Abstract: There is provided, a novel class of compounds exhibiting antibacterial activity, said compounds having the formula: ##EQU1## wherein X and Y each represent a member which may be the same or different selected from the group consisting of H and Cl with the priviso that X and Y cannot represent H simultaneously; R.sub.1 and R.sub.2 each represent a member which may be the same or different selected from the group consisting of an n- or branched alkyl group of from 1 to 20 carbon atoms, an aryl group (phenyl, naphthyl, etc.) and a ##EQU2## (CH.sub.2).sub.n group, wherein n represents an integer of from 2 - 5; and Z represents a member selected from the group consisting of an --OR.sub.3 group, a a ##EQU3## wherein R.sub.4 and R.sub.5 each represent a member which may be the same or different selected from the group consisting of H and an alkyl group of from 1 - 3 carbon atoms, wherein R.sub.6 and R.sub.7 each represent a member which may be the same or different selected from the group consisting of R.sub.1, R.

Abstract: Optically and therapeutically active compounds of the formula: ##SPC1##Wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C.sub.1 -C.sub.5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##EQU1## group, wherein R is as defined above and R.sub.3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are prepared using optically active m-hydroxy-.alpha.-[(methylamino)-methyl]benzyl alcohol (phenylephrine).The compounds prepared by the process of this invention find therapeutic applicaton to warm-blooded animals (e.g., humans) in the management of asthma, nasal congestion and as decongestants, vasoconstrictors, mydriatic agents, and anti-glaucomatous agents in the practice of opthalmology.

Abstract: There is provided, novel pro-drug forms of pyridinium aldoxime type cholinesterase reactivators, namely, dihydropyridinium aldoximes, having the formula: ##SPC1##Wherein R represents a member selected from the group consisting of an alkyl (C.sub.1 -C.sub.4) group, a ##SPC2##Group, a ##SPC3##Group, ##SPC4##Group, and a ##SPC5##Wherein Z represents a member selected from the group consisting of a --CH.sub.2 --CH.sub.2 -- group, a --CH.sub.2 --O--CH.sub.2 -- group, a --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- group, and a --CH.sub.2 O--CH.sub.2 --CH.sub.2 --O--CH.sub.2 -- group; wherein R.sub.1 represents a member selected from the group consisting of a hydrogen atom, a methyl group, an acyl group and a ##EQU1## group; and wherein X.sup.- represents an anion derived from a pharmaceutically acceptable acid addition salt.These compounds are useful in reactivating cholinesterase, inhibited following exposure to and/or ingestion of conventional anti-cholinesterase agents, especially in the brain.

Abstract: Therapeutic levels of L-DOPA are achieved by orally administering a pharmaceutical effervescent-enteric coated tablet comprising:A. a member selected from the group consisting of L-DOPA or a derivative thereof capable of enzymatically cleaving and reverting to L-DOPA in vivo,B. a non-toxic pharmaceutically acceptable inert diluent,C. a non-toxic pharmaceutically acceptable carbon dioxide releasing agent,D. a non-toxic pharmaceutically acceptable effervescing agent, andE. a non-toxic pharmaceutically acceptable enteric coating.This composition is extremely useful in the treatment of Parkinsonism. When administered to warm-blooded animals (e.g., humans), superior therapeutic blood levels of L-DOPA are observed over that normally observed with conventional enteric coated formulations.

Abstract: The intraocular pressure of a warm-blooded animal is substantially reduced by administering topically to the eye thereof, a therapeutically effective amount of a compound of the formula: ##SPC1##Or a pharmaceutically acceptable acid addition salt thereof.

Abstract: Transient, pro-drug forms of phenylbutazone and oxyphenbutazone, which are 1,2-diphenyl-4-butyl-5-oxy-4-pyrazolin-3-one derivatives, are disclosed.These compounds exhibit anti-inflammatory activity in warm-blooded animals. Upon administration to warm-blooded animals, these compounds pass through the gastrointestinal tract and "cleave" in the bloodstream, thus releasing phenylbutazone or oxyphenbutazone in an anti-inflammatory effective amount at their therapeutic site or sites of activity.

Abstract: Alkaline earth metal salts of salicylamide are administered in solid oral dosage forms with substantially improved analgesic, anti-inflammatory, antipyretic and sedative results as compared with salicylamide. Highest blood levels are obtained by administering enteric-coated salicylamide salt dosage forms.

Abstract: There is provided, novel 3-chloro-tetrahydro-1,3-oxazine or oxazolidine compounds, exhibiting antibacterial activity and being of low chlorine potential of the formula: ##SPC1##Wherein each of R.sub.1 and R.sub.2, which may be the same or different, represent an alkyl group of from 1 to 20 carbon atoms (C.sub.1 -C.sub.5 being preferred); wherein each of R.sub.5 and R.sub.6, which may be the same or different, represent a hydrogen atom or an alkyl group of from 1 to 20 carbon atoms (C.sub.1 -C.sub.5 being preferred); wherein l represents an integer of 1 or 2 and wherein each of R.sub.3 and R.sub.4, which may be the same or different, represent an alkyl group of from 1 to 20 carbon atoms (C.sub.1 -C.sub.5 being preferred), a --(CH.sub.2).sub.n X group, wherein n represents an integer of from 1 to 20 and wherein X represents a dimethylamino group, a diethylamino group, a trimethylammonium group, a triethylammonium group, a dimethylammonium group, a diethylammonium group, a --COOR.sub.7 group, a --OOCR.sub.

Abstract: Alkali and alkaline earth metal salts of salicylamide are administered in solid oral dosage forms with substantially improved analgesic, anti-inflammatory, antipyretic and sedative results as compared with salicylamide. Highest blood levels are obtained by administering enteric-coated salicylamide salt dosage forms.

Abstract: There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: ##SPC1##Wherein R represents a member selected from the group consisting of a hydrogen atom, a --COCH.sub.3 group, a --COC.sub.2 H.sub.5 group, a --COOC.sub.2 H.sub.5 group, and a --CO--C(CH.sub.3).sub.3 group; wherein R.sub.1 represents a member selected from the group consisting of a hydroxyl group, a --OM group (wherein M represents an alkali metal or an ammonium ion), a --OCH.sub.2 --C.sub.6 H.sub.5 group, a --OCH.sub.3 group, a --OC.sub.2 H.sub.5 group, and --NH--CH(R.sub.3)COOH group, wherein R.sub.3 represents the residue of any naturally occurring amino acid; and wherein R.sub.2 represents a member selected from the group consisting of a hydrogen atom, a formyl group, a --CO--C.sub.6 H.sub.5 group, a --CO--pyridyl group, a --CO(R.sub.5)--CH=CH(R.sub.4) group, and a NH.sub.2 --CH(R.sub.6)--CO-- group, wherein R.sub.4 represents a methyl group and wherein R.sub.

Abstract: There is provided, novel 3-chloro-tetrahydro 1,3-oxazine or oxazolidine compounds, exhibiting antibacterial activity and being of low chlorine potential of the formula: ##EQU1## WHEREIN EACH OF R.sub.1 and R.sub.2, which may be the same or different, represent an alkyl group of from 1 to 20 carbon atoms (C.sub.1 -C.sub.5 being preferred); wherein each of R.sub.5 and R.sub.6, which may be the same or different, represent a hydrogen atom or an alkyl group of from 1 to 20 carbon atoms (C.sub.1 -C.sub.5 being preferred); wherein l represents an integer of 1 or 2 and wherein each of R.sub.3 and R.sub.4, which may be the same or different, represent an alkyl group of from 1 to 20 carbon atoms (C.sub.1 -C.sub.5 being preferred), a --(CH.sub.2).sub.n X group, wherein n represents an integer of from 1 to 20 and wherein X represents a dimethylamino group, a diethylamino group, a trimethylammonium group, a triethylammonium group, a dimethylammonium group, a diethylammonium group, a --COOR.sub.7 group, a --OOCR.sub.

Abstract: There is provided novel and useful pro-drug forms of theophylline having the formula: ##SPC1##Wherein R represents a member selected from the group consisting of a straight or branched C.sub.4 -C.sub.20 alkyl group, a straight or branched C.sub.4 -C.sub.20 alkenyl group, a substituted phenyl group of a substituted or unsubstituted naphthyl group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom (Cl, Br, I), and a substituted or unsubstituted heteroaromatic group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom (Cl, Br, I), and wherein A represents a member selected from the group consisting of a --CO-- group, a --CO--(CH.sub.2).sub.

Abstract: Antibacterially effective 3-chloro-2-oxazolidinones are prepared by chlorination of an appropriate 2-oxazolidinone either with elemental chlorine in an aqueous medium or with a mono-, di- or trichloroisocyanuric acid (cyanuric chloride) in an inert organic solvent. The 2-oxazolidinones are, in turn, prepared by reaction of an appropriate ethanolamine either with a di-lower-alkyl carbonate in the presence of a strong base or with urea at an elevated temperature.