Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
Type:
Grant
Filed:
April 9, 1997
Date of Patent:
January 19, 1999
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
Type:
Grant
Filed:
April 8, 1997
Date of Patent:
January 19, 1999
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
Type:
Grant
Filed:
April 8, 1997
Date of Patent:
January 19, 1999
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
Abstract: The present invention provides a method for treating a condition associated with muscarinic receptor modulation using a 3-?4-(butylthio)-1,2,5-thiadiazol-3-yl!-1-azabicyclo-?2.2.2!octane transdermal formulation. The invention provides desired transdermal 3-?4-(butylthio)-1,2,5-thiadiazol-3-yl!-1-azabicyclo?2.2.2!octane patch formulations.
Type:
Grant
Filed:
August 25, 1997
Date of Patent:
January 12, 1999
Assignee:
Eli Lilly and Company
Inventors:
Franklin Porter Bymaster, Harlan E. Shannon, Lisa A. Shipley, Kirti H. Valia
Abstract: The present invention relates to therapeutically active heterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
October 13, 1998
Assignee:
Eli Lilly and Company
Inventors:
Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward
Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
October 13, 1998
Assignee:
Eli Lilly and Comany
Inventors:
Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno -?2,3-b!?1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.
Type:
Grant
Filed:
November 13, 1996
Date of Patent:
October 6, 1998
Assignees:
Eli Lilly and Company, Eli Lilly and Company Limited
Inventors:
Jiban Kumar Chakrabarti, Terrence Micharl Hotten, David Edward Tupper
Abstract: This invention provides methods for the treatment or prevention of cerebral focal ischemia 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:
October 6, 1998
Assignee:
Eli Lilly and Company
Inventors:
Jerome H. Fleisch, William T. Jackson, Jason S. Sawyer
Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-?2,3-b!?1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders relating to the use of psychoactive substances.
Type:
Grant
Filed:
November 13, 1996
Date of Patent:
October 6, 1998
Assignees:
Eli Lilly and Company, Eli Lilly and Company Limited
Inventors:
Charles M. Beasley, Jr., Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-?2,3-b!?1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of mental disorders.
Type:
Grant
Filed:
November 13, 1996
Date of Patent:
October 6, 1998
Assignees:
Eli Lilly and Company, Eli Lilly and Company Limited
Inventors:
Charles M. Beasley, Jr., Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
Abstract: A method of protecting a warm-blooded mammal from the progression of Alzheimer's disease, which comprises administering an effective amount of a compound of general formula. ##STR1## in which: R.sup.1 represents an optionally substituted aromatic or heteroaromatic group;L.sup.1 and L.sup.2 each independently represents a bond or an unbranched (1-4C) alkylene group, which alkylene group may optionally bear a (1-4C) alkyl, phenyl or phenyl (1-2C) alkyl substituent;one of Y.sup.1 and Y.sup.2 represents NR.sup.3 and the other represents O, S or NR.sup.3, in which R.sup.3 represent hydrogen, hydroxyl, (1-4C) alkoxy, (1-4C) alkyl or di (1-4C) alkylamino;Z represents O or S; andR.sup.2 represents (3-8C) cycloalkyl, heterocyclyl, and optionally substituted aromatic or heteroaromatic group, or together with L.sup.2, (1-10C) alkyl;or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 2, 1995
Date of Patent:
September 29, 1998
Assignee:
Eli Lilly and Company
Inventors:
Lawrence J. Heinz, Jill A. Panetta, Michael L. Phillips, Jon K. Reel, John K. Shadle, Richard L. Simon, Celia A. Whitesitt
Abstract: A series of hetero-oxy alkanamines 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. 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:
June 6, 1995
Date of Patent:
August 4, 1998
Assignee:
Eli Lilly Company
Inventors:
James E. Audia, David J. Hibschman, Joseph H. Krushinski, Jr., Thomas E. Mabry, Jeffrey S. Nissen, Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson, David T. Wong
Abstract: The present invention relates to a process for making intermediates useful for preparing therapeutically active azacyclic or azabicyclic compounds.
Abstract: The invention provides a method for treating fungal dermatitis comprising administering an effective amount of 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno?2,3-b!?1,5!benzodiazepine to a patient in need thereof.