Abstract: Compounds of structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzables esters, and hydrates thereof, are effective antiinfective agents, useful in treating and preventing infection.

Abstract: Antimicrobial quinolone thiourea compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the thiourea containing moietyand pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

Abstract: Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, and R.sup.4 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and(2) R.sup.6 is part of a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: ##STR2## wherein (3) R.sup.10, R.sup.11, R.sup.12, R.sup.13, and R.sup.

Abstract: Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked, by a non-ester linking moiety, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form any of a variety of lactam-containing moieties similar to those known in the art to have antimicrobial activity;(2) A, R.sup.6, R.sup.7, and R.sup.8 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity; and(3) Y, together with R.sup.5, form a variety of non-ester linking moieties between the lactam-containing moiety and the quinolone moiety.

Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A, R.sup.6, R.sup.7, and R.sup.8 form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.

Abstract: Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2)(1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and(2) X is --R.sup.15 --N(R.sup.16)(R.sup.17) or --R.sup.15 --R.sup.18 --N(R.sup.19)(R.sup.17), where(a)(1) R.sup.15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and(2) R.sup.16 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or(3) when X is R.sup.15 --N(R.sup.16)(R.sup.17), R.sup.16 and R.sup.15 may together comprise a heterocyclic ring including the nitrogen atom to which R.sup.15 and R.sup.16 are bonded;(b) R.sup.17 is C(.dbd.S)--S--M, where M is a pharmaceutically-acceptable salt or biohydrolyzable ester; and(c)(1) R.sup.18 is alkyl, a carbocyclic ring, or a heterocyclic ring; and(2) R.sup.

Abstract: Antimicrobial quinolone thiourea compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2)(1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and(2) X is --R.sup.15 --N(R.sup.16)(R.sup.17) or --R.sup.15 --R.sup.18 --N(R.sup.19)(R.sup.17), where(a)(1) R.sup.15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and(2) R.sup.16 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or(3) when X is R.sup.15 --N(R.sup.16)(R.sup.17), R.sup.16 and R.sup.15 may together comprise a heterocyclic ring including the nitrogen atom to which R.sup.15 and R.sup.16 are bonded;(b) R.sup.17 is C(.dbd.S)--NR.sup.20 R.sup.21 ; where R.sup.20 is, hydrogen, alkyl, alkenyl, a carbocyclic ring or a heterocyclic ring; and R.sup.21 is R.sup.20 or N(R.sup.20)(R.sup.20); or R.sup.20 and R.sup.

Abstract: The present invention provides methods of making compounds of the structure[Q-L.sup.1 ]-L-[L.sup.2 -B[wherein(I) Q is a quinolone moiety;(II) B is a beta-lactam moiety;(III) L, L.sup.1, and L.sup.2 together comprise a carbamate-containing linking moietycomprising the steps of:(1) Reacting a lactam compound of the formula B-L.sup.4 -H with phosgene to form an intermediate compound of the formula B--L.sup.4 --C(=O)--Cl, where L.sup.4 is oxygen; and(2) Coupling said intermediate compound with a quinolone compound of the formula Q-L.sup.3 -R.sup.44 ; wherein L.sup.3 is nitrogen; R.sup.44 is hydrogen, Si(R.sup.45).sub.3, or Sn(R.sup.45).sub.3 ; and R.sup.45 is lower alkyl.Preferably, the process additionally comprises steps prior to the reacting and coupling steps where esters of the lactam and quinolone compounds are made. Also preferably, the coupling step comprises adding a solution containing the quinolone compound to a solution containing the intermediate compound.

Abstract: Antimicrobial quinolnyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A, R.sup.6, R.sup.7, and R.sup.8 form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.

Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A.sup.2, A.sup.2, A.sup.3, R.sup.7, R.sup.8, and R.sup.9 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity.