Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.

Abstract: The present invention is concerned with compounds of formula 1 ##STR1## wherein R.sub.0 is alkyl, alkoxy or alkylthio having 1-4 carbon atoms, hydroxy, halogen,Z, together with the carbon atom and the nitrogen atom and the intermediate carbon atom, constitutes a heterocyclic group which consists of 5-8 ring atoms, in which, besides the already present nitrogen atom, a second hetero atom from the group N, O, or S may be present, which ring may be substituted with 1-4 methyl group, or which ring may be annelated with a phenyl group optionally substituted with fluorine, or a methyl or methoxy group;A is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.3, R.sub.4 and R.sub.

Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radical orR.sub.3 and R.sub.

Abstract: A colloid solution for preparing a suspension, containing one or more components selected from Group A and one or more components selected from Group B as dispersoids, and water as a dispersant medium, the colloid solution being at a pH such that suspensoid particles added thereto are positively charged; wherein Group A consists of xylitol, D-sorbitol, D-mannitol, lactose, saccharose, cyclodextrin, maltose, D-fructose, D-glucose and galactose; and Group B consists of sodium carboxymethylcellulose, sodium alginate, sodium polyacrylate and gum arabic.

Abstract: Benzenes, substituted by a non-aromatic, non-fused 1-azabicycle and a substituent of low lipophilicity or a hydrocarbon substituent, their salts and prodrugs are useful in medicine, for example, in treating dementia. Some formulations of such benzenes are novel as are some of the compounds per se. They can be synthesized by methods analogous to those known in the art.

Abstract: A process is provided for producing alkylthio-substituted carboxylic acids and arylthio-substituted carboxylic acids and their corresponding alkylthio-substituted thioesters and arylthio-substituted thioesters. The process comprises reacting a mercaptan with a lactone in the presence of an acidic catalyst at temperatures of about 100.degree. C. to about 350.degree. C. The process for preparing the thio-substituted carboxylic acids and thio-substituted thioesters may be a continuous process or a batch process.

Abstract: N-Heterocyclomethylspiroheterocycles of the general formula I ##STR1## where A is a radical, II, III or IV ##STR2## R.sup.2 is CH.sub.3, OH or OCH.sub.3, n is from 0 to 3,R.sup.3 is hydroxyl, acyloxy, alkoxy, unsubstituted or substituted benzoyloxy, unsubstituted or substituted benzyloxy, unsubstituted or substituted alkyl or unsubstituted or substituted alkenyl, unsubstituted or substituted aryl,X is oxygen, sulfur or methylene,Y is hydrogen or hydroxyl, andR.sup.1 is hydrogen, alkyl or unsubstituted or substituted cyclohexyl or unsubstituted or substituted phenyl, their addition salts with acids, and fungicides containing these compounds.

Abstract: A defoamer composition including a primary antifoam agent which includes a particulate-type material having a high surface area such as silica, a secondary antifoam agent for acting synergistically with the primary antifoam agent such as polydimethylsiloxane, a water carrier, and a quaternary ammonium salt silane compound which functions as an antimicrobial agent, fixed and adhered to the surface of the particulate material, in order that the defoamer composition be resistant to biological degradation due to the presence in the system of microorganisms. Methods of defoaming cationic, anionic, and nonionic surfactant produced foams are disclosed, as is a method of rendering silica hydrophobic.

Abstract: Pharmacologically active R(-) 3-quinuclidinol derivatives are described which are muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula (I) ##STR1## wherein R represents a linear or branched lower alkyl group, a cycloalkyl-C.sub.1-2 alkyl or an aralkyl group, or it is absent;X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;R.sub.1 represents H, a linear or branched lower alkyl group or an acyl group of the type R.sub.2 --CO, in which R.sub.

Abstract: A series of cis-3-[(cyclic)methylamino]-2-[(.alpha.-substituted)arylmethyl]quinuclidin es, 3-[(cyclic)methylimino]-2-[(.alpha.-substituted)-arylmethyl]quinuclidines and cis-3-[(cyclic)-methyleneamino]-2-[(.alpha.-substituted)arylmethyl]-quinuc lidines, including their pharmaceutically acceptable salts, are disclosed. These particular compounds are found to be useful as substance P antagonists and therefore, are of value in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases and pain or migraine. Preferred member compounds include cis-3-[(2-chlorophenyl)methylamino]-2-benzhydryl-quinuclidine, cis-3-[(2-trifluorophenyl)methylamino]2-benzhydrylquinuclidine and cis-[(2-methoxyphenyl)methylamino]-2-benzhydrylquinuclidine. Methods for preparing these compounds from known starting materials are provided.

Abstract: A process for the preparation of a stable emulsion of at least one water-immiscible liquid phase L in an aqueous phase D is described which comprises mixing the liquid phase or phases L with a dispersion of spheres in an aqueous phase D, the spheres having an average diameter of 0.025 to 5 microns and consisting of substantially concentric lipid laminae encapsulating an aqueous phase E between them, the lipid or lipids constituting the laminae being ionic or nonionic amphiphilic substances capable of forming a lamellar phase in water, and subjecting the whole to mechanical agitation so as to disperse the phase (or phases) L in the phase D in the form of droplets having an average diameter of 0.1 micron to a few microns.

Abstract: The invention relates to novel derivatives of tetrahydro-2,3,6,7,1H,5H,11H-(1)benzopyrano(6,7,8ij)quinolizinone in accordance with the formula: ##STR1## in which R.sup.1 represents 1) --NH--(CH.sub.2).sub.n --R.sup.2 with n being an integer between 1 and 20 and R.sup.2 representing --N.dbd.C.dbd.S or NH--CO--CH.sub.2 X with X representing I, Br or Cl, or2) --NH--(CH.sub.2 --CH.sub.2 --O)m--CH.sub.2 --CH.sub.2 --R.sup.3 with m being an integer between 1 and 30 and R.sup.3 representing a group chosen from among groups of formula ##STR2## in which p is an integer from 1 to 10 and X represents Br, Cl or I. These derivatives can be use as markers for organic compounds, in particular biological substances, for the detection thereof by chemiluminescence or fluorescence.

Abstract: A benzofurancarboxamide of the formula: ##STR1## where: X is hydrogen or methoxy,R.sup.1 is a radical of the formula: ##STR2## wherein R.sup.3 to R.sup.5 are each, independently of one another, hydrogen or C.sub.1-6 alkyl, R.sup.6 is a branched or unbranched C.sub.1-6 alkyl, or benzyl which may be methyl- or halogen-substituted on the nucleus, and is a single or double bond.

Abstract: A substituted benzoyl derivative of the formula: ##STR1## ps wherein R is a lower alkyl group, or a phenyl group unsubstituted or substituted by a lower alkyl group, halogen atom or a lower alkoxy group;n is an integer of 2 0r 3;m is an integer of from 0 to 6, and when m is an integer of from 2 to 6, the plurality of R may be the same or different fron one another;l is an integer of 0, 1 or 2;X is a halogen atom, a nitro group, a cyano group, a lower alkyl group, a lower alkoxy group, or a lower haloalkyl group;Y is a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group unsubstituted or substituted by a halogen atom or a lower alkoxy group, a lower alkoxy group, or a lower alkoxy carbonyl group; andZ is a halogen atom, a nitro group, a cyano group, a trifluoromethyl group, a lower alkoxy group, a lower alkylthio group, a lower haloalkylthio group, a lower alkylsulfinyl group, a lower haloalkylsulfinyl group, a lower alkylsulfonyl group, or a lower haloalkylsulfonyl group.

Abstract: 3-[N-Aroyl(or thioaryol)aminoalkyl]-3-quinuclidinols corresponding to the formula: ##STR1## wherein X is O or S, and Ar is phenyl, substituted phenyl, indole, indazole or pyrimidine; optical isomers and the pharmaceutically acceptable acid addition salts and solvates thereof. These compounds have gastric emptying, antiemetic, anxiolytic and selective serotonin modulating or inhibiting activity.

Abstract: This invention provides a class of nicotine analogs which as therapeutic agents exhibit tranquilizing effects in mammals.Illustrative of an invention nicotine analog is 3-[N-methyl-N-(3-aminopropyl)]aminomethylpyridine ##STR1## the nicotine analogs can exist in the form of acid addition salts.

Abstract: A compound of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl or alkoxy; R.sub.1 is alkyl, alkenyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl or alkoxy; R.sub.2 is: ##STR2## or a pharmaceutically acceptable salt thereof, are ACAT inhibitors.

Abstract: A group of four stereoisomers and their pharmaceutically acceptable salts are disclosed. The stereoisomers have formula I. ##STR1## In Formula I the asymmetric centers a and b may be the same or different and have either the absolute R or S configuration. Also disclosed are pharmaceutical compositions containing the stereoisomers and use of the stereoisomers as antihypertensive agents, as peripheral and cerebral vasodilators and as coronary therapeutic agents.The preferred compound is (R,R)-1-azabicyclo[2.2.2]oct-3-yl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.

Abstract: The invention concerns a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; R.sup.1 if (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 ---, wherein each of A.sup.1 and A.sup.2 is (1-4C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino.The invention also concerns processes for the manufacture of a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said bicyclic derivatives. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.