Abstract: An isoquinolinesulfonyl compound represented by the formula (I): ##STR1## wherein R.sup.1 : H, Cl, OHA : unsubstituted or substituted ethylene or alkyleneR.sup.2, R.sup.3 : H, alkyl, jointly forming unsubstituted or substituted ethylene or trimethyleneR.sup.4 : H, alkyl, amidinoor an acid salt thereof.They can be prepared, for example, by converting 1-R.sup.1 substituted-5-isoquinolinesulfonic acid to the corresponding sulfonyl chloride and subsequently reacting the chloride with a compound of formula ##STR2## They can be advantageously utilized as vasodilator, cerebral circulation ameliorator, antihypertensive agent and drugs for prevention and treatment of various circulatory organ diseases.

Abstract: This invention relates to novel isoquinolinesulfonamide derivatives of Formula (I): ##STR1## wherein A is a C.sub.0-10 alkylene group or a C.sub.0-10 alkylene group having a C.sub.1-10 alkyl group, a phenyl group, a substituted phenyl group or a phenylalkyl group; R.sub.1 and R.sub.2 each is a hydrogen atom; or R.sub.1 and R.sub.2 are linked directly to form an ethylene group unsubstituted or substituted with a C.sub.1-4 alkyl group;R.sub.3 and R.sub.4 each is a hydrogen atom, a C.sub.1-6 alkyl group or linked directly to form a C.sub.2-6 alkylene group; and the pharmaceutically acceptable acid addition salt thereof, and to a process for preparing them. The isoquinoline derivatives possess a relaxatory action for vascular smooth muscle and action for increasing blood flow and are useful as a vasodilator and a hypotensor.

Abstract: A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.

Abstract: A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one;m and n each is an integer of one to nine;m+n is an integer of at least one;R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; orR.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group;R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR3## wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof.

Abstract: A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.

Abstract: A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## group wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## group in ##STR4## group may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent;Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group;Z.sub.2 is a hydrogen atom or an amino group;when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.

Abstract: A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one;m and n each is an integer of one to nine;m+n is an integer of at least oneR.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; orR.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group;R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; orthe ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.

Abstract: A 6-quinazolinesulfonyl derivative of Formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1-12 alkyl group:R.sub.2 is a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.4-10 cycloalkyl group, an aryl group or an aralkyl group; andR.sub.1 and R.sub.2 may be linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring together with the adjacent nitrogen atom; andR.sub.3 is a ##STR2## group wherein R.sub.4 is a C.sub.1-8 alkyl group; a --HN(CH.sub.2).sub.n NH.sub.2 group wherein n is an integer of 2 to 10; or a ##STR3## group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

Abstract: A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## group wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## group wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.

Abstract: A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one;m and n each is an integer of one to nine;m+n is an integer of at least one;R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; orR.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group;R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; orthe ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, and aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.

Abstract: This invention relates to a tetrazole-5-thiol ester having D-configuration of the formula, ##STR1## a process for the preparation of the thiol ester and a process for the preparation of cefamandole using the thiol ester.

Abstract: This invention relates to a tetrazole-5-thiol ester having D-configuration of the formula, ##STR1## a process for the preparation of the thiol ester and a process for the preparation of cefamandole using the thiol ester.

Abstract: A method for preparing a cephalosporin compound represented by the general formula (III) ##STR1## (wherein R represents hydrogen or methyl group) or a pharmaceutically acceptable salt thereof, which is characterized by reacting 7-amino-3-(benzimidazol-2-yl)-thiomethyl-3-cephem-4-carboxylic acid represented by the general formula (I) ##STR2## or a salt thereof with a compound represented by general formula (II) ##STR3## wherein R represents hydrogen or methyl group.

Abstract: Novel substituted phenylglycolic acid represented by the formula ##STR1## AND ITS PHARMACEUTICALLY ACCEPTABLE NON-TOXIC ESTERS AND SALTS HAVE POTENT ANALGESIC, ANTI-INFLAMMATORY AND ANTIPYRETIC ACTIVITIES, A LOW TOXICITY AND A SATISFACTORY THERAPEUTIC INDEX, AND CAN BE FAVORABLY EMPLOYED AS A MEDICINE FOR TREATMENT OF VARIOUS INFLAMMATORY DISEASES SUCH AS ARTHRITIS, COMMON COLD, RHEUMATISM AND LIKE INFLAMMATIONS AND ALSO FOR ANALGESIC AND ANTIPYRETIC PURPOSES. The substituted phenylglycolic acid is prepared by reacting a lower alkyl ester of 2-(2,6-dichloroanilino)phenylglycolic acid with a basic substance, which lower alkyl ester is also a novel compound and can be obtained starting from 1-(2,6-dichlorophenyl)indole-2,3-dione through 2-(2,6-dichloroanilino)phenylglyoxylic acid and, in turn, a lower alkyl ester of 2-(2,6-dichloroanilino)-phenylglyoxylic acid.

Abstract: Process for preparing N.sub.1 -(2'-furanidyl)-5-fluorouracil having effective pharmacological activities such as anti-leukemia and anti-tumor activities comprising reacting 2,4-bis(trialkylsilyl)-5-fluorouracil with 2,3-dihydrofuran in the presence of a proton donor and a catalyst. Such process can be simply, easily conducted to give the desired product having a high purity in good yield.