Additional Ring Attached Directly To The Nitrogen By Nonionic Bonding Patents (Class 548/234)
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Patent number: 5071871Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.Type: GrantFiled: July 10, 1990Date of Patent: December 10, 1991Assignee: Sandoz Ltd.Inventors: Stefan Blarer, John Morley, Ian D. Chapman
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Patent number: 5066666Abstract: compound of the formula: ##STR1## wherein A is the group of the formula:Ar.sup.1 --D--Ar.sup.2 --wherein Ar.sup.1 is a phenyl or thienyl group which may be optionally substituted with at least one of the same or different halogen atom; Ar.sup.2 is a phenylene or thienylene group which may be optionally substituted with at least one of the same or different halogen atom; D is a divalent radical selected from the group consisting of >.dbd.N.dbd.OR.sup.4 [wherein R.sup.4 is a hydrogen atom or lower alkyl group], >C.dbd.O, ##STR2## >CHOH, >NH radical, or single bond, wherein R.sup.5 is a lower alkoxy or a phenyl group which may be optionally substituted with at least one of the same or different halogen atom; E is a methine group or a nitrogen atom; F is a vinylene group or an oxygen atom, ##STR3## wherein R.sup.6 is a lower alkoxy group; R.sup.7 is a lower alkyl group; R.sup.Type: GrantFiled: January 26, 1990Date of Patent: November 19, 1991Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Yukinori Ozato, Nobuhiko Tamura, Hiroaki Masumori, Michihiro Yamamoto, Atsuyuki Kojima, Fumio Nishikaku, Yoshihiko Kimura
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Patent number: 5043454Abstract: 1-Aryl- and 1-hetarylimidazolecarboxylic esters of the general formulae Ia and Ib ##STR1## where R.sup.1 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl;R.sup.2 is substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl; C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.6 -cycloalkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.4 is substituted or unsubstituted phenyl or 5- or 6-membered heteroaromatic,processes for their manufacture, and agents containing them.Type: GrantFiled: January 9, 1990Date of Patent: August 27, 1991Assignee: BASF AktiengesellschaftInventors: Ulrich Wriede, Gerhard Hamprecht, Hermann Koehler, Bruno Wuerzer
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 5008281Abstract: All stereoisomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein X is --O-- or --S--, Y is --C.dbd.O, ##STR2## or --CH.sub.2 --, R.sub.1 is selected from the group consisting of hydrogen, halogen, optionally unsaturated alkyl of 1 to 8 carbon atoms and optionally unsaturated cycloalkyl of 3 to 8 carbon atoms, the latter two being optionally substituted with one or more halogen and aryl of 6 to 14 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, --CF.sub.3, --NO.sub.2, --CN, halogen, alkoxy of 1 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, an ester, optionally unsaturated alkyl of 1 to 8 carbon atoms and optionally unsaturated cycloalkyl of 3 to 8 carbon atoms, the latter two being optionally substituted with one or more halogen, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, --CN and --C.tbd.CH and A is the residue of an ACOOH pyrethrinoid acid having pesticidal properties.Type: GrantFiled: November 7, 1989Date of Patent: April 16, 1991Assignee: Roussel UclafInventors: Jacques Demassey, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4988723Abstract: Benzopyran derivatives of formula (I) wherein the substituents are as defined herein are provided. The compounds possess vasodilating activity and are useful in the treatment of hypertension. Pharmaceutical compositions and methods of treating hypertension are also provided.Type: GrantFiled: May 17, 1989Date of Patent: January 29, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
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Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4985429Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-1-oxo-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.Type: GrantFiled: March 15, 1990Date of Patent: January 15, 1991Assignee: E. I. du Pont de Nemours and CompanyInventors: Chia-Lin J. Wang, Mark A. Wuonola
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Patent number: 4977173Abstract: Aminomethyl oxooxazolidinyl ethenylbenzene derivatives, including the nitriles, sulfoxides, acetamides and nitro compounds, such as l-N-[3-[4-(E-1-methyl-2-cyanoethenyl)phenyl]-2-oxooxazolidin-5-ylmethyl]ac etamide, possess useful antibacterial activity.Type: GrantFiled: July 7, 1989Date of Patent: December 11, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventors: David R. Brittelli, Peter F. Corless, Walter A. Gregory, Chung-Ho Park
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Patent number: 4965268Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-1-oxo-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.Type: GrantFiled: March 15, 1990Date of Patent: October 23, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventors: Chia-Lin J. Wang, Mark A. Wuonola
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4914117Abstract: New substituted benzamides have the general formula: ##STR1## their optical isomers and their physiologically acceptable salts. The compounds are used as activators of the central nervous system.Type: GrantFiled: March 13, 1989Date of Patent: April 3, 1990Assignee: Societe d'Etudes Scientifiques et Industrielle de l'Ile-d-FranceInventors: Jacques Acher, Jean-Claude Monier, Jean-Paul Schmitt, Gardaix-Luthereau Renee, Brenda Costall, Robert Naylor
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Patent number: 4904679Abstract: Pyrrolophenylalkanolamines of the formula ##STR1## R.sup.1 and R.sup.2 represent hydrogen or various radicals, R.sup.3 represents hydrogen, acyl or trialkylsilyl,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen, or, together with R.sup.3, represents ##STR2## wherein R.sup.7 represents hydrogen or alkyl, andR.sup.6 represents branched or cyfclic alkyl, which is optionally substituted,and salts thereof promote the yield of animals. Many new intermediates are also shown.Type: GrantFiled: April 22, 1988Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventors: Hartmund Wollweber, Jurgen Stoltefuss, Friedrich Berschauer, Ann de Jong, Martin Scheer
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Patent number: 4900351Abstract: An iminooxazolidine having the formula ##STR1## wherein X and Y are the same or different and are selected from the group consisting of cyano, halogen, acyl, alkyl, alkylthio, haloalkyl, trihalomethylthio, alkylsulfenyl, alkoxy, carboalkoxy and trihalomethyl wherein the alkyl groups have from 1 to 5 carbon atoms;m is 1 or 2;n is 0, 1 or 2; andR is hydrogen or a lower alkyl group having from 1 to 3 carbon atoms, preferably an ethyl group, and herbicidally effective salts thereof.Type: GrantFiled: March 14, 1988Date of Patent: February 13, 1990Assignee: ICI Americas Inc.Inventor: Raymond A. Felix
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Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
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Patent number: 4892871Abstract: The invention is directed to azido-substituted octopamine agonists and the radiolabeled derivatives thereof. The invention also relates to past controlling compositions comprising the azido-substituted octopamine agonists of the invention.The invention also relates to methods of controlling invertebrate pests by bringing the pest into contact with an invertebrate pest-controlling composition of the invention and to an apparatus for controlling invertebrate pests utilizing the pest-controlling compositions of the invention. The pest-controlling compositions may be used alone or in conjunction with ultraviolet light.The invention also relates to methods for the isolation of octopamine receptor proteins utilizing the radiolabeled azido-substituted octopamine agonists of the invention.Type: GrantFiled: April 12, 1988Date of Patent: January 9, 1990Assignee: The General Hospital CorporationInventor: James A. Nathanson
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Patent number: 4868183Abstract: Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is a lower alkyl group;R.sup.2 and R.sup.3 are each hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together may form --(CH.sub.2 (.sub.4)-- or --CH.dbd.CH--CH.dbd.CH--;.alpha. is a 5- or 6-membered heteroaromatic ring group containing 1 to 3 hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur, or a pyrazine-N-oxide ring, pyridazine-N-oxide ring or pyrimidine-N-oxide ring group, wherein each of these heteroaromatic ring groups may optionally have 1 to 3 substituents selected from the group consisting of a lower alkyl, halogen, phenyl, lower alkoxycarbonyl, amino, lower alkoxy and hydroxy-lower alkyl, with the proviso that said 5- or 6-membered heteroaromatic ring group is not thiazolyl, isothiazolyl, pyridyl or 1,3,5-triazinyl group; or salts thereof. These compounds and salts thereof have anti-inflammatory activity and lipoxygenase-inhibitory activity.Type: GrantFiled: July 20, 1987Date of Patent: September 19, 1989Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kenichi Kanai, Kiyoto Goto, Kinji Hashimoto
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Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4861789Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable acid addition salt and/or a pharmaceutically acceptable solvate thereof, wherein A represents a residue of a benzene ring optionally having up to four substituents selected from the group consisting of halogen, C.sub.1-6 alkyl aNd C.sub.1-6 alkoxy; R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-6 alkyl group; X represents a bond or a moiety CHR.sup.1 wherein R.sup.1 is as defined above; and Z represents O, NH or S.Type: GrantFiled: May 4, 1987Date of Patent: August 29, 1989Assignee: Beecham Group plcInventors: John Berge, Lee J. Beeley
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Patent number: 4835172Abstract: New substituted benzamides have the general formula: ##STR1## A=alkyl, alkenyl, diethylaminoethyl or ##STR2## R.sub.1, R.sub.2 =H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl; R.sub.3, R.sub.4, R.sub.5, R.sub.6 =hydrogen or C.sub.1 -C.sub.6 alkyl;X=halogen;Y=H, halogen;Z=NH, oxygen or sulfur;their optical isomers and their physiologically acceptable salts. The compounds are used as activators of the central nervous system.Type: GrantFiled: December 19, 1986Date of Patent: May 30, 1989Assignee: Societe D'Etudes Scientifiques et Industrielles de L'Ile-de-FranceInventors: Jacques Acher, Jean-Claude Monier, Jean-Paul Schmitt, Renee Gardaix-Luthereau, Brenda Costall, Robert Naylor
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Patent number: 4826990Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is ##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 ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen, lower alkyl, ##STR9## 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, and as antiinflammatory agents.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
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Patent number: 4818270Abstract: 2-(Heteroamino)-4,5-substituted-oxazole/thiazole compounds are antidotes for thiocarbamate, triazine and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds in sorghum.Type: GrantFiled: August 28, 1986Date of Patent: April 4, 1989Assignee: Monsanto CompanyInventors: Raymond C. Grabiak, Robert K. Howe, Cheryl Yearell-Vinson
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Patent number: 4806653Abstract: A process of the preparation of iminooxazolidines which comprises (a) reacting a urea alcohol of the formula ##STR1## X, Y, n and R are as defined, with a dehydrating agent to form an intermediate salt compound of the formula ##STR2## wherein X, Y, n and R are as previously defined and X.degree.Type: GrantFiled: October 17, 1986Date of Patent: February 21, 1989Assignee: Stauffer Chemical CompanyInventor: Raymond A. Felix
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Patent number: 4801600Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-1-oxo-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.Type: GrantFiled: October 9, 1987Date of Patent: January 31, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Chia-Lin J. Wang, Mark A. Wuonola
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Patent number: 4771061Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: May 6, 1987Date of Patent: September 13, 1988Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
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Patent number: 4629794Abstract: A series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.Type: GrantFiled: January 23, 1986Date of Patent: December 16, 1986Assignee: Pfizer Inc.Inventor: John P. Dirlam
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Patent number: 4584385Abstract: A series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.Type: GrantFiled: February 4, 1985Date of Patent: April 22, 1986Assignee: Pfizer Inc.Inventor: John P. Dirlam
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Patent number: 4562201Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: July 26, 1982Date of Patent: December 31, 1985Assignee: American Hospital Supply CorporationInventors: David M. Stout, William L. Matier
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Patent number: 4321394Abstract: The instant invention is directed to a process for the production of addition compounds of compounds containing hydroxyl groups and carbodiimides substantially free from isocyanate groups, comprising reacting the reactants in the presence of from 0.01 to 3% by weight, based on the reaction mixture, of a metal catalyst, the improvement wherein a tin compound is used as said metal catalyst.Type: GrantFiled: September 24, 1980Date of Patent: March 23, 1982Assignee: Bayer AktiengesellschaftInventors: Walter Schafer, Kuno Wagner, Kurt Findeisen
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Patent number: 4221798Abstract: Novel condensed nitrogen containing heterocyclic compounds and pharmaceutically acceptable acid addition salts thereof according to the following formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are selected from hydrogen, halogen, alkyl and alkoxy having one to four carbons, X is selected from oxygen, sulfur, methylene, imino and acylimino having two to five carbons in the acyl group, n and m are positive integers of 1, 2, or 3, and p is a positive integer of 2 or 3, are disclosed which are useful as anti hypertensive agents. Compositions containing said compounds and methods of preparation are also disclosed.Type: GrantFiled: April 16, 1979Date of Patent: September 9, 1980Assignee: Beiersdorf AktiengesellschaftInventor: Erich Cohnen
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Patent number: 4175131Abstract: A class of novel 2-oxazolyl ureas and carbamates having anti-allergic activity are described together with methods of making such compounds and pharmaceutical compositions containing the active compounds of the invention.Type: GrantFiled: December 27, 1977Date of Patent: November 20, 1979Assignee: Lilly Industries LimitedInventors: William J. Ross, Alex Todd, John P. Verge
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas