Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.
Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
Type:
Application
Filed:
January 5, 2007
Publication date:
August 30, 2007
Applicant:
SEPRACOR INC.
Inventors:
Liming Shao, Fengjiang Wang, Scott Malcolm, Michael Hewitt, Larry Bush, Jianguo Ma, Mark Varney, Una Campbell, Sharon Engel, Larry Hardy, Patrick Koch, John Campbell
Abstract: The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.
Type:
Application
Filed:
December 21, 2006
Publication date:
August 23, 2007
Applicant:
SEPRACOR INC.
Inventors:
Liming Shao, Fengjiang Wang, Scott Malcolm, Michael Hewitt, Larry Bush, Mark Varney, Una Campbell, Sharon Engel, Larry Hardy, Patrick Koch, Jianguo Ma
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:
Grant
Filed:
February 28, 2006
Date of Patent:
August 7, 2007
Assignee:
Sepracor Inc.
Inventors:
Mark G. Currie, Steve Jones, Paul Grover, Chris H. Senanayake, Q. Kevin Fang
Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.
Abstract: Methods are disclosed utilizing DCL, a metabolic derivative of loratadine, for the treatment of allergic rhinitis, and other disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines.
Type:
Grant
Filed:
March 16, 1998
Date of Patent:
May 8, 2007
Assignee:
Sepracor Inc.
Inventors:
A. K. Gunnar Aberg, John R. McCullough, Emil R. Smith
Abstract: Methods are disclosed utilizing DCL, a metabolic derivative of loratadine, for the treatment of allergic rhinitis, and other disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines.
Type:
Grant
Filed:
November 17, 2004
Date of Patent:
May 8, 2007
Assignee:
Sepracor Inc.
Inventors:
A. K. Gunnar Aberg, John R. McCullough, Emil R. Smith
Abstract: Methods are disclosed utilizing DCL, a metabolic derivative of loratadine, for the treatment of allergic rhinitis, and other disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines.
Type:
Grant
Filed:
November 23, 1999
Date of Patent:
May 1, 2007
Assignee:
Sepracor Inc.
Inventors:
A. K. Gunnar Aberg, John R. McCullough, Emil R. Smith
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:
November 14, 2006
Publication date:
March 15, 2007
Applicant:
Sepracor Inc.
Inventors:
Mark Currie, Steven Jones, Charles Zepp
Abstract: The invention is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.
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:
September 15, 2006
Publication date:
February 22, 2007
Applicant:
SEPRACOR INC.
Inventors:
Kevin Fang, Paul Grover, Thomas Jerussi
Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein Z1 is N or CR3; Z2 is N or CR4; Z3is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.
Type:
Grant
Filed:
December 28, 2004
Date of Patent:
January 23, 2007
Assignee:
Sepracor Inc.
Inventors:
Q Kevin Fang, Seth Hopkins, Michele Heffernan, Milan Chytil, Peter Wipf
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:
Grant
Filed:
October 28, 2004
Date of Patent:
December 12, 2006
Assignee:
Sepracor Inc.
Inventors:
Kevin Fang, Paul Grover, Thomas P. Jerussi
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:
February 7, 2005
Date of Patent:
December 5, 2006
Assignee:
Sepracor Inc.
Inventors:
Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
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:
August 4, 2006
Publication date:
November 23, 2006
Applicant:
SEPRACOR INC.
Inventors:
Gerald Tanoury, Chris Senanayake, Donald Kessler
Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Type:
Grant
Filed:
June 26, 2003
Date of Patent:
November 7, 2006
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
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:
January 7, 2004
Date of Patent:
October 31, 2006
Assignee:
Sepracor Inc.
Inventors:
Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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: One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize $gm opioid receptors.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
October 3, 2006
Assignee:
Sepracor Inc.
Inventors:
Paul E. Persons, Joanne M. Holland, James Hauske