Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
August 28, 2001
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
Abstract: This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
Abstract: The invention provides isolated nucleic acid compounds encoding enzyme mraY of Streptococcus pneumoniae. Also provided are vectors and transformed host cells for expressing the encoded enzyme, and a method for identifying compounds that inhibit said enzyme.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
August 7, 2001
Assignee:
Eli Lilly and Company
Inventors:
Jo Ann Hoskins, Robert Brown Peery, Paul Luther Skatrud, Michele Louise Young Bellido
Abstract: The invention provides isolated nucleic acid compounds encoding gcp of Streptococcus pneumoniae. Also provided are vectors and transformed host cells for expressing the encoded protein, and a method for identifying compounds that bind and/or inhibit said protein.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
July 31, 2001
Assignee:
Eli Lilly and Company
Inventors:
Jo Ann Hoskins, Joseph Chiou-Chung Tang, Patti Jean Treadway
Abstract: This invention is directed to methods for the preparation of [1S-[1a,2b,3b,4a(S*)]]-4-[7-[[1-(3-chloro-2-thienyl) methyl]propyl]amino]-3H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxyc yclopentanecarboxamide, methods for the preparation of intermediates thereto, and to said intermediates themselves.
Type:
Grant
Filed:
January 19, 1999
Date of Patent:
November 7, 2000
Assignee:
Aventis Pharmaceuticals Products Inc.
Inventors:
Michael K. O'Brien, Herve Garcia, Patrick Leon, Tory H. Powner, Laurence W. Reilly, Harshavadan C. Shah, Michael D. Thompson, Ching T. Tsuei, Benoit J. Vanasse, Francis L. Walther
Abstract: The invention is also directed to pharmaceutical composition comprising a compound having anti-Xa activity, a platelet aggregation antagonist compound and a pharmaceutically acceptable carrier. The invention is also directed to a method of treating or preventing a thrombogenic condition associated with a thrombosis related ischemic disorder in a patient comprising administering to said patient pharmaceutically effective amounts of a compound having anti-Xa activity and a platelet aggregation antagonist compound. In addition, this invention is directed to the use of pharmaceutically effective amounts of a compound having anti-Xa activity and a platelet aggregation antagonist compound in the preparation of a medicament for treating or preventing a physiological condition associated with thrombosis related ischemic disorder.
Type:
Grant
Filed:
November 16, 1998
Date of Patent:
August 15, 2000
Assignee:
Aventis Pharmaceuticals Products Inc.
Inventors:
Andre Uzan, Alain H. Curaudeau, Robert J. Leadley, Christopher T. Dunwiddie, Mark H. Perrone
Abstract: The invention provides isolated nucleic acid compounds encoding the glycosyltransferase protein GtfA of Amycolatopsis orientalis. Also provided are vectors carrying the gtfA gene, transformed heterologous host cells for expressing the GtfA protein, and methods for producing glycopeptide compounds using the cloned gtfA gene.
Type:
Grant
Filed:
July 21, 1998
Date of Patent:
July 11, 2000
Assignee:
Eli Lilly and Company
Inventors:
Richard H. Baltz, Patricia J. Solenberg
Abstract: The invention provides isolated nucleic acid compounds encoding HI1146 of Streptococcus pneumoniae. Also provided are vectors and transformed host cells for expressing the encoded protein, and a method for identifying compounds that bind and/or inhibit said protein.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
June 13, 2000
Assignee:
Eli Lilly and Company
Inventors:
Robert Brown Peery, Paul Luther Skatrud, Patti Jean Treadway, Michele Louise Young Bellido
Abstract: The invention provides isolated nucleic acid compounds encoding Era of Streptococcus pneumoniae. Also provided are vectors and transformed host cells for expressing the encoded protein, and a method for identifying compounds that bind and/or inhibit said protein.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
June 6, 2000
Assignee:
Eli Lilly and Company
Inventors:
Robert Brown Peery, Michele Louise Young Bellido, Genshi Zhao
Abstract: The invention provides isolated nucleic acid compounds encoding dpj of Streptococcus pneumoniae. Also provided are vectors and transformed host cells for expressing the encoded protein, and a method for identifying compounds that bind and/or inhibit said protein.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
May 9, 2000
Assignee:
Eli Lilly and Company
Inventors:
Joseph Chiou-Chung Tang, Patti Jean Treadway, Genshi Zhao
Abstract: This invention is directed to compounds of formula I: ##STR1## wherein the variables are as described herein. Compounds within the scope of the present invention possess useful properties, more particularly pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase.
Type:
Grant
Filed:
September 12, 1997
Date of Patent:
May 2, 2000
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Robert D. Groneberg, Kent W. Neuenschwander, Stevan W. Djuric, Gerald M. McGeehan, Christopher J. Burns, Steven M. Condon, Matthew M. Morrissette, Joseph M. Salvino, Anthony C. Scotese, John W. Ullrich
Abstract: The invention provides isolated nucleic acid compounds encoding the glycosyltransferase protein GtfC of Amycolatopsis orientalis. Also provided are vectors carrying the gtfC gene, transformed heterologous host cells for expressing the GtfC protein, and methods for producing glycopeptide compounds using the cloned gtfC gene.
Type:
Grant
Filed:
July 21, 1998
Date of Patent:
February 22, 2000
Assignee:
Eli Lilly and Company
Inventors:
Richard H. Baltz, Patricia J. Solenberg
Abstract: The invention provides isolated nucleic acid compounds encoding the glycosyltransferase protein GtfB of Amycolatopsis orientalis. Also provided are vectors carrying the gtfB gene, transformed heterologous host cells for expressing the GtfB protein, and methods for producing glycopeptide compounds using the cloned gtfB gene.
Type:
Grant
Filed:
July 21, 1998
Date of Patent:
February 15, 2000
Assignee:
Eli Lilly and Company
Inventors:
Richard H. Baltz, Patricia J. Solenberg
Abstract: The invention provides isolated nucleic acid compounds encoding the glycosyltransferase protein GtfD of Amycolatopsis orientalis. Also provided are vectors carrying the gtfD gene, transformed heterologous host cells for expressing the GtfD protein, and methods for producing glycopeptide compounds using the cloned gtfD gene.
Type:
Grant
Filed:
July 21, 1998
Date of Patent:
February 15, 2000
Assignee:
Eli Lilly and Company
Inventors:
Richard H. Baltz, Patricia J. Solenberg
Abstract: The presently-disclosed IPC synthase-inhibitor assays comprise the steps of: (1) expression of the IPC1 gene in a cell; (2) introducing labeled starting substrates for ceramide conversion as well as potential inhibitor(s) of such conversion to the expressed gene product in an environment which allows time and conditions for conversion, and (3) identifying those potential inhibitors which actually inhibit conversion.
Type:
Grant
Filed:
October 6, 1997
Date of Patent:
February 8, 2000
Assignees:
University of Kentucky Research Foundation, Eli Lilly and Company
Inventors:
Jeffrey Radding, Robert C. Dickson, Robert L. Lester
Abstract: Compositions containing one or more nucleic acids and cationic polymers, and their use in gene therapy, particularly for in vivo nucleic acid transfer.
Type:
Grant
Filed:
February 28, 1997
Date of Patent:
January 11, 2000
Assignee:
Rhone-Poulenc Rorer SA
Inventors:
Jean-Paul Behr, Barbara Demeneix, Franck Lezoualch, Mojgan Mergny, Daniel Scherman, Otmane Boussif
Abstract: This invention provides novel fungal strains altered in IPC synthase production, and a method for screening for inhibitors of fungal IPC synthase using whole cells.
Type:
Grant
Filed:
April 9, 1997
Date of Patent:
November 2, 1999
Assignee:
Eli Lilly and Company
Inventors:
Steven Alan Heidler, Jeffrey Alan Radding, Debra Ann Young
Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
Type:
Grant
Filed:
November 21, 1997
Date of Patent:
September 28, 1999
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
William R. Ewing, Michael R. Becker, Henry W. Pauls, Daniel L. Cheney, Jonathan Stephen Mason, Alfred P. Spada, Yong Mi Choi-Sledeski
Abstract: Pharmaceutical composition useful for transfecting a nucleic acid and characterised in that it contains, in addition to the nucleic acid, at least one transfecting agent and a compound causing the condensation of the nucleic acid, wherein the compound is totally or partly derived from a histone, a nucleoline, a protamine and/or a derivative thereof. The use of the composition for transferring nucleic acids in vitro, ex vivo and/or in vivo is also described.
Type:
Grant
Filed:
August 15, 1997
Date of Patent:
August 31, 1999
Assignee:
Rhone-Poulenc Rorer SA
Inventors:
Daniel Scherman, Gerardo Byk, Bertrand Schwartz
Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
Type:
Grant
Filed:
July 28, 1993
Date of Patent:
August 10, 1999
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker