摘要:
Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
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:
There is disclosed a process for preparing 5-mercapto-1,2,3-thiadiazole salts comprising reacting a hydrazone compound represented by the formula:X.sub.3 C--CH.dbd.N--NH--SO.sub.2 Arwherein X represents a halogen atom and Ar represents an aryl group, with a polysulfide compound represented by the formula:M.sub.2 S.sub.xwherein M represents an alkali metal atom or an NH.sub.4 group and x is an integer of 2 to 6.The present invention provides the 5-mercapto-1,2,3-thiadiazole salt with remarkably increased yield as compared with the conventional method.
摘要:
There is disclosed a process for the preparation of a 2-alkyl-4-amino-5-aminomethylpyrimidine, which comprises subjecting a 2-alkyl-4-amino-5-formylpyrimidine to catalytic reaction with hydrogen and ammonia in the presence of a reduction catalyst.According to the process of this invention, the desired product can be obtained in much higher yield as compared with the processes known to the art.