Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R6)—, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredien

Abstract: Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems.

Abstract: Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems; (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ?O or ?S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on).

Abstract: Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems.

Abstract: A compound of the formula: ##STR1## wherein R is an optionally substituted phenyl group, 5-membered; the A ring is a 5 to 7 membered alicyclic group in which said A ring may have an alkyl group as a substituent, or a pharmaceutically acceptable salt thereof, and is useful as a psychotropic agent.

Abstract: A compound of the formula: ##STR1## wherein R is an optionally substituted aryl group or an optionally substituted aromatic heterocycle group; A ring is a 5 to 9 membered alicyclic group, in which one or more of carbon atoms constituting said A ring may be replaced by O, or S and said A ring may have alkyl as a substituent, or a pharmaceutically acceptable salt thereof.

Abstract: 2-Substituted carbonylimidazo[4,5-c]quinolines of formula: ##STR1## having a high affinity for benzodiazepin receptor and showing an excellent psychostimulating action orally at a dose of 0.1-500 mg are provided through several routes.

Abstract: Tetrahydrothiopyrano[3,2-b]indole derivatives represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, phenyl-C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, or ##STR2## wherein Y is C.sub.1-4 alkylene or C.sub.1-4 oxoalkylene and R.sup.5 and R.sup.6 each is hydrogen or C.sub.1-4 alkyl;R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.3-6 cycloalkyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or ##STR3## wherein Y, R.sup.5 and R.sup.6 each is as defined above; or ##STR4## is pyrrolidino, piperdinyl, piperazinyl, 4-C.sub.1-4 alkylpiperazinyl or morpholino;R.sup.4 is hydrogen or C.sub.1-4 alkyl; andn is 0 or an integer of 1 or 2and the pharmaceutically acceptable salts being useful as analgesic and anti-inflammatory agents as well as psychoanaleptic and nootropic drug.

Abstract: A compound of the formula: ##STR1## (wherein R is phenyl optionally substituted by one or two members selected from the group consisting of trifluoromethyl, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, nitro, amino C.sub.1 -C.sub.5 alkanoylamino and C.sub.1 -C.sub.5 alkoxycarbonyl or 5- or 6-membered heterocyclic group optionally substituted by one or two members selected from the group consisting of halogen, C.sub.1 -C.sub.5 alkyl and C.sub.1 -C.sub.5 alkoxy,Q is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.10 acyl, C.sub.1 -C.sub.5 alkylsulfonyl or C.sub.6 -C.sub.10 arylsulfonyl, ##STR2## R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each is hydrogen, halogen C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or C.sub.1 -C.sub.

Abstract: Compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, alkyl, alkoxycarbonyl, carboxy, halogen, nitro or trifluoromethyl, or R.sup.1 and R.sup.2 taken together may form alkylene; R.sup.3 is hydrogen, alkyl, alkanoyl or alkylsulfonyl; R.sup.4 is hydrogen, alkoxycarbonyl, carboxy or halogen; X is hydrogen, alkyl, alkoxy, halogen or hydroxy; and Y is methine or nitrogen or salts thereof are provided. The compounds (I) show potent psychotropic activity.

Abstract: Tetrahydrothiopyrano[2,3-b]indole derivative represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl, --COR.sup.5 (wherein R.sup.5 is alkyl, alkenyl, aryl or alkoxy) or ##STR2## (wherein Y is alkylene, oxoalkylene, hydroxyalkylene and R.sup.6 and R.sup.7 are each hydrogen or alkyl): R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl or dialkylaminoalkyl or ##STR3## is pyrrolidino, piperidino, piperazino, 4-alkylpiperazino, 4-arylpiperazino or morpholino; R.sup.4 is hydrogen or alkyl; A is methylene, alkylmethylene, ethylene, alkylethylene; X is hydrogen or one or two groups selected from the group consisting of halogen, alkyl, alkoxy, hydroxy and halogenoalkyl; and n is an integer of 0 to 2 and its pharmaceutically acceptacle salts; synthesized from 2-propargylthioindole or 2-(4-hydroxy-2-butynylthio)-indole; useful as analgesic and anti-inflammatory agent.

Abstract: 3-Aminoisoxazoles of the formula: ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, phenyl or halo-phenyl) are prepared by reacting a .beta.-ketonitrile of the formula:R--CO--CH.sub.2 CN(wherein R is as defined above) with a compound of the formula:HY(wherein Y is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio) in the presence of an acid in a solvent to give an iminium salt of the formula: ##STR2## (wherein X is the residue of said acid; R and Y are each as defined above) and further reacting the iminium salt with hydroxylamine in an inert solvent.

Abstract: Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.