Abstract: A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group, an ar(lower)alkyl group or an aryl group, or R.sub.1 and R.sub.2 may be combined together to form a lower alkylene group and/or R.sub.3 and R.sub.4 are combined together to form a lower alkylene group, or R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be combined together to form an o-phenylene group, X is a halogen atom and Y is an oxygen atom or a nitrogen atom substituted with lower alkyl or aryl, which is useful as an intermediate in the synthesis of 1.beta.-methylcarbapenem compounds valuable as antibiotics.

Abstract: The present invention relates to pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as herein. The compounds are useful as anti-amnestic agent.

Abstract: Pyrrolidine derivatives having inhibitory action for proline-specific endopeptidase which are useful for anti-amnestic agent. The disclosed pyrrolidine derivatives as well as their acid addition salts can be administered orally or parenterally in the form of conventional pharmaceutical preparations. For instance, they can be administered orally in the form of conventional solid pharmaceutical preparations such as tablets, capsules, syrups and suspensions. Alternatively, they can be administered parenterally by injection in the form of conventional liquid pharmaceutical preparations such as solutions, emulsions, suspensions, etc. Also, they may be directly applied to rectum in the form of suppository. Further, the preparations may contain physiologically acceptable carriers, excipients, activators, binding agents, stabilizers, etc. In the case of injections, physiologically acceptable buffers, solubilizing agents or isotonic agents may be incorporated therein. Methods of production are also disclosed.

Abstract: A process for preparing racemic 4-demethoxy-7-deoxydaunomycinone which comprises methylating an optically active .alpha.-hydroxyketone to give the corresponding methylated product of either one of the formulas: ##STR1## and reacting the latter with an acid to give a racemate of the .alpha.-hydroxyketone of the formula: ##STR2## .

Abstract: A process for preparing optically active 4-demethoxy-7-deoxydaunomycinone which comprises reacting a racemic mixture of the .alpha.-hydroxyketone of the formula: ##STR1## with an optical isomer of the .alpha.-glycol of the formula: ##STR2## wherein R is a group of the formula: ##STR3## and X is a halogen atom or a lower alkyl group to give a diastereomeric mixture of the acetal of the formula: ##STR4## .

Abstract: A compound of the formula: ##STR1## wherein Ar is a phenyl group substituted with halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, C.sub.1 -C.sub.8 alkylsulfonyl, nitro, trihalomethyl, cyano, C.sub.1 -C.sub.8 alkylamino, di(C.sub.1 -C.sub.8)-alkylamino, amino, hydroxyl, phenyl and/or phenoxy, a naphthyl group or a thienyl group optionally substituted with halogen, which is useful as an antifungal agent.

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: 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: An improved process for preparing indole derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 each are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or trifluoromethyl, or when taken together, form methylenedioxy; R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or dimethylamino; and R.sub.4 is hydrogen or halogen, which comprises cyclizing a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with an acidic condensing agent.The indole derivatives of the formula (I) mentioned above are useful as a key intermediate for the preparation of benzodiazepines, which are useful as tranquilizers, muscle relaxants and the like.