Patents Examined by David E. Wheeler
  • Patent number: 4143041
    Abstract: 4'-Deoxyvincristine, 4'-deoxy-1-formylleurosidine and the corresponding 4-desacetyl derivatives, useful in inhibiting the growth of experimental tumors.
    Type: Grant
    Filed: November 25, 1977
    Date of Patent: March 6, 1979
    Assignee: Eli Lilly and Company
    Inventor: Gerald L. Thompson
  • Patent number: 4142045
    Abstract: Carbamoylalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed.
    Type: Grant
    Filed: February 10, 1978
    Date of Patent: February 27, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 4140688
    Abstract: A new compound with a nucleus containing a benzo-fused carbocyclic .beta.-lactam system is disclosed. The compound has antibacterial activity against B. subtilis.
    Type: Grant
    Filed: April 3, 1978
    Date of Patent: February 20, 1979
    Assignee: SmithKline Corporation
    Inventor: Carl D. Perchonock
  • Patent number: 4139533
    Abstract: A series of 5-endo-(quinoline-carbonyloxy)-,(benzothiophene-carbonyloxy)- and (quinoxaline-carbonyloxy)-N[amino-(lower)alkyl]bicyclo[2.2.1]-heptane-2,3- di-endo-carboxylic acid imides has been found to possess excellent prophylactic and therapeutic activity as anti-arrhythmic agents.
    Type: Grant
    Filed: August 19, 1976
    Date of Patent: February 13, 1979
    Assignee: Bristol-Myers Company
    Inventors: Ronald L. Buchanan, John T. Woolever, Alex M. Jelenevsky
  • Patent number: 4139703
    Abstract: New indole derivatives of cephalosporin compounds have been prepared which are useful as antibiotics.
    Type: Grant
    Filed: December 8, 1977
    Date of Patent: February 13, 1979
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Abraham Nudelman, Abraham Patchornik
  • Patent number: 4138490
    Abstract: Novel 1,2-dihydro-2-oxoquinol-4-ylalkanoic acid derivatives bearing a variety of substituents on the quinoline nucleus but including, at position 1, an aromatic radical linked directly or through a C.sub.1-4 -alkylene or a C.sub.2-4 -alkenylene radical. Representative compounds of the invention are 1-(3,4-dichlorobenzyl)-3-methyl-1,2-dihydro-2-oxoquinol-4-ylacetic acid and .alpha.-(1-benzyl-1,2-dihydro-2-oxoquinol-4-yl)propionic acid. The compounds possess anti-inflammatory or analgesic properties, or are inhibitors of the enzyme aldose reductase.
    Type: Grant
    Filed: September 12, 1977
    Date of Patent: February 6, 1979
    Assignee: Imperial Chemical Industries Limited
    Inventors: David R. Brittain, Edward D. Brown, Walter Hepworth, Gilbert J. Stacey
  • Patent number: 4138401
    Abstract: 2-Keto-6,7,8,9-tetrahydro-2H-pyrano(3,2-g)-quinoline and 2-keto-9-methyl-,8,9-tetrahydro-2H-pyrano(3,2-g)-quinoline, compounds useful as laser dyes, are prepared from 7-hydroxy-1,2,3,4-tetrahydroquinoline.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: February 6, 1979
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Peter R. Hammond, Erhard J. Schimitschek, John A. Trias
  • Patent number: 4138554
    Abstract: 7-[D-.alpha.-(4-hydroxy-1,5-naphthyridine-3-carboxyamido)-.alpha.-phenyl (and p-hydroxyphenyl) acetamido]-3-carbamoyloxymethyl-3-cephem-4-carboxylic acids were synthesized and found to have potent antibacterial activity in vitro especially against many strains of Pseudomonas aeruginosa.
    Type: Grant
    Filed: June 9, 1977
    Date of Patent: February 6, 1979
    Assignee: Bristol-Myers Company
    Inventors: Takayuki Naito, Jun Okumura, Masahisa Oka
  • Patent number: 4137408
    Abstract: Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
    Type: Grant
    Filed: October 27, 1977
    Date of Patent: January 30, 1979
    Assignee: Warner-Lambert
    Inventors: James S. Kaltenbronn, Theodore H. Haskell, Leonard Doub
  • Patent number: 4137312
    Abstract: A series of novel 7-(D-.alpha.-acylaminoarylacetamido)-.DELTA..sup.3 -cephem derivatives have been prepared wherein the acyl moiety contains an epoxy group immediately adjacent to the carbonyl carbon atom. These compounds are useful as antibacterial agents for the treatment of diseases caused by Gram-negative and Gram-positive bacteria. Preferred members include 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]-3-(1-meth yl-1,2,3,4-tetrazol-5-ylthiomethyl)-.alpha..sup.3 -cephem-4-carboxylic acid and 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]cephalospo ranic acid. Alternate methods of preparation are provided for these compounds and the principal synthetic route is described in detail.
    Type: Grant
    Filed: October 3, 1977
    Date of Patent: January 30, 1979
    Assignee: Pfizer Inc.
    Inventors: Barry C. Ross, Braham Shroot
  • Patent number: 4133813
    Abstract: Cyclic nitrile carbonate-containing compounds having the structural formula: ##STR1## wherein T is O, S, or NR"'; R and R' are organic radicals; R" is hydrogen, halogen or an organic radical and R"' is hydrogen or an organic radical are prepared by reacting a cyclic nitrile carbonate-containing chloroformate having the structural formula: ##STR2## with a nucleophilic compound having the structural formula: ##STR3## wherein T, R, R', R" and R"' are as defined above, under conditions such that the TH group will react with the chloroformate group, but no reaction will occur involving either the cyclic nitrile carbonate group or the ##STR4## group. The novel compounds of the invention are useful in the preparation of crosslinkable polymers.
    Type: Grant
    Filed: October 6, 1976
    Date of Patent: January 9, 1979
    Assignee: Atlantic Richfield Company
    Inventors: Karl E. Fuger, Ming N. Sheng
  • Patent number: 4133882
    Abstract: Cephalosporin compounds substituted in the 7-position with a hydroxy-halo substituted .alpha.-aminophenylacetamido group and in the 3-position with a heterocyclicthiomethyl group are prepared by 7-acylation. The products are antibacterial agents.
    Type: Grant
    Filed: June 28, 1976
    Date of Patent: January 9, 1979
    Assignee: SmithKline Corporation
    Inventors: George L. Dunn, John R. E. Hoover
  • Patent number: 4129730
    Abstract: Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinylcarbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds.
    Type: Grant
    Filed: January 13, 1977
    Date of Patent: December 12, 1978
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Isamu Saikawa, Shuntaro Takano, Hiroyuki Imaizumi, Isamu Takakura, Hirokazu Ochiai, Takashi Yasuda, Hideo Taki, Masaru Tai, Yutaka Kodama
  • Patent number: 4128724
    Abstract: New .alpha.-hydrazinocarbonylamino cephalosporins which have the formula ##STR1## are useful as antimicrobial agents.
    Type: Grant
    Filed: January 12, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 4128714
    Abstract: A novel ester of 7-acylamido-3-methyl-cepham-4-carboxylic acid derivative and a process for the preparation thereof which comprises reacting penicillin sulfoxide ester with the metal halide, and a novel 7-acylamido-3-methyl-cepham-4-carboxylic acid derivative and a process for the preparation thereof which comprises reacting penicillin sulfoxide ester with the metal halide and decomposing the resultant in a reductive atmosphere.
    Type: Grant
    Filed: February 2, 1976
    Date of Patent: December 5, 1978
    Assignee: Meiji Seika Kaisha Ltd.
    Inventors: Masao Koyama, Shigeo Seki
  • Patent number: 4128723
    Abstract: Cyanoalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene or ##STR3## R.sub.2 is phenyl, 2-thienyl, or 3-thienyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.
    Type: Grant
    Filed: March 6, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 4128650
    Abstract: Compounds of the formula: ##STR1## wherein the symbols X each represent hydrogen or methoxy, R represents hydrogen or carboxymethyl, the symbols R.sub.1 each represent hydrogen or together represent a valency bond and the symbols R.sub.2 each represent hydrogen or together represent a valency bond, the pair of symbols R.sub.2 having the same significance as the pair of symbols R.sub.1, and when the symbols R.sub.1 and R.sub.2 represent hydrogen the symbol X also represents hydrogen, are new compounds possessing antiviral activity.
    Type: Grant
    Filed: May 18, 1977
    Date of Patent: December 5, 1978
    Assignee: Rhone-Poulenc Industries
    Inventors: Jean-Louis Fabre, Daniel Farge, Claude James
  • Patent number: 4127585
    Abstract: This invention relates to novel amides of 4-hydroxy-6H-thieno[2,3-b]thiopyran-5-carboxylic acid-7,7-dioxide having the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; Ar is aryl or heterocyclic; to the pharmaceutically acceptable salts thereof; and to processes for their preparation. The compounds of this invention exhibit antiinflammatory activity.
    Type: Grant
    Filed: December 27, 1977
    Date of Patent: November 28, 1978
    Assignee: Warner-Lambert Company
    Inventors: Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
  • Patent number: 4126617
    Abstract: Novel chemical compounds of the formula: ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, phenyl, alkali metal, or an amine cation;X and Y can be the same or different and are selected from the group consisting of hydrogen, alkyl or from one to six carbon atoms, inclusive, cycloalkyl of 5 or 6 carbon atoms, inclusive, phenyl, hydroxyl, alkoxy having from one to three carbon atoms, inclusive, halogen, trifluoromethyl, cyano, carboxyamide and ##STR2## where Q is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, alkali metal, and an amine cation, with the proviso that whereR is hydrogen, alkali metal or an amine cation, then Q is the same as R, and whereR is phenyl or alkyl from one to three carbon atoms, then Q is phenyl or alkyl from one to three carbon atoms; andZ is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, and phenyl.
    Type: Grant
    Filed: August 5, 1976
    Date of Patent: November 21, 1978
    Assignee: The Upjohn Company
    Inventors: Charles M. Hall, Herbert G. Johnson, John B. Wright
  • Patent number: 4126616
    Abstract: N-Propylnorapomorphine dialkanoate, dibenzoate and dicyclopropanecarboxylate esters and acid-addition salts thereof, having anti-parkinson activity, are prepared by reaction of N-propylnorapomorphine with a respective alkanoyl, benzoyl or cyclopropanecarbonyl halide or corresponding acid anhydride in the presence of an acid acceptor.
    Type: Grant
    Filed: December 13, 1976
    Date of Patent: November 21, 1978
    Assignee: William B. Hinshaw
    Inventors: William Banks Hinshaw, Jack Pearl