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21. 发明授权

US4681972A Separation of diastereomers 失效
标题翻译：非对映异构体的分离
公开(公告)号：US4681972A
公开(公告)日：1987-07-21
申请号：US908438
申请日：1986-09-16
申请人： James S. Kaltenbronn , Michael A. Stier
发明人： James S. Kaltenbronn , Michael A. Stier
IPC分类号： B01J23/46 , C07B57/00 , C07C67/00 , C07C239/00 , C07C271/08
CPC分类号： C07B57/00 , Y10S530/86
摘要： The S,S-isomers of Boc-benztine and Boc-cyclotine can be produced via the fractional crystallization of R-(+)-alpha-methylbenzylamine salt(s). The products are useful in the production of renin inhibitors.
摘要翻译：可以通过R - （+） - α-甲基苄胺盐的分级结晶来制备Boc-苯并三嗪和Boc-环蛇苷的S，S-异构体。该产品可用于生产肾素抑制剂。

22. 发明授权

US4137408A [Amino sulfonyl-2-oxo-nicotinyl]derivatives of cephalosporin 失效
标题翻译： {8氨基磺酰基-2-氧代 - 烟酰基{9衍生物的头孢菌素
公开(公告)号：US4137408A
公开(公告)日：1979-01-30
申请号：US845996
申请日：1977-10-27
申请人： James S. Kaltenbronn , Theodore H. Haskell , Leonard Doub
发明人： James S. Kaltenbronn , Theodore H. Haskell , Leonard Doub
IPC分类号： C07D499/66 , A61K31/44 , A61K31/545 , A61K31/546 , A61P31/04 , C07D211/22 , C07D213/78 , C07D213/80 , C07D213/82 , C07D213/85 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/20 , C07D501/57 , C07D521/00 , C07D501/34
CPC分类号： C07D213/78 , C07D211/22 , C07D213/80 , C07D213/82 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：通过以下方法提供了具有广谱抗菌效用的N- [6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素和头孢菌素型化合物的新型有机酰胺化合物：（a）使游离氨基酸适当的青霉素或头孢菌素或其酸盐或甲硅烷基化的衍生物或配合物与相应的N-6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸，7-氨基头孢烷酸，7-氨基-3-甲基头孢-3-烯-4-羧酸或其相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [ 6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟酰基] -2-取代的甘氨酸。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

23. 发明授权

US4053470A Substituted-1,2-dihydro-2-oxonicotinyl-cephalosporins 失效
标题翻译：取代的1,2-二羟基-2-氧代丁基胆碱酯
公开(公告)号：US4053470A
公开(公告)日：1977-10-11
申请号：US650098
申请日：1976-01-19
申请人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
发明人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
IPC分类号： C07D499/00 , C07D501/20 , A61K31/545 , C07D499/44
CPC分类号： C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(substituted amino)phenyl] 1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-amino-penicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

24. 发明授权

US3954734A Novel antibacterial amide compounds and process means for producing the same 失效
标题翻译：新型抗菌酰胺化合物及其制备方法
公开(公告)号：US3954734A
公开(公告)日：1976-05-04
申请号：US534031
申请日：1974-12-23
申请人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
发明人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
IPC分类号： C07D499/00 , C07D499/64 , C07D499/68 , C07D499/66 , C07D499/70
CPC分类号： C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-amino-penicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：提供了具有广谱抗菌效用的N- [6 - [（取代氨基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素和头孢菌素型化合物的新型有机酰胺化合物是通过（a）使游离氨基酸的适当的青霉素或头孢菌素或其酸性盐或甲硅烷基化衍生物与相应的N-6 - [（取代的氨基）苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基 - 青霉烷酸，7-氨基头孢烷酸，7-氨基-3-甲基头孢-3-烯-4-羧酸或其相关化合物或其酸盐或甲硅烷基化衍生物与相应DN的反应性衍生物 - [6 - [（取代氨基）苯基] -1,2-二氢-2-氧代烟酰基] -2-取代的甘氨酸。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

25. 发明授权

US3948903A Substituted N-(1,2-dihydro-2-oxonicotinyl)-cephalexins and -cephaloglycins 失效
标题翻译：取代的N-（1,2-二氢-2-氧代烟酰基） - 脑啡肽和脑胶质
公开(公告)号：US3948903A
公开(公告)日：1976-04-06
申请号：US522569
申请日：1974-11-11
申请人： Leonard Doub , James S. Kaltenbronn
发明人： Leonard Doub , James S. Kaltenbronn
IPC分类号： C07D213/80 , C07D213/85 , C07D221/16 , C07D499/00 , C07D501/20 , C07D501/34
CPC分类号： C07D213/80 , C07D213/85 , C07D221/16 , C07D499/00
摘要： Novel organic amide compounds which are substituted N-(1,2-dihydro-2-oxonicotinyl)-ampicillins, -cephalexins and -cephaloglycins having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid ampicillin, cephalexin or cephaloglycin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding 1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid or 7-amino-3-methylceph-3-em-4-carboxylic acid or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-(1,2-dihydro-2-oxonicotinyl)-2-phenylglycine.
摘要翻译：通过（a）使游离氨基酸氨苄青霉素，头孢氨苄或头孢氨呋喃或者头孢氨苄或其他化合物反应，得到具有广谱抗菌效用的取代的N-（1,2-二氢-2-氧代烟碱基） - 滑环蛋白， - 脑啡肽和 - 其酸性盐或甲硅烷基化衍生物与相应的1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸，7-氨基头孢烷酸或7-氨基-3-甲基头孢 -3-em-4-羧酸或其酸式盐或甲硅烷基化衍生物与相应的N-（1,2-二氢-2-氧代烟酰基）-2-苯基甘氨酸的反应性衍生物。

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