Abstract: The compound, ((3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl)oxy)ac etic acid morpholino-N-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
Type:
Grant
Filed:
May 12, 1999
Date of Patent:
October 31, 2000
Assignee:
Eli Lilly and Company
Inventors:
Jason Scott Sawyer, John Michael Morin, Jr., Douglas Wade Beight, Daniel Jon Sall, John Andrew Buben
Abstract: A method is disclosed for the treatment of chronic bronchitis by administering to a mammal in need thereof a therapeutically effective amount of a 1H-indole-3-glyoxylamide compound.
Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
Type:
Grant
Filed:
May 14, 1997
Date of Patent:
July 6, 1999
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
Type:
Grant
Filed:
December 16, 1997
Date of Patent:
July 6, 1999
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
Abstract: The use of a compound of the formula: ##STR1## in which X is --O-- or --NH--, or a pharmaceutically-acceptable acid addition salt thereof, in the treatment of atherosclerosis.
Abstract: This invention relates to a combinatorial process for synthesizing a library of azetidinone peptide-like compounds. The compounds are synthesized as mixtures from a common azetidinone intermediate. The compounds are biologically active as inhibitors of the Vasopressin (V1a) receptor.
Type:
Grant
Filed:
May 3, 1995
Date of Patent:
June 2, 1998
Assignee:
Eli Lilly and Company
Inventors:
Robert F. Bruns, Michael O. Chaney, Robin D. Cooper, David C. Hunden, Gary A. Koppel, Jeffrey J. Skelton
Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
Type:
Grant
Filed:
March 28, 1997
Date of Patent:
March 31, 1998
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
Abstract: A method for photochemical cleavage of carbon-sulfur bonds in conjunction with solid-phase synthesis utilizing a deoxygenated solvent and light to cleave the carbon-sulfur bond from a heterogeneous support. Also disclosed are compounds for use with said photochemical cleavage and methods of preparing them.
Abstract: A class of novel 1-indole-3-acetamides represented by the formula; ##STR1## is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids.
Type:
Grant
Filed:
May 5, 1995
Date of Patent:
November 4, 1997
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
August 5, 1997
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
Abstract: A class of novel 1H-indole-1-functional compounds is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock. The compounds are 1H-indole-1-acetamides, 1H-indole-1-acetic acid hydrazides, and 1H-indole-1-glyoxylamides.
Type:
Grant
Filed:
April 13, 1995
Date of Patent:
June 24, 1997
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
Abstract: This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: ##STR1## and their use as LTD.sub.4 antagonists.
Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
Type:
Grant
Filed:
July 8, 1994
Date of Patent:
April 8, 1997
Assignee:
Eli Lilly and Company
Inventors:
Matthew J. Fisher, Anne M. Happ, Joseph A. Jakubowski, Michael D. Kinnick, Allen D. Kline, John M. Morin, Jr., Daniel J. Sall, Marshall A. Skelton, Robert T. Vasileff
Abstract: Selected acid functional beta-carboline type derivatives effective as thromboxane synthase inhibitors having the formula: ##STR1## where R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.
Type:
Grant
Filed:
May 5, 1995
Date of Patent:
February 18, 1997
Assignee:
Eli Lilly and Company
Inventors:
Joseph A. Jakubowski, Alan D. Palkowitz
Abstract: A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
November 26, 1996
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
Abstract: This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: ##STR1## and their use as LTD.sub.4 antagonists.
Abstract: The instant invention provides a novel process for preparing benzyl-substituted rhodanine derivatives. The process is particularly useful for synthesizing the enantiomers of such derivatives. Also provided are novel benzyl-substituted mercaptopropanoic acids and benzyl-substituted thiazolidinones. Such compounds are useful for treating inflammatory bowel disease and, accordingly, the present invention provides a method of treating inflammatory bowel disease in mammals utilizing such novel compounds as well as pharmaceutical compositions containing same.
Type:
Grant
Filed:
December 21, 1994
Date of Patent:
October 8, 1996
Assignee:
Eli Lilly and Company
Inventors:
Marvin M. Hansen, Allen R. Harkness, Michael J. Martinelli, Vien V. Khau
Abstract: This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Type:
Grant
Filed:
February 14, 1994
Date of Patent:
September 3, 1996
Assignee:
Eli Lilly and Company
Inventors:
Robert D. Dillard, J. Scott Sawyer, Michael J. Sofia
Abstract: Selected acid functional polyhydronorharman type derivatives effective as thromboxane synthase inhibitors having the formula: ##STR1## where R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.
Type:
Grant
Filed:
January 31, 1994
Date of Patent:
August 27, 1996
Assignee:
Eli Lilly and Company
Inventors:
Joseph A. Jakubowski, Alan D. Palkowitz, Sandra K. Sigmund