Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Grant
Filed:
August 4, 1999
Date of Patent:
December 26, 2000
Assignee:
Eli Lilly and Company
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Grant
Filed:
October 6, 1997
Date of Patent:
December 5, 2000
Assignee:
Eli Lilly and Company
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
Abstract: The instant invention provides novel crystalline Form II of (.+-.)-5-{[3,5-bis(1,1dimethylethyl)-4-hydroxyphenyl]methyl}-4-thiazolidin one having an x-ray powder diffraction patter with specific d spacings useful for treating inflammation, inflammatory bowel disease, allergies, arthritis and hypoglycemia utilizing the novel physical form as well as pharmaceutical compositions containing the same. A process for preparing Form II Tazofelone is described.
Type:
Grant
Filed:
February 25, 1998
Date of Patent:
May 16, 2000
Assignee:
Eli Lilly and Company
Inventors:
Marvin M Hansen, Allen R Harkness, Susan M Reutzel
Abstract: This invention provides methods for the treatment or inhibiting of iritis which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a leukotriene B.sub.4 antagonist.
Type:
Grant
Filed:
March 13, 1998
Date of Patent:
December 7, 1999
Assignee:
Eli Lilly and Company
Inventors:
Jerome H. Fleisch, William T. Jackson, Jason S. Sawyer
Abstract: This invention provides thiomorpholinone compounds useful for treating multiple sclerosis of formula I wherein:R.sup.1 and R.sup.2 are each independently selected from C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl; C.sub.2 -C.sub.8 alkynyl; C.sub.1 -C.sub.8 alkyloxy; C.sub.1 -C.sub.8 alkylthio; trifluoromethyl; C.sub.1 -C.sub.4 alkyl substituted with phenyl; phenyl; F; Cl; NO.sub.2 ; phenoxy; C.sub.1 -C.sub.4 alkyl substituted with phenoxy; thiophenyl; C.sub.1 -C.sub.4 alkylthiophenyl; --COOR.sup.7 ; --N(R.sup.7).sub.2 or --N(R.sup.7)SO.sub.2 R.sup.7 where each R.sup.7 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl;R.sup.4 and R.sup.5 are each individually H, or when taken together form a bond;R.sup.6 is H; C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl; C.sub.2 -C.sub.8 alkynyl; --SO.sub.2 CH.sub.3 ; --(CH.sub.2).sub.n NR.sup.8 R.sup.9 ; --(CH.sub.2).sub.n CO.sub.2 R.sup.8 ; --(CH.sub.2).sub.n OR.sup.8 where n is an integer from 1 to 6, both inclusive, and R.
Abstract: The present invention provides a method for treating neuropathic pain comprising administering an analgesic dosage of a compound of formula I to an animal in need of such treatment certain phenyl oxazoles or phenyl thiazoles.
Abstract: The present invention provides a method for treating pain using a composition comprising certain phenyl oxazoles or phenyl thiazoles in combination with a Drug Useful in the Treatment of Pain.
Abstract: This invention provides methods for the treatment or inhibiting of dermatitis which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a leukotriene B.sub.4 antagonist.
Type:
Grant
Filed:
March 13, 1998
Date of Patent:
June 22, 1999
Assignee:
Eli Lilly and Company
Inventors:
Jerome H. Fleisch, William T. Jackson, Jason S. Sawyer
Abstract: A series of 1-(4-indolyloxy)-3-(4-hydroxy-4-naphthylpiperidin-1-yl)propanes are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor, yet lack mutagenic potential as measured by assays of chromosomal aberration. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
Type:
Grant
Filed:
May 22, 1997
Date of Patent:
June 15, 1999
Assignee:
Eli Lilly and Company
Inventors:
Daniel James Koch, Vincent Patrick Rocco
Abstract: This invention provides methods for the treatment or inhibitor of oral squamous cell carcinoma which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a leukotriene B.sub.4 antagonist.
Type:
Grant
Filed:
December 2, 1997
Date of Patent:
June 8, 1999
Assignee:
Eli Lilly and Company
Inventors:
Jerome H. Fleisch, William T. Jackson, Jason S. Sawyer
Abstract: This invention discloses novel piperidine tetrazole compounds which are selective antagonists of EAA receptors particularly the NMDA receptors. The invention also provides formulations of the preferred compounds and for methods of using the compounds to treat various disorders associated with neuronal excitotoxicity.
Type:
Grant
Filed:
October 20, 1997
Date of Patent:
March 9, 1999
Assignee:
Eli Lilly and Company
Inventors:
Lawrence J. Heinz, William H. W. Lunn, Paul L. Ornstein
Abstract: The present invention relates to a novel process for preparing cis-4-O-protected-substituted-2-cyclopentenol derivatives comprising, a) dissolving a 4-O-protected-2-cyclopentenone in a suitable organic solvent; and b) treating the solution with a suitable Lewis acid and a suitable reducing agent at a temperature of from about -100.degree. C. to about 20.degree. C. The cis-4-O-protected-substituted-2-cyclopentenol derivatives are useful intermediates in the preparation of various cyclopentanyl and cyclopentenyl purine analogs which are useful as immunosuppressants and in the preparation of various prostaglandins.
Type:
Grant
Filed:
June 17, 1997
Date of Patent:
September 15, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Timothy T. Curran, David A. Hay, Jonathan C. Evans
Abstract: The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors.
Type:
Grant
Filed:
July 30, 1996
Date of Patent:
June 2, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Donald P. Matthews, Jeffrey S. Sabol, James R. McConnell, Richard E. Donaldson, Robert Duguid
Abstract: The present invention relates to a novel process for the preparation of 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones from 1-halo-3-trialkylsilanyl-benzenes. 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones are useful for the treatment of Alzheimer's disease and senile dementia. In addition, the present invention relates to a novel process for purifying 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones utilizing a novel extraction method.
Type:
Grant
Filed:
June 18, 1996
Date of Patent:
June 2, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Roberto Gandolfi, deceased, Dennis K. Klipa, Neal J. Fetner
Abstract: The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.
Type:
Grant
Filed:
November 1, 1996
Date of Patent:
April 14, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Thomas T. Ortyl, Paul F. Skultety, Kristen C. Mitchell, Deepak S. Phadke, Faraneh Attarchi, Marquerite L. Pierce, Aaron W. Schoeneman, Joseph M. Schnitz
Abstract: The present invention relates to a novel process for preparing cis-4-O-protected-substituted-2-cyclopentenol derivatives comprising, a) dissolving a 4-O-protected-2-cyclopentenone in a suitable organic solvent; and b) treating the solution with a suitable Lewis acid and a suitable reducing agent at a temperature of from about -100.degree. C. to about 20.degree. C. The cis-4-O-protected-substituted-2-cyclopentenol derivatives are useful intermediates in the preparation of various cyclopentanyl and cyclopentenyl purine analogs which are useful as immunosuppressants and in the preparation of various prostaglandins.
Type:
Grant
Filed:
February 1, 1996
Date of Patent:
March 17, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Timothy T. Curran, David A. Hay, Jonathan C. Evans
Abstract: Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
Type:
Grant
Filed:
February 26, 1997
Date of Patent:
March 17, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
David M. Fink, Barbara E. Kurys, Gregory M. Shutske, John D. Tomer, IV
Abstract: The present invention relates to a a novel process for preparing 5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones which have been shown to have antidepressant activity and are useful in the treatment of Wernicke-Korsakoff syndrome and Alzheimer's disease.
Type:
Grant
Filed:
March 28, 1997
Date of Patent:
March 3, 1998
Assignee:
Merrell Pharmaceuticals Inc
Inventors:
Sandra K. Stolz-Dunn, David H. Louks, Yolanda M. Puga, Christian T. Goralski
Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-vital agents.
Type:
Grant
Filed:
January 23, 1997
Date of Patent:
February 10, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
Abstract: This invention relates to compounds of the formula ##STR1## wherein X, Y, Z, m, n and p are as defined within, pharmaceutical compositions containing these compounds and to their use as antipsychotic agents, particularly in the treatment of schizophrenia. Depot derivatives of the compounds are useful for providing long acting effects of the compounds.
Type:
Grant
Filed:
June 27, 1996
Date of Patent:
December 9, 1997
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Mark G. Palermo, Lawrence L. Martin, Peter A. Nemoto