Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or 2 hydrogen radicals; Y may represent --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; q is 2, 4, 6 or 8; wherein p.gtoreq.9; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl. These compositions are useful in topical or transdermal applications of the physiologically-active agent.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carboalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4

Abstract: A transdermal delivery bandage and system is provided which includes a supply of topically and/or systemically-active drug, an adhesive for releasably securing the bandage to a dermal surface and control means which are separate from the supply of topical and/or systemically-active drug for adjustably controlling surface contact area between the topical and/or systemically-active drug and the dermal surface. The control means are manually operable by a user of the bandage for adjustably controlling the dose of drug to be administered. Alternatively, the maximum available dose from a given bandage may be preselected by a dispensing pharmacist.

Abstract: This invention provides novel compounds represented by the general formula: ##STR1## R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrocarbyl radicals and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and halogen atoms; A is a straight or branched chain hydrocarbon moiety containing from 1 to 12 carbon atoms and from 0 to 2 double bonds; R.sub.3 is selected from the group consisting of oxa- or dioxacycloalkanyl radicals which may be substituted with one or more hydroxy, keto, lower alkyl, phenyl or alkylenedioxy radicals; R.sub.4 is an aryl or heteroaryl radical; and R.sub.5 is a lower alkyl radical or A-R.sub.3 ; and pharmaceutically-acceptable salts thereof. These compounds are useful for treating coronary insufficiency, hypertension, angina pectoris, cardiac arrythmia, heart attack, or coronary vasospasm.

Abstract: A toilet seat cover is provided for preventing contact between the human bottocks and the toilet seat when the sheet is disposed and aligned with the toilet seat. A microbiocidal shield is created by the perspiration from the bottocks contacting a water-soluble oxidizing agent along with a water-soluble ene-diol compound dispersed as separate particles in the sheet. The water-soluble oxidizing agent and water-soluble ene-diol compound may be separately microencapsulated by a protective film. Capillary action of the fibers in the sheet provide for conducting free water released during reaction between the water-soluble oxidizing agent and the ene-diol compound throughout the toilet seat cover. Fibers of the sheet are adhesively bonded together within the adhesive that is soluble and dispersible in water to enable the toilet seat cover to be flushed down the toilet after use.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 10 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R.sup.1 and R.sup.2 is 5 or more.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-16 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen.

Abstract: This invention provides a method for treating the symptoms of parkinsonism which comprises administering to a human or other mammal suffering from the symptoms of parkinsonism an effective amount of a compound selected from the group consisting of optically-active or racemic compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of organic radicals methyl, substituted or unsubstituted phenyls, pyridyl, hydroxyphenyl, ##STR2## X is oxygen or sulfur, Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms. and a is an integer of from zero to 3,R.sub.2, R.sub.3 and R.sub.

Abstract: This invention provides a method for treating the symptoms of schizophrenia which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting of optically-active or racemic compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of organic radicals having fused rings, phenyl, pyridyl ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3. R.sub.2, R.sub.3 and R.sub.

Abstract: This invention relates to a selective process for preparing bicyclic lactam-lactone compounds wherein the rings are fused, i.e. the rings share at least two carbon atoms, or are isolated. In particular, the present invention provides a process for selectively reacting novel 1-hydrocarbylamino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-alkanolactonyl or hydrocarbyl (or heteroatom-substituted hydrocarbyl) alkanonylactonyl methane, as the salt of an acid having a pKa of 0 or more, to provide bicyclic lactam-lactone compounds. The selectively of the reaction to either fused or isolated bicyclic compounds is controlled by cyclizing the novel salts, in the absence of a base, a cyclizing said novel salts, in the presence of an amount of base substantially equivalent to said acid, respectively.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comnprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X represents sulfur, oxygen or 2 hydrogen radicals; Y represents --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; wherein p.gtoreq.9; q is 2, 4, 6 or 8; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl.

Abstract: This invention provides a process for preparing lactams, by selectively reacting a novel 1-hydrocarbyl-amino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-hydrocarbyl (or heteroatom-substituted hydrocarbyl) carboxylic acid, alkyl ester methane, as the salt of an acid having a pKa of 0 or more, in the absence or presence of a base, whereby novel lactams wherein one or both hydrocarbyl moieties are incorporated into the lactam ring are obtained. That is, the acid moiety of said novel salt promotes the reaction whereby both hydrocarbyl moieties are incorporated into the ring, while the presence of a base, in an amount substantially equivalent to said acid promotes the reaction whereby only one hydrocarbyl is incorporated into the ring.

Abstract: This invention provides compounds useful for treating coronary insufficiency, hypertension, angina pectoris, cardiac arrythmia, heart attack or coronary vasospasm and represented by the general formula: ##STR1## R.sub.1 and R.sub.2 are each independently selected from the group consisting of lower alkyl, N-alkylphthalimido and derivatives of N-alkylphthalimido, wherein said N-alkyl group comprises at least 2 carbon atoms;A is a straight or branched chain hydrocarbon moiety containing from 1 to 12 carbon atoms and from 0 to 2 double bonds;R.sub.3 is selected from the group of radicals consisting of hydrogen, --NH.sub.2 and --NCS;R.sub.4 is an aryl or heteroaryl radical; andR.sub.5 is a lower alkyl radical or A--R.sub.3 ; provided that when R.sub.3 is a hydrogen radical at least one of R.sub.1 and R.sub.2 is not lower alkyl, including both pure enantiomers as well as mixtures thereof; andpharmaceutically-acceptable salts thereof.

Abstract: Compounds having calcium channel antagonist activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently amino, trifluoromethyl, pentafluoroethyl, alkoxy, lower alkenyl, or lower alkynyl or branched or unbranched lower alkyl, which is unsubstituted or is substituted with cyano, hydroxy, acyloxy, hydrazino, lower alkyl amino, or di(lower alkyl)-amino or 5 or 6 membered saturated nitrogen-containing heterocyclic-1-yl, which is unsubstituted or is substituted with oxo, hydroxy, alkyl, and hydroxy (lower alkyl) R.sub.3 is straight- or branched-chain C.sub.1 to C.sub.12 alkyl, alkenyl, alkynyl, or cycloalkyl, and is either unsubstituted or substituted with hydroxy, acyloxy, cyano, di(lower alkyl) amino 5- or 6-membered saturated nitrogen-containing heterocyclic -1-yl or R.sub.3 is --A--R.sub.4, A is a straight- or branched-chain hydrocarbon moiety containing from 2 to 12 carbon atoms and from 0 to 2 double bonds, R.sub.4 is selected from the group consisting of: ##STR2## R.sub.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 20 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R.sup.1 and R.sup.2 is 5 or more.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## wherein R" is H or halogen.

Abstract: The present invention provides a method for preventing or treating an animal, e.g. a cow, for mastitis, e.g. bovine mastitis, by administering to said animal a composition comprising copper ion and an organic compound having at least two hydroxyl groups and at least one unsaturated carbon-carbon bonds, e.g. ascorbic acid, in an amount effective to prevent or treat mastitis.

Abstract: The disclosure describes compositions and methods for improved delivery of plant growth regulators comprising contacting a plant with a composition comprising an effective amount of a plant growth regulator and an effective delivery enhancing amount of compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group having 1-4 carbon atoms, m is 3-7, n is 0-17 and R is --CH.sub.3, ##STR2## where R" is H or halogen, with the proviso that if m is 3 and R is CH.sub.3, then n is 5-17.

Abstract: This invention provides compositions comprising a physiologically-active agent and an azacycloalkene having at least one double bond in the ring and of the general formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a straight or branched chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3; and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: A toilet seat cover is provided for preventing contact between the human buttocks and the toilet seat when the sheet is disposed and aligned with the toilet seat. A microbiocidal shield is created by the perspiration from the buttocks contacting a water-soluble oxidizing agent along with a water-soluble ene-diol compound dispersed as separate particles in the sheet. The water-soluble oxidizing agent and water-soluble ene-diol compound may be separately microencapsulated by a protective film. Capillary action of the fibers in the sheet provide for conducting free water released during reaction between the water-soluble oxidizing agent and the ene-diol compound throughout the toilet seat cover. Fibers of the sheet are adhesively bonded together within the adhesive that is soluble and dispersible in water to enable the toilet seat cover to be flushed down the toilet after use.