Patents Examined by James H. Turnipseed
  • Patent number: 4977166
    Abstract: New benzopyran derivatives of formula: ##STR1## in which R.sub.1 is hydrogen, halogen, hydroxy, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl) amino or acylamino,X is nitrogen or a >CH-radicalR is a radical of formula: ##STR2## in which A denotes a single bond or methylene or, when X is nitrogen, A may denote carbonyl, and R.sub.2 and R.sub.3, which are identical or different, are hydrogen, halogen, hydroxy, alkyl, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano, or, when they are adjacent, together form a methylenedioxy or ethylenedioxy radical, or elseR is pyridyl or 2(2H)-benzimidazolonyl if X denotes >CH--, andR' and R" are identical and are hydrogen or alkyl, their isomeric forms and mixtures thereof, and their acid addition salts, can be used as antiarrhythmic and antifibrillation agents.
    Type: Grant
    Filed: March 22, 1989
    Date of Patent: December 11, 1990
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Hardy, Christian Renault
  • Patent number: 4977167
    Abstract: A compound of the formula: ##STR1## (wherein R is phenoxy optionally substituted by a halogen, methoxy, or methyl group, ##STR2## one of A and B is ##STR3## and the other is >CH.sub.2 : R.sup.1 is hydrogen or C.sub.1 -C.sub.5 alkyl; Z.sup.1 is phenyl, benzyl, or isoxazolyl each optionally substituted by a halogen, methoxy, or methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, or phenyl optionally mono-, di-, or tri-substituted by a halogen, methoxy, or methyl group; or Z.sup.1 and Z.sup.2 taken together with the adjacent nitrogen atom may form 5-membered heterocyclic group; Z.sup.3 is C.sub.1 -C.sub.5 hydroxyalkyl, di(C.sub.1 -C.sub.5 alkyl)sulfamoyl, 6-membered heterocyclic group, phenyl, benzyl, or phenylsulfonyl each phenyl moiety of the last three members being optionally substituted by a halogen, methoxy, or methyl group; Z.sup.
    Type: Grant
    Filed: August 17, 1988
    Date of Patent: December 11, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiromu Matsumura, Toshisada Yano, Akira Matsushita, Masami Eigyo
  • Patent number: 4977265
    Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.
    Type: Grant
    Filed: May 15, 1990
    Date of Patent: December 11, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
  • Patent number: 4973691
    Abstract: An etheric derivative of 4(3H)-quinazolinone which is a fluorinated 3-[2-(4-biphenylyloxy)ethyl]-4(3H)-quinazolinone, produced by reacting said 4(3H)-quinazolinone with the corresponding fluorinated 4-(2-chloroethoxy)biphenyl, and its acid addition salts, especially the hydrochloride. This compound possesses substantially higher analgesic activity and lower acute toxicity than aminophenazone, ibuprofen, acetylosalicyclic acid and paracetamol.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: November 27, 1990
    Assignee: Spojene Podniky Prozdravotnickou Vyrobu (SPOFA)
    Inventors: Ludmila Fisnerova, Bohumila Brunova, Eva Maturova, Jaroslava Grimova
  • Patent number: 4971970
    Abstract: Novel 3-formyl-4-oxoquinoline compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkanoyl, R.sup.2 is hydrogen atom or a lower alkyl, R.sup.3 is a lower alkyl, and X is halogen, and pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.
    Type: Grant
    Filed: October 20, 1989
    Date of Patent: November 20, 1990
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Hisashi Miyamoto, Hiroshi Yamashita, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 4970063
    Abstract: 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: Grant
    Filed: July 29, 1988
    Date of Patent: November 13, 1990
    Assignee: L'Oreal
    Inventors: Gerard Lang, Jean Maignan, Serge Restle
  • Patent number: 4970310
    Abstract: Isoindoline compounds of the formula ##STR1## in which R is C.sub.1 -C.sub.4 alkyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-, C.sub.1 -C.sub.4 alkoxy- or halogen-substituted phenyl, benzyl or phenylethyl, R.sub.1 and R.sub.2, independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy and X is one of the groups of the formulae ##STR2## in which R, R.sub.1 and R.sub.2 are as defined above, A is one of the groups, --CN, --COO--(C.sub.1 -C.sub.4 alkyl) or --CONH--R.sub.5, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen or have the same meaning as R, V is --NH-- or --O-- and Z is --O--, --S--, --NH-- or --NH(CH)--.These isoindolines containing at least one N-substituted quinazolone radical are distinguished by excellent pigment properties, in particular by very high weather fastness.
    Type: Grant
    Filed: August 17, 1989
    Date of Patent: November 13, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Jost von der Crone
  • Patent number: 4968797
    Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicalsX.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.
    Type: Grant
    Filed: October 30, 1987
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
  • Patent number: 4968698
    Abstract: Compounds of the formula (III): ##STR1## or salts or acyl derivatives thereof, for use as antifungal and antiprotozoal agents are disclosed. Compositions containing the compounds are also disclosed as are method for the preparation of the compounds and intermediates in their preparation.
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: November 6, 1990
    Assignee: Burroughs Wellcome Co.
    Inventor: Karl W. Franzmann
  • Patent number: 4966622
    Abstract: The present invention relates to novel N-phenyl-N-pyrimidin-2-ylureas having a herbicidal and plant growth-regulating activity, to agrochemical compositions containing those substances as active ingredients, to the use of the novel ureas for controlling weeds or for regulating plant growth, and to processes for the preparation of the novel compounds. The invention also relates to novel intermediates and to processes for the preparation thereof.The novel compounds correspond to formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are each, independently of the others, hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 alkoxy; C.sub.1 -C.sub.4 haloalkyl; C.sub.1 -C.sub.4 haloalkoxy; C.sub.1 -C.sub.4 alkyl-S(O).sub.n -; nitro; cyano; C.sub.1 -C.sub.4 alkoxycarbonyl; C.sub.1 -C.sub.4 alkylcarbonyl; di-(C.sub.1 -C.sub.4 alkylamino)-carbonyl; mono-(C.sub.1 -C.sub.4 alkylamino)carbonyl; carbamoyl; C.sub.1 -C.sub.4 haloalkyl-S(O).sub.n -; or -PO[O-(C.sub.1 -C.sub.4)-alkyl].sub.2 ;R.sup.4 is C.sub.1 -C.
    Type: Grant
    Filed: April 3, 1989
    Date of Patent: October 30, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Hermann Rempfler, Dieter Durr, Rudolf C. Thummel
  • Patent number: 4965261
    Abstract: A rifamycin derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, methyl group or ethyl group, R.sup.2 is an alkyl group having 1 to 4 carbon atoms, and A is a group having the formula: ##STR2## in which n is an integer of 3 to 5, or group having the formula: ##STR3## in which R.sup.3 is a alkyl group having 1 to 5 carbon atoms; or a salt thereof. The rifamycin derivative (I) exhibits a strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria, and also exhibits a strong antibacterial activity against tubercle bacilli.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: October 23, 1990
    Assignee: Kanegafuchi Kagaku Kogyo Kabushiki Kaisha
    Inventors: Fumihiko Kanoo, Takehiko Yamane, Hideo Kondo, Takuji Hashizume, Katsuji Yamashita, Kazunori Hosoe, Fumiyuki Kuze, Kiyoshi Watanabe
  • Patent number: 4965360
    Abstract: Novel 4-amino-6,7-dimethoxy-2-(6,7-disubstituted-1,2,3,4-tetrahydroisoquinol-2-y l)quinoline compounds have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred compounds include 4-amino-6,7-dimethoxy-2-(6-hydroxy-7-methoxy-1,2,3,4-tetrahydroisoquinol-2 -yl)quinoline and 4-amino-6,7-dimethoxy-2-(7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinol-2 -yl)-quinoline. Methods for preparing these compounds from known starting materials are provided.
    Type: Grant
    Filed: August 23, 1989
    Date of Patent: October 23, 1990
    Assignee: Pfizer Inc.
    Inventor: Nigel J. Cussans
  • Patent number: 4965266
    Abstract: Heteroarylcarboxamide derivatives of the formula I: ##STR1## wherein A means an alkylene group, X means <NCHPh.sub.2 or <C.dbd.CPh.sub.2 in which Ph means phenyl and .circle.Het means a group of the formulas: ##STR2## in which Y means nitrogen atom or .dbd.CH--, R.sub.1 means hydroxy, a lower alkoxy or mercapto, R.sub.2 means hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, nitro or cyano, R.sub.3 means a lower alkyl group, provided that R.sub.2 is attached at the 7-position when Y means nitrogen atom, or physiologically acceptable salts thereof, a process for preparing the same and a pharmaceutical composition containing the same as an active ingredient. The compounds of the present invention and salts thereof show an excellent antiallergic activity and thus are useful for the prophylaxis and treatment of allergic diseases.
    Type: Grant
    Filed: October 18, 1988
    Date of Patent: October 23, 1990
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Hitoshi Uno, Tatsuya Kon, Yoshinori Nishikawa, Tokuhiko Shindo, Hideo Nakamura, Katsumi Ishii
  • Patent number: 4963563
    Abstract: Compounds of the formula: ##STR1## wherein n=1 or 2; R.sub.1 is lower alkoxy, lower alkyl, halo, ester, carbamate, or substituted amino; and R.sub.2 is thienyl or furyl; or R.sub.2 is ##STR2## wherein R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, hydroxy, methoxy, thioalkoxy, substituted amino and lower alkyl; and pharmaceutically acceptable salts thereof.These compounds are useful as inhibitors of alpha-2-adrenergic receptors and for the treatment of glaucoma and/or controlling intraocular pressure.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: October 16, 1990
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, Robert E. Zelle
  • Patent number: 4963685
    Abstract: Novel Tetrahydroisoquino[2,1-c][1,3]benzodiazepines are disclosed having the formula ##STR1## where X and Y are each independently hydrogen, halogen, loweralkyl, loweralkoxy or --CF.sub.3, and R is hydrogen or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility in enhancing memory.
    Type: Grant
    Filed: December 21, 1989
    Date of Patent: October 16, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Lawrence L. Martin, Richard C. Allen
  • Patent number: 4963554
    Abstract: Novel 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides and their synthesis are described. These novel compounds are cardiotonic agents and bronchodilating agents, and as such are useful for the treatment of heart failure and asthma.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: October 16, 1990
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Donald W. Combs, Robert Falotico, David M. Ritchie
  • Patent number: 4962200
    Abstract: A novel nitrogen-containing compound capable of preventing hardening of blood vessels by controlling formation of peroxide lipids in cell membranes, which is valuable as an anti-arteriosclerotic agent, is disclosed.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: October 9, 1990
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Noriaki Kihara, Ikuo Tomino, Hiroaki Tan, Takafumi Ishihara
  • Patent number: 4962113
    Abstract: Novel pyridinium derivatives represented by the formula (I): ##STR1## wherein ##STR2## is an optionally substituted pyridinium ring; R.sup.1 is a lower alkyl group or aralkyl group;R.sup.7 and R.sup.10 are independently hydrogen, a lower alkyl group, aryl group or aralkyl group;l is 0 or 1;R.sup.5 is a phenylene group or an alkylene group which may be substituted;R.sup.11 is an alkyl group or aryl group;X is a group of the formula: --CH.sub.2 OCH.sub.2 -- or a group of the formula: ##STR3## wherein R.sup.6 is hydrogen, a lower alkyl or a lower alkoxy, and m is an integer of 0 to 3;U is a group of the formula: ##STR4## wherein R.sup.
    Type: Grant
    Filed: July 26, 1988
    Date of Patent: October 9, 1990
    Assignee: Takeda Chemical Industries, Ltd
    Inventors: Susumu Tsushima, Muneo Takatani, Kohei Nishikawa
  • Patent number: 4962112
    Abstract: Naphthyridine and quinoline compounds having the formula: ##STR1## wherein A is CH or N; Z is an amine having the formula: ##STR2## R is o,p-difluorophenyl or p-fluorophenyl; and R.sub.1 is hydrogen or a carboxy protecting group. The compounds of the invention have antibacterial activity and improved solubility and pharmacokinetic properties.
    Type: Grant
    Filed: February 26, 1988
    Date of Patent: October 9, 1990
    Assignee: Abbott Laboratories
    Inventors: Terry J. Rosen, Daniel T. Chu
  • Patent number: 4960893
    Abstract: Halogenated hydroxyquinoline compounds such as 5-chloro-7-bromomethyl-8-hydroxyquinoline are prepared by contacting a 5-halo-8-hydroxyquinoline with formaldehyde to produce a cyclic dioxane and then contacting with concentrated hydrobromic acid to form the desired halogenated hydroxyquinoline compound.The compounds of this invention are usefual as intermediates in the production of ion-exchange resins.
    Type: Grant
    Filed: November 16, 1988
    Date of Patent: October 2, 1990
    Assignee: The Dow Chemical Company
    Inventor: Gordon C. Dunmore