专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明公开

EP0204148A3 [1,4]Benzodioxin and [1,4]benzoxazine derivatives 失效
标题翻译： Û1,4﹑苯并INE嗪和Û1,4-苯并吖嗪衍生物
公开(公告)号：EP0204148A3
公开(公告)日：1987-01-07
申请号：EP86105976
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。

42. 发明公开

EP0185651A1 Intermediates for the production of antibacterial penem derivates 失效
标题翻译： Zwischenprodukte zur Herstellung von antibakteriellen Penemderivaten。
公开(公告)号：EP0185651A1
公开(公告)日：1986-06-25
申请号：EP86100522.1
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： C07D205/08
CPC分类号： C07D205/09 , C07D205/08 , C07D499/88
摘要： Compounds of formula II
with R being hydrogen or an esterifying group; R 1 being unsubstituted or substituted phenyl, naphthyl or thienyl; and Ra-Re being H or C l -C 4 -alkyl are valuable intermediates for the production of penems which exhibit antibacterial activity.
摘要翻译：式II化合物其中R为氢或酯化基团：R 1为未取代或取代的苯基，萘基或噻吩基; 和Ra-Re为H或C 1 -C 4 - 烷基是生产具有抗菌活性的青霉素的有价值的中间体。

43. 发明公开

EP0169969A2 Sulphamoylguanidine derivatives 失效
标题翻译：氨磺酰胍衍生物
公开(公告)号：EP0169969A2
公开(公告)日：1986-02-05
申请号：EP85103157.5
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：描述了式XLI的化合物，其中R 1，R 42和R 43是氢，烷基，苯基或苯基烷基A是苯基，呋喃基，噻唑基或噻二唑基; X是氧或硫; n是0或1; m为2,3或4.描述了它们的制备方法，它们使化合物XLIII（L为X-烷基或X-苯基烷基与化合物XLV反应或者使化合物XLIV与HNR42R43 XLVI反应）化合物XLI是有价值的H-2拮抗剂。

44. 发明公开

EP0069377A3 Antibacterial penem derivatives 失效
标题翻译：抗菌青霉烯衍生物
公开(公告)号：EP0069377A3
公开(公告)日：1983-04-13
申请号：EP82105989
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 , C07F07/18 , C07D333/38 , C07D409/12
CPC分类号： C07D205/08 , C07D205/09 , C07D333/38 , C07D499/88 , C07F7/186
摘要： Penem derivative of the formula 1
in which
R is hydrogen or a carboxyl esterifying group, R 1 is phenyl, napthyl, thienyl, pyridyl, quinolyl or isoquinolyl being unsubstituted or substituted by one, two or three of the same or different substituents selected from halogen, hydroxy, amino, nitro, cyano, azido, alkyl, alkoxy, alkanesulfenyl, alkanesulfinyl, alkanesulfonyl, alkanoyl, alkoxycarbonyl, alkanoyloxy, carbamoyl, ureido, carba- moyloxy, alkanoylamino, aminosulfamoyl, sulfamoyl, guani- dino, trifluormethyl, trifluormethanesulfenyl, trifluor- methanesulfinyl, trifluormethanesulfonoyl and formyl, which may be substituted by one, two or three lower alkyl groups being the same or different. R 2 represents a hydrogen atom or a optionally protected hydroxyl group, or a salt thereof,
process for the production thereof and antibacterial pharmaceutical preparations comprising them.
摘要翻译：其中R为氢或羧基酯化基团的式1的青霉烯衍生物，R 1为未取代的苯基，萘基，噻吩基，吡啶基，喹啉基或异喹啉基或被1,2或3个相同或不同的选自卤素，羟基，氨基，硝基，氰基，叠氮基，烷基，烷氧基，烷烃亚磺酰基，烷烃亚磺酰基，烷磺酰基，烷酰基，烷氧基羰基，烷酰氧基，氨基甲酰基，脲基，甲磺酰基，三氟甲磺酰基和甲酰基，它们可以被一个，两个或三个低级烷基相同或不同。 R2代表氢原子或任选保护的羟基，或其盐，其制备方法和包含它们的抗菌药物制剂。

45. 发明公开

EP0069377A2 Antibacterial penem derivatives 失效
标题翻译：抗菌青霉烯衍生物
公开(公告)号：EP0069377A2
公开(公告)日：1983-01-12
申请号：EP82105989.6
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： C07D205/08 , C07D205/09 , C07D333/38 , C07D499/88 , C07F7/186
摘要： Penem derivative of the formula 1
in which

R is hydrogen or a carboxyl esterifying group,
R 1 is phenyl, napthyl, thienyl, pyridyl, quinolyl or isoquinolyl being unsubstituted or substituted by one, two or three of the same or different substituents selected from halogen, hydroxy, amino, nitro, cyano, azido, alkyl, alkoxy, alkanesulfenyl, alkanesulfinyl, alkanesulfonyl, alkanoyl, alkoxycarbonyl, alkanoyloxy, carbamoyl, ureido, carba- moyloxy, alkanoylamino, aminosulfamoyl, sulfamoyl, guani- dino, trifluormethyl, trifluormethanesulfenyl, trifluor- methanesulfinyl, trifluormethanesulfonoyl and formyl, which may be substituted by one, two or three lower alkyl groups being the same or different.
R 2 represents a hydrogen atom or a optionally protected hydroxyl group,
or a salt thereof,
process for the production thereof and antibacterial pharmaceutical preparations comprising them.
摘要翻译：其中R为氢或羧基酯化基团的式1的青霉烯衍生物，R 1为未取代的苯基，萘基，噻吩基，吡啶基，喹啉基或异喹啉基或被1,2或3个相同或不同的选自卤素，羟基，氨基，硝基，氰基，叠氮基，烷基，烷氧基，烷烃亚磺酰基，烷烃亚磺酰基，烷磺酰基，烷酰基，烷氧基羰基，烷酰氧基，氨基甲酰基，脲基，甲磺酰基，三氟甲磺酰基和甲酰基，它们可以被一个，两个或三个低级烷基相同或不同。 R2代表氢原子或任选保护的羟基，或其盐，其制备方法和包含它们的抗菌药物制剂。

46. 发明公开

EP0051813A3 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：EP0051813A3
公开(公告)日：1982-08-18
申请号：EP81109176
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 , C07F07/18 , C07D285/00 , C07D205/00
CPC分类号： C07D513/04 , C07D205/09 , C07D499/88 , C07F7/186
摘要： The invention relates to compounds of the formula
in which
R is an esterifying group R 2 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower acyloxyalkyl or tri-lower alkylsilyloxyalkyl, a process for their manufacture and intermediate compounds for their synthesis.
摘要翻译：本发明涉及其中R为酯化基团R 2为氢，低级烷基，低级羟烷基，低级烷氧基烷基，低级酰氧基烷基或三低级烷基甲硅烷氧基烷基的下式化合物，它们的制备方法和用于它们的合成的中间体化合物。

47. 发明公开

EP0018305A1 Oxapenem derivatives, their preparation, their use, pharmaceutical compositions containing them, diverse initial compounds and their preparation 失效
标题翻译： 1-氧青霉衍生物，其制备方法，它们的用途，含有它们的，各种起始化合物和它们的制备药物组合物。
公开(公告)号：EP0018305A1
公开(公告)日：1980-10-29
申请号：EP80710008.6
申请日：1980-03-19
申请人： HOECHST UK LIMITED
发明人： Ross, Barry Clive, Dr. , Johnson, Graham, Dr. , Yeomans, Michael Alan, Dr. , Cooke, Michael David
IPC分类号： C07D498/04 , C07D205/08 , C07D499/00 , A61K31/42
CPC分类号： C07D503/00 , C07D499/00
摘要： Disclosed is a process for the production of a compound of the general formula I
or a salt thereof, which comprises reacting a compound of the general formula II
with a tervalent organophosphorus compound and, if desired, simultaneously or subsequently with a thiophilic agent as hereinbefore defined.
Compounds (I) and (II), pharmaceutical compositions containing compounds (I) and the use of these compounds as β-lactamase inhibitors and or as antibacterial agents are described.
Also desribed are initial compounds (penicillins, acetidi- nones) and processes for their preparation.
摘要翻译：公开了一种用于生产通式I或其或其盐，该方法包括使通式II 的化合物的化合物的方法与三价有机磷化合物，并且如果需要清除，同时或随后与如之前所定义的亲硫剂。化合物（I）和（II），将含有化合物（I）和使用合成的化合物作为β-内酰胺酶抑制剂和药物组合物或作为抗菌剂进行了描述。这样描述的是初始化合物（青霉素类，acetidinones）和它们的制备方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式