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公开(公告)号:EP0181172B1
公开(公告)日:1992-03-18
申请号:EP85307950.7
申请日:1985-11-01
申请人: GLAXO GROUP LIMITED
IPC分类号: C07D501/24 , C07D277/20 , A61K31/545
CPC分类号: C07D277/587 , Y02P20/55
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公开(公告)号:EP0181172A3
公开(公告)日:1988-06-01
申请号:EP85307950
申请日:1985-11-01
申请人: GLAXO GROUP LIMITED
IPC分类号: C07D501/24 , C07D277/20 , A61K31/545
CPC分类号: C07D277/587 , Y02P20/55
摘要: Compounds of general formula (I)
(where R' is a carboxyl group, a group COO ⊖ or a blocked carboxyl group;
R 2 is an amino or protected amino group; and R is hydrogen or a group of the formula CH 2 X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR 3 , where R 3 is hydrogen, a C 1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR 4 , where R" is a C 1-4 alkyl group optionally substituted by halogen or a C 1-4 alkoxy group; or a pyridinium, 3-carbamoylpyridinium or 4-carbamoyl-pyridinium group; B is -S- or -SO- (a- or β-); and the dotted line bridging the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R' is other than COO ⊖ ) are disclosed. Processes for their preparation and pharmaceutical compositions containing them are also disclosed.摘要翻译: 通式(I)的化合物(其中R'为羧基,基团COO 8或封端的羧基; R 2为氨基或被保护的氨基;且R为氢或式CH 2 X的基团,其中X代表 卤素原子,羟基,乙酰氧基;式O.CO.NHR 3的基团,其中R 3是氢,任选被1至3个卤素原子取代的C 1-4烷基或N-保护基团; 其中R“为任选被卤素或C1-4烷氧基取代的C1-4烷基;或吡啶鎓,3-氨基甲酰基吡啶鎓或4-氨基甲酰基 - 吡啶鎓基团; B为-S-或 - SO-(α-或β-);桥接2-,3-和4-位置的虚线表明化合物是ceph-2-em或ceph-3-em化合物)及其盐,化合物 当X代表吡啶鎓,3-氨基甲酰基吡啶鎓基团或4-氨基甲酰基吡啶鎓基团且R'不是COO时,式(I)的化合物与阴离子缔合) 还公开了含有它们的药物组合物和药物组合物。
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公开(公告)号:EP0497091A1
公开(公告)日:1992-08-05
申请号:EP92100095.6
申请日:1992-01-05
申请人: GLAXO GROUP LIMITED
发明人: Sidebottom, Philip James , Lester, Michael George , Procopiou, Panayiotis Alexandrou , Watson, Nigel Stephen , Bell, Richard , Giblin, Gerard Martin Paul , Bailey, Esme Joan , Kirk, Barrie Edward , Smith, Colin , Scicinski, Jan Josef , Ross, Barry Clive
CPC分类号: C07D493/08 , C12P17/181
摘要: Compounds are described of the formula
These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.摘要翻译: 化合物被描述为式CHEM。这些化合物抑制角鲨烯合成酶和/或用于制备抑制角鲨烯合酶的化合物的中间体。 本发明的化合物可以配制用于各种条件,其中动物中血浆胆固醇水平的降低将是有益的并且用于抵抗动物中的真菌感染。
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公开(公告)号:EP0181172A2
公开(公告)日:1986-05-14
申请号:EP85307950.7
申请日:1985-11-01
申请人: GLAXO GROUP LIMITED
IPC分类号: C07D501/24 , C07D277/20 , A61K31/545
CPC分类号: C07D277/587 , Y02P20/55
摘要: Compounds of general formula (I)
(where R' is a carboxyl group, a group COO ⊖ or a blocked carboxyl group;
R 2 is an amino or protected amino group; and
R is hydrogen or a group of the formula CH 2 X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR 3 , where R 3 is hydrogen, a C 1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR 4 , where R" is a C 1-4 alkyl group optionally substituted by halogen or a C 1-4 alkoxy group; or a pyridinium, 3-carbamoylpyridinium or 4-carbamoyl-pyridinium group;
B is -S- or -SO- (a- or β-); and the dotted line bridging the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R' is other than COO ⊖ ) are disclosed.
Processes for their preparation and pharmaceutical compositions containing them are also disclosed.
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