Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.
Type:
Grant
Filed:
November 15, 2005
Date of Patent:
October 6, 2009
Assignee:
Eli Lilly and Company
Inventors:
Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
Abstract: Disclosed is a method of preparing a GLP-1 compound that is soluble in aqueous solution at pH 7.4 from a GLP-1 compound that is substantially insoluble in aqueous solution at pH 7.4. The insoluble GLP-1 compound is dissolved in aqueous base or in aqueous acid to form a GLP-1 solution. The GLP-1 solution is then neutralized to a pH at which substantially no amino acid racemization of the GLP-1 compounds occurs, after which the soluble GLP-1 compound is isolated from the neutralized solution.
Type:
Grant
Filed:
January 16, 2001
Date of Patent:
October 6, 2009
Assignee:
Eli Lilly and Company
Inventors:
Walter Francis Prouty, Jr., Joseph Vincent Rinella, Jr.
Abstract: The present invention relates to novel, non-secosteroidal, hydroxyl substituted, carbon-linked diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
Type:
Grant
Filed:
November 16, 2004
Date of Patent:
September 29, 2009
Assignee:
Eli Lilly and Company
Inventors:
Emilio Enrique Bunel, Robert Peter Gajewski, Charles David Jones, Jianliang Lu, Sunil Nagpal, Tianwei Ma, Ying Kwong Yee
Abstract: A novel class of benzisothiazole-3(2H)-one compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases.
Type:
Grant
Filed:
March 25, 2004
Date of Patent:
September 29, 2009
Assignee:
Eli Lilly and Company
Inventors:
Patrick Irving Eacho, Patricia Sue Foxworthy-Mason, Ho-Shen Lin, Jose Eduardo Lopez, Marian Kazimierz Mosior, Michael Enrico Richett
Abstract: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
Type:
Grant
Filed:
August 17, 2007
Date of Patent:
September 29, 2009
Assignee:
Eli Lilly and Company
Inventors:
Jennifer Rebecca Allen, Albert Kudzovi Amegadzie, Kevin Matthew Gardinier, George Stuart Gregory, Stephen Andrew Hitchcock, Paul J. Hoogestraat, Winton Dennis Jones, Jr., Daryl Lynn Smith
Abstract: Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
Type:
Grant
Filed:
December 10, 2004
Date of Patent:
September 29, 2009
Assignee:
Eli Lilly and Company
Inventors:
Peter Thaddeus Gallagher, Carlos Lamas-Peteira, Francisco Javier Agejas-Chicharro
Abstract: The invention relates to an ionophore antibiotic composition capable of diluting with water to a substantially stable dispersed form in all water than present, said composition comprising or including:—at least one ionophore antibiotic (preferably monensin) of a mean particle size of less than 20 microns,—and at least one dispersing agent. A method of preparing the ionophore antibiotic composition is also disclosed.
Type:
Application
Filed:
May 18, 2009
Publication date:
September 24, 2009
Applicant:
ELI LILLY AND COMPANY
Inventors:
Kim Ewing Melville AGNEW, William Austin HEWITT, Craig Richard HANHAM, Kevin Grant PURDY
Abstract: A method to treat conditions characterized by formation of amyloid plaques both prophylactically and therapeutically is described. The method employs humanized antibodies which sequester soluble A? peptide from human biological fluids or which preferably specifically bind an epitope contained within position 13-28 of the amyloid beta peptide A?.
Type:
Application
Filed:
February 8, 2008
Publication date:
September 24, 2009
Applicant:
ELI LILLY CORPORATION
Inventors:
David M. Holtzman, Ronald DeMattos, Kelly R. Bales, Steven M. Paul, Naoya Tsurushita, Maximiliano Vasquez
Abstract: The present invention encompasses isolated antibodies, or antigen-binding portions thereof, that specifically bind to the p19 subunit of IL-23. These antibodies, or antigen-binding portions thereof, are high affinity, neutralizing antibodies useful for the treatment of autoimmune disease.
Type:
Application
Filed:
August 23, 2006
Publication date:
September 24, 2009
Applicant:
ELI LILLY AND COMPANY
Inventors:
Catherine Brautigam Beidler, Stuart Willis Bright, Craig Duane Dickinson, Kristine Kay Kikly, David Matthew Marquis, Alain Philippe Vasserot
Abstract: The invention provides a stable solution formulation comprising a GLP-1-Fc fusion at a pH between about pH 6 and about pH 8.5. analogs fused to specific IgG4-Fc derivatives. These formulations provide unexpected and considerably greater chemical stability than when compared to GLP-1 -Fc fusions at a pH outside the described ranges. The formulations comprising a GLP-1-Fc fusion are useful in treating diabetes, obesity, initable bowel syndrome and other conditions that would be benefited by lowering plasma glucose, inhibiting gastric and/or intestinal motility and inhibiting gastric and/or intestinal emptying, or inhibiting food intake.
Type:
Application
Filed:
December 15, 2005
Publication date:
September 17, 2009
Applicant:
Eli Lilly and Company
Inventors:
Wolfgang Glaesner, Rohn Lee Millican, JR.
Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia.
Type:
Grant
Filed:
August 1, 2008
Date of Patent:
September 8, 2009
Assignee:
Eli Lilly and Company
Inventors:
Bryan Hurst Norman, Lance Allen Pfeifer, Timothy Ivo Richardson
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
Type:
Grant
Filed:
April 9, 2008
Date of Patent:
September 8, 2009
Assignee:
Eli Lilly and Company
Inventors:
Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Scott Alan Jones, Timothy Alan Shepherd, Owen Brendan Wallace, Kin Chlu Fong, Conrad Wilson Hummel, George Sal Lewis
Abstract: The present invention provides methods of treating leukemia comprising administration of a resistance modulating amount of a compound having the formula (2r)-anti-5-{3-[4-(10,11-difluoromethano-dibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline 2.5 hydrochloride.
Type:
Grant
Filed:
May 24, 2007
Date of Patent:
September 1, 2009
Assignee:
Eli Lilly and Company
Inventors:
Julie Kay Bush, Susan Marie Reutzel-Edens
Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzothiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
Type:
Grant
Filed:
November 16, 2004
Date of Patent:
September 1, 2009
Assignee:
Eli Lilly and Company
Inventors:
Jianliang Lu, Tainwei Ma, Sunil Nagpal, Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee, Michael John Rupp
Abstract: The present invention relates to novel muteins of human fibroblast growth factor 21 with reduced capacity of O-glycosylation when expressed in yeast compared to wild-type human FGF-21. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the production of said muteins. Also disclosed are methods for treating type 2 diabetes, obesity, or metabolic syndrome.
Type:
Grant
Filed:
July 26, 2005
Date of Patent:
September 1, 2009
Assignee:
Eli Lilly and Company
Inventors:
Christopher Carl Frye, Lihua Huang, Radmila Micanovic
Abstract: The present invention provides kinase inhibitors of Formula I.
Type:
Grant
Filed:
January 25, 2005
Date of Patent:
September 1, 2009
Assignee:
Eli Lilly and Company
Inventors:
Rosanne Bonjouklian, Chafiq Hamdouchi, Chuan Shih, Alfonso De Dios, Miriam Filadelfa del Prado, Carlos Jaramillo Aguado, Pramila Kotiyan, Mary Margaret Mader, Sheila Pleite Selgas, Concepcion Sanchez-Martinez
Abstract: The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 23, 2006
Date of Patent:
September 1, 2009
Assignee:
Eli Lilly and Company
Inventors:
Alfonso De Dios, Cristina Garcia-Paredes, Beatriz López de Uralde Garmendia, Mary Margaret Mader, Mark Andrew Pobanz, Chuan Shih, Boyu Zhong
Abstract: The present invention provides a pro-inflammatory synthetic polysaccharide antigen (SPA), or a pharmaceutically acceptable salt thereof, comprising a TLR2-targeting synthetic peptidoglycan (PGN) moiety onto which a first epitope and a second epitope are each covalently attached. The first epitope comprises one or more than one generic T helper peptide sequence, and the second epitope comprises one or more than one target epitope. The first and second epitopes are present in one or more copies each within the SPA. Each target epitope is a peptide sequence or a carbohydrate moiety, and is an immunogen to CD8+ T cells or B cells. The present invention also provides a suppressive synthetic polysaccharide antigen (SPA), or a pharmaceutically acceptable salt thereof, comprising a TLR2-targeting synthetic peptidoglycan (PGN) moiety onto which one or more than one target epitope is covalently attached.