Abstract: This invention provides methods for the treatment or prevention of interstitial cystitis or urethral syndrome in a mammal which comprise administering to a mammal in need thereof an effective amount of a substituted benzimidazole, or a pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
August 25, 1998
Date of Patent:
February 15, 2000
Assignee:
Eli Lilly and Company
Inventors:
Smriti Iyengar, Mark A. Muhlhauser, Karl B. Thor
Abstract: The present invention provides novel methods of lowering serum cholesterol and inhibiting smoother muscle cell proliferation, particularly restenosis, in humans, and inhibiting uterine fibroid disease and endometriosis in women comprising administering to a human/woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, or trifluoromethyl;R.sup.1 and R.sup.2 each are the same or different C.sub.1 -C.sub.6 alkyl group;n is an integer from 2 to 6; andR.sup.3 and R.sup.4 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form a substituent selected from the group consisting of pyrrolidino, morpholino, piperidino, piperazino, 4-(C.sub.1 -C.sub.6 alkyl)piperazino, and 4-phenyl-piperazino; or a pharmaceutically acceptable salt thereof.
Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
Type:
Grant
Filed:
April 30, 1997
Date of Patent:
February 15, 2000
Assignee:
Eli Lilly and Company
Inventors:
Jolie Anne Bastian, Nickolay Yuri Chirgadze, Michael Lyle Denney, Matthew Joseph Fisher, Robert James Foglesong, Richard Waltz Harper, Mary George Johnson, Valentine Joseph Klimkowski, Todd Jonathan Kohn, Ho-Shen Lin, Michael Patrick Lynch, Jefferson Ray McCowan, Alan David Palkowitz, Michael Enrico Richett, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Jennifer Marie Tinsley, Minsheng Zhang
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: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
Type:
Grant
Filed:
March 24, 1998
Date of Patent:
February 1, 2000
Assignee:
Eli Lilly and Company
Inventors:
Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Jr., Michael Paal, Gerd Ruhter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
Abstract: An automatic contextual segmentation method which can be used to identify features in QCT images of femora, tibiae and vertebrae. The principal advantages of this automatic approach over traditional techniques such as histomorphometry are, 1) the algorithms can be implemented in a fast, uniform, non-subjective manner across many images allowing unbiased comparisons of therapeutic efficacy, 2) much larger volumes in the region of interest can be analyzed, and 3) QCT can be used longitudinally. Two automatic contextual segmentation algorithms relate to a cortical bone algorithm (CBA) and a whole bone algorithm (WBA). These methods include a preprocessing step, a threshold selection step, a segmentation step satisfying logical constraints, a pixel wise label image updating step, and a feature extraction step; with the WBA including whole bone segmentation, cortical segmentation, spine segmentation, and centrum segmentation.
Type:
Grant
Filed:
June 13, 1996
Date of Patent:
February 1, 2000
Assignee:
Eli Lilly and Company
Inventors:
Jeffrey Donald Helterbrand, Richard Earl Higgs, Jr., Philip Wayne Iversen
Abstract: The instant invention provides dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods for use in the treatment of bone loss or bone resorption.
Type:
Grant
Filed:
July 28, 1998
Date of Patent:
February 1, 2000
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
Abstract: The instant invention provides processes for preparing compounds of formula IV, V, and IX, having the structures provided hereinbelow: ##STR1## These compounds are useful intermediates in the further preparation of benzo[b] thiophenes.
Type:
Grant
Filed:
April 29, 1998
Date of Patent:
January 25, 2000
Assignee:
Eli Lilly and Company
Inventors:
Christopher Randall Schmid, Jerry Wayne Misner
Abstract: This invention describes a novel human glutamate receptors, designated mGluR2. This invention also encompasses nucleic acids encoding this receptor, or a fragment thereof, as well as methods employing this receptor and the nucleic acid compounds.
Type:
Grant
Filed:
November 14, 1994
Date of Patent:
January 25, 2000
Assignee:
Eli Lilly and Company
Inventors:
James Paul Burnett, Jr., Nancy Gail Mayne, Robert Leon Sharp, Yvonne Marie Snyder
Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.
Type:
Grant
Filed:
September 3, 1997
Date of Patent:
January 25, 2000
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
Abstract: This invention provides methods for the treatment or prevention of interstitial cystitis or urethral syndrome in a mammal which comprise administering to a mammal in need thereof an effective amount of a compound of formula (I), where R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, methyl, methoxy, chloro, and trifluoromethyl, with the proviso that no more than one of R.sup.1 and R.sup.2 can be hydrogen; and Y is (1), (2), (3), (4), (5), (6), N--R.sup.a, or CH--NR.sup.b R.sup.c, where R.sup.a, R.sup.b, and R.sup.c are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
August 25, 1998
Date of Patent:
January 25, 2000
Assignee:
Eli Lilly and Company
Inventors:
Smriti Iyengar, Mark A. Muhlhauser, Karl B. Thor
Abstract: This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
Type:
Grant
Filed:
November 7, 1997
Date of Patent:
January 18, 2000
Assignee:
Eli Lilly and Company
Inventors:
Gary Lowell Engel, Nagy Alphonse Farid, Margaret Mary Faul, Michael Robert Jirousek, Lori Ann Richardson, Leonard Larry Winneroski, Jr.
Abstract: The present application relates to a series of novel sulfonic acid metal cation salts of the formula ##STR1## which are useful intermediates to prepare antifolate 5-substituted pyrrolo[2,3-d]pyrimidines. The present invention also relates to a novel process for preparing the sulfonic acid metal cation salts and to a novel process for preparing aldehydes of the formula ##STR2## from the corresponding sulfonic acid metal cation salts.
Type:
Grant
Filed:
September 24, 1998
Date of Patent:
January 11, 2000
Assignee:
Eli Lilly and Company
Inventors:
Douglas Patton Kjell, Brian James Slattery, Charles Jackson Barnett
Abstract: This invention provides novel indenone derivatives, their pharmaceutical formulations and their use for the inhibition of leukocyte adherence to cells.
Type:
Grant
Filed:
May 1, 1998
Date of Patent:
January 11, 2000
Assignee:
Eli Lilly and Company
Inventors:
John Michael Morin, Jr., Michael Dean Kinnick, Robert Theodore Vasileff, William Thomas Jackson
Abstract: The present invention provides novel methods of lowering serum cholesterol and inhibiting smoother muscle cell proliferation, particularly restenosis, in humans, and inhibiting uterine fibroid disease and endometriosis in women comprising administering to a human/woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, or trifluoromethyl;R.sup.1 and R.sup.2 each are the same or different C.sub.1 -C.sub.6 alkyl group;n is an integer from 2 to 6; andR.sup.3 and R.sup.4 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form a substituent selected from the group consisting of pyrrolidino, morpholino, piperidino, piperazino, 4-(C.sub.1 -C.sub.6 alkyl)piperazino, and 4-phenyl-piperazino; or a pharmaceutically acceptable salt thereof.
Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.
Type:
Grant
Filed:
July 24, 1998
Date of Patent:
December 28, 1999
Assignee:
Eli Lilly And Company and Limited
Inventors:
Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper