Chalcogens Bonded Directly To At Least Two Ring Carbons Of The Six-membered Hetero Ring Patents (Class 514/348)
  • Patent number: 4659725
    Abstract: Pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: June 19, 1986
    Date of Patent: April 21, 1987
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Robert J. Ife
  • Patent number: 4659736
    Abstract: A method of combating slugs and snails comprising applying to a plant or to an area from which it is desired to exclude such slugs and snails a repellent amount of at least one benzoyl urea of the formula ##STR1## in which R, R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkoxy or halogen,R.sup.3 and R.sup.4 each independently is hydrogen, alkyl, aralkyl, aryl, alkoxy, aralkoxy, aryloxy, alkylthio, aralkylthio or arylthio,A is an aromatic or heteroaromatic radical, andX and X.sup.1 each independently is oxygen or sulphur.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: April 21, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klemens Schluter, Hans-Jurgen Schnorbach
  • Patent number: 4657908
    Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.
    Type: Grant
    Filed: February 12, 1985
    Date of Patent: April 14, 1987
    Assignees: ICI Americas, Inc., Imperial Chemical Industries PLC
    Inventors: Tobias O. Yellin, David J. Gilman, Philip N. Edwards, Michael S. Large, Derrick F. Jones, Keith Oldham
  • Patent number: 4647569
    Abstract: Pyridylaminoethene derivatives of the formula: ##STR1## wherein R.sup.1 is pyridyl, unsubstituted or substituted by one or more substituents R.sup.4 selected from halogen, amino, carboxy, cyano nitro, hydroxy, formyl, trifluoromethyl, aryl, aryloxy, arylthio, benzyloxycarbonylamino, sulphamoyl, tetrazol-5-yl, carbamoyl, thiocarbamoyl, arylcarbamoyl, aroyl, alkyl, alkoxy, alkylthio, alkylsulphonyl, alkylamino, alkylsulphamoyl, arylalkyl, alkanoyl, alkoxycarbonyl, alkoxycarbonylamino, alkylcarbamoyl, alkanoylamino, N-benzyloxycarbonyl-N-alkylamino, or dialkylsulphamoyl, dialkylamino or dialkylcarbamoyl, wherein the alkyl groups may together form a ring, and R.sup.2 and R.sup.3 each represents phenyl, unsubstituted or substituted by one or more substituents R.sup.4 as hereinbefore defined, possess antiarthritic properties.
    Type: Grant
    Filed: September 19, 1985
    Date of Patent: March 3, 1987
    Assignee: May & Baker Limited
    Inventors: Raymond F. Collins, Philip Knowles, Libert C. Saunders, Francis J. Tierney, Peter J. Warne
  • Patent number: 4624962
    Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.
    Type: Grant
    Filed: February 1, 1985
    Date of Patent: November 25, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
  • Patent number: 4587240
    Abstract: Compounds which are a 1-hydroxypyrid-2-one in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by a substituent selected from aliphatic acyl, aliphatic amide, aliphatic amine, carboxy, cyano, aliphatic ester, halogen, hydroxy and sulpho groups, alkoxy groups and alkoxy groups substituted by an alkoxy, aliphatic amide, aliphatic amine, aliphatic ester, halogen or hydroxy group, aliphatic hydrocarbon groups and aliphatic hydrocarbon groups substituted by an alkoxy, aliphatic ester, halogen or hydroxy group, but excluding compounds in which said replacement of hydrogen atoms in the compound is effected only by substituents selected from aliphatic hydrocarbon groups, halogen groups and aliphatic hydrocarbon groups substituted by a halogen group, or a salt thereof containing a physiolgically acceptable ion or ions, are of value in the treatment of patients having a toxic concentration of a metal, particularly iron, in the body whilst the iron complexes of such compounds are of val
    Type: Grant
    Filed: September 18, 1984
    Date of Patent: May 6, 1986
    Assignee: National Research Development Corp.
    Inventors: Robert C. Hider, George Kontoghiorghes, Jack Silver, Michael A. Stockham
  • Patent number: 4585780
    Abstract: Pharmaceutical compositions containing a 3-hydroxypyrid-2-one or 3-hydroxypyrid-4-one in which the hydrogen atom attached to the nitrogen atom is replaced by an aliphatic acyl group, by an aliphatic hydrocarbon group, or by an aliphatic hydrocarbon group substituted by one or, except in the case of ionizable groups, more than one substituent selected from aliphatic acyl, alkoxy, aliphatic amine, aliphatic amide, carboxy, aliphatic ester, halogen, hydroxy and sulpho groups and, optionally, in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by one of said substituents, by an aliphatic hydrocarbon group, or by an aliphatic hydrocarbon group substituted by an alkoxy, aliphatic ester, halogen or hydroxy group, but excluding compounds in which said replacement of hydrogen atoms in the compound is effected only by aliphatic hydrocarbon groups, or a salt thereof containing a physiologically acceptable ion or ions, are of value for removing toxic amounts of metals, particularly iron,
    Type: Grant
    Filed: March 22, 1984
    Date of Patent: April 29, 1986
    Assignee: National Research Development Corp.
    Inventors: Robert C. Hider, George Kontoghiorghes, Jack Silver
  • Patent number: 4555517
    Abstract: Described are compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl, halo, cyano, hydroxy, amino, lower alkylamino, --CH.sub.2 NH.sub.2, CH.sub.2 OH or COOR"; R' is hydrogen, lower cycloalkyl or lower alkyl; R" is lower alkyl or --CH.sub.2 Ar wherein Ar is phenyl, substituted phenyl, furan or thiophene; R'" is COOR", ##STR2## and x is oxygen or nitrogen; or a pharmaceutically acceptable salt thereof and their use in the treatment of impaired ventricular myocardial contractility.The compounds exhibit cardiotonic activity.
    Type: Grant
    Filed: August 3, 1984
    Date of Patent: November 26, 1985
    Assignee: American Hospital Supply Corporation
    Inventors: David M. Stout, Diane M. Yamamoto, Cynthia Barcelon-Yang
  • Patent number: 4542140
    Abstract: .alpha.-Cyanoacrylic acid lower alkyl esters, and their corresponding amides, characterized by having a heterocyclic containing mercapto radical as one .beta.-substituent and an alkylthio, alkenylthio or a heterocyclic containing mercapto radical as another .beta.-substituent are useful for treating ulcers and for suppressing gastric acid secretion.
    Type: Grant
    Filed: October 20, 1983
    Date of Patent: September 17, 1985
    Assignee: American Home Products Corporation
    Inventors: Jehan Bagli, Tibor Bogri, Bozidar Palameta, Luis E. Borella
  • Patent number: 4515803
    Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.
    Type: Grant
    Filed: September 1, 1982
    Date of Patent: May 7, 1985
    Assignee: Hoechst Aktiengesellschafat
    Inventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
  • Patent number: 4497821
    Abstract: A method of controlling damage to the central nervous system of a patient which comprises administering to such patient a central nervous system-controlling effective amount of a pyridine derivative of the formula ##STR1## in which R is an optionally substituted aryl or heterocyclic radical,R.sup.1 and R.sup.2 are hydrogen or various organic radicals,X and Y are CN, --CO--R.sup.3, --COOR.sup.4 or --SO.sub.2 R.sup.5, or form with R.sup.1 or R.sup.2 a carbonyl-containing ring,R.sup.3 is an alkyl, aryl or aralkyl radical,R.sup.4 is hydrogen or an organic radical, andR.sup.5 is an optionally substituted alkyl or phenyl radical,or a salt thereof.
    Type: Grant
    Filed: February 28, 1983
    Date of Patent: February 5, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Egbert Wehinger, Horst Meyer, Ulrich Benz