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1. 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。

2. 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。

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。

4. 发明授权

US5348951A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US5348951A
公开(公告)日：1994-09-20
申请号：US755618
申请日：1991-09-05
申请人： Frederic H. Jung
发明人： 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'--, --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 hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable 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是键或-CH 2 -YQ（I），其中Y是连接基-NR4-Y'，-O-Y'，-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。

5. 发明授权

US5444057A Carbapenem-antibiotic compounds 失效
标题翻译：碳青霉烯类抗生素化合物
公开(公告)号：US5444057A
公开(公告)日：1995-08-22
申请号：US309594
申请日：1994-09-15
申请人： Frederic H. Jung
发明人： Frederic H. Jung
IPC分类号： A61K31/44 , A61K31/397 , A61P31/04 , C07D401/12 , C07D401/14 , C07D477/00 , C07D477/20 , C07F9/568 , A01N43/00 , A61K31/395 , C07D487/04
CPC分类号： C07D477/20 , C07D401/12 , C07D401/14 , 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 hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;and the pyridyl group is bonded to the nitrogen of the linking carbamoyl group by a carbon atom, is substituted with the carboxy group on a carbon atom and is optionally substituted on one or two pyridyl ring carbon atoms; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
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-氟乙基或羟甲基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; 并且吡啶基通过碳原子与连接的氨基甲酰基的氮键合，被碳原子上的羧基取代，并且任选地被一个或两个吡啶环碳原子取代; 或其药学上可接受的盐或体内可水解的酯。其制备方法，制备中的中间体，其作为治疗剂的用途和含有它们的药物组合物。

6. 发明授权

US5254679A Cephalosporin intermediates 失效
标题翻译：头孢菌素中间体
公开(公告)号：US5254679A
公开(公告)日：1993-10-19
申请号：US723273
申请日：1991-06-28
申请人： robert H. Bradbury , Frederic H. Jung , Jean J. Lohmann , Peter R. Marsham , Georges Pasquet
发明人： robert H. Bradbury , Frederic H. Jung , Jean J. Lohmann , Peter R. Marsham , Georges Pasquet
IPC分类号： C07D207/26 , C07D207/267 , C07D213/61 , C07D213/68 , C07D213/70 , C07D217/10 , C07D237/12 , C07D237/14 , C07D237/18 , C07D237/20 , C07D237/26 , C07D277/20 , C07D401/04 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/06 , C07D417/12 , C07D463/00 , C07D471/04 , C07D487/04 , C07D495/04 , C07D501/46 , C07D505/00 , C07D513/04 , C07D501/18
CPC分类号： C07D207/267 , C07D213/61 , C07D213/68 , C07D213/70 , C07D217/10 , C07D237/12 , C07D237/14 , C07D237/18 , C07D237/20 , C07D237/26 , C07D277/587 , C07D401/04 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/06 , C07D417/12 , C07D463/16 , C07D471/04 , C07D487/04 , C07D495/04 , C07D505/00 , C07D513/04
摘要： A cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, ##STR2## represents one of C-7 acyl groups known in the cephalosporin art, R3 is hydrogen or methoxy, R4 is hydrogen, optionally substituted alkyl or allyl, and R5 is an aromatic heterocyclic ring system which is linked via carbon, and which contains a quaternized nitrogen atom.
摘要翻译：式I的头孢菌素衍生物：其中X为S，O，CH 2或SO的化合物，其中X为S，O，CH 2或SO，IMAGE为头孢菌素领域已知的C 7酰基之一，R 3为氢或甲氧基，R 4为氢，任选取代的烷基或烯丙基，R5是通过碳连接并含有季铵化氮原子的芳族杂环体系。

7. 发明授权

US5057511A 3-heterocyclic thiomethyl cephalosporins 失效
标题翻译： 3-杂环十二烷基硫代吗啉
公开(公告)号：US5057511A
公开(公告)日：1991-10-15
申请号：US133482
申请日：1987-12-15
申请人： Frederic H. Jung , Annie Olivier
发明人： Frederic H. Jung , Annie Olivier
IPC分类号： C07D501/18 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
CPC分类号： C07D501/36
摘要： Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --S--Q--(y).sub.n --Pwherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring 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 hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or P 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; said ring P being further optionally substituted; and --(Y).sub.n -- is a bond or various linking groups or --(Y)--.sub.n may be such so that rings Q and P are fused.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

8. 发明授权

US5441949A Carbapenem antibiotic compounds 失效
标题翻译：碳青霉烯类抗生素化合物
公开(公告)号：US5441949A
公开(公告)日：1995-08-15
申请号：US307048
申请日：1994-09-16
申请人： Frederic H. Jung , Jean-Claude Arnould
发明人： Frederic H. Jung , Jean-Claude Arnould
IPC分类号： A61K31/40 , A61K31/397 , A61K31/435 , A61K31/495 , A61P31/04 , C07D401/00 , C07D401/12 , C07D401/14 , C07D403/00 , C07D403/12 , C07D403/14 , C07D471/04 , C07D477/00 , C07D477/20 , C07D519/00 , C07F9/568 , A01N43/00 , A61K31/395 , C07D487/04
CPC分类号： C07F9/5683 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D477/20
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 hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;P.sup.1 is of the formula: ##STR2## and one or two of A,B,C,D,E,F,G and H, are nitrogen and the remainder are CH; and P is bonded to the nitrogen of the linking carbamoyl group by a carbon atom, in either ring, is substituted by the carboxy group on a carbon atom, in either ring, and is optionally further substituted, by up to three substitutents, on a carbon atom, in either ring; 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-氟乙基或羟甲基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; P1具有下式：，A，B，C，D，E，F，G和H中的一个或两个为氮，其余为CH; 并且P通过碳原子连接到氨基甲酰基的氮上，在任一个环中，被碳原子上的羧基，任一个环取代，并且任选进一步被至多三个取代基取代，碳原子，任一个环; 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。

9. 发明授权

US4868173A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4868173A
公开(公告)日：1989-09-19
申请号：US798804
申请日：1985-11-15
申请人： Frederic H. Jung
发明人： Frederic H. Jung
IPC分类号： C07D501/18 , A61K31/545 , A61K31/546 , A61P31/04 , C07D211/86 , C07D221/04 , C07D463/00 , C07D471/04 , C07D501/46 , C07D501/57 , C07D505/00
CPC分类号： C07D221/04 , C07D211/86 , C07D463/22 , C07D505/00
摘要： According to the invention there is provided a antibacterial cephalosporin derivative of the formula: ##STR1## in which X is sulphur, oxygen, methylene or sulphinyl; R3 is hydrogen or methoxy; R1 and R2 are known in the cephalosporin art and R4 is an aminomethyl group in which the amino group carries one of various positively charged nitrogen-containing species set out in the specification and optionally a further substituent selected from hydrogen, lower alkyl, benzyl or heteroarylloweralkyl groups.
摘要翻译：根据本发明，提供下式的抗菌头孢菌素衍生物：其中X是硫，氧，亚甲基或亚磺酰基; R3是氢或甲氧基; R1和R2在头孢菌素领域是已知的，R4是氨基甲基，其中氨基带有说明书中列出的各种带正电荷的含氮物质之一，以及任选的另外的选自氢，低级烷基，苄基或杂芳基低级烷基团体

10. 发明授权

US4463173A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4463173A
公开(公告)日：1984-07-31
申请号：US219879
申请日：1980-12-24
申请人： Frederic H. Jung
发明人： Frederic H. Jung
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07C205/35 , C07D233/28 , C07D233/68 , C07D233/90 , C07D257/04 , C07D501/16 , C07D501/18
CPC分类号： C07D257/04 , C07C205/35 , C07D233/28 , C07D233/68 , C07D233/90
摘要： A compound of the formula I: ##STR1## in which R.sup.1 is any C-3 substituent from antibacterially-active cephalosporins; R.sup.2 is any C-4 substituent from antibacterially-active cephalosporins; R.sup.3 is H, hydroxy, amino, 1-6C alkyl, 1-6C alkanoyl, 1-6C alkoxy, 1-6C alkanoylamino or 1-6C alkylamino, phenyl(1-6C)-alkyl or phenyl, each optionally substituted by methoxy; ##STR2## is of the formula II or III: ##STR3## in which R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may have a variety of values, e.g. hydrogen, carboxy, cyano or alkyl; and the salts thereof.Manufacturing processes, pharmaceutical compositions and a method of treating a bacterial infection are also disclosed.
摘要翻译：式I的化合物：其中R 1是来自抗菌活性头孢菌素的任何C-3取代基; R2是来自抗菌活性头孢菌素的任何C-4取代基; R3是H，羟基，氨基，1-6C烷基，1-6C烷酰基，1-6C烷氧基，1-6C烷酰基氨基或1-6C烷基氨基，苯基（1-6C） - 烷基或苯基，各自任选被甲氧基取代; 其中R 4，R 5，R 6，R 7，R 8和R 9可具有多种值，例如，氢，羧基，氰基或烷基; 及其盐。还公开了制造方法，药物组合物和治疗细菌感染的方法。

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