Patents Examined by C. Shen
  • Patent number: 4840662
    Abstract: 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: Grant
    Filed: July 16, 1984
    Date of Patent: June 20, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Adolf Hubele, Robert Nyfeler
  • Patent number: 4833141
    Abstract: 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: Grant
    Filed: July 2, 1987
    Date of Patent: May 23, 1989
    Assignee: Heumann Pharma GmbH & Co.
    Inventors: Helmut Schickaneder, Rolf Herter, Hartmut Vergin, Heidrun Engler, Kurt H. Ahrens
  • Patent number: 4792554
    Abstract: 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: Grant
    Filed: November 21, 1986
    Date of Patent: December 20, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Elben, Hiristo Anagnostopulos, Robert R. Bartlett
  • Patent number: 4791111
    Abstract: 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: Grant
    Filed: October 16, 1986
    Date of Patent: December 13, 1988
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo J. J. Backx, Jozef B. A. Thijssen, Alfonsus G. Knaeps
  • Patent number: 4728649
    Abstract: 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: Grant
    Filed: January 8, 1986
    Date of Patent: March 1, 1988
    Assignee: Farmitalia Carlo Erba
    Inventors: Sergio Mantegani, Aldemio Temperilli, Gabriella Traquandi, Alessandro Rossi, Lorenzo Pegrassi
  • Patent number: 4695635
    Abstract: 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: Grant
    Filed: March 28, 1985
    Date of Patent: September 22, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Gregor Haffer
  • Patent number: 4690929
    Abstract: 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: Grant
    Filed: April 26, 1984
    Date of Patent: September 1, 1987
    Assignee: Farmitalia Carlo Erba
    Inventors: Luigi Bernardi, Laura Chiodini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Patricia Salvati
  • Patent number: 4689327
    Abstract: 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: Grant
    Filed: June 24, 1985
    Date of Patent: August 25, 1987
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Hideo Nakai, Hiroshi Wada, Taku Nagao, Hideo Yabana
  • Patent number: 4670456
    Abstract: 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: Grant
    Filed: May 24, 1985
    Date of Patent: June 2, 1987
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Dieter Hinzen, Franz J. Kuhn, Erich Lehr, Helmut Ensinger, Wolfgang Troger
  • Patent number: 4661481
    Abstract: Compounds of the formula ##STR1## having activity as antihistamine or inhibitors of mediator release from basophils or mast cells.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: April 28, 1987
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc
    Inventors: John P. Devlin, Karl D. Hargrave, Edward L. Barsumian, Genus J. Possanza
  • Patent number: 4659728
    Abstract: 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: Grant
    Filed: February 25, 1985
    Date of Patent: April 21, 1987
    Assignee: American Home Products Corporation
    Inventors: Alan J. Lewis, Richard P. Carlson, Horace Fletcher, 3rd
  • Patent number: 4656173
    Abstract: 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: Grant
    Filed: April 24, 1985
    Date of Patent: April 7, 1987
    Assignee: Bristol-Myers Company
    Inventors: Joseph P. Yevich, Walter G. Lobeck, Jr.
  • Patent number: 4652569
    Abstract: 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: Grant
    Filed: March 4, 1985
    Date of Patent: March 24, 1987
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Katsutoshi Ishikawa, Hitoshi Shimotori, Noboru Iida, Shuji Ozawa, Shunichi Inami
  • Patent number: 4595535
    Abstract: 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: Grant
    Filed: August 22, 1984
    Date of Patent: June 17, 1986
    Assignee: Ciba-Geigy Corporation
    Inventor: Isidoros Vlattas
  • Patent number: 4590272
    Abstract: Pesticidally active novel nitromethylene-tetrahydropyrimidines of the formula ##STR1## wherein X represents a halogen atom.
    Type: Grant
    Filed: October 3, 1984
    Date of Patent: May 20, 1986
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Kozo Shiokawa, Shinzo Kagabu, Shinichi Tsuboi