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
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
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
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
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
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.
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.
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
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
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
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
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.
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
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
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
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
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
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