Patents Represented by Attorney, Agent or Law Firm Elizabeth M. Anderson
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Patent number: 6043241Abstract: Compounds of the Formula I ##STR1## are nonpeptide antagonists of endothelin which are useful in treating a variety of diseasses such as elevated levels of endothelin, acute respiratory distress syndrome (ARDS), atherosclerosis, restenosis, Raynaud's phenomenon etc. The compounds are prepared by reacting an alpha-hydroxy butenolide with one or more equivalents of a suitable base, and exposing the solution to UV light.Type: GrantFiled: July 31, 1998Date of Patent: March 28, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, Timothy Robert Hurley, Michael James Lovdahl, William Chester Patt, Joseph Thomas Repine
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Patent number: 6040479Abstract: The present invention is concerned with an improved process for the resolution of racemic 2-(o-chlorophenyl)-2-methylaminocyclohexanone (ketamine).Type: GrantFiled: November 10, 1998Date of Patent: March 21, 2000Assignees: Goedecke Aktiengesellschaft, Cu Chemie Uetikon GmbHInventors: Klaus Steiner, Stefan Gangkofner, Jean-Marie Grunenwald
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Patent number: 6040316Abstract: The small nonpeptides of the instant invention are tachykinin antagonists of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein: R.sub.1 is straight or branched alkyl of from 5 to 15 carbon atoms, aryl, or heteroaryl;R.sub.2 is hydrogen, hydroxy, amino, or thiol;R.sub.3 is aryl, arylsulfonylmethyl, or saturated or unsaturated heterocycle;R.sub.4 is from 1 to 4 groups each independently selected from halogen, alkyl, hydroxy, and alkoxy;n is an integer of from 2 to 6; and the carbon atom of (CH.sub.2).sub.n group can be replaced by oxygen, nitrogen, or sulphur. The compounds are highly selective and functional NK.sub.3 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: GrantFiled: January 22, 1998Date of Patent: March 21, 2000Assignee: Warner-Lambert CompanyInventors: Michael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
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Patent number: 6020370Abstract: Bridged cyclic amino acids of formula ##STR1## 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: GrantFiled: May 19, 1998Date of Patent: February 1, 2000Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, Justin S. Bryans, Clare O. Kneen, Andrew I. Morrell, Giles S. Ratcliffe
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Patent number: 6020519Abstract: The diphenyl-cyclopropene derivatives of the instant invention are kappa opioids useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome, and stroke.The compounds are K-agonists which are centrally acting and peripherally selective acting.Type: GrantFiled: May 7, 1999Date of Patent: February 1, 2000Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Verity Sabin
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Patent number: 6017951Abstract: Novel nonpeptides characterized as having a carbamic group which are antagonists of endothelin I are described, as well as methods for their preparation and pharmaceutical compositions containing the same. The compounds are useful in treating elevated levels of endothelin and are therefore useful in the treatment of hypertension, myocardial infarction, diabetes, cerebral vasospasm, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythminas, asthma, chronic and acute renal failure, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, stroke, head injury, and ischemic bowel syndrome.Type: GrantFiled: February 10, 1999Date of Patent: January 25, 2000Assignee: Warner-Lambert CompanyInventors: William C. Patt, Bill R. Reisdorph, Joseph T. Repine
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Patent number: 6017916Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.Type: GrantFiled: January 22, 1997Date of Patent: January 25, 2000Assignee: Warner-Lambert CompanyInventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
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Patent number: 6017905Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein Ar and Ar.sup.1 are each independently selected from unsubstituted or substituted phenyl which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl;X is --NH--, --O--, --S--, or --(CH.sub.2).sub.0-4 --, andR is hydrogen, alkyl, or phenyl.Type: GrantFiled: June 9, 1998Date of Patent: January 25, 2000Assignee: Warner-Lambert CompanyInventors: William Howard Roark, Bruce David Roth
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Patent number: 6015800Abstract: A novel series of substituted quinoxaline 2-ones 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.Type: GrantFiled: May 15, 1998Date of Patent: January 18, 2000Assignee: Warner-Lambert CompanyInventor: Sham Shridhar Nikam
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Patent number: 6011052Abstract: Pyrazolone derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammatory diseases or conditions, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## where: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 can be independently H,C.sub.1-20 alkyl,C.sub.5-7 cycloalkyl,--(CH.sub.2).sub.n NR.sub.6 R.sub.7--(CH.sub.2).sub.0-6 CONR.sub.6 R.sub.7,--(CH.sub.2).sub.n OH or--(CH.sub.2).sub.0-6 CO.sub.2 R.sub.11,biphenyl,aryl of from 6 to 10 carbon atoms, oraryl of from 6 to 10 carbon atoms substituted up to 3 times by halogen, --CN, lower alkyl of from 1-4 carbon atoms, --OH, nitro, --SO.sub.2 H, SO.sub.2 lower alkyl,--SO.sub.2 NR.sub.6 R.sub.7 lower alkoxy--C0.sub.2 R.sub.11,--CONR.sub.6 R.sub.7,--NR.sub.6 R.sub.7 or CH.sub.2 OH.Type: GrantFiled: April 25, 1997Date of Patent: January 4, 2000Assignee: Warner-Lambert CompanyInventors: Janak Khimchand Padia, Bruce David Roth, John Edward Strode, Bharat Kalidas Trivedi
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Patent number: 6005103Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: December 21, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Elizabeth Lunney, Kimberly Suzanne Para, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
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Patent number: 6001876Abstract: The instant invention is a method of using certain analogs of glutamic acid and gamma-aminobutyric acid in pain therapy.Type: GrantFiled: July 15, 1998Date of Patent: December 14, 1999Assignee: Warner-Lambert CompanyInventor: Lakhbir Singh
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Patent number: 5998435Abstract: The instant invention is directed to a method for the treatment of emesis comprising administering the compound [R,S]-[2-(1H-Indol-3-yl)-1-methyl-1-(1-phenyl-ethylcarbamoly)-ethyl]-carba mic acid benzofuran-2ylmethyl ester.Type: GrantFiled: December 1, 1998Date of Patent: December 7, 1999Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, John Hughes, Martyn Clive Pritchard, Lakhbir Singh
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Patent number: 5998468Abstract: Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prostatic hyperplasia (BPH), and diabetes.Type: GrantFiled: December 15, 1997Date of Patent: December 7, 1999Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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Patent number: 5981755Abstract: The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.Type: GrantFiled: October 8, 1998Date of Patent: November 9, 1999Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
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Patent number: 5968928Abstract: The invention discloses novel fused-azacylic quinoxalinediones. These compounds may be employed as excitatory amino acid antagonists and as analogs for use in immunological assays. The invention is also directed to both a radioimmunoassay and enzyme immunoassay for detecting and quantitating 1,4,7,8,9,10,-hexahydro-9-methyl-6-nitropyrido[3,4-f]-quinoxaline-2,3-dion e PNQX and analogs thereof.Type: GrantFiled: August 11, 1997Date of Patent: October 19, 1999Assignee: Warner-Lambert CompanyInventors: Christopher Franklin Bigge, Gerald David Nordblom, Chung Stephen Yi
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Patent number: 5968968Abstract: Diphenyl-cyclopropene derivatives, their nontoxic, pharmaceutically acceptable acid addition salts and compositions are kapa opiods useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome and stroke.Type: GrantFiled: December 8, 1998Date of Patent: October 19, 1999Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Verity Sabin
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Patent number: 5958950Abstract: A method for the treatment of inflammatory disease or condition atherosclerosis or restenosis or for inhibiting 15 lipaxygenase in a mammal in need thereof comprising administering to such mammal an effect amount of a compound of Formula I ##STR1##Type: GrantFiled: February 5, 1998Date of Patent: September 28, 1999Assignee: Warner-Lambert CompanyInventors: Janak Khimchand Padia, Bruce David Roth, Bharat Kalidas Trivedi
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Patent number: 5945440Abstract: The present invention is concerned with the use of indolocarbazole imides of the general formula (I): ##STR1## for the preparation of pharmaceutical compositions for the treatment and/or prevention of cancer, virus diseases (for example HIV infections), heart and blood vessel diseases (for example high blood pressure, thromboses, heart rhythm disturbances and atheroscleroses), bronchopulmonary diseases, degenerative diseases of the central nervous system (for example Alzheimer's disease), inflammatoryl diseases (for example rheumatism and arthritis), diseases of the immune system (for example allergies), as well as psoriasis and for use as immune suppressives; as well as new compounds of general formula (I).Type: GrantFiled: May 7, 1998Date of Patent: August 31, 1999Assignee: Goedecke AktiengesellschaftInventors: Jurgen Kleinschroth, Christoph Schachtele, Johannes Hartenstein, Claus Rudolph, Hubert Barth, Julian Aranda, Hans Jurgen Betche
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Patent number: 5936128Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.Type: GrantFiled: May 15, 1998Date of Patent: August 10, 1999Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Elizabeth Lunney, Bradley Dean Tait