Patents Represented by Attorney Robert A. Conrad

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  • Enantioselective synthesis of antifolates
    Patent number: 5516776
    Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: May 14, 1996
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Activator gene for macrolide biosynthesis
    Patent number: 5514544
    Abstract: A gene encoding activator protein (srmR) for increasing transcriptional efficiency of macrolide biosynthetic genes is disclosed and claimed. Methods for using srmR to increase macrolide biosynthetic gene transcription and identifying further macrolide biosynthetic pathways are disclosed. Recombinant DNA vectors comprising the srmR gene are disclosed.
    Type: Grant
    Filed: July 26, 1991
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventors: Ramachandra N. Rao, Jan R. Turner
  • Method for treating anxiety
    Patent number: 5488056
    Abstract: The present invention provides a method for treating anxiety in humans using heterocyclic compounds.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: January 30, 1996
    Assignee: Eli Lilly and Company
    Inventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
  • Method for treating anxiety
    Patent number: 5484794
    Abstract: The present invention provides a method for treating anxiety in humans using heterocyclic compounds.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: January 16, 1996
    Assignee: Eli Lilly and Company
    Inventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
  • Pharmaceutical composition
    Patent number: 5470865
    Abstract: The present invention provides an odorless pharmaceutical composition of nizatidine. It also provides a novel form of nizatidine and a process for the preparation of this form.
    Type: Grant
    Filed: August 30, 1994
    Date of Patent: November 28, 1995
    Assignee: Eli Lilly and Company
    Inventors: Mary K. McCauley, Kenneth P. Moder, Jeffrey L. Speakman
  • Method of treating tumors in mammals with 2',2'-difluoronucleosides
    Patent number: 5464826
    Abstract: A method of treating susceptible neoplasms in mammals comprising administering to a mammal in need of such treatment a pharmaceutically effective amount of a compound of the formula ##STR1## wherein: R.sup.1 is hydrogen;R.sup.2 is a base defined by one of the formulae ##STR2## X is C-R.sup.4 ; R.sup.3 is hydrogen;R.sup.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, bromo, fluoro, chloro or iodo;and the pharmaceutically-acceptable salts thereof.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: November 7, 1995
    Assignee: Eli Lilly and Company
    Inventors: Gerald B. Grindey, Larry W. Hertel
  • Substituted phenyl phenol leukotriene antagonists
    Patent number: 5462954
    Abstract: Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: October 31, 1995
    Assignee: Eli Lilly and Company
    Inventors: S. Richard Baker, Robert D. Dillard, Paul E. Floreancig, J. Scott Sawyer, Michael J. Sofia
  • Process for preparing alpha-anomer enriched 1-halo-2-deoxy-2,2-difluoro-D-ribofuranosyl derivatives
    Patent number: 5453499
    Abstract: A stereoselective process for preparing an alpha-anomer enriched 1-.alpha.-halo-2-deoxy-2,2-difluoro-D-ribofuranosyl derivatives involving contacting a 3,5-hydroxy protected-2-deoxy-2,2-difluoro-D-ribofuranosyl-1-.beta.-sulfonate with a halide source in an inert solvent.
    Type: Grant
    Filed: July 29, 1993
    Date of Patent: September 26, 1995
    Inventors: Ta-Sen Chou, Charles D. Jones, Thomas E. Mabry
  • Treatment of lower urinary tract disorders with selective norepinephrine uptake inhibitors
    Patent number: 5441985
    Abstract: This invention provides a method of treating lower urinary tract disorders in mammals employing compounds which inhibit norepinephrine reuptake and having negligible anticholinergic effect.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventor: Mark M. Foreman
  • Intermediates for specific 5-HT3 antagonists
    Patent number: 5442078
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Antithrombotic agents
    Patent number: 5439888
    Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: August 8, 1995
    Assignee: Eli Lilly and Company
    Inventors: Robert T. Shuman, Gerald F. Smith
  • Process for preparing 2',2'-difluoronucleosides
    Patent number: 5434254
    Abstract: The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.
    Type: Grant
    Filed: April 19, 1993
    Date of Patent: July 18, 1995
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath, Lawrence E. Patterson
  • 2'-deoxy-2',2'-difluoro (4-substituted pyrimidine) nucleosides, bicyclic derivatives,pharmaceutical compositions, and synthetic precursors
    Patent number: 5430026
    Abstract: The invention provides certain 2-Deoxy-2,2-Difluoro (4-Substituted) Pyrimidine Nucleosides that are effective as anti-cancer agents and in treating viral infections.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: July 4, 1995
    Assignee: Eli Lilly and Company
    Inventors: Larry Hertel, Julian S. Kroin
  • 1,3-benzenedimethanamines useful as central nervous system active agents
    Patent number: 5428065
    Abstract: Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 27, 1995
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, Graham H. Timms
  • Process for preparing 2,2-difluoroketene silyl O,S-acetals and .alpha.,.alpha.-difluoro-.beta.-silyloxy-1,3-dioxolane-4-propanoic acid O,S-esters
    Patent number: 5428176
    Abstract: Processes for preparing 2,2-difluoroketene silyl O,S-acetals and .alpha.,.alpha.-difluoro-.beta.-silyloxy-1,3-dioxolane-4-propanoic acid O,S-esters.
    Type: Grant
    Filed: April 14, 1994
    Date of Patent: June 27, 1995
    Assignee: Eli Lilly and Company
    Inventor: John A. Weigel
  • Process for the preparation of 4-hydroxy-5-substituted ethynylpyrrolo [2,3-d]pyrimidine intermediates
    Patent number: 5426187
    Abstract: Processes for preparing 4-hydroxy-5-ethynylpyrrolo[2,3-d]pyrimidine intermediates and N-[4-(2-{4-hydroxypyrrolo[2,3-d]pyrimidin-3-yl}ethyl)benzoyl]-L-glutamic acid derivatives having antineoplastic activity are provided.
    Type: Grant
    Filed: November 30, 1993
    Date of Patent: June 20, 1995
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Michael E. Kobierski
  • Catalytic stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
    Patent number: 5426183
    Abstract: A catalytic stereoselective glycosylation process for preparing beta- and alpha-anomer enriched 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides involving reacting an alpha- or beta- anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorocarbohydrate with at least a molar equivalent of a nucleobase derivative in an inert solvent and in the presence of a catalyst.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: June 20, 1995
    Assignee: Eli Lilly and Company
    Inventor: Douglas P. Kjell
  • Pyrimidinyl-glutamic acid derivatives
    Patent number: 5426110
    Abstract: The present invention provides novel pyrimidinyl-glutamic acid derivatives and intermediates thereto. Further provided are methods for inhibiting dihydrofolate reductase in mammals and for treating susceptible neoplasms in mammals, particularly humans.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: June 20, 1995
    Assignee: Eli Lilly and Company
    Inventors: Lynn S. Gossett, Chuan Shih
  • Piperidine opioid antagonists
    Patent number: 5422356
    Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: June 6, 1995
    Assignee: Eli Lilly and Company
    Inventors: Dennis M. Zimmerman, Charles H. Mitch
  • Process for anomerizing nucleosides
    Patent number: 5420266
    Abstract: A process for increasing the amount of a desired anomer nucleoside from an undesired anomeric nucleoside mixture thereof by contacting the mixture with a hydroxide base in an organic solvent.
    Type: Grant
    Filed: January 3, 1994
    Date of Patent: May 30, 1995
    Assignee: Eli Lilly and Company
    Inventors: Thomas C. Britton, Michael E. LeTourneau