Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula 0010wherein:L is --O--, --S--, --SO-- or --SO.sub.2 --; m and n are each independently 0 or 1; R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.

Abstract: 4-Phenylpiperidines of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy or lower-alkoxy;R.sub.2 is hydrogen, hydroxy, lower-alkanoyl, aroyl, lower-alkoxycarbonyl, lower-alkanoyloxy, lower-alkoxycarbonyl, or CONR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are the same or different lower-alkyl or R.sub.3 and R.sub.4 together represent a lower-alkylene chain;X is methylene or carbonyl;Y is methylene, C.dbd.NOH, hydroxymethylene or carbonyl;or pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of psychoses and other ailments of the central nervous system.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## Y is a bond or lower alkylene; R.sub.2 and R.sub.3 are independently hydrogen, lower-alkyl or halogen;R.sub.4 is ##STR3## R.sub.5 is hydrogen, lower-alkyl or halogen; R.sub.6 is hydrogen, lower-alkyl or halogen;R.sub.7 is hydrogen or lower-alkyl;R.sub.8 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.9 is lower-alkyl;R.sub.10 is lower-alkyl, trifluoromethyl or difluoromethyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.

Abstract: This invention is an antacid composition capable of forming a floating gelatinous mass when contacted with aqueous acid and consisting essentially of, as active ingredients, xanthan gum; an effective acid neutralizing amount of hexitol stabilized aluminum hydroxide and a gas producing material capable of producing a non-toxic gas when contacted with aqueous acid which may be formulated as a solid, powder, tablet or suspension.

Abstract: Compounds of formula ##STR1## wherein; R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro;Z is NR.sub.5 or CR.sub.6 R.sub.7 ;R.sub.5 is hydrogen, aryl, arylthio, arylsulfonyl, lower-alkyl, cycloalkyl, heterocycloalkyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, dilower-alkylamino-lower-alkyl, lower-alkoxy, hydroxy or NR.sub.8 R.sub.9 ;R.sub.6 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro or lower-alkylsulfonyl;R.sub.7 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro, aryl, or lower-alkylsulfonyl;R.sub.8 is hydrogen, lower-alkyl, aryl, heterocycloalkyl, carbamyl, alkanoyl, aroyl, hydroxy-lower-alkyl; andR.sub.9 is hydrogen, lower-alkyl or lower-alkanoyl or pharmaceutically acceptable acid addition salts thereof are useful as anticancer agents.

Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 is alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, alkoxyalkyl or hydroxyalkoxy;Y is alkylene of 3 to 9 carbon atoms,R.sub.2 and R.sub.3 independently are hydrogen, alkyl, alkoxy, halo, trifluoromethyl and nitro;R.sub.4 is alkoxy, hydroxy, halomethyl, dihalomethyl, trihalomethyl, cycloalkyl, alkoxycarbonyl, hydroxyalkyl, alkoxyalkyl, alkanecarbonyloxyalkyl, cyano, 2,2,2-trifluoroethyl, (4-methylphenyl)sulfonyloxymethyl, N.dbd.Q or CON.dbd.Q, where N.dbd.Q is amino, alkylamino or dialkylamino; or pharmaceutically acceptable acid-addition salts thereof are useful as antiviral agents.

Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.

Abstract: Low solubility drug coated bead compositions, capsules filled therewith and method of preparation thereof, especially wherein the low solubility drug is an antiandrogenic steroid and most especially wherein the antiandrogenic steroid is (5.alpha.,17.alpha.)-1'-(methylsulfonyl)- 1'-H-pregn-20-yno[3,2-c]pyrazol-17-ol, are disclosed.

Abstract: A lactose-hydrolyzed fluid milk comprising fluid milk, the normal lactose content of which has been reduced by at least about 70% by lactase hydrolysis, having incorporated therein from about 0.01 to about 0.15% by weight of potassium chloride, a process for its preparation and a method of suppressing perceived sweetness of lactose-hydrolyzed milk by incorporating therein potassium chloride.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Y where Y is hydroxy, chloro, lower-alkylamino or dilower-alkylaminoR.sub.3 and R.sub.4 are each independently hydrogen or fluoro;R.sub.5 is hydrogen, lower-alkyl or(a) phenyl, 2-pyridyl, 4-pyridyl, 1-naphthyl or such groups substituted with one or more, the same or different, lower-alkyl, fluoro, hydroxy, or lower-alkoxy;(b) cycloalkyl or cycloalkyl substituted with amino, lower-alkylamino, dilower-alkylamino, formamido, acetamido, lower-alkyl, hydroxy, lower-alkoxy, trifluoromethyl, carboxy, lower-alkoxycarbonyl or halo, or cycloalkyl having a phenyl ring fused thereto;(c) A saturated heterocyclic 5- or 6-membered ring containing oxygen and/or nitrogen or such ring substituted with lower-alkyl; or(d) (CH.sub.2).sub.

Abstract: Soft capsules coated with an enteric coating comprising a 1:1 copolymer of methacrylic acid and methyl or ethyl acrylate or methyl or ethyl methacrylate and a plasticizer without need for a subcoating and optionally additionally coated with a protective coating comprising hydroxypropyl methylcellulose or hydroxypropyl cellulose or a mixture thereof and a plasticizer and method of preparation thereof are disclosed.

Abstract: Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro; andAr is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.

Abstract: A solid effervescent antacid formulation comprising as primary ingredients from about 35 to about 53 percent by weight of calcium carbonate, from about 0 to about 14 percent by weight of magnesium carbonate, from about 3.5 to about 7 percent by weight of a bicarbonate salt, from about 3.5 to about 7 percent by weight of malic acid and from about 21 to about 35 percent by weight of a bulking agent.

Abstract: 2-R.sub.2 -R.sub.4 -substitutea-3-R.sub.3 -CO-1-[(C-attached-N-heteryl)(Alk).sub.n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.

Abstract: 4-R.sup.4 -R.sup.5 -Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.

Abstract: Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclylcarboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.

Abstract: Compounds of the formula ##STR1## wherein Alk is lower-alkylene;R.sub.1 is hydrogen, lower-alkyl, Ar or ArCOO;R.sub.2 is hydrogen or lower-alkyl;R.sub.3 and R.sub.4 are the same or different hydrogen, fluoro, chloro, bromo, hydroxy, lower-alkoxy, lower-alkyl, or trifluoromethyl;Ar is phenyl, naphthyl, anthryl, 2-phenylethenyl or a 5- or 6-membered monocyclic or 9- or 10-membered bicyclic fused aromatic heterocyclic ring containing carbon and one or two heteroatoms independently selected from oxygen, nitrogen and sulfur, or such carbocyclic or heterocyclic rings substituted with from 1 to about 3 of lower-alkoxy, lower-alkyl, lower-alkylthio, lower-alkyl sulfinyl, lower-alkyl sulfonyl, hydroxy, cyano, amino, lower-alkylamino, dilower-alkylamino or halo;or pharmaceutically acceptable acid addition salts thereof are useful as analgesics and in the treatment of glaucoma.

Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl or phenyl-lower-alkyl;R.sup.2 and R.sup.4 are the same or different lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;m is two or three;n is an integer from zero to three; andR.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, allyl, or propargyl;or a pharmaceutically acceptable acid-addition salt thereof.

Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.

Abstract: Extrudable elastic oral pharmaceutical gel compositions, especially containing aetaminophen as the therapeutically active agent, and manually operable metered dose dispensers containing them and method of making and method of use thereof are disclosed.