Abstract: Antiglaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-[1,2,3-de]-1,4-benzoxazines as the active component thereof and the method of use thereof in the treatment of glaucoma.
Abstract: Antiglaucoma compositions containing 3-R.sub.3 -4-arylcarbonyl-1-[(4-morpholinyl)-lower-alkyl]-1H-indoles and a method of use thereof in the treatment of glaucoma.
Abstract: 2-R.sub.2 -R.sub.4 -substituted-3-R.sub.3 -CO-1-[(C-attached-N-herteryl)-(Alk).sub.n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.
Type:
Grant
Filed:
February 26, 1990
Date of Patent:
November 26, 1991
Assignee:
Sterling Drug Inc.
Inventors:
Thomas E. D'Ambra, Edward R. Bacon, Malcolm R. Bell, Philip M. Carabateas, Michael A. Eissenstat, Virendra Kumar, John P. Mallamo, Susan J. Ward
Abstract: 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines , useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.
Abstract: 2-(4,5-Dihydro-1H-imidazol-2-yl)-2,3-dihydro-1H-indoles, 2-(4,5-dihydro-1H-imidazol-2-yl)-1,2,3,4-tetrahydroquinolines and 2-(4,5-dihydro-1H-imidazol-2-yl)-1H-indoles, useful as antidepressant agents, are prepared by reacting a respective lower-alkyl 2,3-dihydro-1H-indole-2-carboxylate 1,2,3,4-tetrahydroquinoline-2-carboxylate or 1H-indole-2-carboxylate derivative with ethylenediamine or an N-lower-alkylethylenediamine in the presence of a Lewis-type acid.
Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.
Abstract: Antiglaucoma compositions containing 3-aryl-carbonyl-1-aminoalkyl-1H-indoles, as the active component thereof, and a method of use thereof in the treatment of glaucoma.
Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindoe with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.
Abstract: Antiglaucoma compositions containing 3-aryl-carbonyl-1-aminoalkyl-1H-indoles, as the active component thereof, and a method of use thereof in the treatment of glaucoma.
Abstract: Rodenticidal compositions comprising an anticoagulant type rodenticide in combination with a fluorosurfactant of the amphoteric, anionic or cationic type, optionally admixed with a cereal grain bait, and a method of killing rodents by oral administration of such compositions.
Abstract: 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines , useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.
Abstract: A connector for attachment of a plunger to a rubber piston in hypodermic syringe cartridge ampoules comprises a pin having a shank portion with a contiguous screw-threaded post portion and a ratchet head portion sized to rotatably fit within a cavity in said piston which thus prevents overtightening the plunger to the piston thereby obviating jamming of the piston in the bore of the cartridge.
Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.
Abstract: 4-Arylcarbonyl-1-[(4-morpholinyl)-lower-alkyl]-1H-indoles, useful as analgesic agents, are prepared by reaction of a 3-arylcarbonyl-2-methylnitrobenzene with DMF dimethyl acetal; reductive cyclization of the product with hydrogen over a catalyst; and N-alkylation of the resulting 4-arylcarbonylindole with an appropriate 4-(halo-lower-alkyl)morpholine in the presence of a strong base.
Abstract: 4-Arylcarbonyl-1-[(4-morpholinyl)-lower-alkyl]-1H-indoles, useful as analgesic agents, are prepared by reaction of a 3-arylcarbonyl-2-methylnitrobenzene with DMF dimethyl acetal; reductive cyclization of the product with hydrogen over a catalyst; and N-alkylation of the resulting 4-arylcarbonylindole with an appropriate 4-(halo-lower-alkyl)morpholine in the presence of a strong base.
Abstract: The invention comprises a syringe for extrusion of a semi-plastic mass, or a mass having a paste-like consistency. In a preferred embodiment, the syringe is so-designed to permit mixing of two components of a plasticizable mixture within the syringe barrel. The bore of the syringe barrel is flared to facilitate extrusion of the plastic mass therefrom. The parts of the syringe ready for use are packaged in a one-piece tray which serves not only for shipping and storing of the syringe, which may be preloaded with one of the components of the plasticizable mixture, together with the associated syringe parts, but which also serves, when opened for use, as a convenient tray for handling the syringe while mixing the two components of the plasticizable mixture prior to extrusion.
Abstract: Stable, isotropic, liquid laundry detergents with good detergency, effective microbicidal and low irritancy properties comprising anionic, nonionic and cationic surfactants and an alkali metal benzoate in an aqueous vehicle.
Abstract: Sustained-release compositions for oral administration comprising medicament-coated nonpareils surrounded by a sustaining coating of at least three admixed polymers afford exceptionally good plasma levels of the medicament.
Type:
Grant
Filed:
May 24, 1985
Date of Patent:
February 21, 1989
Assignee:
Sterling Drug Inc.
Inventors:
Paul J. Harrison, John R. Langridge, Christopher J. Potter
Abstract: Liquid sanitizing and cleaning compositions with diminished skin irritancy comprise a nonionic surfactant and a di-(lower-alkyl)-long-chain-alkylbenzylammonium benzoate or a di-(lower-alkyl)-di-(long-chain-alkyl)-ammonium benzoate, the latter being produced either by ion exchange of the corresponding quaternary ammonium halide with benzoate or by mixing the quaternary ammonium halide with at least about one molar equivalent of an alkali metal benzoate, in water.
Abstract: Composites useful, for example, in dental restorative procedures comprising a mixture of particulate ceramic hydroxylapatite and a polymerizable monomer or mixture of polymerizable monomers wherein said ceramic hydroxylapatite particles, prior to mixing and polymerizing with said polymerizable monomers, are coated first with a siliceous material and then with an organosilane and a process for preparation of the same.