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11. 发明公开

EP0102026A3 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：EP0102026A3
公开(公告)日：1984-05-16
申请号：EP83108102
申请日：1983-08-17
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive , Michael, Jeffrey Daniel
IPC分类号： C07D417/12 , A61K31/425 , A61K31/44 , C07D233/86 , C07D233/96
CPC分类号： C07D401/06 , C07D233/86 , C07D233/96 , C07D405/06 , C07D417/12 , C07D417/14
摘要： New thiazole derivatives of the general formula I
and their salts with physiologically acceptable acids are described as well as a process for their manufacture. The new compounds exhibit histamine H-2 antagonist activity and may thus be used to inhibit gastric acid secretion and to treat gastric and peptic ulcers.

12. 发明公开

EP0069378A2 Antibacterial penem derivatives 失效
标题翻译： Antibakterielle Penemderivate。
公开(公告)号：EP0069378A2
公开(公告)日：1983-01-12
申请号：EP82105990.4
申请日：1982-07-05
申请人： HOECHST UK LIMITED
发明人： Cooke, Michael David , Ross, Barry Clive
IPC分类号： C07D499/00 , C07D205/08 , A61K31/43
CPC分类号： C07D205/09 , C07D205/08 , C07D499/88
摘要： Penem-Derivatives of the formula I
in which

R is hydrogen or a carboxyl esterifying group
R' is phenyl, naphthyl, thienyl, pyridyl, quinolyl or isoquinolyl any of which is optionally substituted by one, two or three substituents of the group halogen, cycloalkyl, -NH 2 , -CONH 2 , -NO 2 , -CN, -R 2 , -OR 2 , -SR 2 , -SO-R 2 , -SO 2 R 2 , -CO-R 2 , -CO-O-R 2 , -CH 2 -CO-O-R 2 , -NHR 2 , -NR 2 R 2' , -CO-NH-R 2 , -CO-NR 2 R 2' , -NH-CO-R 2 , -NH-CO-NH 2 , -NH-CO-NH-R 2 , -NH-S0 2 -R 2 , -CF 3 , -CO-OH, -CH 2 -CO-OH wherein R 2 and R 2' are the same or different and each represents alkyl of 1 to 4 carbon atoms or a salts thereof, process for the manufacture thereof and antibacterial pharmaceutical preparations containing them.
摘要翻译：式I的化合物衍生物... ...其中R是氢或羧基酯化基团R 1是苯基，萘基，噻吩基，吡啶基，喹啉基或异喹啉基，任何一个任选被一个，二个或三个取代基的卤素，环烷基，-NH 2，-CONH 2，-NO 2，-CN，-R 2，-OR 2，-SR 2，-SO-R 2，-SO 2 R -CO-R 2，-CO-OR 2，-CH 2 -CO-OR 2，-NHR 2，-NR 2 R 2 min，-CO- NH-R 2，-CO-NR 2 R 2 min，-NH-CO-R 2，-NH-CO-NH 2，-NH-CO-NH-R 2， NH 2 SO 2 R 2，-CF 3，-CO-OH，-CH 2 -COOH其中R 2和R 2分别相同或不同，并且各自表示1至4个碳原子的烷基或其盐，其制备方法和含有它们的抗菌药物制剂。

13. 发明公开

EP0169969A3 Sulphamoylguanidine derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：EP0169969A3
公开(公告)日：1987-02-04
申请号：EP85103157
申请日：1985-03-19
申请人： HOECHST UK LIMITED
发明人： Cousins, Simon John , Michael, Jeffrey Daniel , Ross, Barry Clive, Dr.
IPC分类号： C07C161/00 , C07D277/48 , C07D285/08 , C07C157/14 , A61K31/41 , A61K31/155
CPC分类号： C07D285/08 , C07C307/04 , C07C333/00 , C07C335/38 , C07D277/48 , C07D295/096 , C07D417/12
摘要： Described are compounds of formula XLI

with R, R 42 and R 43 being hydrogen, alkyl, phenyl or phenalkyl A being phenyl, furyl, thiazolyl or thiadiazolyl; X being oxygen or sulphur; n being 0 or 1; and m being 2, 3 or 4. Described is a process for their production reacting compounds XLIII
(L being X-alkyl or X-phenylalkyl with compound XLV
or reacting compound XLIV

with HNR 42 R 43 XLVI. Compounds XLI are valuable H-2 antagonists.
摘要翻译：描述的是式XLI 的化合物，其中R，R 4和R 4是氢，烷基，苯基或苯基烷基是苯基呋喃基，噻唑基或噻二唑基; X为氧或硫; n为0或1; 描述的是其化合物XLIII （L为X-烷基或X-苯基烷基与化合物XLV A - （CH 2）n -X-（CH 2）m -NH 2）反应的方法 XLV或使化合物XLIV 与HNR 4> R 4> 3 XLVI化合物XLI是有价值的H-2拮抗剂。

14. 发明授权

EP0069378B1 Antibacterial penem derivatives 失效
标题翻译：抗菌素衍生物
公开(公告)号：EP0069378B1
公开(公告)日：1987-01-07
申请号：EP82105990.4
申请日：1982-07-05
申请人： HOECHST UK LIMITED
发明人： Cooke, Michael David , Ross, Barry Clive
IPC分类号： C07D499/00 , C07D205/08 , A61K31/43
CPC分类号： C07D205/09 , C07D205/08 , C07D499/88

15. 发明公开

EP0204148A2 [1,4]Benzodioxin and [1,4]benzoxazine derivatives 失效
标题翻译： ¬1,4苯并二恶英和¬1,4苯并恶嗪
公开(公告)号：EP0204148A2
公开(公告)日：1986-12-10
申请号：EP86105976.4
申请日：1986-04-30
申请人： HOECHST UK LIMITED
发明人： Allen, Robert Manning , Fletcher, Stephen Robert
IPC分类号： C07D319/20 , C07D265/36 , C07D405/08 , C07D413/08 , C07D417/08 , A61K31/535 , A61K31/335 , A61K31/54
CPC分类号： C07D405/12 , C07D265/36 , C07D319/20 , C07D417/12 , Y02P20/55
摘要： A compound of formula I
in which formula

R 1 and R 2 , which may be the same or different, each represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms or, together with the nitrogen atom to which they are attached, R 1 and R 2 form a 4 to 8-membered ring which may contain an oxygen atom or another nitrogen atom, which nitrogen atom may have an alkyl group having from 1 to 4 carbon atoms as substituent.
X represents an oxygen atom or a group NR 4 in which R 4 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, a phenyl group or a phenalkyl group, the alkyl moiety of which has from 1 to 4 carbon atoms.
an alkyl, phenyl or phenalkyl group being unsubstituted or substituted, or
R 4 represents a nitrogen protecting group;
m represents an integer of from 1 to 4;
n represents the integer 1 or 2; and
R 3 represents a group of formula II, III, IV, V or VI

in which formulae
R 5 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; and R 6 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, an alkenyl group having from 2 to 4 carbon atoms, or an alkynyl group having 3 or 4 carbon atoms has histamine H-2 antagonist activity, and may be used to produce medicaments.
摘要翻译：式I化合物其中R 1和R 2可以相同或不同，分别表示氢原子，具有1至4个碳原子的烷基，或者与与它们相连的氮原子，R 1和R 2形成可含有氧原子或另一个氮原子的4至8元环，该氮原子可具有1-4个碳原子的烷基碳原子作为取代基。 X表示氧原子或基团NR 4，其中R 4表示氢原子，具有1至4个碳原子的烷基，苯基或苯烷基，其烷基部分具有1个至4个碳原子。未取代或取代的烷基，苯基或苯烷基，或R 4表示氮保护基; m表示1〜4的整数， n表示整数1或2; R 3表示式II，III，IV，V或VI的化合物，其中式R 5表示氢原子或具有1至4个碳原子的烷基; R 6表示氢原子或具有1至4个碳原子的烷基，具有2至4个碳原子的链烯基或具有3或4个碳原子的炔基具有组胺H 2拮抗剂活性，并可用于生产药物。

16. 发明授权

EP0051813B1 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： 7-氧代-4-硫杂-1-氮杂（3,2,0）庚烷和7-氧代-4-硫杂-1-氮杂（3,2,0）庚-2-烯衍生物
公开(公告)号：EP0051813B1
公开(公告)日：1986-07-30
申请号：EP81109176.8
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： C07D499/00 , C07D513/04 , C07D205/08 , A61K31/43
CPC分类号： C07D513/04 , C07D205/09 , C07D499/88 , C07F7/186

17. 发明公开

EP0170118A2 4-Substituted-1,2,4,6-thiatriazine derivatives 失效
标题翻译： 4-取代的-1,2,4,6-噻三嗪衍生物
公开(公告)号：EP0170118A2
公开(公告)日：1986-02-05
申请号：EP85108581.1
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
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：用于制备其中R代表芳基，特别是苯基的式（I）化合物的方法，该芳基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取代，所述取代基选自甲基，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个碳原子的环烷基，该烷基或环烷基未被取代或被取代，或者R 1表示直链或支链具有2至6个碳原子的链烯基或具有3至6个碳原子的直链或支链炔基; R表示芳氧基，尤其是苯氧基，其未被取代或如上对芳基R所定义的那样被取代; 或R2代表-NHR3基团，其中R3代表氢原子或未取代或取代的具有1至6个碳原子的直链或支链烷基，或如上定义的芳族或非芳族杂环基团; 或R 2代表基团NHR 3，并且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，并且p代表整数1或2，其包含（a）使其中R 1和p如上定义的式II化合物与其中R 1如上所定义的式III胺反应，并且如果需要，（b）使得到的式I化合物其中R 2表示任选取代的芳氧基用式IV的胺（其中R 3如上定义）反应，得到其中R 2表示NHR 3基团的式I化合物; 或（c）将如上定义的式II化合物与其中n表示2或3的式V的二胺反应，得到其中R2表示基团NHR3的式I化合物，并且R1和R3与原子（d）将所得的其中p表示整数1的式I化合物氧化，得到相应的化合物（其中R 1和R 2与它们相连）形成含有两个氮原子并且如果需要的话在任何阶段的5-或6-元环。其中p代表整数2.式I化合物可用于制备5-取代的1,2,4,6-噻三嗪。

18. 发明公开

EP0156286A2 Thiatrizine derivatives 失效
标题翻译： Thiatrizine衍生物
公开(公告)号：EP0156286A2
公开(公告)日：1985-10-02
申请号：EP85103156.7
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.
摘要翻译： 3-氨基-5- [2 - [（2-胍基-4-噻唑基） - 甲硫基]乙氨基] -4-甲基-1,2,4,6-噻三嗪-1,1-二氧化物与各种酸的盐是以结晶形式制备。盐含有不同量的结晶水或结晶溶剂。

19. 发明授权

EP0031509B1 Penem derivatives 失效
标题翻译：笔式衍生物
公开(公告)号：EP0031509B1
公开(公告)日：1984-10-24
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

20. 发明公开

EP0091576A2 7-Oxo-4-thia-1-azabicyclo(3,2,0)heptane derivatives 失效
标题翻译： 7-氧代-4-硫杂-1-氮杂二环（3.2.0）庚烷 - 衍生物。
公开(公告)号：EP0091576A2
公开(公告)日：1983-10-19
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
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.

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