Patents Represented by Attorney, Agent or Law Firm Martin Hay
  • Patent number: 5906985
    Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: May 25, 1999
    Assignees: Eli Lilly and Company Limited, Lilly, S.A.
    Inventors: Stephen Richard Baker, Almudena Rubio Esteban, John Goldsworthy, Concepcion Pedregal Tercero
  • Patent number: 5891899
    Abstract: A pharmaceutical compound of the formula: ##STR1## in which A is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OPO(OH)OR'B is a bond, C.sub.1-6 alkylene or C.sub.2-6 alkenylene,R.sup.1 is hydrogen, hydroxyl, halo or group of the formula A--B--,X is C.sub.1-6 alkylene, C.sub.2-6 alkenylene, C.sub.2-6 alkynylene or C.sub.1-6 alkylene linked through --O--, --S-- or --NR"-- to Y, where R" is hydrogen or C.sub.1-6 alkyl,andY is (1) ##STR2## where p is and Z is ##STR3## or (2) ##STR4## and salts and esters thereof.
    Type: Grant
    Filed: December 15, 1997
    Date of Patent: April 6, 1999
    Assignee: Eli Lilly and Company Limited
    Inventors: Barry Peter Clark, John Richard Harris
  • Patent number: 5882671
    Abstract: The present invention provides a method of treating anxiety and related disorders using an agonist which acts at negatively coupled cAMP-linked metabotropic glutamate receptors.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: March 16, 1999
    Assignee: Eli Lilly and Company
    Inventors: David Reed Helton, Mary Jeanne Kallman, James Allen Monn, Darryle Darwin Schoepp, Joseph Patrick Tizzano
  • Patent number: 5863947
    Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: January 26, 1999
    Assignee: Eli Lilly and Company Limited
    Inventors: Stephen Richard Baker, Barry Peter Clark, John Goldsworthy, John Richard Harris
  • Patent number: 5843997
    Abstract: The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.
    Type: Grant
    Filed: April 2, 1996
    Date of Patent: December 1, 1998
    Assignee: Eli Lilly and Company
    Inventors: Lawrence J. Heinz, William H.W. Lunn, Darryle Darwin Schoepp
  • Patent number: 5795886
    Abstract: Compounds having general formula (I) wherein R is hydrogen or C.sub.1 -C.sub.10 alkyl; X is an aromatic moiety selected from phenyl, thienyl, furyl, pyridyl, imidazolyl, benzimidazolyl, benzothiazolyl and phthalazinyl which is unsubstituted or substituted with one or more moieties chosen from the group consisting of halogen, hydroxy, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, carboxy, C.sub.1 -C.sub.6 alkoxycarbonyl, acetyl, formyl, carboxymethyl, hydroxymethyl, amino, aminomethyl, methylenedioxy and trifluoromethyl; and "Aryl" represents p-nitrophenyl, p-aminophenyl or p-(protected amino) phenyl; or a pharmaceutically acceptable salt thereof, are useful as anticonvulsants.
    Type: Grant
    Filed: February 11, 1997
    Date of Patent: August 18, 1998
    Assignee: Eli Lilly and Company
    Inventors: Benjamin A. Anderson, Marvin M. Hansen, Nancy K. Harn
  • 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: 5747524
    Abstract: This invention discloses methods of using certain aryl-benzo?b!thiophene and benzo?b!furan compounds to block or inhibit cannabinoid receptors in mammals. It also discloses novel compounds which are antagonists of the cannabinoid receptors and also discloses pharmaceutical formulations which contain the compounds as an active ingredient.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: May 5, 1998
    Assignee: Eli Lilly and Company
    Inventors: George J. Cullinan, Kennan J. Fahey, Gary A. Koppel
  • Patent number: 5739164
    Abstract: Disclosed herein is a method of treating a disease of the central nervous system with a compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,Y is --CH.dbd.CH--, andZ is(i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or(iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: April 14, 1998
    Assignee: Eli Lilly and Company
    Inventors: Jesus Ezquerra Carrera, Almudena Rubio Esteban, Andre Mann, Angele Schoenfelder, Darryle Darwin Schoepp, Concepcion Pedregal Tercero, Camille-Georges Wermuth
  • Patent number: 5726320
    Abstract: A process for the preparation of (+)-2-amino-bicyclo?3.1.0!-hexane-2-6-dicarboxylic acid, or a pharmaceutically acceptable salt thereof, which comprises hydrolysing (-)-2-spiro-5'-hydantoinbicyclo?3.1.0!hexane-6-carboxylic acid or a salt thereof, and optionally forming a pharmaceutically acceptable salt. Also disclosed are intermediates useful in the process.
    Type: Grant
    Filed: June 26, 1996
    Date of Patent: March 10, 1998
    Assignee: Eli Lilly and Company
    Inventor: Roger Lewis Robey
  • Patent number: 5717109
    Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.
    Type: Grant
    Filed: July 10, 1995
    Date of Patent: February 10, 1998
    Assignee: Eli Lilly and Company
    Inventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
  • Patent number: 5688826
    Abstract: Compounds for formula I ##STR1## in which X represents O, NR.sup.a, S, SO or SO.sub.2 and R is as defined in the specification; and non-toxic metabolically labile esters or amides thereof; and pharmaceutically acceptable salts thereof are useful as modulators of metabotropic glutamate receptor function.
    Type: Grant
    Filed: November 14, 1996
    Date of Patent: November 18, 1997
    Assignee: Eli Lilly and Company
    Inventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
  • 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: 5665878
    Abstract: A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: September 9, 1997
    Assignee: Eli Lilly and Company
    Inventors: Benjamin A. Anderson, Marvin M. Hansen, David L. Varie, Jeffrey T. Vicenzi, Milton J. Zmijewski
  • 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: 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: 5641798
    Abstract: This invention provides novel bicyclic compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides intermediates useful in the synthesis of excitatory amino acid antagonists.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly and Company
    Inventor: James A. Monn
  • 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: 5624937
    Abstract: A compound of the formula I in which ##STR1## Z is O or S; R.sup.11 is a halogen atom;R.sup.12 is a halogen atom or a trifluoromethyl group; andX is S, SO, SO.sub.2, O or NH;R.sup.4 is naphthyl, quinolinyl, benzimidazolyl, pyridyl, pyradazinyl, benzoxazolyl or benzothiazolyl, unsubstituted or substituted by one or two substituents selected from a halogen atom, (1-4C)alkyl, (1-4C)alkoxy, nitro, (1-4C)alkoxycarbonyl, halo(1-4C)alkyl, and phenyl;or a pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of amyloid beta-protein production.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: April 29, 1997
    Assignee: Eli Lilly and Company
    Inventors: Jon K. Reel, Richard L. Simon, Celia A. Whitesitt