Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 548/213)
  • Patent number: 4228291
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.
    Type: Grant
    Filed: October 4, 1978
    Date of Patent: October 14, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Genellin
  • Patent number: 4221584
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, haloalkyl of 1 to 2 carbon atoms and 1 to 3 of the same or different halogens selected from fluoro, chloro, bromo or iodo, nitro, hydroxy, alkoxyalkyl of 2 to 6 carbon atoms, fluoro, bromo, chloro or iodo, R.sup.2, R.sup.3 and R.sup.4 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, haloalkyl of 1 to 2 carbon atoms and 1 to 3 of the same or different halogens selected from fluoro, chloro, bromo or iodo, nitro, hydroxy, alkoxyalkyl of 2 to 6 carbon atoms, fluoro, bromo, chloro or iodo; R.sup.5 and R.sup.
    Type: Grant
    Filed: February 9, 1979
    Date of Patent: September 9, 1980
    Assignee: Chevron Research Company
    Inventor: Stephen D. Ziman
  • Patent number: 4198339
    Abstract: Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.
    Type: Grant
    Filed: June 7, 1978
    Date of Patent: April 15, 1980
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Masaru Iwanami, Tetsuya Maeda, Yoshinobu Nagano, Masaharu Fujimoto, Noriaki Nagano, Atsuki Yamazaki, Kazaharu Tamazawa, Kiyoshi Murase, Tadao Shibanuma
  • Patent number: 4197305
    Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino), N-(N'-substituted thioureido), N-(nitrometylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)ethyl)isothiour eido]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: September 11, 1978
    Date of Patent: April 8, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Patent number: 4191769
    Abstract: The compounds are N-(heterocyclomethylthioalkyl) derivatives of alkylguanidines, C-alkyl and C-aryl amidines and S-alkylisothioureas. The compounds may also have N'-lower alkyl or N'(heterocyclomethylthioalkyl) substituents. Three compounds of the invention are S-methyl-N-[2-(5-methyl-4-imidazolylmethylthio)ethyl]isothiourea, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: April 17, 1978
    Date of Patent: March 4, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • Patent number: 4180663
    Abstract: A process for the preparation of a disperse methine dye containing at least one dicyanomethylidene group comprising the steps of(A) preparing an anhydrous solution of an aldehyde formed by contacting an aromatic amine, 1,2,3,4-tetrahydroquinoline or benzomorpholine compound capable of undergoing the Vilsmeier-Haack reaction with POCl.sub.3 and a N,N-di-alkylformamide wherein the alkyl moiety is 1-4 carbon atoms;(B) subsequently adding to said solution at least one equivalent of cyanoacetamide based on the equivalents of aldehyde formed in (A), thereby forming a reaction mixture of aldehyde and in situ generated malononitrile; and(C) adjusting the pH of the solution to a point sufficient for the condensation of the aldehyde and in situ generated malononitrile to occur thereby producing a disperse methine dye.
    Type: Grant
    Filed: March 12, 1979
    Date of Patent: December 25, 1979
    Assignee: Eastman Kodak Company
    Inventor: Mark D. Frishberg
  • Patent number: 4173644
    Abstract: The compounds are dithiocarbamates and isothioureas which are histamine H.sub.2 -antagonists. Two compounds of the invention are 2-(5-methyl-4-imidazolylmethylthio)ethyl N-methyldithiocarbamate and S-[2-(5-methyl-4-imidazolyl-methylthio)ethyl]-N-cyano-N'-methylisothiourea .
    Type: Grant
    Filed: July 28, 1978
    Date of Patent: November 6, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin, Robert J. Ife
  • Patent number: 4169949
    Abstract: Isothiazolidin-3-ones of the formula ##STR1## wherein R.sup.1 is a hydrogen atom, or an alkyl, cycloalkyl, aryl, aralkyl, carbamoyl, or thiocarbamoyl group,R.sup.2 and R.sup.3 are halogen atoms or alkyl groups, andX is a halogen atom and compositions containing them are useful in controlling microorganisms, such as bacteria, fungi, algae, and the like.
    Type: Grant
    Filed: June 9, 1977
    Date of Patent: October 2, 1979
    Assignee: Rohm and Haas Company
    Inventor: Ernest D. Weiler
  • Patent number: 4169835
    Abstract: Novel isothiazoles having a 3-amino-2-OR-propoxy or - propyl substituent are disclosed. The isothiazoles have pharmaceutical activity.
    Type: Grant
    Filed: March 6, 1978
    Date of Patent: October 2, 1979
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4167575
    Abstract: Disclosed are certain novel 3-alkoxyisothiazoles. The 3-alkoxyisothiazoles and compositions containing them exhibit useful biocidal properties.
    Type: Grant
    Filed: July 26, 1977
    Date of Patent: September 11, 1979
    Assignee: Rohm and Haas Company
    Inventors: George A. Miller, Sheldon N. Lewis
  • Patent number: 4166856
    Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: March 31, 1978
    Date of Patent: September 4, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young