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1. 发明授权

US5494888A 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid imino ester derivatives, processes for their production and a method for their application as herbicides 失效
标题翻译： 6-氯-2-（4,6-二甲氧基嘧啶-2-基）氧基苯甲酸亚氨基酯衍生物，其制备方法及其作为除草剂的方法
公开(公告)号：US5494888A
公开(公告)日：1996-02-27
申请号：US186589
申请日：1994-01-26
申请人： Chang U. Hur , Jin H. Cho , Ho S. Lee , Sang K. Yoo , Su M. Hong , Hong W. Kim , Jae S. Rim , Yeong T. Bae , Sang H. Chae , Jeong S. Kim , Byoung B. Lee , Hun S. Oh , Woo B. Choi
发明人： Chang U. Hur , Jin H. Cho , Ho S. Lee , Sang K. Yoo , Su M. Hong , Hong W. Kim , Jae S. Rim , Yeong T. Bae , Sang H. Chae , Jeong S. Kim , Byoung B. Lee , Hun S. Oh , Woo B. Choi
IPC分类号： C07D239/60 , A01N43/54 , A01N43/78 , C07D239/66 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/00
CPC分类号： C07D401/12 , A01N43/54 , A01N43/78 , C07D239/66 , C07D405/12 , C07D409/12
摘要： The present invention relates to 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid iminoester derivative of the general formula I; process of their preparation and a method for their application as herbicides: ##STR1## wherein R and Q are as defined in the specification.
摘要翻译：本发明涉及通式I的6-氯-2-（4,6-二甲氧基嘧啶-2-基）氧基苯甲酸亚氨基酯衍生物; 其制备方法及其作为除草剂应用的方法：其中R和Q如说明书中所定义。

2. 发明授权

US5292733A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US5292733A
公开(公告)日：1994-03-08
申请号：US866156
申请日：1992-04-09
申请人： Yong Z. Kim , Hun S. Oh , Jae H. Yeo , Jong C. Lim , Won S. Kim , Chan S. Bang , Hyeon J. Yim
发明人： Yong Z. Kim , Hun S. Oh , Jae H. Yeo , Jong C. Lim , Won S. Kim , Chan S. Bang , Hyeon J. Yim
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/04 , C07D501/36
CPC分类号： C07D501/00
摘要： The present invention relates to a cephalosporin compound including the pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates thereof of the formula(I) and its isomers: ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl or --C(R.sup.3)(R.sup.4)COOH wherein R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl group, or constitute a C.sub.3-7 cycloalkyl group with the carbon atoms to which R.sup.3 and R.sup.4 are attached;R.sup.2, which may be attached to N.sup.a or N.sup.b, is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-7 cycloalkyl, aryl or amino group; andQ.sub.1 and Q.sub.2, which may be the same or different, are CH or N.
摘要翻译：本发明涉及一种头孢菌素化合物，其包括式（I）的药学上可接受的无毒盐，生理上可水解的酯，水合物和溶剂化物及其异构体：（*化学结构*）（I）（*化学结构*）其中：R 1是C 1-4烷基，C 3-4烯基，C 3-4炔基或-C（R 3）（R 4）COOH，其中R 3和R 4可以相同或不同，是氢，C 1-4烷基或者构成与R3和R4相连的碳原子的C3-7环烷基; 可以连接到Na或Nb的R2是C1-4烷基，C3-4烯基，C3-7环烷基，芳基或氨基; 和可以相同或不同的Q1和Q2是CH或N.

3. 发明授权

US5571804A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US5571804A
公开(公告)日：1996-11-05
申请号：US303930
申请日：1994-09-09
申请人： Chan S. Bang , Jae H. Yeo , Young M. Woo , Jong C. Lim , Deog H. Yang , Se H. Kim , Jae H. Jeon , Mi K. Seo , Sam S. Kim , Tae H. Lee , Yong Z. Kim , Hun S. Oh
发明人： Chan S. Bang , Jae H. Yeo , Young M. Woo , Jong C. Lim , Deog H. Yang , Se H. Kim , Jae H. Jeon , Mi K. Seo , Sam S. Kim , Tae H. Lee , Yong Z. Kim , Hun S. Oh
IPC分类号： A61K31/546 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/60 , A61K31/545
CPC分类号： C07D501/00 , Y02P20/55
摘要： Cephalosporin compounds of formula (I): ##STR1## wherein: R.sup.1 is a hydrogen or an amino protecting group;R.sup.2 and R.sup.3 are, independently, a hydrogen or a hydroxy protecting group, or form together a cyclic diol protecting group;R.sup.4 and R.sup.5 are, independently, a hydrogen or a carboxyl protecting group;X and Y are a nitrogen and a carbon atom, respectively, or a carbon and a nitrogen atom, respectively;R.sup.6 and R.sup.7 are, independently, a hydrogen or an amino, substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxy carbonyl group, or jointly form a C.sub.3-7 cycloalkyl group together with the carbon to which they are attached, when X and Y are a nitrogen and a carbon, respectively, or R.sup.7 is a hydrogen or an amino group when X and Y are a carbon and a nitrogen, respectively; andQ is .dbd.CH-- or .dbd.N--, or pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates and isomers thereof, and isomers thereof possess potent and broad antibacterial activities.
摘要翻译：式（I）的头孢菌素化合物： R2和R3独立地是氢或羟基保护基，或者一起形成环状二醇保护基; R4和R5独立地是氢或羧基保护基; X和Y分别是氮和碳原子，或分别是碳和氮原子; R 6和R 7独立地是氢或氨基，取代的氨基，羟基，烷氧基，C 1-4烷基，羧基或烷氧基羰基，或者与它们所连接的碳一起共同形成C 3-7环烷基，当X和Y分别为氮和碳时，或当X和Y分别为碳和氮时，R 7为氢或氨基; 并且Q是= CH-或= N-，或药学上可接受的无毒盐，生理上可水解的酯，水合物和溶剂合物及其异构体及其异构体具有有效和广泛的抗菌活性。

4. 发明授权

US5416081A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US5416081A
公开(公告)日：1995-05-16
申请号：US171535
申请日：1993-12-22
申请人： Chan S. Bang , Yong Z. Kim , Jae H. Yeo , Jong C. Lim , Hun S. Oh , Young M. Woo , Duk H. Yang , Sam S. Kim , Hyeon J. Yim
发明人： Chan S. Bang , Yong Z. Kim , Jae H. Yeo , Jong C. Lim , Hun S. Oh , Young M. Woo , Duk H. Yang , Sam S. Kim , Hyeon J. Yim
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36
CPC分类号： C07D501/00
摘要： The present invention relates to novel cephalosporin compounds, pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates and isomers thereof which possess potent and broad antibacterial activities. The compounds of the present invention have a (4-amino-1-substituted-alkapyrimidinium-4-yl)thiomethyl group in 3-position of the cephem nucleus and is specifically represented by the following formula(I): ##STR1## wherein: R.sup.1 is a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or --C(R.sup.A)(R.sup.B)COOH group wherein R.sup.A and R.sup.B are independently a hydrogen atom or a C.sub.1-4 alkyl group, or form a C.sub.3-7 cycloalkyl group together with the carbon atom to which they are attached;R.sup.2 is an unsubstituted or substituted amino, C.sub.1-4 alkyl or C.sub.3-7 cycloalkyl group; andn is an integer ranging from 2 to 7.
摘要翻译：本发明涉及具有有效和广泛的抗菌活性的新型头孢菌素化合物，药学上可接受的无毒盐，生理上可水解的酯，水合物和溶剂合物及其异构体。本发明的化合物在头孢烯核的3位具有（4-氨基-1-取代 - 烷基嘧啶鎓-4-基）硫代甲基，具体由下式（I）表示：C 1-4烷基，C 2-4的链烯基，C 2-4炔基或-C（RA）（R B）COOH基，其中RA和RB独立地为氢原子或C 1-4烷基，或与碳原子一起形成C 3-7环烷基它们所附着的原子; R2是未取代或取代的氨基，C1-4烷基或C3-7环烷基; n为2〜7的整数。

5. 发明授权

US5202315A Cephalosporin compounds 失效
标题翻译： CEPHALOSPORIN化合物
公开(公告)号：US5202315A
公开(公告)日：1993-04-13
申请号：US494163
申请日：1990-03-15
申请人： Yong Z. Kim , Hun S. Oh , Jae H. Yeo , Jong C. Lim , Won S. Kim , Chan S. Bang , Hyeon J. Yim
发明人： Yong Z. Kim , Hun S. Oh , Jae H. Yeo , Jong C. Lim , Won S. Kim , Chan S. Bang , Hyeon J. Yim
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
CPC分类号： C07D501/36
摘要： The present invention relates to new cephalosporin compounds of the formula(I), pharmaceutically acceptable non-toxic salts thereof, and physiologically hydrolyzable esters and solvates thereof, which have potent and broad antibacterial activities ##STR1## wherein R.sup.1 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl, C.sub.3.about.4 alkynyl group, or --C(R.sup.a)(R.sup.b)CO.sub.2 H.sub.1 wherein R.sup.a and R.sup.b are the same or different, and each is a hydrogen atom or a C.sub.1.about.4 alkyl group, or R.sup.a and R.sup.b form a C.sub.3.about.7 cycloalkyl group with the carbon atom to which they are linked;R.sup.2 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl or C.sub.3.about.4 cycloalkyl group, a substituted or unsubstituted amino group, or a substituted or unsubstituted phenyl group;R.sup.3 is hydrogen or a C.sub.1.about.4 alkyl group; andQ is N or CH.The invention further relates to a process for preparing said compounds, and to pharamaceutical compositions containing said compounds.

6. 发明授权

US4971962A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4971962A
公开(公告)日：1990-11-20
申请号：US350617
申请日：1989-05-11
申请人： Hun S. Oh , Yong Z. Kim , Jae H. Yeo , Jong C. Lim , Won S. Kim , Soon H. An , Chan S. Bang , Hyeon J. Yim
发明人： Hun S. Oh , Yong Z. Kim , Jae H. Yeo , Jong C. Lim , Won S. Kim , Soon H. An , Chan S. Bang , Hyeon J. Yim
IPC分类号： C07D501/00 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention relates to novel cephalosporin compounds having high antimicrobial activity, which are shown by the formula(I), and to a process for preparing them ##STR1## wherein R.sup.1 is a hydrogen atom or an amino protecting group;R.sup.2 is acetoxy; andR.sup.3 is a hydrogen atom or a carboxyl protecting group (wherein when R.sup.2 contains quaternary ammonium, r.sup.2 and R.sup.3 may form a zwitter ion).The present invention also relates to the non-toxic and pharmaceutically acceptable salts of the cephalosporin compounds of the formula (I). Also described are compositions containing the antibiotics according to the present invention.
摘要翻译：本发明涉及具有高抗微生物活性的新型头孢菌素化合物，其由式（I）表示，及其制备方法其中R 1为氢原子或氨基保护基; R2是乙酰氧基; 并且R 3是氢原子或羧基保护基（其中当R 2含有季铵时，r 2和R 3可以形成一个两性离子）。本发明还涉及式（I）的头孢菌素化合物的无毒和药学上可接受的盐。还描述了含有根据本发明的抗生素的组合物。

7. 发明授权

US5605895A Cephalosporin antibiotics and processes for preparation thereof 失效
标题翻译：头孢菌素类抗生素及其制备方法
公开(公告)号：US5605895A
公开(公告)日：1997-02-25
申请号：US277629
申请日：1994-07-20
申请人： Chan S. Bang , Yong Z. Kim , Jae H. Yeo , Jong C. Lim , Young M. Woo , Hun S. Oh , Duk H. Yang , Sam S. Kim , Se H. Kim , Jae H. Jeon , Tae H. Lee , Sung I. Kim , Mi K. Seo , Jae W. Lee
发明人： Chan S. Bang , Yong Z. Kim , Jae H. Yeo , Jong C. Lim , Young M. Woo , Hun S. Oh , Duk H. Yang , Sam S. Kim , Se H. Kim , Jae H. Jeon , Tae H. Lee , Sung I. Kim , Mi K. Seo , Jae W. Lee
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention relates to a cephalosporin compound represented by the following general formula (I), its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, which is useful as an antibiotic agent: ##STR1## in which R.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and each represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a diol-protecting cyclic group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5 represents hydrogen, C.sub.1-4 alkyl, alkoxycarbonyl, carboxyl or sulfomethyl,R.sup.6 represents hydrogen, amino or substituted amino, andR.sup.7 represents C.sub.1-4 alkyl, amino or substituted amino, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a 3 to 7-membered cyclic group, orR.sup.6 and R.sup.7 together with the carbon and nitrogen atoms to which they are attached can form a 3 to 7-membered heterocyclic ring which may optionally contain additional heteroatoms such as nitrogen and/or oxygen and which may be substituted with the substituents selected from C.sub.1-4 alkyl, amino and substituted amino, andQ represents CH or N.
摘要翻译：本发明涉及以下通式（I）表示的头孢菌素化合物，其药学上可接受的无毒盐，生理上可水解的酯，水合物或溶剂化物或其异构体，其可用作抗生素： I），其中R 1表示氢或氨基保护基，R 2和R 3可以相同或不同，各自表示氢或羟基保护基，或者R 2和R 3一起可以形成二醇保护的环状基团，R 4表示氢或羧基保护基，R5表示氢，C1-4烷基，烷氧基羰基，羧基或磺基甲基，R6表示氢，氨基或取代的氨基，R7表示C1-4烷基，氨基或取代的氨基，或R5和R6连同它们连接的碳原子可以形成3至7元环基，或者R6和R7与它们所连接的碳原子和氮原子一起可以形成3至7元杂环，其可以任选地含有另外的杂原子如氮和/或氧并且可以被选自C 1-4烷基，氨基和取代的氨基的取代基取代，Q代表CH或N.

8. 发明授权

US5541175A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US5541175A
公开(公告)日：1996-07-30
申请号：US301619
申请日：1994-09-07
申请人： Jae H. Yeo , Chan S. Bang , Jong C. Lim , Young M. Woo , Deog H. Yang , Se H. Kim , Jae H. Jeon , Mu Y. Kim , Sam S. Kim , Tae H. Lee , Yong Z. Kim , Hun S. Oh
发明人： Jae H. Yeo , Chan S. Bang , Jong C. Lim , Young M. Woo , Deog H. Yang , Se H. Kim , Jae H. Jeon , Mu Y. Kim , Sam S. Kim , Tae H. Lee , Yong Z. Kim , Hun S. Oh
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/04 , C07D501/24 , C07D501/60 , A01K31/545
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention relates to a cephalosporin compound represented by the following general formula (I): ##STR1## its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, in whichR.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and independently of one another represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a cyclic diol-protecting group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen, amino or substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxycarbonyl, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a C.sub.3-7 cycle, andQ represents CH or N,and to a process for preparation thereof and a pharmaceutical composition containing the compound (I) as an active ingredient.
摘要翻译：本发明涉及由以下通式（I）表示的头孢菌素化合物：其药学上可接受的无毒盐，生理上可水解的酯，水合物或溶剂合物或其异构体，其中R 1 表示氢或氨基保护基，R2和R3可以相同或不同，彼此独立地表示氢或羟基保护基，或者R2和R3一起可以形成环状二醇保护基，R4表示氢或羧基保护基，R 5，R 6和R 7彼此独立地表示氢，氨基或取代的氨基，羟基，烷氧基，C 1-4烷基，羧基或烷氧基羰基，或者R 5和R 6与它们所连接的碳原子一起可以形成C3-7周期，Q表示CH或N，以及其制备方法和含有化合物（I）作为活性成分的药物组合物。

9. 发明授权

US5462935A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US5462935A
公开(公告)日：1995-10-31
申请号：US971986
申请日：1993-02-10
申请人： Yong Z. Kim , Hun S. Oh , Jae H. Yeo , Jong C. Lim , Chan S. Bang , Won S. Kim , Hyeon J. Yim
发明人： Yong Z. Kim , Hun S. Oh , Jae H. Yeo , Jong C. Lim , Chan S. Bang , Won S. Kim , Hyeon J. Yim
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/56 , C07D50/36
CPC分类号： C07D501/00
摘要： The present invention provides a cephalosporin compound represented by formulas (I-S) and (I-R) ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 cycloalkyl, amino optionally substituted with a C.sub.1-4 alkyl radical, phenyl, or 2-,4- or 6- substituted phenyl group with two or fewer substitutents chosen from C.sub.1-4 alkyl, C.sub.1-3 alkoxy, halogen and hydroxy radicals;R.sup.2 is hydrogen or a C.sub.1-4 alkyl group;R.sup.a and R.sup.b, which should be different from each other, are hydrogen or a C.sub.1-4 alkyl group; andQ is N or CH,and the pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates thereof, which possess potent and broad antibacterial activities. The invention also provides processes for preparing these compounds and to pharmaceutical compositions containing them as active ingredients.
摘要翻译：本发明提供由式（IS）和（1R）表示的头孢菌素化合物。其中：R1是C1-4烷基，C3-4链烯基，C3-4环烷基，氨基任选被C1-4烷基，苯基或2-，4-或6-取代的苯基取代，具有两个或更少个选自C 1-4烷基，C 1-3烷氧基，卤素和羟基的取代基; R2是氢或C1-4烷基; 应该彼此不同的R a和R b是氢或C 1-4烷基; 和Q是N或CH，以及其药学上可接受的无毒盐，生理上可水解的酯，水合物和溶剂合物，其具有有效和广泛的抗菌活性。本发明还提供了制备这些化合物的方法和含有它们作为活性成分的药物组合物。

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