Nitrogen Bonded Directly To Chalcogen Patents (Class 548/197)
  • Patent number: 4791200
    Abstract: The present invention relates to novel 2-substituted-4-aryloxyalkylamine thiazoles as described herein. The thiazoles are useful as antisecretory agents.
    Type: Grant
    Filed: June 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, Maud Urbanski
  • Patent number: 4766138
    Abstract: Use of 4-(isoxazolyl)-thiazole-2-oxamic acid derivatives; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiarthritic activity; compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: August 23, 1988
    Assignee: Zambon S.p.A.
    Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
  • Patent number: 4766137
    Abstract: 4-(isoxazolyl)-thiazole-2-oxamic acids, esters and salts thereof; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiallergic and antianaphylactic activity and may be used in the pharmaceutical field.Compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: August 23, 1988
    Assignee: Zambon S.p.A.
    Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
  • Patent number: 4742060
    Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: May 3, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4701447
    Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.
    Type: Grant
    Filed: September 23, 1983
    Date of Patent: October 20, 1987
    Assignee: Schering Corporation
    Inventors: Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
  • Patent number: 4663341
    Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: May 5, 1987
    Assignee: Rohm and Haas Company
    Inventor: Richard M. Jacobson
  • Patent number: 4659727
    Abstract: Ethene derivatives of the formula:[R.sup.5 (R.sup.1 CR.sup.4 .dbd.CR.sup.2 R.sup.3).sub.m ].sub.n Iwherein R.sup.5 represents optionally substituted heterocyclyl or a group --CR.sup.4 .dbd.CR.sup.2 R.sup.3, or optionally substituted aryl, heterocyclylalkyl or arylalkyl and R.sup.1 represents --NR.sup.6 -- wherein R.sup.6 represents hydrogen or optionally substituted alkyl or aryl, or R.sup.5 represents a quinonoidal group, and R.sup.1 represents .dbd.N--, R.sup.4 represents hydrogen, alkoxy, alkylthio, trifluoromethyl or optionally substituted alkyl or aryl, R.sup.2 represents cyano, formyl, alkoxycarbonyl, alkylsulphonyl, dialkylcarbamoyl, dialkylthiocarbamoyl, aryloxycarbonyl, arylsulphinyl or arylsulphonyl, R.sup.3 represents a group R.sup.2 or hydrogen, nitro or optionally substituted aryl or aroyl or alkanoyl, and m and n are 1 or 2, and pharmaceutically acceptable salts thereof, with the exclusion of certain compounds in which R.sup.
    Type: Grant
    Filed: September 10, 1985
    Date of Patent: April 21, 1987
    Assignee: May & Baker Limited
    Inventors: Adnan H. Al-Shaar, Barbara J. Broughton, Robert K. Chambers, David W. Gilmour, Diane M. Kelsey, Peter Lowden, Edward Lunt, David J. Lythgoe, Ian McClenaghan, Duncan C. McDougall, Libert C. Saunders, Keith A. J. Stuttle, Peter J. Warne
  • Patent number: 4647557
    Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.
    Type: Grant
    Filed: December 23, 1983
    Date of Patent: March 3, 1987
    Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
  • Patent number: 4625025
    Abstract: Disclosed is a process for producing a heterocyclic compound having a nitromethylene group as the side chain, of the formula ##STR1## wherein Y represents a hydrogen atom, a halogen atom or a lower alkyl group, R represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aralkyl group, an alkenyl group, an alkynyl group or an acyl group, and n represents an integer of 2, 3 or 4,which comprises reacting a 2,2,2-trihalo-1-nitroethane compound with a 1-aminoalkanethiol compound or a 1-N-substituted derivative thereof.
    Type: Grant
    Filed: August 10, 1984
    Date of Patent: November 25, 1986
    Assignee: Ube Industries, Ltd.
    Inventors: Fumio Iwata, Katsumasa Harada, Ryoji Sugise
  • Patent number: 4622330
    Abstract: Novel 3-amino or substituted amino pyrazoles are disclosed as having antiprotozoal and antiparasitic activity in particular anticoccidial activity and are useful for controlling cecal and or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.
    Type: Grant
    Filed: June 19, 1984
    Date of Patent: November 11, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Richard A. Dybas, Edward F. Rogers
  • Patent number: 4604243
    Abstract: An olefin, especially an activated olefin, is arylated by reaction with an arylamine, such as an aniline, in an inert polar organic solvent and in the presence of an alkyl nitrite, a hydrogen halide, and a catalytic amount of a copper catalyst having the copper in an oxidation state below +2.
    Type: Grant
    Filed: July 25, 1985
    Date of Patent: August 5, 1986
    Assignee: Ethyl Corporation
    Inventor: Robert I. Davidson
  • Patent number: 4596811
    Abstract: The invention relates to special heterocyclic compounds corresponding to general tautomeric formula I which are distinguished by improved antagonistic activity on histamine-H.sub.2 -receptors. The invention also relates to a process for producing these compounds and to medicaments containing them.
    Type: Grant
    Filed: October 18, 1983
    Date of Patent: June 24, 1986
    Assignee: Ludwig Heumann & Co., GmbH
    Inventors: Istvan Szelenyi, Stefan Postius, Helmut Schickaneder, Herbert Hansen
  • Patent number: 4514566
    Abstract: Carbamoyl-oxime compounds of the formula ##STR1## wherein A, R.sup.3, R.sup.4 and R.sup.5 are as hereinafter set forth, a process for their preparation, pesticidal compositions containing one or more of these compounds as the active ingredient, methods of use of such compositions for the control of pests, particularly insects, mites, nematodes and molluscs, and intermediates for the production of such compounds are described.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: April 30, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph Luthy, Paul Winternitz
  • Patent number: 4458077
    Abstract: Compounds of the formulaAr--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --ONHRwherein R is ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;X is O or CH.sub.2 ;m=0 or 1;n=2 or 3; andAr is a moiety selected from the group ##STR2## wherein R.sub.2 is hydrogen or lower alkyl, ##STR3## with the proviso that when Ar is ##STR4## and X is CH.sub.2, then R is other than ##STR5## and the pharmacologically acceptable salts thereof have H.sub.2 -antagonist activity and activity in decreasing gastric acid secretions.
    Type: Grant
    Filed: November 22, 1982
    Date of Patent: July 3, 1984
    Assignee: American Home Products Corporation
    Inventor: John R. Potoski
  • Patent number: 4452985
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, cyano or cyano(lower)alkyl;R.sup.2 is hydrogen, cyano, carboxy, carbamoyl, guanyl, (lower)alkoxyimino, hydrazinocarbonyl, (lower)alkylaminoimino, ##STR2## with the proviso that one but never both of R.sup.1 and R.sup.2 is hydrogen; and the pharmacologically acceptable salts thereof exhibit H.sub.2 -receptor antagonist and gastric secretion inhibition activity.
    Type: Grant
    Filed: February 14, 1983
    Date of Patent: June 5, 1984
    Assignee: American Home Products Corporation
    Inventors: Arthur A. Santilli, Anthony C. Scotese, Robert L. Morris, Stanley C. Bell
  • Patent number: 4421757
    Abstract: Thiazoline derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.6 and Y have the meanings given, their physiologically tolerated salts, processes for their preparation, pharmaceutical preparations based on these compounds as well as their use as medicaments comprise the invention. In addition, intermediates are described.
    Type: Grant
    Filed: December 28, 1981
    Date of Patent: December 20, 1983
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Bernhard Seuring, Ernold Granzer
  • Patent number: 4409216
    Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 R.sup.2 are the same or different and represent hydrogen, halogen, C.sub.1-6 alkyl, phenyl, benzyl,C.sub.3-6 cycloalkyl, carbo-C.sub.1-6 alkoxy or C.sub.1-6 carboxy or R.sup.1 and R.sup.2 represent the remaining members of a benzene ring;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl; andR.sup.
    Type: Grant
    Filed: April 11, 1980
    Date of Patent: October 11, 1983
    Assignee: Beecham Group Limited
    Inventor: Barrie C. C. Cantello
  • Patent number: 4346088
    Abstract: Thiazoline derivatives of the general formula I ##STR1## wherein R.sup.1 to R.sup.7 have the specified meanings, physiologically acceptable acid addition salts thereof, processes for their preparation, pharmaceutical preparations based on these compounds and their use for acting on the serum lipoprotein spectrum. The invention moreover relates to compounds of the formulae ##STR2## wherein A, R, R.sup.1 to R.sup.7, Y and Z have the specified meanings.
    Type: Grant
    Filed: July 1, 1980
    Date of Patent: August 24, 1982
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Bernhard Seuring, Ernold Granzer
  • Patent number: 4331680
    Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.
    Type: Grant
    Filed: August 25, 1980
    Date of Patent: May 25, 1982
    Assignee: The Boots Company
    Inventors: David P. Giles, John C. Kerry, Antonin Kozlik, Bryan H. Palmer, Stephen W. Shutler, Robert J. Willis
  • Patent number: 4331668
    Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2- position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with alkyl group interrupted by sulfur or oxygen. The 4- and 5- positions of the pyrrole ring can also be substituted.
    Type: Grant
    Filed: June 16, 1980
    Date of Patent: May 25, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Patent number: 4315931
    Abstract: Unsubstituted or substituted 5-phenyl- and 5-benzyl-4-amino-pyrimidine-2-imidoacid esters, their preparation, drugs containing these compounds, and their use in infectious diseases.
    Type: Grant
    Filed: July 3, 1978
    Date of Patent: February 16, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Scharwaechter, Klaus Gutsche, Wilhelm Kohlmann, Gerd Kroemer, deceased, by Norma Kroemer, legal representative, by Helmut Kroemer, legal representative, by Maria M. Kroemer, legal representative
  • Patent number: 4307104
    Abstract: The compounds of this invention are 2,3-unsaturated nitrogen containing heterocyclic compounds with a 3-nitro group and a 2-(2-guanidino-4-thiazolyl alkylamino) group. These compounds have histamine H.sub.2 -antagonist activity. A particular compound of this invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethylamino]-3-nitro-1,4,-5,6-tetra hydropyridine.
    Type: Grant
    Filed: October 14, 1980
    Date of Patent: December 22, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Patent number: 4283408
    Abstract: Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.
    Type: Grant
    Filed: December 27, 1979
    Date of Patent: August 11, 1981
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Yasufumi Hirata, Isao Yanagisawa, Yoshio Ishii, Shinichi Tsukamoto, Noriki Ito, Yasuo Isomura, Masaaki Takeda
  • Patent number: 4200578
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 and R.sup.3 each are independently hydrogen, (lower)alkyl, guanidino or --(CH.sub.2).sub.p NR.sup.4 R.sup.5 ; R.sup.4 and R.sup.5 each are independently hydrogen, (lower)alkyl or phenyl; n is 2 or 3; p is 1, 2 or 3; X is NR.sup.6 or CHR.sup.6 ; R.sup.6 is cyano, nitro, SO.sub.2 Ar or SO.sub.2 (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.
    Type: Grant
    Filed: December 18, 1978
    Date of Patent: April 29, 1980
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • 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