Patents Examined by Paul M. Coughlan, Jr.
  • Cephem compounds
    Patent number: 4463003
    Abstract: The invention relates to novel cephem compounds, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is carboxy (C.sub.1 -C.sub.6) alkyl or esterified carboxy (C.sub.1 -C.sub.6) alkyl, R.sup.2 is carboxy or esterified carboxy, and R.sup.3 is (C.sub.1 -C.sub.6) alkanoyloxy (C.sub.1 -C.sub.6) alkyl, tetrazolopyridazinylthio (C.sub.1 -C.sub.6) alkyl, tetrazolothio (C.sub.1 -C.sub.6) alkyl, or (C.sub.1 -C.sub.6) alkyl tetrazolothio (C.sub.1 -C.sub.6) alkyl, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 22, 1982
    Date of Patent: July 31, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Hideaki Yamanaka
  • Cephalosporin derivatives
    Patent number: 4463173
    Abstract: A compound of the formula I: ##STR1## in which R.sup.1 is any C-3 substituent from antibacterially-active cephalosporins; R.sup.2 is any C-4 substituent from antibacterially-active cephalosporins; R.sup.3 is H, hydroxy, amino, 1-6C alkyl, 1-6C alkanoyl, 1-6C alkoxy, 1-6C alkanoylamino or 1-6C alkylamino, phenyl(1-6C)-alkyl or phenyl, each optionally substituted by methoxy; ##STR2## is of the formula II or III: ##STR3## in which R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may have a variety of values, e.g. hydrogen, carboxy, cyano or alkyl; and the salts thereof.Manufacturing processes, pharmaceutical compositions and a method of treating a bacterial infection are also disclosed.
    Type: Grant
    Filed: December 24, 1980
    Date of Patent: July 31, 1984
    Assignee: ICI Pharma
    Inventor: Frederic H. Jung
  • Diglycidyl-pteridine compounds
    Patent number: 4463006
    Abstract: Diglycidyl-substituted pteridine compounds of the general formula: ##STR1## wherein n is the whole number 1 or 2, R.sub.2 and R.sub.2 are the same or different, and are either hydrogen, a hydrocarbon radical, or together form a 5- or 6-membered carbocyclic or heterocyclic ring; processes for their preparation; and compositions and methods for their use as cytostatic agents.
    Type: Grant
    Filed: June 23, 1982
    Date of Patent: July 31, 1984
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Hinrich Moller, Brigitte Hase, Gunther Konrad, Hans-Christoph Wilk, Ulrich Zeidler
  • Process for producing chalcogen containing compounds
    Patent number: 4462938
    Abstract: Phosgene iminium chloride has been used as a reagent in a variety of reactions to produce compounds useful in the preparation of organic conductors, inorganic complexes, and heterocyclic compounds. This reagent undergoes expedient reactions with either H.sub.2 Se or H.sub.2 S. Of particular interest is a synthetic process beginning with the production of dichalcogen carbamate by the reaction of phosgene iminium chloride with, for example, H.sub.2 Se followed by subsequent processing steps to produce tetramethyl tetraselenafulvalene.
    Type: Grant
    Filed: May 15, 1980
    Date of Patent: July 31, 1984
    Assignee: AT & T Bell Laboratories
    Inventor: Fred Wudl
  • Syn-isomers of 7-substituted-3-cephem-4-carboxylic acid esters
    Patent number: 4463002
    Abstract: This invention relates to novel cephem compounds of high antimicrobial activity comprising the syn-isomers of 7-substituted-3-cephem-4-carboxylic acid esters of the formula: ##STR1## wherein R is lower alkanoyloxy (C.sub.2 -C.sub.6)alkyl, isobutyryloxymethyl, 2-ethylbutyryloxymethyl or 3,3-dimethylbutyryloxymethyl,or salts thereof.
    Type: Grant
    Filed: May 14, 1982
    Date of Patent: July 31, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Kiyoshi Tsuji, Toshiyuki Chiba
  • 1H-1,2,3-triazol-5-ylthio ester of N-carbobenzyloxy-p-hydroxyphenylglycine
    Patent number: 4463179
    Abstract: Novel thioesters effective as acylating agents for amines or hydrazines, especially effective as active esters in synthesis of cephalosporin compounds are disclosed. The novel thioester of the present invention can be prepared by reacting a thiol or a derivative thereof with an acetic acid derivative or a reactive derivative thereof. By reacting the thioester of the present invention with a 7-aminocephalosporin derivative or a salt thereof, cephalosporin derivatives or pharmacologically acceptable salts thereof which are excellent antibiotic substances having a high antimicrobial activity can be obtained in high yield very safely.
    Type: Grant
    Filed: September 2, 1981
    Date of Patent: July 31, 1984
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Masahiro Murakami, Masateru Kobayashi, Kimiyo Yamamoto, Chisei Shibuya
  • Cephem compounds
    Patent number: 4463000
    Abstract: This invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group which may be substituted with suitable substituents(s), cyclo(lower)alkyl or cyclo(lower)alkenyl; andR.sup.3 is a thiazolio group which may be substituted with suitable substituents(s) or a pyridinio group substituted with substituent(s) selected from the group consisting of halogen, cyano, hydroxy, amino, acylamino, lower alkanoyl, hydroxycarbamoyl, alkylcarbamoyl, carboxy, protected carboxy, lower alkyl, hydroxy(lower)alkyl, sulfo(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl and hydroxyimino(lower)alkyl.
    Type: Grant
    Filed: August 19, 1981
    Date of Patent: July 31, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Tsutomu Teraji, Kazuo Sakane, Jiro Goto
  • Dibenzo(de,g)quinolines
    Patent number: 4461895
    Abstract: The present invention provides dibenzo(de,g)quinoline derivatives of the general formula: ##STR1## wherein R is an unsaturated aliphatic hydrocarbon radical containing up to 6 carbon atoms or a cycloalkylalkyl radical containing 4 to 6 carbon atoms; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for combating colds and allergies.
    Type: Grant
    Filed: May 7, 1982
    Date of Patent: July 24, 1984
    Assignee: Warner-Lambert Company
    Inventors: Edgar Fritschi, Johannes Hartenstein, Wolfgang Heidt, Gerhard Satzinger
  • Pyrrolidine 2-one derivatives
    Patent number: 4461906
    Abstract: 1-Substituted-2-pyrrolidinones of the formula ##STR1## wherein one of R.sup.1, R.sup.2 and R.sup.3 represents hydroxy and the remaining substituents represent hydrogen,are capable of counteracting cerebral insufficiency produced experimentally in animal tests. They can be used therapeutically in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. They can be manufactured from novel intermediates and can be processed to provide medicaments.
    Type: Grant
    Filed: July 28, 1980
    Date of Patent: July 24, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Emilio Kyburz
  • Iminothiazolyl ureido cephalosporins
    Patent number: 4461767
    Abstract: Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, ##STR2## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, ##STR3## or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2 ; R.sub.6 is hydrogen, sodium, or potassium; n is an integer from 1 to 4; are disclosed. These compounds are useful as anti-bacterial agents.
    Type: Grant
    Filed: June 6, 1979
    Date of Patent: July 24, 1984
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner, Theodor Denzel
  • 1-[Acylthio) and (mercapto)-1-oxoalkyl]-1,2,3,4-tetrahydroquinoline-2-carboxylic acids
    Patent number: 4461896
    Abstract: A series of 1-[acylthio) and (mercapto)-1-oxoalkyl]-1,2,3,4-tetrahydroquinoline-2-carboxylic acids and salts thereof are useful as Angiotensin I converting enzyme inhibitors.
    Type: Grant
    Filed: November 2, 1979
    Date of Patent: July 24, 1984
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventor: David E. Portlock
  • Diglycidyl substituted heterocyclic compounds
    Patent number: 4460590
    Abstract: Diclycidyl substituted heterocyclic compounds of the formula: ##STR1## wherein X and Y can be the same or different and are either nitrogen or the radical C-R, where R is a hydrogen, or a hydrocarbon group, e.g., a straight or branched chain saturated or unsaturated hydrocarbon group, a substituted or unsubstituted cycloaliphatic group, an aromatic hydrocarbon-substituted alkyl group, a cycloaliphatic hydrocarbon-substituted alkyl group, an aromatic hydrocarbon group, a heterocyclic group, or a hetero-cyclic-substituted alkyl group, and where the glycidyl group in the five-membered ring is attached to a ring nitrogen atom; processes for their preparation; and compositions and methods for their use as cytostatic agents.
    Type: Grant
    Filed: June 23, 1982
    Date of Patent: July 17, 1984
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventor: Hinrich Moller
  • 3-Carboxybenzyl cephems
    Patent number: 4460582
    Abstract: The present invention provides a compound of the formula (I): ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof wherein R.sup.1 is carboxy, R.sup.2 is hydrogen or carboxy, R.sup.3 is hydrogen, acyl, C.sub.1-6 akyl or C.sub.2-6 alkenyl, any of such R.sup.3 groups being optionally substituted, and R.sup.4 is an amino or protected amino group.Processes for the preparation of these compounds are described as is their use in the treatment of bacterial infection.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: July 17, 1984
    Assignee: Beecham Group P.L.C.
    Inventor: John H. C. Nayler
  • 2-Ethoxymethyl and 2-methoxymethyl N-(3,5-dichlorophenyl) succinamides
    Patent number: 4460782
    Abstract: The invention relates to a selection of succinic acid imides that have, in the 2-position, alkoxy, alkoxyalkyl or acyloxy substituents having up to 4 carbon atoms and the imine components of which are derived from aliphatic amines having up to 5 carbon atoms or from aniline optionally having up to 2 substituents. The succinic acid imides according to the invention are used as fungicides. A method for their manufacture is also disclosed.
    Type: Grant
    Filed: July 24, 1981
    Date of Patent: July 17, 1984
    Assignee: Consortium fur Elektrochemische Industrie GmbH
    Inventors: Norman Haberle, Otto Eberle
  • 6-[N-(.omega.-Carboxyalkyl)amino]-1,3-dimethyl-5-formamidouracils
    Patent number: 4460772
    Abstract: Intermediates in the preparation of 9-position derivatives of theophylline useful in synthesizing theophylline immunogens and labeled conjugates. The labeled conjugates and the antibodies produced against the immunogens are particularly useful in homogeneous nonradioisotopic immunoassay for measuring theophylline in biological fluids such as serum.
    Type: Grant
    Filed: May 11, 1983
    Date of Patent: July 17, 1984
    Assignee: Miles Laboratories, Inc.
    Inventors: Jeffrey L. Benovic, Robert T. Buckler, John F. Burd, Thomas M. Li
  • Amides of retinoic acids with 5-amino tetrazole
    Patent number: 4459404
    Abstract: 5-Amino-tetrazole derivatives of retinoic acids and their physiologically tolerated salts, processes for their preparation and pharmaceutical formulations which contain these derivatives and salts and which may, in particular, be used in the treatment of dermatoses.
    Type: Grant
    Filed: November 16, 1981
    Date of Patent: July 10, 1984
    Assignee: BASF Aktiengesellschaft
    Inventors: Fritz-Frieder Frickel, Axel Nuerrenbach
  • Process for the preparation of 2,3-quinolinedicarboxylic acids
    Patent number: 4459409
    Abstract: There is provided a novel process for the preparation of a substituted or unsubstituted 2,3-quinolinedicarboxylic acid, utilizing as the starting material, 2-methyl-3-quinolinecarboxylic acid or 3-methyl-2-quinolinecarboxylic acid or the alkyl ester of either of the above compounds.
    Type: Grant
    Filed: May 25, 1982
    Date of Patent: July 10, 1984
    Assignee: American Cyanamid Company
    Inventor: David W. Ladner
  • Process for the preparation of 2-(5-isopropyl-5-methyl-4-oxo-2-imidazolin-2-yl)-3-quinoline-carboxylic acid and alkyl 2-trichloromethyl-3-quinoline-carboxylate intermediates therefor
    Patent number: 4459408
    Abstract: The invention is related to a novel process for the prepartion of 2-(5-isopropyl-5-methyl-4-oxo-2-imidazolin-2-yl)-3-quinolinecarboxylic acid, a useful and valuable herbicide.
    Type: Grant
    Filed: May 25, 1982
    Date of Patent: July 10, 1984
    Assignee: American Cyanamid Company
    Inventors: Donald R. Maulding, Robert F. Doehner, Jr.
  • Desacetylcephalosporin sulfones
    Patent number: 4459405
    Abstract: 7-(S)-Acylamino-3-hydroxymethyl-3-cephem sulfones are disclosed. These compounds are intermediates in the synthesis of 1-oxa .beta.-lactam antibiotics.
    Type: Grant
    Filed: November 16, 1982
    Date of Patent: July 10, 1984
    Assignee: Eli Lilly and Company
    Inventor: David A. Hall
  • Process for the preparation of 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indoleacetoxyacetic acid
    Patent number: 4459415
    Abstract: The invention relates to a process for the preparation of the known 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indoleacetoxyacetic acid which comprises reacting an indolecarboxylic acid ester of Formula (II) or its derivative with an alcohol of Formula (III). The final product is known to have antiinflammatory activity.
    Type: Grant
    Filed: February 25, 1983
    Date of Patent: July 10, 1984
    Assignee: Troponwerke GmbH & Co. KG
    Inventor: Karl-Heinz Boltze