Patents Represented by Attorney, Agent or Law Firm Steven P. Caltrider
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Patent number: 5811120Abstract: This invention provides solid orally administerable pharmaceutical formulations comprising raloxifene hydrochloride, a surfactant being sorbitan fatty acid ester or a polyoxyethylene sorbitan fatty acid ester, polyvinylpyrrolidone, and a water soluble diluent which is polyol or sugar.Type: GrantFiled: March 26, 1997Date of Patent: September 22, 1998Assignee: Eli Lilly and CompanyInventors: Lowell L. Gibson, Kerry J. Hartauer, Julian L. Stowers, Stephanie A. Sweetana, Arvind L. Thakkar
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Patent number: 5780461Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals. The compounds of the present invention can be used to treat cancer and inhibiting tumor growth in mammals.Type: GrantFiled: May 6, 1996Date of Patent: July 14, 1998Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5770397Abstract: The present invention is a method of using the BK enhancer in tandem with a eukaryotic promoter to promote transcription of DNA that encodes a useful substance. The method of the present invention requires the presence of the E1A gene product for maximum expression of the useful substance. The present invention also comprises a number of useful expression vectors that comprise the BK enhancer in tandem with the adenovirus 2 late promoter positioned to drive expression of a variety of proteins, such as protein C, chloramphenicol acetyltransferase, and tissue plasminogen activator. The present invention further comprises a method for increasing the activity of the BK enhancer involving placement of the BK enhancer immediately upstream of the eukaryotic promoter used in tandem with the BK enhancer to drive expression of a useful substance. Furthermore, the present invention also comprises a method for coamplification of genes in primate cells.Type: GrantFiled: June 2, 1995Date of Patent: June 23, 1998Assignee: Eli Lilly and CompanyInventor: Brian W. Grinnell
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Patent number: 5747642Abstract: The present invention discloses various parenteral pharmaceutical formulations, which comprise: a monomeric insulin analog, zinc, protamine, and phenolic derivative. The analog formulations provide a prolonged duration of action. A process for preparing insulin analog-protamine formulations is also described.Type: GrantFiled: June 1, 1995Date of Patent: May 5, 1998Assignee: Eli Lilly and CompanyInventor: Michael R. De Felippis
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Patent number: 5739322Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R1, R2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: March 20, 1997Date of Patent: April 14, 1998Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5721272Abstract: This invention provides compounds of the formula: ##STR1## The invention further provides the use of this compound to prepare N,N'-bridged bisindolylmaleimides. Furthermore, the invention provides pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: November 18, 1996Date of Patent: February 24, 1998Assignee: Eli Lilly and CompanyInventors: Margaret Mary Faul, Christine Ann Krumrich, Leonard Larry Winneroski, Jr.
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Patent number: 5719266Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.Type: GrantFiled: March 17, 1995Date of Patent: February 17, 1998Assignee: Eli Lilly and CompanyInventors: Richard D. DiMarchi, Ronald N. Hermeling, James A. Hoffmann
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Patent number: 5719175Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: May 6, 1996Date of Patent: February 17, 1998Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5710145Abstract: This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: ##STR1## and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: November 18, 1996Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Gary Lowell Engel, Nagy Alphonse Farid, Margaret Mary Faul, Michael Robert Jirousek, Lori Ann Richardson, Leonard Larry Winneroski, Jr.
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Patent number: 5700904Abstract: A method for recovering an acylated protein as a powder, especially in cases where said acylated protein is one that resists isolation by isoelectric precipitation from aqueous solutions of the protein, said method comprising in combination adjusting said aqueous solution to near the isoelectric pH of the protein and providing a suitable alcohol concentration to cause precipitation of the protein in the form of filterable particles at said pH.Type: GrantFiled: June 7, 1995Date of Patent: December 23, 1997Assignee: Eli Lilly and CompanyInventors: Jeffrey Clayton Baker, Brian A. Moser, Warren E. Shrader
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Patent number: 5698578Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: October 21, 1996Date of Patent: December 16, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5696108Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: May 6, 1996Date of Patent: December 9, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5693609Abstract: The present invention relates to the field of diabetes. More particularly, the invention relates to a monomeric insulin analog wherein the A chain is the naturally occurring sequence of the human insulin A chain and the B chain is modified at either position B28 and B29 or both. The analog is mono-acylated at the N-terminal of the A chain or B chain or at the lysine. The acylated insulin analogs have an extended duration of action.Type: GrantFiled: November 17, 1994Date of Patent: December 2, 1997Assignee: Eli Lilly and CompanyInventors: Jeffrey C. Baker, Jose M. Hanquier
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Patent number: 5691309Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.Type: GrantFiled: February 6, 1995Date of Patent: November 25, 1997Assignee: Eli Lilly and CompanyInventors: Margret B. Basinski, Richard D. DiMarchi, David B. Flora, William F. Heath, Jr., James A. Hoffmann, Brigitte E. Schoner, James E. Shields, David L. Smiley
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Patent number: 5674862Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: June 1, 1995Date of Patent: October 7, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5672618Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: May 25, 1995Date of Patent: September 30, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Michael Paal, Theo Schotten, Wolfgang Stenzel
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Patent number: 5668152Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: May 25, 1995Date of Patent: September 16, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Gerd Ruhter, Theo Schotten
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Patent number: 5665877Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.Type: GrantFiled: May 17, 1996Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
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Patent number: 5663375Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.Type: GrantFiled: August 22, 1994Date of Patent: September 2, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
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Patent number: 5661173Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: May 25, 1995Date of Patent: August 26, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III