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1. 发明授权

US5017569A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5017569A
公开(公告)日：1991-05-21
申请号：US117619
申请日：1987-11-06
申请人： Alain M. Bertrandie , Thomas G. C. Bird , Frederic H. Jung , Jean-Jacques M. Lohmann
发明人： Alain M. Bertrandie , Thomas G. C. Bird , Frederic H. Jung , Jean-Jacques M. Lohmann
IPC分类号： C07D501/38 , A61K20060101 , A61K9/00 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D471/00 , C07D501/00 , C07D501/18 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D501/36 , C07D501/34 , C07D501/46
摘要： Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --Y--Q (I)wherein Y is a linking group --NR.sup.4 CO--Y'--, --NR.sup.4 SO.sub.2 --Y'--, --OCO--Y;-- or --SCO--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups or alkenyl and Y' is a bond or various optionally substituted alkylene or alkenylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring (or in the case of naphthyl either benzene ring) being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; ring Q being further optionally substituted.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.
摘要翻译：描述了具有式（I）的3-位取代基的头孢菌素化合物：其中Y是连接基-NR4CO-Y'-，-NR4SO2-Y'-，-OCO-Y的-CH2-YQ（Ⅰ）或-SCO-Y'-，其中R 4是氢，各种任选取代的烷基或烯基，Y'是一个键或各种任选取代的亚烷基或亚烯基; 并且Q是苯环（任选地与另外的苯环稠合形成萘基或任选地与含有1,2或3个选自氮，氧和硫的杂原子的5或6元杂环芳族基团稠合），所述苯环（或萘基为苯环的情况）被相互相邻的基团R1和R2取代，其中R1是羟基或其体内可水解的酯，R2是羟基，其体内可水解的酯，羧基，磺基，羟甲基，甲磺酰氨基或脲基; 或Q是式（II）或（III）的基团：其中M是氧或NR 3，其中R 3是氢或C 1-4烷基; 环Q进一步任选被取代。这些化合物作为抗菌剂的使用被描述为它们的制备方法及其中间体。

2. 发明授权

US5114933A Cephalosporin compounds 失效
标题翻译： CEPHALOSPORIN化合物
公开(公告)号：US5114933A
公开(公告)日：1992-05-19
申请号：US124213
申请日：1987-11-23
申请人： Alain M. Bertrandie , Thomas G. C. Bird , Frederic H. Jung
发明人： Alain M. Bertrandie , Thomas G. C. Bird , Frederic H. Jung
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D463/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/46 , C07D501/57 , C07D507/04 , C07D507/06 , C07D507/08
CPC分类号： A61K31/545
摘要： Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --Y--Q (I)wherein Y is a bond or a linking group --NR.sup.4 --Y'--, --O--Y'--, 13 S--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Y' is a bond or various optionally substituted alkylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.2 is hydroxy, and in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; ring Q being further optionally substituted.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.
摘要翻译：描述了具有式（I）的3-位取代基的头孢菌素化合物：其中Y是一个键的-CH 2 -YQ（I）或连接基-NR4-Y'，-Y-Y'，13 S- Y'-其中R 4是氢，各种任选取代的烷基，烯基，烷酰基或烷磺酰基，Y'是一个键或各种任选取代的亚烷基; 并且Q是苯环（任选地与另外的苯环稠合形成萘基或任选地与含有1,2或3个选自氮，氧和硫的杂原子的5或6元杂环芳族基团稠合），所述苯环其中R 1为羟基或其体内可水解的酯，R2为羟基，其体内可水解的酯，羧基，磺基，羟基甲基，甲磺酰氨基或脲基的基团R 1和R 2取代; 或Q是式（II）或（III）的基团：其中M是氧或NR 3，其中R 3是氢或C 1-4烷基; 环Q进一步任选被取代。这些化合物作为抗菌剂的使用被描述为它们的制备方法及其中间体。

3. 发明授权

US5571805A Antibiotic compounds 失效
标题翻译：抗生素化合物
公开(公告)号：US5571805A
公开(公告)日：1996-11-05
申请号：US302394
申请日：1994-09-08
申请人： Frederic H. Jung , Alain M. Bertrandie , Ronald H. B. Galt
发明人： Frederic H. Jung , Alain M. Bertrandie , Ronald H. B. Galt
IPC分类号： A61K31/40 , A61K31/397 , A61K31/41 , A61P31/04 , C07D207/16 , C07D403/12 , C07D409/12 , C07D409/14 , C07D477/00 , C07D477/20 , C07D487/04 , C07F7/10 , C07F9/568
CPC分类号： C07D207/16 , C07D403/12 , C07D409/12 , C07D409/14 , C07D477/20 , C07F9/5683
摘要： The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxyethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;P is of the formula (IA), (IB) or (IC) ##STR2## and in the formula (IB) the naphthyl group may be bonded to the nitrogen of the linking carbamoyl group at either ring; Z is carboxy, sulfonic acid, sulfinic acid, C.sub.1-4 alkanamidosulfonyl (--SO.sub.2 NHCOC.sub.1-3 alkyl), benzamidosulfonyl, C.sub.1-4 alkylsulfonylcarbamoyl (--CONHSO.sub.2 C.sub.1-4 alkyl), phenylsulfonylcarbamoyl, C.sub.1-4 alkoxy carbamoyl, hydroxycarbamoyl, sulfoamino, N--C.sub.1-4 alkanesulfonamido, cyanocarbamoyl, cyanosulfamoyl, tetrazol-5-yl, 3-hydroxyisoxazol-4-yl and 3-hydroxyisoxazol-5-yl; and P is optionally further substituted provided that when P is of the formula (IA) or (IC), Z is not carboxy;or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及碳青霉烯并提供式（I）化合物其中：R1是1-羟基乙基，1-氟乙基或羟乙基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; P是式（IA），（IB）或（IC）（IA），（IB）的化合物（IC），在式（IB）中，萘基可以键合到氮的连接氨基甲酰基; Z是羧基，磺酸，亚磺酸，C 1-4烷酰氨基磺酰基（-SO 2 NHCOC 1-3烷基），苯甲酰氨基磺酰基，C 1-4烷基磺酰基氨基甲酰基（-CONHSO 2 C 1-4烷基），苯基磺酰基氨基甲酰基，C 1-4烷氧基氨基甲酰基，羟基氨基甲酰基，磺氨基，E， -C 1-4烷基磺酰氨基，氰基氨基甲酰基，氰基氨磺酰基，四唑-5-基，3-羟基异恶唑-4-基和3-羟基异恶唑-5-基; 并且P任选进一步被取代，条件是当P为式（IA）或（IC）时，Z不为羧基; 或其药学上可接受的盐或体内可水解的酯。还描述了其制备方法，其制备中的中间体，它们作为治疗剂的用途和含有它们的药物组合物。

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