Patents Represented by Attorney Charles J. Metz
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Patent number: 5677310Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein 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 C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl-S-, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.Type: GrantFiled: February 5, 1996Date of Patent: October 14, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
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Patent number: 5675027Abstract: Intermediate for making 4-?2-Benzothiazolyl)methylamino!-alpha-?93,4-difluorophenoxy0methyl!1-pipe ridineethanol having the formula ##STR1##Type: GrantFiled: March 24, 1995Date of Patent: October 7, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond Antoine Stokbroekx, Gilbert Arthur Jules Grauwels
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Patent number: 5674868Abstract: Method of treating 5-HT.sub.3 -mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) ##STR1## the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.C(Cl)--CH.dbd.CH-- (b) or --CH.dbd.CH--C(Cl).dbd.CH-- (c); n represents 2, 3 or 4; R.sup.3 represents hydrogen or methoxy; m represents 1 or 2; R.sup.4 represents hydrogen, amino or C.sub.1-3 -alkylcarbonylamino; and R.sup.5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.Type: GrantFiled: June 16, 1995Date of Patent: October 7, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges Henri Paul Van Daele, Jean-Paul Rene Marie Andre Bosmans, Willy Joannes Carolus Van Laerhoven
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Patent number: 5674866Abstract: The present invention is concerned with novel imidazoazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; --A--B-- is a radical of formula --X--CH.dbd.CH-- (a-1); --CH.dbd.CH--X-- (a-2); or --CH.dbd.CH-- CH.dbd.CH-- (a-3); X represents O, S or NR.sup.1 ; R.sup.1 represents hydrogen or C.sub.1-6 alkyl; -----Y is a radical of formula .dbd.O (b-1); --OH (b-2); or .dbd.N--OH (b-3); and L represents hydrogen, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkyloxycarbonyl, phenylcarbonyl, C.sub.1-6 alkyl or C.sub.1-6 alkyl substituted with C.sub.1-4 alkyloxycarbonyl, hydroxycarbonyl, aryl, aryloxy or a radical of formula ##STR2## --D--Z-- is --S--CH.dbd.CH--, --S--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --; and aryl is phenyl or phenyl substituted with halo, hydroxy or C.sub.1-4 alkyloxy.Type: GrantFiled: December 13, 1995Date of Patent: October 7, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts
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Patent number: 5674871Abstract: The present invention relates to the iontophoretic delivery to a patient, more in particular to a migraine patient, of a compound of formula (I) as shown hereinunder. The invention also relates to a device for the iontophoretic delivery of a compound of formula (I), as well as to a composition containing a compound of formula (I), which can be applied in a device for iontophoretic delivery. Said compounds are benzopyranalkylaminoalkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein 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 taken together 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 form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.Type: GrantFiled: January 26, 1996Date of Patent: October 7, 1997Assignee: Janssen Pharmaceutica N. V.Inventors: Jean Louis Mesens, Gustaaf Van Reet, Frank Maria Jozef De Beukelaar
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Patent number: 5663354Abstract: A process for preparing (+)-6-[(4-chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotri azole comprising the resolution of (.+-.)-6-[(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-[(4-chlorophenyl)(1 H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole.Type: GrantFiled: April 18, 1995Date of Patent: September 2, 1997Assignee: Janssen Pharmaceutica, N.V.Inventors: Albert Louis Anna Willemsens, Walter Louis Antoine Verstappen, Alex Herman Copmans, Anna Maria Jozefa Vandendriessche, Alfons Gaston Maria De Knaep, Marc Gaston Venet
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Patent number: 5654293Abstract: The present invention relates to a topical oil-in-water emulsion composition comprising ketoconazole, an acetonide glucocorticosteroid and a dermatologically acceptable carrier, characterized by a pH above 2.5 and below 6, and a method of preparing said composition.Type: GrantFiled: June 14, 1995Date of Patent: August 5, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Marc Karel Jozef Fran.cedilla.ois, Alfons Jeanne Wouters, Gerard Frans Maria Jan Cauwenbergh
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Patent number: 5650411Abstract: The use for the manufacture of a medicament for treating Helicobacter-related diseases of a compound of formula ##STR1## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, whereinX and Y each independently are 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;Z is C.dbd.O or CHOH; andAr is phenyl optionally substituted with up to three substituents selected from hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, halo, trifluoromethyl, triC.sub.1-4 alkylsilyloxy, nitro, amino and cyano or pyridinyl substituted with hydroxy or C.sub.Type: GrantFiled: July 18, 1995Date of Patent: July 22, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Joseph Hector Mostmans, Luc Alfons Leo Van Der Eycken, Frank Christopher Odds, Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa
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Patent number: 5643603Abstract: A composition of a bioadhesive carrier for a prolonged, sustained and controlled delivery of a drug having a local or systemic action contains pregelatinized or thermally modified, food accepted starches and optionally a synthetic polymer.The pregelatinized starches are preferably precooked and dried starches.Type: GrantFiled: July 13, 1994Date of Patent: July 1, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Peter Bottenberg, Jean Paul Louis August Remon, Christian Dominique Erwin De Muynck, Dick Slop
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Patent number: 5641494Abstract: The use of a compound having the formula ##STR1## wherein R represents methyl or ethyl, for regulating the greasiness of the skin, particular novel physical forms of said compound, cosmetic compositions comprising said agent, processes for preparing said agent and compositions, and a method of reducing the greasiness of the skin.Type: GrantFiled: October 6, 1995Date of Patent: June 24, 1997Assignee: Janssen Pharmaceutica N.V.Inventor: Gerard Frans Maria Jan Cauwenbergh
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Patent number: 5639754Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X is O or S; 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; C.sub.1-4 alkyl substituted with arylcyclohexyl; aryl or arylcarbonyl; wherein aryl is phenyl optionally substituted with one or two substituents selected from halo and C.sub.1-4 alkyl;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: GrantFiled: May 23, 1995Date of Patent: June 17, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond Antoine Stokbroekx, Marc Willems, Marcel Jozef Maria Van der Aa
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Patent number: 5637592Abstract: 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, trifiuoromethyl, trifiuoromethyloxy or difluoromethyloxy; R.sup.6 is hydrogen; or R.sup.6 is phenyl optionally substituted with halo; pyridinyl; furanyl; thienyl; 3-chloro-benzo[b]thien-2-yl; trifiuoromethyl; C.sub.1-4 alkyloxycarbonyl; dihalophenylcyclopropanyl; C.sub.3-6 cycloalkyl; adamantyl; C.sub.2-6 alkenyl optionally substituted with halophenyl; or C.sub.1-4 alkyl optionally substituted with halo, phenyl, halophenyl, dihalophenyl, phenyloxy, piperidinyl, pyrrolidinyl, piperazinyl, C.sub.1-4 alkylpiperazinyl, C.sub.1-4 alkylcarbonylpiperazinyl, C.sub.1-4 alkyloxycarbonylpiperazinyl, phthalimino, amino, mono- or di(C.sub.Type: GrantFiled: May 23, 1995Date of Patent: June 10, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond A. Stokbroekx, Joseph H. Mostmans, Louis J. E. Van der Veken
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Patent number: 5633015Abstract: The present invention is concerned with beads comprising a 25-30 mesh core, a coating of a hydrophilic polymer and an antifungal agent, and a seal outer coating layer; pharmaceutical dosage forms comprising said beads and a method of preparing said beads. Preferred antifungal agents are lipophilic azole antifungals, such as itraconazole and saperconazole.Type: GrantFiled: March 13, 1995Date of Patent: May 27, 1997Inventors: Paul M. V. Gilis, Valentin F. V. De Conde, Roger P. G. Vandecruys
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Patent number: 5629308Abstract: Antiallergic imidazo[1,2-a](pyrrolo, thieno or furano)[2,3-d]azepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond;R.sup.1 represents hydrogen, C.sub.1-4 alkyl, halo, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC.sub.1-4 alkyl;R.sup.2 represents hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl;R.sup.3 represents hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, phenyl or halo;X represents O, S or NR.sub.4 ;L represents hydrogen; C.sub.1-6 alkyl; substituted C.sub.1-6 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; or a radical of formula-Alk-Y-Het.sup.1 (a-1), --Alk-NH-CO-Het.sup.Type: GrantFiled: May 8, 1995Date of Patent: May 13, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels, Joseph E. Leenaerts
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Patent number: 5624952Abstract: 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.sub.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: GrantFiled: April 15, 1996Date of Patent: April 29, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, Marcel F. L. De Bruyn, Walter J. J. Janssens
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Patent number: 5616738Abstract: 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: GrantFiled: March 31, 1995Date of Patent: April 1, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5616583Abstract: 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: GrantFiled: April 13, 1995Date of Patent: April 1, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5616587Abstract: The present invention is concerned with physicochemically stable aqueous solutions of risperidone for oral and parenteral administration; processes for preparing such formulations.Type: GrantFiled: April 26, 1995Date of Patent: April 1, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Marc K. J. Fran.cedilla.ois, Willy M. A. C. Dries
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Patent number: 5612346Abstract: A compound which is a pamoate acid addition salt of risperidone, compositions comprising the same and processes for preparing said compound and compositions.Type: GrantFiled: September 22, 1995Date of Patent: March 18, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jean L. Mesens, Jozef Peeters
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Patent number: 5612354Abstract: (1H-azol-1-ylmethyl)substituted quinoline 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: GrantFiled: March 23, 1995Date of Patent: March 18, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymaekers