Abstract: Described are piperidines of Formula I
and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
November 4, 2003
Assignee:
Warner-Lambert Company LLC
Inventors:
Brian Edward Kornberg, Russell Andrew Lewthwaite, David Manning, Sham Shridhar Nikam, Ian Leslie Scott
Abstract: A process of preparing compounds having the formula I:
or an optical isomer or racemic or optically active mixture thereof, which are useful as selective kappa-receptor agonists.
Type:
Grant
Filed:
April 26, 2002
Date of Patent:
September 23, 2003
Assignee:
Warner-Lambert Company LLC
Inventors:
Keith M. DeVries, Michel A. Couturier, Brian M. Andresen, John L. Tucker, Fumitaka Ito
Abstract: The present invention provides a method for measuring diacylglycerol acetyltransferase (DGAT) activity which utilizes a novel solvent system to reduce and/or eliminate the activities of related compounds.
The present invention also discloses a method for determining whether a compound is useful for modulating DGAT biological activity. The method is capable of being utilized for mass screening of compounds as modulators of the biological activity of DGAT.
Type:
Grant
Filed:
December 19, 2001
Date of Patent:
August 19, 2003
Assignee:
Warner-Lambert Company
Inventors:
Randy Ranjee Ramharack, Mark Allan Spahr
Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
Type:
Grant
Filed:
June 21, 2002
Date of Patent:
August 5, 2003
Assignee:
Warner-Lambert Company
Inventors:
Michael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
Abstract: Cyclic amino acids, such as gabapentin and pregabalin, are used for treating physiological conditions associated with the use, or sequelae of use, of cocaine or other psychomotor stimulants and other addictive drugs/substances. Physiological conditions include stimulant-induced toxicities.
Type:
Grant
Filed:
August 29, 2000
Date of Patent:
May 20, 2003
Assignee:
Pfizer Inc.
Inventors:
Hyacinth Chi Akunne, Ann Elizabeth Corbin, David James Dooley, Alysia Latrese Green, Thomas Gary Heffner
Abstract: Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof,
wherein
R1 is hydrogen, lower alkyl, COOR7, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl, or (un)substituted heteroarylalkyl;
R3 is hydrogen or lower alkyl;
R2, R4, R5, and R6 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, nitro, amino, mono- or dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, sulfamoyl, trifluoromethyl, or alkylthio;
R7 is hydrogen or lower alkyl; and
R8 is hydrogen or oxo.
Also provided is a method for selectively antagonizing the M4 muscarinic receptor and a method for treating Parkinson's disease.
Type:
Grant
Filed:
September 14, 2001
Date of Patent:
December 31, 2002
Assignee:
Warner-Lambert Company
Inventors:
Corinne Elizabeth Augelli-Szafran, Thomas M. Boehme
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Type:
Grant
Filed:
January 25, 2001
Date of Patent:
December 17, 2002
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
Abstract: Novel substituted amino acids of formula
are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
Type:
Grant
Filed:
August 8, 2001
Date of Patent:
December 3, 2002
Assignee:
Warner-Lambert Company
Inventors:
Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonist,
where R is aryl, R1 and R2 are H or alkyl, m, n and q are integers from 0 to 4, X is NR8 or NHCONH, R3 and R9 are H or alkyl, R4 is naphthyl or indolyl, R5 and R2 are H or alkyl, and R6 is aryl.
The compounds are useful agents for treating inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia and emesis.
Type:
Grant
Filed:
June 18, 2001
Date of Patent:
October 29, 2002
Assignee:
Warner-Lambert Company
Inventors:
Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Type:
Grant
Filed:
September 18, 2000
Date of Patent:
October 22, 2002
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
Abstract: The present invention provides compounds that block calcium channels and have the Formula I:
The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
Type:
Grant
Filed:
October 25, 1999
Date of Patent:
October 1, 2002
Inventors:
David Thomas Connor, Lain-Yen Hu, Thomas Charles Malone, Michael Francis Rafferty, Bruce David Roth, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
Abstract: (−)E-2-(3,4-dichlorocinnamyl)-1-cyclo-propylmethyl-piperidine of formula I:
and its pharmaceutically acceptable salts, is useful for treating diarrhea in mammals. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula I.
Type:
Grant
Filed:
November 10, 1999
Date of Patent:
August 27, 2002
Assignee:
Warner-Lambert Company
Inventors:
Alain Calvet, Maria Chovet, Svein Dahl, Henry Jacobelli, Vassilia Theodorou, Pierre Riviere
Abstract: The instant invention is a novel series of amino heterocycles useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, and sleep disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
August 20, 2002
Assignee:
Warner-Lambert Company
Inventors:
Thomas Richard Belliotti, Andrew John Thorpe, David Juergen Wustrow
Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
Type:
Grant
Filed:
June 4, 2001
Date of Patent:
August 13, 2002
Assignee:
Warner-Lambert Company
Inventors:
Michael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
Abstract: GABA analogs are useful to prevent and treat gastrointestinal damage and ethanol withdrawal syndrome. Preferred treatments employ gabapentin or pregabalin.
Type:
Grant
Filed:
March 13, 2001
Date of Patent:
July 30, 2002
Assignees:
Warner-Lambert Company, University of Oklahoma
Inventors:
Lionel Bueno, Maria Chovet, Laurent Diop, Antonio Guglietta, Hilary J. Little, Michael Francis Rafferty, Jiayuan Ren, Charles Price Taylor, Jr., William Patrick Watson
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Inventors:
Richard John Booth, Louis Brogley, Wayne Livingston Cody, David Thomas Connor, Harriet Wall Hamilton, John Xiaoqiang He, Lain-Yen Hu, Leonard Joseph Lescosky, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Bruce David Roth, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
Abstract: The present invention relates to a method of purifying 1,3,5-triisopropylbenzene that comprises combining inpure 1,3,5-triisopropylbenzene with a sulfonating agent to form a reaction mixture, mixing the reaction mixture at a temperature in the range of about 0° C. to about 50° C., and collecting the purified 1,3,5-triisopropylbenzene.
Type:
Grant
Filed:
July 29, 1999
Date of Patent:
June 4, 2002
Assignee:
Warner-Lambert Company
Inventors:
Gretchen Crumbaugh, Dieter Schweiss, Jonathan Charles Walker
Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.