摘要:
A cyclic amine derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a substituted of unsubstituted C.sub.1 -C.sub.8 aliphatic acyl group, a substituted or unsubstituted benzoyl group or a C.sub.1 -C.sub.4 alkoxycarbonyl group, and R.sup.3 represents a substituted 3 to 7 membered saturated cyclic amino group which may form a fused ring; or pharmaceutically acceptable salts thereof. The compounds and salts have excellent platelet aggregation inhibitory action. They are useful for the treatment and prevention of such diseases as embolism, thrombosis or arteriosclerosis and for the preparation of pharmaceutical compositions for such uses.
摘要:
A cyclic amino compound represented by the following formula: or a pharmacologically acceptable salt thereof. R1 is a substitutable phenyl group. R2 is a substitutable aliphatic acyl group, a substitutable benzoyl group or an alkoxycarbonyl group. R3 is a substituted, saturated cyclic amino group which may optionally have a fused ring. These compounds and salts have excellent platelet aggregation inhibitory action. They are useful for the prevention and/or treatment of embolism, thrombosis or arteriosclerosis and other conditions resulting from platelet aggregation.
摘要:
Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.
摘要翻译:式(I)化合物:其中R1是氢,烷基,卤素,卤代烷基,羟基,烷氧基,卤代烷氧基,烷硫基,卤代烷硫基,氨基,烷酰基,卤代烷酰基,羧基,烷氧基羰基,氨基甲酰基,氰基,硝基, 烷磺酰基,卤代烷磺酰基或氨磺酰基; R 2是5,6-二氢-1,4,2-二恶嗪-3-基; R3是氢,羟基,任选取代的烷氧基,芳烷氧基,烷酰氧基,烯酰基氧基,环烷基羰基氧基,芳基羰基氧基,烷氧基羰基氧基,芳烷氧基羰基氧基,邻苯二甲酰氧基,(5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基)甲氧基,(5- 苯基-2-氧代-1,3-二氧杂环戊烯-4-基)甲氧基,任选取代的氨基或硝基; Y是-NH-或氧或硫; n为1至5; 和所述式(I)化合物的互变异构体和盐具有抑制血小板聚集的能力,因此可用于治疗和预防血栓形成和栓塞。
摘要:
Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted cycloalkylcarbonyl, substituted benzoyl, or 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.
摘要翻译:式(I)化合物:(*化学结构*)(I)其中:R1是氢,烷基,卤素,卤代烷基,羟基,烷氧基,卤代烷氧基,烷硫基,卤代烷硫基,氨基,烷酰基,卤代烷酰基,羧基,烷氧基羰基,氨基甲酰基, 氰基,硝基,烷磺酰基,卤代烷磺酰基或氨磺酰基; R 2是任选取代的烷酰基,任选取代的烯酰基,任选取代的环烷基羰基,取代的苯甲酰基或5,6-二氢-1,4,2-二恶嗪-3-基; R3是氢,羟基,任选取代的烷氧基,芳烷氧基,烷酰氧基,烯酰氧基,环烷基羰基氧基,芳基羰基氧基,烷氧基羰基氧基,芳烷氧基羰基氧基,邻苯二甲酰氧基,(5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基)甲氧基,(5- 苯基-2-氧代-1,3-二氧杂环戊烯-4-基)甲氧基,任选取代的氨基或硝基; Y是-NH-或氧或硫; n为1至5; 和所述式(I)化合物的互变异构体和盐具有抑制血小板聚集的能力,因此可用于治疗和预防血栓形成和栓塞。
摘要:
A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
摘要:
A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
摘要:
A method for the prevention of diseases caused by thrombus or embolus. The method is to separately administer 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, in their pharmacologically effective amounts, to a warm-blooded animal.
摘要:
A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
摘要:
A method for the prevention of diseases caused by thrombus or embolus. The method is to separately administer 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, in their pharmacologically effective amounts, to a warm-blooded animal.
摘要:
Acid addition salts of 2-acetoxy-5-(&agr;-cyclopropyl-carbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]-pyridine. The acid addition salts of tetrahydrothienopyridine derivatives of the present invention exhibit excellent oral absorption, metabolization into the active compound, and platelet aggregation-inhibiting effects, low toxicity, and excellent storage and handling stabilities, and are useful as medicaments, preferably preventive or therapeutic agents (particularly therapeutic agents) for diseases caused by a thrombus or an embolus, still more preferably preventive or therapeutic agents (particularly therapeutic agents) for thrombosis or embolism.