公开(公告)号：EP0255335A2

公开(公告)日：1988-02-03

申请号：EP87306649.2

申请日：1987-07-28

申请人： Pfizer Limited

发明人： Goudie, Alexander Crossan ,  Walshe, Nigel Derek Arthur

IPC分类号： C07H19/01 ,  A61K31/70

CPC分类号： C07H19/01

摘要： A new acidic polycyclic antibiotic UK-61,689 has the formula:
or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilisation in swine and ruminants.

摘要翻译： 一种新的酸性多环抗生素UK-61,689具有下式：或其药学上可接受的阳离子盐。 抗生素及其阳离子盐对多种微生物具有活性，有效控制球虫病，肠炎和猪痢疾，以及有效促进猪和反刍动物生长和/或提高饲料利用效率。

公开(公告)号：EP0255335B1

公开(公告)日：1991-02-06

申请号：EP87306649.2

申请日：1987-07-28

申请人： Pfizer Limited

发明人： Goudie, Alexander Crossan ,  Walshe, Nigel Derek Arthur

IPC分类号： C07H19/01 ,  A61K31/70

CPC分类号： C07H19/01

公开(公告)号：EP0042731A1

公开(公告)日：1981-12-30

申请号：EP81302745.5

申请日：1981-06-18

申请人： Pfizer Limited ,  Pfizer Corporation

发明人： Banks, Bernard Joseph ,  Leeming, Michael Raymond Graves ,  Penrose, Alexander Ballingall ,  Walshe, Nigel Derek Arthur

IPC分类号： C07D333/34 ,  C07D409/12 ,  C07D417/12 ,  C07D413/12 ,  C07F7/08 ,  A01N43/00

CPC分类号： C07F7/0814 ,  A01N43/10 ,  A01N43/30 ,  A01N43/40 ,  A01N43/42 ,  A01N43/50 ,  A01N43/58 ,  A01N43/60 ,  A01N43/76 ,  A01N47/22 ,  A01N47/46 ,  A01N47/48 ,  A01N55/00 ,  C07D333/34

摘要： Compounds of the formula:
and their alkali metal or non-toxic acid addition salts, wherein:

(a) R' is hydrogen or lower alkyl; and R 2 is lower alkyl lower alkoxy, 2,2,2-trifluoroethyl, hydroxy-lower alkyl, 2-methoxyethoxymethyl, lower alkoxycarbonyl-lower alkyl, lower alkanoyloxy-lower alkyl, aryl-lower alkyl, aryloxy-lower alkyl, thiocyanatoacetyl, lower cycloalkyl-lower alkyl, lower cycloalkyl, lower cycloalkenyl, lower alkenyl, allenyl, lower alkynyl, C 2 -C 16 alkanoyl, halo-lower alkanoyl, aryl-lower alkanoyl, N,N-di(lower alkyl)sulfamoyl, 1,2,3,4-tetrahydronaphthyl, arylthio, aryl or aroyl; or R' and R 2 together with the nitrogen atom to which they are attached form a saturated 5- or 6- membered heterocyclic group optionally containing a further heteroatom selected from 0, S and N, said N atom bearing a hydrogen atom or a lower alkyl or aryl group, said heterocyclic group optionally being substituted on a carbon atom by 1 or 2 lower alkyl groups;
(b) X is 0, S, SO or S0 2 ;
(c) Y is halogen, lower alkyl, tri(lower alkyl)silyl, lower alkoxy, or a group of the formula R 3 S- or R 3 S0 2 - wherein R 3 is lower alkyl or aryl; n is 0 or 1; and
(d) R is lower alkyl, lower alkenyl, lower cycloalkyl, allenyl, lower alkoxy-lower alkyl, aryl-lower alkyl, aryl, heteroaryl or heteroaryl-phenyl, with the proviso that when X is SO 2 , R can also be-NR 1 R 2 wherein R' and R 2 are as defined above;

the term "lower" as applied to an alkyl, alkoxy, alkanoyl, alkenyl or alkynyl group means that said group has up to 6 carbon atoms; "lower" as applied to a cycloalkyl group means that said group has from 3 to 7 carbon atoms; "lower" as applied to a cycloalkenyl group means that said group has from 4 to 7 carbon atoms;
and the term "aryl" means unsubstituted phenyl, unsubstituted naphthyl or substituted phenyl.
The compounds are insecticidal, particularly larvicidal agents, and some have acaricidal and miticidal activity. They are particularly used as blowfly larvicides on sheep and cattle.

摘要翻译： 下式的化合物：及其碱金属或无毒性的酸加成盐，worin：（1）R <1>是氢或低级烷基; 且R <2>是低级烷基，低级烷氧基，2,2,2，三氟乙基，羟基 - 低级烷基，2-甲氧基乙氧基甲基，低级烷氧羰基 - 低级烷基，低级链烷酰氧基 - 低级烷基，芳基 - 低级烷基，芳氧基 - 低级 烷基，thiocyanatoacetyl，低级环烷基 - 低级烷基，低级环烷基，低级环烯基，低级烯基，丙二烯基，低级炔基，C2-C16烷酰基，卤代 - 低级链烷酰基，芳基 - 低级链烷酰基，N，N-二（低级烷基）氨磺酰基， 1,2,3,4-四氢萘基，芳硫基，芳基或芳酰基; 或R <1>和R <2>与氮原子一起与它们所连接形成任选含有另外的杂原子的饱和5-或6-元杂环基团选自O，S和N，所述N原子带有氢选择 原子或低级烷基或芳基，杂环基任选地，所述substituiertem被1或2个低级烷基的基团是碳原子上的; （B）X是O，S，SO或SO 2; （C）Y是卤素，低级烷基，三（低级烷基）甲硅烷基，低级烷氧基，或基团的式R <3> S-或R <3> SO2 worin - [R <3>是低级烷基或芳基的; n是0或1; 和（d）R是低级烷基，低级烯基，低级环烷基，丙二烯基，低级烷氧基 - 低级烷基，芳基 - 低级烷基，芳基，杂芳基或杂芳基 - 苯基，其条件没有当X是SO 2，R可以因此是 - NR <1> [R <2> worin - [R <1>和R <2>如上面所定义; 术语“低级”用于上烷基，烷氧基，烷酰基，烯基或炔基bedeutet，DASS所述基团具有至多6个碳原子; “低级”用于环烷基bedeutet，DASS所述基团具有3至7个碳原子; “低级”用于环烯基bedeutet，DASS所述基团具有4至7个碳原子; 并且术语“芳基”意指苯基unsubstituiertem，萘基或unsubstituiertem substituiertem苯基。 该化合物的杀虫，杀幼虫特别剂和一些有杀螨和杀螨活性。 它们特别用作羊和牛蝇幼虫剂。

公开(公告)号：EP0255335A3

公开(公告)日：1988-06-08

申请号：EP87306649

申请日：1987-07-28

申请人： Pfizer Limited

发明人： Goudie, Alexander Crossan ,  Walshe, Nigel Derek Arthur

IPC分类号： C07H19/01 ,  A61K31/70

CPC分类号： C07H19/01

摘要： A new acidic polycyclic antibiotic UK-61,689 has the formula:
or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilisation in swine and ruminants.

公开(公告)号：EP0042731B1

公开(公告)日：1984-12-05

申请号：EP81302745.5

申请日：1981-06-18

申请人： Pfizer Limited ,  Pfizer Corporation

发明人： Banks, Bernard Joseph ,  Leeming, Michael Raymond Graves ,  Penrose, Alexander Ballingall ,  Walshe, Nigel Derek Arthur

IPC分类号： C07D333/34 ,  C07D409/12 ,  C07D417/12 ,  C07D413/12 ,  C07F7/08 ,  A01N43/00

CPC分类号： C07F7/0814 ,  A01N43/10 ,  A01N43/30 ,  A01N43/40 ,  A01N43/42 ,  A01N43/50 ,  A01N43/58 ,  A01N43/60 ,  A01N43/76 ,  A01N47/22 ,  A01N47/46 ,  A01N47/48 ,  A01N55/00 ,  C07D333/34