| abstract |
Carbostyril and oxindole derivs. of formula (I) are new: (W is vinylene (opt. substd. by a methyl gp.), methylene or ethylene; m is 0, 1 or 2; D is opt. branched 2-6C alkylene or 3-6C hydroxyalkylene or xylylene; R1 is H or 1-3C alkyl; R2 is 3-6C cycloalkyl, 6-10C aryl, 7-11C aralkyl, 4-9C heteroaryl contg. one N atom and/or one O or S atom or two N atoms or 5-10C heteroaralkyl; all aromatic rings are opt. substd. by a 1-4C alkyl, OH, OMe, NH2, MeCONH, NO2, CO2H, cyclohexyl, phenyl or halo gp. and opt. further substd. by one or two 1-4C alkyl or halo gps., substituents being same or different; R2 may also be 1,2,4-triazolyl, CPh3, 4,5-bis-(p-chlorophenyl)-oxazol-2-yl, N-methyl-N-cyclohexyl-carbamoylmethyl or amino-iminomethyl, and may additionally be 1-6C alkyl when either m is 1 or D is opt. branched 3-6C hydroxyalkylene or xylylene; R3 and R4 are same or different H, halogen, 1-4C alkyl, NH2, MeCONH or NO2). (I) have positive inotropic and antithrombotic activity. They can be used for prophylaxis of thromboembolic diseases such as coronary infarct, cerebral infarct, transient ischaemic attacks and Amaurosis fugax, and for prophylaxis of arteriosclerosis. Daily dose is 100-300 mg.LD50 is >1g/kg mouse p.o. |