Patents Represented by Attorney, Agent or Law Firm Arlene K. Musser
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Patent number: 6060484Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Stephen W. Kaldor, Jeffrey A. Kyle, John E. Munroe
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Patent number: 6037447Abstract: The present invention is directed to certain glycopeptide dimers in which two glycopeptide units are covalently linked to one another through their disaccharide amine, via a linking radical. This invention is also directed to the monomeric intermediates. All of these compounds are useful as antibacterials, especially for the control of gram positive bacteria; the compounds are particularly useful for the control of resistant bacterial strains, such as vancomycin-resistant-enterococci ("VRE").Type: GrantFiled: August 31, 1998Date of Patent: March 14, 2000Assignee: Eli Lilly and CompanyInventors: Douglas R Stack, Richard C Thompson
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Patent number: 6001810Abstract: The present invention provides antiretroviral methods using the compounds of formula (I)X-X1-P1-Val-Z-Leu-P2-Ywherein:Z is Statine or ACHPA;and when Z is Statine,X is H-Pro-paF, H-Pro-His, Ac-Tyr, Ac-NA, Ac-Trp, Ac-YOM, Ac-Phe, Ac-paF, H-His, Ac-His or Ac-Gly-Tyr-YOM,X1 is Pro Ser or Ac,P1 is Phe, paF or YOM,P2 is Phe or Leu, andY is NH.sub.2, paF--NH.sub.2, His--NH.sub.2, Phe--NH.sub.2 or Tyr-Lue--NH.sub.2,provided that when X1 is Ac then there is no X residue;and when Z is ACHPA,X is H-Pro-His, H-Pro-paF, Ac-paF or Ac-His,P1 is Phe,P2 is Phe, andY is paF--NH.sub.2 and His--NH.sub.2.The invention further provides methods for determining the retroviral protease inhibitory activity of compounds using viral polypeptides made using recombinant DNA techniques.Type: GrantFiled: August 31, 1990Date of Patent: December 14, 1999Assignee: Eli Lilly and CompanyInventors: Kwan Yuk Hui, Mei-Huei T. Lai
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Patent number: 5998581Abstract: This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics. The improvement residing in providing a source of copper which results in the initial production of a copper complex of the glycopeptide antibiotic. Reductive alkylation of this complex favors regioselective alkylation and increased yields. Copper complexes of the glycopeptide antibiotic starting materials and of the alkylated products are also part of the invention.Type: GrantFiled: April 12, 1999Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventors: Richard Alan Berglund, Nancy Anne Lockwood, Howard Eugene Magadanz, Hua Zheng
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Patent number: 5994297Abstract: The present invention is directed to methods for treating infections caused by Staphylococcus aureus with reduced glycopeptide sensitivity. The invention is preferably practiced with strains of Staphylococcus aureus which are methicillin resistant, such as the Mu5O strain.Type: GrantFiled: July 15, 1998Date of Patent: November 30, 1999Assignee: Eli Lilly and CompanyInventors: Thalia Ioanna Nicas, David Albert Preston, Michael Lee Zeckel
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Patent number: 5977062Abstract: The present invention provides glycopeptide antibiotic derivative compounds. These derivative compounds possess antibacterial activity against a wide variety of bacteria, including activity against vancomycin-resistant isolates. Methods of making and using these glycopeptide antibiotic derivative compounds are also provided.Type: GrantFiled: April 17, 1998Date of Patent: November 2, 1999Assignee: Eli Lilly and CompanyInventors: Robin D. G. Cooper, Bret E. Huff, Thalia I. Nicas, John T. Quatroche, Michael J. Rodriguez, Nancy J. Snyder, Michael A. Staszak, Richard C. Thompson, Stephen C. Wilkie, Mark J. Zweifel
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Patent number: 5977063Abstract: The present invention is directed to N.sup.1 -alkylated derivatives of desleucyl A82846B. These derivatives are useful as antibacterials and also as starting materials from which further antibacterial compounds are prepared.Type: GrantFiled: April 30, 1998Date of Patent: November 2, 1999Assignee: Eli Lilly and CompanyInventors: Richard Craig Thompson, Stephen Charles Wilkie
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Patent number: 5965525Abstract: 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: GrantFiled: May 24, 1995Date of Patent: October 12, 1999Assignee: Eli Lilly and CompanyInventors: Frederick J. Burkhardt, Manuel Debono, Jeffrey S. Nissen, William W. Turner, Jr.
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Patent number: 5952310Abstract: The present invention is directed to glycopeptides and more particularly to derivatives of the glycopeptide A82846B. In these derivatives, the leucyl has been removed to create "hexapeptides" of A82846B and its N.sup.DISACC variations. These hexapeptides are useful as antibacterials and also as starting materials from which further antibacterial compounds are prepared.Type: GrantFiled: April 30, 1998Date of Patent: September 14, 1999Assignee: Eli Lilly and CompanyInventors: Richard Craig Thompson, Stephen Charles Wilkie
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Patent number: 5952466Abstract: This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics. The improvement residing in providing a source of copper which results in the initial production of a copper complex of the glycopeptide antibiotic. Reductive alkylation of this complex favors regioselective alkylation and increased yields. Copper complexes of the glycopeptide antibiotic starting materials and of the alkylated products are also part of the invention.Type: GrantFiled: November 12, 1997Date of Patent: September 14, 1999Assignee: Eli Lilly and CompanyInventors: Richard Alan Berglund, Nancy Anne Lockwood, Howard Eugene Magadanz, Hua Zheng
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Patent number: 5939382Abstract: This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics, the improvement residing in employing pyridine.borane as reducing agent.Type: GrantFiled: November 12, 1997Date of Patent: August 17, 1999Assignee: Eli Lilly and CompanyInventors: Richard Alan Berglund, Hua Zheng
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Patent number: 5932543Abstract: 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: GrantFiled: June 12, 1997Date of Patent: August 3, 1999Assignee: Eli Lilly and CompanyInventors: Frederick J. Burkhardt, Manuel Debono, Jeffrey S. Nissen, William W. Turner, Jr.
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Patent number: 5919756Abstract: The present invention is directed to amides of antibiotic A82846B (also known as chloroorienticin A), and of N.sup.4 -derivatives of A82846B. The present amide compounds are useful as antibacterials, especially for the control of gram positive bacteria; the compounds are particularly useful for the control of resistant bacterial strains, such as vancomycin-resistant-enterococci ("VRE").Type: GrantFiled: May 1, 1997Date of Patent: July 6, 1999Assignee: Eli Lilly and CompanyInventors: Robin David Grey Cooper, Michael John Rodriguez, Nancy June Snyder, Mark James Zweifel
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Patent number: 5916873Abstract: The present invention is directed to teicoplanin derivatives of the following general formula, wherein R.sup.1 and R.sup.2 are as defined in the specification. ##STR1## These derivatives are useful as antibiotics for the control of gram-positive bacteria.Type: GrantFiled: April 1, 1998Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Robin David Grey Cooper, Nancy June Snyder
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Patent number: 5910395Abstract: A photosensitive composition is prepared containing a polymer of the formula B(X)(Y) wherein B represents an organic backbone, each X independently is an acidic group or salt thereof and each Y independently is a photocurable group and a photoinitating compound or compounds. Preferably, free-radically polymerizable multi-functional monomer and/or oligomer is added to the photosensitive composition. The photosensitive composition can be coated on a suitable substrate for planographic printing plate applications. Imagewise irradiation causes the light struck regions to photocure, becoming insoluble in aqueous and organic mediums, while the non-light struck regions remain highly soluble/dispersable. Printing plates of this construction do not require processing prior to being run on a press.Type: GrantFiled: March 4, 1997Date of Patent: June 8, 1999Assignee: Minnesota Mining and Manufacturing CompanyInventors: Minyu Li, James P. Gardner, John E. Kluge, Sumita B. Mitra
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Patent number: 5891874Abstract: A series of benzimidazole compounds having the following general structure are provided which inhibit the growth of picornaviruses (e.g., rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus) and flaviviruses (e.g., hepatitis C and bovine diarrheal virus). ##STR1## A method for inhibiting picornaviruses and flaviviruses is also provided which includes administering to a host an effective amount of the inventive benzimidazole compounds.Type: GrantFiled: June 4, 1997Date of Patent: April 6, 1999Assignee: Eli Lilly and CompanyInventors: Joseph Matthew Colacino, Beverly Ann Heinz, Louis Nickolaus Jungheim, Shawn Christopher Miller, Wayne Alfred Spitzer, Joseph Chiou-chung Tang, Mark Joseph Tebbe, Frantz Victor
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Patent number: 5861141Abstract: Pharmaceutical formulations of cefaclor, suitable for the direct-compression manufacture of dispersible tablets, containing the antibiotic cefaclor in an amount between 35% and 50% by weight of the total weight of the formulation, along with suitable excipients and coadjuvants selected from disintegrators, diluents, lubricants, antiadherents, sweeteners, fragrances and, optionally, flavorings, opacifiers and colorants. Said formulations are suitable for the manufacture of dispersible tablets which disintegrate in less than three minutes in water at 19.degree.-21.degree. C., and are suitable for the treatment of infections caused by bacteria strains sensitive to cefaclor.Type: GrantFiled: October 13, 1995Date of Patent: January 19, 1999Assignee: Lilly S.A.Inventor: Flavia Arce Mendizabal
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Patent number: 5773170Abstract: An image-forming element comprising a substrate, and an image-forming medium comprising (a) a compound absorbing at a first wavelength in the UV/blue region and (b) a dye absorbing at a second wavelength which is longer than the first wavelength, irradiation at said second wavelength bleaching absorption of said compound at said first wavelength, said element being free of thermally unstable urea and/or carbamate molecules.Type: GrantFiled: April 2, 1996Date of Patent: June 30, 1998Assignee: Minnesota Mining and Manufacturing Co.Inventors: Ranjan C. Patel, Robert J. D. Nairne
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Patent number: 5773207Abstract: Tabular gain silver halide emulsions prepared in the presence of a block copolymer selected from the group consisting of:A--B, A--(B--A).sub.m, B--(A--B).sub.m, (A--B).sub.p --X, (B--A).sub.p --X, ?A--(B--A).sub.m !.sub.p --X, and ?B--(A--B).sub.m !.sub.p --Xwhere m is an integer of 1 or more, p is an integer of 3 or more, X represents a p-valent linking group, A represents a poly(tetrahydrofuran) block, and B represents a poly(ethylene oxide) block.Type: GrantFiled: December 16, 1996Date of Patent: June 30, 1998Assignee: Imation Corp.Inventors: Richard A. Barcock, Rachel J. Hobson
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Patent number: 5770354Abstract: Silver halide photographic element comprising a support having coated thereon red-, green- and blue-sensitive silver halide emulsion layers comprising, respectively, cyan, magenta and yellow dye-forming couplers, wherein the blue-sensitive emulsion layer comprises at least two blue-sensitive emulsion layers, the uppermost of which has the highest-sensitivity and the lowermost of which has the lowest sensitivity, characterized in that the uppermost highest sensitivity blue-sensitive silver halide emulsion layer comprises a yellow dye-forming coupler and a cyan dye-forming coupler.Type: GrantFiled: April 25, 1996Date of Patent: June 23, 1998Assignee: Imation Corp.Inventors: Sergio Massirio, Raffaella Biavasco, Flavio Costa