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1. 发明授权

US4438092A 5-Amino-N-(3-chloro- 2-methyl-, or 2-fluorophenyl)-1,3-dimethyl-1H-pyrazole-4-carboxamides and use as an anti-convulsant 失效
标题翻译： 5-氨基-N-（3-氯-2-甲基 - 或2-氟苯基）-1,3-二甲基-1H-吡唑-4-甲酰胺并用作抗惊厥药
公开(公告)号：US4438092A
公开(公告)日：1984-03-20
申请号：US388344
申请日：1982-06-14
申请人： Dietrich Schweiss , Ivan C. Nordin
发明人： Dietrich Schweiss , Ivan C. Nordin
IPC分类号： C07D231/16 , C07D231/20 , C07D231/38 , A61K31/415
CPC分类号： C07D231/38 , C07C255/00 , C07D231/16 , C07D231/20
摘要： New 5-amino-N-(substitutedphenyl)-1,3-disubstituted-1H-pyrazole-4-carboxamides useful as anticonvulsant agents for treating warm-blooded animals are disclosed. Also disclosed are intermediates and methods for preparing the new compounds and methods for using the new compounds.
摘要翻译：公开了用作治疗温血动物的抗惊厥剂的新的5-氨基-N-（取代苯基）-1,3-二取代-1H-吡唑-4-甲酰胺。还公开了制备新化合物的中间体和方法以及使用新化合物的方法。

2. 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。

3. 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。

4. 发明授权

US4346097A Method for treating convulsions with pyrazole-4-carboxamide derivatives 失效
标题翻译：用吡唑-4-甲酰胺衍生物治疗惊厥的方法
公开(公告)号：US4346097A
公开(公告)日：1982-08-24
申请号：US192407
申请日：1980-09-30
申请人： Dietrich Schweiss , Ivan C. Nordin
发明人： Dietrich Schweiss , Ivan C. Nordin
IPC分类号： A61K31/415 , C07D231/16 , C07D231/20 , C07D231/38
CPC分类号： C07D231/38 , C07C255/00 , C07D231/16 , C07D231/20
摘要： New 5-amino-N-(substituted phenyl)-1,3-disubstituted-1H-pyrazole-4-carboxamides useful as anticonvulsant agents for treating warm-blooded animals are disclosed. Also disclosed are intermediates and methods for preparing the new compounds and methods for using the new compounds.
摘要翻译：公开了用作治疗温血动物的抗惊厥剂的新的5-氨基-N-（取代的苯基）-1,3-二取代-1H-吡唑-4-甲酰胺。还公开了制备新化合物的中间体和方法以及使用新化合物的方法。

5. 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。

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