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-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: 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4-or 3-pyridinyl, or N-oxides thereof, or phenyl or substituted phenyl.
Type:
Grant
Filed:
August 7, 1990
Date of Patent:
April 23, 1991
Assignee:
Sterling Drug Inc.
Inventors:
George Y. Lesher, deceased, Edward R. Bacon, Baldev Singh, Gee-Hong Kuo
Abstract: Compounds of the formulas: ##STR1## wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed. Also disclosed are novel intermediates, N-halo-alkyl-4-(isoxazol-5-yl)alkoxybenzamides, also useful as antiviral agents.
Abstract: N-[(alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.
Abstract: Onset-hastened and enhanced antipyretic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage onset-hastening/enhancing antipyretically effective amount of the S(+) ibuprofen enantiomer, said enantiomer being substantially free of its R(-) ibuprofen antipode.
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: A vented package for a plurality of dispensers for flowable products. The vented package includes a base member having a fluid passage therein and an overcap having an aperture therein to allow venting of product vapors which escape from the dispensers. The dispenser includes a container body, a mounting member fitted on the container body and a dispensing head such as an applicator head movably mounted on the mounting member. The mounting member includes an axially extending closure member with a pin member thereon. The dispensing head includes an aperture and a skirted chamber beneath the aperture, the skirted chamber including slits for controlling flow of material into the skirted chamber from the container body. The dispensing head is movable from an open position to a closed position wherein the closure member fits within the skirted chamber and the pin member fits within the aperture.
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: An aqueous-based formulation for coating aspirin granules to provide granules that may be compressed into tablets and that show approximately zero-order release kinetics for release rates of 5 to 15 mg/hour over a period extending five to eight hours is provided. The coating formulation preferably consists of an acrylate/methacrylate copolymer, hydroxypropylmethylcellulose, sodium chloride and talc. A film-coated tablet comprised of the coated granules, filler granules, excipients, binders and disintegrants is also provided, as are processes for preparing the tablets and granules and methods for their use in the treatment of vascular occlusive diseases.
Abstract: A wiper for one step polishing and protecting of a hard surface such as wood and plastic surfaces, e.g. furniture, comprises a nonwoven substrate impregnated with a liquid polish composition comprising by weight of the composition: (a) from about 0.7 to about 7% of an organic polysiloxane having a viscosity of from about 50 to about 100 centistokes at 25.degree. C.; (b) from about 0.1 to about 3.5 of an organic polysiloxane having a viscosity of about 1000 to about 25,000 centistokes at 25.degree. C.; (c) from 0 to about 1.4% of an aminofunctional silicone fluid; (d) from about 0.1 to about 1% of a wax; (e) from about 1 to about 15% of a hydrocarbon solvent having an initial boiling point above about 98.degree. C. and an end boiling point below about 200.degree. C.; (f) from about 0.05 to about 2% of a nonionic emulsifier; and (g) the remainder to 100% water; wherein the ratio of (a) to (b) is from about 2 to 1 to about 5 to 1, the substrate has a basis weight of from about 30 to about 90 g/sq.yd.
Abstract: Novel 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4- or 3-pyridinyl, or phenyl or substituted phenyl.
Type:
Grant
Filed:
February 28, 1990
Date of Patent:
October 16, 1990
Assignee:
Sterling Drug Inc.
Inventors:
George Y. Lesher, Edward R. Bacon, Baldev Singh, Gee-Hong Kuo
Abstract: N-[(alkylamino)alkyl]-4,5-diaryl-1H-imidazole-1-acetamides useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of a diaryl imidazole-1-acetic acid with an appropriate diamine.
Abstract: Compounds of the formula ##STR1## where R is hydrogen, hydroxy, amino or lwer-alkyl; R.sup.1 is lower-alkyl, lower-alkenyl, cycloalkyl, pyridinyl, phenyl or substituted phenyl; R.sup.2 is hydrogen, amino or hydroxy; R.sup.6 is hydrogen or fluoro; and R.sup.7 is phenyl, pyridinyl or selected other heterocycles, have antiviral acitivity against herpes virus.The compounds are prepared from the corresponding carboxylic acids or ester, or by a tin-coupling reaction on the corresponding 7-halo compounds.