Nitrogen Of The Hetero Ring Is Shared By An Additional Cyclo Of The Tricyclo Ring System Patents (Class 540/558)
  • Patent number: 5532359
    Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.
    Type: Grant
    Filed: October 25, 1994
    Date of Patent: July 2, 1996
    Assignees: Genentech, Inc., Board of Regents, The University of Texas System
    Inventors: James C. Marsters, Jr., Michael S. Brown, Craig W. Crowley, Joseph L. Goldstein, Guy L. James, Robert S. McDowell, David Oare, Thomas E. Rawson, Mark Reynolds, Todd C. Somers
  • Patent number: 5521173
    Abstract: Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: May 28, 1996
    Assignee: American Home Products Corporation
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright, George T. Grosu
  • Patent number: 5516774
    Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: May 14, 1996
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Marvin F. Reich, Fuk-Wah Sum, Efren G. Delos Santos
  • Patent number: 5387585
    Abstract: The novel imidazodiazepine derivatives of the formula: ##STR1## wherein the substituents are as described in the specification, can be used for the control or prevention of epileptic seizures, anxiety, tension and excitation states, sleep disorders, schizophrenic symptoms, hepatic encephalopathy and senile dementia, as well as, in the partial or complete antagonization of undesired side-effects of substances acting on benzodiazepine receptors after over-dosage or after their use in intensive medicine and in anesthesia.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: February 7, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Borer, Walter Gassner, Max Gerecke, Emilio Kyburz
  • Patent number: 5380721
    Abstract: Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## .delta.-aminoamides of formula III and aryldimethanamines of formula XXXVII ##STR2## wherein A is an aryl or hetaryl ring;R.sup.1 is hydrogen, alkyl, aryl or hetaryl;R.sup.2 is hydrogen, alkyl, substituted alkyl, or aryl;R.sup.3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl;R.sup.4 is hydrogen or alkyl;R.sup.5 is hydrogen, alkyl, aryl or hetaryl;R.sup.6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring;R.sup.9 is hydrogen, alkyl, or substituted alkyl; andR.sup.10 is hydrogen, alkyl, or substituted alkyl.The invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: January 10, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Robert E. Johnson, Donald C. Schlegel, Alan M. Ezrin
  • Patent number: 4985420
    Abstract: The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.
    Type: Grant
    Filed: December 7, 1988
    Date of Patent: January 15, 1991
    Assignee: Duphar International Research B.V.
    Inventors: Derk Hamminga, Hans H. Haeck, Ineke Van Wijngaarden, Wouter Wouters
  • Patent number: 4847248
    Abstract: Aromatic 1,4-benzodiazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment employing these compounds.
    Type: Grant
    Filed: January 6, 1988
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Roger M. Freidinger, Ben E. Evans, Mark G. Bock