摘要:
A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
摘要:
A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
摘要:
A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
摘要:
[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.
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.
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## (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.