Patents Represented by Attorney Leroy Whitaker

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  • Pharmaceutical compounds
    Patent number: 5185361
    Abstract: A pharmaceutical compound of the formula ##STR1## in which A is selected from --NHCOR.sup.1, --NHCOOR.sup.1, --NHCONHR.sup.1, --NHCSNHR.sup.1, --CONHR.sup.1, where R.sup.1 is optionally halo-substituted C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl or phenyl-C.sub.1-4 alkyl B is optionally substituted phenyl, and --X--Y-- is --CH=CH-- or --CH.sub.2 --CH.sub.2 --; and salts thereof. The compounds are leukotriene antagonists.
    Type: Grant
    Filed: September 18, 1991
    Date of Patent: February 9, 1993
    Assignee: Lilly Industries Limited
    Inventor: Jeremy Gilmore
  • Process and intermediates for chiral epoxides
    Patent number: 5183910
    Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.
    Type: Grant
    Filed: October 3, 1991
    Date of Patent: February 2, 1993
    Assignee: Eli Lilly and Company
    Inventor: Leland O. Weigel
  • 1-Carba(dethia)cephalosporin antibiotics
    Patent number: 5179088
    Abstract: 1-Carba(1-dethia)cephem antibacterial agents possessing a 3-(substituted or unsubstituted)thiazolo group are provided. Further provided is a method for treating bacterial infections in man and other animals and a pharmaceutical formulation utilziing said 1-carba(1-dethia)cephems.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: January 12, 1993
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, John E. Munroe
  • Process and intermediates to 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxylic acids
    Patent number: 5177244
    Abstract: This invention provides a process and intermediates for preparing 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxylic acids.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: January 5, 1993
    Assignee: Eli Lilly and Company
    Inventor: Christopher R. Schmid
  • Leukotriene antagonists
    Patent number: 5171882
    Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: December 15, 1992
    Assignee: Eli Lilly and Company
    Inventor: D. Mark Gapinski
  • Monoclonal antibodies reactive with a cell-surface gylcoprotein expressed on human carcinomas
    Patent number: 5171666
    Abstract: The present invention relates to a novel tumor-associated antigen that is a cell-surface glycoprotein having a molecular weight in the range of 110,000-140,000 daltons that is present in a variety of carcinomas, including squamous cell carcinomas and adenocarcinomas. The invention also comprises antibodies reactive with the antigen, hybridoma cell lines that produce the antibodies of the invention, and methods for using the antibodies in the diagnosis and treatment of cancer.
    Type: Grant
    Filed: October 19, 1988
    Date of Patent: December 15, 1992
    Assignee: Eli Lilly and Company
    Inventors: Magda C. Gutowski, David A. Johnson
  • Antitumor compositions and methods of treatment
    Patent number: 5169860
    Abstract: This invention provides the use of certain benzofuransulfonamide, benzothiophenesulfonamide, and indolesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzofuransulfonamide and benzothiophenesulfonamide derivatives and their pharmaceutical formulations.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: December 8, 1992
    Assignee: Eli Lilly and Company
    Inventors: Fariborz Mohamadi, Michael M. Spees
  • Amino protecting group
    Patent number: 5169945
    Abstract: The present invention provides a process for protecting an amino group in a compound exposed to nucleophilic reaction conditions in which the imido group used for protection is reacted with a secondary amine to form an acyl group which protects the amino group during exposure to the nucleophilic reaction conditions, after which the acylamino group may be reacted with an acid to reform the imido group so that the compound may then undergo non-nucleophilic manipulations. Also provided is a resolution method in which diasteriometric compounds having the acylamino group as described above are reacted with acid, and as these diasteriomers react at different rates to form the imido group, the reaction may be monitored so as to isolate the desired product at the appropriate point to maximize optical purity.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: December 8, 1992
    Assignee: Eli Lilly and Company
    Inventor: Leland O. Weigel
  • Method for producing 20-deoxotylosin
    Patent number: 5168052
    Abstract: The present invention, utilizing recombinant DNA technology, provides a novel method for obtaining 20-deoxotylosin from a tylosin producing microorganism. 20-deoxotylosin is useful as an antibiotic with a microbial inhibitory activity similar to tylosin.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: December 1, 1992
    Assignee: Eli Lilly and Company
    Inventors: Karen L. Cox, Eugene T. Seno
  • Immobolization of biomolecules by enhanced electrophoretic precipitation
    Patent number: 5166063
    Abstract: The present invention provides a method for immobilizing biomolecules on a conductive substrate to produce a biosensor.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: November 24, 1992
    Assignee: Eli Lilly and Company
    Inventor: Kirk W. Johnson
  • Defibrillation method and apparatus
    Patent number: 5161528
    Abstract: The present invention provides a method, and apparatus for accomplishing same, for defibrillating a mammal in need of defibrillation employing multiple bursts of electrical current delivered to the mammal, the timing between said bursts being based upon the mammal's fibrillation cycle length.
    Type: Grant
    Filed: September 5, 1990
    Date of Patent: November 10, 1992
    Assignee: Eli Lilly and Company
    Inventor: Robert J. Sweeney
  • Method of inhibiting gastric acid secretion with benzodioxanes
    Patent number: 5158956
    Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 29, 1991
    Date of Patent: October 27, 1992
    Assignee: Eli Lilly and Company
    Inventors: Jaswant S. Gidda, John M. Schaus
  • Intermediates to 1-carbacephalosporins and process for preparation thereof
    Patent number: 5159073
    Abstract: Disclosed is a process using hydrolysis and hydrogenation for converting enamino .beta.-lactams to their saturated alkyl ester acid salts, key intermediates to 1-carbacephalosporins. Also disclosed are intermediates resulting from the process.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: October 27, 1992
    Assignee: Eli Lilly and Company
    Inventors: James A. Aikins, Eddie V. Tao
  • Method of treating type I diabetes
    Patent number: 5158966
    Abstract: Provided is a method for treating Type I diabetes in mammals utilizing certain aryl-substituted rhodanine derivatives.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: October 27, 1992
    Assignee: The University of Colorado Foundation, Inc.
    Inventors: Kevin Lafferty, Jill A. Panetta
  • Pharmaceutical compounds
    Patent number: 5158971
    Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1 is halo-C.sub.1-10 alkyl, C.sub.1-10 alkylthio, halo-C.sub.1-10 alkylthio or optionally substituted phenylthio, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 and R.sup.4 are each hydrogen or C.sub.1-4 alkyl, and X is oxygen or sulphur; and salts thereof.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: October 27, 1992
    Assignee: Lilly Industries limited
    Inventors: Trafford Clarke, David J. Steggles
  • Intermediates of peripherally selective N-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists
    Patent number: 5159081
    Abstract: Intermediates of N-carbonyl-3,4,4-substituted piperidines are provided which are useful in the preparation of peripheral opioid antagonists.
    Type: Grant
    Filed: March 29, 1991
    Date of Patent: October 27, 1992
    Assignee: Eli Lilly and Company
    Inventors: Buddy E. Cantrell, Dennis M. Zimmerman
  • Enantioselective synthesis of antifolates
    Patent number: 5159090
    Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: October 27, 1992
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • 2-piperidones as intermediates for 5-deaza-10-oxo- and 5-deaza-10-thio-5,6,7,8-tetrahydrofolic acids
    Patent number: 5159079
    Abstract: 4-Deaza-10-oxo- and 5-deaza-10-thio-5,6,7,8-tetrahydrofolic acid derivatives are provided as agents useful for treatment susceptible neoplasms in mammals. Pharmaceutical formulations and intermediates are also provided.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: October 27, 1992
    Assignee: Eli Lilly and Company
    Inventors: Homer L. Pearce, Mark A. Winter
  • Excitatory amino acid receptor antagonists and methods for the use thereof
    Patent number: 5153196
    Abstract: Excitatory amino acid receptor antagonists and methods for the use thereof are disclosed. The antagonists include compounds having the preferred formula: ##STR1## in which: each of A.sub.1, A.sub.2 and A.sub.3 is independently either C or N, except that at least one of A.sub.1, A.sub.2 and A.sub.3 is N; one of A.sub.4 and A.sub.5 is C and the other is N; each R.sub.1 and R.sub.2 is independently hydrogen, halogen, CN, NO.sub.2, alkyl, aromatic, azido or CF.sub.3 ; and R.sub.3 is hydrogen, alkyl, aromatic or CF.sub.3. Also included are the tautomers thereof, and the pharmaceutically acceptable salts of (III) and (IV) and the tautomers thereof. These compounds are useful as EAA antagonists for blocking one or more EAA receptors, as neurological disorders associated with EAA receptors.
    Type: Grant
    Filed: June 5, 1991
    Date of Patent: October 6, 1992
    Assignee: Eli Lilly and Company
    Inventors: Loretta A. McQuaid, Charles H. Mitch, Paul L. Ornstein, Darryle D. Schoepp, Edward C. R. Smith
  • Methods of using recombinant human protein C
    Patent number: 5151268
    Abstract: The present invention comprises novel DNA compounds which encode human protein C activity. A variety of eukaryotic and prokaryotic recombinant DNA expression vectors have been constructed that comprise the novel protein C activity-encoding DNA and drive expression of protein C activity when transformed into an appropriate host cell. The novel expression vectors can be used to produce protein C derivatives, such as non-carboxylated, non-glycosylated, or non-hydroxylated protein C, and to produce protein C precursors, such as nascent or zymogen protein C, and to produce sub-fragments of protein C, such as active or inactive light and heavy chain. The recombinant-produced protein C activity is useful in the treatment and prevention of a variety of vascular disorders.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: September 29, 1992
    Assignee: Eli Lilly and Company
    Inventors: Nils U. Bang, Robert J. Beckmann, S. Richard Jaskunas, Mei-Huei T. Lai, Sheila P. Little, George L. Long, Robert F. Santerre