Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 544/252)
  • Patent number: 4192944
    Abstract: A novel series of optionally substituted 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-N-(1H-tetrazol-5-yl)carboxamides is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.
    Type: Grant
    Filed: April 3, 1978
    Date of Patent: March 11, 1980
    Assignee: Bristol-Myers Company
    Inventor: Peter F. Juby
  • Patent number: 4175193
    Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxyquinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxyquinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxypyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.
    Type: Grant
    Filed: March 27, 1978
    Date of Patent: November 20, 1979
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4133884
    Abstract: Substituted pyrroloquinoxalinones and diones, useful as anti-inflammatory and anti-thrombotic agents.
    Type: Grant
    Filed: December 12, 1977
    Date of Patent: January 9, 1979
    Assignee: Eli Lilly and Company
    Inventor: Richard E. Holmes
  • 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: 4128647
    Abstract: 2,3,8,9-Tetrahydro-5H,6H-thiazolo[3,2-a]thiopyrano[4,3-d]pyrimidines of the structure ##STR1## are provided wherein R is hydrogen, lower alkyl, halogen, acyl, cyano, carboxyl, trifluoromethyl or lower alkoxy, n is 0 or 2 and m is 2 or 3. These compounds are useful in the treatment of auto-immune disorders, such as rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • Patent number: 4128648
    Abstract: 2,3,8,9-Tetrahydro-5H,6H-pyrano[4,3-d]thiazolo[3,2-a]pyrimidines of the structure ##STR1## are provided wherein R.sup.1 and R.sup.2 may be the same or different and are hydrogen, lower alkyl, halogen, cyano, carbethoxy, carboxyl, trifluoromethyl or lower alkoxy, and n is 2 or 3, and m is 0 to 2. These compounds are useful in the treatment of auto-immune disorders, such as rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • Patent number: 4127720
    Abstract: A series of novel pyrimido[2,1-a]isoquinoline derivatives is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.
    Type: Grant
    Filed: September 21, 1977
    Date of Patent: November 28, 1978
    Assignee: Bristol-Myers Company
    Inventors: Peter F. Juby, Thomas W. Hudyma, Richard A. Partyka
  • Patent number: 4126683
    Abstract: The invention concerns novel fused ring indole derivatives of the formula ##STR1## and the pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein n represents 1 or 2 and R.sup.1 represents hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl, halogen, amino or mono- or di-(lower)alkylamino. The compounds are useful as anti-depressant agents.
    Type: Grant
    Filed: June 8, 1977
    Date of Patent: November 21, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robert F. Sugden
  • 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: 4112096
    Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 or ##STR2## R.sup.2 is ##STR3## hydrogen, lower alkyl or phenyl optionally substituted by R.sup.4 with the proviso that at lest one of R.sup.1 and R.sup.2 is ##STR4## R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl optionally substituted by R.sup.4 ; and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (C1, Br and F), nitro, and trifluoromethyl; R.sup.6 is hydrogen, lower alkyl, alkanoyl, aroyl, aralkanoyl, aralkyl or phenyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter.These compounds are useful as anti-allergics.
    Type: Grant
    Filed: March 17, 1977
    Date of Patent: September 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Patent number: 4112098
    Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1 to 3 carbons, 1-(hydroxyimino)alkyl, alkanoylamino, amino, or ##STR2## wherein alkyl in the above groups contains 1 to 4 carbons; R.sup.2 is 1-(hydroxyimino)alkyl, alkanoylamino, amino, ##STR3## hydrogen, lower alkyl or phenyl (optionally substituted by R.sup.4) wherein alkyl in the above groups contains 1 to 4 carbons; R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl (optionally substituted with R.sup.4), dialkylaminoalkyl, hydroxyalkyl, ##STR4## (wherein R.sup.6 is hydrogen or alkyl, and R.sup.7 is alkyl); with the proviso that R.sup.1 or R.sup.2 is 1-(hydroxyimino)alkyl, alkanoylamino or amino, when R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl; and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl. The above compounds are useful as anti-allergy agents and antiinflammatory agents.
    Type: Grant
    Filed: October 17, 1977
    Date of Patent: September 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Patent number: 4110452
    Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is alkylamino, dialkylamino, or ##STR2## wherein alkyl in the above groups contains 1 to 4 carbons; R.sup.2 is alkylamino, dialkylamino or ##STR3## wherein alkyl in the above groups contains 1 to 4 carbons; at least one of R.sup.1 and R.sup.2 being alkylamino or dialkylamino; R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl (optionally substituted with R.sup.8), or ##STR4## (wherein R.sup.6 is amino, alkylamino or dialkylamino, and R.sup.7 is alkyl); and R.sup.4, R.sup.5 and R.sup.8 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl.
    Type: Grant
    Filed: October 17, 1977
    Date of Patent: August 29, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: George C. Rovnyak, B. Richard Vogt
  • Patent number: 4096145
    Abstract: Compounds of the formula ##STR1## where A is a heterocyclic group containing a pyridone moiety and R to R.sup.5 are each hydrogen or substituents conventionally encountered in dyes. The compounds are eminently suitable for coloring resins and for dyeing textile materials, particularly polyester textile materials.
    Type: Grant
    Filed: March 14, 1977
    Date of Patent: June 20, 1978
    Assignee: BASF Aktiengesellschaft
    Inventor: Ernst Schefczik