Abstract: Processes for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.
Abstract: A stereoselective process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates by contacting a lactol with an amine base in an inert solvent, adjusting the temperature and adding a sulfonating reagent.
Abstract: A stereoselective fusion glycosylation process for prearing beta-anomer enriched 2'-deoxy-2',2'-difluoronucleotides and 2'-deoxy-2'-fluoronucleosides by reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorcarbohydrate with at least a 3 molar equivalent of a nucleobase derivative at a temperature sufficient to melt the carbohydrate and nucleobase derivative.
Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
Type:
Grant
Filed:
April 26, 1993
Date of Patent:
November 15, 1994
Assignee:
Eli Lilly and Company
Inventors:
Marlene L. Cohen, William B. Lacefield, David W. Robertson
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:
September 17, 1991
Date of Patent:
May 17, 1994
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: Targeted drug conjugates which enable a large number of molecules of drug to be directed to a cell by a single molecule of antibody are provided. The invention also provides intermediates for the synthesis of such conjugates and cytotoxic drugs modified in accordance with the cluster concept of the invention.
Type:
Grant
Filed:
July 1, 1991
Date of Patent:
December 21, 1993
Assignee:
Eli Lilly and Company
Inventors:
Gary A. Koppel, Robin E. Offord, Keith Rose, William L. Scott
Abstract: This compound provides the compound (-)-N"-cyano-N-3-pyridyl-N'-1,2,2-trimethylpropylguanidine, its salts and pharmaceutical formulations, and its method of use for opening potassium channels in mammals.
Type:
Grant
Filed:
October 29, 1992
Date of Patent:
November 23, 1993
Assignee:
Eli Lilly and Company
Inventors:
David W. Robertson, Mitchell I. Steinberg
Abstract: The present invention provides (S)-norfluoxetine and pharmaceutically acceptable salts thereof capable of inhibiting the uptake of serotonin.
Type:
Grant
Filed:
April 21, 1992
Date of Patent:
October 5, 1993
Assignee:
Eli Lilly and Company
Inventors:
Ray W. Fuller, David Mitchell, David W. Robertson, Gregory A. Stephenson, David T. Wong
Abstract: This invention provides new stabilized methylene Meldrum's acid precursors, a process for their preparation, and a process for using such compounds in the preparation of methylene Meldrum's acid.
Abstract: The present invention provides 3-(4-substitutedphenoxy)-3-phenyl propanamines capable of inhibiting the uptake of serotonin. These compounds are useful for treating many pharmacological disorders, including depression and obesity. These compounds can also be used to reduce the desire to smoke and consume alcohol.
Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: The present invention comprises an .about.0.8 kb Sac II restriction fragment of phage FP43, which confers the pin phenotype. The present invention allows transduction at high m.o.i. using the phage FP43 high frequency transduction system.
Type:
Grant
Filed:
January 19, 1990
Date of Patent:
March 30, 1993
Assignee:
Eli Lilly and Company
Inventors:
Margaret M. Ballou, Richard H. Baltz, Margaret A. McHenney
Abstract: Novel fusion reporter genes, fusion reporter proteins, and an improved reporter system for measuring the relative activity of a promoter sequence. A luxAB fusion gene of the present invention is particularly useful as a reporter gene and is derived from the fusion of a luxA gene and a luxB gene from Vibrio harveyi. The gene products of the luxA and luxB genes are the .alpha.- and .beta.-subunits, respectively, of a bacterial luciferase. A fusion protein encoded by a luxAB fusion gene is a single active protein and is particularly useful as a reporter protein having luciferase activity. An advantage of such a reporter system to assay gene expression in many cells which contain FMNH.sub.2, such as bacterial and yeast cells, is that an immediate and quantitative assessment of gene expression may be made from real-time light measurements using intact cells.
Type:
Grant
Filed:
January 6, 1989
Date of Patent:
March 23, 1993
Assignee:
Eli Lilly and Company
Inventors:
Gary D. Gustafson, Thomas D. Ingolia, Gretchen Kirchner, Jean L. Roberts
Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.