Patents Represented by Attorney, Agent or Law Firm Martin Hay
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Patent number: 5906985Abstract: 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: GrantFiled: August 21, 1997Date of Patent: May 25, 1999Assignees: Eli Lilly and Company Limited, Lilly, S.A.Inventors: Stephen Richard Baker, Almudena Rubio Esteban, John Goldsworthy, Concepcion Pedregal Tercero
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Patent number: 5891899Abstract: 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: GrantFiled: December 15, 1997Date of Patent: April 6, 1999Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
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Patent number: 5882671Abstract: 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: GrantFiled: January 21, 1997Date of Patent: March 16, 1999Assignee: Eli Lilly and CompanyInventors: David Reed Helton, Mary Jeanne Kallman, James Allen Monn, Darryle Darwin Schoepp, Joseph Patrick Tizzano
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Patent number: 5863947Abstract: 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: GrantFiled: May 9, 1997Date of Patent: January 26, 1999Assignee: Eli Lilly and Company LimitedInventors: Stephen Richard Baker, Barry Peter Clark, John Goldsworthy, John Richard Harris
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Patent number: 5843997Abstract: 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: GrantFiled: April 2, 1996Date of Patent: December 1, 1998Assignee: Eli Lilly and CompanyInventors: Lawrence J. Heinz, William H.W. Lunn, Darryle Darwin Schoepp
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Patent number: 5795886Abstract: 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: GrantFiled: February 11, 1997Date of Patent: August 18, 1998Assignee: Eli Lilly and CompanyInventors: Benjamin A. Anderson, Marvin M. Hansen, Nancy K. Harn
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Patent number: 5750566Abstract: 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: GrantFiled: June 29, 1995Date of Patent: May 12, 1998Assignee: Eli Lilly and CompanyInventors: James A. Monn, Darryle D. Schoepp
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Patent number: 5747524Abstract: 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: GrantFiled: September 30, 1996Date of Patent: May 5, 1998Assignee: Eli Lilly and CompanyInventors: George J. Cullinan, Kennan J. Fahey, Gary A. Koppel
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Patent number: 5739164Abstract: 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: GrantFiled: September 13, 1996Date of Patent: April 14, 1998Assignee: Eli Lilly and CompanyInventors: Jesus Ezquerra Carrera, Almudena Rubio Esteban, Andre Mann, Angele Schoenfelder, Darryle Darwin Schoepp, Concepcion Pedregal Tercero, Camille-Georges Wermuth
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Patent number: 5726320Abstract: 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: GrantFiled: June 26, 1996Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventor: Roger Lewis Robey
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Patent number: 5717109Abstract: 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: GrantFiled: July 10, 1995Date of Patent: February 10, 1998Assignee: Eli Lilly and CompanyInventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
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Patent number: 5688826Abstract: 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: GrantFiled: November 14, 1996Date of Patent: November 18, 1997Assignee: Eli Lilly and CompanyInventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
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Patent number: 5675008Abstract: 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: GrantFiled: June 1, 1995Date of Patent: October 7, 1997Assignee: Eli Lilly and CompanyInventors: Carl F. Bertsch, Bret Huff, Michael J. Martinelli, Paul L. Ornstein
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Patent number: 5670516Abstract: 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: GrantFiled: June 1, 1995Date of Patent: September 23, 1997Assignee: Eli Lilly and CompanyInventors: M. Brian Arnold, Nancy K. Augenstein, William H. W. Lunn, Paul L. Ornstein, Darryle D. Schoepp
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Patent number: 5665878Abstract: 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: GrantFiled: March 28, 1995Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Benjamin A. Anderson, Marvin M. Hansen, David L. Varie, Jeffrey T. Vicenzi, Milton J. Zmijewski
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Patent number: 5661184Abstract: 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: GrantFiled: June 29, 1995Date of Patent: August 26, 1997Assignee: Eli Lilly and CompanyInventors: David R. Helton, Mary Jeanne Kallman, James A. Monn, Darryle D. Schoepp, Joseph P. Tizzano
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Patent number: 5648492Abstract: 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: GrantFiled: June 1, 1995Date of Patent: July 15, 1997Assignee: Eli Lilly and CompanyInventors: M. Brian Arnold, Carl F. Bertsch, Marvin M. Hansen, Allen R. Harkness, Bret Huff, Michael J. Martinelli, Paul L. Ornstein
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Patent number: 5641798Abstract: 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: GrantFiled: June 1, 1995Date of Patent: June 24, 1997Assignee: Eli Lilly and CompanyInventor: James A. Monn
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Patent number: 5637712Abstract: 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: GrantFiled: November 21, 1994Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventors: Carl F. Bertsch, Bret Huff, Michael J. Martinelli
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Patent number: 5624937Abstract: 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: GrantFiled: March 2, 1995Date of Patent: April 29, 1997Assignee: Eli Lilly and CompanyInventors: Jon K. Reel, Richard L. Simon, Celia A. Whitesitt