摘要:
Diazabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, oxoalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyl, dialkylaminoalkyl, hydroxyalkyl, haloalkyl, cyanoalkyl, heterocycloalkyl, aryl, heteroarylalkyl or arylalkyl, the aryl group and the aryl moiety being optionally substituted by alkoxy, nitro, alkyl, amino or halo;R.sup.2 is hydrogen or alkyl;R.sup.3 and R.sup.4 may be the same or different and each is hydrogen, alkyl, alkenyl, acyl, alkoxyalkyl or arylalkyl wherein the aryl moiety is optionally substituted by alkoxy, nitro, alkyl, amino or halo;with the proviso that when R.sup.2 is hydrogen and both R.sup.3 and R.sup.4 are methyl, R.sup.1 does not represent hydrogen, alkyl, unsubstituted benzyl or dimethylaminoethyl; having 5-HT.sub.3 receptor antagonist activity.
摘要:
Compounds of formula (I) and pharmaceutically acceptable salts thereof are selective agonists for 5-HT.sub.4 receptors. ##STR1## wherein Ak is a C.sub.3 -C.sub.6 alkyl group, and R is a C.sub.2 -C.sub.6 alkyl group, a C.sub.3 -C.sub.6 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.3 -C.sub.7 cycloalkyl group or a C.sub.3 -C.sub.6 cycloalkylmethyl group.
摘要:
Pyrimidine derivatives useful as a gastrointestinal prokinetic agent, represented by formula ##STR1## wherein X is O or NR.sup.5, Y is O, S or NR.sup.5 wherein R.sup.5 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or the like; R.sup.1 and R.sup.2 may be the same or different and each is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or the like; R.sup.3 is CN, or COOR.sup.6 wherein R.sup.6 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group, an aryl group or the like; R.sup.4 is --SR.sup.7 or --NR.sup.8 R.sup.9 wherein R.sup.7 is a C.sub.1 -C.sub.6 alkyl group; R.sup.8 is a C.sub.1 -C.sub.6 alkyl group or the like; R.sup.9 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or the like, or R.sup.8 and R.sup.9 may represent, together with the nitrogen atom to which they are attached, an N-substituted piperazine ring of formula (X) ##STR2## wherein R.sup.10 represents a C.sub.1 -C.sub.6 alkyl group or the like or a pharmacologically acceptable salt thereof. The above-mentioned compounds are useful as a gastrointestinal prokinetic agent used for the therapy of digestive tract diseases.
摘要:
Novel diaminomethylidene derivatives represented by formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group and others, R.sup.2 is a group of the following formula ##STR2## and others, R.sup.3 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group and others, X is O, S, CHNO.sub.2, C(COOR.sup.4).sub.2, C(COOR.sup.4)CN or C(CN).sub.2) or pharmacologically acceptable salts thereof. The above-mentioned compounds are useful as a gastrointestinal prokinetic agent to be used for the treatment of digestive tract diseases.
摘要:
An indazole compound having a piperazinyl moiety in the structure thereof, which is a 5-HT.sub.4 receptor agonist which is useful in the treatment of digestive tract disorders.
摘要:
An indazole compound having the formula (I): wherein:R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 cycloalkyl;Q is carbonyl, thiocarbonyl or methylene; andR.sub.2 is a group of the formula (II) or (IV); ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or benzyl, of which a phenyl group thereof is optionally mono- or di-substituted by the same or different halogen or methoxy; m is 0 to 2; n and o is 1 or 2. The compound exhibits 5-HT.sub.4 receptor agonist activity.
摘要:
An image forming apparatus includes a latent image bearer, a latent image writing device, a developing device, a conveyance unit to convey a recording medium, a transfer device, a length data acquisition unit to obtain a length of the recording medium in a conveyance direction of the recording medium, an image forming processor to form a test pattern, and a light quantity correction calculator that acquires image density data of the test pattern and calculates a light quantity correction value to correct a light quantity. The image forming processor sets a position of the test pattern on the recording medium in the conveyance direction of the recording medium and a length of the test pattern in the conveyance direction of the recording medium based on the length of the recording medium in the conveyance direction of the recording medium obtained by the length data acquisition unit.
摘要:
The invention is concerning the writing controlling apparatus that includes an acquiring unit configured to acquire a plurality of light amounts of a light source driven while changing an input current in non-effective scanning periods during which an image carrier is not irradiated with light from the light source, as a plurality of output results; a detecting unit configured to detect characteristics of the light source using the output results thus acquired; and a correcting unit configured to correct a current to be applied to the light source based on the characteristics thus detected.
摘要:
Using betaKlotho or a substance that increases or inhibits betaKlotho activity as an agent for controlling the activity of FGF21 mediated by an FGF receptor, the present invention provides a pharmaceutical composition comprising such betaKlotho or such substance as an active ingredient, particularly, a pharmaceutical composition for anti-metabolic syndrome, and further particularly, a pharmaceutical composition for therapeutic or preventive use associated with the control of blood glucose level. In addition, the present invention provides a screening system for each of a substance that enhances or suppresses betaKlotho activity, an FGF21-like active substance, and a betaKlotho-like active substance, which uses a cell system that has expressed an FGF receptor and/or betaKlotho on the surface thereof.
摘要:
Disclosed is an agent for skin external preparation which is hardly reduced in viscosity even when stored for a long period under extreme high temperature storage conditions and is therefore stable. The preparation is in an emulsion form, and comprises (1) an alginic acid polyol ester having an esterification degree ranging from 75 to 95% (e.g., alginic acid propylene glycol ester) and/or a salt thereof; (2) a polyvalent metal ion (e.g., a calcium ion); and (3) a 4-alkylresolcinol (e.g., 4-n-butylresolcinol) and/or a salt thereof.