Abstract: 6-Heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz?cd!indoles are provided which are useful in modifying the function of serotonin in mammals.
Type:
Grant
Filed:
June 20, 1994
Date of Patent:
July 21, 1998
Assignee:
Eli Lilly and Company
Inventors:
Richard N. Booher, Michael E. Flaugh, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.
Abstract: The present invention provides derivatives of tissue plasminogen activator that lack the Finger, Growth Factor and Kringle 1 domains and comprise a Kringle 2 domain that is monoglycosylated at a site other than that of t-PA. Using recombinant DNA techniques, an alternate glycosylation sequence is provided within the Kringle 2 domain of these t-PA derivatives. This alternate glycosylation consensus sequence, as well as the glycosylation consensus sequence within the Serine Protease domain, is glycosylated upon the expression and secretion of these molecules from eucaryotic host cells. Thus, a homogeneous population of diglycosylated t-PA derivatives that lack the Finger, Growth Factor and Kringle 1 domains is produced.
Abstract: Indazolecarboxamides are used as antagonists and partial agonists for the serotonin receptor 5-HT.sub.4 and provide therapeutic methods for treatment of disorders caused by or affected by dysfunction of the 5-HT.sub.4 receptor.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 5, 1997
Assignee:
Eli Lilly and Company
Inventors:
John T. Catlow, Michael J. Martinelli, John M. Schaus, Steven Swanson, Dennis C. Thompson
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 hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
May 6, 1997
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, David J. Hibschman, Joseph H. Krushinski, Jr., Thomas E. Mabry, Jeffrey S. Nissen, Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson, David T. Wong
Abstract: A stereoselective process for forming compounds related to 4-endotropanamine through the reactive amination of a corresponding ketone with a triacyloxy borohydride.
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: The invention provides compounds of the formula: ##STR1## wherein the variables are hereinbelow described; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.
Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 25, 1997
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson, David T. Wong
Abstract: A stereoselective glycosylation process for preparing beta- and alpha-anomer enriched 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides by reacting a concentrated alpha- or beta-anomer enriched 2 -deoxy-2,2-difluorocarbohydrate or 2-deoxy-2 -fluorocarbohydrate with at least a molar equivalent of a nucleobase derivative in a high boiling inert solvent.
Type:
Grant
Filed:
November 17, 1994
Date of Patent:
February 25, 1997
Assignee:
Eli Lilly and Company
Inventors:
Ta-Sen Chou, Laurie M. Poteet, Douglas P. Kjell
Abstract: This invention provides certain sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.
Type:
Grant
Filed:
November 21, 1994
Date of Patent:
January 14, 1997
Assignee:
Eli Lilly and Company
Inventors:
Richard W. Harper, J. Jeffry Howbert, Gerald A. Poore, Brent J. Rieder, Eddie V. P. Tao, James A. Aikins
Abstract: New N-alkyl and N-acyl derivatives of A82846A, A82846B, A82846C and PA-42867-A are provided. The new glycopeptide derivatives are useful for the treatment of susceptible bacterial infections, especially infections due to Gram-positive microorganisms.
Type:
Grant
Filed:
October 13, 1994
Date of Patent:
January 7, 1997
Assignee:
Eli Lilly and Company
Inventors:
Ramakrishnan Nagarajan, Amelia A. Schabel
Abstract: The disclosure relates to a new process for the synthesis of the macrolide antibiotic dirithromycin in crystalline form. The process is carried out in a single reaction vessel whereby an acetal dissolved in acetonitrile, in the presence of an acid catalyst, is hydrolyzed to the related hemiacetal which then reacts directly with erythromycylamine to form crystalline dirithromycin.
Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 19, 1996
Assignee:
Eli Lilly and Company
Inventors:
Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.
Type:
Grant
Filed:
August 22, 1995
Date of Patent:
November 5, 1996
Assignee:
Eli Lilly and Company
Inventors:
Craig S. Hoechstetter, Diane L. Huser, John M. Schaus, Robert D. Titus