Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein N represents a tertiary aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.

Abstract: A method and drug form are provided for increasing the oral absorption of glycosidic and related antibiotics such as macrolide, aminoglycoside, lincomycin and anthracycline antibiotics and related chemical species by the oral administration of said glycosidic and related antibiotics in a suitable pharmaceutically accepted excipient to which has been added a hydroxyaryl or hydroxyaralkyl acid or salt thereof. The hydroxyaryl or hydroxyaralkyl acid or salt thereof is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of glycosidic and related antibiotic.

Abstract: Novel prodrug forms of known non-steroidal anti-inflammatory agents are disclosed, said prodrugs having the structural formula ##STR1##

Abstract: Novel, transient inotropic prodrug forms of the N-(2-phenylethyl)-.omega.-phenylalkylamines, notably of dobutamine, have (i) the structural formula (I): ##STR1## with the proviso that at least one R.sup.1, R.sup.2 or OR.sup.1, when R.sup.7 and/or R.sup.10 is OR.sup.1, must be R.sup.3 COXCH(R.sup.4)-- or R.sup.3 COXCH(R.sup.4)O--, respectively.

Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.

Abstract: The invention provides novel aldehyde adducts of triamterene having improved solubility and bioavailability as compared to triamterene. Pharmaceutical compositions containing the novel adducts and having diuretic activity are also described.

Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.

Abstract: Compounds of the formula: ##STR1## useful in treating dermal inflammation in warm-blooded animals are provided.

Abstract: Transient, orally active thiazolidine type prodrug forms of conventional, natural and synthetic ketosteroidal sex hormones, e.g., of progesterone, testosterone, and the like, are disclosed. The subject compounds can be prepared by known methods, for example, by reacting the corresponding 3-keto or 3,20-diketo steroids with a thiazolidine-forming reagent such as an L-cysteine alkyl ester.

Abstract: Novel pyridiniumaldoximes having micellar characteristics are useful in the deactivation of organophosphates. Fast and effective detoxification of areas and equipment contaminated with organophosphate pesticides and insecticides results from use of the reagents.

Abstract: Novel 5,5-diphenylhydantoins useful as anticonvulsants, antiepileptics and antiarrhythmics have the structural formula: ##STR1## wherein each R is hydrogen or --CH(R.sub.1)--X--P(O)(OH).sub.2, R.sub.1 is hydrogen or C.sub.1 -C.sub.7 straight or branched chain alkyl, and X is O or S, with the proviso that both R's cannot simultaneously be hydrogen.

Abstract: Gastric ulcer-prone patients are treated by introducing into the stomach thereof an effective amount of a non-toxic, non-absorbable active agent, preferably an anion exchange resin having strong hydrophobic binding tendencies (e.g., a styrene-divinylbenzene copolymer bearing quaternary ammonium functional groups), or a hydrophobic, nonionic polymeric adsorbent, capable of effectively binding free and conjugated bile acids present in the stomach as a result of duodenogastric regurgitation.

Abstract: Complexes of the formula:A.X.sub.nwherein A represents doxorubicin; wherein X represents Ca.sup.++, Mg.sup.++, Zn.sup.++, or Ni.sup.++ ; and wherein n represents one or two having enhanced stability are disclosed.The above-described compounds are inorganic complexes of a well-known and regulatory approved compound, doxorubicin, useful in the treatment of a variety of carcinomas. These complexes offer enhanced stability over doxorubicin per se.

Abstract: Novel 3,2'-spiro(1',3'-thiazolidine) compounds which are transient prodrug forms of known anti-inflammatory corticosteroids are disclosed. The subject compounds can be prepared by known methods, for example, by reacting the corresponding 3-keto steroids with a thiazolidine forming reagent such as an L-cysteine alkyl ester. Preferred compounds are derived from such known anti-inflammatory corticosteroids as cortisone acetate, hydrocortisone, prednisone, prednisolone and the like.

Abstract: Transient, C-21 and/or C-17 esteramide prodrugs of the anti-inflammatory corticosteroids, prepared by esterification of hydroxy steroids, are disclosed.

Abstract: Transient, topically active thiazolidine type prodrug forms of progesterone are disclosed.

Abstract: Novel prodrug forms of carboxylic acid, non-steroidal, anti-inflammatory agents are disclosed, having the structural formula ##STR1## wherein ##STR2## represents the acyloxy residue of any non-steroidal anti-inflammatory drug which contains a carboxylic acid function; R.sub.1 and R.sub.2, which can be the same or different, each represents a member selected from the group consisting of C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, aryl, aralkyl, C.sub.5 -C.sub.6 cycloalkyl and C.sub.5 -C.sub.6 cycloalkenyl; or R.sub.1 and R.sub.2 are combined so that --NR.sub.1 R.sub.2 together form a member selected from the group consisting of a cycloheteroalkyl radical such as morpholino, 1-pyrrolidinyl, 4-methyl-1-piperazinyl or piperidino and a heteroaryl radical, such as 1-imidazolyl or 1-pyrazolyl; and the nontoxic pharmaceutically acceptable acid addition salts thereof.

Abstract: Soft quaternary surface active agents having the formula: ##STR1## wherein >N represents a tertiary open chain or cyclic aliphatic amine; wherein >N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.20 open chain or cyclo alkyl group, a C.sub.1 -C.sub.20 alkoxyalkyl group, a C.sub.1 -C.sub.20 acyloxyalkyl group, a C.sub.1 -C.sub.20 haloalkyl group, a C.sub.1 -C.sub.20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O--C.sub.1 -C.sub.4 alkyl group, an O--C.sub.1 -C.sub.8 acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 represents a C.sub.9 -C.sub.22 straight or branched alkyl group, a --(CH.sub.2).sub.n -- ##STR2## group, wherein R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C.sub.0 -C.sub.

Abstract: A method for treating circulatory shock in warm-blooded animals via parenteral administration of 3,4-Dipivalyl-.alpha.-[(methylamino)methyl]benzyl alcohol and its nontoxic pharmaceutically acceptable acid addition salts is disclosed.

Abstract: Rapid therapeutically effective antimalarial levels of a member selected from the group consisting of 6,8-Dichloro-.alpha.-(dibutyl-amino-methyl-2-(3',4'-dichlorophenyl-4-quino linemethanol, 3-Dibutylamino-1-[2,6-bis(4-trifluoromethylphenyl)-4-pyridyl]propanol and 1,3-Dichloro-6-trifluoromethyl-9-[1-hydroxy-3-(dibutylamino) propyl]-phenanthrene are achieved by dissolving the same in an organic fatty acid of the formula: R-CCOH, wherein R represents a member selected from the group consisting of a saturated aliphatic hydrocarbon group of from seven to twenty carbon atoms and a mono-, di-, tri-, or tetra-unsaturated hydrocarbon group of from seven to twenty carbon atoms, and subsequently administering said acid containing the dissolved compound to a warm-blooded animal (e.g., human) afflicted with malaria.