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    Process for the preparation of DNA gyrase inhibitors
    1.
    发明授权
    Process for the preparation of DNA gyrase inhibitors 失效
    DNA促旋酶抑制剂的制备方法

    公开(公告)号：US5486466A

    公开(公告)日：1996-01-23

    申请号：US339442

    申请日：1994-11-14

    申请人： Mikio Arisawa ,  Erwin Gotschi ,  Paul Hebeisen ,  Tsutomu Kamiyama ,  Helmut Link ,  Raffaello Masciadri ,  Hisao Shimada ,  Junko Watanabe

    发明人： Mikio Arisawa ,  Erwin Gotschi ,  Paul Hebeisen ,  Tsutomu Kamiyama ,  Helmut Link ,  Raffaello Masciadri ,  Hisao Shimada ,  Junko Watanabe

    IPC分类号： A61K31/395 ,  A61K31/42 ,  A61K31/425 ,  A61K38/00 ,  A61P31/04 ,  C07C317/24 ,  C07C317/28 ,  C07C317/46 ,  C07C317/48 ,  C07C323/56 ,  C07C323/58 ,  C07C323/64 ,  C07D291/08 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D419/12 ,  C07K5/02 ,  C07K5/078 ,  C07K5/097 ,  C07K5/103 ,  C07K7/06 ,  C12P13/04 ,  C12N1/20

    CPC分类号： C07D419/04 ,  C07D291/08 ,  C07K5/0202 ,  C07K5/06139 ,  C07K5/0821 ,  C07K5/1008 ,  C07K7/06 ,  A61K38/00 ,  Y10S435/886

    摘要： Bicyclic derivatives of the general formula ##STR1## wherein X.sup.1 is --S-- or --SO--;X.sup.2 is --CO-- or --CS--;R.sup.1 is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy;R.sup.2 and R.sup.3 are each independently hydrogen, lower alkyl, halogen, amino, lower alkylamino, di-lower alkylamino, acylamino, lower alkexy, lower alkoxymethoxy or a group OR.sup.4 ;R.sup.4 is hydrogen or an easily hydrolyzable group;R.sup.5 is hydrogen, optionally esterified carboxy or amidated (thio)carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl;R.sup.6 and R.sup.7a are each independently hydrogen or lower alkyl;R.sup.7b is hydrogen, optionally substituted hydroxy, --NR--A or --N.dbd.B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene;R.sup.7a and R.sup.7b together represent oxo, lower alkoxycarbonylmethylidene or optionally substituted hydroxyimino; andR.sup.8 is hydrogen, optionally substituted alkyl, optionally esterified carboxy or amidated (thio)carboxy; provided that no more than two of R.sup.1 -R.sup.3 are nitrogen-containing groups; no more than two of R.sup.1 -R.sup.3 are oxygen containing groups and no more than two of R.sup.1 -R.sup.3 are either nitrogen containing or oxygen containing groups;and pharmaceutically acceptable salts of the compounds of formula I carrying an acidic and/or basic substituent.The products are antimicrobially active.

    摘要翻译： 通式为其中X 1为-S-或-SO-的通式为其的双环衍生物; X2是-CO-或-CS-; R 1为氢，卤素或任选被卤素或低级烷氧基取代的低级烷基; R2和R3各自独立地为氢，低级烷基，卤素，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，低级烷基，低级烷氧基甲氧基或基团OR4; R4是氢或易水解基团; R 5为氢，任选酯化的羧基或酰胺基（硫代）羧基，任选取代的烷基，任选取代的烯基，任选取代的酰基或杂环基; R6和R7a各自独立地为氢或低级烷基; R7b是氢，任选取代的羟基，-NR-A或-N = B，其中R是氢或低级烷基，A是氢，任选取代的烷基，低级环烷基，亚氨酰基，（硫代）酰基，酯化的羧基或酰胺基（ 硫代）羧基，B是低级亚烷基; R7a和R7b一起代表氧代，低级烷氧基羰基亚甲基或任选取代的羟基亚氨基; 和R 8是氢，任选取代的烷基，任选酯化的羧基或酰胺基（硫代）羧基; 条件是R1-R3中不超过两个为含氮基团; R1-R3中不超过两个为含氧基团，R1-R3中不超过两个为含氮基团或含氧基团; 和具有酸性和/或碱性取代基的式I化合物的药学上可接受的盐。 该产品具有抗微生物活性。

    Cephalosporin derivatives
    5.
    发明授权
    Cephalosporin derivatives 失效
    CEPHALOSPORIN衍生物

    公开(公告)号：US5055572A

    公开(公告)日：1991-10-08

    申请号：US179199

    申请日：1988-04-08

    申请人： Andre Furlenmeier ,  Erwin Gotschi ,  Paul Hebeisen ,  Werner Hofheinz ,  Helmut Link

    发明人： Andre Furlenmeier ,  Erwin Gotschi ,  Paul Hebeisen ,  Werner Hofheinz ,  Helmut Link

    IPC分类号： C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

    CPC分类号： C07D501/36 ,  C07D519/00 ,  Y02P20/55

    摘要： Acyl derivatives of the formula ##STR1## in which R is an acyl group, excluding those acyl groups of the formula ##STR2## in which A is a group of the formulae --NHCO--, --NHCONHCO--, --NHCOCH.dbd.CH--, ##STR3## wherein R.sup.6 is hydrogen or lower alkyl; R.sup.1 and R.sup.2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or --OR.sup.2, n is 1 or 2, R.sup.4 and R.sup.5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R.sup.4 and R.sup.5 both represent hydrogen) or a group of the formula --O--B-- (where R.sup.4 and R.sup.5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene;and wherein R.sup.3 is a substituted bicyclic group of the formulae ##STR4## wherein R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R" and R"' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R.sup.4 and R.sup.5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates,as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts.These compounds are useful as antibiotics.

    摘要翻译： 除了那些其中A是式-NHCO-，-NHCONHCO-，-NHCOCH = CH-的基团的式“IMAGE”的酰基之外，其中R是酰基的式Ⅰ的酰基衍生物， 其中R6是氢或低级烷基; R1和R2是氢或保护基，X是氢，卤素，低级烷氧基，硝基或-OR2，n是1或2，R4和R5是氢或一起代表另外的键，Z是直接键或羰基（ 其中R4和R5都表示氢）或式-BB-（其中R4和R5一起代表附加键）的基团，其中B是直链，支链或环状低级亚烷基; 并且其中R 3是下式的取代的双环基团：其中R 7和R 8独立地是氢，低级烷基或三氟甲基，或者在式（a），（b）中， ），（e）和（f）共同表示具有3或4个碳原子的亚烷基，R'，R“和R”'独立地是氢，低级烷基或低级环烷基; 其中R 4和R 5一起代表另外的键的式Ⅰ化合物以顺式异构形式存在，或作为其中顺式异构体形式占优势的抗异构体形式的混合物以及容易水解的酯和盐 的这些化合物和式I化合物的水合物或它们的酯和盐。 这些化合物可用作抗生素。