Abstract: The compounds of the present invention relates to tetrahydropyridine derivatives and have high affinity and specificity to .sigma. receptors, whereby these are thought to be effective for some psychoses.

Abstract: A compound of the formula: ##STR1## wherein n is an integer of from 2 to 6; and p and q each is an integer of 0 or 1, excluding the case where p is 0 when q is 1; or a pharmaceutically acceptable acid addition salt thereof. This compound has a high affinity and specificity to .sigma. receptors, and is thought to be effective for treatment of some psychoses.

Abstract: A compound of the formula (I): ##STR1## wherein X.sup.1 nd X.sup.2 each independently represents lower alkyl, lower alkoxy or halogen or a pharmaceutically acceptable salt thereof, which is useful as an active ingredient for a pharmaceutical composition for treating antidepressant or aftereffects of cerebrovascular impairments.

Abstract: The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 14 C.sub.6 alkyl; n is an integer of from 2 to 3; Z.sup.1 is phenyl, benzyl, or isoxazolyl and each is optionally substituted by a halogen, a methoxy, or a methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, allyl, unsubstituted phenyl, or phenyl substituted by halogen, methyl, or methoxy; orZ.sub.1 and Z.sub.2 are taken together with the adjacent nitrogen atom to form triazolyl, imidazolyl or pyrazolyl; or a pharmaceutically acceptable acid addition salt thereof.

Abstract: The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.

Abstract: A compound of the formula: ##STR1## (wherein R is phenoxy optionally substituted by a halogen, methoxy, or methyl group, ##STR2## one of A and B is ##STR3## and the other is >CH.sub.2 ;R.sup.1 is hydrogen or C.sub.1 -C.sub.5 alkyl;Z.sup.1 is phenyl, benzyl, or isoxazolyl each optionally substituted by a halogen, methoxy, or methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, or phenyl optionally mono-, di-, or tri-substituted by a halogen, methoxy, or methyl group; or Z.sup.1 and Z.sup.2 taken together with the adjacent nitrogen atom may form 5-membered heterocyclic group; Z.sup.3 is C.sub.1 -C.sub.5 hydroxyalkyl, di(C.sub.1 -C.sub.5 alkyl) sulfamoyl, 6-membered heterocyclic group, phenyl, benzyl, or phenylsulfonyl each phenyl moiety of the last three members being optionally substituted by a halogen, methoxy, or methyl group; Z.sup.

Abstract: A compound of the formula: ##STR1## (wherein R is phenoxy optionally substituted by a halogen, methoxy, or methyl group, ##STR2## one of A and B is ##STR3## and the other is >CH.sub.2 : R.sup.1 is hydrogen or C.sub.1 -C.sub.5 alkyl; Z.sup.1 is phenyl, benzyl, or isoxazolyl each optionally substituted by a halogen, methoxy, or methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, or phenyl optionally mono-, di-, or tri-substituted by a halogen, methoxy, or methyl group; or Z.sup.1 and Z.sup.2 taken together with the adjacent nitrogen atom may form 5-membered heterocyclic group; Z.sup.3 is C.sub.1 -C.sub.5 hydroxyalkyl, di(C.sub.1 -C.sub.5 alkyl)sulfamoyl, 6-membered heterocyclic group, phenyl, benzyl, or phenylsulfonyl each phenyl moiety of the last three members being optionally substituted by a halogen, methoxy, or methyl group; Z.sup.

Abstract: A compound of the formula: ##STR1## wherein Y is ##STR2## R is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkanoyl, or C.sub.7 -C.sub.9 phenylalkyl, and X is hydrogen, C.sub.1 -C.sub.5 alkoxy, or halogen being useful for the treatment of senile dementia, psychoneurosis, and/or amnesia.

Abstract: A compound of the formula: ##STR1## (wherein R is --SO.sub.2 R.sup.1 or --CONHR.sup.2 ; R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.8 -C.sub.12 phenylalkenyl, amino, dimethylamino, optionally substituted C.sub.8 -C.sub.12 aryl, or 5- or 6-membered heterocyclic group including at least one hetero atom selected from the group consisting of N, S, and O; R.sup.2 is amino, C.sub.1 -C.sub.8 alkylamino, C.sub.1 -C.sub.8 alkyl, or optionally substituted C.sub.8 -C.sub.12 aryl) or its pharmaceutically acceptable acid-addition salt, being useful as a drug for senile dementia, psychotropic, or antiamnesia agent is provided through several routes.

Abstract: A process for introducing thiocarboxylic ester at ortho-position of phenols or phenylamines which comprises reacting a phenyl compound having group or optionally substituted amino or cyclic amino group, of which at least one ortho-position is vacant, with C.sub.1 -C.sub.5 alkyl thiocyanate, C.sub.7 -C.sub.13 aralkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and hydrolyzing the resultant product under acidic conditions is provided, and said process is useful in the synthesis of medicinals, pesticides and dyes.

Abstract: A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C.sub.1 -C.sub.5 alkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.

Abstract: A useful intermediate for synthesizing penicillins or cephalosporins {i.e., 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid half ester (VI)} is prepared by a process comprising (1) treating haloacetylmalonic acid ester (I) with thiourea to give 2-(2-amino-4-thiazolyl)malonic acid ester (II), (2) protecting the amino group of the latter to give 2-(2-protected amino-4-thiazolyl)malonic acid ester (III), (3) treating the product with haloalkenoic acid ester to give 1-(2-protected amino-4-thiazolyl)-2-propene-(1,1,3-tri or 1,1,3,3-tetra)carboxylic acid ester (IV), (4) hydrolyzing and decarboxylating the latter to give 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid (V), and (5) treating the product with alcohol and a hemi-esterifying reagent to give the objective 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid half ester (VI).

Abstract: A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-[1-(2-hydroxyethyl)-1H-tetrazol -5-yl]thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 is hydrogen or alkyl optionally substituted by halogen or pyridinium; R.sup.2 is hydrogen or a hydroxy-protecting group; and R.sup.3 is hydrogen, a light metal, or a carboxy-protecting group.

Abstract: A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-(1-carbamoylmethyl-1H-tetrazol- 5-yl)thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein Ar is phenyl, hydroxyphenyl, or thienyl and R is hydrogen, a light metal, or a carboxy-protecting group.

Abstract: Antibacterial 7.alpha.-methoxy-3-cephem derivatives of the formula: ##STR1## [wherein R.sup.1 is hydrogen, or organic or inorganic acyl;R.sup.2 is alkyl; andCOR.sup.3 is carboxy or protected carboxy],methods of production, and pharmaceutical preparations thereof.

Abstract: Antibacterial 7.beta.-arylmalonamido-7.alpha.-methoxy-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acids of the formula: ##STR1## wherein Ar is a heterocyclic group or p-oxysubstituted phenyl; COB.sup.1 and COB.sup.2 are each a carboxy or protected carboxy group; and Het is an unsubstituted or substituted heterocyclic group. These compounds are prepared from, e.g., 7.beta.-amino-7.alpha.-methoxy-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acid derivatives by acylation with arylmalonic acid or reactive derivatives thereof. They are useful as an active ingredient in antibacterial pharmaceutical preparations.