Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
Type:
Grant
Filed:
July 2, 2008
Date of Patent:
November 23, 2010
Assignee:
Allergan, Inc.
Inventors:
Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gill, John E. Donello, Michael E. Garst, Larry A. Wheeler
Abstract: Substituted 2-aminotetralin derivatives as selective alpha 2B agonists can be incorporated in a pharmaceutical composition and can be used in methods of treating an alpha 2B receptor mediated diseases or conditions. The compounds are represented by Formula 1: wherein R1=H, methyl, ethyl, propyl, or cyclobutyl; R2=methyl or H; R3=pyridinyl X=C or O.
Type:
Grant
Filed:
January 9, 2008
Date of Patent:
November 9, 2010
Assignee:
Allergan, Inc.
Inventors:
John R. Cappiello, Dario G. Gomez, Ken Chow, Michael E. Garst, Daniel W. Gil, Larry A. Wheeler
Abstract: Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists and partial agonists of the 2c subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Type:
Grant
Filed:
October 21, 2004
Date of Patent:
June 1, 2010
Assignee:
Wyeth LLC
Inventors:
Jonathan Laird Gross, Gary Paul Stack, Hong Gao
Abstract: The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
Type:
Grant
Filed:
December 12, 2007
Date of Patent:
May 18, 2010
Assignee:
Wyeth LLC
Inventors:
Joel Adam Goldberg, Andrew Fensome, Casey Cameron McComas, Puwen Zhang
Abstract: The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
March 30, 2010
Assignee:
Wyeth LLC
Inventors:
Casey Cameron McComas, Puwen Zhang, Eugene Anthony Terefenko, An Thien Vu, Stephen Todd Cohn
Abstract: Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agorophobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.
Type:
Grant
Filed:
July 13, 2006
Date of Patent:
March 30, 2010
Assignee:
Wyeth LLC
Inventors:
Syed M. Shah, Mahdi B. Fawzi, Panolil Raveendranath, Eric C. Ehrnsperger
Abstract: Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
Abstract: The present invention is directed to arylamino-arylpropanolamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
October 2, 2007
Date of Patent:
March 2, 2010
Assignee:
Wyeth LLC
Inventors:
An Thien Vu, Stephen Todd Cohn, Eugene Anthony Terefenko, William Jay Moore, Puwen Zhang, Paige Erin Mahaney, Eugene John Trybulski
Abstract: The present invention relates to methods for synthesizing compounds useful as 5HT2C agonists or partial agonists, derivatives thereof, and to intermediates thereto.
Type:
Grant
Filed:
July 24, 2006
Date of Patent:
March 2, 2010
Assignee:
Wyeth LLC
Inventors:
Sreenivasulu Megati, Anita Wai-Yin Chan, Gregg B. Feigelson
Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.
Type:
Grant
Filed:
January 12, 2007
Date of Patent:
January 12, 2010
Assignee:
Wyeth LLC
Inventors:
Robert E. McDevitt, Yanfang Li, Albert J. Robichaud, Gavin D. Heffernan, Richard D. Coghlan, Ronald C. Bernotas
Abstract: A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described.
Type:
Grant
Filed:
December 4, 2006
Date of Patent:
November 3, 2009
Assignee:
Wyeth
Inventors:
Paige Erin Mahaney, Madelene Miyoko Antane, Jerry Shunneng Sun
Abstract: The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
Type:
Grant
Filed:
December 12, 2007
Date of Patent:
October 13, 2009
Assignee:
Wyeth
Inventors:
Casey Cameron McComas, Stephen Todd Cohn, Andrew Fensome, Joel Adam Goldberg, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, Jr., Puwen Zhang
Abstract: The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 13, 2009
Assignee:
Wyeth
Inventors:
Casey Cameron McComas, Puwen Zhang, Eugene John Trybulski, An Thien Vu, Eugene Anthony Terefenko
Abstract: Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agoraphobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.
Type:
Grant
Filed:
July 13, 2006
Date of Patent:
September 29, 2009
Assignee:
Wyeth
Inventors:
Syed M. Shah, Mahdi B. Fawzi, Eric C. Ehrnsperger, Panolil Raveendranath