Abstract: Novel indoloisoquinoline derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.4 are each hydrogen, a halogen, nitro or C.sub.1-4 alkoxy and R.sub.2 and R.sub.3 are each hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, a C.sub.3-6 cycloalkyl-C.sub.1-3 alkyl or a group of the formula, ##STR2## or -A-O-B wherein A is a C.sub.1 -C.sub.7 alkylene; R.sub.5 and R.sub.6 are each hydrogen or C.sub.1-4 alkyl, or, when taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocyclic ring and B is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl, provided that, when both R.sub.1 and R.sub.4 are hydrogen and R.sub.3 is methyl, then R.sub.2 can not be hydrogen, have potent anti-tumor activities.

Abstract: A method for separation of diastereoisomeric 3-(3,4-dibenzyloxyphenyl)serine, which comprises reacting a mixture of the threo isomer and erythro isomer of 3-(3,4-dibenzyloxyphenyl)serine with a mineral acid and separating the mixture of the resulting mineral acid salts of the threo isomer and erythro isomer into each mineral acid salt by a conventional fractional crystallization utilizing the difference in solubility of the mineral acid salts, and optionally converting the separated mineral acid salt into a free isomer. Said 3-(3,4-dibenzyloxyphenyl)serine or a mineral acid salt thereof thus separated can give 3-(3,4-dihydroxyphenyl)serine which is a precursor of norepinephrine and which has activity in the circulatory system or psychotropic activities by removing the benzyl group therefrom.

Abstract: 2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sub.3 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl, and pharmaceutically acceptable salts thereof, which are useful as non-addicting analgesics with sedative effects, are prepared by the reaction of a 6,7-benzomorphan derivative of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, with a reactive derivative of an alcohol compound of the formula: ##STR3## wherein X is an optionally protected carbonyl group; and R.sub.3 is as defined above, optionally followed by the elimination of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.

Abstract: Spiro amine derivatives having excellent antihypertensive activity and central nervous system depressant activity, and represented by the formula: ##STR1## and their preparation and use.

Abstract: Prostanoic acid derivatives of the formula, ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is C.sub.4-8 alkyl and >C=Z is >C=O or ##STR2## are prepared by reacting a cyclopentane of the formula, ##STR3## wherein R.sub.2 is defined above and R is hydrogen or tetrahydropyranyl, with Wittig reagent of the formula,(R.sub.3).sub.3 P.dbd.CH(CH.sub.2).sub.3 COOMwherein R.sub.3 is aryl and M is alkali metal and, if necessary, hydrolyzing, or by oxidizing a compound of the formula, ##STR4## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.9 is tetrahydropyranyl group, with an oxidizing agent. The compounds (I) are useful as anti-ulcer agent.

Abstract: Quinazoline compounds of the formula: ##STR1## wherein A is ##STR2## wherein n is an integer of 1 or 2, or ##STR3## wherein X is O or CH.sub.2, and n and m are independently an integer of 1 or 2, and its non-toxic pharmaceutically acceptable salts, having an excellent antihypertensive activity without causing adverse effects such as orthostatic hypotension.

Abstract: Novel 9-aminoalkyl-methanoanthracenes of the formula: ##STR1## wherein A is C.sub.1 -C.sub.4 alkylene or C.sub.3 -C.sub.4 alkenylene and R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl(C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl or polyhalo(C.sub.2 -C.sub.4)alkyl or, when taken together with the adjacent nitrogen atom, they may form a 5 to 7-membered nitrogen-containing heterocyclic ring which may contain an additional hetero atom, and their non-toxic salts, which are useful as anti-anxiety, anti-depressant, major tranquilizer, anti-histamine and anti-allergy drugs and can be prepared through a novel key intermediate, i.e., 9-formyl-9,10-dihydro-9,10-methanoanthracene, by various methods.

Abstract: Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 -C.sub.3)alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

Abstract: Prostanoic acid derivatives of the formula, ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is C.sub.4-8 alkyl and >C.dbd.Z is >C.dbd.0 or ##STR2## are prepared by reacting a cyclopentane of the formula, ##STR3## wherein R.sub.2 is defined above and R is hydrogen or tetrahydropyranyl, with Wittig reagent of the formula,(R.sub.3).sub.3 P.dbd.CH(CH.sub.2).sub.3 COOMwherein R.sub.3 is aryl and M is alkali metal and, if necessary, hydrolyzing, or by oxidizing a compound of the formula, ##STR4## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.9 is tetrahydropyranyl group, with an oxidizing agent. The compounds (I) are useful as anti-ulcer agent.

Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.

Abstract: Novel indan compounds of the formula ##STR1## wherein A and X are each ethylene or vinylene; B is C.sub.2-4 alkylene; R and R.sub.2 are each hydrogen or C.sub.1-4 alkyl; R.sub.1 is C.sub.1-8 alkyl; <C = Z is <C = O, or ##STR2## and its non-toxic salts, which are useful as antiulcers, gastric secretion inhibitors, and hypotensors.

Abstract: Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 14 C.sub.3) alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

Abstract: Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.

Abstract: Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.

Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.

Abstract: Novel bicycloheptene compounds of the formula: ##STR1## wherein A is C.sub.2 -C.sub.4 alkylene; X and B are each ethylene or vinylene; R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkoxyalkyl, C.sub.5 -C.sub.7 cycloalkyl, C.sub.5 -C.sub.8 cycloalkylalkyl, aryl, C.sub.7 -C.sub.10 arylalkyl, C.sub.7 -C.sub.10 aryloxyalkyl; R.sub.2 is hydrogen, or C.sub.1 -C.sub.4 alkyl; and Z is carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl or C.sub.1 -C.sub.5 carbamoyl, and its non-toxic salts, which are useful as antiulcers, gastric secretion inhibitors, central nervous system regulators, and labor inducing agents.

Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, aryl(C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl and n represents 1 or 2, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

Abstract: Novel tricyclic compounds of the formula: ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH=CH-- or ##STR2## X is hydrogen, halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.3 -C.sub.6 cycloalkyl (C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl, polyhalo(C.sub.1 -C.sub.2)alkyl, C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.3)alkyl or hydroxy(C.sub.1 -C.sub.3)alkyl, and non-toxic salts thereof which are useful as antidepressants and can be prepared by reduction of a compound of the formula: ##STR3## wherein A, X, R.sub.1, R.sub.2 and R.sub.3 are each as defined above.

Abstract: Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1.sub.-4 alkyl, or C.sub.1.sub.-4 alkoxy, R.sup.2 is hydrogen or halogen, and R.sup.3 and R.sup.4 are each hydrogen, halogen, C.sub.1.sub.-4 alkyl or trifluoromethyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, with formaldehyde and an amine of the formula: ##STR3## wherein R.sup.3 and R.sup.4 are each as defined above; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.

Abstract: Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, R.sup.2 is hydrogen or halogen, and X is a group of the formula: ##STR2## and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each as defined above with formaldehyde and an piperidine compound of the formula: , or its non-toxic salt; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.