Patents Represented by Attorney Charles J. Metz
  • Patent number: 5824336
    Abstract: The present invention relates to compositions comprising flubendazole of formula (I), which are palatable to companion animals, especially dogs. ##STR1## These find utility as palatable anthelmintic compositions for the treatment of helminthiasis.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: October 20, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Eugene Maria Jozef Jans, Paul Marie Victor Gilis
  • Patent number: 5746349
    Abstract: A childproof device (1) for holding and dispensing liquids, in particular medicines, that provides precise dosages of liquid, comprising a bottle (2), a cap (5) which is irremovable from the bottleneck (4), said cap being associated with a hollow cylinder (6) extending axially to near the bottle bottom (3) and a reciprocating dispenser comprising a barrel (8) and a plunger (9). The dispenser provides the only means of getting medicine out of the bottle since the cylinder associated with the cap prevents the contents of the bottle from being poured or shaken out. The device is easily assembled and can be stored, sold and used as supplied by the manufacturer.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: May 5, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Peter Putteman, Alfons Jeanne Wouters
  • Patent number: 5739134
    Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: April 14, 1998
    Assignee: Janssen Pharmacetuica N.V.
    Inventors: Georges H.P. Van Daele, deceased, Frans M.A. Van den Keybus, Marie L. Hendrickx, heiress, Kurt G.C.E. Van Daele, heir, Peter J.V. Van Daele, heir, Glenn K.L. Van Daele, heir
  • Patent number: 5728700
    Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-4 alkyl; or phenyl optionally substituted with halo, C.sub.1-4 alkylcarbonylamino, C.sub.1-4 alkyloxy, C.sub.1-4 alkyl or nitro; Z is C.dbd.O or CHOH; and ##STR2## is a radical of formula ##STR3## Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: March 17, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Raymond Antoine Stokbroekx, Joseph Hector Mostmans, Louis Jozef Elisabeth Van der Veken
  • Patent number: 5714507
    Abstract: Synergistic fungicidal compositions containing a fungicidal triazole and metconazole for treating plants or the loci thereof, or for use in wood-preservation or protection of biodegradable materials. Method of treating plants comprising the administration of a fungicidal triazole and metconazole. Method of protecting wood, wood-products and biodegradable materials from fungal attack and destruction.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: February 3, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Alex Raymond Albert Valcke, Mark Arthur Josepha Van Der Flaas
  • Patent number: 5712275
    Abstract: Use of 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides having the formula ##STR1## wherein n is 0, 1 or 2; R.sup.1 is hydrogen, C.sub.1-4 alkyl or benzyl; and R represents (a) phenyl; phenyl substituted with 1 to 3 substituents independently selected from hydroxyl, halo, C.sub.1-12 alkyl, C.sub.5-6 cycloalkyl, trihalomethyl, phenyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, tetrahydropyranyloxy, phenoxy, C.sub.1-4 alkylcarbonyl, phenylcarbonyl, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, carboxy or its alkali metal salt, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylaminocarbonyl, phenylaminocarbonyl, tolylaminocarbonyl, morpholinocarbonyl, amino, nitro, cyano, dioxolanyl or C.sub.1-4 alkyloxyiminomethyl; naphthyl; pyridinyl; thienyl, preferably when n is not 2; furanyl; or thienyl or furanyl substituted with one to three substituents independently selected from C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, halo, cyano, formyl, acetyl, benzoyl, nitro, C.sub.
    Type: Grant
    Filed: January 25, 1996
    Date of Patent: January 27, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventor: Jozef Frans Elizabetha Van Gestel
  • Patent number: 5710156
    Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric form thereof, wherein X and Y are CH or N; R.sup.1, R.sup.2 and R.sup.3 are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-4 alkyloxyC.sub.1-6 alkyl, phenyl or phenylC.sub.1-4 alkyl; Z is C.dbd.O or CHOH; and ##STR2## compositions comprising said compounds, processes for preparing the same and the use of these compounds for treating Helicobacter related diseases.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: January 20, 1998
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Joseph Hector Mostmans, Robert Jozef Maria Hendrickx, Louis Jozef Elisabeth Van der Veken, Raymond Antoine Stokbroekx, Marcel Jozef Maria Van de Aa
  • Patent number: 5707977
    Abstract: A compound of formula (I), ##STR1## an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form --N.dbd.CH--, --CH.dbd.N--, --CH.sub.2 --CH.sub.2, CH.dbd.CH--, --C(.dbd.O)--CH.sub.2 --, --CH.sub.2 --C(.dbd.O); D is a radical of formula ##STR2## L is a radical of formula ##STR3## Alk is a C.sub.1-4 alkanediyl radical; R.sup.1 is halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, or R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: January 13, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Luc Alfons Leo Van der Eycken, Frank Christopher Odds, Jean Louis Mesens
  • Patent number: 5707975
    Abstract: The present invention concerns a formulation for oral administration comprising an antifungal, a sufficient amount of a cyclodextrin or a derivative thereof, an aqueous acidic medium as bulk liquid carrier and an alcoholic co-solvent Addition of one or more pharmaceutically acceptable sweeteners and one or more pharmaceutically acceptable flavors thereto yields palatable oral formulations. A process of preparing such formulations and pharmaceutical dosage forms comprising said formulations.
    Type: Grant
    Filed: February 22, 1996
    Date of Patent: January 13, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Karel Jozef Fran.cedilla.ois, Willy Maria Albert Carlo Dries
  • Patent number: 5703115
    Abstract: The present invention is concerned with vasoconstricive ?benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.
    Type: Grant
    Filed: April 15, 1996
    Date of Patent: December 30, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
  • Patent number: 5700814
    Abstract: An aqueous suspension for oral administration comprising sabeluzole and a pharmaceutically acceptable carrier, having a pH in the range from 8 to 10; processes for preparing the same.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: December 23, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Karel Jozef Fran.cedilla.ois, Christine Frieda Augusta Agemans
  • Patent number: 5691354
    Abstract: 2-??1-?4-(4-fluorophenoxy)butyl!-4-piperidinyl!methylamino!-benzothiazolole s ##STR1## wherein R.sup.1 or R.sup.2 is hydroxy, the other variable always being hydrogen, and the pharmaceutically acceptable acid addition salts thereof. Novel compounds, pharmaceutical compositions, as well as their use as a class III antiarrhythmicum is disclosed.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: November 25, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jozef Jan Pieter Heykants, Marcel Jan Maria Borgers, Doris Wilhelm
  • Patent number: 5691344
    Abstract: The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, the N-oxides thereof and the stereochemically isomeric forms thereof, wherein .dbd.a.sub.1 --a.sub.2 .dbd.a.sub.3 --a.sub.4 .dbd. is a bivalent radical of formula:.dbd.N--CH.dbd.CH--CH.dbd. (a),.dbd.CH--N.dbd.CH--CH.dbd. (b),.dbd.CH--CH.dbd.N--CH.dbd. (c),.dbd.CH--CH.dbd.CH--N.dbd. (d),wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is C.sub.1-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## wherein R.sup.4 is hydrogen, cyano, aminocarbonyl or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: November 25, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil, Maria Encarnacion Matesanz-Ballesteros
  • Patent number: 5691201
    Abstract: The present invention is concerned with the use of sabeluzole for the manufacture of a medicament for the treatment of patients suffering from chronic neuro-degenerative diseases such as dementia of the Alzheimer type (DAT) or Alzheimer's disease, amyotrophic lateral sclerosis (ALS), dementia associated with Parkinson's disease and related diseases which are characterized by progressive dementia.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: November 25, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Gilbert Henri Camiel Clincke, Luc Remi Mathilde Tritsmans, Hugo Alfons Gabriel Geerts
  • Patent number: 5691358
    Abstract: Piperidinyl substituted benzamides of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is halo; R.sup.3 is hydrogen or halo; R.sup.4 and R.sup.5 each independently are hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl; and the group NR.sup.4 R.sup.5 may also be azido, Alk is C.sub.2-4 alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT.sub.2 -receptor sites; and process for imaging an organ are disclosed.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: November 25, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Josepha Eduarda Maria Francisca Leysen, Georges Henri Paul Van Daele
  • Patent number: 5688799
    Abstract: The present invention is concerned with novel compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl;D is a bicyclic heterocycle of formula ##STR2## wherein each R.sup.1 independently is C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl; C.sub.1-19 alkyl optionally substituted with C.sub.3-6 cycloalkyl, halo, C.sub.1-6 alkyloxy or cyano; and each R.sup.2 independently is hydrogen or C.sub.1-4 alkyl. Novel compounds; compositions; processes for preparing novel compounds and intermediates are described.
    Type: Grant
    Filed: March 3, 1996
    Date of Patent: November 18, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis
  • Patent number: 5688814
    Abstract: Piperidinyl substituted benzamides of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is halo; R.sup.3 is hydrogen or halo; R.sup.4 and R.sup.5 each independently are hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl; and the group NR.sup.4 R.sup.5 may also be azido, Alk is C.sub.2-4 alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT.sub.2 -receptor sites; and process for imaging an organ are disclosed.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: November 18, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Josepha Eduarda Maria Francisca Leysen, Georges Henri Paul Van Daele
  • Patent number: 5688952
    Abstract: The present invention is concerned with vasoconstricive ?(benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.
    Type: Grant
    Filed: April 15, 1996
    Date of Patent: November 18, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
  • Patent number: 5684049
    Abstract: A compound for use as a medicine having the formula ##STR1## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cyclo-alkyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom bearing said R.sup.1 and R.sup.2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C.sub.1-4 alkylpiperazinyl group; X is O or S; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl-carbonyl, aminocarbonyl, or hydroxy; R.sup.7 is hydrogen or halo; and R.sup.8, R.sup.9 and R.sup.10 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: November 4, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges Henri Van Daele, Marc Gustaaf Verdonck, Jean-Paul Rene Bosmans, Paul Adriaan Janssen
  • Patent number: 5681582
    Abstract: The present invention is concerned with an extended release, film coated tablet comprising as active ingredients the antihistaminic, antiallergic agent astemizole and the adrenergic, decongestant agent pseudoephedrine hydrochloride and with a process of preparing such tablets.
    Type: Grant
    Filed: November 8, 1995
    Date of Patent: October 28, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Paul Marie Victor Gilis, Eugene Marie Jozef Jans, Guido Jozef Maria Gijs