The Diazine Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/115)
  • Patent number: 4472400
    Abstract: 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: Grant
    Filed: September 21, 1982
    Date of Patent: September 18, 1984
    Assignee: Roussel Uclaf
    Inventors: Wilfred R. Tully, Robert Westwood, David A. Rowlands, Stephen Clements-Jewery
  • Patent number: 4472578
    Abstract: 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: Grant
    Filed: March 23, 1983
    Date of Patent: September 18, 1984
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Noriichi Oda, Kazuhiro Kobayashi, Isoo Ito
  • Patent number: 4444768
    Abstract: 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: Grant
    Filed: July 1, 1982
    Date of Patent: April 24, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Ulrich Renner, Knut A. Jaeggi
  • Patent number: 4409224
    Abstract: 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: Grant
    Filed: July 13, 1981
    Date of Patent: October 11, 1983
    Assignee: American Home Products Corp.
    Inventor: Ivo L. Jirkovsky
  • Patent number: 4408047
    Abstract: Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: November 19, 1981
    Date of Patent: October 4, 1983
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, William C. Lumma, Jr.
  • Patent number: 4391806
    Abstract: 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: Grant
    Filed: July 12, 1982
    Date of Patent: July 5, 1983
    Assignee: The Dow Chemical Company
    Inventors: Catherine A. Alexander, Robert J. Cregge, Norton P. Peet
  • Patent number: 4391807
    Abstract: 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: Grant
    Filed: July 12, 1982
    Date of Patent: July 5, 1983
    Assignee: The Dow Chemical Company
    Inventors: Catherine A. Alexander, Robert J. Cregge, Norton P. Peet
  • Patent number: 4390697
    Abstract: 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: Grant
    Filed: November 3, 1981
    Date of Patent: June 28, 1983
    Assignee: Roussel Uclaf
    Inventor: Wilfred R. Tully
  • Patent number: 4350695
    Abstract: 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: Grant
    Filed: February 13, 1981
    Date of Patent: September 21, 1982
    Assignee: Roussel Uclaf
    Inventors: Robert Westwood, Wilfred R. Tully, Robert Murdoch
  • Patent number: 4337255
    Abstract: 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: Grant
    Filed: July 19, 1978
    Date of Patent: June 29, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Patent number: 4330543
    Abstract: Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: March 28, 1980
    Date of Patent: May 18, 1982
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, William C. Lumma, Jr.
  • Patent number: 4328223
    Abstract: 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: Grant
    Filed: April 5, 1979
    Date of Patent: May 4, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Joachim Kabbe, Hildegard E. Mayer, Annedore Mayer, Andrea Mayer, Heinz Ziemann, Kurt Stoepel
  • Patent number: 4307234
    Abstract: 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: Grant
    Filed: September 11, 1978
    Date of Patent: December 22, 1981
    Assignee: American Home Products Corp.
    Inventor: Ivo L. Jirkovsky
  • Patent number: 4297355
    Abstract: 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: Grant
    Filed: November 15, 1979
    Date of Patent: October 27, 1981
    Assignee: Schering Corporation
    Inventor: David J. Blythin
  • Patent number: 4291033
    Abstract: 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: Grant
    Filed: February 4, 1980
    Date of Patent: September 22, 1981
    Assignee: Roussel Uclaf
    Inventors: Alan C. Barnes, David P. Kay
  • Patent number: 4272535
    Abstract: 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: Grant
    Filed: July 27, 1979
    Date of Patent: June 9, 1981
    Assignee: Schering Corporation
    Inventor: David J. Blythin
  • Patent number: 4269836
    Abstract: 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: Grant
    Filed: July 13, 1976
    Date of Patent: May 26, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4268671
    Abstract: 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: Grant
    Filed: April 13, 1978
    Date of Patent: May 19, 1981
    Assignee: Mitsubishi Chemical Industries Ltd.
    Inventors: Seiichi Imahori, Yukichi Murata, Syuichi Maeda, Sumio Suzuki
  • Patent number: 4232887
    Abstract: 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: Grant
    Filed: March 5, 1979
    Date of Patent: November 11, 1980
    Assignee: Appleton Papers Inc.
    Inventors: William J. Becker, Sheldon Farber, Troy E. Hoover
  • Patent number: 4233300
    Abstract: 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: Grant
    Filed: November 13, 1979
    Date of Patent: November 11, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4202899
    Abstract: 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: Grant
    Filed: April 21, 1976
    Date of Patent: May 13, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4164578
    Abstract: 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: Grant
    Filed: July 19, 1978
    Date of Patent: August 14, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Patent number: 4145420
    Abstract: 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: Grant
    Filed: July 19, 1978
    Date of Patent: March 20, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Patent number: 4139530
    Abstract: 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: Grant
    Filed: January 10, 1977
    Date of Patent: February 13, 1979
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Kalk, Karl H. Schundehutte
  • Patent number: 4129653
    Abstract: Substituted pyrrolo[1,2-c] quinazolines useful for their cardiovascular activities and as antiasthmatic agents.
    Type: Grant
    Filed: January 5, 1977
    Date of Patent: December 12, 1978
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Seymour Levine
  • Patent number: 4128643
    Abstract: (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: Grant
    Filed: May 26, 1977
    Date of Patent: December 5, 1978
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
  • Patent number: 4128645
    Abstract: 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: Grant
    Filed: September 1, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4128644
    Abstract: 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: Grant
    Filed: July 29, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Patent number: 4127657
    Abstract: 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: Grant
    Filed: September 1, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4127655
    Abstract: 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: Grant
    Filed: January 9, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4113867
    Abstract: 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: Grant
    Filed: November 15, 1976
    Date of Patent: September 12, 1978
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Jurgen Seubert, Herbert Thomas, Peter Andrews
  • Patent number: 4110454
    Abstract: 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: Grant
    Filed: January 9, 1978
    Date of Patent: August 29, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4109087
    Abstract: 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: Grant
    Filed: December 12, 1977
    Date of Patent: August 22, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4109091
    Abstract: 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: Grant
    Filed: December 12, 1977
    Date of Patent: August 22, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4105764
    Abstract: 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: Grant
    Filed: August 19, 1977
    Date of Patent: August 8, 1978
    Assignee: Sterling Drug Inc.
    Inventor: E. John Alexander
  • Patent number: 4087423
    Abstract: 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: Grant
    Filed: July 20, 1977
    Date of Patent: May 2, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Uwe D. Treuner, Hermann Breuer
  • Patent number: 4077956
    Abstract: 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: Grant
    Filed: August 30, 1976
    Date of Patent: March 7, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Uwe D. Treuner
  • Patent number: 4078064
    Abstract: 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: Grant
    Filed: August 18, 1976
    Date of Patent: March 7, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4072679
    Abstract: 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: Grant
    Filed: June 15, 1976
    Date of Patent: February 7, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4070466
    Abstract: 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: Grant
    Filed: February 19, 1976
    Date of Patent: January 24, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4061632
    Abstract: 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: Grant
    Filed: September 17, 1976
    Date of Patent: December 6, 1977
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4053474
    Abstract: 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: Grant
    Filed: April 21, 1976
    Date of Patent: October 11, 1977
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Uwe D. Treuner, Hermann Breuer
  • Patent number: 4053600
    Abstract: 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: Grant
    Filed: June 25, 1975
    Date of Patent: October 11, 1977
    Assignee: Sandoz, Inc.
    Inventors: Goetz E. Hardtmann, Faizulla G. Kathawala
  • Patent number: 4052393
    Abstract: 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: Grant
    Filed: March 22, 1976
    Date of Patent: October 4, 1977
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Uwe D. Treuner
  • Patent number: 4052398
    Abstract: 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: Grant
    Filed: February 13, 1976
    Date of Patent: October 4, 1977
    Assignee: BASF Aktiengesellschaft
    Inventors: Hellmut Kast, Guenter Dunkelmann