Six-membered Hetero Ring Consists Of Oxygen, Sulfur, Nitrogen And Carbon (e.g., Oxathiazines, Etc.) Patents (Class 544/2)
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Patent number: 4741765Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: April 3, 1987Date of Patent: May 3, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4740231Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.Type: GrantFiled: May 22, 1986Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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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
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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
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Patent number: 4723988Abstract: Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophen esulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: March 27, 1987Date of Patent: February 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Rafael Shapiro
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Patent number: 4713456Abstract: A process for the preparation of a 5-acylpyrimidine of the formula ##STR1## in which R is an organic radical comprising reacting a methyl ketone of the formulaR--CO--CH.sub.3in a first stage with a formylating reagent in the presence of a base to form an enolketone of the formulaR--CO--CH.dbd.CH--OR.sup.10in which R.sup.10 represents hydrogen or a base radical, thereafter reacting the enolketone in 2nd and 3rd stages with formamidine or a formamidine salt, and with an amino-formylating agent, and, in a 4th stage heating to cyclize the compound formed.The end products, some of which are new, are intermediates for making herbicides.Type: GrantFiled: August 26, 1985Date of Patent: December 15, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Graham Holmwood
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Patent number: 4695629Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by(a) reacting, in an inert organic solvent, a salt of sulfamic acid, which is at least partially soluble therein, with at least approximately the equimolar amount of an acetoacetylating agent, in the presence of an amine or phosphine catalyst, and by cyclizing the acetoacetamide-N-sulfonate which is formed in this reaction, or the free sulfonic acid,(b) by the action of at least approximately the equimolar amount of SO.sub.3, where appropriate in an inert inorganic or organic solvent, to give 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide, which is produced in the form of the acid in this reaction;it is possible, if desired, to obtain from the acid form(c) the appropriate salts by neutralization with bases. The non-toxic salts - in particular the potassium salt - are valuable synthetic sweeteners.Type: GrantFiled: June 3, 1986Date of Patent: September 22, 1987Assignee: Hoechst AktiengesellschaftInventors: Karl Clauss, Adolf Linkies, Dieter Reuschling
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Patent number: 4689414Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.Type: GrantFiled: February 24, 1986Date of Patent: August 25, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4684656Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.Type: GrantFiled: March 14, 1986Date of Patent: August 4, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4683228Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.Type: GrantFiled: January 22, 1985Date of Patent: July 28, 1987Assignees: ICI Americas Inc., Imperial Chemical Industries PLCInventors: Karin M. Kirkland, Derrick M. Mant
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Patent number: 4678499Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4668279Abstract: Novel pyridinesulfonamide compounds containing ortho-heterocyclic substituents such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-(1H-1,2,4-triazol-1-yl)-3 -pyridinesulfonamide display utility as herbicides and plant growth regulants.Type: GrantFiled: April 22, 1985Date of Patent: May 26, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4665177Abstract: This invention relates to new tetrahydropyrimidines, to a process for their production and to their use as catalysts in the production of polyurethane plastics, including polyurethane foams.Type: GrantFiled: August 5, 1985Date of Patent: May 12, 1987Assignee: Bayer AktiengesellschaftInventors: Werner Rasshofer, Gerhard Grogler, Richard Kopp
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Patent number: 4638063Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by reaction of acetoacetamide with at least approximately twice the molar amount of SO.sub.3 per mole of acetoacetamide, if appropriate in an inert inorganic or organic solvent. Relevant salts can be obtained, using bases, from the product which results in the form of the acid.The non-toxic salts, in particular the potassium salt, are valuable synthetic sweeteners.Type: GrantFiled: November 19, 1985Date of Patent: January 20, 1987Assignee: Hoechst AktiengesellschaftInventors: Karl Clauss, Adolf Linkies, Dieter Reuschling
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Patent number: 4634689Abstract: Phosphinylalkanoyl imino acids useful in the treatment of hypertension are disclosed.Type: GrantFiled: October 31, 1985Date of Patent: January 6, 1987Assignee: Schering CorporationInventors: Joseph T. Witkowski, Michael F. Czarniecki
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Patent number: 4629495Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.Type: GrantFiled: July 13, 1983Date of Patent: December 16, 1986Assignee: May & Baker LimitedInventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
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Patent number: 4625024Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide and its non-toxic salts are prepared by reacting acetoacetamide with an S-O compound of the formula IFSO.sub.2 Y (I)wherein Y.dbd.F, Cl, --OSO.sub.2 F or --OSO.sub.2 Cl, preferably only F,in the presence of bases.The non-toxic salts--especially the potassium salt--are valuable synthetic sweeteners.Type: GrantFiled: August 5, 1985Date of Patent: November 25, 1986Assignee: Hoechst AktiengesellschaftInventors: Erwin Schmidt, Karl Clauss
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Patent number: 4607100Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by(a) reacting, in an inert organic solvent, a salt of sulfamic acid, which is at least partially soluble therein, with at least approximately the equimolar amount of an acetoacetylating agent, in the presence of an amine or phosphine catalyst, and by cyclizing the acetoacetamide-N-sulfonate which is formed in this reaction, or the free sulfonic acid,(b) by the action of at least approximately the equimolar amount of SO.sub.3, where appropriate in an inert inorganic or organic solvent, to give 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide, which is produced in the form of the acid in this reaction;it is possible, if desired, to obtain from the acid form(c) the appropriate salts by neutralization with bases.The non-toxic salts--in particular the potassium salt--are valuable synthetic sweeteners.Type: GrantFiled: March 20, 1985Date of Patent: August 19, 1986Assignee: Hoechst AktiengesellschaftInventors: Karl Clauss, Adolf Linkies, Dieter Reuschling
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Patent number: 4585793Abstract: Certain novel heterocyclic compounds, aromatic thioesters, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like and elastase-like specificity and in the treatment of diseases such as emphysema which involve tissue proteolysis.Type: GrantFiled: May 9, 1983Date of Patent: April 29, 1986Assignee: Georgia Tech Research InstituteInventor: James C. Powers
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Patent number: 4569690Abstract: Disclosed are derivatives of 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides for use as herbicides, fungicides, plant dessicants and defoliants in agricultural and biocidal applications. Also disclosed are methods of making these compounds.Type: GrantFiled: September 12, 1983Date of Patent: February 11, 1986Assignees: Uniroyal, Inc., Uniroyal, Ltd.Inventors: Walter G. Brouwer, Allyn R. Bell, Allen R. Blem, Robert A. Davis
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Patent number: 4563452Abstract: This invention relates to new derivatives of oxazinobenzothiazine-6,6-dioxide, to a process for the production thereof and to the use thereof as medicaments.The new derivatives according to the present invention correspond to the general formula I: ##STR1## wherein: R represents a linear or branched lower C.sub.1 -C.sub.4 alkyl radical, in particular the methyl and ethyl radicals,X represents an oxygen atom or a sulphur atom, andHet represents a mono- or bicyclic unsaturated heterocycle containing a nitrogen heteroatom in the ortho position relative to the link between the said heterocycle and the nitrogen atom of the oxazine ring, the said heterocycle optionally containing one or two other additional heteroatoms selected from nitrogen, oxygen and sulphur, and also being able to be substituted by one or two methyl radicals.Type: GrantFiled: June 8, 1983Date of Patent: January 7, 1986Assignee: Provesan S.A.Inventor: Jose Esteve Soler
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Patent number: 4563521Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by reaction of acetoacetamide with at least approximately twice the molar amount of SO.sub.3 per mole of acetoacetamide, if appropriate in an inert inorganic or organic solvent. Relevant salts can be obtained, using bases, from the product which results in the form of the acid.The non-toxic salts, in particular the potassium salt, are valuable synthetic sweeteners.Type: GrantFiled: March 20, 1985Date of Patent: January 7, 1986Assignee: Hoechst AktiengesellschaftInventors: Karl Clauss, Adolf Linkies, Dieter Reuschling
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Patent number: 4555261Abstract: This invention relates to a novel class of sulfonamides and their use as herbicides and plant growth regulants.Type: GrantFiled: November 1, 1984Date of Patent: November 26, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Wallace C. Petersen
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Patent number: 4474746Abstract: A radiopharmaceutical chemical compound comprising a radioactive isotope, other than an isotope of iodine, in chemical combination with at least one amine group. The compound has a lipophilicity sufficiently high at a pH of 7.6 to permit passage of the compound from the blood of a mammal into a target organ or tissue and sufficiently low at a pH of 6.6 to prevent rapid return of the compound from the target organ or tissue to the blood. The compound has a percent protein binding of less than ninety percent.A method for selectively depositing a radiopharmaceutical compound in at least one target tissue or organ of a mammal, which tissue or organ has a significantly different intracellular pH than the blood of the mammal, by introducing the compound of the invention into the bloodstream of the mammal.Type: GrantFiled: July 16, 1982Date of Patent: October 2, 1984Assignee: State University of New YorkInventors: Monte Blau, Hank F. Kung
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Patent number: 4412994Abstract: Novel prodrug forms of known non-steroidal anti-inflammatory agents are disclosed, said prodrugs having the structural formula ##STR1##Type: GrantFiled: May 28, 1982Date of Patent: November 1, 1983Assignee: INTERx Research CorporationInventors: Kenneth B. Sloan, Roy Little
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Patent number: 4397849Abstract: This invention relates to novel benzothiazine derivatives having therapeutic effect on autoimmune diseases, to processes for preparation of such derivatives, and to pharmaceutical compositions containing such derivatives, the derivatives having the formula: ##STR1## wherein R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, aryl and carboxy(lower)cycloalkyl; aryl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy; haloarylamino; or heterocyclic group;R.sup.2 is hydrogen, lower alkyl, lower alkylamino(lower)alkyl, aryl or ar(lower)alkyl;R.sup.3 is hydrogen, halogen, lower alkyl or lower alkoxy; andn is an integer 0 to 2.Type: GrantFiled: December 11, 1981Date of Patent: August 9, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Tsutomu Teraji, Teruo Oku, Youichi Shiokawa
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Patent number: 4356024Abstract: A process for the preparation of a 1-amino-1,3,5-triazine-2,4(1H, 3H)-dione compounds comprising the steps of reacting an N-substituted imido-dicarboxylic acid diaryl ester with an isothiosemicarbazone at a temperature of between 50.degree. and 150.degree. C. to form a 1-alkylidene-amino-1,3,5-triazine-2,4(1H, 3H)-dione reaction product; and thereafter, hydrolyzing the reaction product in an acid medium. The reaction product need not be separated from the reaction mixture before the hydrolysis step. Certain novel 1-amino-1,3,5-triazine-2,4(1H, 3H)-dione compounds are provided. The compounds are useful as herbicides.Type: GrantFiled: February 10, 1981Date of Patent: October 26, 1982Assignee: Bayer AktiengesellschaftInventors: Karlfried Dickore', Engelbert Kuhle
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Patent number: 4166177Abstract: The invention relates to novel 2,2-dioxo-1,2,3-benzoxathiazines substituted in the benzene nucleus, as well as the 3,4-dihydro analogs thereof, useful as anti-inflammatory, antipyretic, analgesic agents.Type: GrantFiled: December 27, 1977Date of Patent: August 28, 1979Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Robert L. Smith, Gerald E. Stokker
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Patent number: 4154828Abstract: N.sup.2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: October 21, 1977Date of Patent: May 15, 1979Assignees: Mitsubishi Chemical Industries, Ltd., Shosuke 0KAMOTOInventors: Shosuke Okamoto, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Shinji Tonomura
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Patent number: 4139529Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides and the pharmaceutically acceptable acid addition salts thereof which have antithrombotic properties.Type: GrantFiled: August 31, 1977Date of Patent: February 13, 1979Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Hyogi Kikumoto, Yoshikuni Tamao, Kazdo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4133880Abstract: N.sup.2 -substituted-L-arginine esters and amides, and the pharmaceutically acceptable acid addition salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: July 28, 1977Date of Patent: January 9, 1979Assignees: Mitsubishi Chemical Industries Ltd., Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura