Patents Represented by Attorney Charles J. Metz
  • Patent number: 5371079
    Abstract: The compounds are of the class of tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing antiretroviral, especially anti-HIV-1, activity. An illustrative compound is (+)-S-4,5,6,7-tetrahydro-9-chloro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4 ,5,1-jk][1,4]benzodiazepine-2(1H)-thione. These compounds are represented by the formula: ##STR1## The application also discloses compositions containing these compounds as active ingredients and methods of treating subjects suffering from retroviral infections by administering said compounds.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: December 6, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael J. Kukla, Henry J. Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul A. J. Janssen
  • Patent number: 5369084
    Abstract: Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: November 29, 1994
    Assignee: Janssen Pharmaceutical N.V.
    Inventors: Hans-Rudolf Waespe, Guy R. E. Van Lommen, Victor K. Sipido
  • Patent number: 5354902
    Abstract: Stabilized aqueous solutions containing sorbic acid or salt thereof in an antimicrobial proportion, and further containing from 0.1, and preferably from 0.2, to about 5 ppm of manganous ion, said manganous ion being in an amount sufficient to inhibit oxidation of said sorbic acid or salt thereof to oxidative products such as acetaldehyde.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: October 11, 1994
    Assignee: McNeil-PPC, Inc.
    Inventors: Mel Merciadez, Kas Mohammed, Francois Y. Maniere
  • Patent number: 5342957
    Abstract: A method for treating skin disorders in warm-blooded animals, said method comprising administering to said warm-blooded animals an effective mount of an appropriately substituted benzimidazole or benzotriazole which suppresses the metabolism of retinoids. Compositions comprising said compounds and an effective amount of a retinoid.
    Type: Grant
    Filed: August 10, 1992
    Date of Patent: August 30, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean P. F. Van Wauwe, Alfons H. M. Raeymaekers
  • Patent number: 5321028
    Abstract: 3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.
    Type: Grant
    Filed: December 3, 1992
    Date of Patent: June 14, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Vandenberk, Ludo E. J. Kennis, Albertus H. M. T. Van Heertum
  • Patent number: 5311223
    Abstract: A ophthalmic lens comprising a polymer composition composed of the reaction product of a hydrophilic monomer and an acyclic monomer is disclosed. The preferred hydrophilic monomer is hydroxyethyl methacrylamide (HMA), and the preferred acyclic monomer is hydroxyoctyl methacrylate (HOMA). The monomeric components can be polymerized in a polystyrene mold to make contact lenses, and when swollen with water, are suitable for use as soft hydrogel contact lenses.The preferred compositions also include a zwitterionic monomer, such as a sulfobetaine, and a crosslinking agent, such as ethylene glycol dimethacrylate (EGDMA).Hydrogel contact lenses made from these polymers exhibit high water content and mechanical strength, and are compatible with polystyrene molds.
    Type: Grant
    Filed: June 7, 1993
    Date of Patent: May 10, 1994
    Assignee: Johnson & Johnson Vision Products, Inc.
    Inventor: Douglas G. Vanderlaan
  • Patent number: 5298611
    Abstract: A process for producing substantially pure sucralose pentaester from a mixture of 6-O-acyl-4,1' ,6' -trichloro-4,1',6'-trideoxygalactosucrose in a reaction medium comprising a tertiary amide, wherein said process comprises the steps of:(a) recovering the 6-O-acyl-4,1' ,6' -trichloro-4,1' ,6' -trideoxygalactosucrose from said mixture;(b) peracylating the 6-O-acyl-4,1' ,6' -trichloro-4,1' ,6' -trideoxygalactosucrose product of step (a) to produce thereby 4,1',6' -trichloro-4,1' ,6' -trideoxygalactosucrose pentaester; and(c) crystallizing the 4,1',6' -trichloro-4,1' ,6' -trideoxygalactosucrose pentaester product of step (b) to produce substantially pure 4,1',6' -trichloro-4,1' ,6' -trideoxygalactosucrose pentaester.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: March 29, 1994
    Assignee: McNeil-PPC, Inc.
    Inventors: Juan L. Navia, Robert E. Walkup, Nicholas M. Vernon, Robert E. Wingard, Jr.
  • Patent number: 5292738
    Abstract: Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.
    Type: Grant
    Filed: August 13, 1992
    Date of Patent: March 8, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Joannes J. M. Willems, Marcel G. M. Luyckx
  • Patent number: 5292350
    Abstract: An improved method is disclosed of imparting a tint or color to a soft, hydrogel contact lens by uniformly dispersing a dye throughout the lens. The dye is composed of a water-soluble compound essentially free of ethylenic unsaturation. A homogeneous solution of the dye in a hydrophilic monomer is prepared, the solution is subjected to polymerization conditions to yield a hydrophilic polymer from which the lens is formed, and the dye dispersed within the polymer is bonded to the polymer by contact with aqueous base prior to final hydration.The finished lens does not require soaking in an aqueous solution of the dye to impart the desired tint or color to the lens. Additionally, the dye uniformly dispersed throughout the lens according to the improved method does not leach out of the lens or migrate within the lens.
    Type: Grant
    Filed: April 24, 1992
    Date of Patent: March 8, 1994
    Assignee: Vistakon, Inc.
    Inventors: Frank F. Molock, James D. Ford, John C. Heaton, Edmund C. Rastrelli, Gregory A. Hill
  • Patent number: 5284854
    Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: February 8, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo E. J. Kennis, Jan Vandenberk, Jozef M. Boey
  • Patent number: 5278165
    Abstract: Oxazolyl derivatives of formula (I) ##STR1## wherein --A.sup.1 .dbd.A.sup.2 --A.sup.3 .dbd.A.sup.4 -- represents a bivalent radical having the formula--CH.dbd.CH--CH.dbd.CH-- (a-1),--N.dbd.CH--CH.dbd.CH-- (a-2),--CH.dbd.N--CH.dbd.CH-- (a-3),--CH.dbd.CH--N.dbd.CH-- (a-4),--CH.dbd.CH--CH.dbd.N-- (a-5),--N.dbd.CH--N.dbd.CH-- (a-6)or--CH.dbd.N--CH.dbd.N-- (a-7);R represents hydrogen or C.sub.1-4 alkyl; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or hydroxyC.sub.1-6 alkyl; m represents 1 or 2; D represents C.sub.1-4 alkanediyl; B represents NR.sup.2, CH.sub.2, O, S, SO or SO.sub.2 wherein R.sup.2 is hydrogen or C.sub.1-4 alkyl; n represents 0, 1 or 2; L represents hydrogen; C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; C.sub.3-6 alkenyl optionally substituted with aryl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; arylcarbonyl; arylC.sub.1-6 alkyloxycarbonyl; or a radical of formula --Alk--R.sup.3 (b-1); --Alk--Y--R.sup.4 (b-2); --Alk--Z.sup.1 --C(.dbd.X)--Z.sup.2 --R.sup.5 (b-3); or --CH.sub.2 --CHOH--CH.sub.
    Type: Grant
    Filed: March 23, 1993
    Date of Patent: January 11, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Francois M. Sommen, Ann C. J. Dierckx, Ludwig P. Cooymans
  • Patent number: 5272150
    Abstract: Hydroxyalkylfuranyl derivatives, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof having antiallergic properties, compositions containing the same and methods of treating warm-blooded animals suffering from allergic diseases.
    Type: Grant
    Filed: February 26, 1992
    Date of Patent: December 21, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels, Joseph E. Leenaerts
  • Patent number: 5270071
    Abstract: A reduced calorie fruit spread comprising the gelled product of:a. water;b: fruit or fruit flavoring;c. sucralose high intensity sweetener;d. low methoxy pectin or carrageenan;e. carboxymethylcellulose;f. guar gum; andg. locust bean gum.
    Type: Grant
    Filed: June 18, 1992
    Date of Patent: December 14, 1993
    Assignee: McNeil-PPC, Inc.
    Inventors: Susan E. Sharp, Robert N. Antenucci
  • Patent number: 5270464
    Abstract: Novel tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing anti-HIV-1 activity, compositions containing these compounds as active ingredients, and methods of treating subjects suffering from HIV-1 infection by administering these compounds.
    Type: Grant
    Filed: April 5, 1993
    Date of Patent: December 14, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael J. Kukla, Henry J. Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul A. J. Janssen
  • Patent number: 5268380
    Abstract: (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: Grant
    Filed: November 10, 1992
    Date of Patent: December 7, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymakers
  • Patent number: 5262418
    Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula--CH.sub.2 --CH.sub.2 -- (a-1),--CH.sub.2 --CH.sub.2 --CH.sub.2 -- (a-2), or--CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -- (a-3),wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula--Alk--R.sup.4 (b-1),--Alk--X--R.sup.5 (b-2),--Alk--Y--C(.dbd.O)--R.sup.7 (b-3), or--Alk--Y--C(.dbd.O)--NR.sup.9 R.sup.10 (b-4),the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties.
    Type: Grant
    Filed: November 17, 1992
    Date of Patent: November 16, 1993
    Assignee: Tanssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
  • Patent number: 5258380
    Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: November 2, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels
  • Patent number: 5256681
    Abstract: [5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates of formula (I) wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, halo, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 is C.sub.1-4 alkyl; and X is O, S, SO, SO.sub.2 or NR.sup.3, said R.sup.3 being hydrogen, C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl. The compounds of formula (I) have anthelminthic properties. Compositions containing said compounds as active ingredient, a method of combating helminths, and a process for preparing said compounds and compositions.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: October 26, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Gustaaf M. Boeckx
  • Patent number: 5256659
    Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and antihistaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering from sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.
    Type: Grant
    Filed: June 19, 1992
    Date of Patent: October 26, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo E. J. Kennis, Jan Vandenberk, Jozef M. Boey
  • Patent number: 5254556
    Abstract: The invention relates to C.sub.2-20 alkanoic acid esters of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6, 7,8,9-tetrahydro-9-hydroxy-2 -methyl-4H-pyrido[1,2-a]pyrimidin-4-one, pharmaceutically acceptable acid addition salts thereof, and enantiomeric forms thereof, which are useful in the treatment of warm-blooded animals suffering from psychotic diseases.
    Type: Grant
    Filed: August 19, 1992
    Date of Patent: October 19, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Cornelus G. M. Janssen, Alfonsus G. Knaeps, Ludo E. J. Kennis, Jan Vandenberk