Patents Examined by Paul M. Coughlan, Jr.
  • Patent number: 4548818
    Abstract: Compounds having activity against chronic obstructive airway disease or cardiac disease, characterized by the formula ##STR1## wherein R.sup.1 is n-propyl, n-butyl, isobutyl, n-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexylmethyl, and R.sup.2 is hydrogen or methyl, provided that R.sup.2 is methyl when R.sup.1 is n-propyl, n-butyl or isobutyl, or a physiologically acceptable salt thereof.
    Type: Grant
    Filed: November 23, 1981
    Date of Patent: October 22, 1985
    Inventors: Per G. Kjellin, Carl G. A. Persson
  • Patent number: 4520194
    Abstract: A 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporin derivative of the formula; ##STR1## wherein R.sub.3 is hydrogen or a residue of a nucleophilic compound; R.sub.2 NH is an amino group which may optionally be protected, pharmaceutically acceptable salt or ester thereof, is found to have excellent anti-bacterial activity against a broad spectrum of bacteria inclusive of gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae and Citrobacter freundii. Thus, this compound may be used for an antibacterial agent in therapeutical purposes.
    Type: Grant
    Filed: July 6, 1978
    Date of Patent: May 28, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
  • Patent number: 4518754
    Abstract: Novel imido copolymers are prepared by copolymerizing:[i] a bis-maleimide of the structural formula: ##STR1## [ii] an olefinically unsaturated comonomer copolymerizable therewith. The subject copolymers are applicable to the production of a variety of useful shaped articles, coatings, laminates, foams, and the like.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: May 21, 1985
    Assignee: Rhone-Poulenc Industries
    Inventors: Jean L. Locatelli, Bernard Rollet
  • Patent number: 4518755
    Abstract: Novel imido copolymers are prepared by copolymerizing:[i] a bis-maleimide of the structural formula: ##STR1## with [ii] a (meth)acrylic acid amide.The subject copolymers are applicable to the production of a variety of useful shaped articles, coatings, laminates, foams, and the like.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: May 21, 1985
    Assignee: Rhone-Poulenc Industries
    Inventors: Jean L. Locatelli, Bernard Rollet
  • Patent number: 4517361
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula -NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula -SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.
    Type: Grant
    Filed: March 31, 1983
    Date of Patent: May 14, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuo Numata, Isao Minamida, Masayoshi Yamaoka, Mitsuru Shiraishi, Toshio Miyawaki
  • Patent number: 4515945
    Abstract: N-alkyl-4-(4-pyridinyl)isatoic anhydrides are prepared by alkylating a 4-(4-pyridinyl)isatoic anhydride, suitably in the presence of sodium hydride and N,N-dimethylformamide. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.
    Type: Grant
    Filed: August 15, 1983
    Date of Patent: May 7, 1985
    Assignee: Ethyl Corporation
    Inventors: Paul F. Ranken, Thomas J. Walter
  • Patent number: 4515789
    Abstract: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.
    Type: Grant
    Filed: April 7, 1983
    Date of Patent: May 7, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl G. Metzger, Wilfried Schrock, Dieter Habich, Paul Naab, Hans-Joachim Zeiler
  • Patent number: 4515956
    Abstract: A process has been discovered for selective preparation of isomers and enantiomers of 2,2-dimethyl-3-(2,2-dihalovinyl)cyclopropane carboxylic acids. In this process an adduct of an alkyl 3,3-dimethyl-4-pentenoate and a substituted 2-oxazolidone is reacted with a substituted dihalomethane compound. The resulting compound is cyclized, dehydrohalogenated and hydrolyzed to yield the desired product. These cyclopropane carboxylic acids are useful precursors for pyrethroid insecticides.
    Type: Grant
    Filed: August 13, 1984
    Date of Patent: May 7, 1985
    Assignee: The Dow Chemical Company
    Inventor: William A. Kleschick
  • Patent number: 4515788
    Abstract: This invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen or lower alkyl, andR.sup.4 is lower alkyl, lower alkoxy, acyloxymethyl, lower alkylthiomethyl, lower alkoxymethyl, halogen, lower alkenyl or hydrogen,and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 27, 1982
    Date of Patent: May 7, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Hideaki Yamanaka
  • Patent number: 4515795
    Abstract: A pharmaceutical composition containing as an essential ingredient a compound of the formula ##STR1## wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is an .omega.- or (.omega.-1)-hydroxyalkyl group having from 5 to 8 carbon atoms in which the hydroxy group is separated from the xanthine nucleus by at least 2 carbon atoms, radicals R.sub.1 and R.sub.3 which are no hydroxyalkyl group, are hydrogen or methyl and equal or different, and R.sub.2 is said hydroxyalkyl group or methyl, a compound of formula (I) and a pharmaceutical product for treatment of diseases involving insufficiency of cerebral blood flow.
    Type: Grant
    Filed: March 4, 1977
    Date of Patent: May 7, 1985
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Joachim Hinze, Alfons Soder, Kurt Popendiker
  • Patent number: 4514403
    Abstract: A hydrouracil compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein A represents --CH.dbd.CH--CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, and R represents hydrogen or methyl. Such compounds are useful as analgesics.
    Type: Grant
    Filed: September 17, 1981
    Date of Patent: April 30, 1985
    Assignee: Yoshitomi Pharmaceutical Industries Ltd.
    Inventors: Chiaki Tashiro, Takeshi Kawakita, Ichiro Horii, Koretake Anami
  • Patent number: 4509972
    Abstract: Compounds of the formula ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types, and salts thereof. The compounds as well as their salts are useful as herbicides.
    Type: Grant
    Filed: March 28, 1983
    Date of Patent: April 9, 1985
    Assignee: Celamerck GmbH & Co. KG
    Inventors: Rudolf Mengel, Ludwig Schroder, Werner Stransky, Gerbert Linden, Gerhart Schneider, Sigmund Lust
  • Patent number: 4510138
    Abstract: An antibacterial composition is provided consisting of a 7-[2-(2-aminothiazol)-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporin compound of the formula ##STR1## wherein R.sub.2 NH is amino or a protected amino group, n is an integer of 1 to 3 and R is a di-C.sub.1-3 alkylamino, carboxyl or sulfo group, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: April 9, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
  • Patent number: 4507299
    Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;R is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.1-3 alkyl substituted amino; heteroaryl; formyl C.sub.2-4 alkenyl; or C.sub.2-4 alkenyl; andR.sup.2 is straight or branched C.sub.
    Type: Grant
    Filed: December 27, 1982
    Date of Patent: March 26, 1985
    Assignee: Merck & Co., Inc.
    Inventor: David B. R. Johnston
  • Patent number: 4507298
    Abstract: The invention relates to new 6-{4-(.omega.-(1-imidazolyl)-alkyl)-phenyl}-3-oxo-2,3,4,5-tetrahydro-pyrid azines having the general formula I ##STR1## and acid addition salts thereof, and to a process for the treatment of inflammatory, atherosclerotic and thromboembolic diseases especially in humans.
    Type: Grant
    Filed: July 12, 1982
    Date of Patent: March 26, 1985
    Assignee: A. Nattermann & Cie GmbH
    Inventors: Hans-Heiner Lautenschlager, Gerd Hilboll, Hugo Friehe, Josef P. Lohr
  • Patent number: 4507293
    Abstract: The invention relates to novel cephem compounds, of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 15, 1983
    Date of Patent: March 26, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Toshiyuki Chiba, Kiyoshi Tsuji
  • Patent number: 4506076
    Abstract: The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5, --NHCO--R.sup.5, or ##STR2## R.sup.5 is aryl or heterocyclic, either of which may be substituted, R.sup.6 is hydrogen or lower alkyl, andA is lower alkylene, or a salt thereof.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: March 19, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
  • Patent number: 4504481
    Abstract: The invention relates to new benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: March 12, 1985
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Edit Toth, Jozsef Torley, Eva Palosi, Szabolcs Szeberenyi, Laszlo Szporny, Sandor Gorog, Istvan Hajdu
  • Patent number: 4504478
    Abstract: An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X.sup.1 is sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is hydrogen, 1-6C alkoxy or 1-6C alkylthio; X.sup.2 is nitrogen or a radical N.sup..sym. R.sup.5 ; R.sup.4 and R.sup.5 are a variety of radicals described in the specification; --A-- is of the formula II or III: ##STR2## in which R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a variety of substituents described in the specification; and the pharmaceutically-acceptable acid- and base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.
    Type: Grant
    Filed: September 7, 1982
    Date of Patent: March 12, 1985
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Frederic H. Jung, Gareth M. Davies
  • Patent number: 4503221
    Abstract: The process for preparing cephalosporanic acid derivatives ##STR1## and salts thereof with bases as well as solvates thereof, comprising reacting a compound of the formula II: ##STR2## wherein R.sub.3 represents hydrogen or an amino protecting group and R.sub.2 represents hydrogen, an easily removable ester group or other carboxyl protecting group, with a compound of formula IIIa, ##STR3## wherein R.sub.1 represents hydrogen, an easily removable ester group or other carboxyl protecting group, and R.sub.4 is a 2-benzothiazol group and salts thereof with bases, and if required removing any ester group or protecting group.
    Type: Grant
    Filed: June 20, 1983
    Date of Patent: March 5, 1985
    Assignee: Sandoz Ltd.
    Inventors: Hans Fliri, Helmut Hamberger