摘要:
Described is a pyridine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 individually represent H, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkoxyalkyl group which may have a substituent, a carboxyalkyl group, an alkoxycarbonylalkyl group, an aralkyl group which may have a substituent, a phenacyl group or an acyl group, R.sup.3 represents an alkyl group, a phenyl group which may have a substituent, a heteroaryl group or a cyclic amino group, X represents O or combination of OH and H, or a salt thereof; and a medicament, such as cytokine production suppressant, comprising the derivative or salt thereof as an effective ingredient. The invention compound has potential, highly specific and highly safe immunoregulating capacity so that it can suppress the excessive production of a specific cytokine in various diseases related to the immune system.
摘要:
Disclosed herein are an imidazole derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonyl group, and R.sup.2, R.sup.3 and R.sup.4 are the same or different from one another and are independently a hydrogen or halogen atom, an alkyl, halogenoalkyl, hydroxyl or alkoxy group, or the like, or a salt thereof, and a medicine comprising such a compound. The compound specifically suppresses the production of particular cytokine and is hence useful as an active ingredient for immune function modulators and the like.
摘要:
The present invention relates to a substituted vinylpyridine derivative represented by the following formula (1): ##STR1## (wherein R.sup.1 represents a hydrogen atom, an alkyl group, etc., R.sup.2 represents an alkyl group; one of R.sup.3 and R.sup.4, which are different from each other, represents a hydrogen atom and the other represents a nitrile group, R.sup.5 represents an aryl group or a heteroaryl group, X represents an oxygen atom, etc., and one of Q.sup.1, Q.sup.2, and Q.sup.3 represents a nitrogen atom and the other two represent CH); a salt of the derivative; and a drug containing the derivative or salt as the active ingredient. Due to strong PDE inhibitory action and TNF-.alpha. production inhibitory action, the derivative, salt, and drug are useful for the prevention and treatment of a wide variety of inflammatory diseases and autoimmune diseases.
摘要:
Quinoline derivatives of the formula, ##STR1## wherein > A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.
摘要:
Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.
摘要:
Imidazole derivatives of the formula (1) or salts thereof, pharmaceuticals containing the derivatives or the salts, and intermediates for the synthesis of the derivatives or the salts (wherein R1 is lower alkyl; R2 is alkyl or aralkyl; and X1 is halogeno). These compounds exhibit G-CSF-like activities and can be substituted for G-CSF preparations.
摘要翻译:式(1)的咪唑衍生物或其盐,含有衍生物或盐的药物,以及用于合成衍生物或盐的中间体(其中R 1为低级烷基; R 2为烷基或芳烷基; X 1为卤素)。 这些化合物表现出G-CSF样活性,可代替G-CSF制剂。
摘要:
A pyrrole derivative having excellent anti-microbial activities is disclosed. This compound is represented by the following formula (I): ##STR1## wherein X.sub.1 and X.sub.2 are the same or different and mean individually a halogen atom, R.sub.1 denotes an alkyl, cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl group or a group --COR.sub.3 in which R.sub.3 is an alkyl group having at least five carbon atoms or a cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl, or heterocyclic group, and R.sub.2 stands for a hydrogen or halogen atom or an alkyl group, with a proviso that R.sub.1 is other than a hydrogen atom or methyl group when X.sub.1, X.sub.2 and R.sub.2 are each a bromine atom.
摘要:
Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1 and R2 are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3 represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4 and R5 each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9 or —OCOR10 (in which R6, R9 and R10 each independently represents a hydrogen atom, a lower alkyl group, or the like, R7 and R8 are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.
摘要翻译:描述了由下式(1)表示的4-羟基-4-苯基哌啶衍生物:[其中,R 1和R 2相同或不同,各自独立地表示氢原子,低级烷基等,R 3表示 氢原子或基团 - (CR 4 R 5)n Y(其中,R 4和R 5各自表示氢原子或低级烷基,Y表示-COOR 6,-CONR 7 R 8,-OR 9或-OCOR 10(其中R 6,R 9和 R 10各自独立地表示氢原子,低级烷基等,R 7和R 8相同或不同,各自独立地表示氢原子,低级烷基等),n表示1〜6 )]或其盐。该化合物表现出优异的外周镇痛作用。
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.