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1. 发明授权

EP0055062B1 Compounds containing beta-lactams 有权
标题翻译：包含BETA-LACTAMS的化合物
公开(公告)号：EP0055062B1
公开(公告)日：1984-05-23
申请号：EP81305871.6
申请日：1981-12-14
申请人： BEECHAM GROUP PLC
发明人： Harbridge, John Barry , Stirling, Irene
IPC分类号： C07D498/04 , A61K31/42 , A61K31/43 , A01N43/74
CPC分类号： A61K31/43 , A01N43/74 , C07D503/00 , Y02A50/473
摘要： A compound of formula (I) or a salt or ester thereof: (I) Pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt or pharmaceutically acceptable ester thereof are also disclosed.

2. 发明授权

EP0232966B1 Process for the preparation of penem compounds and intermediates for this preparation 有权转让
标题翻译：一种用于生产青霉烯衍生物和中间体的对该制备方法
公开(公告)号：EP0232966B1
公开(公告)日：1997-10-08
申请号：EP87300193.7
申请日：1987-01-09
申请人： BEECHAM GROUP PLC
发明人： Coulton, Steven , Harbridge, John Barry , Osborne, Neal Frederick , Walker, Graham
IPC分类号： C07D499/00
CPC分类号： C07D417/12 , C07D205/09 , C07D499/88 , C07F9/5683

3. 发明公开

EP0023093A1 Penicillanic acid derivatives, their preparation and their pharmaceutical compositions with a penicillin or cephalosporin 有权转让
标题翻译： Penizillansäure衍生物，其制备方法及其用青霉素或头孢菌素的药物组合物。
公开(公告)号：EP0023093A1
公开(公告)日：1981-01-28
申请号：EP80302152.6
申请日：1980-06-26
申请人： BEECHAM GROUP PLC
发明人： Harbridge, John Barry , Denerley, Paul Millington
IPC分类号： A61K31/43 , A61K31/545 , C07D499/00
CPC分类号： A61K31/43 , A61K31/545 , C07D499/00
摘要： The present invention provides the compounds of the formula (I):
and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof, wherein n is 0 or 2, R' is a C 1-6 alkyl group optionally substituted with one, two or three fluorine, chlorine or bromine atoms, or is a di-C 1-6 alkylamino group or is a group of the formula (I):
wherein X is a bond, or a -CH =CH group, or a methylene or ethylene group; R 2 is a hydrogen, fluorine, bromine or chlorine atom, or is an amino, protected amino, hydroxy, protected hydroxy, C,-, alkyl, nitro, di-C 1-6 alkylamino, acetamido, C 1-6 alkoxy or trifluromethyl group; R is a hydrogen or chlorine atom or a C,-, alkyl or trifluoromethyl group; and R 4 is a hydrogen or chlorine atom, or a C 1-6 alkyl or
C 1-6 alkoxy group; or R 5 and R' on any two adjacent carbon atoms may together represent a buta-1, 3-dienylene moiety which is optionally substituted by a C,-, alkyl or C,-, alkoxy group. These compounds are β-lactamase inhibitors. Their use is described as is a process for their preparation.
摘要翻译：本发明提供了式（I）的化合物：和药学上可接受的盐和体内可水解的酯，worin n是0或2，R <1>被C 1-6烷基任选被一个substituiertem，两个或三个氟，氯或溴原子，或者是二C 1-6烷基氨基或为基团的式（i）的： worin X是键，或CH = CH基团，或亚甲基或亚乙基; [R <2>为氢，氟，溴或氯原子，或为氨基，保护的氨基，羟基，保护的羟基，C 1-6烷基，硝基，二C 1-6烷基氨基，乙酰氨基，C 1-6烷氧基或三氟甲基组; R是氢或氯原子或C 1-6烷基或三氟甲基; 且R <4>是氢或氯原子，或C 1-6烷基或C 1-6烷氧基; 或R <2>和R上的任意两个相邻的碳原子可以一起代表丁1，3-二烯基部分的所有其任选地被一个C 1-3烷基或C 1-3烷氧基substituiertem。这些化合物是β-内酰胺酶抑制剂。它们的使用被描述为是它们的制备方法。

4. 发明公开

EP0010369A1 Clavulanic acid derivatives, processes for their preparation and pharmaceutical compositions containing them 有权转让
标题翻译：克拉维酸的衍生物，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0010369A1
公开(公告)日：1980-04-30
申请号：EP79302025.6
申请日：1979-09-28
申请人： BEECHAM GROUP PLC
发明人： Harbridge, John Barry , Stirling, Irene , Clarke, Brian Peter
IPC分类号： C07D498/04 , A61K31/42 , A61K31/43 , A61K31/545
CPC分类号： C07D503/00
摘要： Compounds of formula (II):
wherein R, is a hydrogen, fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms, an alkoxyl group of 1-3 carbon atoms or an acyloxy group of 1-3 carbon atoms, R 4 is a hydrogen, fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms or an alkoxy group of 1-3 carbon atoms, and R 7 is a nitro, cyano, amino or aminomethyl group, are antibacterial agents and beta-lactamase inhibitors. Their use and process for their preparation are described.
摘要翻译：式（II）化合物：... ... worin R 3为氢，氟或氯原子或烷基的1-3个碳原子的基团的烷氧基在1-酰氧基的1-3个碳原子的基团或 3个碳原子，R4是氢氟或氯原子或烷基以1-3个碳原子的烷氧基为1〜3个碳原子的或基团，并且R 7是硝基，氰基，氨基或氨甲基，有抗菌剂和 β-内酰胺酶抑制剂。它们的用途和它们的制备方法进行了描述。

5. 发明公开

EP0104010A1 Intermediates for clavulanic-acid derivatives 有权
标题翻译：中间体克拉维酸衍生物。
公开(公告)号：EP0104010A1
公开(公告)日：1984-03-28
申请号：EP83304956.2
申请日：1983-08-26
申请人： BEECHAM GROUP PLC
发明人： Harbridge, John Barry
IPC分类号： C07D498/04
CPC分类号： C07D503/00 , C07F7/0812
摘要： A compound of formula I
or a salt or ester thereof.
Processes for the preparation of these compounds and the use of these compounds in the preparation of further bicyclic compounds are also disclosed.

6. 发明授权

EP0002320B1 Process for the preparation of clavulanic acid derivatives and compounds used as intermediates therein 失效
标题翻译：制备酚醛酸衍生物及其作为中间体的化合物的方法
公开(公告)号：EP0002320B1
公开(公告)日：1981-04-29
申请号：EP78300582.0
申请日：1978-11-02
申请人： BEECHAM GROUP PLC
发明人： Stirling, Irene , Harbridge, John Barry
IPC分类号： C07D498/04
CPC分类号： C07D503/00

7. 发明公开

EP0024372A1 Derivatives of clavulanic acid, their preparation and pharmaceutical compositions containing them 失效
标题翻译：克拉维酸衍生物及其制备和含有它们的药物组合物
公开(公告)号：EP0024372A1
公开(公告)日：1981-03-04
申请号：EP80302658.2
申请日：1980-08-04
申请人： BEECHAM GROUP PLC
发明人： Denerley, Paul Millington , Eglington, Alfred John , Harbridge, John Barry
IPC分类号： C07D498/04 , A61K31/42
CPC分类号： C07D503/00
摘要： The compounds of the formula (II):
and salts and esters thereof wherein the hydroxyl group occupies position 2 or 4 R 1 and R 2 may be the same or different and represent hydrogen, halogen, hydroxy, lower alkyl, cyclopentyl, cyclohexyl, lower alkoxy or R, and R 2 when an adjacent carbon atoms may together represent a 1,4-buta-1,3-dienylene group or a polymethylene group containing from 3 to 5 carbon atoms; have been found to be β-lactam antibiotics and synergists with penicillins and cephalosporins. Their preparation and use is described. The synthesis of intermediates useful in their preparation is also described.
摘要翻译：其中羟基占据2或4位的式（Ⅱ）化合物及其盐和酯，R1和R2可以相同或不同，代表氢，卤素，羟基，低级烷基，环戊基，环己基，低级烷氧基或当相邻碳原子可以一起代表1,4-丁-1,3-亚二烯基或含有3至5个碳原子的多亚甲基时，已被发现是β-内酰胺抗生素和青霉素和头孢菌素的增效剂。描述了他们的准备和使用。还描述了在其制备中有用的中间体的合成。

8. 发明公开

EP0005014A1 Clavulanic acid derivatives, preparation and compositions 失效
标题翻译： Clavulansäure-Derivate，Herstellung und Zusammensetzungen。
公开(公告)号：EP0005014A1
公开(公告)日：1979-10-31
申请号：EP79300515.8
申请日：1979-03-29
申请人： BEECHAM GROUP PLC
发明人： Stirling, Irene , Clarke, Brian Peter , Harbridge, John Barry
IPC分类号： C07D498/04 , A61K31/42
CPC分类号： C07D503/00 , C07D307/52
摘要： This invention provides the β-lactamase inhibitory compounds of the formula (II):
ana esters and acia addition salts of esters thereof wherein R 1 is an optionally substituted aromatic monocyclic or bicyclic heterocyclic group bonded via a carbon atom and R; is a group CH 2 R 1 , a hydrogen atom, a C 1-6 alkyl or hydroxyai- kyl group, an optionally substituted benzyl group, or a group of the sub-formula (a):
where R a is a C 1-3 alkyl group, and R b and R c are mdepen- dently hydrogen, C 1-3 alkyl or phenyl.
The invention also relates to processes for their preparation and pharmaceutical compositions containing them.
摘要翻译：本发明提供了式（II）的β-内酰胺酶抑制性化合物：其中R 1是通过碳原子键合的任选被取代的芳族单环或双环杂环基团和其酯的酯和酸加成盐，R 2 是基团CH 2 R 1，氢原子，C 1-6烷基或羟烷基，任选取代的苄基或下式（a）的基团：其中R a是C 1-3烷基的基团，和 Rb和Rc独立地是氢，C 1-3烷基或苯基。本发明还涉及其制备方法和含有它们的药物组合物。

9. 发明公开

EP0232966A1 Process for the preparation of penem compounds and intermediates for this preparation 有权转让
标题翻译： Penem-Verbindungen und Azetidinon-Zwischenprodukte zu ihrer Herstellung。
公开(公告)号：EP0232966A1
公开(公告)日：1987-08-19
申请号：EP87300193.7
申请日：1987-01-09
申请人： BEECHAM GROUP PLC
发明人： Coulton, Steven , Harbridge, John Barry , Osborne, Neal Frederick , Walker, Graham
IPC分类号： C07D499/00
CPC分类号： C07D417/12 , C07D205/09 , C07D499/88 , C07F9/5683
摘要： Compounds of the general formula I
in which
X denotes a halogen atom;
Y denotes a hydrogen atom, a halogen atom, or a moiety of the general formula II
Z denotes a halogen atom, a hydroxy group, a substituted hydroxy group, an -S(O) n R⁵ group, or an -Se(O) m R⁵ group;
n denotes 0, 1 or 2, preferably 0 or 1;
m denotes 0 or 1;
R³ denotes a hydrogen atom or an organic group;
R⁴ denotes a hydrogen atom, a carboxy-salt-forming ion, or a carboxy-ester-forming group;
R⁵ denotes a hydrogen atom, a hydrocarbon group, or a heterocyclyl group; and
R¹² denotes a hydrogen atom, an unsubstituted or substituted hydrocarbon group, or an unsubstituted or substituted heterocyclyl group;
are novel intermediates useful in the preparation of 6-methylene-penems of the general formula X:
摘要翻译：通式I 的化合物，其中X表示卤素原子; Y表示氢原子，卤素原子或通式II的部分 Z表示卤素原子，羟基，取代羟基，-S（O）nR 5基团或 -Se（O）m R 5基团; n表示0,1或2，优选0或1; m表示0或1; R 3表示氢原子或有机基团; R 4表示氢原子，羧基成盐离子或羧基酯形成基团; R 5表示氢原子，烃基或杂环基; R 1表示氢原子，未取代或取代的烃基，或未取代或取代的杂环基; 是用于制备通式X的6-亚甲基 - 青铜的新型中间体： c

10. 发明公开

EP0167050A1 Clavulanate compounds, their preparation and use and intermediates thereof 失效
标题翻译： Clavulanatverbindungen，ihre Herstellung und Verwendung sowie Zwischenprodukte。
公开(公告)号：EP0167050A1
公开(公告)日：1986-01-08
申请号：EP85107476.5
申请日：1985-06-15
申请人： BEECHAM GROUP PLC
发明人： Harbridge, John Barry , Brooks, Gerald
IPC分类号： C07D498/04 , A61K31/42
CPC分类号： C07D503/00
摘要： Compounds of the general formula I:

and their pharmaceutically acceptable salts and in-vivo hydrolysable esters,
in which

each of R' and R 2 , which may be the same or different, denotes a hydrogen atom, an aryl group, or a heterocyclyl group;
X denotes a hydrogen atom, or a hydroxy, substituted hydroxy, mercapto, substituted mercapto, azido, cyano, halo, nitro, isothiocyanato, amino, substituted amino, aryl, or heterocyclyl group, or the residue of a carbon nucleophile; and
n denotes 0, 1 or 2.
are novel compounds with (ß-lactamase inhibitory and antibacterial properties.
摘要翻译：通式I：的化合物及其药学上可接受的盐和体内可水解的酯，其中R 1和R 2各自可以相同或不同，表示氢原子，芳基或杂环基; X表示氢原子，或羟基，取代的羟基，巯基，取代的巯基，叠氮基，氰基，卤素，硝基，异硫氰酸酯基，氨基，取代的氨基，芳基或杂环基，或碳亲核试剂的残基; 并且n表示0,1或2.是具有β-内酰胺酶抑制和抗菌性质的新化合物。

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