Patents Represented by Attorney Arthur R. Whale

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  • Antibiotic A80190, pharmaceutical compositions containing same and method of use
    Patent number: 4582822
    Abstract: New polyether antibiotic A80190, its acyl and alkyl ester, acyl ester and urethane derivatives, and salts thereof, are useful antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Methods of making A80190 by culture of Actinomodura oligospora NRRL 15877 and synergistic compositions of the A80190 compounds with nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds and metichlorpindol are also provided.
    Type: Grant
    Filed: October 9, 1984
    Date of Patent: April 15, 1986
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Raymond C. Yao
  • Purification of phenylethanolamine N-methyltransferase
    Patent number: 4582806
    Abstract: The present invention provides an efficient process for purifying the enzyme phenylethanolamine N-methyltransferase suitable for use in radioenzymatic assays of endogenous compounds.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: April 15, 1986
    Assignee: Eli Lilly and Company
    Inventors: Ronald R. Bowsher, David P. Henry
  • Processes for preparing picenadol precursors and novel intermediates thereof
    Patent number: 4581456
    Abstract: The present invention relates to processes for preparing precursors of picenadol, (.+-.)3-(1,3.alpha.-dimethyl-4.alpha.-propyl-4.beta.-piperidinyl)phenol, hydrochloride, a known analgesic. Certain of the compounds prepared by the present process are novel as well.
    Type: Grant
    Filed: September 21, 1983
    Date of Patent: April 8, 1986
    Assignee: Eli Lilly and Company
    Inventor: Charles J. Barnett
  • Thienothienylglycyl cephalosporin derivatives
    Patent number: 4581352
    Abstract: 7-(Thienothienyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.
    Type: Grant
    Filed: December 3, 1984
    Date of Patent: April 8, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bennie J. Foster, David C. Hunden, Edward R. Lavagnino
  • Sustained release intranasal formulation and method of use thereof
    Patent number: 4581225
    Abstract: Administration of a catecholamine by a novel intranasal delivery system provides prolonged blood levels of the drug.
    Type: Grant
    Filed: January 28, 1985
    Date of Patent: April 8, 1986
    Assignee: Eli Lilly and Company
    Inventors: Kenneth S. E. Su, Kristina M. Campanale, Harve C. Wilson
  • Anti-diabetic compounds
    Patent number: 4581165
    Abstract: A class of compounds having insulin-like activity is described. These compounds have the formula ##STR1## in which X is --OH, -Arg-Arg-OH, or -Arg-Arg-Glu-Ala-Glu-Asp-Leu-Gln-Val-Gly-Gln-Val-Glu-Leu-Gly-Gly-Gly-Pro-G ly-Ala-Gly-Ser-Leu-Gln-Pro-Leu-OH.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: April 8, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bruce H. Frank, Allen H. Pekar
  • Macrolide derivatives
    Patent number: 4581346
    Abstract: C-8, 20-cyclo-derivatives of the macrolide antibiotics tylosin, desmycosin, macrocin, lactenocin, 2'"-O-demethylmacrocin and 2"-O-demethyllactenocin, which inhibit pathogenic bacteria, especially gram-positive bacteria, and Mycoplasma species, and pharmaceutical compositions thereof, are provided.
    Type: Grant
    Filed: July 12, 1984
    Date of Patent: April 8, 1986
    Assignee: Eli Lilly and Company
    Inventor: Joseph H. Kennedy
  • Inotropic agents
    Patent number: 4578387
    Abstract: This invention provides for certain phenyl-substituted imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents and vasodilators.
    Type: Grant
    Filed: March 5, 1984
    Date of Patent: March 25, 1986
    Assignee: Eli Lilly and Company
    Inventor: Wayne A. Spitzer
  • Thieno and furopyridinium-substituted cephalosporins
    Patent number: 4577014
    Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with a thienopyridinium methyl group or a furopyridinium methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino]-3-iodomethyl-3-cephem-4-carboxyl ic acid with the thienopyridine or the furopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.
    Type: Grant
    Filed: December 7, 1984
    Date of Patent: March 18, 1986
    Assignee: Eli Lilly and Company
    Inventors: William H. W. Lunn, Robert T. Vasileff
  • 6-Substituted-4-dialkylaminotetrahydrobenz[c,d]indoles
    Patent number: 4576959
    Abstract: (.+-.)-4-substitutedamino-6-substituted-1,3,4,5-tetrahydrobenz[c,d]indoles and pharmaceutically acceptable salts thereof, useful as anti depressants.
    Type: Grant
    Filed: February 1, 1985
    Date of Patent: March 18, 1986
    Assignee: Eli Lilly and Company
    Inventor: Michael E. Flaugh
  • Alkylsulfonamidophenylalkylamines
    Patent number: 4569801
    Abstract: The present invention relates to a new class of alkylsulfonamidophenylalkylamines which are potent antiarrhythmic agents having good oral bioavailability properties.
    Type: Grant
    Filed: October 15, 1984
    Date of Patent: February 11, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bryan B. Molloy, Mitchell I. Steinberg
  • Anti-diabetic compounds
    Patent number: 4569792
    Abstract: A class of compounds having insulin-like activity is described. These compounds have the formula ##STR1## in which X is --OH, -Ala-Leu-Glu-Gly-Ser-Leu-Gln-OH, or -Ala-Leu-Glu-Gly-Ser-Leu-Gln-Lys-Arg-OH.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: February 11, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bruce H. Frank, Allen H. Pekar
  • Anti-diabetic compounds
    Patent number: 4569791
    Abstract: A class of compounds having insulin-like activity is described. These compounds have the formula ##STR1## in which n is zero or one.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: February 11, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bruce H. Frank, Allen H. Pekar
  • Process for purifying proteins and compounds useful in such process
    Patent number: 4569794
    Abstract: This invention describes a process for separating a biologically active polypeptide or protein in the form of its precursor from a mixture containing said precursor and impurities, which comprises contacting said precursor with a resin containing immobilized metal ions, said precursor comprising the biologically active polypeptide or protein covalently linked directly or indirectly to an immobilized metal ion chelating peptide, binding said precursor to said resin, and selectively eluting said precursor from said resin. Such precursor compounds are also described.
    Type: Grant
    Filed: December 5, 1984
    Date of Patent: February 11, 1986
    Assignee: Eli Lilly and Company
    Inventors: Michele C. Smith, Charles Pidgeon
  • Method of preparing octahydro-1H(and 2H)-pyrazolo[3,4-g]quinolines
    Patent number: 4567266
    Abstract: A 1-substituted-3-permissibly-substituted-6 (or 7)-oxodecahydroquinoline is converted to the corresponding 7 (or 6)-formyl derivative. The 6-oxo-7-formyl compound, upon treatment with hydrazine, is cyclized to a tautomeric mixture of 5-substituted-7-permissibly-substituted-4,4a,5,6,7,8,8a,9-octahydro-1H(and 2H)-pyrazolo[3,4-g]quinolines.
    Type: Grant
    Filed: August 2, 1984
    Date of Patent: January 28, 1986
    Assignee: Eli Lilly and Company
    Inventor: John M. Schaus
  • N-Acyloxy monocyclic .beta.-lactams
    Patent number: 4565654
    Abstract: Process for N-acyloxy or sulfooxy 2-azetidinones comprising O-acylation of a .beta.-hydroxy or .beta.-halo hydroxamic acid, and cyclizing the O-acylhydroxamate with TPP-CCl.sub.4 -TEA or with TPP-dialkylazodicarboxylate to the N-acyloxy-2-azetidinone. Solvolysis of the acyl group provides an N-hydroxy-2-azetidinone. E.g., N-Cbz-L-serine is converted to the O-acetyl hydroxamate, cyclized and solvolyzed to N-hydroxy-3-(Cbz-amino)-2-azetidinone. The N-hydroxy-2-azetidinones are useful intermediates to monocyclic .beta.-lactam antibiotics and .beta.-lactamase inhibitors.
    Type: Grant
    Filed: March 28, 1983
    Date of Patent: January 21, 1986
    Assignee: University of Notre Dame Du Lac
    Inventor: Marvin J. Miller
  • Diazabicyclononene antibacterials
    Patent number: 4565655
    Abstract: Fused 4,7-.beta.-lactam bicyclic antibacterials, namely 8-acylamino-4-anilino-9-oxo-6-thia-1,3-diazabicyclo[5.2.0]non-3-ene-2-carb oxylic acids, and the esters, salts and sulfoxides thereof, are provided. The compounds as esters are prepared by process comprising heating a 3-azido-3-cephem ester with aniline, a substituted aniline, or an N-(C.sub.1 -C.sub.3 alkyl) derivative thereof.
    Type: Grant
    Filed: September 28, 1983
    Date of Patent: January 21, 1986
    Assignee: Eli Lilly and Company
    Inventor: Douglas O. Spry
  • 1-Alkyl-6-pyrrolidino-octahydroquinolines
    Patent number: 4565871
    Abstract: Trans-(.+-.) or trans-(-)-2,4-permissibly-substituted-6-alkyl or allyl octahydropyrimido[4,5-g]quinolines and related compounds, ultraviolet light absorbers.
    Type: Grant
    Filed: December 11, 1984
    Date of Patent: January 21, 1986
    Assignee: Eli Lilly and Company
    Inventors: Cynthia L. Nicholas, Edmund C. Kornfeld, John M. Schaus
  • Herbicidal 5-halo-1-halophenyl-1H-pyrazole-4-carbonitriles
    Patent number: 4563210
    Abstract: The present invention is directed to herbicidal compounds of the formula ##STR1## wherein each R.sup.1 independently is halogen; R.sub.2 is halo or trifluoromethyl; and n is 1-5; with the provisos that when n is 1, R.sup.1 is other than fluorine, and when n is 2 and each R.sup.1 is chlorine, at least one R.sup.1 is located at a para or ortho position on the phenyl ring.
    Type: Grant
    Filed: September 13, 1984
    Date of Patent: January 7, 1986
    Assignee: Eli Lilly and Company
    Inventors: James R. Beck, Michael P. Lynch
  • Glycopeptide bioconversion products
    Patent number: 4563442
    Abstract: New glycopeptide antibiotics of the formula: ##STR1## wherein W is the remaining portion of a glycopeptide antibiotic selected from actaplanin factors B.sub.1, B.sub.2, B.sub.3, C.sub.1, C.sub.2, C.sub.3, D.sub.1, D.sub.2, E.sub.1, G, K, L, M, N, O and actaplanin .psi.aglycone, and salts thereof, particularly the pharmaceutically acceptable salts, are useful new antibiotics are active against gram-positive bacteria and increase feed-efficiency utilization and enhance milk production in ruminants.
    Type: Grant
    Filed: September 24, 1984
    Date of Patent: January 7, 1986
    Assignee: Eli Lilly and Company
    Inventors: Gladys M. Clem, LaVerne D. Boeck, Marie T. Anderson, Karl H. Michel