摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.
摘要:
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.1-8 alkyl 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.
摘要:
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.1-8 alkyl 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.
摘要:
A method of producing Nb3Sn superconducting wire, including the steps of: preparing a plurality of Sn modules obtained by burying Sn-based metal cores in a Cu-based metal matrix and a plurality of Nb modules obtained by burying Nb-based metal filaments in a Cu-based metal matrix; bundling the Nb modules and the Sn modules such that the Nb modules surround the Sn modules and obtaining an assembly; inserting the assembly in a tubular member of Cu-based metal which internally comprises tube-like shaped Ta-based metal or Nb-based metal which serves as a diffusion barrier and obtaining a composite; drawing the composite; and heat-treating the composite.
摘要:
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.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## group; and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## group; and the pharmaceutically acceptable acid addition salt thereof having antiinflammatory, analgesic and digestive tract ulcer suppressing activity.
摘要:
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.