediates of said method.
Type:
Grant
Filed:
January 11, 2005
Date of Patent:
August 24, 2010
Assignees:
Consejo Superior de Investigaciones Cientificas, Universidad de Granada
Inventors:
Juan Carlos Lacal Sanjuán, Joaquin Campos Rosa, Miguel Ángel Gallo Mezo, Antonio Espinosa Úbeda
Abstract: The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 22, 2004
Date of Patent:
July 27, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Isaacs, Christopher J. Dinsmore, B. Wesley Trotter, Nigel Liverton, Douglas C. Beshore, Nathan R. Kett, Charles J. McIntyre, Kausik K. Nanda, David A. Claremon
Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to a mammal.
Type:
Grant
Filed:
February 23, 2005
Date of Patent:
July 27, 2010
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Martine Clozel, Walter Fischli, Ralf Koberstein, Thomas Weller
Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.
Type:
Grant
Filed:
June 10, 2005
Date of Patent:
July 13, 2010
Assignee:
Vanderbilt University
Inventors:
Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.
Type:
Grant
Filed:
August 12, 2004
Date of Patent:
June 29, 2010
Assignees:
D-Pharm Ltd., Advanced Neuroprotective Systems Ltd.
Inventors:
Svetlana Dolina, Vitaly Shteiman, Marina Vinnikova, Israel Shapiro
Abstract: The invention discloses an improved process for producing an intermediate to produce large quantity of 2-(Phenyl methyl thio)-3-pyridine carboxylic acid. The process comprises reacting 2-chloro-3-cyanopyridine with benzyl mercaptan in presence of a base and an aprotic solvent. The resulting intermediate 2-(phenyl methyl thio)-3-cyanopyridine is hydrolyzed in presence of a base in an autoclave and isolated under acidic condition to get the desired product.
Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
June 22, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, Richard Isaacs, David A. Claremon
Abstract: The invention is concerned with novel substituted thiophene derivatives of formula (I) wherein R1 to R8, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.
Type:
Grant
Filed:
December 13, 2006
Date of Patent:
June 8, 2010
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Robert Narquizian, Constantinos G. Panousis
Abstract: The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].