At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Patent number: 5153324Abstract: A process for preparing herbicidal sulfonylureas which comprises mixing a sulfonylisocyanate and a heterocyclic amine in the absence of a solvent.Type: GrantFiled: December 26, 1991Date of Patent: October 6, 1992Assignee: E. I. du Pont de Nemours and CompanyInventor: Teddy H. Grindstaff
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Patent number: 5149700Abstract: This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.Type: GrantFiled: October 30, 1991Date of Patent: September 22, 1992Assignee: American Home Products CorporationInventors: John W. Ellingboe, Jehan F. Bagli, Michael W. Winkley
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Patent number: 5149357Abstract: Compound of the formula ##STR1## in which A is O, S, or NR.sup.3 ; G is CH or N; R and R.sup.1 are independently alkyl, alkoxy, haloalkoxy or alkylamino; R.sup.2 is phenyl, substituted phenyl, alkyl, cycloalkyl, haloalkyl or --CH.sub.2 [(R.sup.4)C(R.sup.5).sub.n --Z; R.sup.3 and R.sup.7 are, independently, hydrogen, alkyl, --C(O)NH.sub.2 or --C(O)alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, or halogen; R.sup.6 is halogen, alkyl, alkoxy, haloalkoxy, NO.sub.2, amino, alkyl substituted amino, or acyl substituted amino; n is 0 to 5; Z is cyano, amino, alkylamino, dialkylamino, --NHCO.sub.2 alkyl, alkoxy, alkylthio, alkylsulfonyl, alkenyl, alkynyl, phenyl or substituted phenyl; and Q is hydrogen, halogen, alkyl, alkoxy, haloalkoxy, nitro, amino, haloalkyl, alkythio, alkylsulfonyl, phenyl, substituted phenyl or phenoxy; or a 5 or 6 membered aromatic heterocycle having the formula ##STR2## in which "m" is 0 or 1; A' is O, S, or NR.sup.Type: GrantFiled: June 19, 1990Date of Patent: September 22, 1992Assignee: FMC CorporationInventors: John A. Dixson, Natesan Murugesan, Keith D. Barnes
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Patent number: 5147876Abstract: 2,6-di-, 2,4,6-, 2,5,6-tri- or 2,4,5,6-tetra-substituted pyrimidines, and 2,6-di-substituted pyridines. These compounds are useful for treatment of neurological diseases.Type: GrantFiled: December 29, 1989Date of Patent: September 15, 1992Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Akira Mizuchi, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Mitsuyuki Takesue, Noriaki Kihara
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Patent number: 5145967Abstract: The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group.The anionic reagent in step (b) above has the general formula:X--CYM--Zwherein X is an anion stabilizing group, Y is hydrogen or lower-alkyl, Z is lower-alkoxy or phenylmethoxy, M is an alkali or alkaline earth metal, and C is a carbon atom.Type: GrantFiled: November 2, 1990Date of Patent: September 8, 1992Assignee: Anaquest, Inc.Inventors: Bor-Sheng Lin, H. Kenneth Spencer, Joseph W. Scheblein
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Patent number: 5141941Abstract: Disclosed are a compound of the formula (I) or an acid addition salt thereof: ##STR1## wherein Q represents R.sup.1 , R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n and z are defined as in the specification, preparation method thereof and fungicides containing the same.Type: GrantFiled: November 15, 1989Date of Patent: August 25, 1992Assignee: Ube Industries, Ltd.Inventors: Katsutoshi Fujii, Toshinobu Tanaka, Yasuhisa Fukuda
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Patent number: 5129941Abstract: Sulfonylureas of the formula ##STR1## where A is a bond or a C.sub.1 -C.sub.10 -hydrocarbon radical,R.sup.1 is an optionally unsaturated hydrocarbon radical which is optionally substituted by halogen, optionally unsaturated alkoxy, alkylthio, alkylsulfonyl or alkylsulfinyl, cycloalkyl, optionally substituted phenyl or a heterocycle, or is optionally substituted phenyl, NRR' with R and R' being alkyl, alkoxy or alkylene (cyclic with N),Y is S, SO or SO.sub.2,R.sup.1 is optionally unsaturated alkoxy which is optionally substituted, or is cycloalkoxy, cycloalkenyloxy, cyclopropylmethyloxy, epoxypropyloxy, furfuryloxy, tetrahydrofurfuryloxy or optionally substituted phenoxyalkoxy or phenoxy,R.sup.3 is alkyl which is optionally unsaturated, or is alkoxy,R.sup.4 is optionally substituted pyrimidinyl, pyrimidinylmethyl, pyrimidinyl with a fused-on cyclopentane, oxolane, oxolene, oxane, pyridine or pyrazine ring or purinyl or triazolyl, andZ is O or S,have herbicidal and/or plant-growth-regulatory properties.Type: GrantFiled: July 17, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Heinz-Josef Loher, Lothar Willms, Michael Frey, Klaus Bauer, Hermann Bierigner
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Patent number: 5126345Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.Type: GrantFiled: February 8, 1991Date of Patent: June 30, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: William A. Slusarchyk, Robert Zahler
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Patent number: 5126453Abstract: In a first stage of a process for the preparation of 6-piperidino-2,4-diaminopyrimidine-3-oxide at least one of the two amino groups of a compound having formula (1): ##STR1## where X represents a halogen atom or OH group, is protected by an addition reaction with an isocyanate having formula:R--N=C=OIn this formula R represents an alkyl group, or one of the amino groups. The resulting urea derivative is then oxidized to produce the corresponding N-oxide which is then reacted with piperidine. The protective group(s) are then eliminated by reaction with an organic or inorganic base.Type: GrantFiled: December 31, 1990Date of Patent: June 30, 1992Assignee: L'OrealInventors: Jean Maignan, Serge Restle, Gerard Lang
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Patent number: 5125960Abstract: Herbicidal substituted arylsulphonylaminoguanidinoazines of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,R.sup.2 represents hydroxyl or amino, or represents in each case optionally substituted alkoxy or alkylamino,R.sup.3 represents hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X represents nitrogen or a --CH group,Y represents nitrogen or a --CR.sup.4 group, where R.sup.4 represents hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl, andZ represents nitrogen or a --CR.sup.5 group, where R.sup.5 represents hydrogen, halogen, hydroxyl, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino,with the exception of the compound N'-(4,6-dimethylpyrimidin-2-yl)-N"-(2-methoxycarbonyl-phenylsulphonylamino )-N"'-(2-methoxycarbonyl-phenylsulphonyl)guanidine.Type: GrantFiled: August 1, 1990Date of Patent: June 30, 1992Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Hans-Jochem Riebel, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5118339Abstract: A pyrimidine or triazine derivative and its salt, said pyrimidine or triazine derivative having the formula: ##STR1## wherein R represents a group of the formula OR.sub.3 {wherein R.sup.3 represents a hydrogen atom, an alkyl gorup, etc.}, a group of the formula SR.sup.6 {wherein R.sup.6 represents a hydrogen atom, an alkyl group, etc.}, a group of the formula ##STR2## {wherein R.sup.7 and R.sup.8 represent a hydrogen atom, an alkyl group, etc.}, or an imidazolyl group:R.sup.1 represents a hydrogen atom, an alkyl group, etc.;R.sup.2 represents a hydroxyl group, an alkyl group, etc.;A and B represent an alkyl group, etc.;Y represents an oxygen atom, etc.; andZ represents a methine group or a nitrogen atom.Type: GrantFiled: December 20, 1990Date of Patent: June 2, 1992Assignees: Kumiai Chemical Co., Ihara Chemical Industry Co., Ltd.Inventors: Masatoshi Tamaru, Norihiro Kawamura, Masahiro Sato, Fumiaki Takabe, Shigehiko Tachikawa, Ryo Yoshida
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Patent number: 5116404Abstract: The present invention provides novel uracil derivatives and pesticides which contain the novel uracil derivatives as an active ingredient, and exhibit preventing and controlling effects against harmful living things, especially agricultural insect pests, sanitary insect pests, stored product insect pests, house insect pests and veterinary insect pests at a very low drug-concentration.Type: GrantFiled: January 8, 1991Date of Patent: May 26, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Shigeru Ishii, Kazunari Nakayama, Kazuo Yagi, Jun Satow, Kenzou Fukuda, Kaoru Itoh, Toshiyuki Umehara, Masaki Kudo, Yoichi Inoue, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 5104443Abstract: Compounds of the formula I or salts thereof ##STR1## where R.sup.1 is ethyl, propyl or isopropyl,R.sup.2 is halogen, NO.sub.2, CF.sub.3, CN, alkyl, alkoxy, alkylthio or alkoxycarbonyl,n is 0, 1, 2 or 3, Y is O or S,R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl or alkoxy;R.sup.4 is a heterocyclic radical of the formulae ##STR2## E is CH or N; G is O or CH.sub.2, R.sup.5 and R.sup.6 are hydrogen, halogen, or are alkyl, alkoxy or alkylthio, which are optionally substituted by halogen, alkoxy or alkylthio, or are --NR.sup.12 R.sup.13, --OCHR.sup.7 --CO.sub.2 R.sup.12, (C.sub.3 -C.sub.6 cycloalkyl, (C.sub.3 -C.sub.5)alkenyl, (C.sub.2 -C.sub.4) -alkynyl, (C.sub.3 -C.sub.5)alkenyloxy or (C.sub.3 -C.sub.5 (alkynyloxy; R.sup.7 is hydrogen or alkyl, R.sup.8 is alkyl, --CHF.sub.2 or --CH.sub.2 CF.sub.3 ; R.sup.9 and R.sup.10 are hydrogen, alkyl, alkoxy or halogen; R.sup.11 is hydrogen, alkyl, --CHF.sub.2 or CH.sub.2 CF.sub.3 ; R.sup.12 and R.sup.Type: GrantFiled: May 15, 1989Date of Patent: April 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5104440Abstract: The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylures of the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, nitro, amino, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 haloalkyl or a --Q--R.sub.7, --CO--OR.sub.8 or --(CO).sub.n --NR.sub.9 R.sub.10 radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, halogen or alkoxyalkyl containing not more than 4 carbon atoms,R.sub.3 is C.sub.2 -C.sub.10 alkenyl which is substituted by one or more fluorine or bromine atoms or by one or more hydroxyl, cyano, nitro, --(Y).sub.m --CO--(Z).sub.n --R.sub.8, --SO.sub.2 --NR.sub.11 R.sub.12, --S(O).sub.P --C.sub.1 -C.sub.3 haloalkyl or --S(O).sub.n --C.sub.1 -C.sub.3 alkyl groups and which may additionally be substituted by one or more chlorine atoms,R.sub.4 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.Type: GrantFiled: May 8, 1991Date of Patent: April 14, 1992Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Dieter Reinehr, Konrad Oertle, Rolf Schurter
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Patent number: 5102443Abstract: Heterocyclically substituted phenoxysulfonylureas, processes for the preparation thereof, and the use thereof as herbicides or plant growth regulators. Compounds of the formula I or the salts thereof ##STR1## where R.sup.1 is (C.sub.1 -C.sub.8)alkyl, (C.sub.2 -C.sub.8)alkenyl or (C.sub.2 -C.sub.8)alkynyl, these radicals being substituted by halogen, saturated or unsaturated (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylthio, -sulfinyl or -sulfonyl, (C.sub.1 -C.sub.6)alkoxycarbonyl, NO.sub.2, CN or phenyl; furthermore is (C.sub.2 -C.sub.8)alkenyl, (C.sub.2 -C.sub.8)alkynyl or (C.sub.3 -C.sub.8)cycloalkyl, which can be substituted by halogen or by alkoxy or alkylthio; (C.sub.5 -C.sub.8)cycloalkenyl, cyclopropylmethyl, epoxypropyl; furfuryl, tetrahydrofurfuryl or phenoxy (C.sub.1 -C.sub.4)alkyl, it being possible for the last three substituents mentioned to be substituted by halogen, alkyl or alkoxy; or phenyl which can be substituted by halogen, alkyl, alkoxy, NO.sub.2, CF.sub.3, CN or OCHF.sub.Type: GrantFiled: May 15, 1989Date of Patent: April 7, 1992Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5100896Abstract: The present invention provides a compound of formula (I) ##STR1## and salts and solvates and pharmaceutically acceptable derivatives thereof, and describes processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of viral diseases, especially those caused by the Herpetoviridae.Type: GrantFiled: July 23, 1990Date of Patent: March 31, 1992Assignee: Glaxo Group LimitedInventors: Alan D. Borthwick, Keith Biggadike, Barrie E. Kirk, Richard Storer, Niall G. Weir, Anthony D. Baxter, Chi L. Mo
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Patent number: 5096905Abstract: The invention relates to elaiophylin derivatives of the formulae (I), (I'), (III) and (III') ##STR1## in which the C.dbd.C double bonds in the 2,3 and 4,5 position may also be hydrogenated and in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings indicated. The invention furthermore relates to a process for the preparation of these elaiophylin derivatives, and the use thereof as pharmaceuticals, in particular as anthelmintic pharmaceuticals.Type: GrantFiled: September 14, 1989Date of Patent: March 17, 1992Assignee: Hoechst AktiengesellschaftInventors: Gerhard Kretzschmar, Peter Hammann, Dieter Duwel, Gerhard Wohner, Rudiger Marquardt, Klaus Kuhlein
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Patent number: 5092917Abstract: Herbicidal aminoguanidinoazines of the formula ##STR1## in which R.sup.1 stands for an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and hetaryl,R.sup.2 stands for hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X stands for nitrogen or a --CH group,Y stands for nitrogen or a --CR.sup.3 group whereR.sup.3 stands for hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl, andZ stands for nitrogen or a --CR.sup.4 group whereR.sup.Type: GrantFiled: May 19, 1989Date of Patent: March 3, 1992Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Hans-Jochem Riebel, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5087697Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. The invention also relates to pharmaceutical formulations and processes for the preparation of compounds according to the invention.Type: GrantFiled: December 19, 1990Date of Patent: February 11, 1992Assignee: Burroughs Wellcome Co.Inventor: Susan M. Daluge
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Patent number: 5086177Abstract: A process for the preparation of an oxyguanidine of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2, R.sup.3 each is hydrogen or an organic or inorganic substituent,X is N or CH,Y is N or CR.sup.3, andZ is N or CR.sup.4,comprising reacting ##STR2## in which R.sup.5 is optionally substituted alkyl or aralkyl, or its hydrogen halide, with a hydroxylamine derivative of the formulaH.sub.2 N--O--R.sup.1 (III)at a temperature between about 0.degree. C. and 150.degree. C. New isothioureas of the formula ##STR3## are also shown.Type: GrantFiled: May 24, 1990Date of Patent: February 4, 1992Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Klaus-Helmut Muller
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Patent number: 5071469Abstract: This invention relates to certain herbicidal sulfonamides, agriculturally suitable compositions thereof and a method for their use as a general or selective preemergent or postemergent herbicide or as a plant growth regulant.Type: GrantFiled: January 24, 1990Date of Patent: December 10, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Steven P. Artz
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Patent number: 5069710Abstract: N-((6-Trifluoromethylpyrimidin-2-yl)- aminocarbonyl)-2-carboalkoxybenzenesulfonamides of the general formula Ia ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen or halogen;R.sup.2 is hydrogen, C.sub.1 -C.sub.5 -alkyl, C.sub.3 -C.sub.4 -alkenyl, C.sub.3 -C.sub.4 -alkynyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.3 -C.sub.5 -alkoxyalkyl, C.sub.3 -C.sub.5 -haloalkoxyalkyl or C.sub.5 -C.sub.6 -cycloalkyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.2 -alkyl, allyl, propargyl or C.sub.1 -C.sub.5 -alkoxy,R.sup.4 is halogen, C.sub.1 -C.sub.2 -alkyl, C.sub.1 -C.sub.3 -alkylthio or C.sub.1 -C.sub.3 -alkylamino,R.sup.3 not denoting hydrogen or C.sub.1 -C.sub.2 -alkyl when R.sup.4 is C.sub.1 -C.sub.2 -alkyl, and their environmentally tolerated salts, processes for their manufacture, and their use.Type: GrantFiled: April 14, 1989Date of Patent: December 3, 1991Assignee: BASF AktiengesellschaftInventors: Karl-Otto Westphalen, Gerhard Hamprecht, Bruno Wuerzer, Norbert Meyer
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Patent number: 5068271Abstract: Disclosed are novel 2,4,6 substituted pyrimidines where the substituents may be the same or different groups. At least one substituent must be N-alkyl paraphenylenediamino, and the other substituents may be various radicals containing sulfur, oxygen or nitrogen or hydrogen or alkyl groups. The compounds are useful as antioxidants and antiozonants for unsaturated compounds and polymers.Type: GrantFiled: July 30, 1990Date of Patent: November 26, 1991Assignee: Uniroyal Chemical Company, Inc.Inventors: Edward L. Wheeler, Franklin H. Barrows, Robert J. Franko
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Patent number: 5066662Abstract: Oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones substituted in the 4-position of the oxazolidin-2-one ring and the 3-position of the 1,2,4-oxadiazolin-5-one ring with a 5- or 6-member heteroaromatic, a bicyclic heteroaromatic group or a 5- or 6-member heterocyclic group either directly or via a one or two carbon bridge and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetycholine production or release.Type: GrantFiled: May 21, 1990Date of Patent: November 19, 1991Assignee: Warner-Lambert CompanyInventors: Sheila H. Hobbs, Stephen J. Johnson
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Patent number: 5066663Abstract: Substituted-hetero-cyclopentanones and cyclopentenones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: May 21, 1990Date of Patent: November 19, 1991Assignee: Warner-Lambert CompanyInventor: Sheila H. Hobbs
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Patent number: 5066665Abstract: Substituted isoxazolidin-3-ones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: May 21, 1990Date of Patent: November 19, 1991Assignee: Warner-Lambert Co.Inventor: Sheila H. Hobbs
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Patent number: 5047409Abstract: Salts of thiazolidine-4-carboxylic acids with 6-Piperidino-2,4-diaminopyrimidine-3-oxide are described of Formula I. ##STR1## Compounds I are useful in the field of cosmetics and pharmaceuticals for the treatment of loss of hair or in pathological forms such as alopecia, flaking dermatitis, etc. . . . Topical formulations containing compounds I are also described.Type: GrantFiled: May 21, 1986Date of Patent: September 10, 1991Assignee: Serono OTC S.A.Inventors: Michele G. Di Schiena, Vittoria Orru
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Patent number: 5043443Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.Type: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 5030270Abstract: Sulfonylureas with heterocyclic substituents, a process for the preparation thereof, and the use thereof as herbicides or plant-growth regulators.Sulfonylureas with heterocyclic substituents, of the formula ##STR1## in which the variables are defined in the specification, as well as the salts thereof have herbicidal and plant-growth regulatory properties on mon- and dicotyledonous plants.Type: GrantFiled: August 3, 1989Date of Patent: July 9, 1991Assignee: Hoechst AktiengesellschaftInventors: Heinz-Josef Loher, Lothar Willms, Michael Frey, Klaus Bauer, Hermann Bieringer
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Patent number: 5015284Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.Type: GrantFiled: April 6, 1989Date of Patent: May 14, 1991Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4987135Abstract: A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R.sup.1 is --X.sup.1 Z.sup.1 (X.sup.1 is an oxygen atom or a sulfur atom and Z.sup.1 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), --COZ.sup.1 group (Z.sup.1 is as defined above), ##STR3## group (Z.sup.1 is as defined above, Z.sup.2 is --CO.sub.2 Z.sup.3 wherein Z.sup.3 is the same as Z.sup.1, or --SO.sub.2 Z.sup.3 wherein Z.sup.3 is as defined above and n is 0 or 1), ##STR4## (Z.sup.1 and Z.sup.3 are as defined above) or ##STR5## (X.sup.2, X.sup.3 and X.sup.4 are, respectively, an oxygen atom or a sulfur atom and Z.sup.4 and Z.sup.5 are the same as Z.sup.1), and R.sup.3 is a nitro group or ##STR6## (R.sup.4 and R.sup.Type: GrantFiled: March 16, 1989Date of Patent: January 22, 1991Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi, Hiroshi Okada
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Patent number: 4985563Abstract: In a first stage of a process for the preparation of 6-piperidino-2,4-diaminopyrimidine-3-oxide at least one of the two amino groups of a compound having formula (1): ##STR1## where x represents a halogen atom or OH group, is protected by an addition reaction with an isocyanate having formula:R--N=C=OIn this formula R represents an alkyl group, or one of the amino groups. The resulting urea derivative is then oxidized to produce the corresponding N-oxide which is then reacted with piperidine. The protective group(s) are then eliminated by reaction with an organic or inorganic base.Type: GrantFiled: July 29, 1988Date of Patent: January 15, 1991Assignee: L'OrealInventors: Jean Maignan, Serge Restle, Gerard Lang
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Patent number: 4983608Abstract: This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or lowealkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.Type: GrantFiled: September 5, 1989Date of Patent: January 8, 1991Assignee: Hoechst-Roussell Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
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Patent number: 4980469Abstract: A process for the preparation of an oxyguanidine of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2, R.sup.3 and R.sup.4 each is hydrogen or an organic or inorganic substituent,X is N or CH,Y is N or CR.sup.3, andZ is N or CR.sup.4,comprising reacting ##STR2## in which R.sup.5 is optionally substituted alkyl or aralkyl, or its hydrogen halide, with a hydroxylamine derivative of the formulaH.sub.2 N--O--R.sup.1 (III)at a temperature between about 0.degree. C. and 150.degree. C. New isothioureas of the formula ##STR3## are also shown.Type: GrantFiled: August 30, 1989Date of Patent: December 25, 1990Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Klaus-Helmut Muller
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Patent number: 4970063Abstract: A compound has the following composition: ##STR1## or its corresponding ionic form: ##STR2## wherein: n equals 0, 1 or 2, andR.sub.1 and R.sub.2 may be identical or different and represent a hydrogen atom or a linear or branched low alkyl radical having 1 to 6 carbon atoms.Type: GrantFiled: July 29, 1988Date of Patent: November 13, 1990Assignee: L'OrealInventors: Gerard Lang, Jean Maignan, Serge Restle
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Patent number: 4968796Abstract: Disclosed is a process for the preparation of a sulphonylisothiourea of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, and Z are as defined herein, which comprises reacting a sulphonic acid amide of the formulaR.sup.1 --SO.sub.2 --NH.sub.2, (II)or a metal salt thereof, with an N-heteroaryl-iminodithiocarbonic acid S,S-diester of the formula ##STR2## at a temperature between about 20.degree. C. and 200.degree. C. Intermediates and a process for their preparation are also disclosed.Type: GrantFiled: August 17, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventor: Hans-Jochem Riebel
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Patent number: 4968781Abstract: A reactive dye of the formula ##STR1## in which Fa is the radical of an organic dye of the monoazo, polyazo, metal complex azo, anthraquinone, phthalocyanine, formazan, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide series, T is a negative substituent, one X is a detachable substituent and the other X is a group of the formula ##STR2## A is arylene, V is hydrogen, a substituted or unsubstituted C.sub.1 -C.sub.4 alkyl radical or a radical of the formula --(CH.sub.2).sub.q --SO.sub.2 --Z, Z is a --CH.dbd.CH.sub.2 or CH.sub.2 --Y radical and Y is an inorganic or organic radical which is detachable under alkaline conditions, q, m and n are independently of one another an integral number from 2 to 6, R and R' are independently of one another hydrogen or substituted or unsubstituted C.sub.1 -C.sub.4 alkyl, and r is 1 or 2.Type: GrantFiled: March 28, 1988Date of Patent: November 6, 1990Assignee: Ciba-Geigy CorporationInventors: Karl Seitz, Karl Hoegerle
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Patent number: 4963180Abstract: Compounds of the formula I or their salts ##STR1## wherein R.sup.1 denotes substituted alkyl; (subst.) alkenyl; (subst.) alkynyl; R.sup.2 denotes halogen; nitro; (subst.) alkyl or (subst.) alkoxy; R.sup.3 denotes hydrogen; alkyl; alkenyl or alkynyl; R.sup.4 denotes a heterocyclic radical or the formulae ##STR2## where E is CH or N; and n denotes 0, 1, 2 or 3, possess excellent herbicidal and plant growth-regulating properties.Type: GrantFiled: August 3, 1988Date of Patent: October 16, 1990Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Heinz Kehne, Klaus Bauer, Hermann Bieringer
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Patent number: 4960888Abstract: The invention relates to a new process for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine of the formula (I), ##STR1## which comprises reacting a pyrimidine derivative of the general formula (II), ##STR2## wherein R.sub.1 stantds for hydrogen or a ##STR3## group, wherein R means a C.sub.1-6 alkyl group or an aryl group optionally substituted by halogen;R.sub.2 stands for a hydroxyl group or an ##STR4## group, wherein R is as defined above; andX represents chlorine or bromine or an optionally mono- or polysubstituted arenesulfonyloxy group,with the proviso that R.sub.2 is different from a hydroxyl group when R.sub.1 stands for hydrogen, with piperidine and hydrolyzing, optionally after isolation, the thus-obtained 4-piperidino derivative of the general formula (III), ##STR5## wherein R.sub.1 and R.sub.2 are as defined above.Type: GrantFiled: March 9, 1989Date of Patent: October 2, 1990Assignee: Richter Gedeon Vegyeszeti Gyar R.T.Inventors: Andras Vedres, Csaba Szantay, Bela Stefko, Janos Kreidl, Andras Nemes, Gabor Blasko, Erik Bogsch, Denes Mathe, Istvan Hegedus, Adrien Szuchovszky, nee Gergely, Tamas Mester
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Patent number: 4959474Abstract: A novel class of 2,4-diamino-6-(2,5-dialkoxybenzyl)-5-methyl[2,3-d]-pyrimidines is described. These compounds are antibacterial agents, active against certain Streptococcus species. They are also active antiproliferative agents.Type: GrantFiled: October 15, 1985Date of Patent: September 25, 1990Assignee: Burroughs Wellcome Co.Inventor: Eugene M. Grivsky
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Patent number: 4954628Abstract: The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.Type: GrantFiled: March 2, 1989Date of Patent: September 4, 1990Assignees: Nitrokaelepek, Magyar Tudomanyos Akademia Kozponti Kemiai Kutato IntezeteInventors: Gabor Besenyei, Sandor Nemeth, Laszlo Simandi, Maria Belak, Maria Szabo, Jozsef Dukai, Lajos Nagy, Elemer Tomordi, Csaba Soptei, Erzsebet E. Dioszegine
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Patent number: 4952679Abstract: Reactive dyes suitable for dyeing and printing cellulosic fiber materials by the cold pad-batch process having the formula ##STR1## wherein Fa is a monoazo or polyazo, metal complex azo, anthraquinone, phthalocyanine, formazane, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide dye radical, X.sub.1 is halogen, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl, a sulfonic acid or phosphoric acid group or a quaternized ammonium group, X.sub.2 independently has the meaning of X.sub.1 or is C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, carboxyl, sulfo, sulfato, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 alkoxy, R is hydrogen or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, carboxyl, sulfo, sulfato, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 -alkoxy, and r is 1 or 2.Type: GrantFiled: August 19, 1988Date of Patent: August 28, 1990Assignee: Ciba-Geigy CorporationInventor: Karl Hoegerle
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Patent number: 4952233Abstract: Herbicidally active sulphonylamino guanidinoazines of the formula ##STR1## in which R.sup.1 stands for a optionally substituted radical from the series comprising alkyl, aralkyl, aryl and hetaryl, R.sup.2 stands for an optionally substituted radical from the series comprising alkyl, aralkyl, aryl, hetaryl and dialkylamino, R.sup.3 stands for hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X stands for nitrogen or a --CH-- grouping,Y stands for nitrogen or a --CR.sup.4 -- grouping,whereinR.sup.4 stands for hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl,Z stands for mitrogen or a --CR.sup.5 -- grouping,whereinR.sup.Type: GrantFiled: August 2, 1988Date of Patent: August 28, 1990Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Muller, Christa Fest, Rolf Kirsten, Theodor Pfister, Hans-Jochem Riebel, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 4948416Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.Type: GrantFiled: March 27, 1989Date of Patent: August 14, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4946956Abstract: Disclosed are novel 2,4,6 substituted pyrimidines where the substituents may be the same or different groups. At least one substituent must be N-alkyl parphenylenediamino, and the other substituents may be various radicals containing sulfur, oxygen or nitrogen or hydrogen or alkyl groups. The compounds are useful as antioxidants and antiozonants for unsaturated compounds and polymers.Type: GrantFiled: September 21, 1988Date of Patent: August 7, 1990Assignee: Uniroyal Chemical Company, Inc.Inventors: Edward L. Wheeler, Franklin H. Barrows, Robert J. Franko
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Patent number: 4944792Abstract: N-phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the general formula ##STR1## and the salts of these compounds with amines, alkali metal or alkaline-earth metal bases or with quaternary ammonium bases have good selective, pre- and post-emergence, herbicidal and growth-regulating properties.The symbols in this formula have the following meanings:A is a C.sub.3 -C.sub.6 -alkynyl group, a C.sub.1 -C.sub.6 -alkyl group which is substituted by halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl, C.sub.1 -C.sub.4 -alkylsulfonyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.1 -C.sub.4 -haloalkylsulfinyl or C.sub.1 -C.sub.4 -haloalkylsulfonyl, or it is a C.sub.2 -C.sub.6 -alkenyl group substituted by one of the above substituents,E is the methine group or nitrogen,X is oxygen, sulfur, or a sulfinyl or sulfonyl bridge,Z is oxygen or sulfur,m is the number one or two,R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.2 -C.sub.Type: GrantFiled: January 16, 1986Date of Patent: July 31, 1990Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Werner Fory, Karl Gass
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Patent number: 4945093Abstract: A compound having formula: ##STR1## is described, where R.sub.3 and R.sub.4 may be identical or different and represent a hydrogen atom, alkyl, alkenyl, cycloalkyl;or R.sub.3 and R.sub.4 represent aryl aralkyl;or R.sub.3 and R.sub.4 together with the nitrogen atom linked thereto form a heterocycle;R.sub.1 and/or R.sub.2, independent of each other, represent hydrogen or carbanoyl having formula: ##STR2## where R.sub.7 represents alkyl, alkenyl, cycloalkyl, aryl or aralkyl. The compounds of formula (I) can be used in cosmetic or pharmaceutical compositions for the cosmetic treatment of hair, the treatment of alopecia, and also for the treatment of desquamating dermatitis.Type: GrantFiled: July 29, 1988Date of Patent: July 31, 1990Assignee: L'OrealInventors: Jean Maignan, Serge Restle, Gerard Lang
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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: 4940792Abstract: Novel substituted N-sulfonyl-N'-pyrimidinylureas or N-sulfonyl-N'-triazinylureas of the formula I ##STR1## have good pre- and postemergence selective herbicidal and growth regulating properties.In this formulaE is nitrogen or --CH.dbd.,the group ##STR2## is a phenyl, naphthyl, furyl, thiophenyl, pyrrole or pyridinyl radical which is substituted in accordance with the definitions ofR.sup.1 and R.sup.2,R.sup.3 and R.sup.4 are hydrogen, lower alkyl or lower alkoxy, or one of R.sup.3 and R.sup.4 may also be halogen, lower alkenyl, lower haloalkenyl, lower haloalkoxy, amino, lower alkylamino, --CH(OCH.sub.3).sub.2, a cyclized ketal group or a saturated 5- or 7-membered heterocycle which is bound through the nitrogen atom,R.sup.5 is hydrogen, lower alkyl, lower haloalkyl, or an unsubstituted or substituted phenyl, benzyl or naphthyl radical, andR.sup.Type: GrantFiled: December 4, 1987Date of Patent: July 10, 1990Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Willy Meyer, Hans-Dieter Schneider
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Patent number: RE33298Abstract: The invention relates to new 1-(2-oxyaminosulphonylphenylsulphonyl)-3-heteroaryl-ureas of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl and aralkyl andR.sup.Type: GrantFiled: June 21, 1989Date of Patent: August 14, 1990Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt