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1. 发明授权

US4315933A Antibacterial amide compounds and pharmaceutical compositions containing the same 失效
标题翻译：抗菌酰胺化合物和含有它的药物组合物
公开(公告)号：US4315933A
公开(公告)日：1982-02-16
申请号：US190154
申请日：1980-09-24
申请人： Thomas F. Mich , Theodore H. Haskell , Marland P. Hutt, Jr.
发明人： Thomas F. Mich , Theodore H. Haskell , Marland P. Hutt, Jr.
IPC分类号： C07D239/36 , C07D499/00 , C07D499/64 , A61K31/505 , C07D499/70
CPC分类号： C07D239/36 , C07D499/00
摘要： Novel organic amide compounds which are N-[2-(acylaminophenyl)-4-hydroxy-5-pyrimidinylcarbonyl]penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-(acylaminophenyl)-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-(acylaminophenyl)-4-hydroxy-5-pyrimidinylcarbonyl]-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（a）使适当的青霉素或酸式盐的游离氨基酸反应，得到具有广谱抗菌效用的N- [2-（酰基氨基苯基）-4-羟基-5-嘧啶基羰基]青霉素化合物的新型有机酰胺化合物或甲硅烷基化的衍生物或其配合物与相应的N-2-（酰氨基苯基）-4-羟基-5-嘧啶羧酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸或相关化合物或酸盐或其甲硅烷基化衍生物与相应的DN- [2-（酰氨基苯基）-4-羟基-5-嘧啶基羰基] -2-取代的甘氨酸的反应性衍生物。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。

2. 发明授权

US4278681A Antibacterial amide compounds and means for using the same 失效
标题翻译：抗菌酰胺化合物及其使用方法
公开(公告)号：US4278681A
公开(公告)日：1981-07-14
申请号：US112657
申请日：1980-01-31
申请人： Theodore H. Haskell , Marland P. Hutt, Jr. , Ernest D. Nicolaides , Peter W. K. Woo , Gin G. Huang
发明人： Theodore H. Haskell , Marland P. Hutt, Jr. , Ernest D. Nicolaides , Peter W. K. Woo , Gin G. Huang
IPC分类号： C07D207/16 , C07D207/28 , C07D213/80 , C07D213/85 , C07D499/00 , C07D499/64 , C07F7/10 , A61K31/455 , C07D499/68
CPC分类号： C07D213/80 , C07D207/16 , C07D207/28 , C07D213/85 , C07D499/00 , C07F7/10
摘要： Novel organic amide compounds which are N-[6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(acylaminoacylamino or aminoacylamino)-phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(acylaminoacylamino or aminoacylamino) 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 - [（酰氨基酰氨基或氨基酰氨基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素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其酸盐或甲硅烷基化衍生物或其配合物与相应的N-6 - [（酰氨基酰基氨基或氨基酰氨基） - 苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）氨基酸6-氨基青霉烷酸或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 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -1,2-二氢-2-氧代烟酰基] - 2-取代甘氨酸。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。

3. 发明授权

US4267180A 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：US4267180A
公开(公告)日：1981-05-12
申请号：US117318
申请日：1980-01-31
申请人： Theodore H. Haskell , Marland P. Hutt, Jr. , Ernest D. Nicolaides
发明人： Theodore H. Haskell , Marland P. Hutt, Jr. , Ernest D. Nicolaides
IPC分类号： C07D239/36 , C07D499/00 , C07D499/64 , C07D521/00 , A61K31/505 , C07D499/68
CPC分类号： C07D239/36 , C07D231/12 , C07D233/56 , C07D249/08 , C07D499/00
摘要： Novel organic amide compounds which are N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid of 6-aminopenicillamic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]-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（a）使适当的青霉素的游离氨基酸反应，得到具有广谱抗菌效用的N- [2 - [（酰氨基酰氨基或氨酰氨基）苯基] -4-羟基-5-嘧啶基羰基]青霉素化合物的新型有机酰胺化合物或其酸性盐或甲硅烷基化衍生物或其配合物与相应的N-2 - [（酰氨基酰基氨基或氨基酰基氨基）苯基] -4-羟基-5-嘧啶羧酸的反应性衍生物或（b）游离氨基酸6 - 氨基青霉胺酸或相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [2 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -4-羟基-5-嘧啶基羰基] -2-取代的甘氨酸的反应性衍生物。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。

4. 发明授权

US4311699A Aminoacid derivatives of cephalosporin compounds 失效
标题翻译：头孢菌素化合物的氨基酸衍生物
公开(公告)号：US4311699A
公开(公告)日：1982-01-19
申请号：US112656
申请日：1980-01-31
申请人： Theodore H. Haskell , Thomas F. Mich , Joseph P. Sanchez , Dietrich Schweiss
发明人： Theodore H. Haskell , Thomas F. Mich , Joseph P. Sanchez , Dietrich Schweiss
IPC分类号： C07D239/36 , C07D501/24 , C07D521/00 , A61K31/545 , C07D501/34 , C07D501/56
CPC分类号： C07D239/36 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Novel organic amide compounds which are N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]cephalosporin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid 7-aminocephalosporanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]-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（a）使适当头孢菌素的游离氨基酸反应，得到具有广谱抗菌效用的N- [2 - [（酰氨基酰氨基或氨基酰氨基）苯基] -4-羟基-5-嘧啶基羰基]头孢菌素的新型有机酰胺化合物或其相应的N-2 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -4-羟基-5-嘧啶羧酸的反应性衍生物的酸式盐或甲硅烷基化衍生物或其配合物，或（b）使游离氨基酸7- 氨基头孢烷酸或相关化合物或其酸盐或甲硅烷基化衍生物与相应的DN- [2 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -4-羟基-5-嘧啶基羰基] -2-取代的甘氨酸的反应性衍生物。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。

5. 发明授权

US4311698A Aminoacid derivatives of cephalosporin compounds 失效
标题翻译：头孢菌素化合物的氨基酸衍生物
公开(公告)号：US4311698A
公开(公告)日：1982-01-19
申请号：US112655
申请日：1980-01-31
申请人： Theodore H. Haskell , Thomas F. Mich , Dietrich Schweiss , Townley P. Culbertson
发明人： Theodore H. Haskell , Thomas F. Mich , Dietrich Schweiss , Townley P. Culbertson
IPC分类号： C07D213/80 , C07D213/85 , C07D501/24 , C07D521/00 , A61K31/545 , C07D501/34 , C07D501/56
CPC分类号： C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Novel organic amide compounds which are N-[6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl]cephalosporin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 7-aminocephalosporanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-(acylaminoacylamino or aminoacylamino)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：具有广谱抗菌效用的N- [6 - [（酰氨基酰氨基或氨酰氨基）苯基] -1,2-二氢-2-氧代烟酰基]头孢菌素化合物的新型有机酰胺化合物是通过（a）使游离氨基酸适当的头孢菌素或其酸盐或甲硅烷基化衍生物或其配合物与相应的N-6 - [（酰氨基酰基氨基或氨酰基氨基）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7-氨基头孢烷酸或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-（酰氨基酰基氨基或氨酰基氨基）苯基] -1,2-二氢-2-氧代烟酰基] -2- 取代甘氨酸。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。

6. 发明授权

US4315858A Antibacterial amide compounds 失效
标题翻译：抗菌酰胺化合物
公开(公告)号：US4315858A
公开(公告)日：1982-02-16
申请号：US190128
申请日：1980-09-24
申请人： Leonard Doub , Theodore H. Haskell , Thomas F. Mich , Dietrich Schweiss
发明人： Leonard Doub , Theodore H. Haskell , Thomas F. Mich , Dietrich Schweiss
IPC分类号： C07D213/64 , C07D499/00 , C07D499/64 , C07D499/70 , C07D401/12
CPC分类号： C07D213/64 , C07D499/00
摘要： Novel organic amide compounds which are N-[6-(acylaminophenyl)-1,2-dihydro-2-oxonicotinoyl]penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[acylaminophenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[acylaminophenyl]-1,2-dihydro-2-oxonicotinoyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：具有广谱抗菌效用的N- [6-（酰氨基苯基）-1,2-二氢-2-氧代烟酰基]青霉素化合物的新型有机酰胺化合物是通过（a）使适当的青霉素或酸的游离氨基酸盐或甲硅烷基化衍生物或其配合物与相应的N-6- [酰氨基苯基] -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-氨基青霉烷酸或相关化合物或其酸盐或甲硅烷基化衍生物与相应的DN- [6- [酰氨基苯基] -1,2-二氢-2-氧代烟酰基] -2-取代的甘氨酸的反应性衍生物。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。

7. 发明授权

US4123609A Process for the production of 9-(.beta.-D-arabinofuranosyl)adenine, 5'-phosphate 失效
标题翻译：生产9 - （{62 -D-阿拉伯呋喃糖基）腺嘌呤，5（40-磷酸）的方法
公开(公告)号：US4123609A
公开(公告)日：1978-10-31
申请号：US831703
申请日：1977-09-12
申请人： Walter E. Behnke , William R. Marsh , Theodore H. Haskell
发明人： Walter E. Behnke , William R. Marsh , Theodore H. Haskell
IPC分类号： C07H19/20 , C07H17/00
CPC分类号： C07H19/20
摘要： Process for the production of an ester product, 9-(.beta.-D-arabinofuranosyl)adenine, 5'-phosphate, in which the mixture resulting from reaction of 9-(.beta.-D-arabinofuranosyl)adenine with phosphorylating agent in trialkyl phosphate solvent is subjected to aqueous hydrolysis, the pH of the hydrolysis mixture is adjusted upward sufficiently to cause separation into aqueous and non-aqueous liquid phases, the trialkyl phosphate solvent is removed, and the product is precipitated from the residual aqueous mixture and isolated.
摘要翻译：制备9-（β-D-阿糖呋喃糖基）腺嘌呤，5'-磷酸酯的酯产物的方法，其中由9-（β-D-阿拉伯呋喃糖基）腺嘌呤与磷酸化剂在三烷基磷酸酯溶剂中反应得到的混合物进行水解，水解混合物的pH被充分调高以使其分离成水相和非水相液体相，除去三烷基磷酸酯溶剂，并将产物从残留的含水混合物中沉淀并分离。

8. 发明授权

US4101661A 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：US4101661A
公开(公告)日：1978-07-18
申请号：US803004
申请日：1977-06-03
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 , A61K31/43 , A61K31/455
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 corresponing 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对应的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。

9. 发明授权

US4404201A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4404201A
公开(公告)日：1983-09-13
申请号：US321021
申请日：1981-11-13
申请人： Theodore H. Haskell , Marland P. Hutt
发明人： Theodore H. Haskell , Marland P. Hutt
IPC分类号： C07D215/54 , C07D215/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D501/34 , C07D501/36 , A61K31/545
CPC分类号： C07D215/56 , C07D215/54 , C07D401/06 , C07D401/12 , C07D401/14
摘要： Novel organic amide compounds which are N-[[(acylaminoacylamino or aminoacylamino)]-dihydro-oxo-3-quinolinylcarbonyl]cephalosporin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate cephalosporin or the acid addition salt or silylated derivative or complex thereof with a reactive derivative of the corresponding (acylaminoacylamino or aminoacylamino)dihydro-oxo-3-quinolinecarboxylic acid or (b) reacting the free amino acid 7-aminocephalosporanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[(acylaminoacylamino or aminoacylamino)dihydro-oxo-3-quinolinylcarbonyl]-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（a）使适当的头孢菌素或酸的游离氨基酸反应，得到具有广谱抗菌效用的N - [[（酰氨基酰氨基或氨基酰氨基）] - 二氢 - 氧代-3-喹啉基羰基]头孢菌素化合物加成盐或甲硅烷基化的衍生物或其配合物与相应的（酰基氨基酰基氨基或氨酰基氨基）二氢 - 氧代-3-喹啉羧酸的反应性衍生物或（b）使游离氨基酸7-氨基头孢烷酸或相关化合物或酸盐或甲硅烷基化衍生物与相应的DN - [（酰氨基酰氨基或氨酰氨基）二氢 - 氧代-3-喹啉基羰基] -2-取代的甘氨酸的反应性衍生物。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。

10. 发明授权

US4374138A Antibacterial amide compounds, compositions, and methods of use 失效
标题翻译：抗菌酰胺化合物，组合物和使用方法
公开(公告)号：US4374138A
公开(公告)日：1983-02-15
申请号：US321020
申请日：1981-11-13
申请人： Theodore H. Haskell , Marland P. Hutt
发明人： Theodore H. Haskell , Marland P. Hutt
IPC分类号： C07D215/54 , C07D215/56 , C07D499/00 , C07D499/64 , A61K31/47 , C07D215/22 , C07D499/70
CPC分类号： C07D215/54 , C07D215/56 , C07D499/00
摘要： Novel organic amide compounds which are N-[ureidodihydro-oxo-3-quinolinylcarbonyl]penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding ureido-dihydro-oxo-3-quinolinecarboxylic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[ureidodihydro-oxo-3-quinolinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：通过以下方法提供具有广谱抗菌效用的N- [脲基二氢 - 氧代-3-喹啉基羰基]青霉素化合物的新型有机酰胺化合物：（a）使适当的青霉素或其酸盐或甲硅烷基化衍生物或其络合物的游离氨基酸与使相应的脲基 - 二氢 - 氧代-3-喹啉羧酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸或相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [脲基二氢 - 氧代-3-喹啉基羰基] -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。

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