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1. 发明授权

EP0128525B1 Auslaufsperre für Behälter, insbesondere für Tuben, und Anwendungen 失效
标题翻译：集装箱封闭件，特别适用于管件及其应用
公开(公告)号：EP0128525B1
公开(公告)日：1990-01-17
申请号：EP84106465.2
申请日：1984-06-06
申请人： Lingner + Fischer GmbH
发明人： Flier, Gustav, Dipl.-Phys.
IPC分类号： B65D35/46
CPC分类号： B65D35/46 , Y10T137/7781 , Y10T137/784 , Y10T137/7843 , Y10T137/788

2. 发明公开

EP0307177A3 Erythromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：EP0307177A3
公开(公告)日：1989-10-25
申请号：EP88308257.0
申请日：1988-09-07
申请人： BEECHAM GROUP PLC
发明人： Brain, Edward George
IPC分类号： C07H17/08 , A61K31/00
CPC分类号： C07H17/08
摘要： 11,12-Carbonate derivatives of certain erythromycin 6-ethers are novel, antibacterially active compounds which can be prepared by treatment of an erythromycin 6-ether with a reactive carbonyl compound.
摘要翻译：某些红霉素6-醚的11,12-碳酸酯衍生物是新型的抗菌活性化合物，其可以通过用反应性羰基化合物处理红霉素6-醚来制备。

3. 发明公开

EP0321185A2 Erythromycin derivatives 失效
标题翻译：红霉素衍。
公开(公告)号：EP0321185A2
公开(公告)日：1989-06-21
申请号：EP88311785.5
申请日：1988-12-13
申请人： BEECHAM GROUP PLC
发明人： Davies, John Sidney
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： 9- N ,11- O -methylene derivatives of erythromycin-9-imine (wherein the methylene group is optionally substituted) of the general formula IA or IB:
or a pharmaceutically acceptable ester or acid addition salt thereof,
wherein
R¹ denotes hydrogen, an unsubstituted or substituted hydrocarbon group, a heterocyclyl group, or an acyl group;
R³ denotes hydrogen or hydroxy;
R⁶ denotes hydrogen or methyl;
one of R⁷ and R⁸ denotes hydrogen, hydroxy, alkoxy,alkanoyloxy, amino, substituted amino, or a group of the formula R⁹-SO₂-O-, and the other of R⁷ and R⁸ denotes hydrogen, or
R⁷ and R⁸ together denote an oxo group, an oxime group, or a substituted oxime group; and
R⁹ denotes an organic group,
possess improved acid stability, compared with erythromycin A, whilst retaining good antibacterial activity.
摘要翻译：通式IA或IB的红霉素-9-亚胺（其中亚甲基任选被取代）的9-N，11-O-亚甲基衍生物或其药学上可接受的酯或酸加成盐，其中R 1， 1>表示氢，未取代或取代的烃基，杂环基或酰基; R 3表示氢或羟基; R 6表示氢或甲基; R 7和R 8中的一个表示氢，羟基，烷氧基，烷酰氧基，氨基，取代的氨基或式R 9 -SO 2 -O-的基团，R 7和 R 8表示氢，或R 7和R 8一起表示氧代基，肟基或取代的肟基; R 9表示有机基团，与红霉素A相比具有改善的酸稳定性，同时保持良好的抗菌活性。

4. 发明公开

EP0234688A1 Thiophene-3-carboxaldehyde derivatives, their preparation and their use in preparing 3-thienyl acetonitrile 失效
标题翻译：噻吩-3-甲醛衍生物，它们的制备方法和它们用于3-噻吩基 - 乙腈的制造中的用途。
公开(公告)号：EP0234688A1
公开(公告)日：1987-09-02
申请号：EP87300188.7
申请日：1987-01-09
申请人： BEECHAM GROUP PLC , Wendstone Chemicals P.L.C.
发明人： Ramage, Robert , Johnstone, Alexander
IPC分类号： C07D333/22 , C07D333/24 , C07D333/32
CPC分类号： C07D333/22 , C07D333/24 , C07D333/32
摘要： The novel compound 2,5-dihydrothiophene-3-carboxaldehyde (which exists in equilibrium with the further novel compound 4-hydroxy-tetrahydrothiophene-3-carboxaldehyde) may be prepared by the reaction of mer- captoacetaldehyde with acrolein. It may be used for the manufacture of 3-thienylacetonitrile, by reaction with a cyanide followed by elimination of an appropriate hydroxy compound.
摘要翻译：新化合物2,5- dihydrothiophenes -3-甲醛（在与另外的新化合物4-羟基-3-甲醛tetrahydrothiophenes-平衡哪个存在）可通过mercaptoacetaldehyde与丙烯醛的反应来制备。它可用于3-thienylacetonitrile的制造中，通过与随后消除适当的羟基化合物的氰化物反应。

5. 发明公开

EP0041768A2 Beta-lactam compounds, their preparation and use 失效
标题翻译： Beta-Lactam-Verbindungen，ihre Herstellung und Verwendung。
公开(公告)号：EP0041768A2
公开(公告)日：1981-12-16
申请号：EP81301683.9
申请日：1981-04-15
申请人： BEECHAM GROUP PLC
发明人： Osborne, Neal Frederick
IPC分类号： C07D499/00 , C07D205/08 , A61K31/43
CPC分类号： C07F9/5683 , C07C335/32 , C07D205/09 , C07D499/88 , C07F7/186
摘要： Compounds of formula (II)
having antibacterial and beta-lactamase inhibitory properties and in which R 1 and R 2 represent hydrogen or an optionally substituted hydrocarbon or heterocyclic group, and R 3 represents hydrogen or an organic group.
Their preparation, a pharmaceutical composition and an intermediate of formula (VII)
are also claimed.
摘要翻译：具有抗细菌和β-内酰胺酶抑制性质的式（II）... 的化合物，其中R 1和R 2表示氢或任选取代的烃或杂环基，R 3表示氢或一个有机组织。他们的制剂，药物组合物和式（VII）... ...的中间体也被加压。

6. 发明授权

EP0026073B2 Detergent-oil bath additives and process 失效
标题翻译：除臭油浴添加剂和工艺
公开(公告)号：EP0026073B2
公开(公告)日：1989-11-08
申请号：EP80303191.3
申请日：1980-09-11
申请人： Lingner + Fischer GmbH
发明人： Hermann, Claus , Krings, Helmut
IPC分类号： A61K7/50 , C11D1/29
CPC分类号： A61K8/463 , A61K2800/596 , A61Q19/10 , C11D1/29

7. 发明公开

EP0321185A3 Erythromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：EP0321185A3
公开(公告)日：1989-11-02
申请号：EP88311785.5
申请日：1988-12-13
申请人： BEECHAM GROUP PLC
发明人： Davies, John Sidney
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： 9- N ,11- O -methylene derivatives of erythromycin-9-imine (wherein the methylene group is optionally substituted) of the general formula IA or IB:
or a pharmaceutically acceptable ester or acid addition salt thereof,
wherein
R¹ denotes hydrogen, an unsubstituted or substituted hydrocarbon group, a heterocyclyl group, or an acyl group;
R³ denotes hydrogen or hydroxy;
R⁶ denotes hydrogen or methyl;
one of R⁷ and R⁸ denotes hydrogen, hydroxy, alkoxy,alkanoyloxy, amino, substituted amino, or a group of the formula R⁹-SO₂-O-, and the other of R⁷ and R⁸ denotes hydrogen, or
R⁷ and R⁸ together denote an oxo group, an oxime group, or a substituted oxime group; and
R⁹ denotes an organic group,
possess improved acid stability, compared with erythromycin A, whilst retaining good antibacterial activity.
摘要翻译：通式IA或IB的红霉素-9-亚胺（其中亚甲基任选被取代）的9-N，11-O-亚甲基衍生物或其药学上可接受的酯或酸加成盐，其中R 1， 1>表示氢，未取代或取代的烃基，杂环基或酰基; R 3表示氢或羟基; R 6表示氢或甲基; R 7和R 8中的一个表示氢，羟基，烷氧基，烷酰氧基，氨基，取代的氨基或式R 9 -SO 2 -O-的基团，R 7和 R 8表示氢，或R 7和R 8一起表示氧代基，肟基或取代的肟基; R 9表示有机基团，与红霉素A相比具有改善的酸稳定性，同时保持良好的抗菌活性。

8. 发明授权

EP0087953B1 Antibacterial 1-normon-2-yl-heterocyclic compounds 失效
标题翻译：抗菌1-正二-2-杂环化合物
公开(公告)号：EP0087953B1
公开(公告)日：1988-04-27
申请号：EP83301022.6
申请日：1983-02-25
申请人： BEECHAM GROUP PLC
发明人： Rogers, Norman Harold , O'Hanlon, Peter John , Walker, Graham , Crimmin, Michael John
IPC分类号： C07D413/14 , C07D417/14 , A61K31/42 , A61K31/425
CPC分类号： C07D277/22 , C07C205/45 , C07C255/00 , C07C309/00 , C07C323/00 , C07D261/08 , C07D261/18 , C07D263/32 , C07D333/22 , C07D333/28 , C07D407/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/653

9. 发明公开

EP0123378A2 1-Normonyl derivatives, processes and use 失效
标题翻译： 1-Normonyl衍生物，方法和用途。
公开(公告)号：EP0123378A2
公开(公告)日：1984-10-31
申请号：EP84300991.1
申请日：1984-02-16
申请人： BEECHAM GROUP PLC
发明人： Rogers, Norman Harold , Walker, Graham , Crimmin, Michael John , O'Hanlon, Peter John
IPC分类号： C07D413/14 , C07D405/14 , C07D407/06 , A61K31/35 , A61K31/41
CPC分类号： C07D405/14 , C07D407/06 , C07D413/14
摘要： Compounds of formula (I):
wherein
is a 5-membered heterocyclic group having a 6-π electron system, the five ring atoms being either

a) one carbon atom and four atoms selected from carbon and nitrogen,
b) two carbon atoms, two nitrogen atoms and one atom selected from oxygen and sulphur, or
c) four carbon atoms and one atom selected from oxygen and sulphur
and R' is a substituent on a carbon or nitrogen of
selected from C 1-20 alkyl, C 2 - 8 alkenyl aryl, aralkyl and heterocyclyl, each of which may optionally be substituted; hydrogen and C 3 - 7 cycloalkyl,
and, where appropriate, R 2 is a substituent on a carbon or nitrogen of
and when present is the same or different to R' and is selected from C 1-20 alkyl, C 2 - 8 alkenyl, aryl, aralkyl and heterocyclyl each of which may optionally be substituted; hydrogen and C 3 - 7 cycloalkyl, have antibacterial and antimycoplasmal activity.

10. 发明公开

EP0112049A1 Process for the preparation of beta-lactam compounds 失效
标题翻译： Verfahren zur Herstellung von beta-Lactamverbindungen。
公开(公告)号：EP0112049A1
公开(公告)日：1984-06-27
申请号：EP83306964.4
申请日：1983-11-15
申请人： BEECHAM GROUP PLC
发明人： Geerlandt, Hervé , Grand'Henry, Claudine
IPC分类号： C07D499/04 , C07D499/72 , C07D501/04 , C07D498/04
CPC分类号： C07D499/00 , C07D505/00
摘要： The present invention provides a process for the substitution of an acylamino β-lactam compound at the carbon atom carrying the acylamino group, which process comprises reacting the β-lactam compound with an halogenating agent and a nucleophilic reagent; characterised in that the acylamino group has an acidic group on the carbon atom adjacent the carbonyl group.
In particular the process of this invention comprises reacting a β-lactam of partial structure (I):
where X represents an acidic group; with an halogenating agent and a nucleophilic reagent.
摘要翻译：本发明提供了在携带酰基氨基的碳原子上取代酰基氨基β-内酰胺化合物的方法，该方法包括使β-内酰胺化合物与卤化剂和亲核试剂反应; 其特征在于酰氨基在与羰基相邻的碳原子上具有酸性基团。特别地，本发明的方法包括使部分结构（I）的β-内酰胺：其中X表示酸性基团的与卤化剂和亲核试剂。

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