Chalcogen In The Tricyclo Ring System Patents (Class 540/560)
-
Patent number: 5153190Abstract: 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: GrantFiled: March 7, 1991Date of Patent: October 6, 1992Assignee: Adir et CompagnieInventors: Sylvain Rault, Michel Boulouard, Marie P. Foloppe, Max Robba, Beatrice Guardiola, Michelle Devissague
-
Patent number: 5130301Abstract: 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: GrantFiled: March 26, 1991Date of Patent: July 14, 1992Assignee: Adir et CompagnieInventors: Sylvain Rault, Michel Boulouard, Max Robba, Beatrice Guardiola, Michelle Devissaguet
-
Patent number: 5116971Abstract: 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: GrantFiled: September 19, 1990Date of Patent: May 26, 1992Assignee: Boehringer Ingelheim KGInventors: Albrecht Harreus, Karl-Heinz Weber, Werner Stransky, Gerhard Walther, Gojko Muacevic, Jorge C. Stenzel, Wolf-Dietrich Bechtel
-
Patent number: 5104543Abstract: 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: GrantFiled: April 1, 1991Date of Patent: April 14, 1992Assignee: Boehringer Ingelheim GmbHInventors: Klaus Brandt, Jurgen Nagel
-
Patent number: 5028603Abstract: There are provided novel ester-substituted thienotriazolodiazepines useful for the treatment of various PAF-induced diseases.Type: GrantFiled: February 3, 1989Date of Patent: July 2, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tetsuya Tahara, Minoru Moriwaki, Masao Abe, Michio Terasawa
-
Patent number: 5008263Abstract: 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: GrantFiled: March 20, 1990Date of Patent: April 16, 1991Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael J. Fray
-
Patent number: 4968794Abstract: 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: GrantFiled: October 3, 1988Date of Patent: November 6, 1990Assignee: Boehringer Ingelheim KGInventors: Karl-Heinz Weber, Albrecht Harreus, Jorge C. Stenzel, Gojko Muacevic, Wolfgang Troger, Gerhard Walther
-
Patent number: 4959361Abstract: 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: GrantFiled: October 3, 1988Date of Patent: September 25, 1990Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
-
Patent number: 4914096Abstract: 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: GrantFiled: March 31, 1989Date of Patent: April 3, 1990Assignee: Sandoz Pharmaceuticals Corp.Inventors: William J. Houlihan, Seung H. Cheon
-
Patent number: 4910194Abstract: 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: GrantFiled: May 16, 1989Date of Patent: March 20, 1990Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Minoru Moriwaki, Yoichi Akiyama, Kenichi Demizu, Hiroshi Mikashima
-
Patent number: 4900729Abstract: 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: GrantFiled: October 11, 1988Date of Patent: February 13, 1990Assignee: Boehringer Ingelheim KGInventors: Werner Stransky, Karl-Heinz Weber, Gerhard Walther, Albrecht Harreus, Jorge C. Stenzel, Gojko Muacevic, Wolf-Dietrich Bechtel
-
Patent number: 4820703Abstract: 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: GrantFiled: November 17, 1987Date of Patent: April 11, 1989Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Tetsuya Tahara, Minoru Moriwaki, Masao Abe, Shuji Yuasa
-
Patent number: 4678499Abstract: 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: GrantFiled: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan