Patents Assigned to Eli Lilly & Company
  • 4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine derivatives
    Patent number: 4833145
    Abstract: Derivatives of N-[4-(N-[2-amino-4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-ylme thyl]-amino)benzoyl]-L-glutamic acid are antineoplastic agents. Their preparation and use, and intermediates useful for their preparation are described.
    Type: Grant
    Filed: November 13, 1987
    Date of Patent: May 23, 1989
    Assignees: The Trustees of Princeton University, Eli Lilly and Company
    Inventors: Edward C. Taylor, George P. Beardsley, Chuan Shih
  • 7-phenylsulfonyloxymethylene-6-oxo-perhydroquinolines
    Patent number: 4831145
    Abstract: This invention provides a process for preparing trans 2-aminopyrimido[4,5-g]quinolines employing novel intermediates.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: May 16, 1989
    Assignee: Eli Lilly and Company
    Inventors: Leland O. Weigel, Gilbert S. Staten
  • Process for producing antibiotic A80438
    Patent number: 4830967
    Abstract: A new strain of Streptomyces pactum, NRRL 15970, and an improved fermentation process for producing the polyether antibiotic A80438 using this microorganism are provided.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: May 16, 1989
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Raymond C. Yao
  • Capsule rectification apparatus
    Patent number: 4828142
    Abstract: An apparatus for handling empty two-piece capsules includes a vertically reciprocating feeder which extracts capsules from a hopper and forms randomly ordered linear arrays. A horizontal row of capsules are fed by the feeder to key-shaped slots in a block below the feeder. A blade reciprocally positioned adjacent the wider portion of the key-shaped slots moves into the slot at about the middle of the capsule to turn the capsules so as to be partly positioned within the narrower portion of the key-shaped slot. Each capsule is then ejected by projectable pins into a channel where the capsules are pneumatically accelerated into a pair of mated receiving rings which separate the two halves of the capsule.
    Type: Grant
    Filed: August 6, 1987
    Date of Patent: May 9, 1989
    Assignee: Eli Lilly & Company
    Inventor: Hugh P. McKnight
  • Substituted diazolidinones
    Patent number: 4826993
    Abstract: 4-Substituted 1-(optionally substituted)diazolidinones are intermediates to 7-substituted bicyclic pyrazolidinone antimicrobials.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: May 2, 1989
    Assignee: Eli Lilly and Company
    Inventors: Richard E. Holmes, Louis N. Jungheim
  • Alkanoyl anilides as pesticides
    Patent number: 4826841
    Abstract: The present invention is in alkanoyl anilides exhibiting insecticidal and arachnicidal activity, wherein the alkanoyl is both branched and substantially or totally fluorinated.
    Type: Grant
    Filed: March 5, 1986
    Date of Patent: May 2, 1989
    Assignee: Eli Lilly and Company
    Inventor: Robert P. Gajewski
  • 6-Oxo-trans-octa- and decahydroquinolines
    Patent number: 4826986
    Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.
    Type: Grant
    Filed: June 16, 1986
    Date of Patent: May 2, 1989
    Assignee: Eli Lilly and Company
    Inventors: Diane L. Huser, John M. Schaus
  • 2,3-(Dihydro) bicyclic pyrazolidinones
    Patent number: 4826992
    Abstract: 2,3-(Dihydro) bicyclic pyrazolidinones are intermediates for bicyclic pyrazolidinone antimicrobials.
    Type: Grant
    Filed: November 24, 1986
    Date of Patent: May 2, 1989
    Assignee: Eli Lilly and Company
    Inventors: Louis N. Jungheim, Sandra K. Sigmund
  • Antibiotic A80438
    Patent number: 4824863
    Abstract: New polyether antibiotic A80438, its acyl and alkyl ester, alkyl ether and urethane derivatives, and salts thereof, are useful antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Method of making A80438 by culture of Streptomyces bobili NRRL 15971 and synergistic compositions comprising (1) and A80438 compound and (2) nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds or metichlorpindol are also provided.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: April 25, 1989
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Walter M. Nakatsukasa, Raymond C. Yao
  • Ketoalkanol esters of dihydrolysergic acid useful as 5HT receptor antagonists
    Patent number: 4820713
    Abstract: Ketoalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Gifford P. Marzoni, William L. Garbrecht
  • Process for preparing 3-unsubstituted cephalosporins and 1-carba(dethia)cephalosporins
    Patent number: 4820832
    Abstract: A process for preparing 7.beta.-acylamino (or 7.beta.-protected amino)-3-H-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters and the corresponding cephalosporins is provided. 7.beta.-Acylamino (or 7.beta.-protected amino)-3-halo (or 3-sulfonyl ester)-1-carba(dethia)-3-cephem carboxylic acid esters and the corresponding cephalosporins are reduced with Pd(O) and a tetra-C.sub.2 -C.sub.6 alkyl stannane and, when a 3-sulfonyloxy ester is reduced, the process is carried out in the presence of an alkali metal halide. 3-Sulfonyloxy-3-cephem esters such as 3-mesylate, 3-tosylate and 3-triflate are employed.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Gwendolyn K. Cook, John H. McDonald, III
  • C-20-dihydro-deoxy-(cyclic amino)-derivatives of macrolide antibiotics
    Patent number: 4820695
    Abstract: C-20-Dihydro-deoxy-(cyclic amino)-derivatives of the macrolide antibiotics tylosin, desmycosin, macrocin, lactenocin, 2"'-O-demethylmacrocin and 2"-O-demethyllactenocin, which inhibit pathogenic bacteria, especially gram-positive bacteria, Pasteurella species, and Mycoplasma species, and pharmaceutical compositions thereof, are provided.
    Type: Grant
    Filed: May 28, 1987
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Manuel Debono, Herbert A. Kirst
  • Alkylation of 3(5)-cyano-1H-pyrazole-4-carboxylic acid esters
    Patent number: 4820845
    Abstract: The present invention provides a process for selectively alkylating pyrazoles comprising reacting a 3(5)-cyano-1H-pyrazole-4-carboxylic acid ester with a C.sub.4 -C.sub.8 alkene, or a C.sub.5 -C.sub.6 cycloalkene substituted at the 1-position with a C.sub.1 -C.sub.4 alkyl group, and a strong acid in a solvent which contains a strong electron withdrawing group. Also provided are new 3(5)-cyano-1H-pyrazole-4-carboxylic acid ester useful as starting materials in the process of the invention.
    Type: Grant
    Filed: April 1, 1987
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: James R. Beck, James A. Aikins, Eddie V. P. Tao
  • Disubstituted tetrazoles and their use as leukotriene antagonists
    Patent number: 4820722
    Abstract: The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C.sub.4, D.sub.4 and E.sub.4 in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive amounts of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: F. Patrick Carr, Robert D. Dillard, Winston S. Marshall, Doris E. McCullough
  • Disubstituted tetrazole leukotriene antagonists and methods for their use thereas
    Patent number: 4820723
    Abstract: The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive release or production of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof. Such conditions include an immediate hypersensitivity reaction of the type represented by asthma, or by shock or other adverse cardiovascular effects.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, Sandra K. Sigmund, Celia A. Whitesitt
  • Modifications of 3-O-demethylmycinose in macrocin and lactenocin
    Patent number: 4820694
    Abstract: New 3'" and/or 4'"-modified macrocin and 3" and/or 4"-modified-lactenocin derivatives of formula 1 have significant antibacterial activity. Compositions positions containing and methods of using these derivatives are also provided.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Manuel Debono, Herbert A. Kirst, James P. Leeds
  • Growth hormone and thyroid hormone
    Patent number: 4818531
    Abstract: This invention describes a method of increasing the feed intake of pigs, chickens, or dairy cattle, which have elevated levels of growth hormone, by administering a thyroid-active substance.
    Type: Grant
    Filed: February 6, 1985
    Date of Patent: April 4, 1989
    Assignee: Eli Lilly and Company
    Inventors: David B. Anderson, Jack F. Wagner
  • Immunoglobulin conjugates of 2',2'-difluronucleosides
    Patent number: 4814438
    Abstract: Immunoglobulin conjugates are formed by reacting a difluoronucleoside with an immunoglobulin via an alkane dioic acid linking group.
    Type: Grant
    Filed: November 23, 1987
    Date of Patent: March 21, 1989
    Assignee: Eli Lilly and Company
    Inventors: Henry K. Armour, G. Davon Kennedy, Gary A. Koppel, William L. Scott
  • 4-hydroxycyclohexyl 1-isopropyl-9,10-dihydro-lysergate for the treatment of migraine
    Patent number: 4810710
    Abstract: Method of blocking 5HT without effect on alpha receptors with 1-loweralkyl-6-straight chain alkyl-8.beta.-hydroxycycloalkyloxycarbonylergolines.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: March 7, 1989
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, Ray W. Fuller, William L. Garbrecht, Kathleen R. Whitten
  • Difluoro antivirals and intermediate therefor
    Patent number: 4808614
    Abstract: A 2,2-difluoro-2-desoxycarbohydrate is used to prepare antiviral nucleosides.
    Type: Grant
    Filed: June 4, 1987
    Date of Patent: February 28, 1989
    Assignee: Eli Lilly and Company
    Inventor: Larry W. Hertel