Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
Type:
Grant
Filed:
November 2, 2000
Date of Patent:
March 4, 2003
Assignee:
Warner-Lambert Company
Inventors:
Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
Abstract: The present invention related to novel dihydropyrones possessing 3-position nitrogen atom, which inhabit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections, and diseases, including AIDS.
Type:
Grant
Filed:
August 17, 2000
Date of Patent:
January 28, 2003
Assignee:
Warner-Lambert Company
Inventors:
Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
Abstract: The invention concerns cholecystokinin (CCK) antagonists useful in the treatment of cognitive disorders. Especially useful are CCKB antagonists such as CI-988.
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: 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: Benzo[de]isoquinoline-1,3-diones which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents are described as well as methods for their preparation and formulation. Novel intermediates useful in the preparation of the final products are also described.
Type:
Grant
Filed:
August 11, 2000
Date of Patent:
March 26, 2002
Assignee:
Warner-Lambert Company
Inventors:
Albert Kudzoi Amegadzie, Maureen Elizabeth Carey, John Michael Domagala, Liren Huang, Ronald George Micetich, Joseph Peter Sanchez, Rajeshwar Singh, Michael Andrew Stier, Arkadii Vaisburg
Abstract: Described are neuroprotective agents of Formula I
wherein
R is an amino acid or nitrogen heterocyclic ring which is saturated or unsaturated of from 5 to 8 members which may have additional oxygen or sulfur atoms therein. The other provisions or substituents are described in the specification.
Type:
Grant
Filed:
November 25, 1998
Date of Patent:
January 22, 2002
Assignee:
Warner-Lambert Company
Inventors:
Brian Edward Kornberg, Sham Shridhar Nikam, Michael Francis Rafferty
Abstract: The invention is a series of 7-substituted quinazolin-2,4-diones useful as antibacterial agents, processes for the preparation of the compounds, and a pharmaceutical composition containing one or more of the compounds.
Type:
Grant
Filed:
March 15, 2000
Date of Patent:
December 18, 2001
Assignee:
Warner-Lambert Company
Inventors:
John Michael Domagala, Edmund Lee Ellsworth, Liren Huang, Thomas Eric Renau, Rajeshwar Singh, Michael Andrew Stier
Abstract: Novel nonpeptide endothelin I antagonists of Formula
are described wherein R1 is unsubstituted or substituted cycloalkyl, phenyl, naphthyl or heteroaryl, R2 is unsubstituted or substituted alkyl, aryl or heteroaryl, R3 is unsubstituted or substituted alkyl, cycloalkyl, aryl or heteroayl, and R1 and/or R2 and/or R3 are independently substituted by a total of from 1 to 4 substituents which enhance aqueous solubility with the proviso that when R2 is alkyl and is substituted, the substituent is not oxygen at the &agr;-position of the furanone ring.
Type:
Grant
Filed:
August 4, 1998
Date of Patent:
October 2, 2001
Assignee:
Warner-Lambert Company
Inventors:
Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
Abstract: Dyskinesias in humans are treated by administering a therapeutically effective dose of an NR1A/2B site-selective NMDA receptor antagonist compound to a human suffering therefrom.
Abstract: A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.
Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1
The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
Type:
Grant
Filed:
December 8, 1999
Date of Patent:
July 24, 2001
Assignee:
Warner-Lambert Company
Inventors:
Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
Abstract:
The instant invention provides aqueous soluble prodrugs of formula (I) or a pharmaceutically acceptable salt thereof wherein R is —CH2OZ, —C(═O)OCH2OZ or Z, wherein Z is formula (a), —P(═O)(OH)2 or —C(═O)Q: n is an integer of from 0 to 3; m is an integer of from 0 to 1, of certain tachykinin antagonists (NK1 antagonists) useful in the treatment of emesis.
Type:
Grant
Filed:
August 3, 2000
Date of Patent:
July 10, 2001
Assignee:
Warner-Lambert Company
Inventors:
Michael Huai Gu Chen, Om Prakash Goel, Fred M. Hershenson, Zhijian Zhu, Oilun Helen Chan
Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1
The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
Type:
Grant
Filed:
August 7, 2000
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert Company
Inventors:
Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
Abstract:
Branched alkyl pyrrolidines of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropatnological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
Type:
Grant
Filed:
October 13, 2000
Date of Patent:
June 12, 2001
Assignee:
Warner-Lambert Company
Inventors:
Justin Stephen Bryans, Ihoezo Victor Ekhato, David Christopher Horwell, Rong Ling, Jean-Marie Receveur, David Juergen Wustrow
Abstract: This invention is for low molecular weight dendritic polymers (dendroids) of Formula I
are useful as agents in the treatment of cancer, Alzheimers disease, thrombosis, inflammatory diseases, and bacterial resistance.
Type:
Grant
Filed:
February 4, 1999
Date of Patent:
May 1, 2001
Assignee:
Warner-Lambert Company
Inventors:
David Christopher Horwell, Giles Stuart Ratcliffe
Abstract: The compounds of the instant invention are novel compounds of Formula I
or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.
Type:
Grant
Filed:
February 3, 1999
Date of Patent:
February 27, 2001
Assignee:
Warner-Lambert Company
Inventors:
David Christopher Horwell, Martyn Clive Pritchard
Abstract: A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.