摘要:
The present invention provides novel benzimidazole derivatives or salts thereof represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom or a halogen atom; R.sup.2 is a phenyl-lower alkyl group; R.sup.3 is a heterocyclic group selected from the group consisting of an indolyl group, indolinyl group, 1H-indazolyl group, 2(1H)-quinolinonyl group, 3,4-dihydro-2(1H)-quinolinonyl group and 1,4-benzoxazinyl group; A is a lower alkylene group; n is 0 or 1.The benzimidazole derivatives or salts of the present invention are effective agents for treating various arteriosclerotic diseases.
摘要:
A carbostyril derivative or salt thereof of the formula ##STR1## the carbon-to-carbon bond between the 3- and 4-positions of the carbostyril skeleton being a single bond or a double bond. The carbostyril derivatives are useful as a platelets aggregation inhibitory agent.
摘要:
The present invention provides a carbostyril derivative represented by the following general formula ##STR1## (wherein A, R and W have the same definitions as given above; and the carbon-to-carbon bond between the 3- and 4-positions of the carbostyril skeleton represents a single bond or a double bond.Said carbostyril derivative is useful as a platelets aggregation inhibitory agent.
摘要:
The present invention provides an agent for inhibiting skin erythema and/or skin pigmentation, containing at least one selected from the group consisting of the carbostyril derivative and salt thereof represented by the general formula, ##STR1## (wherein R.sup.1 is a hydrogen atom, a lower alkyl group or the like; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group or the like; R.sup.3 and R.sup.4 are lower alkyl groups which may have hydroxyl groups as substituents or the like; the carbon--carbon bond between 3- and 4-positions in the carbostyril skeleton is a single bond or double bond).
摘要:
Carbostyril derivatives and salts thereof represented by the general formula (1a), including some known compounds, possess activities for inhibiting adhesion of thrombocytes. ##STR1## Z, A, X, R, R.sup.1 and R.sup.2 are defined in the specification. Some carbostyril derivatives having chemical structural formulas similar to those of carbostyril derivatives and salts thereof represented by the general formula (1a) have been known in prior art references, however the above-mentioned pharmacological activities have not been known to the present date.
摘要:
The novel carbostyril derivative represented by the general formula (1) ##STR1## [in the formula, A, R.sup.1, R.sup.2 and the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton have the same definitions as above] has an excellent platelet aggregation inhibitory activity, a phosphodiesterase inhibitory activity, a venticular contraction activity (a positive contraction activity), an anti-ulcer activity, an anti-inflammatory activity, a cerebral blood flow increasing activity, a thrombus dissociation activity, a thromboxane A.sub.2 antagonism activity, etc. The carbostyril derivative of the present invention is characterized in that it exhibits the above activities for a long time, is low in toxicity (particularly low in toxicity to hearts of cardiovascular hyperplasia, myocardipathy, etc.), and is low in circulation activities such as heart rate increasing activity, blood pressure decreasing activity and the like. Also, the carbostyril derivative of the present invention has advantages in that it is easily absorbed by the intestinal tract and easily migrates into blood. Therefore, the carbostyril derivative of the present invention can be used most suitably as a preventive and remedy for thrombi such as apoplexia, cerebral infarction, myocardial infarction and the like, a cerebral circulation improving agent, an anti-inflammatory agent, an anti-asthmatic agent, a cardiotonic agent and a phosphodiesterase inhibitory agent.
摘要:
Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio, l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 and R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.
摘要:
The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.
摘要:
The present invention provides novel cyclic amide derivatives having activity for protecting against the ultraviolet rays, activity for scavenging active oxygen species and activity for inhibiting the formation of lipid peroxides, which is represented by the following general formula (1): ##STR1## wherein R.sup.2 is a hydroxyl group, a lower alkenyloxy group, a phenyl-lower alkenyloxy group, a cycloalkenyloxy group, a tetrahydropyranyloxy group, a pyridyloxy group, or a lower alkanoyloxy group which may have carboxyl group(s).