Patents Represented by Attorney, Agent or Law Firm Steven P. Caltrider
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Patent number: 5491242Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. The present invention also 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: March 15, 1995Date of Patent: February 13, 1996Assignee: Eli Lilly and CompanyInventors: James R. Gillig, Michael R. Jirousek
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Patent number: 5484780Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: December 14, 1994Date of Patent: January 16, 1996Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
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Patent number: 5481003Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. The present invention also 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: June 22, 1994Date of Patent: January 2, 1996Assignee: Eli Lilly and CompanyInventors: James R. Gillig, Michael R. Jirousek
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Patent number: 5474978Abstract: The present invention discloses a human insulin analog hexamer complex and formulations. More specifically, the present invention relates to various parenteral formulations, which comprise: human insulin analogs in a hexamer conformation, zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol. The formulation provides a rapid onset of action.Type: GrantFiled: June 16, 1994Date of Patent: December 12, 1995Assignee: Eli Lilly and CompanyInventors: Diane L. Bakaysa, David N. Brems, Bruce H. Frank, Henry A. Havel, Allen H. Pekar
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Patent number: 5461031Abstract: 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 16, 1994Date of Patent: October 24, 1995Assignee: Eli Lilly and CompanyInventor: Michael R. De Felippis
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Patent number: 5457066Abstract: This specification describes a process for converting a human insulin precursor to human insulin, which comprises treating such human insulin precursor with trypsin and carboxypeptidase B in an aqueous medium containing per mole of human insulin precursor from about 0.1 to about 10 moles of one or more metal ions of those metals having Atomic Numbers 21 to 34, 39 to 52, 57 to 84, and 89 to 92.Type: GrantFiled: May 11, 1992Date of Patent: October 10, 1995Assignee: Eli Lilly and CompanyInventors: Bruce H. Frank, Walker E. Prouty, Richard E. Heiney, Mark R. Walden
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Patent number: 5441947Abstract: Wortmannin and certain of its analogs are inhibitors of restinosis.Type: GrantFiled: August 25, 1993Date of Patent: August 15, 1995Assignee: Eli Lilly and CompanyInventors: Jeffrey A. Dodge, Masahiko Sato
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Patent number: 5434160Abstract: Pharmaceutical compound of the formula ##STR1## R.sup.1 is phenyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl and heteroaryl groups being optionally substituted, or R.sup.1 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.2 is nitrile, carboxy, --COOR.sup.4 where R.sup.4 is an ester group, --CONR.sup.5 R.sup.6 where R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-4 alkyl, or R.sup.7 SO.sub.2 -- where R.sup.7 is C.sub.1-4 alkyl or optionally substituted phenyl;R.sup.3 is --NR.sup.8 R.sup.9, --NHCOR.sup.8, --N(COR.sup.8).sub.2, --N.dbd.CHOR.sup.8 where R.sup.8 and R.sup.9 are each hydrogen or C.sub.1-4 alkyl, or --NHSO.sub.2 R.sup.10 where R.sup.10 is C.sub.1-4 alkyl or optionally substituted phenyl; or ##STR2## where X is C.sub.2-4 alkylene; and the group ##STR3## represents a pyridine ring fused to the benzopyran nucleus; and salts thereof.Type: GrantFiled: November 12, 1993Date of Patent: July 18, 1995Assignee: Lilly Industries LimitedInventors: Colin P. Dell, Andrew C. Williams
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Patent number: 5401851Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: April 20, 1993Date of Patent: March 28, 1995Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
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Patent number: 5397799Abstract: Crystalline 4-(di-n-propyl)amino-6-aminocarbonyl-1,3,4,5-tetrahydrobenz[cd]indole hippurate and its method of preparation and use are provided.Type: GrantFiled: May 19, 1993Date of Patent: March 14, 1995Assignee: Eli Lilly and CompanyInventors: Thomas J. Kress, David L. Varie
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Patent number: 5380866Abstract: This invention provides the substantially pure (R) enantiomer of a compound of the Formula II: ##STR1## The compounds of Formula II are useful in the preparation of the substantially pure (R) enantiomer of angiotensin II antagonists of Formula III: ##STR2## wherein R.sub.1, Ar, R.sub.2 and X are variables.Type: GrantFiled: March 15, 1994Date of Patent: January 10, 1995Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5378717Abstract: This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are variables.Type: GrantFiled: March 22, 1993Date of Patent: January 3, 1995Assignee: Eli Lilly and CompanyInventors: Michael Brunavs, Colin P. Dell, Peter T. Gallagher, William M. Owton, Colin W. Smith
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Patent number: 5378699Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which 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; and salts thereof.Type: GrantFiled: February 5, 1993Date of Patent: January 3, 1995Assignees: Lilly Industries Limited, Eli Lilly and CompanyInventors: Michael Brunavs, Colin P. Dell, Peter T. Gallagher, William M. Owton, Jai P. Singh, Colin W. Smith
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Patent number: 5344937Abstract: This invention provides the substantially pure (R) enantiomer of a compound of the Formula II: ##STR1## The compounds of Formula II are useful in the preparation of the substantially pure (R) enantiomer of angiotensin II antagonists of Formula III: ##STR2## wherein R.sub.1, Ar, R.sub.2 and X are variables.Type: GrantFiled: April 20, 1993Date of Patent: September 6, 1994Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5314688Abstract: A method of inhibiting cell proliferation in mammals which comprises the local delivery of an inhibitory amount of dipyridamole. Inhibiting cell proliferation is useful for the treatment of proliferative diseases such as vascular restonesis, scleroderma, psoriasis, and rheumatoid arthritis. This method includes the local delivery of dipyridamole to the proliferative site by various techniques including local delivery catheters, site specific carriers, implants, direct injection, or direct application.Type: GrantFiled: February 9, 1993Date of Patent: May 24, 1994Assignee: Eli Lilly and CompanyInventors: Raymond F. Kauffman, Jai P. Singh
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Patent number: 5312936Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: September 17, 1991Date of Patent: May 17, 1994Assignee: Eli Lilly and CompanyInventors: Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
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Patent number: 5284868Abstract: A pharmaceutical compound of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 5, 6, 7, 8, 9 or 10, and each R.sup.1 is halo, trifluoromethyl, C.sub.1-4 alkoxy, hydroxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, trifluoromethoxy, carboxy, --COOR.sup.5 where R.sup.5 is an ester group, --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, --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl, or R.sup.11 SO.sub.2 -- where R.sup.11 is C.sub.1-4 alkyl or optionally substituted phenyl; and R.Type: GrantFiled: September 25, 1992Date of Patent: February 8, 1994Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Colin P. Dell, Jai P. Singh, Colin W. Smith
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Patent number: 5281619Abstract: This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables.Type: GrantFiled: March 22, 1993Date of Patent: January 25, 1994Assignee: Eli Lilly and CompanyInventors: Colin P. Dell, Colin W. Smith