Abstract: 7-substituted 3-cephem or cepham compounds characterized by the grouping, in the 7-position thereof, of the formula:R'--A--CONH--where R' is thiadiazolyl or amino thiazolyl, and A is methylene carrying oxyiimino, or R' is haloacetyl and A may also be methylene, their preparation, and pharmaceutical uses.

Abstract: The compound 7[2-(aminothiazol-4-yl)-2-methyoxyiminoacetamido]-methylthiomethyl-3-cephe m-4-carboxylic acid or carboxylic ester thereof, or a pharmaceutically acceptable salt thereof is disclosed as an antimicrobial agent.

Abstract: Cephalosporin intermediates have been synthesized.

Abstract: A cephem compound of the formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 is amino or protected amino, R.sup.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, carboxy(lower) alkyl, protected carboxy(lower) alkyl, cyclo(lower) alkyl or cyclo (lower)alkenyl, and Z is CH or N;R.sup.2 is hydrogen, phenyl, pyridyl which may have a lower alkyl group, or cyano; andR.sup.3 is carboxy or protected carboxy; and pharmaceutically acceptable salt thereof.

Abstract: Intermediates for cephalosporins have been synthesized.

Abstract: The invention relates to an antimicrobial agent of the formula: ##STR1## wherein R.sup.1 is amino or conventional protected amino, R.sup.2 is hydrogen or tetrahydropyranyl, and ##STR2## wherein R.sup.4 is lower alkyl, and R.sup.5 is hydrogen or lower alkyl substituted with hydroxy or conventional protected hydroxy, and pharmaceutically acceptable salts thereof.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, aryl, ar(lower)alkyl or a heterocyclic group, each of which may have suitable substituent(s),R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, lower alkylthio, lower alkenyl, lower alkenylthio, lower alkynyl, heterocyclicthio or a heterocyclic group, in which lower alkylthio, lower alkenyl, lower alkenylthio, heterocyclicthio and a heterocyclic group may have suitable substituent(s),R.sup.4 and R.sup.5 are each hydrogen, halogen or arylthio,A is lower alkylene, andn is an integer of 0 or 1,and a pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical composition comprising the same.

Abstract: An N-containing heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted with hydroxy, halogen or a heterocyclic group, carboxy, esterified carboxy, carbamoyl optionally substituted with heterocyclic(lower)alkyl or lower alkylamino(lower)alkyl, N-containing heterocycliccarbonyl optionally substituted with lower alkyl, or ureido optionally substituted with lower alkylamino(lower)alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andX is .dbd.N--or ##STR2## in which R.sup.4 is lower alkyl or halo(lower)alkyl, or is taken together with R.sup.1 to form an N-containing heterocyclic group optionally substituted with oxo and lower alkylamino(lower)alkyl; orR.sup.2 is lower alkyl, andX is ##STR3## in which R.sup.4 is phenyl substituted with nitro; and a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical (e.g. antihypertension) compositions comprising the same.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is cyclo(lower)alkyl or lower alkynyl having 2 to 6 carbon atoms, andR.sup.6 is amino or protected amino, or the reactive derivative at the carboxy group, are disclosed as intermediates for the preparation of cephem and cepham compounds having antimicrobial activity.

Abstract: The invention relates to compounds for treatment of hypertension, and cardiovascular and cerebrovascular diseases, which compounds are of the formula: ##STR1## wherein R.sup.1 is piperazinyl(lower)alkyl, carbamoyl substituted with piperazinyl(lower)alkyl, or piperazinylcarbonyl, in each of which a piperazinyl group may be substituted with lower alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl or halo(lower)alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substitured with nitro;and a pharmaceutically acceptable salt thereof.

Abstract: New pyrimidine derivatives of the formula: ##STR1## wherein Z is a group selected from ##STR2## in which R.sup.1 and R.sup.2 are each hydrogen, alkenyl, ar(lower)alkyl or lower alkyl optionally substituted with epoxy, hydroxy, amino and/or lower alkylamino and R.sup.5 is lower alkyl,R.sup.3 is hydrogen, aryl optionally substituted with lower alkyl, lower alkoxy and/or halogen, or pyridyl optionally substituted with lower alkyl,R.sup.4 is hydrogen, lower alkyl or phenyl optionally substituted with lower alkoxy, andY is.dbd.O, .dbd.S or .dbd.N--R.sup.6,in which R.sup.6 is lower alkyl; cyclo(lower)alkyl; ar(lower)alkyl optionally substituted with lower alkoxy; N-containing unsaturated heterocyclic group optionally substituted with lower alkyl; or aryl optionally substituted with hydroxy, lower alkyl, halogen or lower alkoxy, in which lower alkoxy substituent may be substituted with epoxy, hydroxy, amino and/or lower alkylamino,provided that Y is.dbd.N--R.sup.6 when R.sup.3 and R.sup.

Abstract: A compound of the formula: ##STR1## wherein R.sup.2 is halo(lower)alkyl, andR.sup.6 is amino or protected amino, its reactive derivative at the carboxy group or its lower alkyl ester, is disclosed, having utility as an intermediate for producing cephems or cephams.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is pyridyl,R.sup.2 is hydrogen, lower alkyl or hydroxy (lower) alkyl,R.sup.3 is hydrogen, hydroxy or lower alkyl, andR.sup.4 is aryl optionally substituted with substituent(s) selected from the group consisting of lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, nitro, amino, substituted amino, hydroxy, lower alkoxy, lower alkynyloxy, substituted or unsubstituted ar(lower)alkoxy, halogen, halo(lower)alkyl, carboxy and esterified carboxy,and a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.

Abstract: New syn-isomers of 3-cephem-4-carboxylic acids having anti-bacterial activities, processes for preparation thereof, pharmaceutical compositions thereof, with the acids being substituted at the 3 position with acyloxymethyl, hydroxymethyl, formyl or heterocyclic thiomethyl groups and at the 7 position with alkoxyiminoacetamido substituted with substituted phenyl or substituted thiazolyl.

Abstract: The invention relates to antimicrobial compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is carboxy or a protected carboxy group andR.sup.3 is thiadiazolylthiomethyl or thiadiazolylthiomethyl substituted with lower alkyl, and pharmaceutically acceptable salts thereof.

Abstract: New pyrimidine derivatives of the formula: ##STR1## wherein Z is a group selected from ##STR2## in which R.sup.1 and R.sup.2 are each hydrogen, alkenyl, ar(lower)alkyl or lower alkyl optionally substituted with epoxy, hydroxy, amino and/or lower alkylamino and R.sup.5 is lower alkyl,R.sup.3 is hydrogen, aryl optionally substituted with lower alkyl, lower alkoxy and/or halogen, or pyridyl optionally substituted with lower alkyl,R.sup.4 is hydrogen, lower alkyl or phenyl optionally substituted with lower alkoxy, andY is .dbd.O, .dbd.S or .dbd.N--R.sup.6, in which R.sup.6 is lower alkyl; cyclo(lower)alkyl; ar(lower)alkyl optionally substituted with lower alkoxy; N-containing unsaturated heterocyclic group optionally substituted with lower alkyl; or aryl optionally substituted with hydroxy, lower alkyl, halogen or lower alkoxy, in which lower alkoxy substituent may be substituted with epoxy, hydroxy, amino and/or lower alkylamino,provided that Y is .dbd.N--R.sup.6 when R.sup.3 and R.sup.

Abstract: This invention relates to novel compounds of the formula: ##STR1## wherein R.sup.1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR.sup.6 is carboxy or protected carboxy, and a slat, thereof, and processes for preparing the same, useful in the preparation of compounds of high antimicrobial activity.

Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.

Abstract: The invention relates to novel intermediates for the preparation of antimicrobial compounds, the intermediate being a compound of the formula: ##STR1## in which R.sup.2 is carboxy or a protected carboxy group,R.sup.8 is 2-hydroxyphenyl andZ is a group of the formula:--CH.dbd.CH.sub.2, --CH.sub.2 --X.sup.2, --CH.sub.2 P.sup.+ (R.sup.7).sub.3.X.sup.3-,--CH.dbd.P(R.sup.7).sub.3 OR--CH.sub.2 OH,wherein X.sup.2 and X.sup.3 are each halogen and R.sup.7 is selected from the group consisting of phenyl, tolyl, xylyl and naphthyl, or a salt thereof.

Abstract: The invention relates to new pyrimidine derivatives, useful in the treatment of cerebrovascular disease, of the formula: ##STR1## wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification.