公开(公告)号：US4863914A

公开(公告)日：1989-09-05

申请号：US849387

申请日：1986-04-08

申请人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

发明人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

IPC分类号： C07D519/06 ,  A61K31/425 ,  A61K31/43 ,  A61K31/431 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/06 ,  C07D499/861 ,  C07D499/88 ,  C07D499/897 ,  C07D519/00

CPC分类号： C07D499/88

摘要： Compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene, heterocyclediyl, C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.4 alkenylene, alkynylene, ##STR2## C.sub.3 -C.sub.8 cycloalkylene, aralkylene radical optionally substituted, and O.sup.(+) represents a group +NR.sub.1 R.sub.2 R.sub.3, wherein R.sub.1, R.sub.2 and R.sub.3 are each either:(i) a optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical, or(iii) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical, or(iv) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused pyridinium, pyrazinium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof, are disclosed.A method of preparation is also provided. The compounds show high antibacterial activity.

摘要翻译： 其中R是氢原子或任选被卤素原子或羟基取代的任选被保护的C 1 -C 4烷基的化合物，A是Z，ZOCO-或ZC）残基，其中Z是亚苯基，亚萘基，杂环基， C 1 -C 7亚烷基，C 2 -C 4亚烯基，亚炔基，C 3 -C 8亚环烷基，任选取代的亚芳基，O（+）表示基团+ NR 1 R 2 R 3，其中R 1，R 2和R 3各自为：（ⅰ） 任选取代的烷基，芳烷基或芳基，或（ii）R 1如（i）中所定义，R 2和R 3一起表示任选取代或稠合的杂环基，或（iii）R 1，R 2和R 3一起 代表任选取代的亚氮基 - 双环或三环基团，或（iv）R 1，R 2和R 3一起表示任选取代或稠合的吡啶鎓，吡嗪鎓，吡唑鎓或哒嗪鎓基，其药学或兽医学上可接受的盐是 披露 还提供了一种制备方法。 该化合物显示出高抗菌活性。

公开(公告)号：US4837215A

公开(公告)日：1989-06-06

申请号：US849388

申请日：1986-04-08

申请人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

发明人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

IPC分类号： C07D519/06 ,  A61K31/425 ,  A61K31/43 ,  A61K31/435 ,  A61K31/44 ,  A61K31/535 ,  A61P31/04 ,  C07D499/00 ,  C07D499/88 ,  C07D499/897

CPC分类号： C07D499/00

摘要： Compounds of the following formula I ##STR1## wherein X represents a sulphur or an oxygen atom,R is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;A is a Z, Z--O--CO-- or --Z--CO-- residue, whereinZ represents(a) an optionally substituted phenylene or naphthylene group,(b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;(c) an optionally substituted linear or branched C.sub.1 -C.sub.7 alkylene radical;(d) a C.sub.2 -C.sub.4 alkenylene or alkynylene group or a group of formula ##STR2## (e) an optionally substituted C.sub.3 -C.sub.8 cycloalkylene ring; (f) an aralkylene radical of the formula ##STR3## wherein n is 1, 2 or 3; andQ.sup.(+) represents a +NR.sub.1 R.sub.2 R.sub.3 group, wherein(i) R.sub.1, R.sub.2, R.sub.3, are each independently an optionally substituted alkyl, aralkyl or aryl radical; or p1 (ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3 taken together with the nitrogen atom represent an optionally substituted heterocyclic or fused heterocyclic radical; or(iii) R.sub.1, R.sub.2, R.sub.3, taken together with the nitrogen atom, represent an optionally substituted azoniabicyclo or azoniatricyclo radical; or(iv) R.sub.1, R.sub.2, R.sub.3, taken together with nitrogen atom, represent an optionally substituted pyridinium, pirazinium, pyrazolium, or pyridazinium radical, such radicals being optionally fused with one phenyl ring or with a 5-7 membered, saturated or unsaturated cycloaliphatic or heterocyclic ring,or a pharmaceutically or veterinarily acceptable salt thereof having high antibacterial activity.

摘要翻译： 下式I的化合物其中X表示硫或氧原子，R是氢或未被取代或被一个或多个选自游离或保护的羟基的取代基取代的C 1 -C 4烷基， 卤素原子; A是Z，ZO-CO-或-Z-CO-残基，其中Z表示（a）任选取代的亚苯基或亚萘基，（b）任选取代的杂环二基，其中杂环是单或双环，饱和或 不饱和的含有至少一个选自氧，硫和氮的杂原子; （c）任选取代的直链或支链C 1 -C 7亚烷基; （d）C 2 -C 4亚链烯基或亚炔基或式（A）的基团：（e）任选取代的C 3 -C 8亚环烷基环; （f）下式的芳亚烷基：其中n为1,2或3; 并且Q（+）表示+ NR 1 R 2 R 3基团，其中（i）R 1，R 2，R 3各自独立地为任选取代的烷基，芳烷基或芳基; 或p1（ii）R1如上文（i）和（R2）中所定义，R3与氮原子一起表示任选取代的杂环或稠合杂环基; 或（iii）与氮原子一起的R 1，R 2，R 3代表任选取代的二氮杂双环或氮杂三环基; 或（iv）R 1，R 2，R 3与氮原子一起代表任选取代的吡啶鎓，吡嗪鎓，吡唑鎓或哒嗪鎓基团，该基团任选地与一个苯环或与5-7元饱和或不饱和的 脂环族或杂环，或其具有高抗菌活性的药学上或兽医学上可接受的盐。

公开(公告)号：US4713378A

公开(公告)日：1987-12-15

申请号：US747829

申请日：1985-06-24

申请人： Ettore Perrone ,  Marco Alpegiani ,  Franco Zarini ,  Costantino D. Bruna ,  Giovanni Franceschi

发明人： Ettore Perrone ,  Marco Alpegiani ,  Franco Zarini ,  Costantino D. Bruna ,  Giovanni Franceschi

IPC分类号： C07D513/04 ,  A61K31/425 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/06 ,  C07D499/88 ,  C07D499/897 ,  C07D519/00 ,  C07D519/06

CPC分类号： C07D499/88

摘要： There are provided compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.3 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, and Q.sup.(+) represents a group ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each either: (i) optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical or(iii) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical or(iv) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted fused pyridinium radical or(v) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted pyrazimium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof.A method of preparation is also provided.The compounds show high antibacterial activity.

摘要翻译： 提供式IMA的化合物，其中R是氢原子或任选被卤素原子或任选被保护的羟基取代的C 1 -C 3烷基，Q（+）代表基团，其中R 1，R 2和R 3各自是 （i）任选取代的烷基，芳烷基或芳基，或（ii）R 1如（i）中所定义，R 2，R 3一起表示任选取代或稠合的杂环基，或（iii）R 1，R 2， R 3一起代表任选取代的亚氮基 - 双环或三环基或（iv）R 1，R 2，R 3一起代表任选取代的稠合吡啶鎓基或（ⅴ）R 1，R 2，R 3一起代表 任选取代的吡嗪鎓，吡唑鎓或哒嗪基，以及其药学或兽医学上可接受的盐。 还提供了一种制备方法。 该化合物显示出高抗菌活性。