Chalcogen In The Tricyclo Ring System Patents (Class 540/560)
  • Patent number: 5153190
    Abstract: The invention relates to pyrrolo [1,2-a] thieno [3,2-f][1,4]diazepine compounds of the formula (I) ##STR1## in which: R.sub.1 is hydrogen; alkyl optionally substituted with alkoxy, hydroxy, cycloalkyl, or phenyl; or alkyl- or arylsulfonyl; R.sub.2 is hydrogen, phenyl, or phenylalkyl; alkyl optionally substituted with hydroxyl, alkoxy, oxo, cycloalkyl or phenyl; or optionally substituted amino; R.sub.3 represents hydrogen or alkyl, and R.sub.4 and R.sub.5 independently represent: hydrogen, alkyl optionally substituted with alkoxy, cycloalkyl, or phenyl; or phenyl; their isomers, diastereoisomers and enantiomers as well as their addition salts with pharmaceutically-acceptable acids. The compounds are useful for treating cerebral ischemia, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, and hyperglycemia and are obtained in a few steps from the corresponding substituted 2-(1-pyrrolyl)thiophenes ##STR2## Y=--CHO or H; X= CN, CONH.sub.2, CH.sub.2 NHCOR.sub.2, or CH.sub.2 NH.sub.2.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: October 6, 1992
    Assignee: Adir et Compagnie
    Inventors: Sylvain Rault, Michel Boulouard, Marie P. Foloppe, Max Robba, Beatrice Guardiola, Michelle Devissague
  • Patent number: 5130301
    Abstract: Novel 4H-pyrrolo[1,2-a]thieno[2,3-f][1,4]diazepine which are usable as a medicinal product and correspond to the general formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meaning as given in the specification.These compounds, as well as their physiologically tolerable salts, may be used in therapy, in particular in the treatment of disorders linked to hypoxemia and to certain metabolic disorders.
    Type: Grant
    Filed: March 26, 1991
    Date of Patent: July 14, 1992
    Assignee: Adir et Compagnie
    Inventors: Sylvain Rault, Michel Boulouard, Max Robba, Beatrice Guardiola, Michelle Devissaguet
  • Patent number: 5116971
    Abstract: The invention relates to new 1,4-diazepines of the general formula ##STR1## in which R.sub.1, R.sub.2 R.sub.3, X and A have the meaning indicated in the specification.The new compounds are intended for use for the treatment of pathological states and diseases in which PAF (platelet activating factor) is involved.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: May 26, 1992
    Assignee: Boehringer Ingelheim KG
    Inventors: Albrecht Harreus, Karl-Heinz Weber, Werner Stransky, Gerhard Walther, Gojko Muacevic, Jorge C. Stenzel, Wolf-Dietrich Bechtel
  • Patent number: 5104543
    Abstract: The invention relates to a method of separation by liquid chromatography for preparing enantiomerically pure hetrazines, using cellulose triacetate as a stationary phase and a polar solvent as a mobile phase.
    Type: Grant
    Filed: April 1, 1991
    Date of Patent: April 14, 1992
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Klaus Brandt, Jurgen Nagel
  • Patent number: 5028603
    Abstract: There are provided novel ester-substituted thienotriazolodiazepines useful for the treatment of various PAF-induced diseases.
    Type: Grant
    Filed: February 3, 1989
    Date of Patent: July 2, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tetsuya Tahara, Minoru Moriwaki, Masao Abe, Michio Terasawa
  • Patent number: 5008263
    Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: April 16, 1991
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael J. Fray
  • Patent number: 4968794
    Abstract: The invention relates to new thieno-traizolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: November 6, 1990
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Albrecht Harreus, Jorge C. Stenzel, Gojko Muacevic, Wolfgang Troger, Gerhard Walther
  • Patent number: 4959361
    Abstract: The invention relates to compounds of the formula ##STR1## wherein X is --CH.dbd.CH-- or S; R.sub.1 is lower alkyl, lower alkoxy or trifluoromethyl;R.sub.2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or alkanoyloxy;R.sub.3 and R.sub.4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy;s is an integer from 0 to 1, provided that when s is 1,R.sub.2 cannot be hydroxy, lower alkoxy or alkanoyloxy;R.sub.5 is a radical of the formula R.sub.6 --(CH.sub.2).sub.n -- or R.sub.7 --O--(CH.sub.2).sub.m --wherein R.sub.6 and R.sub.7 are aryl or a heterocyclic radical, n is an integer of from 0 to 2 and m is an integer of from 1 to 2, provided that, when n is 0, R.sub.6 must be attached through a carbon to carbon bond, and provided that R.sub.7 is always attached through a carbon to oxygen bond,and, when at least one asymmetric carbon is present, its enantiomers and racemates, and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: September 25, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4914096
    Abstract: The invention discloses certain 6-aryl-substituted-4H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]diazepines useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated bronchoconstriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lung injury, for controlling hyperreactive airways and for protecting against endotoxin-induced hypotension and death.
    Type: Grant
    Filed: March 31, 1989
    Date of Patent: April 3, 1990
    Assignee: Sandoz Pharmaceuticals Corp.
    Inventors: William J. Houlihan, Seung H. Cheon
  • Patent number: 4910194
    Abstract: A thienotriazolodiazepine compound of the formula: ##STR1## wherein each symbol is as defined in the spedification, or a pharmaceutically acceptable acid addition salt thereof, and pharmaceutically uses thereof.Said compounds exhibit PAF-antagonistic acitivty and are useful for the prevention or treatment of various PAF-induced diseases.
    Type: Grant
    Filed: May 16, 1989
    Date of Patent: March 20, 1990
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Minoru Moriwaki, Yoichi Akiyama, Kenichi Demizu, Hiroshi Mikashima
  • Patent number: 4900729
    Abstract: The invention relates to new thieno-1,4-diazepines of general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.degree., R', Z, X, Y and n have the meanings given in the specification.The new compounds are intended to be used in the treatment of pathological conditions and diseases in which PAF (platelet activating factor) is implicated.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: February 13, 1990
    Assignee: Boehringer Ingelheim KG
    Inventors: Werner Stransky, Karl-Heinz Weber, Gerhard Walther, Albrecht Harreus, Jorge C. Stenzel, Gojko Muacevic, Wolf-Dietrich Bechtel
  • Patent number: 4820703
    Abstract: A thienotriazolodiazepine compound of the formula: ##STR1## wherein A is alkylene or substituted alkylene and each other symbol is as defined in the specification and a pharmaceutically acceptable acid addition salt thereof, and pharmaceutical uses thereof.Said compounds exhibit PAF-antagonistic activity and are useful for the prevention or treatment of various PAF-induced diseases.
    Type: Grant
    Filed: November 17, 1987
    Date of Patent: April 11, 1989
    Assignee: Yoshitomi Pharmaceutical Industries Ltd.
    Inventors: Tetsuya Tahara, Minoru Moriwaki, Masao Abe, Shuji Yuasa
  • Patent number: 4678499
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: January 30, 1986
    Date of Patent: July 7, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan