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1. 发明授权

EP0000633B1 Process for the preparation of alpha-substituted-thien-3-ylacetic acid and derivatives thereof 失效
标题翻译：制备ALPHA替代的3-乙酸及其衍生物的方法
公开(公告)号：EP0000633B1
公开(公告)日：1981-11-04
申请号：EP78300140.7
申请日：1978-07-12
申请人： BEECHAM GROUP PLC
发明人： Guest, Angela Wendy , Taylor, Andrew William , Ramage, Robert
IPC分类号： C07D333/24
CPC分类号： C07C255/00 , C07C45/00 , C07C57/52 , C07D333/24 , C07C49/227

2. 发明公开

EP0090656A1 Penicillins, a process for the preparation and compositions containing them 失效
标题翻译：青霉素类，用于制备的方法和含有它们的组合物。
公开(公告)号：EP0090656A1
公开(公告)日：1983-10-05
申请号：EP83301786.6
申请日：1983-03-30
申请人： BEECHAM GROUP PLC
发明人： Taylor, Andrew William , Cook, Richard Thomas
IPC分类号： C07D499/68 , C07D501/32 , A61K31/43 , A61K31/545
CPC分类号： C07D499/00 , C07D231/20 , C07D231/26
摘要： A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof:
wherein R 1 is phenyl, substituted phenyl or a 5- or 6 mem hered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substi tuted with rvdroxy. amino. halogen or C 1-6 alkoxy: X represents
wherein R Y is methyl or acetyl; R 2 and R 3 may be the same or different and each is hydrogen, an aryl group, a heterocyclyl group or a C 1-6 alkyl group optionally substituted by ar aryl group or a heterocycly group; and R 4 is hydrogen a C 1- 6 alkyl carbonyl group. an aryl group, a heterocyclyl group, a C 1- 6 alkyl group optionally substituted by an aryl group or a hetere- cyclyl group; R 5 represents, hydrogen, methoxy or -NHCHO; and Y is:
wherein Y 1 is oxygen, sulphur or -CH 2 - and Z represents hydrogen, halogen or an organic group such as C 1-4 alkoxy, -CH 2 O or -CH=CH-Q wherein Q represents hydrogen, halogen, hydroxy, mercepto, cyano, carboxy, carbamoyloxy carboxylic ester, C 1-4 alkyloxy, acyloxy, aryl, a heterocyclyl group bonded via carbon, a heterocyclylthio group or a a nitrogen containing heterocyclic group bonded via nitrogen.

3. 发明公开

EP0067610A1 Penicillins, a process for their preparation and compositions containing them 失效
标题翻译：青霉素类，它们的制备方法和含有它们的组合物。
公开(公告)号：EP0067610A1
公开(公告)日：1982-12-22
申请号：EP82302819.6
申请日：1982-06-01
申请人： BEECHAM GROUP PLC
发明人： Taylor, Andrew William , Adams, Richard George
IPC分类号： C07D499/68 , C07D499/70 , A61K31/43
CPC分类号： C07D239/47 , C07D499/00
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof:
wherein R 1 is phenyl, 4-hydroxy phenyl, 3,4-dihydroxyphenyl, 3,4-diacetoxyphenyl or a 5- or 6- membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C 1-6 alkoxy; and R 2 is a sub-group of formula (A):
wherein R 3 is an optionally substituted C 1-10 alkyl or C 3-7 cycloalkyl group; or R 2 is a sub-group of formula (B):
wherein R 4 is an aryl group, an optionally substituted C 1-10 alkyl group or a C 1-6 alkyloxy group optionally substituted by an aryl group.

4. 发明公开

EP0081320A3 Preparation of acetic acid derivatives 失效
标题翻译：乙酸衍生物的制备
公开(公告)号：EP0081320A3
公开(公告)日：1984-07-18
申请号：EP82306275
申请日：1982-11-25
申请人： BEECHAM GROUP PLC
发明人： Taylor, Andrew William , Guest, Angela Wendy , Lashford, Andrew Gerard
IPC分类号： C07C143/68 , C07D333/24 , C07C139/00
CPC分类号： C07D333/24 , C07C309/00 , C07D333/18
摘要： A process for the preparation of a compound of formula (I) or a salt thereof:
wherein R' is an optionally substituted aryl group and R 2 is hydrogen, a salting ion or a sulphonyl ester forming group; characterised in that a mono-deprotonated methylene compound of the formula (II):
wherein R 1 and R 2 are as defined with respect to formula (I) and wherein any reactive groups may be protected, is reacted with carbon dioxide.
摘要翻译：制备式（I）化合物或其盐的方法：其中R 1是任选取代的芳基，R 2是氢，盐析离子或磺酰酯形成基团; 其特征在于式（II）的单脱质子亚甲基化合物：其中R 1和R 2如式（I）所定义，其中任何反应性基团可以被保护，反应与二氧化碳。

5. 发明公开

EP0081320A2 Preparation of acetic acid derivatives 失效
标题翻译： Herstellung vonEssigsäure-Derivaten。
公开(公告)号：EP0081320A2
公开(公告)日：1983-06-15
申请号：EP82306275.7
申请日：1982-11-25
申请人： BEECHAM GROUP PLC
发明人： Taylor, Andrew William , Guest, Angela Wendy , Lashford, Andrew Gerard
IPC分类号： C07C143/68 , C07D333/24 , C07C139/00
CPC分类号： C07D333/24 , C07C309/00 , C07D333/18
摘要： A process for the preparation of a compound of formula (I) or a salt thereof:
wherein R' is an optionally substituted aryl group and R 2 is hydrogen, a salting ion or a sulphonyl ester forming group; characterised in that a mono-deprotonated methylene compound of the formula (II):
wherein R 1 and R 2 are as defined with respect to formula (I) and wherein any reactive groups may be protected, is reacted with carbon dioxide.
摘要翻译：制备式（I）化合物或其盐的方法：其中R 1是任选取代的芳基，R 2是氢，盐析离子或磺酰酯形成基团; 其特征在于式（II）的单脱质子亚甲基化合物：其中R 1和R 2如式（I）所定义，其中任何反应性基团可以被保护，反应与二氧化碳。

6. 发明公开

EP0023726A1 2,5-disubstituted-3 substituted methyl-penta-2,4-dienoic acid and derivatives and process for their preparation 失效
标题翻译： 2,5-Disubstituierte-3-substitutionierte Methylpenta-2,4-diensäureund Derivate und Verfahren zu ihrer Herstellung。
公开(公告)号：EP0023726A1
公开(公告)日：1981-02-11
申请号：EP80105285.3
申请日：1978-07-12
申请人： BEECHAM GROUP PLC
发明人： Ramage, Robert , Guest, Angela Wendy , Taylor, Andrew William
IPC分类号： C07C69/65 , C07C67/343 , C07C57/13 , C07C51/353 , C07C121/413 , C07C120/00
CPC分类号： C07C255/00 , C07C45/00 , C07C57/52 , C07D333/24 , C07C49/227
摘要： A class of intermediates useful in the preparation of 3-substituted thiophenes and a process for preparing said intermediates. The thiophenes are useful for the preparation of penicillins and cephalosporins
A compound of formula (II):
where R 1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R 2 represents a group suitable for use as an a-substituent in the side-chain of a penicillin or cephalosporin; X represents halogen or optionally functionalised hydroxyl and Y represents halogen, hydroxyl, or alkoxy.
摘要翻译：一类可用于制备3-取代噻吩的中间体和一种制备所述中间体的方法。噻吩可用于制备青霉素和头孢菌素式（II）化合物：其中R 1表示羧酸基团或其酯或酰胺或腈基的式CHEM： R 2表示适合用作青霉素或头孢菌素的侧链中的α-取代基的基团; X表示卤素或任选官能化的羟基，Y表示卤素，羟基或烷氧基。

7. 发明公开

EP0067612A1 Penicillin derivatives 失效
标题翻译： Penicillinderivate。
公开(公告)号：EP0067612A1
公开(公告)日：1982-12-22
申请号：EP82302824.6
申请日：1982-06-02
申请人： BEECHAM GROUP PLC
发明人： Driver, Michael John , Taylor, Andrew William
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D239/48 , C07D499/00
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof:
wherein R is phenyl, 4-hydroxyphenyl, 2- or 3-thienyl, cyclohexyl, cyclohexan-1-yl, cyclohexa-1,4-dien-1-yl, or 3,4- disubstituted phenyl wherein the substituents may be the same or different and are selected from chlorine, hydroxy and methoxy; and R 1 represents hydrogen, an alkyl, alkenyl, cycloalkyl or cycloalkenyl group, an optionally substituted phenyl, a cyclopropyl alkyl group, a hydroxy group optionally substituted by alkyl, alkenyl, cycloalkyl, phenyl or benzyl, an optionally substituted mercapto group, an alkylsulphenyl group, a free or substituted amino group, an optionally substituted piperazino or phenylalkylamino group, an acylamino group or an alkyl, aralkyl or arylsulphonyl amino group.
摘要翻译：式（I）化合物或其药学上可接受的盐或体内可水解的酯：其中R是苯基，4-羟基苯基，2-或3-噻吩基，环己基，环己烷-1-基，环己烷-1， 4-二烯-1-基或3,4-二取代苯基，其中取代基可以相同或不同，并且选自氯，羟基和甲氧基; R 1表示氢，烷基，烯基，环烷基或环烯基，任选取代的苯基，环丙基烷基，任选被烷基，烯基，环烷基，苯基或苄基取代的羟基，任选取代的巯基，烷基亚磺酰基，游离或取代的氨基，任选取代的哌嗪基或苯基烷基氨基，酰氨基或烷基，芳烷基或芳基磺酰基氨基。

8. 发明授权

EP0023726B1 2,5-disubstituted-3 substituted methyl-penta-2,4-dienoic acid and derivatives and process for their preparation 失效
标题翻译： 2,5-取代的-3取代的甲基 - 戊-2-醇二酸及其衍生物及其制备方法
公开(公告)号：EP0023726B1
公开(公告)日：1982-05-19
申请号：EP80105285.3
申请日：1978-07-12
申请人： BEECHAM GROUP PLC
发明人： Ramage, Robert , Guest, Angela Wendy , Taylor, Andrew William
IPC分类号： C07C69/65 , C07C67/343 , C07C57/13 , C07C51/353 , C07C121/413 , C07C120/00
CPC分类号： C07C255/00 , C07C45/00 , C07C57/52 , C07D333/24 , C07C49/227

9. 发明公开

EP0000633A3 2,5 -disubstituted-3-substituted methyl-penta-2,4-dienoic acid and derivatives, process for their preparation and their use in the preparation of alpha-substituted-thien-3-yl acetic acid and derivatives 失效
标题翻译： 2,5 - 取代的3-取代的甲基 - 2,4-二戊酸和衍生物，其制备方法及其在制备α-取代的三乙酸乙酸和衍生物中的用途
公开(公告)号：EP0000633A3
公开(公告)日：1979-06-13
申请号：EP78300140
申请日：1978-07-12
申请人： BEECHAM GROUP PLC
发明人： Guest, Angela Wendy , Taylor, Andrew William , Ramage, Robert
IPC分类号： C07D333/24 , C07C57/02 , C07C69/52 , C07C49/22
CPC分类号： C07C255/00 , C07C45/00 , C07C57/52 , C07D333/24 , C07C49/227
摘要： A process for the preparation of 3-substituted thiophenes which involves cyclisation of a novel intermediate, avoids the use of previously employed expensive starting materials. The thiophenes are useful for the preparation of penicillins and cephalosporins. The process is for the preparation of a thiophene of formula (I):
where R 1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R 2 represents a group suitable for use as an α-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating a compound of formula (II):
wherein X represents halogen or optionally functionalised hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur under basic conditions.
摘要翻译：一类可用于制备3-取代噻吩的中间体和一种制备所述中间体的方法。噻吩可用于制备青霉素和头孢菌素式（II）化合物：其中R 1表示羧酸基团或其酯或酰胺或腈基的式CHEM： R 2表示适合用作青霉素或头孢菌素的侧链中的α-取代基的基团; X表示卤素或任选官能化的羟基，Y表示卤素，羟基或烷氧基。

10. 发明公开

EP0000633A2 Process for the preparation of alpha-substituted-thien-3-ylacetic acid and derivatives thereof 失效
标题翻译： Verfahren zur Herstellung von alpha-substituteierter-Thien-3-yl-essigsäureund deren Derivaten。
公开(公告)号：EP0000633A2
公开(公告)日：1979-02-07
申请号：EP78300140.7
申请日：1978-07-12
申请人： BEECHAM GROUP PLC
发明人： Guest, Angela Wendy , Taylor, Andrew William , Ramage, Robert
IPC分类号： C07D333/24
CPC分类号： C07C255/00 , C07C45/00 , C07C57/52 , C07D333/24 , C07C49/227
摘要： A process for the preparation of 3-substituted thiophenes which involves cyclisation of a novel intermediate, avoids the use of previously employed expensive starting materials. The thiophenes are useful for the preparation of penicillins and cephalosporins.
The process is for the preparation of a thiophene of formula (I):
where R 1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R 2 represents a group suitable for use as an α-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating a compound of formula (II):
wherein X represents halogen or optionally functionalised hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur under basic conditions.
摘要翻译：一类可用于制备3-取代噻吩的中间体和一种制备所述中间体的方法。噻吩可用于制备青霉素和头孢菌素式（II）化合物：其中R 1表示羧酸基团或其酯或酰胺或腈基的式CHEM： R 2表示适合用作青霉素或头孢菌素的侧链中的α-取代基的基团; X表示卤素或任选官能化的羟基，Y表示卤素，羟基或烷氧基。

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