Patents Represented by Attorney George Tarnowski
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Certain 3,3'-[[[(2-phenyl-4-thiazolyl)methoxy]phenyl]methylene]dithiobis-propano ic acid derivatives
Patent number: 5103014Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is --(CH.sub.2).sub.n O--, --(CH.sub.2).sub.n S--, ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or --O--, --S-- or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluroloweralkyl, polyfluroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen lower alkyl, --COOR.sup.4 or ##STR9## R.sup.7 is OR.sup.4 or N(R.sup.4).sub.2 ; R.sup.8 is OR.sup.4 or N(R.sup.4).sub.2 ;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstruction airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, as antiinflammatory agents.Type: GrantFiled: May 18, 1990Date of Patent: April 7, 1992Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III, James A. Nelson -
Patent number: 5084460Abstract: This invention provides 3-quinuclidinyl benzamides which in the form of pharmaceutical compositions have utility as therapeutic agents which exhibit anxiolytic antipsychotic and cognitive improving effects in warm blooded animals.Illustrative of an invention compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-4-dimethylamino-2-hydroxythiobenz amide: ##STR1## or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 24, 1990Date of Patent: January 28, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Harry R. Munson, Jr., Gunnar E. Jagdmann, Jr.
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Quinoline substituted naphthalenepropionic acid derivatives as anti-inflammatory/antiallergic agents
Patent number: 5084575Abstract: There are disclosed compounds of the formula ##STR1## wherein a is alkyl 3-19 carbon atoms, diloweralkyl allyl, diahaloallyl, diphenylallyl, lower alkynyl, ##STR2## W is --CR.sub.2 O--, --CH.dbd.CH-- or --CH.dbd.CHCH.sub.2 O-- X is N or CR;Z is ##STR3## R is hydrogen or lower alkyl; Y is ##STR4## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, optionally substituted by halo;R.sup.3 is --OR, ##STR5## -- NHSO.sub.2 R.sup.4 ; R.sup.4 is phenyl or loweralkyl substituted phenyl;R.sup.5 is halo;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as alelrgic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.Type: GrantFiled: September 6, 1990Date of Patent: January 28, 1992Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III., John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak, Annette L. Banker -
Patent number: 5075303Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.Type: GrantFiled: April 6, 1990Date of Patent: December 24, 1991Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
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Patent number: 5071988Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is ##STR1## n is 1-2; B is ##STR2## wherein R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro; ##STR3## R.sup.8 is lower alkyl; m is 0-3;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated nasobronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.Type: GrantFiled: February 27, 1991Date of Patent: December 10, 1991Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah
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Patent number: 5070207Abstract: There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma, psoriasis, inflammatory bowel disease and inflammation in mammals which comprises administering to a mammal so afflicted an effective amount of a compound having the formula: ##STR1## wherein Z is a group having the formula ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl of 1-20 carbon atoms, halo, halo lower alkyl, halo lower alkoxy, lower alkoxy, halo lower alkylsulfonyl, nitro or trifluoromethyl, where at least one of R.sup.3 and R.sup.4 is other than hydrogen;R.sup.5 is hydrogen, lower alkyl or halo;A is --CH.sub.2 --, --O-- or --S--;m is 0-10;n is 1-8;X is hydrogen, fluoro, lower alkyl or aralkyl of 7-12 carbon atoms;or a pharmacologically acceptable salt thereof.Type: GrantFiled: April 26, 1990Date of Patent: December 3, 1991Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Gregory F. Von Burg
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Patent number: 5070095Abstract: Novel 1-(azabicyclo[2.2.2]oct-3- or -4-yl)benzamides substituted on the benzene ring with the basic substituted aminomethyleneamino group have been found to be useful in treating emesis, including emesis due to chemical and radiation anticancer therapy, anxiety, and impaired gastric emptying. These compounds are represented by Formula I below.Type: GrantFiled: December 12, 1990Date of Patent: December 3, 1991Assignee: A. H. Robins Company, IncorporatedInventors: Gunnar E. Jagdmann, Jr., Harry R. Munson, Jr.
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Patent number: 5068104Abstract: Methods and compositions are disclosed for vaccinating warm-blooded animals against coccidiosis utilizing suspensions of excysted coccidial sporozoites in physiologically balanced medium containing water-soluble polymeric stabilizers selected from gels, gelatins, polysaccharide gums, cellulose or cellulose derivatives which extend viability or storage, additional extension of viability in storage being attained when the suspensions are finely divided and the polymeric stabilizers are hardened to form microcapsules.Prior to administration, the microcapsule is treated with a chelating agent in order to provide greater efficiency and speed of sporozoite release from the microcapsule and thus improved innoculation against oocyst challenge when compared with microcapsules which have not been treated with a chelating agent.Type: GrantFiled: August 1, 1988Date of Patent: November 26, 1991Assignee: A. H. Robins Company IncorporatedInventors: Balbir S. Bhogal, Michael G. Williams, Glenn A. Miller
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Patent number: 5066671Abstract: There are disclosed a method for the treatment or prevention of immunoinflammatory conditions by administering to a mammal an effective amount of a compound having the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, aryl, or ##STR2## X is alkyl, aryl, or -NR.sup.5 R.sup.6 ; R.sup.5 and R.sup.6 are each independently hydrogen, alkyl, or aryl; aryl is ##STR3## where the dotted line represents an optional double bond; R.sup.7, and R.sup.8 and R.sup.9 are each, independently, hydrogen, alkyl, hydroxy, alkoxy, carbalkoxy, halo, nitro, amino, cyano, trifluoromethyl, or a carboxylic acid;n=1-3;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 16, 1990Date of Patent: November 19, 1991Assignee: American Home Products CorporationInventor: Craig E. Caufield
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Patent number: 5053508Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 taken together represent ##STR2## R.sup.3 and R.sup.4 are hydrogen; R.sup.5 is 2-pyridinyl, 2-pyrazinyl, 2-pyrimidinyl, 3-pyridazinyl or any of the foregoing R.sup.5 moieties substituted by lower alkyl, lower alkoxy, halo lower alkyl, cyano, nitro or halo;X, Y and Z are, independently, N, S, O, NR.sup.6, SO, SO.sub.2, CR.sup.6 or CH.sub.2 ;A is lower alkylene, O or S;R.sup.6 is hydrogen, lower alkyl, aryl, aralkyl;m is 3-7;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/-anxiolytic agents having a low liability for extrapyramidal side effects.Type: GrantFiled: March 9, 1990Date of Patent: October 1, 1991Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Magid A. Abou-Gharbia, Charles Lin
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Patent number: 5026854Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 which is optionally present represents single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.Type: GrantFiled: August 8, 1990Date of Patent: June 25, 1991Assignee: John Wyeth & Brother LimitedInventor: Robin G. Shepherd
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Patent number: 5021576Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydroxy, lower alkoxy or lower alkoxyamino;R.sup.1 is hydrogen or A(CH.sub.2).sub.n O--;R.sup.2 is hydrogen or A(CH.sub.2).sub.n O--, with the proviso that one of R.sup.1 and R.sup.2 is A(CH.sub.2).sub.n O-- and the other is hydrogen;n is 1-2;A is phenoxyethyl, phenoxyphenyl or a group having the formula ##STR2## X is --N-- or ##STR3## Z is ##STR4## R.sup.3 is hydrogen, lower alkyl or phenyl; R.sup.4 is hydrogen or lower alkyl; orR.sup.3 and R.sup.4 taken together form a benzene ring;R.sup.5 is hydrogen or lower alkyl;R.sup.Type: GrantFiled: October 27, 1989Date of Patent: June 4, 1991Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser
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Patent number: 5001131Abstract: The invention provides a method of relieving inflammation in a mammal inflicted with an imflammatory disease which method comprises treating said mammal with a therapeutically effective amount of a compound of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, loweralkyl, cycloloweralkyl, loweralkoxy, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, loweralkoxycarbonyl, aryl or aralkyl or 7-12 carbon atoms, or R.sup.1 and R.sup.2 taken together, or R.sup.2 and R.sup.3 taken together form a5,6, or 7 membered ring with the carbon atoms to which they are attached, which ring may be saturated or unsaturated and unsubstituted or substituted by loweralkyl or loweralkoxy, R.sup.Type: GrantFiled: June 16, 1989Date of Patent: March 19, 1991Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Albert Opalko
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Patent number: 4983600Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.Type: GrantFiled: October 16, 1989Date of Patent: January 8, 1991Assignee: John Wyeth & Brother LimitedInventors: Terence J. Ward, Janet C. White, Gerald Bradley
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Patent number: 4975431Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is O or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.Type: GrantFiled: June 16, 1989Date of Patent: December 4, 1990Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Albert Opalko
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Patent number: 4970316Abstract: There are disclosed compounds of the formula ##STR1## wherein X is O, S, SO, SO.sub.2 or CR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, carboxyl, lower alkoxy carbonyl, lower cycloalkyl, phenyl, anphthyl, pyridyl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing aryl or hetaryl substituents substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, COOR.sup.3, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, SO.sub.3 R.sup.3, SO.sub.2 N(R.sup.3).sub.2, phenylsulfonyl, lower alkyl sulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl;R.sup.4 is halo, morpholino, 4-methylpiperazino, R.sup.5 NNHR.sup.6, R.sup.5 NCH.sub.2 CH.sub.2 OCH.sub.3, or ##STR2## R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.7 and R.sup.Type: GrantFiled: May 3, 1989Date of Patent: November 13, 1990Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman
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Patent number: 4960892Abstract: There are disclosed compounds of the formula ##STR1## wherein A is alkyl of 3-19 carbon atoms, diloweralkyl allyl, dihaloallyl, diphenylallyl, lower alkynyl, ##STR2## X is N or CR; Z is ##STR3## R is hydrogen or lower alkyl; R.sup.1 is hydrogen, lower alkyl or phenyl;R.sup.2 is hydrogen or loweralkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.Type: GrantFiled: May 12, 1989Date of Patent: October 2, 1990Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III, John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak
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Patent number: 4942234Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.Type: GrantFiled: February 28, 1989Date of Patent: July 17, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
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Patent number: 4942236Abstract: There are disclosed compounds of the formula ##STR1## n is 0-5; R.sup.2 is, independently, hydrogen, loweralkyl, loweralkoxy, trifluoromethyl or halo; ##STR2## W represents a bond or ##STR3## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR4## or a pharmaceutically acceptable salt thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.Type: GrantFiled: February 15, 1989Date of Patent: July 17, 1990Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
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Patent number: 4937347Abstract: These are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is >1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that where R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.Type: GrantFiled: May 5, 1989Date of Patent: June 26, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Usha R. Patel