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。

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。

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.

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。