摘要:
A benzoazine derivative represented by the following formula (1), ##STR1## wherein R.sup.1 represents an alkyl group, alkoxy group, halogen atom, halogenoalkyl group, amino group, hydroxy group, benzyloxy group which may have a substituent, cyano group, carbamoyl group, acyl group, nitro group, carboxy group, or sulfonamide group; R.sup.2 and R.sup.3 may be the same or different and each individually represents a hydrogen atom or an alkyl group, or R.sup.2 and R.sup.3 indicate in combination an alkylene group having 2-7 carbon atoms; R.sup.4 and R.sup.5 may be the same or different and each individually represents a hydrogen atom or an alkyl group; X denotes O, S, or N--R.sup.6 (wherein R.sup.6 represents a hydrogen atom, an alkyl group, or an aryl group or pyridyl group which may have a substituent); m is an integer from 0 to 4; and n is an integer from 1 to 3, or a salt of the benzoazine derivative. The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity.
摘要翻译:由下式(1)表示的苯并嗪衍生物,其中R1表示烷基,烷氧基,卤素原子,卤代烷基,氨基,羟基,可具有取代基的苄氧基,氰基 ,氨基甲酰基,酰基,硝基,羧基或磺酰胺基; R2和R3可以相同或不同,各自独立地表示氢原子或烷基,或R2和R3组合表示具有2-7个碳原子的亚烷基; R 4和R 5可以相同或不同,各自独立地表示氢原子或烷基; X表示O,S或N-R6(其中R6表示氢原子,烷基或可具有取代基的芳基或吡啶基); m为0〜4的整数; n为1〜3的整数,或苯并嗪衍生物的盐。 该化合物对于降低血糖值,血浆胰岛素值和血浆甘油三酯值具有优异的效果,并且可用作预防或治疗糖尿病,高脂血症和肥胖症的药物。
摘要:
Disclosed are chromene derivatives represented by the following formula: ##STR1## wherein R.sup.1 s represent alkyl, alkoxy or like groups, R.sup.2 represents a hydrogen atom or an alkyl group, R.sup.3 represents a substituted or unsubstituted phenyl, naphthyl or heterocyclic group, and m stands for an integer of from 0 to 4, and their salts; and pharmaceuticals containing them as effective ingredients. The chromene derivatives and their salts show excellent AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.
摘要:
A 8-piperazinyl-1,7-naphthyridine derivative represented by the following formula (I): ##STR1## in which R represents a hydrogen atom, formyl group, acyl group, aroyl group, heteroaroyl group, substituted phenyl group, pyridyl group, aralkyl group or substituted or unsubstituted benzenesulfonyl group; and an acid adduct salt thereof. The compound has excellent antiinflammatory, antiarrhythmic and cardiotonic effects, and thus is useful as an antiinflammatory drug and a medicine for circulatory organs.
摘要:
Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.
摘要:
The invention is directed to an imidazole derivative represented by formula (1): wherein each of R1 and R2 represents an aryl group, a heteroaryl group, etc.; each of A, X1, and X2 represents N or CH; each of Y and Z represents O, S, etc.; each of R3, R4, and R5 represents a hydrogen atom, an alkyl group, etc.; m is a number of 1 to 4; and n is a number of 0 to 4, or a salt thereof. The invention is also directed to a drug containing the derivative or the salt as an active ingredient. These compounds exert excellent effects of inhibiting production of NO and IL-6 and are useful for preventing or treating diseases induced by overproduction of NO and IL-6.
摘要:
Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): wherein R1 means an aryl or heteroaryl group which may have at least one substituent, R2 denotes an alkyl, alkenyl or aralkyl group, R3 stands for a hydrogen atom or an alkyl group, and R4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.
摘要:
Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 means an aryl or heteroaryl group which may have at least one substituent, R.sup.2 denotes an alkyl, alkenyl or aralkyl group, R.sup.3 stands for a hydrogen atom or an alkyl group, and R.sup.4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.
摘要:
Described is an arylacetic amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents an aryl group or the like, R.sup.2 and R.sup.3 each independently represents an alkyl group, a cycloalkyl group or the like, and R.sup.4 represents an aralkyl group, an alkyl group or the like; or salt thereof. The compound according to the present invention has both excellent anticholinergic action and calcium antagonism and at the same time has high selectivity to bladder, so that it is useful as a preventive or remedy for urinary disorders.
摘要:
Substituted quinolone derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted (hetero)aryl group, R.sup.2 represents H or an alkoxycarbonyl, substituted aminocarbonyl, cyano or like group, and R.sup.3 and R.sup.4 each independently represent H or a substituted alkyl, aryl, amino or like group, and salts thereof; pharmaceuticals containing the same. These derivatives and salts have excellent anti-ulcer activities.
摘要:
Certain 1,7-naphthyridine derivatives and their acid addition salts have strong antiarrhythmic effects, cardiotonic effects, diuretic effects, bronchodilation effects, anti-acetylcholine effects, anti-inflammatory effects, analgesic effects and the like and are hence useful for various diseases such as heart diseases, hypertension, asthma, arthritis, lumbago, toothache, etc.