Abstract: Disclosed are a compound represented by formula (1) and a non-toxic salt thereof, a production method thereof, and a pharmaceutical composition for treating a serotonergic neuron-related disease comprising the same as an active ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents a pyridyl group which is unsubstituted or substituted with 1 to 3 substituents each independently selected from the group consisting of a halogen atom, a lower alkyl group, a trifluoromethyl group, a lower alkoxy group, a carbamoyl group and a cyano group, or a pyrimidinyl group which is unsubstituted or substituted with 1 to 2 substituents each independently selected from the group consisting of a lower alkyl group and a lower alkoxy group; and n is an integer of from 2 to 5.

Abstract: A compound of the formula ##STR1## wherein A is adenine-9-yl and X is halogen, Preferably iodine, or a pharmaceutically acceptable salt thereof. It is a novel derivative of neplanocin A and has almost the same level of cytotoxic activity. However, it is not inactivated by the action of adenosine deaminase. It is produced by replacing a hydroxyl at position-6' in neplanocin A or 2', 3'-O-protected neplanocin A with halogen by use of a halogenating agent, and when hydroxyl at position-2' or -3' is protected, removing the protective group thereof.

Abstract: An aldose reductase inhibitor, comprising a compound of the formula (I) ##STR1## or a pharmaceutically acceptable salt thereof as the effective component, in which R is lower alkyl or cyclohexylmethyl and n is 2 or 3. The compounds of formula (I) and salts thereof according to the invention exhibit a superior aldose reductase inhibiting activity with simultaneous high stability, so that they are useful for the prevention and therapy of diabetic complications.

Abstract: An aldose reductase inhibitor, comprising a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof as the effective component, in which R denotes an alkyl of C.sub.1-12, ##STR2## wherein X.sub.1 and X.sub.2 are same or different and are hydrogen or halogen, cyclohexylmethyl, cyclohexyl, tetra-hydro-2H-pyran-1-yl-methyl, carboxy-lower alkyl or cyclo-lower alkyl and n is 2 or 3. These compounds exhibit a superior aldose reductase inhibiting activity with simultaneous high stability, and are for use in the prevention and therapy of diabetic complications.

Abstract: A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## is dilower alkylamino, cycloalkylamino, morpholino, ##STR3## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.

Abstract: A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## in which ##STR3## is dilower alkylamino, cycloalkylamino, morpholino, ##STR4## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.

Abstract: 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanocyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

Abstract: 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of 1-methyltetrazole-5-yl-thio, 1-imidazolyl, morpholino, ##STR2## in which R.sub.5 is hydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A and R.sub.1 are as defined above, R.sub.2 and R.sub.3 are each lower alkyl or together form tetramethylene, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

Abstract: A compound of the formula ##STR1## wherein Z is N or NH, is a single or double bond, R.sub.1 is hydrogen, C.sub.1-20 alkyl or optionally substituted phenyl, A is lower alkylene, R is carboxyl, lower alkoxycarbonyl, ##STR2## or 1-cycloalkyl-tetrazole-5-yl, R.sub.2 is lower alkyl, hydroxy-lower alkyl or optionally substituted phenyl-lower alkyl, R.sub.3 is lower alkyl or cycloalkyl, or R.sub.2 and R.sub.3 together constitute ##STR3## and R.sub.5 and R.sub.6 are hydrogen or optionally substituted phenyl, or a pharmacologically acceptable salt thereof, has platelet aggregation inhibitory activity and/or cyclic AMP/phosphodiesterase inhibitory activity.

Abstract: 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanoyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkoxy or halogen, and A is lower alkylene, or a pharmacologically acceptable salt thereof, has sympatholytic .alpha.-receptor blocking activity and is useful for the treatment of hypertension.

Abstract: 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof.

Abstract: A method for inhibiting blood platelet aggregation in humans, and promoting vasodilation in humans, by administering to a human in need of the same an effective amount of 2-hydroxy-3-isopropyl-5,6-dimethylpyrazine or a hydrate or a pharmaceutically acceptable non-toxic salt thereof. Administration can be orally in an amount of about 0.02-12 mg/kg body weight per day, or parenterally in an amount of about 0.01-6 mg/kg of body weight per day.

Abstract: Cephalosporins having a sulfur-containing functional group of the formula ##STR1## present at the carbon atom directly bonded to the thienyl or furyl group in the side chain of the 7-position of cephem derivatives. These compounds are useful as anti-bacterial agents against Gram-positive and Gram-negative bacteria.