Abstract: A process to make .alpha.,.alpha.-difluoro-.beta.-hydroxy thiol esters of formula (IIIA) ##STR1## comprising reacting a difluoroethanethioate of formula (IVA) ##STR2## with a second reactant selected from the group consisting of aldehydes, ketones, acid halides and esters; in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound. These thiol esters are useful as intermediates in organic syntheses of pharmaceutical products.
Abstract: A stereoselective anion glycosylation process for preparing beta- and alpha-anomer enriched 2', 2'-difluoro-2'-deoxynucleosides and 2'-deoxy-2'-fluoronucleosides by reacting an alpha- or beta-anomer enriched 2-deoxy-2-fluorocarbohydrate or 2-deoxy-2,2-difluorocarbohydrate with at least a molar equivalent of a salt of a nucleobase derivative in an inert solvent.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
April 28, 1998
Assignee:
Eli Lilly and Company
Inventors:
Ta-Sen Chou, Cora S. Grossman, Larry Wayne Hertel, Richard E. Holmes, Charles D. Jones, Thomas E. Mabry
Abstract: This invention relates to hexa- and octahydrobenzo?f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
December 2, 1997
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
Abstract: This invention relates to hexa- and octaahydrobenzo?f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
Type:
Grant
Filed:
April 17, 1996
Date of Patent:
September 23, 1997
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Kenneth S. Hirsch, Charles D. Jones, David E. Lawhorn, Loretta A. McQuaid, Leland O. Weigel
Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in preventing the development of prostatic cancer, or preventing or treating the metastasis to bone of prostatic cancer.
Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in preventing the development of prostatic cancer, or preventing or treating the metastasis to bone of prostatic cancer.
Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.
Type:
Grant
Filed:
May 11, 1995
Date of Patent:
April 22, 1997
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.
Type:
Grant
Filed:
May 11, 1995
Date of Patent:
April 22, 1997
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
April 20, 1993
Date of Patent:
March 18, 1997
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase and their preparation is disclosed.
Type:
Grant
Filed:
September 20, 1994
Date of Patent:
November 26, 1996
Assignee:
Eli Lilly and Company
Inventors:
Kevin L. Haehl, Thomas J. Kress, James P. Wepsiec
Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
January 19, 1994
Date of Patent:
November 5, 1996
Assignee:
Eli Lilly and Company
Inventors:
Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
October 29, 1996
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
October 8, 1996
Assignee:
Eli Lilly and Company
Inventors:
Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
September 17, 1996
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghaven Vasudevan, Celia A. Whitesitt
Abstract: This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
July 30, 1996
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Kenneth S. Hirsch, Charles D. Jones, David E. Lawhorn, Loretta A. McQuaid, Leland O. Weigel