Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
Type:
Application
Filed:
March 17, 2008
Publication date:
September 25, 2008
Applicant:
Sepracor, Inc.
Inventors:
Brian M. Aquila, James R. Hauske, Liming Shao
Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.
Type:
Application
Filed:
May 15, 2008
Publication date:
September 11, 2008
Applicant:
SEPRACOR INC.
Inventors:
Mark G. Currie, Steven Jones, Charles M. Zepp
Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.
Type:
Grant
Filed:
May 3, 2006
Date of Patent:
September 9, 2008
Assignee:
Sepracor Inc.
Inventors:
Thomas Jerussi, Qun Kevin Fang, Mark G. Currie
Abstract: The present disclosure provides a unit dosage form with an anxiolytic dosage of zopiclone particularly eszopiclone. Also provided is a method for treatment or prophylaxis of anxiety using a subsedative dosage of zopiclone particularly eszopiclone.
Type:
Application
Filed:
December 1, 2007
Publication date:
July 24, 2008
Applicant:
Sepracor Inc.
Inventors:
Seth C. Hopkins, Mark A. Varney, Tushar Misra, Gary Maier, Judy Caron, Randall S. Wagner
Abstract: A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, a low incidence of the development of tolerance and an increased duration of action, as compared to racemic formoterol.
Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.
Type:
Grant
Filed:
November 14, 2006
Date of Patent:
June 24, 2008
Assignee:
Sepracor Inc.
Inventors:
Mark G. Currie, Steven Jones, Charles M. Zepp
Abstract: Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it which are usable as tranquillisers and hypnotics.
Abstract: This invention related to methods of treating, preventing and managing various pulmonary diseases or disorders using stereomerically pure (R,R)-formoterol in combination with other pharmacological agents such as leukotriene inhibitors and neurokinin receptor antagonists. Pharmaceutical compositions comprising (R,R)-formoterol and other pharmacological agents are also disclosed.
Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
Type:
Application
Filed:
January 14, 2008
Publication date:
May 15, 2008
Applicant:
SEPRACOR INC.
Inventors:
Gerald Tanoury, Chris Senanayaka, Donald Kessler
Abstract: A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, a low incidence of the development of tolerance and an increased duration of action, as compared to racemic formoterol.
Abstract: Compositions containing ?2 adrenergic agonists in combination with carbonates and carbamates of the formula and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.
Type:
Application
Filed:
July 13, 2007
Publication date:
May 1, 2008
Applicant:
SEPRACOR INC.
Inventors:
Mark G. Currie, Steve Jones, Paul Grover, Chris H. Senanayake, Q. Kevin Fang
Abstract: Imidazo[1,2-a]pyridines of the formulae I and II: are disclosed. The compounds are useful to treat anxiety and insomnia. Pharmaceutical compositions and methods are also disclosed.
Type:
Application
Filed:
October 28, 2004
Publication date:
April 24, 2008
Applicant:
Sepracor inc.
Inventors:
Q. Kevin Fang, Paul Grover, Thomas P. Jerussi
Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
Type:
Grant
Filed:
April 11, 2002
Date of Patent:
April 22, 2008
Assignee:
Sepracor, Inc.
Inventors:
Brian M. Aquila, James R. Hauske, Liming Shao
Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
Type:
Grant
Filed:
August 4, 2006
Date of Patent:
March 11, 2008
Assignee:
Sepracor Inc.
Inventors:
Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
Abstract: This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. Also provided are methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein Q is a member selected from O, S, CR1 and N, X and Y are members independently selected from CR2, O, S, N and NR3.
Type:
Application
Filed:
July 2, 2007
Publication date:
March 6, 2008
Applicant:
SEPRACOR INC.
Inventors:
Michele Heffernan, James Dorsey, Qun Fang, Robert Foglesong, Seth Hopkins, Michael Jones, Steven Jones, Cyprian Ogbu, Joe Perales, Mustapha Soukri, Kerry Spear, Mark Varney
Abstract: This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O?X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.
Type:
Application
Filed:
July 2, 2007
Publication date:
January 3, 2008
Applicant:
SEPRACOR INC.
Inventors:
Michele Heffernan, Robert Foglesong, Seth Hopkins, Mustapha Soukri, Steven Jones, Kerry Spear, Mark Varney
Abstract: This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O?X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl.
Type:
Application
Filed:
August 3, 2007
Publication date:
January 3, 2008
Applicant:
SEPRACOR INC.
Inventors:
James Dorsey, Michele Heffernan, Qun Fang, Robert Foglesong, Seth Hopkins, Cyprian Ogbu, Mustapha Soukri, Kerry Spear
Abstract: One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine.
Type:
Application
Filed:
June 11, 2007
Publication date:
December 27, 2007
Applicant:
SEPRACOR INC.
Inventors:
Karim Lalji, Timothy Barberich, Judy Caron, Thomas Wessel
Abstract: Treatment of pain disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful in treatment of pain disorders.
Type:
Application
Filed:
March 30, 2007
Publication date:
December 6, 2007
Applicant:
SEPRACOR INC.
Inventors:
Paul Michael Tarantino, Una Campbell, Larry Bush
Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.
Type:
Grant
Filed:
February 4, 2004
Date of Patent:
November 13, 2007
Assignee:
Sepracor, Inc.
Inventors:
Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao