Abstract: Described herein are vitamin C prodrugs of Formula (I), (II), or (III), and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, cosmetic or personal care composition, neutraceutical composition, and medical food composition thereof. Methods of using the compounds or compositions thereof for treating diseases are also provided.

Abstract: Described herein are vitamin C prodrugs of Formula (I), (II), or (III), and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, cosmetic or personal care composition, neutraceutical composition, and medical food composition thereof. Methods of using the compounds or compositions thereof for treating diseases are also provided.

Abstract: A soluble UVA and/or UVB absorbing chromophore-comprising polymer useful for preparation of a sunscreen lotion has a multiplicity of repeating units where one or more of the repeating units includes at least one UVA and/or UVB absorbing chromophore. The repeating units are those formed from the ring-opening metathesis polymerization (ROMP) of a strained cycloakene, cycloalkadiene, bicycloalkene, or bicycloalkadiene, or where one or more sp3 hybridized carbons of the strained cycloakene, cycloalkadiene, bicycloalkene, or bicycloalkadiene is replaced with a heteroatom. The UVA and/or UVB absorbing chromophore-comprising polymer can be formed from a UVA and/or UVB absorbing chromophore-comprising monomer, which can be homopolymerized or copolymerized by ROMP. Alternately, the UVA and/or UVB absorbing chromophore-comprising polymer can be formed by polymerization of monomers that can subsequently be substituted with UVA and/or UVB absorbing chromophores.

Abstract: A pharmaceutical composition in unit dosage form adapted for topical administration to a human or non-human animal in need thereof comprising a pharmacologically effective amount of a prodrug of 5-fluorouracil having the formula: ##STR1## wherein R.sub.3 is bonded to C=O by a carbon-to-carbon bond and is a group such that the prodrug (1) has an enhanced delivery across topical membranes and (2) hydrolyzes after delivery to 5-fluorouracil.

Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.

Abstract: A compound of the formula: ##STR1## wherein: R and R.sub.1 may be the same or different and are selected from the group consisting of H; cycloalkyl groups having up to 10 carbon atoms; or straight or branched chain alkyl, alkenyl or alkynyl of 1 to 10 carbon atoms;R.sub.2 and R.sub.3 together with the nitrogen atom to which they are bonded form a pyrrolidine, piperidine, N-methyl piperazine, piperazine or morpholine ring;or a non-toxic pharmaceutically acceptable salt, adduct, oxide or other derivative thereof; and pharmaceutical compositions adapted for topical administration to a human or non-human animal and methods of topically administering the compositions to humans and non-human animals.

Abstract: N-methylamino derivatives of biologically active substances which have enhanced delivery across topical membranes and pharmaceutical compositions adapted for topical administration containing same.

Abstract: Novel, transient prodrug forms of biologically active agents containing mercapto groups have (i) the structural formula (I): ##STR1## wherein X is O, S, or NR.sup.5 ;R.sup.1 S is the residue of any biologically active agent R.sup.1 SH;R.sup.

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

Abstract: Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C.sub.1 -C.sub.4 alkyl; n is 0 or 1; R.sub.1 and R.sub.2 are each selected from a variety of unsubstituted or substituted hydrocarbon radicals, or are combined so that --NR.sub.1 R.sub.2 represents the residue of a saturated or unsaturated heterocyclic compound containing one secondary nitrogen atom; and R.sub.3 is H or one of a variety of other substituents. Salts and N-oxides of compounds of formula (I) and the corresponding diacyloxy derivatives of known bio-affecting carboxylic acids HOOC-R'-COOH are disclosed also.

Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.

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 the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.

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: Novel 3,2'-spiro(1',3'-thiazolidine) compounds which are transient prodrug forms of known 6- and/or 9-haloglucocorticosteroids are described. The subject prodrugs provide improved delivery of the prior art steroids for therapeutic purposes, particularly in alleviating inflammation, and 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.

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 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: 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.