Abstract: Topical composition for transdermal delivery of morphine. The composition contains certain morphine esters in association with a carrier. The compositions relieved pain or tranquilize a mammal when delivered transdermally.

Abstract: Compounds of formula (I), wherein R.sub.1 is selected from the group consisting of an alkyl group, an aralkyl group, an alkenyl group, a cycloalkyl group, in which the alkyl, aralkyl, alkenyl or cycloalkyl group is unsubstituted or substituted with one or more substituents selected from the group consisting of a halogen atom, e.g. Cl or Br, a hydroxyl group or a straight or branched-chain alkoxy group containing from 1 to 6 carbon atoms; and the pharmaceutically acceptable acid addition salts thereof. Such compounds are prodrugs of TRH and are characterized by having a higher lipophilicity than TRH and possessing a high resistance toward degradation by TRH-inactivating enzymes. Such compounds will after administration be converted into TRH.

Abstract: A compound having the formula ##STR1## where X is a radical of myo-inositol or a radical of a configuration isomer thereof where at least one R is ##STR2## where Y is (1) oxygen, (2) a straight or branched alkyl with 1-10 carbon atoms, where Z is ##STR3## where A.sup.1 and A.sup.2 are the same or different and are hydrogen or methyl and n is 3-10, or ##STR4## where A.sup.1 and A.sup.2 are hydrogen or methyl and where m is 1-5, where R.sup.1 is hydrogen, straight or branched alkyl, aryl or alkaryl, alkoxy or aryloxy, where R.sup.2 is(1) R.sup.1,(2) hydroxyl, or(3) OZOCOR.sup.1,and where the remaining R is/are hydroxyl.

Abstract: Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R.sub.1 and R.sub.2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R.sub.1 and R.sub.2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution.

Abstract: Compounds having the formula ##STR1## wherein R.sup.1, R.sup.4, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or a substituent, R.sup.2 is a substituent, R.sup.5 is an optionally-substituted bicyclic ring system, especially a 7-benzofuranyl or 2,3-dihydrobenzofuran-7-yl substituent, R.sup.9 is hydrogen, alkyl, alkoxycarbonyl or, together with R.sup.8, forms the remainder of a heterocyclic ring, their pharmaceutically-accceptable salts, as well as their pharmaceutical compositions and use as prodrugs for compounds active for the treatment of mental disorders, are disclosed.

Abstract: Compounds are disclosed of the general formula I ##STR1## wherein R.sub.1 is a group of the formula IIR.sub.3 --X-- IIwherein R.sub.3 is alkyl; phenyl; phenyl substituted with halogen, lower alkyl, hydroxy, lower alkoxy, or phenoxy; phenyl-lower alkyl in which the phenyl group may be substituted with halogen, lower alkyl, hydroxy, lower alkoxy, or phenoxy; phenyl-lower alkenyl in which the phenyl group may be substituted with halogen, lower alkyl, hydroxy, lower alkoxy or phenoxy; and X is oxygen or sulfur; or R.sub.1 is a group of the formula III ##STR2## wherein R.sub.4 has the same meaning as R.sub.3 as defined above; or R.sub.4 is a group of the formula IV ##STR3## wherein R.sub.7 has the same meaning as R.sub.3 as defined above; or R.sub.7 is an aromatic 5- or 6-membered heterocyclic ring containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; and wherein R.sub.5 and R.sub.6 are the same or different and each represent hydrogen or have the same meaning as R.

Abstract: Compounds of the formula Ia and Ib ##STR1## are prodrugs of allopurinol and have i.a. a much higher solubility in water and/or a higher lipophilicity than allopurinol, which makes such compounds useful for oral, parenteral and rectal administration to a warm-blooded animal such as a human. Such compounds will after administration be converted into allopurinol.

Abstract: N,N-dimethylglycine ester of metronidazole, acid addition salt thereof and method of preparing such ester or acid addition salt. The novel compounds exhibit favorable solubility in water and are especially useful for the parenteral treatment of certain anaerobic infections.