Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof:R.sup.1 --(CH.sub.2).sub.n --Zin which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R.sup.2 and R.sup.4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Abstract: The present invention relates to a process for preparing 3-amino-9,13b-dihydro-1H-dibenz[c,f]-imidazo[1,5-a]azepine-hydrochloride, as follows:a) hydrogenating 6-phthalimidomethyl-5H-dibenz[b,e]-azepine, to produce 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine;b) reacting the 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine with hydrazine, to produce 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine;c) reacting the 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine with bromooyanogen, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine; andd) precipitating the 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine in the presence of DMF and HCl, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine-hydrochloride.

Abstract: The invention relates to the compounds of general formula ##STR1## in which R.sub.1, R.sub.2, R.sub.4, R.sub.5 and A are as defined in the description.their isomers, diastereoisomers, and enantiomers as well as their addition salts with a pharmaceutically acceptable inorganic or organic acid, andmedicinal products containing the same which are usable for the treatment of psycho-behavioral disorders.

Abstract: Aminophenol derivatives of the following formula (I) ##STR1## wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen atom, lower alkyl, halogen atom or trifluoromethyl, A is hydrogen atom or lower alkyl, t is an integer of 1 to 5, l and m are respectively an integer of 2 to 4, E and W are nitrogen atoms, F is a direct bond or oxygen atom, P and Q are each hydrogen atom, halogen atom, lower alkyl or lower alkoxy, and R.sup.8 is hydrogen atom, hydroxy or a hydroxy-protecting group, and their pharmcologically acceptable salts. Since the aminophenol derivatives (I) of the present invention have excellent antioxidative action and antiinflammatory and antiallergic action in mammalian animals including human, they are extremely useful as pharmaceuticals such as an antiinflammatory or an antiallergic.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.

Abstract: The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for pharmaceutical purposes. According to the invention the reaction of 1 mole of 2-acetonyl-3'-chloro-4,5-dimethoxybenzophenone of formula (II) ##STR2## with 3-7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents at a temperature between 15.degree. C. and 85.degree. C. is carried out in the absence of air oxygen, optionally in the presence of water. The crude product is then recrystallized from an aliphatic alcohol containing 1 to 5 carbon atom(s).

Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a compound of Formula I: ##STR1##

Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a compound of Formula I: ##STR1##

Abstract: This invention relates to 1-(pyrido[3,4-b]-1,4-oxazinyl-4-yl)-1H-indoles of the formula ##STR1## where R.sub.1 -R.sub.3 are as defined herein which are useful for alleviation of depression and various memory dysfunction characterized by a cholinergic or adrenergic deficit. This invention also relates to intermediate compounds of the formula ##STR2## where R.sub.1, R.sub.2, R.sub.3, R.sub.7 and X are as defined herein.

Abstract: A new compound of the formula: ##STR1## wherein ##STR2## is an optionally substituted benzene ring; R.sup.1 is a carbocyclic or heterocyclic group which is linked to the 4-position of the 1,3-benzoxazine ring through a carbon-carbon bond, a hydrocarbon residue, etc.; and R.sup.2 and R.sup.3 are independently a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, etc., or a salt thereof is useful for treating and preventing heart, circulatory, respiratory and cerebral diseases.

Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description. Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.

Abstract: The invention relates to a compound of formula (I) ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halo, hydroxy, nitro, C.sub.1-4 alkylcarbonyl, hydroxy-C.sub.1-4 alkyl, R.sup.3 is hydrogen or optionally substituted phenylsulphonyl, R.sup.4 is optionally substituted phenyl, benzofuranyl or dihydrobenzofuranyl, and R.sup.5 is hydrogen or C.sub.1-4 alkyl; and salts thereof. These compounds are useful dopaminergic agents.

Abstract: Heterocyclic compounds of the formula ##STR1## in which R represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,A represents C--R.sup.1, N,R.sup.1 represents substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,X, Y represent O, NH,Z represents hydrogen, --CN, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,W represents O, N--R.sup.5,R.sup.5 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic radical andB represents a substituted or unsubstituted carbocyclic-aromatic or heterocyclic ring onto which one or more further rings can be fused,and the use of these compounds as dyestuffs or pigments.

Abstract: A novel compound and compositions containing S-(-)-3-morpholino-4-(3-tert-butylamino-2-hydroxypropoxy)-1,2,5 thiadiazole hemihydrate useful for administration to a patient particularly for topical administration as a pharmaceutical agent for treating known conditions and disorders treatable with timolol.

Abstract: 2-Methyl-10-(4-methyl-1-piperazinyl)-4H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.

Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.

Abstract: Substituted 3-aminosydnonimines of the formula I ##STR1## and pharmacologically acceptable acid addition salts thereof, in which R.sup.1 denotes hydrogen or the radical --COR.sup.4,R.sup.2 denotes alkyl or phenyl alkyl having 1 to 4 C atoms in the alkyl group,R.sup.4 denotes, for example, an aryl radical, and processes and formulations for controlling or preventing cardiovascular diseases by administering an effective amount of such compounds to a host in need thereof.

Abstract: The specification describes cellulose reactive unsymmetrical triphenodiaxazine dyes of the Formula (1): ##STR1## wherein each of T.sup.1 and T.sup.2, independently, represents H, Cl, Br, F, SO.sub.3 H or an optionally substituted alkyl or aryl radical;each of A.sup.1 and A.sup.2 independently represents alkyl, alkoxy, Cl, Br, COOH, SO.sub.3 H or optionally substituted sulphamoyl;each n independently has a value of 0, 1 or 2;each m independently has a value of 1 or 2;R.sup.1 represents H or an optionally substituted hydrocarbon radical;Q represents O or S;x has a value of 0 or 1;B represents an optionally substituted divalent hydrocarbon radical;each of R.sup.2 and R.sup.3, independently, represents H or an optionally substituted hydrocarbon radical or R.sup.2 and R.sup.3 are joined together to form, with B and the two N atoms, a piperazine ring;y has a value of 0 or 1, andZ represents H, or an optionally substituted hydrocarbon radical or a fibre-reactive group;provided that (1) at least one of R.sup.

Abstract: Indazole-3-carboxylic acid derivatives represented by the following general formula (I) and their physiologically acceptable acid addition salts or quaternary ammonium salts, ##STR1## are useful as a potent and selective antagonist of serotonin 3 (5-HT.sub.3) receptor. Also disclosed are compounds of the formula ##STR2## which are useful as intermediates in the production of the disclosed final product compounds.