Patents Represented by Attorney Charles J. Metz
  • Patent number: 5130312
    Abstract: N-(3-hydroxy-4-piperidinyl)substituted benzamides, their N-oxide forms and pharmaceutically acceptable acid-addition salts having gastro-intestinal motility stimulating properties, compositions containing the same, and methods of treating warm blooded animals suffering from a decreased peristalsis of the gastrointestinal system.
    Type: Grant
    Filed: January 23, 1990
    Date of Patent: July 14, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Karel J. Van Loon
  • Patent number: 5126339
    Abstract: Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which compounds are useful agents in the treatment of allergic diseases.
    Type: Grant
    Filed: March 19, 1991
    Date of Patent: June 30, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens
  • Patent number: 5120845
    Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.
    Type: Grant
    Filed: July 24, 1991
    Date of Patent: June 9, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
  • Patent number: 5112825
    Abstract: Novel pyridazinamines having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.
    Type: Grant
    Filed: April 30, 1990
    Date of Patent: May 12, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa
  • Patent number: 5106973
    Abstract: Novel pyridazinamine derivatives having antiviral activity, compositions containing these compounds as active ingredient, and a method of destructing viruses or preventing the growth thereof in warm-blooded animals suffering from diseases caused by these viruses. Processes for preparing said compounds and compositions.
    Type: Grant
    Filed: November 15, 1990
    Date of Patent: April 21, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Marcel G. M. Luyckx, Gilbert A. J. Grauwels
  • Patent number: 5100893
    Abstract: Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula ##STR1## wherein one or two carbon atoms of the ##STR2## moiety may be substituted with C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or two carbon atoms of the CH.sub.2 groups of said moiety may be bridged with a C.sub.2-4 alkanediyl radical;X represents CH or N; R.sup.1 represents hydrogen, C.sub.1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylcarbonyl or aryl; R.sup.2 and R.sup.3 each independently represent hydrogen or C.sub.1-4 alkyl; Alk represents C.sub.1-4 alkanediyl;R.sup.4 and R.sup.5 each independently represent hydrogen, C.sub.1-4 alkyl or halo; andHet represents ##STR3## the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity.
    Type: Grant
    Filed: November 27, 1990
    Date of Patent: March 31, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Gilbert A. J. Grauwels, Cyriel A. M. Van der Eycken
  • Patent number: 5089608
    Abstract: There is disclosed a process which comprises the steps of:(a) reacting a di(hydrocarbyl)tin oxide such as a dialkyltin oxide with a dihydric alcohol, alkanolamine, or an enolizable .alpha.-hydroxyketone in an inert organic reaction vehicle, with removal of water, at a temperature and for a period of time sufficient to produce a cyclic adduct of said dialkyltin oxide and said dihydric alcohol, alkanolamine, or enolizable .alpha.-hydroxyketone;(b) reacting said cyclic adduct product of Step (a) with sucrose in an inert organic reaction vehicle such as a dipolar aprotic liquid, at a temperature and for a period of time sufficient to produce a 6-O-[dihydrocarbyl(hydroxy- or amino- or oxohydrocarbyl)stannoxyl]sucrose; and(c) reacting the product of Step (b) with an acylating agent to produce a sucrose-6-ester.
    Type: Grant
    Filed: March 23, 1990
    Date of Patent: February 18, 1992
    Assignee: McNeil-PPC, Inc.
    Inventors: Robert E. Walkup, Nicholas M. Vernon, Robert E. Wingard, Jr.
  • Patent number: 5086056
    Abstract: 2-(Heterocyclylalkyl)imidazopyridines having antihistaminic properties, compositions containing these compounds as active ingredient and novel 2-(Heterocyclylalkyl)imidazopyridines.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: February 4, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Francois M. Sommen, Joseph L. G. Torremans, Gaston S. M. Diels
  • Patent number: 5075315
    Abstract: Novel hexahydro-2H-indeno[1,2-c]pyridines and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties.
    Type: Grant
    Filed: May 17, 1990
    Date of Patent: December 24, 1991
    Assignee: McNeilab, Inc.
    Inventor: Chris R. Rasmussen
  • Patent number: 5075309
    Abstract: 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]m ethoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones, their pharmaceutically acceptable acid addition salts and stereoisomeric forms having improved antifungal properties, compositions containing the same, and methods of inhibiting and/or preventing the growth or the development of fungi, or of destroying fungi, in warm-blooded animals suffering from diseases caused by these fungi.
    Type: Grant
    Filed: May 1, 1990
    Date of Patent: December 24, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Leo J. J. Backx
  • Patent number: 5071846
    Abstract: [(Bicyclic heterocyclyl)methyl and --hetero] substituted hexahydro--1H--azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti--histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.
    Type: Grant
    Filed: November 6, 1990
    Date of Patent: December 10, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels, Geert Pille
  • Patent number: 5070090
    Abstract: Novel (thio)morpholinyl and piperazinyl alkylphenol ethers having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting, combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.
    Type: Grant
    Filed: April 25, 1990
    Date of Patent: December 3, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa
  • Patent number: 5066656
    Abstract: (6,7-dihydro-5H-pyrrolo[1,2-c]imidazolyl-5-yl)- and (5,6,7,8-tetrahydroimidazo[1,5-a]pyridinyl-5-yl) substituted 1H-benzotriazole derivatives, compositions containing the same and methods of treating estrogen dependent disorders.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: November 19, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael N. Greco, Marcel A. C. Janssen
  • Patent number: 5057525
    Abstract: Novel N-(3-hydroxy-4-pipridinyl)benzamides and derivatives thereof, said compounds being used as stimulators of the motility of the gastro-intestinal system.
    Type: Grant
    Filed: June 11, 1990
    Date of Patent: October 15, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventor: Georges Van Daele
  • Patent number: 5043327
    Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: August 27, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
  • Patent number: 5041454
    Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.
    Type: Grant
    Filed: April 19, 1990
    Date of Patent: August 20, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
  • Patent number: 5041448
    Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.
    Type: Grant
    Filed: March 9, 1989
    Date of Patent: August 20, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels
  • Patent number: 5039677
    Abstract: (1H-azol-1-ylmethyl)substituted benzotriazole derivatives, compositions containing the same, and methods of treating estrogen dependent disorders.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: August 13, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Josephus L. H. Van Gelder, Marc G. Venet
  • Patent number: 5037829
    Abstract: (1H-azol-1-ylmethyl)substituted quinazoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: August 6, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Gerard C. Sanz, Marc G. Venet
  • Patent number: RE33833
    Abstract: Novel N-(bicyclic heterocyclyl)-4-piperidinamines having anti-histamimic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases.
    Type: Grant
    Filed: November 29, 1990
    Date of Patent: February 25, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens, Theophilus T. J. M. Van Offenwert