Abstract: This invention relates to a novel solid phase process for the preparation of thiophene combinatorial libraries. These libraries have use for drug discovery and are used to form wellplate components of novel assay kits.
Abstract: The present invention is in the field of human medicine, particularly in the treatment of Non-insulin Dependent Diabetes Mellitus (NIDDM) and other insulin resistant states such as those associated with obesity and aging. The invention provides a method of treating insulin resistant mammals, which comprises administering to a mammal in need thereof a growth hormone releasing agent.
Type:
Grant
Filed:
September 5, 1996
Date of Patent:
August 17, 1999
Assignee:
Eli Lilly and Company
Inventors:
Carol Lynn Broderick, Richard Dennis DiMarchi, Mark Louis Heiman, Lawrence Edward Stramm
Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.
Type:
Grant
Filed:
June 25, 1997
Date of Patent:
August 17, 1999
Assignee:
Eli Lilly and Company
Inventors:
Michael Gregory Bell, Thomas Alan Crowell, Christine Ann Droste, Donald Paul Matthews, John Hampton McDonald, III, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
Abstract: A multi-use pen-shaped medication dispensing device made of a plastic material that is recyclable after the contents of the medication cartridge have been exhausted. The device is made of a minimal number of parts, which include a housing, a dial assembly, a generally cylindrical button assembly located within the proximal end of the dial assembly, an internally threaded nut, and an externally threaded leadscrew. The device is arranged so that the dial must be rotated to the zero dose position prior to setting a dose. The device includes a lockout mechanism that prevents the dial from being depressed during dosing. The device further includes a mechanism that limits the maximum dosage that can be dialed up and a mechanism that prevents the user from dialing up a dosage greater than that remaining in the cartridge.
Type:
Grant
Filed:
January 23, 1998
Date of Patent:
August 17, 1999
Assignee:
Eli Lilly and Company
Inventors:
Andrew Burroughs, Dave Hixson, Andrew Hodge
Abstract: This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics, the improvement residing in employing pyridine.borane as reducing agent.
Abstract: A process for preparing two connected powder transfer conduits for cleaning without releasing powder from the conduits. The conduits are connected to each other by flexible tube of a water-dissolvable material to enable powder communication between the two conduits. A sealing operation is performed to form a seal in the tube sufficient to prevent the powder communication from one side of the seal to the other. The seal is then severed to produce two tube sections where each tube section is sealed at the point of severance. A cleaning conduit is then place over at least one of the two tube sections and connected to the respective conduit. The cleaning conduit is connected to a liquid cleaning source which is adapted to deliver a cleaning liquid capable of dissolving the tube section thereunder upon contact therewith.
Abstract: The invention provides substituted-2-amino-1,2,3,4-tetrahydrodibenzofurans and 2-aminocyclohepta?b!benzo-furans useful as 5-HT.sub.1F agonists.
Type:
Grant
Filed:
June 3, 1998
Date of Patent:
August 10, 1999
Assignee:
Eli Lilly and Company
Inventors:
Michael E. Flaugh, Anton D. Kiefer, Jr.
Abstract: The present invention is based of the discovery of two modified forms of human platelet factor-4, herein named MPF-4 and CPF-4, which were isolated from serum free culture medium of lipopolysaccharide-stimulated peripheral blood leukocytes. Amino acid sequence determination revealed that MPF-4 shares homology with platelet factor-4 beginning at N-terminal residue 17. CPF-4 consists of MPF-4 disulfide bonded to the 16 N-terminal residues of platelet factor-4. Both MPF-4 and CPF-4 are potent inhibitors of endothelial cell proliferation, approximately 10-100 fold more potent than native or recombinant platelet factor-4, making them useful in the treatment of angiogenic diseases.
Abstract: The present invention is directed to deacyl teicoplanin, and to a process for preparing deacyl teicoplanin by reacting teicoplanin with ECB deacylase. Deacyl teicoplanin can be alkylated to produce compounds useful for their antibacterial activity.
Type:
Grant
Filed:
April 1, 1998
Date of Patent:
August 10, 1999
Assignee:
Eli Lilly and Company
Inventors:
Barbara Shreve Briggs, Robin David Grey Cooper, Adam Joseph Kreuzman, Milton Joseph Zmijewski, Jr.
Abstract: The present invention is directed to novel halo-substituted bis-indolemaleimide compounds of the formula: ##STR1## The invention further provides a method of preparing the disclosed compounds and the preparation of pharmaceutical formulation for use in inhibiting Protein Kinase C in mammals.
Type:
Grant
Filed:
April 30, 1997
Date of Patent:
August 10, 1999
Assignees:
Eli Lilly and Company, Mississippi State University
Inventors:
Michael R. Jirousek, Peter G. Goekjian, Guo-Zhang Wu
Abstract: The invention provides isolated nucleic acid compounds encoding a glycosyltransferase enzyme of Amycolatopsis orientalis. Also provided are vectors carrying genes that encode the enzyme, transformed heterologous host cells for expressing the enzyme, and methods for producing glycopeptide compounds using the cloned genes that encode the enzyme.
Type:
Grant
Filed:
July 21, 1998
Date of Patent:
August 3, 1999
Assignee:
Eli Lilly and Company
Inventors:
Richard H. Baltz, Patricia J. Solenberg, Patti J. Treadway
Abstract: The invention provides substituted-2-amino-1,2,3,4-tetrahydrodibenzofurans and 2-aminocyclohepta?b!benzo-furans useful as 5-HT.sub.1F agonists.
Type:
Grant
Filed:
June 3, 1998
Date of Patent:
August 3, 1999
Assignee:
Eli Lilly and Company
Inventors:
Michael E. Flaugh, Anton D. Kiefer, Jr.
Abstract: Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --;R" and R'" are independently methyl or hydrogen;R and R.sup.Y are independently hydroxy or hydrogen;R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy;R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy;R.sub.2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R=H) forms of the compounds.
Type:
Grant
Filed:
June 12, 1997
Date of Patent:
August 3, 1999
Assignee:
Eli Lilly and Company
Inventors:
Frederick J. Burkhardt, Manuel Debono, Jeffrey S. Nissen, William W. Turner, Jr.
Abstract: The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl;R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl), or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogenR.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ;R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.
Type:
Grant
Filed:
October 3, 1997
Date of Patent:
July 27, 1999
Assignee:
Eli Lilly and Company
Inventors:
George Joseph Cullinan, Raymond Francis Kauffman
Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
July 27, 1999
Assignee:
Eli Lilly and Company
Inventors:
Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
Abstract: A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3,R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form an alkylene link of formula --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group,R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino,the dotted line represents an optional double bond, andthe fluorine atom is attached at the 6 or 7-position;and salts and esters thereof.
Abstract: The invention provides isolated nucleic acid compounds encoding a multiple drug resistance protein of Aspergillus nidulans. Vectors and transformed host cells comprising the multiple drug resistance-encoding DNA of Aspergillus nidulans atrD are also provided. The invention further provides assays which utilize these transformed host cells.
Type:
Grant
Filed:
December 23, 1997
Date of Patent:
July 27, 1999
Assignee:
Eli Lilly and Company
Inventors:
Paul Luther Skatrud, Maarten A. de Waard, Alan C. Andrade, Robert Brown Peery
Abstract: The present invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; having activity as a selective estrogen receptor modulator, pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for treating conditions resulting from estrogen deprivation or the inappropriately high presence of estrogen. Also provided are methods and chemical intermediates for the production of a compound of formula I above.
Type:
Grant
Filed:
September 12, 1997
Date of Patent:
July 27, 1999
Assignee:
Eli Lilly and Company
Inventors:
Kenneth Lee Hauser, Alan David Palkowitz
Abstract: The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
Type:
Grant
Filed:
September 23, 1997
Date of Patent:
July 20, 1999
Assignee:
Eli Lilly and Company
Inventors:
David R. Helton, James A. Monn, Darryle D. Schoepp, Joseph P. Tizzano