Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
-
Patent number: 5378703Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: February 18, 1993Date of Patent: January 3, 1995Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Hwang-Hsing Chen, Jesse A. May
-
Patent number: 5373007Abstract: The invention concerns a bicyclic heterocyclic compound of the formula I ##STR1## wherein Q is an optionally substituted 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's and a further O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which,together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: March 25, 1994Date of Patent: December 13, 1994Assignees: Zeneca Limited, Pharma ZenegaInventors: Pierre A. R. Bruneau, Graham C. Crawley
-
Patent number: 5356862Abstract: The invention relates to herbicidal sulfonylurea compounds, agriculturally suitable compositions thereof and a method for their use as general or selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: July 22, 1992Date of Patent: October 18, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: William T. Zimmerman
-
Patent number: 5344929Abstract: A process for synthesizing carbonic anhydrase inhibitors is disclosed.Type: GrantFiled: February 18, 1993Date of Patent: September 6, 1994Assignee: Alcon Laboratories, Inc.Inventors: William D. Dean, Paul W. Zinke, Steven J. Sproull, Michael E. Deason, Raymond E. Conrow, Anura P. Dantanarayana
-
Patent number: 5274097Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 9, 1991Date of Patent: December 28, 1993Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
-
Patent number: 5262418Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula--CH.sub.2 --CH.sub.2 -- (a-1),--CH.sub.2 --CH.sub.2 --CH.sub.2 -- (a-2), or--CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -- (a-3),wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula--Alk--R.sup.4 (b-1),--Alk--X--R.sup.5 (b-2),--Alk--Y--C(.dbd.O)--R.sup.7 (b-3), or--Alk--Y--C(.dbd.O)--NR.sup.9 R.sup.10 (b-4),the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties.Type: GrantFiled: November 17, 1992Date of Patent: November 16, 1993Assignee: Tanssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
-
Patent number: 5240923Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: October 9, 1991Date of Patent: August 31, 1993Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Hwang-Hsing Chen, Jesse A. May
-
Patent number: 5232930Abstract: The invention concerns a benzodioxole derivative of the formula I ##STR1## wherein Ar.sup.1 is an optionally substituted 9- or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 -- which, together with the carbon atom to which A.sup.1 and A.sup.2 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X is oxy, thio, sulphinyl or sulphonyl, and which ring may bear one or two substituents;or a pharmaceutically-acceptable salt thereof;which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.Type: GrantFiled: January 9, 1992Date of Patent: August 3, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: John F. Kingston, David Waterson
-
Patent number: 5212301Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.Type: GrantFiled: May 8, 1992Date of Patent: May 18, 1993Assignee: Imperial Chemical Industries PLCInventors: John S. Moilliet, Richard D. Chambers, Michael H. Rock
-
Patent number: 5185335Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula ##STR2## wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula ##STR3## the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: February 4, 1991Date of Patent: February 9, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
-
Patent number: 5183816Abstract: This invention relates to the compounds of the formula [I] and salts thereof, which are useful for treatment of liver disorders, ##STR1## wherein X is oxygen or sulfur; andA is straight C.sub.2 alkylene which can be substituted by one or more lower alkyl.Type: GrantFiled: June 20, 1991Date of Patent: February 2, 1993Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takakazu Morita, Shiro Mita, Yoichi Kawashima
-
Patent number: 5166343Abstract: Substituted 1,2,4-triazolo[1,5-c]pyrimido[1,4]azines have been found to have potent bronchodilator activity. Pharmacological methods for inducing bronchodilation using such compounds, pharmaceutical compositions containing such compounds, and synthetic intermediates for preparing such compounds are also described.Type: GrantFiled: November 5, 1991Date of Patent: November 24, 1992Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
-
Patent number: 5153192Abstract: Thiophene sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: November 27, 1990Date of Patent: October 6, 1992Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Hwang-Hsing Chen, Jesse A. May
-
Patent number: 5140033Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.Type: GrantFiled: October 1, 1990Date of Patent: August 18, 1992Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
-
Patent number: 5114934Abstract: The compounds of the formula ##STR1## wherein R.sub.a, R.sub.b, R.sub.c, R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed. The compounds of formula I have valuable pharmacological properties and can be used for the control of prevention of illnesses. In particular, they have muscle relaxant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.Type: GrantFiled: June 1, 1989Date of Patent: May 19, 1992Assignee: Hoffman-La Roche, Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
-
Patent number: 5106969Abstract: 5-Methylimidazo[4,5-e]-1,2-thiazin-4(5-H)-one, having the structure ##STR1## a cytotoxic metabolite of the marine sponge Neamphius huxleyi, has been isolated from the sponge by extraction and chromatography.Type: GrantFiled: April 11, 1991Date of Patent: April 21, 1992Assignees: Cornell Research Foundation, Inc., The University of Alberta, The University of British ColumbiaInventors: Raymond J. Andersen, Theresa M. Allen, E. Dilip de Silva, Julie S. Racok, Jon Clardy, Linda S. Brinen
-
Patent number: 5093332Abstract: Thieno[2,3-b][1,4]thiazine-6-sulfonamides having the structural formula: ##STR1## wherein Z, R.sup.1, R.sup.2, and n are as hereinafter defined, are carbonic anhydrase inhibitors useful in the topical treatment of elevated intraocular pressure and glaucoma.Type: GrantFiled: October 1, 1990Date of Patent: March 3, 1992Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Cecilia A. Hunt
-
Patent number: 5082838Abstract: Disclosed is a compound represented by the formula (I) or a salt thereof: ##STR1## wherein R.sup.1 represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R.sup.2 represents hydrogen, an aliphatic hydrocarbon group having one or more substituents, an aryl group which may be substituted, an amino group which may be substituted, a formyl group, a nitro group or a halogeno group; A represents a divalent hydrocarbon chain of 2 to 4 carbon atoms which may be substituted; and m represents an integer of 0 to 2, which is useful for treatment and prevention of diseases induced by abnormalities in regulation of reactions in vivo mediated through endothelin or interleukin 1, and of immune diseases and inflammatory diseases.Type: GrantFiled: June 13, 1990Date of Patent: January 21, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Norio Shimamoto, Taketoshi Saijo, Masahiro Suno
-
Patent number: 5071849Abstract: The invention relates to new dihydropyrimidothiazine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same and new intermediates useful in the preparation of the said dihydropyrimidothiazine derivatives.The new dihydropyrimidothiazine derivatives of the general formula I, ##STR1## wherein R.sup.1 represents C.sub.1-6 alkoxy, amino or phenylamino,R.sup.2 stands for C.sub.1-6 alkyl or phenyl,R.sup.3 represents hydrogen or C.sub.1-6 alkyl, andR.sup.4 denotes C.sub.1-11 alkyl or phenyl optionally bearing one or more identical or different substituent/s/ selected from halogen, nitro, amino, di-(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy and hydroxy,and pharmaceutically acceptable acid addition salts thereof exert valuable antianginal and/or antiinflammatory effect/s/ and are useful in therapy.Type: GrantFiled: July 19, 1990Date of Patent: December 10, 1991Assignee: Egis GyogyszergyarInventors: Daniel Bozsing, Lujza Petocz, Maria Szecsey nee Hegedus, Peter Tompe, Gabor Gigler, Istvan Gacsalyi, Istvan Gyertyan
-
Patent number: 5053071Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: May 2, 1990Date of Patent: October 1, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple
-
Patent number: 5017212Abstract: A compound of the general formula: ##STR1## wherein Q is a condensed heterocyclic group having an N atom in the bridgehead which may be substituted, W is O or S, R.sub.1 and R.sub.2 each are an alkyl group, an alkoxy group or halogen and Z is CH or N, and a salt thereof, which is useful as a herbicide.Type: GrantFiled: March 17, 1987Date of Patent: May 21, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuo Ishida, Kazunari Ohta, Tatsuo Nakahama, Harutoshi Yoshikawa
-
Patent number: 5011842Abstract: 2-(Heterocyclylalkyl)imidazopyridines having antihistaminic properties, compositions containing these compounds as active ingredient and novel 2-(Heterocyclylalkyl)imidazopyridines.Type: GrantFiled: August 2, 1990Date of Patent: April 30, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Francois M. Sommen, Joseph L. G. Torremans, Gaston, S. M. Diels
-
Patent number: 5008390Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.Type: GrantFiled: November 3, 1988Date of Patent: April 16, 1991Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Ivan Lantos, Michael A. McGuire, Lendon N. Pridgen, Herbert B. Winicov
-
Patent number: 4981850Abstract: Substituted 1,2,4-triazolo[1,5-c]pyrimido[1,4]-azines have been found to have potent bronchodilator activity. Also, pharmacological methods for inducing bronchodilation using such compounds, pharmaceutical compositions containing such compounds, and synthetic intermediates, including 1,2,4-triazolo[4,3-c]-pyrimido[1,4]azines, for preparing such compounds.Type: GrantFiled: January 17, 1989Date of Patent: January 1, 1991Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
-
Patent number: 4957916Abstract: 3-Piperazinyl-1,2-benzazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of disorders in which serotonin and/or dopamine release is of predominant importance.Type: GrantFiled: June 14, 1989Date of Patent: September 18, 1990Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk, Josephus C. Mertens
-
Patent number: 4948418Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: August 30, 1989Date of Patent: August 14, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple
-
Patent number: 4927821Abstract: The invention relates to new enol ethers of 6-chloro-4-hydroxy-2-methyl-N-(2-pyridyl)-2H-thieno(2,3-e)-1,2- thiazine-3-carboxamide 1,1-dioxide of the formula ##STR1## in which R denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.5 -C.sub.7)-cycloalkyl or benzyl, and a process for their preparation. The new compounds have an antiinflammatory activity and are suitable for the treatment of rheumatism.Type: GrantFiled: October 18, 1988Date of Patent: May 22, 1990Assignee: CL Pharma AktiengesellschaftInventors: Dieter Binder, Franz Rovenszky, Hubert P. Ferber
-
Patent number: 4881967Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable composition containing them, and their use as broad spectrum herbicides.Type: GrantFiled: June 2, 1988Date of Patent: November 21, 1989Assignee: E. I. Du Pont De Nemours and CompanyInventor: Joseph E. Semple
-
Patent number: 4861878Abstract: New potent lipoxygenase inhibitors which are 1H-pyrido-[2,3-b][1,4] thiazines are disclosed. The new thiazines are of the formula ##STR1## in which R.sup.1 denotes hydrogen, halogen, optionally substituted alkyl or alkoxy or the group ##STR2## in which R.sup.5 and R.sup.6 are identical or different and denote hydrogen, optionally substituted alkyl or aryl, or can be linked to form a 5- or 6-membered heterocyclic ring,R.sup.2 and R.sup.3 are identical or different and denote hydrogen or optionally substituted alkyl or alkoxy andR.sup.4 denotes hydroxyl, the group ##STR3## in which R.sup.5 and R.sup.6 have the abovementioned meaning, or, in the case where R.sup.3 denotes hydrogen or optionally substituted alkoxy, also denotes optionally substituted alkoxy.Type: GrantFiled: November 6, 1986Date of Patent: August 29, 1989Assignee: Bayer AktiengesellschaftInventors: Gerd Fengler, Alexander Klausener, Hans-Josef Buysch, Mithat Mardin, Bernhard Pelster
-
Patent number: 4846874Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene- , furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide. 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: December 16, 1987Date of Patent: July 11, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Robert J. Pasteris
-
Patent number: 4838929Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-aminocarbonyl]-1,3-dihydro-6-methyl-3-oxofuro [3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: September 14, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mary A. Hanagan
-
Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
-
Patent number: 4803279Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.Type: GrantFiled: April 28, 1986Date of Patent: February 7, 1989Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Ivan Lantos, Michael A. McGuire, Lendon N. Pridgen, Herbert B. Winicov
-
Patent number: 4784997Abstract: 1-H-pyrido-[3,2-b][1,4]-thiazines of the formula ##STR1## are prepared by the reaction of 2-halogenocarbonyl compounds an 2-amino-3-pyridinethiols. These compounds are useful as medicaments especially as inhibitors of lipoxygenase.Type: GrantFiled: December 16, 1986Date of Patent: November 15, 1988Assignee: Bayer AktiengesellschaftInventors: Alexander Klausener, Gerd Fengler, Hans-Josef Buysch, Bernhard Pelster
-
Patent number: 4749403Abstract: The compounds of formula I ##STR1## in which the substituents X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6, are defined hereinbelow. The compounds have advantageous herbicidal properties and are useful, for example, for combating undesired plants.Type: GrantFiled: February 6, 1987Date of Patent: June 7, 1988Assignee: Hoechst AktiengesellschaftInventors: Rainer Liebl, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer
-
Patent number: 4737184Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: May 10, 1985Date of Patent: April 12, 1988Assignee: E. I. Du Pont De Nemours and CompanyInventor: Robert J. Pasteris
-
Patent number: 4723987Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3-dihydro-6-methyl-3-oxof uro[3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: April 22, 1986Date of Patent: February 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mary A. Hanagan
-
Patent number: 4715885Abstract: Pyrazole sulfonylureas are expected to show pre- and post-emergence herbicidal activity. Specifically preferred in this class of compounds is N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-4,6-dihydro-2-methyl-4-oxo- 2H-furo[3,4-c]pyrazole-3-sulfonamide.Type: GrantFiled: September 10, 1986Date of Patent: December 29, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Barry A. Wexler
-
Patent number: 4715886Abstract: Pyrazole sulfonamides are found to have utility as preemergent and/or postemergent herbicides or plant growth regulants.Type: GrantFiled: March 16, 1987Date of Patent: December 29, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Barry A. Wexler
-
Patent number: 4683306Abstract: Process for the preparation of 3,4-dihydro-2-substituted-4(or 3)-oxo-2H-1,2-thiazine-3(or 4)-carboxylic acid 1,1,-dioxide magnesium chelate derivatives and its acids by reacting appropriately 3,4-dihydro-2-substituted-4(or 3)-oxo-2H-1,2-thiazine 1,1-dixoides with alkylmagnesiumcarbonate and then hydrolyzing and its use as intermediates for the preparation of N-substituted-2-substituted-2H-1,2-thiazine-3(or 4)-carboxamide-1,1-dioxide derivatives, effective antiinflammatory agents.Type: GrantFiled: July 13, 1984Date of Patent: July 28, 1987Assignee: YuHan Corporation Co., Ltd.Inventors: Jung J. Suh, You H. Hong
-
Patent number: 4671817Abstract: Pyrazole sulfonamides are found to have utility as preemergent and/or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 23, 1985Date of Patent: June 9, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Barry A. Wexler
-
Patent number: 4622062Abstract: Pyrazole sulfonylureas are expected to show pre- and post-emergence herbicidal activity. Specifically preferred in this class of compounds is N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-4,6-dihydro-2-methyl-4-oxo- 2H-furo[3,4-c]pyrazole-3-sulfonamide.Type: GrantFiled: December 10, 1984Date of Patent: November 11, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Barry A. Wexler
-
Patent number: 4610982Abstract: Certain novel 2-acetoxybenzoyl and ring-substituted .alpha.-arylpropionyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as non-steroidal anti-arthritic agents. Typical member compounds include 4-(2-acetoxybenzoyloxy)-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-ca rboxamide 1,1-dioxide, 4-[.alpha.-(4-isobutylphenyl)propionyloxy]-2-methyl-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxyamide N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxyamide 1,1-dioxide, 4-[.alpha.-(3-benzoylphenyl)propionyloxy]-2-methyl-N-(2-pyridinyl)-2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide, "d-4-[.alpha.-6-methoxynaphth-2-yl)propionyloxy]-2-methyl-N-(2-pyridinyl)- 2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide" to -- d-4-[.alpha.-(6-methoxynaphth-2-yl)propionyloxy]-2-methyl-N-(2-pyridinyl)- 2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide.Type: GrantFiled: June 3, 1985Date of Patent: September 9, 1986Assignee: Pfizer Inc.Inventor: Joseph G. Lombardino
-
Patent number: 4581171Abstract: Novel [[bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones, wherein the pyrimidinone-ring is embraced within a bicyclic system, being useful compounds in the treatment of psychosomatic disorders.Type: GrantFiled: September 27, 1984Date of Patent: April 8, 1986Assignee: Janssen Pharmaceutica, N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk, Josephus C. Mertens
-
Patent number: 4576942Abstract: Compounds of the formulae ##STR1## wherein, A is benzo, pyrido, thieno, pyrazolo, imidazo, pyrimido, isoxazolo, thiazolo, furo or pyrrolo;X is O, S, SO or SO.sub.2 ;R.sub.1 is H, alkyl, aryl, OH, OR, aryloxy, halogen, amino, nitro, cyano, COOR, trihalomethyl, ##STR2## R.sub.2. R.sub.3, R.sub.4 and R.sub.5 are identical or different and each represent H, alkyl, aryl, OH, OR, amino, alkylamino, dialkylamino, COOR, thio, alkylthio, cyano, or halogen; and n is 1-2; and pharmaceutically acceptable salts thereof having anti-allergy and anti-inflammatory activity.Type: GrantFiled: July 12, 1984Date of Patent: March 18, 1986Assignee: USV Pharmaceutical Corp.Inventor: Raymond D. Youssefyeh
-
Patent number: 4563453Abstract: New thiazine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or acyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkyl or lower alkoxy,Z is taken together with the adjacent carbon atoms to form an unsaturated heterocyclic ring which may be substituted with phenyl, halogen, acyl or lower alkyl, andthe heavy solid line means single or double bond,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiinflammatory, analgesic and antirheumatic agents.Type: GrantFiled: October 9, 1984Date of Patent: January 7, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Yosiharu Kasai
-
Patent number: 4551452Abstract: Certain enol ether derivatives of oxicams (1,1-dioxides of N-heteroaryl-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamides and N-heteroaryl-4-hydroxy-2-methyl-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamid es) are useful as prodrugs of these antiinflammatory compounds.Type: GrantFiled: May 2, 1984Date of Patent: November 5, 1985Assignee: Pfizer Inc.Inventor: Anthony Marfat
-
Patent number: 4548938Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.Type: GrantFiled: February 19, 1985Date of Patent: October 22, 1985Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Josephus C. Mertens
-
Patent number: 4544655Abstract: 4-Hydroxy-2-methyl-3-(2-pyridylcarbamoyl)-6-trifluoromethyl-2H-thieno[2,3-e ]-1,2-thiazine 1,1-dioxide of the formula ##STR1## and its pharmaceutically acceptable salts which possess valuable pharmacodynamic properties are described. More particularly, the compound and its salts display antiinflammatory, analgesic and antirheumatic activities and they are readily accessible by reacting a corresponding alkyl ester with 2-aminopyridine and, if desired, subsequent salt formation.Type: GrantFiled: August 31, 1983Date of Patent: October 1, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Rudolf Pfister, Paul Zeller, Dieter Binder, Otto Hromatka
-
Patent number: 4529727Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]-pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b][1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.Type: GrantFiled: February 2, 1984Date of Patent: July 16, 1985Assignee: Janssen Pharmaceutical, N.V.Inventors: Ludo E. J. Kennis, Josephus C. Mertens