Patents Examined by David E. Wheeler
  • Patent number: 4010176
    Abstract: Novel substituted nitroimidazoles are provided, for example, 2-(4,5-substituted-isoxazol-3-yl)-1-substituted-5-nitroimidazole; 2-(4,5-disubstituted-.DELTA..sup.2 -isoxazolin-3-yl)-1-substituted-5-nitroimidazole; or 2-(4,5-disubstituted-2-loweralkyl-isoxazolidin-3-yl)-1-substituted-5-nitro imidazole. These compounds have antibacterial and antiprotozoal activity, especially against human and animal trypanosomiasis and trichomoniasis.
    Type: Grant
    Filed: July 30, 1975
    Date of Patent: March 1, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Peter Kulsa, Clarence S. Rooney
  • Patent number: 4010270
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, alkyl of 1 to 4 carbon atoms, phenyl, hydroxyl, alkoxy of 1 to 3 carbon atoms, alkylmercapto of 1 to 3 carbon atoms, hydroxycarbonyl or ##STR2## where R.sub.3 and R.sub.4 are each alkyl of 1 to 4 carbon atoms or, together with each other and the nitrogen atom to which they are attached, morpholino, piperidino, methylpiperidino or phenyl-piperidino; orR.sub.1 and R.sub.2, together with each other and adjacent carbon atoms of the benzene ring to which they are attached, --CH=CH--CH=CH--, --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --O--CH.sub.2 --O--;and salts thereof. The compounds are useful as antiallergics.
    Type: Grant
    Filed: September 23, 1975
    Date of Patent: March 1, 1977
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Friedrich Karl Hess, Patrick Brian Stewart
  • Patent number: 4009273
    Abstract: Racemates and optically active isomers of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, lower alkyl optionally substituted with a member of the group consisting of hydroxy and halogen, lower alkenyl, lower alkynyl, --(CH.sub.2).sub.n -- COCH.sub.3 where n is 0 or 1, ##STR2## wherein X is selected from the group consisting of lower alkyl and optionally substituted phenyl, aralkyl or 7 to 8 carbon atoms, acyl of an organic carboxylic acid of 1 to 6 carbon atoms optionally substituted with ##STR3## where m is an integer from 0 to 6 and X.sub.1 is selected from the group consisting of hydrogen and lower alkyl, ##STR4## where p is an integer from 1 to 6 and X.sub.1 is as before and ##STR5## wherein X.sub.2 is lower alkyl and R.sub.1 and R.sub.
    Type: Grant
    Filed: April 14, 1975
    Date of Patent: February 22, 1977
    Assignee: Roussel-UCLAF
    Inventors: Lucien Nedelec, Daniel Frechet
  • Patent number: 4009169
    Abstract: The invention relates to novel 5,6,7,8-tetrahydroquinoline derivatives which have a group X situated at the 8-position said group X is CONHR.sup.3, or CO.sub.2 R.sup.5 wherein R.sup.3 is hydrogen lower alkyl and R.sup.5 is hydrogen, lower alkyl or a lower aralkyl radical.The compounds are intermediates for corresponding compounds where X is CSNHR.sup.3 and these are anti-ulcer agents.
    Type: Grant
    Filed: October 20, 1975
    Date of Patent: February 22, 1977
    Assignee: John Wyeth & Brother Limited
    Inventors: Adrian Charles Ward Curran, Roger Crossley, David George Hill
  • Patent number: 4008237
    Abstract: Novel antibacterial agents consisting of a 2,3,5,8-tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid of the formula: ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, a process for producing the derivatives and pharmaceutical compositions containing the same. The above-identified derivatives possess antibacterial activity against gram-negative bacteria at test concentration levels of about 0.0001 to 1.0 mg/cc.
    Type: Grant
    Filed: October 28, 1975
    Date of Patent: February 15, 1977
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hideo Agui, Iwao Nakatsuka, Toru Mitani, Mitsuo Nakashita, Takenari Nakagome, Toshiaki Komatsu, Akio Izawa, Yasuko Eda
  • Patent number: 4008245
    Abstract: 7-Substituted imidazo[2,1-b]thiazolium and 9-substituted thiazolo-[3,2-a]benzimidazolium salts as blood-sugar lowering agents and growth promotants.
    Type: Grant
    Filed: July 8, 1975
    Date of Patent: February 15, 1977
    Assignee: Pfizer Inc.
    Inventors: Richard M. Acheson, John K. Stubbs, Charles A. R. Baxter, Donald E. Kuhla
  • Patent number: 4008244
    Abstract: Oxazolidine and thiazolidine carbodithioates of sodium, potassium and specified alkyl substituted ammonium which are useful as vulcanization accelerators for EPDM elastomers while demonstrating non-blooming characteristics.
    Type: Grant
    Filed: August 15, 1975
    Date of Patent: February 15, 1977
    Assignee: Pennwalt Corporation
    Inventors: Ivan Christoff Popoff, Paul Gordon Haines
  • Patent number: 4008243
    Abstract: Certain thiazolinyl or thiazinyl benzimidazole ester compounds are useful as antiviral agents.
    Type: Grant
    Filed: November 19, 1975
    Date of Patent: February 15, 1977
    Assignee: Eli Lilly and Company
    Inventors: James H. Wikel, Charles J. Paget
  • Patent number: 4007188
    Abstract: Disclosed are disperse dyes of formula I, ##STR1## in which X signifies O or NH, either R.sub.1 and R.sub.2 each signify an alkyl or phenyl radical,Or R.sub.1 is as defined above, and R.sub.2 is hydrogen,Or R.sub.1 and R.sub.2, together with the nitrogen atom, signify a heterocyclic ringR.sub.3 signifies acyl, alkyl, phenyl or a heterocyclic, andR.sub.4 signifies a chain forming a carbocyclic or heterocyclic ring of aromatic character.
    Type: Grant
    Filed: November 25, 1974
    Date of Patent: February 8, 1977
    Assignee: Sandoz Ltd.
    Inventor: Werner Koch
  • Patent number: 4007275
    Abstract: N-(7- or 8-substituted-quinolyl-4)-anthranilates of the formula ##STR1## wherein X in the 7 or 8 position is trihalomethylthio, Z is --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.p --, n is a whole number from 2 to 6, m and p are whole numbers from 2 to 3 and Y.sub.1 and Y.sub.2 are alkyl having 1 to 6 carbon atoms, as well as their non-toxic, pharmaceutically acceptable acid addition salts having analgesic and anti-inflammatory activity and their preparation.
    Type: Grant
    Filed: December 10, 1975
    Date of Patent: February 8, 1977
    Assignee: Roussel-UCLAF
    Inventors: Anne Farthouat, Jean Meier
  • Patent number: 4007173
    Abstract: Cephalosporins with a .alpha.-amino-(ureidophenyl)acetamido substituent at position 7 are prepared by acylation of a 7-aminocephalosporin with a derivative of .alpha.-amino-p(or m)-ureidophenylacetic acid. These compounds are antibacterial agents.
    Type: Grant
    Filed: May 7, 1973
    Date of Patent: February 8, 1977
    Assignee: SmithKline Corporation
    Inventors: John Russel Eugene Hoover, Jerry Arnold Weisbach
  • Patent number: 4007178
    Abstract: A method for O-acylating the 3-hydroxymethyl group of 7-acylaminocephalosporadesic acids by reaction with an azolide and new O-acyl-7-acylaminocephalosporadesic acids in which the O-acyl group is derived from an alkoxyalkanoic acid or an amino acid.
    Type: Grant
    Filed: May 15, 1975
    Date of Patent: February 8, 1977
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Patent number: 4006230
    Abstract: Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4.sup.' wherein R.sup.4.sup.' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.
    Type: Grant
    Filed: November 26, 1975
    Date of Patent: February 1, 1977
    Assignee: Pfizer Inc.
    Inventors: David A. Cox, Braham Shroot
  • Patent number: 4006156
    Abstract: Novel insecticidal 3-alkyl-2-(nitromethylene)-thiazolidines.
    Type: Grant
    Filed: June 27, 1975
    Date of Patent: February 1, 1977
    Assignee: Shell Oil Company
    Inventor: James E. Powell
  • Patent number: 4005092
    Abstract: A class of pyrylium dyes, having at least one rigidized, nitrogen-containing heterocyclic ring fused thereto is described. The rigidized dyes are useful lasing components in lasing media.
    Type: Grant
    Filed: October 29, 1975
    Date of Patent: January 25, 1977
    Assignee: Eastman Kodak Company
    Inventor: George A. Reynolds
  • Patent number: 4003912
    Abstract: The Dicarboximido-N-Monosubstituted Carbamates of this invention are pesticidally active and particularly useful as herbicides.
    Type: Grant
    Filed: March 21, 1975
    Date of Patent: January 18, 1977
    Assignee: Monsanto Company
    Inventor: John E. Franz
  • Patent number: 4003894
    Abstract: Process for the preparation of 7-substituted amino-desacetoxycephalosporanic derivatives comprising converting a 6-substituted amino-penicillanic acid sulfoxide into an anhydride of a 6-substituted amino-penicillanic acid sulfoxide, heating the said acid anhydride intermediate at a temperature up to at most 160.degree. C in a dry inert organic solvent with an anhydrous acid which is capable of causing ring expansion of the penam ring to a .DELTA..sup.3 -cephem ring, in the presence of a silicon-containing compound capable of (a) removing water formed during the ring enlargement of the penam structure fast enough to prevent water hydrolysis of the acid anhydride moiety present and (b) forming neutral or basic products on hydrolysis, the aforesaid acid being strong enough not to be, or not to a substantial extent to be, silylated under the reaction conditions employed, and hydrolyzing the resulting compound in situ to form the .DELTA..sup.
    Type: Grant
    Filed: May 5, 1975
    Date of Patent: January 18, 1977
    Assignee: Gist-Brocades N.V.
    Inventors: Jan Verweij, Hong Sheng Tan, Hermanus Jacobus Kooreman
  • Patent number: 4003913
    Abstract: Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[3,4-b]indole or thiopyrano[3,4-b]indole nucleus or having said radical attached to the 1 position of a pyrano[4,3-b]indole or thiopyrano[4,3-b]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3,4,5,6,7,8, and 9.
    Type: Grant
    Filed: March 5, 1975
    Date of Patent: January 18, 1977
    Assignee: Ayerst McKenna and Harrison Ltd.
    Inventors: Christopher A. Demerson, Lesie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
  • Patent number: 4002631
    Abstract: A lactone compound represented by the following formula ##STR1## or ##STR2## or a mixture thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined hereinafter and a process for preparing the same are disclosed.
    Type: Grant
    Filed: July 24, 1974
    Date of Patent: January 11, 1977
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Yoshihide Miyazawa, Minoru Ozutsumi, Satoshi Ogawa
  • Patent number: RE29119
    Abstract: 7-Aminopyridiniumacetylamino-cephalosporanic acids and derivatives thereof. The new compounds have antibacterial properties.
    Type: Grant
    Filed: September 18, 1975
    Date of Patent: January 18, 1977
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Bickel, Johannes Muller, Rolf Bosshardt, deceased, Heinrich Peter, Bruno Fechtig