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 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 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.
Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzofuran 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:
August 25, 2009
Assignee:
Eli Lilly and Company
Inventors:
Jianliang Lu, Tianwei Ma, Sunil Nagpal, Quanrong Shen, Alan M. Warshawsky, Jason Matthew Ochoada, Ying Kwong Yee
Abstract: The invention provides specific FGF-21 compounds fused to specific IgG4-Fc or HSA derivatives resulting in fusion proteins that are biologically active with an extended elimination half-life and a slower clearance. These FGF-21 compound fusion proteins and compositions are useful in treating type 2 diabetes, obesity, and metabolic syndrome.
Type:
Grant
Filed:
May 2, 2005
Date of Patent:
August 18, 2009
Assignee:
Eli Lilly and Company
Inventors:
Wolfgang Glaesner, Rohn Lee Millican, Jr., Yu Tian, Sheng-Hung Rainbow Tschang
Abstract: The present invention is concerned with certain novel spiro substituted heterocylic ring derivatives. These compounds may be useful in the manufacture of pharmaceutical compositions for treating disorders mediated by lipoxygenases. They may also be useful in the manufacture of pharmaceutical formulations for the treatment of lipoxygenase-mediated disorders.
Type:
Grant
Filed:
December 9, 2005
Date of Patent:
August 18, 2009
Assignee:
Eli Lilly and Company
Inventors:
Daniel T. W. Chu, Jian Chen, Wei Zhang, Xianfeng Li, Jiangao Song, Bing Wang, Qiang Cong, Donald R. James
Abstract: The present invention relates to novel, non-secosteroidal, 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.
Abstract: Compound 5-(2-Methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof, useful for the treatment of irritable bowel syndrome.
Type:
Grant
Filed:
March 21, 2008
Date of Patent:
July 14, 2009
Assignee:
Eli Lilly and Company
Inventors:
Charles Howard Mitch, Michael Angelo Statnick
Abstract: A method for producing one or more pseudomycins is described including cultures of Pseudomonas syringae that produce one or more pseudomycins having general formula (I) where R is a lipophilic moiety.
Type:
Grant
Filed:
May 12, 2005
Date of Patent:
July 7, 2009
Assignee:
Eli Lilly and Company
Inventors:
Matthew Dale Hilton, Robert Joseph Strobel, Jr., Penelope Jane Beverly Millar, Dennis Nelson Thomas, Andrew Richard Cockshott, Brian Gerald Getman, Jack Richard Eastridge, Cathleen Alice Cantwell
Abstract: The invention provides GLP-1 compounds coupled to at least one polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating diabetes, obesity, irritable 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:
Grant
Filed:
March 19, 2004
Date of Patent:
July 7, 2009
Assignee:
Eli Lilly and Company
Inventors:
Richard Dennis DiMarchi, Wolfgang Glaesner, Rohn Lee Millican, Jr., Andrew Mark Vick, Lianshan Zhang
Abstract: The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I) pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.
Type:
Grant
Filed:
April 3, 2006
Date of Patent:
July 7, 2009
Assignee:
Eli Lilly and Company
Inventors:
Elizabeth Aaron Collins, Pablo Garcia-Losada, Chafiq Hamdouchi, Philip Arthur Hipskind, Jianliang Lu, Takako Takakuwa
Abstract: A complex of an echinocandin compound with a carbohydrate is described having improved thermal stability and water solubility. A process for making the echinocandin/carbohydrate complex is also described as well as the use of the complex in pharmaceutical formulations and treatments of fungal infections.
Type:
Grant
Filed:
August 30, 2005
Date of Patent:
June 23, 2009
Assignee:
Eli Lilly and Company
Inventors:
Larry A. Larew, Nathaniel Milton, James Lawrence Sabatowski, Kenneth Philip Moder
Abstract: A stabilized pharmaceutical composition in the form of a solution for parenteral administration of a parathyroid hormone is described wherein the therapeutically active ingredient is stabilized with a buffer and a polyol. Preferred preparations contain in an aqueous solution human PTH(1-34), mannitol, an acetate or tartrate buffering agent and m-cresol or benzyl alcohol as a preservative.
Abstract: Thiazolidinedione (TZD) and its pharmacologically active derivatives can be used in combination with agonists of glucagon-like peptide-1 (GLP-1), to treat non-insulin dependent diabetes mellitus, optionally with other therapies, by improving glycemic control while minimizing side effects, such as heart hypertrophy and elevated fed-state plasma glucose, which are associated with both TZD and GLP-1 monotherapies. Thus, the co-administration of TZD and GLP-1 helps regulate glucose homeostasis in Type II diabetic patients.
Type:
Grant
Filed:
June 6, 2000
Date of Patent:
August 18, 2009
Assignee:
Eli Lilly and Company
Inventors:
Fatima Emitsel Yakubu-Madus, Lawrence Edward Stramm, Louis Vignati, William Terry Johnson