Abstract: The compounds of the invention are a 2'-deoxy-5-fluorouridine derivative represented by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 is a hydrogen atom or a group easily hydrolyzable in vivo, the other is a benzyl group which may optionally have at least one halogen atom or trifluoromethyl group as a substituent on the phenyl ring, and R.sub.3 is a lower alkyl group, and a pharmaceutically acceptable salt thereof.The compounds of the invention can be suitably used as an antitumor agent.

Abstract: This invention relates to: (1) a compound represented by the formula (V), its tautomer and a mixture of the same; (2) a process for producing the compound represented by the above-mentioned formula (V), its tautomer or a mixture of the same, which comprises reacting N-vinylpiperidone represented by the formula (I) with a nicotinate represented by the formula (II), wherein R represents a lower alkyl group, in the presence of a sodium alkoxide; (3) a process for producing a pyridine derivative represented by the formula (III), which comprises producing the compound represented by the formula (V), its tautomer or a mixture of the same by the process as described in the above (2), and then treating the obtained compound with an acid; and (4) a process for producing a pyridine derivative represented by the formula (IV), in which the treatment with an acid as described in the above (3) is followed by another treatment with a base.

Abstract: The present invention provides carbamoyl-2 -pyrrolidinone compounds useful as medicaments for improving cerebral functions and activating cerebral metabolism or protecting against anoxic brain damage.

Abstract: A benzothiadiazine derivative, hydrate thereof and acid addition salt thereof, the derivative being represented by the general formula (I) ##STR1## wherein X is methylene or a nitrogen atom substituted with a lower alkyl, Y and Z are each methylene or carbonyl, A is phenylene or phenylene substituted with methoxycarbonyl, R.sub.4 is lower alkylene or lower alkenylene, R.sub.1 is a hydrogen atom, acetoxyacetyl, cyclohexylmethyl or benzyl wherein the benzene ring may be substituted with lower alkoxyl, halogen atom, nitro, lower alkyl, methylenedioxy or hydroxyl, R.sub.2 is lower alkyl or phenyl, and R.sub.3 is a hydrogen atom, halogen atom or lower alkoxyl with the exception of the case where X, Y and Z are each methylene, A is unsubstituted phenylene, R.sub.4 is lower alkylene and R.sub.1 is a hydrogen atom; and a peptic ulcer treating agent containing as an effective component the above derivative, hydrate thereof or acid addition salt thereof.

Abstract: A isoxazole compound represented by the formula (1): ##STR1## wherein R represents a hydrogen atom or a lower alkoxy group, R.sub.1 is a group represented by the formula (2): ##STR2## (wherein A represents --NH-- or --O--, B represents a methylene group or a carbonyl group, m is 0 or 1, n is an integer of 1 to 12, X represents a hydrogen atom, a hydroxy group or a lower alkoxycarbonyl group, Y represents a phenyl group which can be substituted with one or more halogen atoms, or a hydrogen atom), a group represented by the formula (3): ##STR3## (wherein Z represents a pyrimidinyl group), or a group represented by the formula (4): ##STR4## (wherein R.sub.2 represents a styryl group which can be substituted with one or more hydroxy groups); a pharmaceutically acceptable salt thereof; or a medical use thereof in a method of inhibiting lipoxygenase, inhibiting 5-lipoxygenase or inhibiting cyclooxygenase.

Abstract: The present invention provides a process for producing isoxazole derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each a hydrogen atom or lower alkoxyl, and R.sup.3 is cyano or alkoxycarbonyl, the process being characterized by oxidizing an .alpha., .beta.-unsaturated ketoxime derivative represented by the formula ##STR2## wherein R.sup.1 , R.sup.2 and R.sup.3 are as defined above. The isoxazole derivatives (II) to be produced by the process of the present invention are useful as intermediates for preparing (3,4-diarylisoxazol-5-yl) acetic acid derivatives which are useful as anti-inflammatory agents, analgesics and antipyretics.

Abstract: The present invention provides a carbamoyl-2-pyrrolidinone compound which has the following formula (2) and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.3 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having lower alkoxyl, lower alkylamino, a halogen atom or halogenomethyl as a substituent.Further, the present invention provides novel carbamoyl-2-pyrrolidinone compounds represented by the formula ##STR2## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.2 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having methoxy or lower alkylamino as a substituent, provided that when R.sup.1 is a hydrogen atom or unsubstituted lower alkyl, R.sup.2 is not unsubstituted phenyl.

Abstract: The present invention provides a bicyclolactam derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.

Abstract: The present invention provides an oxindole derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is hydrogen atom, halogen atom, lower alkyl group or lower alkoxyl group, R.sup.2 is hydrogen atom or lower alkyl group, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being alkyl group which may form a ring; benzodioxanyl group; or phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group, diethylamino group, trifluoromethyl group, nitrile group, nitro group and benzyloxy group), R.sup.2 and R.sup.3 may form together .dbd.CH--R.sup.5 (R.sup.5 being same as above), R.sup.

Abstract: The present invention provides a bicyclolactam derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.

Abstract: Disclosed are a piperazine compound of the formula below or a pharmaceutically acceptable salt thereof, medical uses thereof, and processes for preparing the same: ##STR1## wherein each of R and R' is --OH, a lower alkoxy, a halo, H, a di(lower alkyl) hydrogenphosphate residue or a group --OR" (R" is an aralkyl group, etc.), etc., Y is --CH.dbd.CH-- or --(CH.sub.2).sub.m -- (m is 0, 1 or 2), and Y.sub.1 is a group of the formula ##STR2## (wherein A is --NH-- or --O--, A.sub.1 is a methylene or a carbonyl, n is 6-20, X is --OH, H or a lower alkoxycarbonyl, and X.sub.1 is an optionally halo-substituted phenyl or H) or a group of the formula ##STR3## (wherein X and n are as defined above), provided that when Y.sub.1 is the group of the formula (3), each of R and R' is an --OH group.

Abstract: The present invention provides an .alpha., .beta.-unsaturated ketone and ketoxime derivative represented by the formula ##STR1## wherein Y is oxygen atom or hydroxyimino group, Z is cyano or alkoxycarbonyl group, R.sup.1 and R.sup.2 are the same or different and are each hydrogen atom or lower alkoxyl group.The .alpha., .beta.-unsaturated ketones and ketoxime derivatives of the invention are useful as an intermediate for preparing a (3,4-diarylisoxazol-5-yl)acetic acid derivatives which is useful as an anti-inflammatory agent, analgesic and antipyretic.

Abstract: The present invention provides a diazabicycloalkane derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is phenyl group, thiazolyl group or furyl group, the phenyl group may have lower alkoxy, lower alkyl or halogen atom as a substituent, R.sup.2 is oxygen atom or sulfur atom, m is 3 or 4, n is 1 or 2.

Abstract: This invention provides a penicillin derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, C.sub.1-6 hydroxyalkyl, C.sub.3-9 acyloxyalkyl, C.sub.8-13 benzyloxyalkyl, C.sub.2-7 alkoxyalkyl, C.sub.2-7 alkoxycarbonyl, C.sub.3-8 alkenyloxycarbonyl, C.sub.3-8 alkynyloxycarbonyl, phenyl, amino, cyano, formyl, trifluoromethyl, C.sub.2-6 acyl, carbamoyl, C.sub.2-7 alkylcarbamoyl, benzyloxycarbonylamino, C.sub.2-7 alkoxycarbonylamino; and R.sub.3 is hydrogen, a group for forming a pharmaceutically acceptable salt, or a penicillin carboxyl protecting group, with the proviso that both of R.sub.1 and R.sub.2 are not hydrogen or C.sub.2-7 alkoxycarbonyl at the same time and that when one of R.sub.1 and R.sub.2 is hydrogen, the other is not C.sub.2-7 alkoxycarbonyl, or a pharmaceutically acceptable acid addition salt, process for preparing the derivative, and a pharmaceutical composition containing the derivative.

Abstract: An analgesic compositon containing as active ingredient an allophanoylpiperazine compound represented by the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group or phenyl group; R.sup.2 and R.sup.3 each represents a hydrogen atom or a lower alkyl group; and R.sup.4 represents a phenyl group or a substituted phenyl group having as substituent a halogen atom or methyl, trifluoromethyl, hydroxyl, methoxy, methylenedioxy, nitro, or carboxyl group; pyridyl group, pyrimidyl group, thiazolyl group, benzyl group, cinnamyl group, cyclohexyl group, a lower alkyl group, a substituted lower alkyl group having chlorine atom or hydroxyl group as substituent; or a lower alkenyl group.

Abstract: This invention provides a penam derivative represented by the formula ##STR1## wherein R is hydrogen or methyl and R.sub.1 is (hexahydro-1H-azepin-1-yl)methyleneamino, 2-phenylacetamido, 2-phenoxyacetamido, 2-amino-2-phenylacetamido, 2-amino-2-(p-hydroxyphenyl)acetamido or 2-(4-ethyl-2,3-dioxo-1-piperazine)carboxamido-2-phenylacetamido, and a salt thereof, and processes for preparing them.

Abstract: A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 is hydrogen or trialkylsilyl; R.sub.2 is hydrogen, trialkylsilyl or COOR.sub.2 ' wherein R.sub.2 ' is hydrogen, C.sub.1-18 alkyl, C.sub.2-7 alkoxymethyl, C.sub.3-8 alkylcarbonyloxymethyl, C.sub.4-9 alkylcarbonyloxyethyl, (C.sub.5-7 cycloalkyl)carbonyloxymethyl, C.sub.9-14 benzylcarbonyloxyalkyl, C.sub.3-8 alkoxycarbonylmethyl, C.sub.4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.-butyrolacton-4-yl, halogenated C.sub.1-6 alkyl substituted with 1 to 3 halogen atoms, C.sub.1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, dimethylaminoethyl, dimethylchlorosilyl, trichlorosilyl, (5-substituted C.sub.1-6 alkyl or phenyl or unsubstituted-2-oxo-1,3-dioxoden-4-yl)methyl, C.sub.8-13 benzoyloxyalkyl or group for forming a pharmaceutically acceptable salt; and R.sub.3 has the same meaning as above R.sub.2 '.

Abstract: An analgesic, anti-inflammatory or anti-pyretic composition containing 1,1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a lower alkyl group or a phenyl group; R.sup.2 is a lower alkyl group, a phenyl group or a substituted phenyl group having chlorine atom(s), methyl group(s) or methoxy group(s) as the substituent(s), further R.sup.1 and R.sup.2 may form a single ring containing one or two hetero atoms including the adjacent nitrogen atom; R.sup.3 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.4 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), dimethyl-amino group(s), nitro group(s), hydroxyl group(s), acetyl group(s), or methylthio group(s) as the substituent(s), a benzyl group, a cyclohexyl group or a lower alkyl group, as the active ingredient.

Abstract: An analgesic, anti-inflammatory or anti-pyretic composition containing 1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl group having chlorine atom(s), cyano group(s), dimethylamino group(s), hydroxy group(s), methoxy group(s) or carboxy group(s) as the substituent(s), a lower alkenyl group, a hydroxy group, a methoxy group, an acetyl group or a phenyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), methylenedioxy group(s), hydroxy group(s), dimethylamino group(s), carboxy group(s) or carboxymethyl group(s) as the substituent(s), a benzyl group, a pyridyl group, a substituted pyridyl group having methyl group(s) as the substituent(s), a pyridylmethyl group, pyrimidinyl group, a thiazolyl group or a thienyl group, as the active ingredient.

Abstract: A novel 1,1,3,5-substituted biuret compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are respectively the same or different, and each are alkyl groups having 1 to 4 carbon atoms; R.sup.3 is a cyclohexyl group or a phenyl group which may be unsubstituted or may have at least one substituent selected from the group consisting of chlorine, bromine, fluorine, methyl, trifluoromethyl, dimethylamino, methoxy, methylthio, nitro and acetyl. The novel 1,1,3,5-substituted biuret compounds are useful as an analgesic, anti-inflammatory and/or anti-pyretic agent.