Patents Represented by Attorney Arthur R. Whale
  • Patent number: 4495179
    Abstract: Antibiotic A51568 is produced by submerged, aerobic fermentation of new Nocardia orientalis NRRL 15232. The antibiotic is gram-positive.
    Type: Grant
    Filed: December 16, 1983
    Date of Patent: January 22, 1985
    Assignee: Eli Lilly and Company
    Inventors: Marvin M. Hoehn, Gary G. Marconi
  • Patent number: 4495195
    Abstract: Aryl pyrazole carboxylic acids and derivatives thereof, are xanthine oxidase inhibitors in vivo.
    Type: Grant
    Filed: November 1, 1982
    Date of Patent: January 22, 1985
    Assignee: Eli Lilly and Company
    Inventors: James R. Beck, Robert P. Gajewski, Ronald E. Hackler
  • Patent number: 4495202
    Abstract: This invention provides for certain novel terphenyl derivatives, their pharmaceutical formulations, and a method of treating pain, fever, thrombosis, inflammation, and arthritis.
    Type: Grant
    Filed: June 22, 1983
    Date of Patent: January 22, 1985
    Assignee: Eli Lilly and Company
    Inventors: Ken Matsumoto, John S. Ward
  • Patent number: 4493699
    Abstract: Long chain alkyl and alkenyl sulfonates, sulfates and sulfoalkyl alkanoate salts, administered intravaginally for contraception.
    Type: Grant
    Filed: April 8, 1982
    Date of Patent: January 15, 1985
    Assignee: Eli Lilly and Company
    Inventors: Ronald E. Zimmerman, Philip J. Burck, C. David Jones, Arvind L. Thakkar
  • Patent number: 4492704
    Abstract: This invention relates to a class of quinoline quinones, which are useful for the therapy of immediate hypersensitivity reactions, such as asthma, and in treating any condition characterized by excessive release of leukotrienes. This invention also includes a method for treating these conditions, which comprises administering to animals, including humans, an effective dose of the quinoline quinone compounds. A further part of this invention is pharmaceutical formulations containing these pharmacologically-active compounds.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: January 8, 1985
    Assignee: Eli Lilly and Company
    Inventors: Jerome H. Fleisch, Winston S. Marshall, George J. Cullinan
  • Patent number: 4492650
    Abstract: Antibiotic A54556, a complex of 8 individual factors, produced by submerged, aerobic fermentation of new Streptomyces hawaiiensis NRRL 15010. The complex and the individual, separated factors are active against Staphylococcus and Streptococcus which are penicillin resistant.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: January 8, 1985
    Assignee: Eli Lilly and Company
    Inventors: Karl H. Michel, Ralph E. Kastner
  • Patent number: 4492699
    Abstract: These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.
    Type: Grant
    Filed: October 13, 1983
    Date of Patent: January 8, 1985
    Assignee: Lilly Industries Limited
    Inventors: Jiban K. Chakrabarti, Terrence M. Hotten, David J. Steggles
  • Patent number: 4492694
    Abstract: 7-(3-Indolyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.
    Type: Grant
    Filed: April 12, 1983
    Date of Patent: January 8, 1985
    Assignee: Eli Lilly and Company
    Inventors: Larry C. Blaszczak, Jan R. Turner
  • Patent number: 4492708
    Abstract: Certain N-substituted benzimidazoles are disclosed. The compounds are potent antiviral agents. Pharmaceutical formulations containing such compounds and a method of treating viral infections are provided.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: January 8, 1985
    Assignee: Eli Lilly and Company
    Inventor: Wayne A. Spitzer
  • Patent number: 4490370
    Abstract: Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and are particularly useful as oral treatments for upper respiratory infections.
    Type: Grant
    Filed: April 12, 1983
    Date of Patent: December 25, 1984
    Assignee: Eli Lilly and Company
    Inventors: Robin D. G. Cooper, Larry C. Blaszczak, Jan R. Turner
  • Patent number: 4487923
    Abstract: An improved method of preparing 23-monoester derivatives of 5-O-mycaminosyl tylonolide (OMT) and demycinosyltylosin (DMT) is provided. This method comprises esterifying the antibiotic with an acylating agent in the presence of an external base, such as pyridine or 2,4,6-collidine, until acylation of the 23-hydroxyl group is substantially complete, and separating the 23-monoester derivative. 23-Monoester derivatives of OMT and DMT are useful antibiotics and/or intermediates to antibiotics.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: December 11, 1984
    Assignee: Eli Lilly and Company
    Inventors: Herbert A. Kirst, John E. Toth
  • Patent number: 4486432
    Abstract: This invention provides for novel quinoxalinedione derivatives, the use of quinoxalinedione derivatives in treating animals suffering from immediate hypersensitivity reactions and conditions characterized by excessive release of leukotrienes, and formulations of the quinoxalinedione derivatives.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: December 4, 1984
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, Jerome H. Fleisch, George J. Cullinan
  • Patent number: 4486591
    Abstract: Compounds are described of the formula ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, halogen, C.sub.1-4 haloalkyl, C.sub.1-4 alkanoyl, nitro, amino, C.sub.2-4 acylamino, cyano, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 haloalkoxy or a group of the formula -SO.sub.2 N(R.sup.8).sub.2, -SO.sub.2 R.sup.8 or -SO.sub.3 R.sup.8 where R.sup.8 is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R.sup.10 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl and where n is 0 or 1; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: December 4, 1984
    Assignee: Lilly Industries Limited
    Inventors: Jiban K. Chakrabarti, Terrence M. Hotten
  • Patent number: 4486584
    Abstract: 2'"-O-demethylmacrocin (DOMM) which has the formula: ##STR1## 20-dihydro-DOMM, 2'"-O-demethyllactenocin (DOML), 20-dihydro-DOML, specified acyl ester derivatives, and their acid addition salts are useful antibacterial agents.
    Type: Grant
    Filed: December 20, 1982
    Date of Patent: December 4, 1984
    Assignee: Eli Lilly and Company
    Inventors: Richard H. Baltz, Gene M. Wild, Eugene T. Seno
  • Patent number: 4486592
    Abstract: 9-Carbamoylfluorene derivatives are useful intermediates in a synthesis of 9-carbamoyl-9-(3-aminopropyl)fluorene antiarrhythmic agents.
    Type: Grant
    Filed: October 19, 1983
    Date of Patent: December 4, 1984
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Terry D. Lindstrom
  • Patent number: 4483986
    Abstract: A compound of the formula I ##STR1## and other compounds and process for preparing, which compounds are useful as intermediates.
    Type: Grant
    Filed: May 3, 1982
    Date of Patent: November 20, 1984
    Assignee: Eli Lilly and Company
    Inventor: Samuel J. Dominianni
  • Patent number: 4482487
    Abstract: A-21978C cyclic peptides of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, an amino-protecting group, 8-methyldecanoyl, 10-methylundecanoyl, 10-methyldodecanoyl, the specific C.sub.10 -alkanoyl group of A-21978C factor C.sub.0 and the specific C.sub.12 -alkanoyl groups of A-21978C factors C.sub.4 and C.sub.5 ; R.sup.1 and R.sup.2 are, independently, hydrogen or an amino-protecting group, and salts thereof, are prepared by enzymatic deacylation of an antibiotic selected from A-21978C complex, A-21978C factors C.sub.0, C.sub.1, C.sub.2, C.sub.3, C.sub.4 amd C.sub.5 and blocked A-21978C complex and factors C.sub.0, C.sub.1, C.sub.2, C.sub.3, C.sub.4 and C.sub.5, using an enzyme produced by the Actinoplanaceae, preferably by Actinoplanes utahensis. The A-21978C cyclic peptides and salts thereof are useful intermediates to prepare new semi-synthetic antibacterial agents.
    Type: Grant
    Filed: January 31, 1984
    Date of Patent: November 13, 1984
    Assignee: Eli Lilly and Company
    Inventors: Bernard J. Abbott, Manuel Debono, David S. Fukuda
  • Patent number: 4482484
    Abstract: Compounds of formula (I) ##STR1## in which n is 1 or 2, R.sup.1 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, halo or hydroxy, m is 0, 1 or 2, R.sup.2 is an immunogenic determinant and x is 1 or 2, provided that when n is 1, x is 1 or 2 and there is one diazo moiety at the 3-position or two diazo moieties at the 3- and 5-positions, with respect to the isothiocyanate group, and the hydroxy group is at the 4-position; and provided that when n is 2, x is 1 and the diazo moiety is at the 4-position and the hydroxy groups are at the 3- and 5-positions, are described. The compounds are useful in the preparation of immunoglobulin conjugates for employment in diagnostic techniques.
    Type: Grant
    Filed: December 5, 1983
    Date of Patent: November 13, 1984
    Assignee: Lilly Industries Limited
    Inventor: Robin G. Simmonds
  • Patent number: 4482553
    Abstract: 7-(2-Benzothienyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.
    Type: Grant
    Filed: April 12, 1983
    Date of Patent: November 13, 1984
    Assignee: Eli Lilly and Company
    Inventors: Robin D. G. Cooper, Bernard J. Graves, Edward R. Lavagnino
  • Patent number: 4482712
    Abstract: Substituted 1-thia-3-aza-4-ones having utility as plant fungicides, herbicides and terrestrial and aquatic plant growth regulators, together with methods for the use thereof and compositions containing the compounds.
    Type: Grant
    Filed: November 21, 1983
    Date of Patent: November 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: Eriks V. Krumkalns