Patents Represented by Attorney, Agent or Law Firm James P. Leeds
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Patent number: 6472531Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 29, 2002Assignee: Eli Lilly and CompanyInventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
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Patent number: 6399778Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 4, 2002Assignee: Eli Lilly and CompanyInventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
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Patent number: 6372945Abstract: The present invention is directed to a new process for the synthesis of vinyl sulfoxides, in particular diarylvinyl sulfoxidesType: GrantFiled: June 7, 1995Date of Patent: April 16, 2002Assignee: Eli Lilly and CompanyInventors: James A. Aikins, Randal Scot Miller, Tony Y. Zhang
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Patent number: 6252064Abstract: This invention provides a process for preparing diastereomerically pure cryptophycin compounds.Type: GrantFiled: March 31, 2000Date of Patent: June 26, 2001Assignees: Eli and Company, University of Hawaii, Wayne State UniversityInventors: Michael John Martinelli, Eric David Moher
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Patent number: 5935928Abstract: 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: GrantFiled: February 14, 1996Date of Patent: August 10, 1999Assignee: Eli Lilly and CompanyInventors: Shalley K. Gupta, Jai Pal Singh
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Patent number: 5843938Abstract: 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: GrantFiled: October 3, 1996Date of Patent: December 1, 1998Assignee: Beiersdorf-Lilly GmbHInventors: Hans-Juergen Mest, Wolfgang Stenzel
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Patent number: 5792797Abstract: 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: GrantFiled: February 25, 1997Date of Patent: August 11, 1998Assignee: Lilly Industries LimitedInventors: Peter Thaddeus Gallagher, William Martin Owton, Andrew Caerwyn Williams
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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: 5731327Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 24, 1998Assignee: Eli Lilly and CompanyInventor: Wayne Douglas Luke
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Patent number: 5702937Abstract: 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: GrantFiled: May 23, 1995Date of Patent: December 30, 1997Assignee: Eli Lilly and CompanyInventor: Craig M. Zwickl
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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: 5668172Abstract: 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: GrantFiled: August 23, 1995Date of Patent: September 16, 1997Assignee: Lilly Industries LimitedInventors: Peter Thaddeus Gallagher, William Martin Owton, Andrew Caerwyn Williams
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Patent number: 5663375Abstract: 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: GrantFiled: August 22, 1994Date of Patent: September 2, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
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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: 5659087Abstract: The present invention is directed to new diarylvinyl sulfoxides.Type: GrantFiled: June 7, 1995Date of Patent: August 19, 1997Assignee: Eli Lilly and CompanyInventors: James A. Aikins, Tony Y. Zhang
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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: 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: 5637692Abstract: 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: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventors: James Aikins, John P. Gardner, Billy G. Jackson, John R. Rizzo, Eddie V. Tao
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Patent number: 5629425Abstract: 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: GrantFiled: September 19, 1994Date of Patent: May 13, 1997Assignee: Eli Lilly and CompanyInventors: Elizabeth S. LaBell, John M. McGill, Randal S. Miller