The Diazine Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/115)
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Patent number: 4472400Abstract: Novel triazoloquinazolones of the formula ##STR1## wherein R and R' are individually selected from the group consisting of hydrogen, halogen, nitro and alkyl and alkoxy of 1 to 3 carbon atoms, Y is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 4 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms, B is an alkylene of 1 to 3 carbon atoms, X is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms, aralkyl of 7 to 8 carbon atoms, aminoalkyl of 2 to 4 carbon atoms, mono- and dialkylaminoalkyl with each alkyl having 2 to 4 carbon atoms, piperidinoalkyl of 1 to 4 alkyl carbon atoms, morpholinoalkyl of 1 to 4 alkyl carbon atoms and piperazinylalkyl of 1 to 4 alkyl carbon atoms or R.sub.1 and R.sub.Type: GrantFiled: September 21, 1982Date of Patent: September 18, 1984Assignee: Roussel UclafInventors: Wilfred R. Tully, Robert Westwood, David A. Rowlands, Stephen Clements-Jewery
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Patent number: 4472578Abstract: There have been prepared novel benzo[a]phenazine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or methoxy, R.sup.2 is hydrogen, methyl, acetyl, haloacetyl or substituted aminoalkyl, and R.sup.3 is ethoxy or substituted amino. These compounds are useful as antimicrobiological agents.Type: GrantFiled: March 23, 1983Date of Patent: September 18, 1984Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Noriichi Oda, Kazuhiro Kobayashi, Isoo Ito
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Patent number: 4444768Abstract: Novel amidines, especially N,N'-bridged carboxylic acid amidines of the general formula ##STR1## in which R.sub.1 represents an aromatic radical, R.sub.2 represents optionally esterified or amidated 1-carboxy-lower alkyl, Ph represents optionally substituted 1,2-phenylene and alk represents an aliphatic hydrocarbon radical separating the imino group from the methine group by from 1 to 3 carbon atoms, and their salts, have, inter alia, anti-inflammatory activity and can be used as active medicament substances in pharmaceutical preparations. They are produced according to methods known per se.Type: GrantFiled: July 1, 1982Date of Patent: April 24, 1984Assignee: Ciba-Geigy CorporationInventors: Ulrich Renner, Knut A. Jaeggi
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Patent number: 4409224Abstract: Pyrimido[1,6-a]indole derivatives characterized by having a substituted ethyl group at position 5 and optionally being further substituted at various positions on the pyrimido[1,6-a]indole nucleus are disclosed. The foregoing compounds are useful as antihypertensive agents in a mammal. Methods for their preparation also are disclosed.Type: GrantFiled: July 13, 1981Date of Patent: October 11, 1983Assignee: American Home Products Corp.Inventor: Ivo L. Jirkovsky
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Patent number: 4408047Abstract: Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.Type: GrantFiled: November 19, 1981Date of Patent: October 4, 1983Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, William C. Lumma, Jr.
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Patent number: 4391806Abstract: Substituted tetrahydropyridazino[1,6-a]benzimidazole compounds such as 2-methylamino-6,7,8,9-tetrahydropyridazino[1,6-a]benzimidazole are prepared by reacting a 2-halo-6,7,8,9-tetrahydropyridazino[1,6-a]benzimidazole with an appropriate amine. The compounds are useful as bronchodilators.Type: GrantFiled: July 12, 1982Date of Patent: July 5, 1983Assignee: The Dow Chemical CompanyInventors: Catherine A. Alexander, Robert J. Cregge, Norton P. Peet
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Patent number: 4391807Abstract: Substituted tetrahydroimidazo[2,1-a]phthalazine compounds such as 6-methylamino-7,8,9,10-tetrahydroimidazo[2,1-a]phthalazine are prepared by reacting a 6-halo-7,8,9,10-tetrahydroimidazo[1,2-a]phthalazine with an appropriate amine. The compounds are useful as bronchodilators.Type: GrantFiled: July 12, 1982Date of Patent: July 5, 1983Assignee: The Dow Chemical CompanyInventors: Catherine A. Alexander, Robert J. Cregge, Norton P. Peet
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Patent number: 4390697Abstract: A novel process for the preparation of triazoloquinazolinones of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, --NO.sub.2, --CF.sub.3, --CH.sub.3 and --OCH.sub.3, n is an integer from 2 to 5, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and hydroxyalkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom which they are attached form a saturated heterocycle optionally containing another heteroatom and optionally substituted with at least one member of the group consisting of hydroxy, alkyl and hydroxy alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, acyl of an aliphatic carboxylic acid of 1 to 5 carbon atoms, alkoxycarbonyl of 2 to 6 carbon atoms, aryl and aryl substituted with halogen or --CF.sub.3 and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and novel intermediates.Type: GrantFiled: November 3, 1981Date of Patent: June 28, 1983Assignee: Roussel UclafInventor: Wilfred R. Tully
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Patent number: 4350695Abstract: Novel triazoloquinazolinones of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, --NO.sub.2, methyl, methoxy and --CF.sub.3, n is an integer from 2 to 5, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl and hydroxyalkyl of 1 to 5 carbon atoms and taken together with the nitrogen atom to which they are attached form a saturated heterocycle optionally containing another heteroatom and optionally substituted with at least one member of the group consisting of hydroxy, alkyl and hydroxyalkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, acyl of an aliphatic carboxylic acid of 1 to 5 carbon atoms, alkoxycarbonyl of 2 to 6 carbon atoms and aryl optionally substituted with a halogen or --CF.sub.3 and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and their preparation.Type: GrantFiled: February 13, 1981Date of Patent: September 21, 1982Assignee: Roussel UclafInventors: Robert Westwood, Wilfred R. Tully, Robert Murdoch
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Patent number: 4337255Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter. The above compounds are useful as anti-allergy agents.Type: GrantFiled: July 19, 1978Date of Patent: June 29, 1982Assignee: E. R. Squibb & Sons, Inc.Inventor: B. Richard Vogt
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Patent number: 4330543Abstract: Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.Type: GrantFiled: March 28, 1980Date of Patent: May 18, 1982Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, William C. Lumma, Jr.
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Patent number: 4328223Abstract: The invention includes new 2-amino-3a,4,5,6-tetrahydro-perimidines and method for their preparation from corresponding racemacic compounds. Also included in the invention are pharmaceutical compositions containing said 2-amino-3a,4,5,6-tetrahydro-perimidines and methods for the use of said compounds and compositions.Type: GrantFiled: April 5, 1979Date of Patent: May 4, 1982Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Hildegard E. Mayer, Annedore Mayer, Andrea Mayer, Heinz Ziemann, Kurt Stoepel
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Patent number: 4307234Abstract: Pyrimido[1,6-a]indole derivatives characterized by having a substituted ethyl group at position 5 and optionally being further substituted at various positions on the pyrimido[1,6-a]indole nucleus are disclosed. The foregoing compounds are useful as antihypertensive agents in a mammal. Methods for their preparation also are disclosed.Type: GrantFiled: September 11, 1978Date of Patent: December 22, 1981Assignee: American Home Products Corp.Inventor: Ivo L. Jirkovsky
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Patent number: 4297355Abstract: This invention relates to (1H,3H,5H)-(1)-benzopyrano-(2,3-d)-pyrimidine-4-one-2-thiones, to pharmaceutically acceptable salts thereof, to the methods for their preparation and to their use as agents in the prophylactic treatment of allergic conditions such as asthma, allergic rhinitis, urticaria and ulcerative colitis.Type: GrantFiled: November 15, 1979Date of Patent: October 27, 1981Assignee: Schering CorporationInventor: David J. Blythin
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Patent number: 4291033Abstract: Novel oxoimidazoquinoxalines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, chlorine and bromine, X is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and cycloalkyl-alkyl of 4 to 6 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms, alkali metal, alkaline earth metal, aluminum, --NH.sub.4, organic amine and ##STR2## R.sub.4 and R.sub.5 are individually alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom form a saturated heterocycle of 4 to 6 carbon atoms optionally containing an oxygen atom or second nitrogen atom and n is a number from 1 to 5 and their non-toxic, pharmaceutically acceptable acid addition salts having antiallergic activity and their preparation.Type: GrantFiled: February 4, 1980Date of Patent: September 22, 1981Assignee: Roussel UclafInventors: Alan C. Barnes, David P. Kay
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Patent number: 4272535Abstract: Novel 2,4-(1H,3H,5H)-(1)benzopyrano-(2,3-d)-pyrimidinediones of the formula ##STR1## and their pharmaceutically acceptable salts are useful in the treatment of such diseases as asthma, allergic rhinitis, urticaria and ulcerative colitis.Type: GrantFiled: July 27, 1979Date of Patent: June 9, 1981Assignee: Schering CorporationInventor: David J. Blythin
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Patent number: 4269836Abstract: New 4H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidin-5(8H)on e and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: July 13, 1976Date of Patent: May 26, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4268671Abstract: Fluorescent dyes having the formula ##STR1## wherein R.sup.1 represents hydrogen, (C.sub.1 -C.sub.8) alkyl, trifluoromethyl, (C.sub.1 -C.sub.4) alkoxycarbonyl, (C.sub.1 -C.sub.4) alkoxycarbonyl (C.sub.1 -C.sub.4) alkyl, phenyl, or aralkyl group; R.sup.2 represents hydrogen, cyano, acyl, (C.sub.1 -C.sub.8) alkoxycarbonyl, (C.sub.1 -C.sub.4) alkoxy (C.sub.1 -C.sub.4) alkoxycarbonyl, (C.sub.1 -C.sub.4) alkoxy (C.sub.1 -C.sub.4) alkoxy (C.sub.1 -C.sub.4) alkoxycarbonyl, di(C.sub.1 -C.sub.4) alkylamino (C.sub.1 -C.sub.4) alkoxycarbonyl, cyclohexyloxycarbonyl, aryloxycarbonyl, benzyloxycarbonyl, tetrahydrofurfuryloxycarbonyl, carbamoyl, N-(C.sub.1 -C.sub.4) alkylcarbamoyl, N,N-di(C.sub.1 -C.sub.4)alkylcarbamoyl, N-phenylcarbamoyl, or morpholinocarbonyl group; and R.sup.3 and R.sup.4 can be the same or different and each represents hydrogen, (C.sub.1 -C.sub.8) alkyl, (C.sub.1 -C.sub.4) alkoxy(C.sub.1 -C.sub.4) alkyl, aralkyl or phenyl group which can be substituted by halogen atoms, (C.sub.1 -C.sub.Type: GrantFiled: April 13, 1978Date of Patent: May 19, 1981Assignee: Mitsubishi Chemical Industries Ltd.Inventors: Seiichi Imahori, Yukichi Murata, Syuichi Maeda, Sumio Suzuki
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Patent number: 4232887Abstract: Chromogenic compounds of normally colorless form are disclosed having the following structural formula: ##STR1## wherein E represents a six-membered aromatic or heterocyclic ring which may have an aromatic condensed ring and both the E ring and the condensed ring may be substituted, A represents an optionally substituted aminophenyl, indolyl, benzoindolyl, julolidinyl or kairolyl radical or the radical represented by B, and B represents a family of indolizine radicals. The compounds of this invention are eligible for use in pressure-sensitive and heat sensitive record materials and manifold marking systems.Type: GrantFiled: March 5, 1979Date of Patent: November 11, 1980Assignee: Appleton Papers Inc.Inventors: William J. Becker, Sheldon Farber, Troy E. Hoover
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Patent number: 4233300Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: November 13, 1979Date of Patent: November 11, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4202899Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]-pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: April 21, 1976Date of Patent: May 13, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4164578Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## (wherein R.sup.9. is hydrogen or alkyl, Q is CH or N); ##STR4## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR5## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter. These compounds are useful as anti-allergy agents.Type: GrantFiled: July 19, 1978Date of Patent: August 14, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: B. Richard Vogt
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Patent number: 4145420Abstract: Compounds are provided having the structure ##STR1## whereinR.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter.Type: GrantFiled: July 19, 1978Date of Patent: March 20, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: B. Richard Vogt
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Patent number: 4139530Abstract: Cationic dyestuffs of the general formula ##STR1## IN WHICH THE SYMBOLS HAVE THE MEANING MENTIONED ABOVE INTERMEDIATES AND PROCESSES FOR THEIR PRODUCTION AND THEIR USE FOR DYEING AND PRINTING OF NATURAL AND SYNTHETIC MATERIALS.Type: GrantFiled: January 10, 1977Date of Patent: February 13, 1979Assignee: Bayer AktiengesellschaftInventors: Walter Kalk, Karl H. Schundehutte
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Patent number: 4129653Abstract: Substituted pyrrolo[1,2-c] quinazolines useful for their cardiovascular activities and as antiasthmatic agents.Type: GrantFiled: January 5, 1977Date of Patent: December 12, 1978Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Seymour Levine
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Patent number: 4128643Abstract: (2-Amino-4-quinazolinyl)-quanidines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the defined meanings, and their physiologically tolerable acid addition salts, process for preparing these compounds, pharmaceutical preparations containing them and their use as medicines.Type: GrantFiled: May 26, 1977Date of Patent: December 5, 1978Assignee: Hoechst AktiengesellschaftInventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
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Patent number: 4128645Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: September 1, 1977Date of Patent: December 5, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4128644Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are defined hereinafter.Type: GrantFiled: July 29, 1977Date of Patent: December 5, 1978Assignee: E. R. Squibb & Sons, Inc.Inventor: B. Richard Vogt
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Patent number: 4127657Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',4':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: September 1, 1977Date of Patent: November 28, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4127655Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e]-[1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: January 9, 1978Date of Patent: November 28, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4113867Abstract: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.Type: GrantFiled: November 15, 1976Date of Patent: September 12, 1978Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Jurgen Seubert, Herbert Thomas, Peter Andrews
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Patent number: 4110454Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: January 9, 1978Date of Patent: August 29, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4109087Abstract: New 1,4- and 4,10-dihydro-4-oxo-pyrimido[1,2-a]-benzimidazole-3-carboxamides have the general formulas ##STR1## They are useful as central nervous system depressants and anti-inflammatory agents.Type: GrantFiled: December 12, 1977Date of Patent: August 22, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4109091Abstract: New derivatives, and their salts, of 1,4- and 4,10-dihydro-4-oxo-pyrimido[1,2-a]benzimidazole-3-carboxylic acid amides have the general formula ##STR1## They are useful as central nervous system depressants and anti-inflammatory agents.Type: GrantFiled: December 12, 1977Date of Patent: August 22, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4105764Abstract: 4,5-Dihydro-5-oxopyrazolo[1,5-a]quinazoline-3-carboxamides, useful as anti-secretory agents, are prepared by reaction of an appropriate 4-R.sub.2 -4,5-dihydro-5-oxopyrazolo[1,5-a]quinazoline-3-carboxylic acid halide with an appropriate amine.Type: GrantFiled: August 19, 1977Date of Patent: August 8, 1978Assignee: Sterling Drug Inc.Inventor: E. John Alexander
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Patent number: 4087423Abstract: New pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidines have the general formula ##STR1## They are useful as antiinflammatory agents.Type: GrantFiled: July 20, 1977Date of Patent: May 2, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Uwe D. Treuner, Hermann Breuer
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Patent number: 4077956Abstract: New 5-substituted derivatives of dipyrazolo[1,5-a:4',3'-e]pyrazine-6-carboxylic acid, esters and their salts have the formula ##STR1## R.sup.1 is hydrogen, lower alkyl or phenyl-lower alkylene; R.sup.2 and R.sup.3 each is hydrogen or lower alkyl; X is oxygen or sulfur; and R.sup.4 is hydrogen, lower alkyl, phenyl-lower alkylene or amino-lower alkylene.The new compounds are useful as anti-inflammatory agents and immunosuppressive agents.Type: GrantFiled: August 30, 1976Date of Patent: March 7, 1978Assignee: E. R. Squibb & Sons, Inc.Inventor: Uwe D. Treuner
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Patent number: 4078064Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: August 18, 1976Date of Patent: March 7, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4072679Abstract: New derivatives, and their salts, of 1,4- and 4,10-dihydro-4-oxo-pyrimido[1,2-a]benzimidazole-3-carboxylic acids, esters and carboxamides have the general formulas ##STR1## They are useful as central nervous system depressants and anti-inflammatory agents.Type: GrantFiled: June 15, 1976Date of Patent: February 7, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4070466Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido-[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: February 19, 1976Date of Patent: January 24, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4061632Abstract: New 3,11-dihydro-6H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[4,3-d]pyrimidin-6 -one derivatives have the general formula ##STR1## The compounds are useful as anti-inflammatory agents.Type: GrantFiled: September 17, 1976Date of Patent: December 6, 1977Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn
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Patent number: 4053474Abstract: New pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidines have the general formula ##STR1## They are useful as antiinflammatory agents.Type: GrantFiled: April 21, 1976Date of Patent: October 11, 1977Assignee: E. R. Squibb & Sons, Inc.Inventors: Uwe D. Treuner, Hermann Breuer
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Patent number: 4053600Abstract: The invention discloses 5-substituted-1,2,4-triazolo[4,3-c]quinazolines and 1,2,4-triazolo[1,5-c]quinazolines having pharmacological activity in animals and useful, for example, as hypotensive and anti-inflammatory agents. The compounds may be prepared, for example, by reacting a 5-halo-1,2,4-triazolo-quinazoline with a compound representing the function to be introduced at the 5-position. The 5-halo-1,2,4-triazolo[4,3-c]quinazolines also have pharmacological activity, e.g., hypotensive and anti-inflammatory activity, and may be prepared by reacting a 4-hydrazino-quinazoline with trimethoxy methane. The 5-halo-1,2,4-triazolo[1,5-c]quinazolines also have hypotensive and anti-inflammatory activity and are prepared from the corresponding 1,2,4-triazolo-[1,5-c]quinazolin-5(1H)-one using phosphorus oxychloride, the quinazolin-5(1H)-one being in turn prepared from the 5-halo-1,2,4-triazolo[4,3-c]quinazoline.Type: GrantFiled: June 25, 1975Date of Patent: October 11, 1977Assignee: Sandoz, Inc.Inventors: Goetz E. Hardtmann, Faizulla G. Kathawala
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Patent number: 4052393Abstract: New 4-substituted derivatives of pyrazolo[1,5-a]-quinoxaline-3-carboxylic acid, esters and their salts have the formula ##STR1## R.sub.1 is hydrogen, lower alkyl or a salt forming ion; R.sub.2 is hydrogen, lower alkyl, phenyl-lower alkylene or amino-lower alkylene; R.sub.3 is hydrogen, lower alkyl, halogen or lower alkoxy; and X is oxygen or sulfur.The new compounds are useful as anti-inflammatory agents.Type: GrantFiled: March 22, 1976Date of Patent: October 4, 1977Assignee: E. R. Squibb & Sons, Inc.Inventor: Uwe D. Treuner
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Patent number: 4052398Abstract: New diazarhodamine-lactones of the formula ##STR1## where R.sup.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sup.2 is alkyl of 1 to 4 carbon atoms, unsubstituted phenyl or phenyl substituted by one or two alkyls of 1 to 3 carbon atoms, chlorine and/or bromine, R.sup.3 and R.sup.4 independently of one another are hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, phenylalkyl of 7 to 10 carbon atoms or alkoxyalkyl of a total of 3 to 8 carbon atoms, or the group ##STR2## is a 5-membered, 6-membered or 7-membered saturated heterocyclic ring or a 6-membered saturated heterocyclic ring which additionally contains an --O--, --S-- or --N--group, wherein R.sup.6 is hydrogen, methyl or ethyl and R.sup.5 is unsubstituted phenyl or phenyl substituted by alkyl of 1 to 3 carbon atoms, methoxy, chlorine or bromine.The lactones (I) exhibit improved stability and therefore do not stain coated paper.Type: GrantFiled: February 13, 1976Date of Patent: October 4, 1977Assignee: BASF AktiengesellschaftInventors: Hellmut Kast, Guenter Dunkelmann