Patents Examined by C. Shen
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Patent number: 4840662Abstract: The invention discloses novel N-(2-nitrophenyl)-5-aminopyrimidine derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently NO.sub.2 or CF.sub.3, or one of R.sub.1 and R.sub.2 is hydrogen,R.sub.3 is hydrogen or halogen,R.sub.4 is hydrogen or the --C(O)R' group, in which R' is C.sub.1 -C.sub.4 alkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio,R.sub.5, R.sub.6 and R.sub.7 are each independently hydrogen, halogen, nitro, cyano, thiocyano, mercapto, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxy which is substituted by halogen, nitro, cyano, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio and/or N(C.sub.1 -C.sub.4 alkyl).sub.2 ; or are C.sub.3 -C.sub.6 cycloalkoxy, C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.6 alkylthio, C.sub.3 -C.sub.6 alkenylthio, C.sub.1 -C.sub.6 alkylsulfonyl, C.sub.1 -C.sub.6 alkylsulfoxyl, C.sub.3 -C.sub.Type: GrantFiled: July 16, 1984Date of Patent: June 20, 1989Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Adolf Hubele, Robert Nyfeler
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Patent number: 4833141Abstract: The invention relates to new 1,4-piperazine compounds corresponding to the following general formula ##STR1## which show improved antimycotic activity in relation to the known compounds miconazol and ketoconazol.Type: GrantFiled: July 2, 1987Date of Patent: May 23, 1989Assignee: Heumann Pharma GmbH & Co.Inventors: Helmut Schickaneder, Rolf Herter, Hartmut Vergin, Heidrun Engler, Kurt H. Ahrens
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Patent number: 4792554Abstract: A pyridine compound of the formula I ##STR1## in which R.sup.1 and R.sup.2 independently of each other represent hydrogen or alkyl having from 1 to 4 carbon atoms,R.sup.3 represents hydrogen or alkyl having up to 2 carbon atoms andA represents alkylene having 2 to 4 carbon atoms, n is O or 1,Z is a group of the formula Za, Zb or Zc ##STR2## in which either R.sup.4 is hydrogen andR.sup.5 is phenyl or cinnamyl orR.sup.4, R.sup.5, R.sup.7 and R.sup.8 independently of each other are pyridyl, phenyl or phenyl which is substituted by up to 2 equal or different substituents from the group halogen and alkoxy having up to 2 carbon atoms,R.sup.6 is hydrogen or hydroxy andX is hydrogen, a cyano, amino or nitro group or the group --CO--R.sup.9, in whcih R.sup.9 is hydroxy or alkoxy having from 1 to 4 carbon atoms,and the physiologically tolerable salts of these compounds. The invention also relates to a process for the manufacture of such compounds and to their use in pharmaceutical compositions.Type: GrantFiled: November 21, 1986Date of Patent: December 20, 1988Assignee: Hoechst AktiengesellschaftInventors: Ulrich Elben, Hiristo Anagnostopulos, Robert R. Bartlett
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Patent number: 4791111Abstract: Novel [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles, having anti-microbial activity, compositions containing the same, and methods of inhibiting and/or eliminating the development of fungi and bacteria in warm-blooded animals suffering from diseases caused by these fungi and/or bacteria.Type: GrantFiled: October 16, 1986Date of Patent: December 13, 1988Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo J. J. Backx, Jozef B. A. Thijssen, Alfonsus G. Knaeps
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Patent number: 4728649Abstract: The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: January 8, 1986Date of Patent: March 1, 1988Assignee: Farmitalia Carlo ErbaInventors: Sergio Mantegani, Aldemio Temperilli, Gabriella Traquandi, Alessandro Rossi, Lorenzo Pegrassi
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Patent number: 4695635Abstract: 2-bromoergolines can be reduced in good yields, without dimerization as determined by NMR product analysis, to the corresponding 2,3-dihydroergolines under otherwise conventional reducing conditions by introducing 2-bromoergolines, together with sodium borohydride, into trifluoroacetic acid under cooling to prevent the reaction mixture from rising above ambient temperature.Type: GrantFiled: March 28, 1985Date of Patent: September 22, 1987Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Gregor Haffer
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Patent number: 4690929Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.Type: GrantFiled: April 26, 1984Date of Patent: September 1, 1987Assignee: Farmitalia Carlo ErbaInventors: Luigi Bernardi, Laura Chiodini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Patricia Salvati
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Patent number: 4689327Abstract: A novel thiazolidine derivative of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl group, Q is a single bond, a lower alkylene group or a lower alkenylene group, R.sup.2 and R.sup.3 are the same or different and each is hydrogen atom, a lower alkyl group, a cycloalkyl group, a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkylsulfonyl group, a benzoyl group, a phenyl group or a di(lower alkyl)phosphoryl group, Alk is a lower alkylene group, and Y and Z are the same or different and each is oxygen atom or sulfur atom, or a pharmaceutically acceptable salt thereof, which is useful as a cardiotonic agent is disclosed together with processes for the preparation of the compound and a pharmaceutical composition containing said compound.Type: GrantFiled: June 24, 1985Date of Patent: August 25, 1987Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hideo Nakai, Hiroshi Wada, Taku Nagao, Hideo Yabana
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Patent number: 4670456Abstract: The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.Type: GrantFiled: May 24, 1985Date of Patent: June 2, 1987Assignee: Boehringer Ingelheim KGInventors: Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Dieter Hinzen, Franz J. Kuhn, Erich Lehr, Helmut Ensinger, Wolfgang Troger
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Patent number: 4661481Abstract: Compounds of the formula ##STR1## having activity as antihistamine or inhibitors of mediator release from basophils or mast cells.Type: GrantFiled: December 4, 1985Date of Patent: April 28, 1987Assignee: Boehringer Ingelheim Pharmaceuticals, IncInventors: John P. Devlin, Karl D. Hargrave, Edward L. Barsumian, Genus J. Possanza
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Patent number: 4659728Abstract: This invention discloses 5-(4-hydroxyphenyl)-4-phenyl-2-oxazolepropanoic acid, 4-(4-hydroxyphenyl-5-phenyl-2-oxazolepropanoic acid and pharmaceutically acceptable salts thereof as antiinflammatory agents, pharmaceutical compositions thereof and methods for their use.Type: GrantFiled: February 25, 1985Date of Patent: April 21, 1987Assignee: American Home Products CorporationInventors: Alan J. Lewis, Richard P. Carlson, Horace Fletcher, 3rd
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Patent number: 4656173Abstract: 8-[4-[4-(1-Oxo-1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5 ]decane-7,9-dione is an antipsychotic agent having reduced side effect liability.Type: GrantFiled: April 24, 1985Date of Patent: April 7, 1987Assignee: Bristol-Myers CompanyInventors: Joseph P. Yevich, Walter G. Lobeck, Jr.
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Patent number: 4652569Abstract: Disclosed herein are thiocyanopyrimidine derivatives represented by the following general formula: ##STR1## wherein R means an alkyl group having 1-3 carbon atoms and X denotes a halogen atom, their production process, and agricultural and horticultural fungicides containing same as active ingredients. The compounds of this invention can provide ideal agricultural and horticultural fungicides, since they exhibit outstanding fungicidal activities against plant pathogens led by late blight and downy mildew, their toxicity to animals are low and they are not phytotoxic.The compounds of this invention can be obtained by reacting pyrimidine derivatives represented by the following general formula: ##STR2## with thiocyanates while using an organic acid as a solvent. Good results can be obtained particularly when formic acid is used as a solvent.Type: GrantFiled: March 4, 1985Date of Patent: March 24, 1987Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Katsutoshi Ishikawa, Hitoshi Shimotori, Noboru Iida, Shuji Ozawa, Shunichi Inami
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Patent number: 4595535Abstract: Described are 5-diazacycloalkyltriazolo[2,3-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen, trifluoromethyl, lower alkylthio, lower alkoxy or lower alkyl; R.sub.2 represents hydrogen, lower alkyl or hydroxy-C.sub.2 -C.sub.7 alkyl wherein the hydroxy group is separated from the nitrogen atom by at least 2 carbon atoms; R.sub.3 represents hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen or trifluoromethyl; and C.sub.n H.sub.2n represents ethylene. The synthesis, pharmaceutical compositions and methods of use as neuroleptic and/or antihistaminic agents are given.Type: GrantFiled: August 22, 1984Date of Patent: June 17, 1986Assignee: Ciba-Geigy CorporationInventor: Isidoros Vlattas
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Patent number: 4590272Abstract: Pesticidally active novel nitromethylene-tetrahydropyrimidines of the formula ##STR1## wherein X represents a halogen atom.Type: GrantFiled: October 3, 1984Date of Patent: May 20, 1986Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinzo Kagabu, Shinichi Tsuboi