Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.

Abstract: This invention pertains to novel 3-substituted-aminomethyl-3-substituted-oxy-17a-methyl-17a-lower-alkyl-17a -aza-D-homo-5-alpha-androstane compounds useful as muscle relaxants, methods for preparing such compounds, and methods for administering muscle relaxation, wherein the novel compounds are represented the general Formula: ##STR1## including optically active isomeric forms, and pharmaceutically acceptable acid addition salts thereof, wherein:R is selected from the group consisting of hydrogen, lower-alkyl, lower-alkyl carbonyl, and di(lower-alkyl)amino carbonyl;R.sub.1 is selected from the group consisting of: di(lower-alkyl)substituted amino; lower-cycloalkyl lower-alkyl, lower-alkyl substituted amino;, 1-piperidinyl; 1-pyrrolidinyl; 1-hexamethyleneimino; 4-morpholinyl; 1-piperazinyl, 1-(4-methylpiperazinyl), tri(lower-alkyl)substituted amino, 1-(1-methylpiperidinyl); 1-(1-methylpyrrolidinyl); and 1-(4,4-dimethylpiperazinyl), each lower-alkyl group having from 1 to 6 carbon atoms;R.sub.

Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is a 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is either a CO.sub.2 R.sup.8 group or a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect or antitumor drugs.

Abstract: Novel compounds of the general formula ##STR1## which have antitussive activity, wherein R.sub.1 -R.sub.4 are as defined herein.

Abstract: Novel quinolonecarboxylic acids of the formula: ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 each is identically or differently hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.4 is cyclopropyl, phenyl, halo-phenyl, or thienyl optionally substituted by C.sub.1 -C.sub.4 alkyl or halogen, and R.sup.5 is halogen, or pharmaceutically acceptable salts thereof having a more potent and longer lasting antibacterial activities against G(+) and G(-) bacteria than known analogues, useful as antibacterial agents at an oral dose of 1-500 mg, preferably 50-100 mg per day to an adult.

Abstract: This invention provides a novel method for the preparation of optically active arylalykylsulfone derivatives, having a chiral center in the alkyl moiety in either the (R)- or the (S)-configuration. These optically active sulfones find use in the stereospecific synthesis of steroid or vitamin D compounds having chiral center at either carbon 24 or carbon 25 of the side chain. The method comprises the steps of reacting an optically active sulfinate ester having a chiral center at sulfur with a racemic alkyl Grignard reagent to obtain a mixture of diastereomeric sulfoxides, separating the mixture of diastereomeric sulfoxides, and oxidizing separately each of the diastereomers to obtain the desired optically active sulfone.

Abstract: A formulation for administration of a metalloporphyrin compound useful in the treatment or prevention of jaundice is described. The formulation comprises the metalloporphyrin in admixture with an excipient which is a water-soluble organic amine, said composition having been neutralized to neutral pH. The formulation may advantageously contain a stabilizer, such as human serum albumin.

Abstract: Ester and amide derivatives of N-(((alkoxy-(alkylthio)phosphinyl)amino)carbonyl)amino)alkanecarboxylic acids of the formula: ##STR1## (wherein R.sup.2 represents an alkyl group containing a carboxylic acid ester or amide moiety) were prepared by the reaction of O,S-dialkyl phosphoroisocyanatidothioates and ester and amide derivatives of naturally occurring and synthetic aminoacids and were found to be effective plant systemic and contact insecticides. Ethyl N-(((methoxy(methylthio)phosphinyl)amino)-carbonyl)methioninate, for example, were prepared from O,S-dimethyl phosphoroisocyanatidothioate and ethyl methioninate and found to control aster leafhoppers when applied to rice plants.

Abstract: invention relates to heterocyclic phospholipids of formula III which are useful in treating multiple sclerosis:where R .sub.2 is n-C.sub.14 -C.sub.20 alkyl;each R.sub.1, independently, is methyl or ethyl; Y is --O-- or --S--;n is an integer 2 to 6.

Abstract: The invention relates to an anti-inflammatory or antiallergic composition containing a compound of the formula ##STR1## wherein A is ##STR2## R.sup.1 is aryl which may have cyano or carbamoyl, or heterocyclic group which may have lower alkyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is lower alkyl,X is hydrogen, halogen, hydroxy or lower alkyl,m is an integer 1 or 2, andn is an integer 1 to 4, or pharmaceutically acceptable salts thereof.

Abstract: The invention relates to thiazepine derivatives, which are antagonists of platelet activating factor, of the formula: ##STR1## wherein R.sup.1 is ar(lower)alkyl which may have suitable substituent(s),R.sup.2 is hydrogen, lower alkyl which may have suitable substituent(s), or a group of the formula: ##STR2## in which A is lower alkylene and X is halogen, n is 0, 1 or 2 and Y is --CH.sub.2 --CH.sub.2 -- or ##STR3## or a pharmaceutically acceptable salt thereof.

Abstract: Novel benzoxazine compounds of the structure ##STR1## wherein X and Y are independently selected from the group hydrogen, alkyl, alkoxyalkyl, aminoalkyl, hydroxyalkyl and hydroxyaminoalkyl, each alkyl moiety having 1 to 6 carbons, and m=1, 2 or 3, have been found suitable as hair dyes.

Abstract: Imidazole derivatives are described which are useful in restoring learning and treating memory difficulties. A compound of the invention is 2,5-dioxohexahydro-1H-pyrrolo[1,2-a]imidazole.

Abstract: The invention relates to a method of treating asthma comprising administering a compound of the formula: ##STR1## wherein A is ##STR2## R.sup.1 is quinolyl, R.sup.2 is hydrogen or lower alkyl,R.sup.3 is lower alkyl,X is hydrogen, halogen, hydroxy or lower alkyl,m is integer 1 or 2, andn is an integer 1 or 4, or pharmaceutically acceptable salts thereof.

Abstract: Novel dithiolane derivatives of formula: ##STR1## wherein X is, a C.sub.2 -C.sub.7 alkylcarbonyl group, benzoyl group, benzoyl group substituted with 1-3 groups selected from halogen, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; Y represents C.sub.2 -C.sub.7 alkylcarbonyl group, C.sub.2 -C.sub.7 alkoxycarbonyl group or cyano group; and R represents di (C.sub.1 -C.sub.4 alkylamino) group, morpholino group or piperidino group, are produced by reacting glyoxal sodium bisulfite adduct with amine compounds in the presence of acids and then with dithiolates. The dithiolane derivatives can activate liver functions and are effective for treatment and prophylaxis of hepatitis and other hepatic disorders.

Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.

Abstract: Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha.,2.alpha.,6.alpha.,7.alpha.,7.alpha..beta.-1,2,6-7-tetrahydroxypyr rolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.

Abstract: It has been discovered that 6-(substituted amino)purine cytokinins, such as kinetin, induce differentiation, and consequently reduce or eliminate the abnormally high rate of proliferation, of hyperproliferating cells associated with hyperproliferative skin diseases, such as psoriasis. Thus, the present invention provides methods and compositions for treating hyperproliferative skin diseases in mammals, particularly such diseases associated with hyperproliferating epidermal cells in humans, by administering to the hyperproliferating cells associated with such a disease, in the skin of a mammal suffering therefrom, a differentiation-inducing effective amount of a 6-(substituted amino)purine cytokinin.

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: (Hydrocarbylthio)aromatic amines are prepared by reacting an aromatic amine, such as an aminobenzene, with a hydrocarbyl disulfide, such as an alkyl disulfide, in the presence of iodine, iodine monochloride, or iodine monobromide as a catalyst.