Abstract: A method of topically treating subjects suffering from acne, hyperkeratotic dermatoses and photo-aging of the skin, by administering to the skin of said subjects an effective amount of the antifungal compound ketoconazole and a retinoid is disclosed. Compositions comprising an inert carrier and as active ingredients the compound ketoconazole and a retinoid are described.
Abstract: Sucrose is mono-acylated in the 6-position by reacting sucrose with a carboxylic acid anhydride such as acetic or benzoic anhydride in a reaction mixture containing a polar aprotic solvent and a catalytic quantity of a 1,3-diacyloxy-1,1,3,3-tetra(hydrocarbyl)distannoxane, for a period of time and at a temperature sufficient to produce a sucrose-6-ester.
Type:
Grant
Filed:
May 2, 1994
Date of Patent:
November 28, 1995
Assignee:
McNeil-PPC, Inc.
Inventors:
George H. Sankey, Nicholas M. Vernon, Robert E. Wingard, Jr.
Abstract: The present invention is concerned with novel imidazo[2, 1-b][3]benzazepines 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, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.3 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.4 represents hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, phenyl or halo; R.sup.5 represents hydrogen, C.sub.1-4 alkyl or halo; L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.
Type:
Grant
Filed:
November 29, 1993
Date of Patent:
November 21, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans E. Janssens, Gaston S. M. Diels, Joseph E. Leenaerts
Abstract: Process for preparing enantiomerically pure imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) prepared in the course of the present process.
Type:
Grant
Filed:
February 15, 1994
Date of Patent:
October 31, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Alfons G. M. De Knaep, Luc J. R. Moens, Eduard J. C. Vreysen
Abstract: The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomefic 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, hydroxy C.sub.1-4 alkyl, formyl, hydroxycarbonyl or hydroxycarbonyl C.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, hydroxy C.sub.1-4 alkyl, formyl or hydroxycarbonyl;R.sup.3 represents hydrogen, C.sub.1-4 alkyl, hydroxy C.sub.1-4 alkyl, phenyl or halo;L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.
Type:
Grant
Filed:
November 29, 1993
Date of Patent:
October 24, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans E. Janssens, Gaston S. M. Diels, Joseph E. Leenaerts, Ludwig P. Cooymans
Abstract: A shampoo that contains ketoconazole, a surfactant, a foaming agent, thickener sufficient to give the final formulation a viscosity in the range of about 4,000 to about 9,000 cps at room temperature (i.e., about 20.degree.-25.degree. C.), preservative, butylated hydroxytoluene or butylated hydroxyanisole in an amount sufficient to retard degradation of the ketoconazole, and acid, base or buffer sufficient to give the final composition a pH in the range of from about 4 to about 10.
Type:
Grant
Filed:
April 7, 1994
Date of Patent:
October 10, 1995
Assignee:
Johnson & Johnson Consumer Products, Inc.
Inventors:
Jue-Chen Liu, Jonas C. T. Wang, Mohammed Yusuf
Abstract: The present invention is concerned with physicochemically stable aqueous solutions of risperidone for oral administration which do not contain sorbitol.
Type:
Grant
Filed:
July 11, 1994
Date of Patent:
September 26, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Marc K. J. Francois, Willy M. A. C. Dries
Abstract: A process for the preparation of partially acylated derivatives of sucrose by the enzyme catalyzed deacylation of sucrose esters, wherein said process comprises treating a sucrose ester selected from the group consisting of sucrose octaacylate, sucrose heptaacylate, and sucrose hexaacylate in an anhydrous organic medium, with an enzyme or combination of enzymes capable of catalyzing the deacylation of said sucrose ester to produce a partially deacylated sucrose derivative having free hydroxyl group(s) in pre-selected position(s), and recovering the resulting partially deacylated sucrose derivative.
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:
October 5, 1993
Date of Patent:
August 15, 1995
Assignee:
Janssen Pharmaceutica N. V.
Inventors:
Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymaekers
Abstract: A compound of formula ##STR1## the racemic mixture, the (S)-form and the acid addition salts thereof, said compound having anti-stroke properties. Pharmaceutical compositions containing this compound as active ingredient and a method of preparing said compound and pharmaceutical compositions.
Type:
Grant
Filed:
August 3, 1993
Date of Patent:
July 18, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Raymond A. Stokbroekx, Gilbert A. J. Grauwels
Abstract: A method for treating skin disorders in warm-blooded animals, said method comprising administering to said warm-blooded animals an effective amount 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:
April 26, 1994
Date of Patent:
May 30, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Jean P. F. Van Wauwe, Alfons H. M. Raeymaekers
Abstract: The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.
Type:
Grant
Filed:
May 12, 1994
Date of Patent:
April 18, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Marcel A. C. Janssen, Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Frans M. A. Van den Keybus, Karin J. M. M. Nuyens, Paul A. J. Janssen
Abstract: A method of highlighting intagliations in white or colored coated tablets by spraying onto said tablets a suspension comprising a filling material having a different color, a waxy material and a solvent, and removing the solvent and the excess of filling material and waxy material.
Type:
Grant
Filed:
July 30, 1993
Date of Patent:
April 11, 1995
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Paul M. V. Gilis, Valentin F. V. De Conde
Abstract: A reduced calorie fruit spread comprising the gelled product of:a. water;b. fruit or fruit flavoring;c. one or more high intensity sweeteners selected from the group consisting of aspartame; saccharin; acesulfame-K; mixtures thereof; and mixtures of aspartame, saccharin, or acesulfame-K with sucralose;d. low methoxy pectin or carrageenan;e. carboxymethylcellulose;f. guar gum; andg. locust bean gum.
Type:
Grant
Filed:
October 21, 1993
Date of Patent:
March 14, 1995
Assignee:
McNeil-PPC, Inc.
Inventors:
Robert N. Antenucci, Thomas R. Davis, Francois Y. Maniere, Susan E. Sharp
Abstract: Synergistic antifungal compositions containing tebuconazole and propiconazole 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 tebuconazole and propiconazole. Method of protecting wood, wood-products and biodegradable materials from fungal attack and destruction.
Abstract: Method of treating addiction to alcohol and symptoms related to withdrawal of said alcohol comprising the administration of certain 4-[bis(halophenyl)methylene]-1-piperidinyl derivatives.
Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
Type:
Grant
Filed:
November 4, 1991
Date of Patent:
January 3, 1995
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
Abstract: The present invention relates to a new pharmaceutical composition for parenteral and local administration comprising an aqueous solution of erythropoietin and a .beta.- or .gamma.-cyclodextrin hydroxyalkyl derivative. The invention also relates to novel lyophilized or spray-dried erythropoietin compositions comprising a .beta.- or .gamma.-cyclodextrin hydroxyalkyl derivative, to processes for preparing such aqueous, lyophilized or spray-dried compositions and to a method for simultaneously stabilizing erythropoietin in an aqueous solution and preventing it from being adsorbed to surfaces.
Type:
Grant
Filed:
June 30, 1992
Date of Patent:
December 27, 1994
Inventors:
Frank J. Konings, Marcus J. M. Noppe, Jean L. Mesens
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:
March 6, 1990
Date of Patent:
December 20, 1994
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Georges H. P. Van Daele, Frans M. A. Van den Keybus