Patents Represented by Attorney, Agent or Law Firm James P. Leeds
  • Patent number: 6472531
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 29, 2002
    Assignee: Eli Lilly and Company
    Inventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
  • Patent number: 6399778
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 4, 2002
    Assignee: Eli Lilly and Company
    Inventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
  • Patent number: 6372945
    Abstract: The present invention is directed to a new process for the synthesis of vinyl sulfoxides, in particular diarylvinyl sulfoxides
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 16, 2002
    Assignee: Eli Lilly and Company
    Inventors: James A. Aikins, Randal Scot Miller, Tony Y. Zhang
  • Patent number: 6252064
    Abstract: This invention provides a process for preparing diastereomerically pure cryptophycin compounds.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: June 26, 2001
    Assignees: Eli and Company, University of Hawaii, Wayne State University
    Inventors: Michael John Martinelli, Eric David Moher
  • Patent number: 5935928
    Abstract: The present invention is based of the discovery of two modified forms of human platelet factor-4, herein named MPF-4 and CPF-4, which were isolated from serum free culture medium of lipopolysaccharide-stimulated peripheral blood leukocytes. Amino acid sequence determination revealed that MPF-4 shares homology with platelet factor-4 beginning at N-terminal residue 17. CPF-4 consists of MPF-4 disulfide bonded to the 16 N-terminal residues of platelet factor-4. Both MPF-4 and CPF-4 are potent inhibitors of endothelial cell proliferation, approximately 10-100 fold more potent than native or recombinant platelet factor-4, making them useful in the treatment of angiogenic diseases.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: August 10, 1999
    Assignee: Eli Lilly and Company
    Inventors: Shalley K. Gupta, Jai Pal Singh
  • Patent number: 5843938
    Abstract: The use of a compound of the formula: ##STR1## in which X is --O-- or --NH--, or a pharmaceutically-acceptable acid addition salt thereof, in the treatment of atherosclerosis.
    Type: Grant
    Filed: October 3, 1996
    Date of Patent: December 1, 1998
    Assignee: Beiersdorf-Lilly GmbH
    Inventors: Hans-Juergen Mest, Wolfgang Stenzel
  • Patent number: 5792797
    Abstract: A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--;or a salt, amide or ester thereof.
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: August 11, 1998
    Assignee: Lilly Industries Limited
    Inventors: Peter Thaddeus Gallagher, William Martin Owton, Andrew Caerwyn Williams
  • Patent number: 5750566
    Abstract: The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
    Type: Grant
    Filed: June 29, 1995
    Date of Patent: May 12, 1998
    Assignee: Eli Lilly and Company
    Inventors: James A. Monn, Darryle D. Schoepp
  • Patent number: 5731327
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-?4-(2-aminoethoxy)benzoyl!benzo?b!-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-?4-(2-piperidinoethoxy)benzoyl!-benzo?b!th iophene hydrochloride, as well as processes for their preparation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 24, 1998
    Assignee: Eli Lilly and Company
    Inventor: Wayne Douglas Luke
  • Patent number: 5702937
    Abstract: A method for potentiating the activity of tissue plasminogen activator proteins by adding certain amounts of beta-lactoglobulin A is claimed. In particular, the invention includes an enhanced solid-phase immunoassay for measuring tissue plasminogen activator (nt-PA) activity in a mammalian serum sample with sufficient sensitivity to detect neutralizing activity in samples containing .mu.g/ml levels of total nt-PA antibody. Neutralizing activity can be easily detected in serum dilutions containing as little as 0.038 to 0.48 .mu.g of total nt-PA antibody in a 20 .mu.l sample. The assay has a sensitivity of 1 pM of nt-PA (67 pg/ml) in 5 hr.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: December 30, 1997
    Assignee: Eli Lilly and Company
    Inventor: Craig M. Zwickl
  • Patent number: 5675008
    Abstract: This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 7, 1997
    Assignee: Eli Lilly and Company
    Inventors: Carl F. Bertsch, Bret Huff, Michael J. Martinelli, Paul L. Ornstein
  • Patent number: 5670516
    Abstract: This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: September 23, 1997
    Assignee: Eli Lilly and Company
    Inventors: M. Brian Arnold, Nancy K. Augenstein, William H. W. Lunn, Paul L. Ornstein, Darryle D. Schoepp
  • Patent number: 5668172
    Abstract: A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--; or a salt, amide or ester thereof, useful in the treatment of skeletal diseases.
    Type: Grant
    Filed: August 23, 1995
    Date of Patent: September 16, 1997
    Assignee: Lilly Industries Limited
    Inventors: Peter Thaddeus Gallagher, William Martin Owton, Andrew Caerwyn Williams
  • Patent number: 5663375
    Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: September 2, 1997
    Assignees: Eli Lilly and Company, Lilly Industries Limited
    Inventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
  • Patent number: 5661184
    Abstract: The present invention provides a method of treating substance dependence disorders using an agonist which acts at negatively coupled cAMP-linked metabotropic glutamate receptors.
    Type: Grant
    Filed: June 29, 1995
    Date of Patent: August 26, 1997
    Assignee: Eli Lilly and Company
    Inventors: David R. Helton, Mary Jeanne Kallman, James A. Monn, Darryle D. Schoepp, Joseph P. Tizzano
  • Patent number: 5659087
    Abstract: The present invention is directed to new diarylvinyl sulfoxides.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 19, 1997
    Assignee: Eli Lilly and Company
    Inventors: James A. Aikins, Tony Y. Zhang
  • Patent number: 5648492
    Abstract: This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 15, 1997
    Assignee: Eli Lilly and Company
    Inventors: M. Brian Arnold, Carl F. Bertsch, Marvin M. Hansen, Allen R. Harkness, Bret Huff, Michael J. Martinelli, Paul L. Ornstein
  • Patent number: 5637712
    Abstract: This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.
    Type: Grant
    Filed: November 21, 1994
    Date of Patent: June 10, 1997
    Assignee: Eli Lilly and Company
    Inventors: Carl F. Bertsch, Bret Huff, Michael J. Martinelli
  • Patent number: 5637692
    Abstract: 7.beta.-Amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are provided via cyclization of cis-3-(substituted amino)-1-(2-substituted 2-oxoethyl)-4-substituted azetidinones. The 7.beta.-amino-3-hydroxy-1-carba (1-dethia)-3-cephem-4-carboxylic acid esters are useful chiral intermediates to .beta.-lactam antibiotics.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 10, 1997
    Assignee: Eli Lilly and Company
    Inventors: James Aikins, John P. Gardner, Billy G. Jackson, John R. Rizzo, Eddie V. Tao
  • Patent number: 5629425
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thi ophene hydrochloride, as well as processes for their preparation.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: May 13, 1997
    Assignee: Eli Lilly and Company
    Inventors: Elizabeth S. LaBell, John M. McGill, Randal S. Miller