摘要:
Novel antibacterial agents consisting of a 2,3,5,8-tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid of the formula: ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, a process for producing the derivatives and pharmaceutical compositions containing the same. The above-identified derivatives possess antibacterial activity against gram-negative bacteria at test concentration levels of about 0.0001 to 1.0 mg/cc.
摘要:
Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##SPC1##wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##SPC2##Wherein R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a preparation of the compounds of the general formula (I).
摘要:
Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##STR2## WHEREIN R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a peparation of the compounds of the general formula (I).
摘要:
A cephalosporin of the formula (I): ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted; R is a phenyl group which may be unsubstituted or substituted, a thienyl group, a furyl group, a cyclohexadienyl group or a cyclohexenyl group; X is an acetoxy group, a pyridinium group which may be unsubstituted or substituted with a methyl or carbamoyl group, a group of the formula: ##STR2## in which R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, or a group of the formula:--S--Hetin which Het is a heterocyclic ring containing 1 to 5 oxygen, nitrogen and sulfur atoms as a hetero atom, in which the heterocyclic ring system may be either polycyclic or 5- or 6-membered monocyclic and may be unsubstituted or substituted; and M is a hydrogen atom or a biologically active carboxyl-protecting group, or is an anionic charge only when X is a pyridinium group; and the pharamaceutically acceptable salts thereof, which are useful as antimicrobial agents and prepared by the reaction of a compound of the formula (II):HO--A--COOH (II)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III): ##STR3## wherein R, M and X are as defined above, or a derivative thereof.
摘要:
A compound of the formula (I): ##STR1## wherein A is a monocyclic or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted with one or more substituents;R is a phenyl group which can be unsubstituted or substituted or a thienyl group;T is (1) a --CH.sub.2 --S--Het group, where Het is a tetrazolopyridazine ring, a triazolopyridazine ring, or a triazolopyridine ring, (2) a ##STR2## group where R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group, (3) a --CH.sub.2 N.sub.3 group or (4) a --CH.sub.2 S--D group in which D is a group selected from the group consisting of ##STR3## where m and n each is 0 to 3: with the proviso that (a) when the HO--A-- moiety is a ##STR4## group where B represents the non-metallic atoms necessary to complete a pyridine ring, a pyrimidine ring or a pyrazole ring, each of which may be unsubstituted or substituted, then T is the --CH.sub.2 SD group wherein D is as defined above, and(b) when T is the --CH.sub.2 N.sub.3 group, then R is a substituted phenyl groupand the non-toxic, pharmaceutically acceptable salts thereof, processes for preparing the same, and anti-microbial compositions containing the same.
摘要:
A compound of the formula (I): ##STR1## wherein A is a monocyclic or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted with one or more substituents;R is a phenyl group which can be unsubstituted or substituted or a thienyl group;T is (1) a --CH.sub.2 --S--Het group, where Het is a tetrazolopyridazine ring, a triazolopyridazine ring, or a triazolopyridine ring, (2) a ##STR2## group wherein R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, (3) a --CH.sub.2 N.sub.3 group or (4) is --CH.sub.2 S--D group in which D is a group selected from the group consisting of ##STR3## where m and n each is 0 to 3: with the proviso that (a) when the HO--A-- moiety is a ##STR4## group where b represents the non-metallic atoms necessary to complete a pyridine ring, a pyrimidine ring or a pyrazole ring, each of which may be unsubstituted or substituted, then T is the --CH.sub.2 SD group wherein D is as defined above, and(b) when T is the --CH.sub.2 N.sub.3 group, then R is a substituted phenyl group and the non-toxic, pharmaceutically acceptable salts thereof, processes for preparing the same, and anti-microbial compositions containing the same.
摘要:
A compound of the formula (I): ##STR1## wherein A is a monocyclic or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted with one or more substituents;R is a phenyl group which can be unsubstituted or substituted or a thienyl group;T is (1) a -CH.sub.2 -S-Het group, where Het is a tetrazolopyridazine ring, a triazolopyridazine ring, or a triazolopyridine ring, (2) ##STR2## WHERE R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, (3) a -CH.sub.2 N.sub.3 group or (4) a --CH.sub.2 S--D group in which D is a group selected from the group consisting of ##STR3## where m and n each is 0 to 3; with the proviso that (A) WHEN T is the --CH.sub.2 SD group wherein D is as defined above then the HO-A- moiety is a ##STR4## where B represents the non-metallic atoms necessary to complete a pyridine ring, a pyrimidine ring or a pyrazoline ring, each of which may be unsubstituted or subsituted, and(b) when T is the --CH.sub.2 N.sub.3 group, then R is a substituted phenyl groupAnd the non-toxic, pharmaceutically acceptable salts thereof, processes for preparing the same, and anti-microbial compositions containing the same.
摘要:
A cephalosporin of the formula (I): ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted; R is a phenyl group which may be unsubstituted or substituted, a thienyl group, a furyl group, a cyclohexadienyl group or a cyclohexenyl group; X is an acetoxy group, a pyridinium group which may be unsubstituted or substituted with a methyl or carbamoyl group, a group of the formula: ##STR2## in which R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 - C.sub.4) alkyl group, or a group of the formula:-S-Hetin which Het is a heterocyclic ring containing 1 to 5 oxygen, nitrogen and sulfur atoms as a hetero atom, in which the heterocyclic ring system may be either polycyclic or 5- or 6-membered monocyclic and may be unsubstituted or substituted; and M is a hydrogen atom or a biologically active carboxyl-protecting group, or is an anionic charge only when X is a pyridinium group; and the pharmaceutically acceptable salts thereof, which are useful as antimicrobial agents and prepared by the reaction of a compound of the formula (II):ho--a--cooh (ii)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III): ##STR3## wherein R, M and X are as defined above, or a derivative thereof.
摘要:
Viral infections caused by viruses which belong to, e.g. Pox, Herpes, Adeno, Myxo, Paramyxo groups are controlled by administering an effective amount of quinazoline derivatives of the formula ##STR1## wherein R.sub.1 is cyclo, C.sub.3 -C.sub.8 alkyl, cyclo C.sub.3 -C.sub.8 alkyl C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.2-C.sub.5 alkenyloxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio C.sub.1 -C.sub.4 alkyl, polyhalo C.sub.1- C.sub.4 alkyl, a group of the formula ##STR2## (wherein m is an integer of 1 to 3; and R.sub.4 and R.sub.5 are individually C.sub.1 -C.sub.4 alkyl, and may form together with the adjacent nitrogen atom an unsubstituted or C.sub.1 -C.sub.4 alkyl substituted 3 to 6 membered saturated heterocyclic ring, which may contain another nitrogen or oxygen atom) or a group of the formula --C.sub.n H.sub.2n --R.sub.6 (wherein n is 0 or an integer of 1 to 3; and R.sub.6 is a phenyl group, a substituted phenyl group or an aromatic or non-aromatic 3 to 6 membered heterocyclic ring which contains one or two hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atom, and may be optionally substituted by one or two C.sub.1 -C.sub.4 alkyl, and further, those substituents on adjacent carbon atoms may be joined to form a benzene or cyclohexane ring); R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, trifluoromethyl or nitro; and R.sub.3 is phenyl, substituted phenyl, cyclo C.sub.3 -C.sub.6 alkyl, pyridyl, furyl, nitrofuryl, thienyl, nitrothienyl, methylthienyl or pyrimidinyl.
摘要:
A clutch device is used in combination with a differential device. The clutch device is comprised of: a clutch housed in and rotatable with the differential device and axially movable from a disengaged state into an engaged state; a plunger slidably fit on the differential device and being axially movable from a first position where the plunger does not force the clutch to a second position where the plunger forces the clutch into the engaged state; an anti-rotated solenoid configured to drive the plunger; and a retainer supported by the differential device and in contact with both the plunger at the first position and the solenoid, whereby the plunger is barred from going beyond the first position and the solenoid is axially positioned in place.