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1. 发明授权

US5232918A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5232918A
公开(公告)日：1993-08-03
申请号：US653149
申请日：1991-02-11
申请人： Jean C. Arnould , Dominique Boucherot , David H. Davies , Frederick H. Jung , Colin J. Strawson
发明人： Jean C. Arnould , Dominique Boucherot , David H. Davies , Frederick H. Jung , Colin J. Strawson
IPC分类号： A61K31/545 , C07D241/44 , C07D501/36 , C07D501/46
CPC分类号： C07D501/46 , C07D501/40
摘要： Cephalosporin derivatives having a 3-position substituent of formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;R.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.4 has various values. 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衍生物：其中R 1是氢，烯基或任选取代的烷基，Het是通过碳原子与酰胺键键合的5-或6-元杂环，其中 Het选自式II-III的基团：其中A是CH或氮原子; B是氧，硫或NR4基团; D，E，F和G中的一个或两个是氮原子，其余是CH基团：或Het是吡嗪酮，吡啶酮，哒嗪酮或嘧啶酮环，或者是这样的环的硫酮当量，所述环具有取代基R 4 在一个氮原子上，或是吡喃酮或吡喃硫酮; 环Het被任何两个相邻的碳原子融合到苯环上; Het通过碳原子连接到-CH 2 NR 1 CO-基团; R2为羟基或其体内可水解的酯; R3是R2的邻位，是羟基或其体内可水解的酯; R4具有各种价值。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

US5371220A Bicyclo-heterocyclic intermediates for cephalosporin compounds 失效
标题翻译：双环杂环中间体用于头孢菌素化合物
公开(公告)号：US5371220A
公开(公告)日：1994-12-06
申请号：US886392
申请日：1992-05-21
申请人： Dominique Boucherot , Frederick H. Jung , Colin J. Strawson
发明人： Dominique Boucherot , Frederick H. Jung , Colin J. Strawson
IPC分类号： A61K31/545 , C07D241/44 , C07D501/36 , C07D501/46
CPC分类号： C07D501/46 , C07D501/40
摘要： Cephalosporins derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atomR.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.4 has various values. 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衍生物：其中R 1是氢，烯基或任选取代的烷基，Het是通过碳原子与酰胺键连接的5-或6-元杂环，其中Het选自式II-III的基团：其中A是CH或氮原子; B是氧，硫或NR4基团; D，E，F和G中的一个或两个是氮原子，其余是CH基团：或Het是吡嗪酮，吡啶酮，哒嗪酮或嘧啶酮环，或者是这样的环的硫酮当量，所述环具有取代基R 4 在一个氮原子上，或是吡喃酮或吡喃硫酮; 环Het被任何两个相邻的碳原子融合到苯环上; Het通过碳原子连接到-CH 2 NR 1 CO-基团上，R2是羟基或其体内可水解的酯; R3是R2的邻位，是羟基或其体内可水解的酯; R4具有各种价值。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

US5200404A 3-tetrazolylthiomethyl cephalosporin antibiotics 失效
标题翻译： 3-四氢唑硫代吗啉抗生素
公开(公告)号：US5200404A
公开(公告)日：1993-04-06
申请号：US670863
申请日：1991-03-18
申请人： Frederick H. Jung
发明人： Frederick H. Jung
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36
CPC分类号： C07D501/00
摘要： A compound of the formula (II): ##STR1## and pharmaceutically acceptable salts an in vivo hydrolysable esters are described as is their preparation and use as antibacterial agents.

4. 发明授权

US5008258A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5008258A
公开(公告)日：1991-04-16
申请号：US221945
申请日：1988-07-18
申请人： Thomas G. C. Bird , Frederick H. Jung
发明人： Thomas G. C. Bird , Frederick H. Jung
IPC分类号： C07D501/56 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/46 , C07D501/48
CPC分类号： C07D501/46
摘要： Cephalosporin compounds having as a 3-substituent the group: ##STR1## wherein Y represents a bond, optionally substituted alkylene or --CH.sub.2 CH.sub.2 NHCO--, P is a benzene ring substituted by groups W and Z ortho with respect to one another wherein W is hydroxy or an in vivo hydrolyzable ester thereof, Z is hydroxy, an in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, --NHSO.sub.2 CH.sub.3 or NHCONH.sub.2, Q is a mono- or bicyclic ring system substituted by R.sup.7 wherein R.sup.7 is hydrogen or a range of groups and ring Q is optionally further substituted; are described as antibacterial agents. Processes for their preparation and their methods of use are described.

5. 发明授权

US5019570A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US5019570A
公开(公告)日：1991-05-28
申请号：US223988
申请日：1988-07-25
申请人： Jean C. Arnould , Dominique Boucherot , David H. Davies , Frederick H. Jung , Colin J. Strawson
发明人： Jean C. Arnould , Dominique Boucherot , David H. Davies , Frederick H. Jung , Colin J. Strawson
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D209/04 , C07D209/42 , C07D215/22 , C07D215/48 , C07D215/54 , C07D215/56 , C07D217/22 , C07D217/26 , C07D237/28 , C07D239/28 , C07D239/72 , C07D239/74 , C07D239/80 , C07D239/88 , C07D239/90 , C07D241/00 , C07D241/44 , C07D251/54 , C07D311/04 , C07D311/08 , C07D311/18 , C07D311/22 , C07D311/76 , C07D471/00 , C07D501/00 , C07D501/04 , C07D501/24 , C07D501/38 , C07D501/40 , C07D501/46 , C07D501/48 , C07D501/56 , C07D501/57
CPC分类号： C07D501/46 , C07D501/40
摘要： Cephalosporin derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het us a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;R.sup.2 is hydroxy or an in vivo hydrolyzable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolyzable ester thereof; and R.sup.4 has various values. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

6. 发明授权

US5008259A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US5008259A
公开(公告)日：1991-04-16
申请号：US349663
申请日：1989-05-10
申请人： Patrice J. Siret , Frederick H. Jung , William Bell
发明人： Patrice J. Siret , Frederick H. Jung , William Bell
IPC分类号： C07D501/38 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/46
CPC分类号： C07D501/00
摘要： Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described, wherein R.sup.1 is hydrogen or certain optionally substituted alkyl groups; X is a benzene ring or certain 5 or 6-membered heterocyclic ring and is fused to ring Y which is a nitrogen containing heteroaryl group; R.sup.2 and R.sup.3 are independently hydroxy or an in vivo hydrolysable ester thereof, and ring system X-Y is optionally substituted. Processes for their preparation and use are described.
摘要翻译：描述了具有下式的3位取代基的头孢菌素抗生素：其中R 1是氢或某些任选取代的烷基; X是苯环或某些5或6元杂环，并且与作为含氮杂芳基的环Y稠合; R2和R3独立地是羟基或其体内可水解的酯，环系X-Y任选地被取代。描述了其制备和使用的方法。

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