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1. 发明公开

EP0170118A3 4-Substituted-1,2,4,6-thiatriazine derivatives 失效
标题翻译： 4-取代的1,2,4,6-噻二唑衍生物
公开(公告)号：EP0170118A3
公开(公告)日：1986-12-03
申请号：EP85108581
申请日：1985-07-10
申请人： HOECHST UK LIMITED
发明人： Michael, Jeffrey Daniel , Ross, Barry Clive, Dr.
IPC分类号： C07D285/00 , C07C161/00 , A01N43/72 , C07D513/04 , C07D235/00
CPC分类号： C07D285/15 , A01N43/72 , C07D513/04
摘要： A process for the production of a compound of formula

in which
R represents an aryl group, especially a phenyl group, which may be unsubstituted or substituted by one or two substituents, which may be the same or different, selected from methyl, trifluoromethyl, nitro and cyano groups, and chlorine, fluorine and bromine atoms; R 1 represents a hydrogen atom, a straight or branched chain alkyl group having from 1 to 6 carbon atoms or a cycloalkyl group having from 3 to 7 carbon atoms, which alkyl or cycloalkyl group is unsubstituted or substituted, or R 1 represents a straight or branched chain alkenyl group having from 2 to 6 carbon atoms or a straight or branched chain alkynyl group having from 3 to 6 carbon atoms; R represents an aryloxy group, especially a phenoxy group, which is unsubstituted or is substituted as defined above for aryl groups R; or R 2 represents an -NHR 3 group in which R 3 represents a hydrogen atom or a straight or branched chain alkyl group having from 1 to 6 carbon atoms that is unsubstituted or substituted, or an aromatic or non-aromatic heterocyclic group as defined above; or R 2 represents a group NHR 3 , and R 1 and R 3 , together with the atoms to which they are attached, form a 5- or 6-membered ring containing two nitrogen atoms, and p represents the integer 1 or 2, which comprises (a) reacting a compound of formula II
in which R and p are as defined above, with an amine of formula III in which R 1 is as defined above and, if desired, (b) reacting a resulting compound of formula I in which R 2 represents an optionally substituted aryloxy group with an amine of formula IV
in which R 3 is as defined above, to give a compound of formula I in which R 2 represents group NHR 3 ; or (c) reacting a compound of formula II as defined above with a diamine of formula V in which n represents 2 or 3 to give a compound of formula I in which R 2 represents a group NHR 3 , and R 1 and R 3 , together with the atoms to which they are attached, form a 5- or 6-membered ring containing two nitrogen atoms and, if desired, at any stage, (d) oxidising a resulting compound of formula I in which p represents the integer 1 to give the corresponding compound in which p represents the integer 2. The compounds of formula I are useful in the manufacture of 5-substituted 1, 2, 4, 6-thiatriazines.
摘要翻译：一种制备式...化合物的方法，其中... R表示芳基，特别是苯基，其可以是未取代的或被一个或两个可以相同或不同的取代基所取代甲基，三氟甲基，硝基和氰基以及氯，氟和溴原子; R 1表示氢原子，具有1至6个碳原子的直链或支链烷基或具有3至 7个碳原子，其中烷基或环烷基是未取代的或取代的，或... R 1表示具有2至6个碳原子的直链或支链烯基或具有3至6个碳原子的直链或支链炔基 R 2表示芳氧基，特别是苯氧基，其未被取代或被如上对芳基R所定义而被取代; 或R 2表示-NHR 3基团，其中R 3表示氢原子或具有未取代或取代的具有1至6个碳原子的直链或支链烷基，或芳族或非芳族基团 - 芳族杂环基; 或者R 2代表基团NHR 3，R 1和R 3与它们连接的原子一起形成含有两个氮原子的5-或6-元环，和 p表示整数1或2，其包括（a）使其中R和p如上定义的式II ... ...的化合物与式III的胺反应，其中R 1，R 2，其中R 1如上所定义，并且如果需要，（b）使得到的其中R 2表示被取代的芳氧基的式I化合物与式IV的胺反应，得到式其中R 3如上定义，得到其中R 2表示NHR 3基团的式I化合物; 或（c）使如上定义的式II化合物与式V 2 H 2 N - （CH 2）n -NH 2 V 2的二胺反应，其中n表示2或3，得到式I化合物，其中R 2，代表基团NHR 3，R 1和R 3与它们所连接的原子一起形成含有两个氮原子的5或6元环，如果需要，在任何阶段，（d）氧化得到的式I化合物，其中p表示整数1，得到其中p表示整数2的相应化合物。式I化合物可用于制备5-取代的 1，2,4,6-噻二嗪。

2. 发明公开

EP0099059A1 Antibacterial penem derivatives 失效
标题翻译：抗菌青霉烯衍生物。
公开(公告)号：EP0099059A1
公开(公告)日：1984-01-25
申请号：EP83106589.1
申请日：1983-07-06
申请人： HOECHST UK LIMITED
发明人： Cooke, Michael David , Ross, Barry Clive, Dr.
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D409/12 , C07D205/08 , C07D205/09 , C07D333/34 , C07D333/38 , C07D499/88 , C07F7/1856
摘要： The present invention relates to certain penem derivatives of the general formula I
in which R represents a hydrogen atom or a carboxyl esterifying group, R 1 represents certain unsubstituted and substituted aromatic and heterocyclic groups, and R 2 represents a hydrogen atom, an unsubstituted or substituted alkyl or aryl group.
The compound of formula I and salts thereof may be used in the treatment of bacterial infections in man and other animals.

3. 发明公开

EP0156286A3 Thiatrizine derivatives 失效
标题翻译：噻吗啉衍生物
公开(公告)号：EP0156286A3
公开(公告)日：1986-08-20
申请号：EP85103156
申请日：1985-03-19
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Allen, Robert Manning , Cousins, Simon John
IPC分类号： C07D417/12 , C07D285/00 , A61K31/54
CPC分类号： C07D285/15 , C07D417/12
摘要： Salts of 3-amino-5-[2-[ (2-guanidino-4-thiazolyl) -methylthio] ethylamino] -4-methyl-1,2,4,6-thiatriazine-1, 1-dioxide with various acids are prepared in crystalline form. The salts contain varying amounts of crystal water or crystal solvent.

4. 发明公开

EP0091576A3 7-Oxo-4-thia-1-azabicyclo(3,2,0)heptane derivatives 失效
标题翻译： 7-氧代-4-噻唑-1-亚氨基（3,2,0）二氢衍生物
公开(公告)号：EP0091576A3
公开(公告)日：1983-12-14
申请号：EP83102818
申请日：1983-03-22
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Johnson, Graham, Dr.
IPC分类号： C07D499/00 , C07D205/08 , C07D409/06 , C07F07/28
CPC分类号： C07D409/06 , C07D205/08 , C07D205/09 , C07D499/88 , C07F7/186
摘要： Compounds of the formula la and their tautomers Ib
in which formulae R represents a carboxyl esterifying group are described, as well as processes and intermediates for their manufacture. la and Ib are valuable starting materials for the preparation of various derivatives substituted at position 3 that possess antibacterial properties.

5. 发明公开

EP0031509A1 Penem derivatives 失效
标题翻译：青霉烯衍。
公开(公告)号：EP0031509A1
公开(公告)日：1981-07-08
申请号：EP80107722.3
申请日：1980-12-08
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Johnson, Graham, Dr.
IPC分类号： C07D487/04 , A61K31/415
CPC分类号： C07D487/04 , C07D205/09 , C07D499/00 , C07D513/04
摘要： A penem derivative of the formula I
wherein R is hydrogen, kation or a carboxyl esterifying group, R 1 is alkyl or aryl, its manufacture, its use as a β-lactame inhibitor or an antibacterial agent and a preparation comprising it.
摘要翻译：式I的青霉烯衍生物... 其中R是氢，kation或羧基酯化基团，R 1是烷基或芳基，其制备，其作为β-反乳糖抑制剂或抗菌剂的用途和包括它的制备。

6. 发明授权

EP0091576B1 7-Oxo-4-thia-1-azabicyclo(3,2,0)heptane derivatives 失效
标题翻译： 7-氧代-4-硫杂-1-氮杂双环（3,2,0）庚烷衍生物
公开(公告)号：EP0091576B1
公开(公告)日：1987-07-29
申请号：EP83102818.8
申请日：1983-03-22
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Johnson, Graham, Dr.
IPC分类号： C07D499/00 , C07D205/08 , C07D409/06
CPC分类号： C07D409/06 , C07D205/08 , C07D205/09 , C07D499/88 , C07F7/186

7. 发明公开

EP0176064A1 Intermediates for the production of 7-oxo-4-thia-1-aza[3,2,0]heptane and 7-oxo-4-thia-1-aza[3,2,0]hept-2-ene derivatives 失效
标题翻译： Zwischenprodukte zur Herstellung von 7-氧代-4-硫杂-1-氮杂-3,2,0庚-7-烯-4-硫杂-1-氮杂-3,2,0庚-2-烯衍生物
公开(公告)号：EP0176064A1
公开(公告)日：1986-04-02
申请号：EP85111993.3
申请日：1981-10-29
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Johnson, Graham, Dr. , Yeomans, Michael Alan, Dr.
IPC分类号： C07D205/08 , C07F7/18
CPC分类号： C07D513/04 , C07D205/09 , C07D499/88 , C07F7/186
摘要： Compounds of formula
are valuable intermediates for the production of 7-oxo-4-thia-1-azabicyclo [3,2,0] hept-ene derivatives.
摘要翻译：式的化合物是生产7-氧代-4-硫杂-1-氮杂双环[3,2,0]庚烯衍生物的有价值的中间体。

8. 发明公开

EP0159533A2 Thiatriazine derivatives 失效
标题翻译：噻三嗪衍生物
公开(公告)号：EP0159533A2
公开(公告)日：1985-10-30
申请号：EP85103158.3
申请日：1985-03-19
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Michael, Jeffrey Daniel , Cousins, Simon John
IPC分类号： C07D285/00 , C07D417/12 , A61K31/54 , C07C161/00
CPC分类号： C07D285/15 , C07C307/04 , C07C333/00 , C07C335/38 , C07D417/12
摘要： Compounds of formula I
are valuable H-2 antagonists; R represents hydrogen, alkyl, phenyl or phenalkyl; W and Z represent groups E-(CH 2 ) n -X-(CH 2 ) m- NH with E being phenyl, imidazolyl, thiazolyl, furyl, thienyl or pyridyl; or W or Z is hydrogen, alkyl, phenyl, O-alkyl, NR 4 R 5 (R 4 /R 5 are hydrogen, alkyl or phenyl); X is O or S; n is 0 or 1, m is 2, 3 or 3.
Moreover compounds XXXI are described
in which R 31 /R 32 are H, alkyl, cycloalkyl, phenyl, phenylkyl or part of 4-to 7-membered ring: L 3 /L 4 are X-(alkyl-phenyl, -phenalkyl), compounds XXXI are versatile intermediates for the production of i.a. compounds I.
ComDounds XXXV
with R 42 /R 43 being hydrogen, alkyl, phenyl, phenyalkyl are also versatile intermediates inter alia for the preparation of compounds I.
Processes for the preparation of these compounds are disclosed as well.
摘要翻译：式I化合物是有价值的H-2拮抗剂; R代表氢，烷基，苯基或苯基烷基; W和Z代表E-（CH2）n-X-（CH2）m-NH基团，其中E为苯基，咪唑基，噻唑基，呋喃基，噻吩基或吡啶基; 或W或Z为氢，烷基，苯基，O-烷基，NR 4 R 5（R 4 / R 5为氢，烷基或苯基）。 X是O或S; 此外，描述了其中R 31 / R 32是H，烷基，环烷基，苯基，苯基烷基或部分4-至7-元环的化合物XXXI：其中R 3 / L 4是X - （烷基 - 苯基， - 苯基烷基），化合物XXXI是用于生产ia的通用中间体化合物I.化合物XXXV与R42 / R43是氢，烷基，苯基，苯基烷基也是用于制备化合物I的通用中间体。此外，还公开了制备这些化合物的方法。

9. 发明公开

EP0127847A1 7-Oxo-4-thia-1-azabicyclo(3.2.0)hept-2-ene derivatives 失效
标题翻译： 7-氧代-4-硫杂-1-氮杂二环（3.2.0）庚-2-烯 - 衍生物。
公开(公告)号：EP0127847A1
公开(公告)日：1984-12-12
申请号：EP84105904.1
申请日：1984-05-24
申请人： HOECHST UK LIMITED
发明人： Blumbach, Jürgen, Dr. , Ross, Barry Clive, Dr. , Johnson, Graham, Dr.
IPC分类号： C07D499/00 , C07D519/00 , A61K31/43
CPC分类号： C07D257/04 , C07D499/88
摘要： A process for the preparation of a compound of the general formula I
is described according to which a compound of the general formula IIb
is reacted with a compound of formula III
in which

L represents a leaving group, generally carrying out the reaction in the presence of a base.
R' represents an alkylene, alkenylene or alkynylene group, having from 1 to 4 carbon atoms, and
R 2 represents a heterocyclic group having a five-membered or 6-membered ring with 1 to 4 heteroatoms, selected from oxygen sulfur and nitrogen, and being linked to the adjacent sulphur atom via a ring carbon atom.
摘要翻译：描述了制备通式I 的化合物的方法，根据该方法，使通式IIb的化合物与式III的化合物反应。L-R 1 -S- （III）其中L代表离去基团，通常在碱的存在下进行反应。 R 1表示具有1至4个碳原子的亚烷基，亚烯基或亚炔基，R 2表示具有1至4个杂原子的五元或六元环的杂环基，其选自氧硫和氮，并且通过环碳原子与相邻的硫原子连接。

10. 发明授权

EP0099059B1 Antibacterial penem derivatives 失效
标题翻译：抗菌青霉烯衍生物
公开(公告)号：EP0099059B1
公开(公告)日：1988-06-22
申请号：EP83106589.1
申请日：1983-07-06
申请人： HOECHST UK LIMITED
发明人： Cooke, Michael David , Ross, Barry Clive, Dr.
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D409/12 , C07D205/08 , C07D205/09 , C07D333/34 , C07D333/38 , C07D499/88 , C07F7/1856

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