摘要:
Carbostyril compounds represented by the formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a phenylalkyl group, R.sub.2 represents an alkenyl group, an alkoxyalkyl group, a hydroxyalkyl group, a carboxyalkyl group, an alkylcarbonyl group, a cycloalkylcarbonyl group, an alkylcarbonylalkyl group, an alkoxycarbonylalkyl group, an alkynyl group or a carbamoylalkyl group, R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxyalkyl group, an alkenyl group, a phenylalkyl group, a phenoxyalkyl group or a phenyl group, and the 3,4-bond of the carbostyril nucleus represents a single or double bond, pharmaceutically acceptable salts thereof, and a process for preparing the same.
摘要:
Novel tetrazolylalkoxycarbostyril derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a low alkenyl group, a lower alkanoyl group, a benzoyl group or phenylalkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## R.sup.3 is a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, a phenyl group or a phenylalkyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is either single or double bond; and the substituted position of a group of the formula, ##STR3## in the carbostyril skeleton is either 4-, 5-, 6-, 7- or 8-position provided that the only one such group of the formula can be substituted in the whole carbostyril skeleton, thus when R.sup.2 in 4-position is a group of the formula ##STR4## then 5-, 6-, 7- or 8-position will have no such substituted group; furthermore, the phenyl group in the above-mentioned benzoyl group, phenylalkyl group or phenyl group may have substituted group(s).The above-mentioned novel tetrazolylalkoxycarbostyril derivatives have pharmacological activities such as platelet aggregation inhibitory action, antiinflammatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful as anti-thrombosis agent, cerebral blood flow improving agent, antiinflammatory agent, antiulcer agent, anti-hypertensive agent and anti-asthmatic agent.
摘要:
Novel compounds represented by the formula ##STR1## wherein R.sup.1, R.sup.2, and R' and R" are defined as hereinafter, having a blocking activity on .beta.-adrenergic nerves, novel intermediates useful for synthesis thereof and processes for preparing the same are disclosed. When substitution is at the 5-position and R.sup.1 and R.sup.2 are hydrogen, R' and R" are not simultaneously hydrogen and a 1 to 4 carbon atom alkyl group in the claimed compound.
摘要:
Carbostyril derivative represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group; R.sup.4 represents a hydrogen atom or an alkyl group, R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, an alkyl group, a cycloalkyl group, or a phenylalkyl group, or R.sup.5 and R.sup.6 may, when taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen or oxygen atoms as hetero atoms; and the ring A has a partial structure: ##STR2## wherein R.sup.3 represents a hydrogen atom, a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group, with the proviso that at least one of R.sup.1, R.sup.2 and R.sup.3 when R.sub.3 is present, or at least one of R.sub.1 and R.sub.2 when R.sub.3 is absent, represents a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group; the pharmaceutically acceptable acid addition salts of the above carbostyril compounds represented by the formula (I), and processes for preparing the above carbostyril compounds represented by the formula (I).
摘要:
A glycerol derivative represented by the formula (I) ##STR1## wherein A is hereinafter defined, including the optically active isomers per se and mixtures of the optically active isomers, which are useful as a central nervous system depressant, an intermediate for the preparation of .beta.-adrenergic blocking agents, an inhibitor of blood platelet aggregation or a choleretic agent, and a process for preparing the above glycerol derivative.
摘要:
5-[1-Hydroxy-2-(substituted-amino)]alkyl -8-hydroxy-carbostyril derivatives represented by the formula (I) ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 4 carbon atoms and R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group containing a straight or branched chain alkyl moiety having 1 to 4 carbon atoms or a cycloalkyl group having 4 to 6 carbon atoms, or R.sup.2 and R.sup.3 may, when taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen, oxygen or sulfur atoms as hetero atoms, the pharmaceutically acceptable acid addition salts thereof, and a process for preparing the same.
摘要:
2-Hydroxy-3-alkylaminopropoxycarbostyrils represented by the formula (I) ##SPC1##wherein R represents a straight or branched chain alkyl group having 1 to 4 carbon atoms useful as .beta.-adrenergic blocking agents and a process for preparing the same are disclosed.