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    • 6. 发明申请
    • ANTIMICROBIAL QUINOLONYL LACTAMS
    • 抗微生物喹诺酮类LACTAMS
    • WO1991016327A1
    • 1991-10-31
    • PCT/US1991002476
    • 1991-04-12
    • NORWICH EATON PHARMACEUTICALS, INC.
    • NORWICH EATON PHARMACEUTICALS, INC.DEMUTH, Thomas, Prosser, Jr.WHITE, Ronald, Eugene
    • C07D501/28
    • C07D477/14C07D477/20C07D499/00C07D499/88C07D501/00
    • Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of formula (I), wherein (1) A , A , A , R , and R generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and (2) R is part of a linking moiety, linking hte quinolone moiety to a lactam-containing moiety having formula (II), wherein (3) R , R , R , R , and R , together with bonds ''a'' and ''b'', form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, ester, thioester, amide, and hydrazide groups.
    • 包含与式(I)的喹诺酮部分连接的含内酰胺部分的抗微生物喹诺酮内酰胺化合物,其中(1)A 1,A 2,A 3,R 1和R 4 >通常形成本领域已知的各种喹诺酮,萘啶或相关的环状部分以具有抗微生物活性; 和(2)R 6是连接部分的一部分,将喹诺酮部分与具有式(II)的含内酰胺部分连接,其中(3)R 10,R 11,R 12, R 13和R 14与键“a”和“b”一起形成本领域已知的具有抗微生物活性的各种含内酰胺的部分; 连接部分包括(例如)氨基甲酸酯,二硫代氨基甲酸酯,脲,硫脲,异脲,异硫脲,胍,碳酸酯,三硫代碳酸酯,反相氨基甲酸酯,黄原酸酯,反式异卤素,反式二硫代氨基甲酸酯,反式异硫脲,胺,亚胺, 杂芳基,醚,硫醚,酯,硫酯,酰胺和酰肼基团。
    • 8. 发明申请
    • ANTIMICROBIAL QUINOLONE THIOUREAS
    • 抗微生物喹诺酮类药物
    • WO1991016310A1
    • 1991-10-31
    • PCT/US1991002203
    • 1991-04-01
    • NORWICH-EATON PHARMACEUTICALS, INC.
    • NORWICH-EATON PHARMACEUTICALS, INC.DEMUTH, Thomas, Prosser, Jr.WHITE, Ronald, Eugene
    • C07D215/00
    • C07D401/04C07D215/56C07D401/12C07D401/14C07D417/14C07D455/04C07D471/04C07D477/10C07D487/04C07D499/00C07D501/00C07D503/00C07D505/00C07D513/04
    • Antimicrobial quinolone thiourea compounds of general formula (I), wherein (1) A , A , A , R , R , R , and R 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 is X, R is X, or both R and R are X; and (2) X is -R -N(R )(R ) or -R -R -N(R )(R ), where (a) (1) R is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) when X is R -N(R )(R ), R and R may together comprise a heterocyclic ring including the nitrogen atom to which R and R are bonded; (b) R is C(=S)-NR R ; where R is hydrogen, alkyl, alkenyl, a carbocyclic ring or a heterocyclic ring; and R is R or N(R )(R ); or R and R , together with the nitrogen to which they are bonded, form a heterocyclic ring; and (c) (1) R ) is alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) R and R may together comprise a heterocyclic ring including the nitrogen atom to which R and R are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.
    • 通式(I)的抗菌喹诺酮硫脲化合物,其中(1)A 1,A 2,A 3,R 1,R 3,R 4和R 6, 形成与本领域已知的具有抗微生物活性的各种喹诺酮和相关杂环结构中的任何一种; 和(2)(1)R 1是X,R 3是X,或者R 1和R 3都是X; 和(2)X是-R 15 -N(R 16)(R 17)或-R 15 -R 18 -N(R 19)(R 17) 其中(a)(1)R 15为无,烷基,碳环或杂环; 和(2)R 16是氢; 烷基; 烯基; 碳环 杂环; 或(3)当X是R 15 -N(R 16)(R 17)时,R 16和R 15可以一起包含包含氮原子的杂环,R 15 >和R 16键合; (b)R 17是C(= S)-NR 20 R 21; 其中R 20为氢,烷基,烯基,碳环或杂环; 并且R 21是R 20或N(R 20)(R 20); 或R 20和R 21与它们所键合的氮一起形成杂环; 和(c)(1)R 18)是烷基,碳环或杂环; 和(2)R 19是氢; 烷基; 烯基; 碳环 杂环; 或(3)R 18和R 19可以一起包含包含R 18和R 19键合的氮原子的杂环; 及其药学上可接受的盐和可生物水解的酯,及其水合物。