Abstract: A therapeutic and/or prophylactic agent for nausea and/or vomiting is provided. A therapeutic and/or prophylactic agent for nausea and/or vomiting, comprising a compound of the Formula (I) or a pharmaceutically acceptable salt or solvate thereof: R1 and R2 are each independently hydrogen or lower alkyl; R3 is hydrogen or lower alkoxycarbonyl; and R4 is hydrogen or lower alkyl; with the proviso that all of R1 to R3 are not simultaneously hydrogen; and R1 and R4 are not simultaneously hydrogen).

Abstract: A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid ? receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid ? receptor antagonist activity, e.g., a compound of Formula (I): (wherein R1 represents hydrogen, lower alkyl, cycloalkyl lower alkyl or the like; R2 and R3 independently represent hydrogen, hydroxy or the like; R4 is hydrogen, hydroxy or the like; R5 is hydrogen; R4 and R5 may optionally form —O— or the like; R6 represents hydrogen, lower alkyl or the like (wherein X represents —O— or —N(R10)— or the like; R7, R8, R9a and R9b independently represent hydrogen, lower alkyl, lower alkoxycarbonyl or the like; r represents an integer of 0 to 5; Y represents —CH— or the like; Z represents a crosslinkage composed of 2 to 5 atoms) or a pharmaceutically acceptable salt thereof or a solvate of either.

Abstract: A benzodiazepine derivative of the formula (I): ##STR1## wherein R.sub.1 is a bond, --CH.sub.2 --, --CH.sub.2 O--, --SCH.sub.2 -- or a group of the formula: ##STR2## R.sub.2 is a lower alkyl, --COOR.sub.5, --CONH(CH.sub.2).sub.n COOR.sub.5, --CONHSO.sub.2 R.sub.5, --SO.sub.2 NHCOR.sub.5, or an optionally substituted heterocyclic group (R.sub.5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R.sub.3 is a bond, --CO-- or --CONH--; and R.sub.4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.

Abstract: A compound of the formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or lower alkyl; R.sub.2 is a lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic group; R.sub.3 is an optionally substituted phenyl; R.sub.4 is an optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocyclic group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.

Abstract: 9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.