Patents Represented by Attorney Arthur R. Whale
  • Patent number: 4595532
    Abstract: N-Mono or N-disubstituted methyl-2-azetidinones are provided via cyclization of .beta.-hydroxy or .beta.-halo substituted acid sec-amides wherein the amide nitrogen is substituted with a mono- or di-substituted methyl group having activating substituents. Cyclization of .beta.-hydroxy acid amides is mediated by triphenylphosphine-dialkylazodicarboxylate while cyclization of .beta.-halo acid amides is mediated by strong bases e.g. lithium dialkylamides. E.g. Diethyl amino-protected L-serylaminomalonate is cyclized with 200 mole % TPP-diisopropylazodicarboxylate to N-(diethoxycarbonylmethyl)-3-protected-amino-2-azetidinone. The 2-azetidinones provided are useful intermediates.
    Type: Grant
    Filed: April 1, 1985
    Date of Patent: June 17, 1986
    Assignee: University of Notre Dame du Lac
    Inventor: Marvin J. Miller
  • Patent number: 4595586
    Abstract: The present invention provides a novel moisturizing lotion which increases the rate of cell renewal on the skin without causing skin irritation and which facilitates the subsequent application of make-up.
    Type: Grant
    Filed: August 30, 1985
    Date of Patent: June 17, 1986
    Assignee: Eli Lilly and Company
    Inventor: Merlyn G. Flom
  • Patent number: 4594337
    Abstract: Methods of controlling Mycoplasma infections which comprise administering to an infected or susceptible warm-blooded animal an effective amount of a new macrocin or lactenocin ester derivative of the formula: ##STR1## wherein R is formyl or hydroxymethyl; R.sup.1 is hydrogen, acetyl or propionyl; R.sup.2 is hydrogen or ##STR2## and R.sup.3 is hydrogen, acetyl, propionyl, n-butyryl or isovaleryl; provided that one of R.sup.1 or R.sup.3 must be other than hydrogen; or a pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: February 27, 1985
    Date of Patent: June 10, 1986
    Assignee: Eli Lilly and Company
    Inventors: Earl E. Ose, Jan R. Turner
  • Patent number: 4594417
    Abstract: Crystalline cephalosporin hydrochloride salt represented by the formula ##STR1## wherein the oxime is in the syn configuration, is a useful pharmaceutical form of, and tool for purification of, the corresponding antibiotic free base; processes for its preparation are provided.
    Type: Grant
    Filed: December 3, 1984
    Date of Patent: June 10, 1986
    Assignee: Eli Lilly Company
    Inventor: Kuo S. Yang
  • Patent number: 4594247
    Abstract: Antibiotic compositions comprising a 1-oxa .beta.-lactam antibiotic compound of the formula ##STR1## or pharmaceutically acceptable salts thereof and either tobramycin, amikacin or piperacillin exhibit synergistic activity against multiple-antibiotic-resistant organisms. The 1-oxa compound can be used in conjunction with tobramycin, amikacin or piperacillin in a method of treating infections caused by resistant organisms.
    Type: Grant
    Filed: January 27, 1984
    Date of Patent: June 10, 1986
    Assignee: Eli Lilly and Company
    Inventor: Gordon L. Brier
  • Patent number: 4594358
    Abstract: This invention provides a method of producing analgesia in mammals which comprises administering dextropropoxyphene and fluoxetine or norfluoxetine. Pharmaceutical formulations useful in this method are also provided.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: June 10, 1986
    Assignee: Eli Lilly and Company
    Inventor: Martin D. Hynes
  • Patent number: 4594338
    Abstract: 11-Thioether and certain C-20 acetal and thioacetal derivatives of tylosin and demycarosyltylosin are effective antibacterial agents. Processes for preparing, formulations containing, and methods of treating bacterial infections with these derivatives are provided.
    Type: Grant
    Filed: February 19, 1985
    Date of Patent: June 10, 1986
    Inventors: Satoshi Omura, Kazuo Tsuzuki
  • Patent number: 4594431
    Abstract: Octahydro-5-oxoindolizine-6-propanoic acids and octahydro-6-oxopyrido[1,2-A]pyridine-7-propanoic acids, the decarboxy and related ester and perhydro derivatives thereof inhibit angiotensin I converting enzyme and are hypotensive agents. Hydrogenation of A58365 factors A and B, obtained by culturing Streptomyces chromofuscus, provides the ACE inhibitors. Also provided are O-acyl and O-sulfonyl derivatives of A and B factors which are useful in preparing deoxy factors A and B via hydrogenolysis.
    Type: Grant
    Filed: August 1, 1983
    Date of Patent: June 10, 1986
    Assignee: Eli Lilly Company
    Inventors: Jon S. Mynderse, David S. Fukuda
  • Patent number: 4591591
    Abstract: This invention provides for the use of certain pyridazinones as positive inotropic agents.
    Type: Grant
    Filed: March 8, 1984
    Date of Patent: May 27, 1986
    Assignee: Eli Lilly and Company
    Inventor: David W. Robertson
  • Patent number: 4590213
    Abstract: This invention provides for a method of treating anxiety which comprises the administration of fluoxetine or norfluoxetine or pharmaceutically aceptable salts thereof.
    Type: Grant
    Filed: April 8, 1983
    Date of Patent: May 20, 1986
    Assignee: Eli Lilly and Company
    Inventor: Paul Stark
  • Patent number: 4589905
    Abstract: The present invention is directed to compounds of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, ##STR2## each of R.sup.2 and R.sup.3 is taken separately and is independently hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.4 cycloalkyl or C.sub.1 -C.sub.3 alkoxy, orR.sup.2 and R.sup.3 are taken together with the nitrogen atom to which they are attached and form piperidine, morpholine or pyrrolidine;each R.sup.4 independently is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -Cphd 4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy or cyano;X is 0 or S; andm is 0-3;with the provisos that when R.sup.4 is C.sub.1 -C.sub.4 alkyl, that substituent exists at other than the 2 or 6 position of the phenyl ring; and when R.sup.2 is C.sub.1 -C.sub.3 alkoxy, R.sup.3 is other than C.sub.1 -C.sub.3 alkoxy.These compounds exhibit activity as terrestrial herbicides, aquatic herbicides, and aquatic algicides.
    Type: Grant
    Filed: September 13, 1984
    Date of Patent: May 20, 1986
    Assignee: Eli Lilly and Company
    Inventor: James R. Beck
  • Patent number: 4588484
    Abstract: The present invention relates to electrochemical reduction of a 3-chlorobenzo[b]thiophene to the corresponding 3-hydrobenzo[b]thiophene compound.
    Type: Grant
    Filed: February 28, 1985
    Date of Patent: May 13, 1986
    Assignee: Eli Lilly and Company
    Inventors: Richard M. Justice, Jr., David A. Hall
  • Patent number: 4587218
    Abstract: New Actinoplanes missouriensis strains CUC 014 (NRRL 15647) and CSV 558 (NRRL 15646) which operate together to cosynthesize the useful glycopeptide antibiotic CUC/CSV.
    Type: Grant
    Filed: October 21, 1983
    Date of Patent: May 6, 1986
    Assignee: Eli Lilly and Company
    Inventor: Charles L. Hershberger
  • Patent number: 4587344
    Abstract: N-methyl-S-methyl-N'-[2-(2-dimethylaminomethylthiazol-4-ylmethylthio)ethyl] isothiourea is prepared by the reaction of 2-dimethylaminomethyl-4-(2-aminoethyl)thiomethylthiazole with methylcarbonimidodithioic acid, dimethyl ester, and is a useful intermediate for the preparation of nizatidine, a pharmaceutically valuable H.sub.2 -receptor inhibitor.
    Type: Grant
    Filed: November 29, 1984
    Date of Patent: May 6, 1986
    Assignee: Eli Lilly and Company
    Inventor: Charles W. Ryan
  • Patent number: 4587351
    Abstract: The present invention pertains to a process for preparing ketones employing a silica catalyzed oxidation of a secondary alcohol with calcium hypochlorite in acetonitrile.
    Type: Grant
    Filed: April 18, 1984
    Date of Patent: May 6, 1986
    Assignee: Eli Lilly and Company
    Inventors: Randall K. Atkins, Leland O. Weigel
  • Patent number: 4587348
    Abstract: The herbicide 5-cyano-1-phenyl-N-methyl-1H-pyrazole-4-carboxamide is prepared in high yield and high purity in a two-step process without isolation of the intermediate.
    Type: Grant
    Filed: September 6, 1984
    Date of Patent: May 6, 1986
    Assignee: Eli Lilly and Company
    Inventors: John Brennan, Eddie V. P. Tao
  • Patent number: 4587053
    Abstract: Oxazolino-azetidinones are prepared by reaction of a phosphorus compound with a 3-exomethylenecepham sulfoxide.
    Type: Grant
    Filed: April 26, 1984
    Date of Patent: May 6, 1986
    Assignee: Eli Lilly and Company
    Inventors: Robin D. G. Cooper, John M. Morin, Jr., Lynn R. Peters
  • Patent number: 4585861
    Abstract: This invention relates to certain amino-5,6-diaryl-1,2,4-triazines and -pyrazines useful as activators of GABA and benzodiazepine binding.
    Type: Grant
    Filed: January 4, 1985
    Date of Patent: April 29, 1986
    Assignee: Eli Lilly and Company
    Inventors: David T. Wong, William B. Lacefield
  • Patent number: 4585894
    Abstract: Processes are described for preparing pharmaceutical 9-carbamoyl-9-aminoalkylfluorenes and intermediates in their preparation.
    Type: Grant
    Filed: October 19, 1983
    Date of Patent: April 29, 1986
    Assignee: Eli Lilly and Company
    Inventors: Derek Johnson, Alan C. Spreadbury
  • Patent number: 4584404
    Abstract: Selective biogenic amine uptake inhibitors, 3-substituted phenyloxy-3-phenylpropyldimethylamines.
    Type: Grant
    Filed: October 24, 1983
    Date of Patent: April 22, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bryan B. Molloy, Klaus K. Schmiegel