公开(公告)号：US06468995B1

公开(公告)日：2002-10-22

申请号：US08781924

申请日：1996-12-30

申请人： Kohji Kawabata ,  Takeshi Terasawa ,  Ayako Ohki ,  Fumiyuki Shirai ,  Hirofumi Yamamoto

发明人： Kohji Kawabata ,  Takeshi Terasawa ,  Ayako Ohki ,  Fumiyuki Shirai ,  Hirofumi Yamamoto

IPC分类号： C07D50134

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of the formula: wherein R1 is amino or protected amino; R2 is hydrogen, lower alkyl or hydroxy protective group; R3 is carboxy or protected carboxy; R4 is an unsubstituted 5, 6 or 7-membered heteromonocyclic group containing two nitrogen atoms as heteroatoms, and which optionally further contains one oxygen or sulfur atom; or R4 is said 5, 6 or 7-membered heteromonocyclic group substituted by 1 to 4 groups selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, cyclo(lower)alkyl, cyclo(lower)alkenyl, halogen, amino, protected amino, protected hydroxy, cyano, nitro, carboxy, hydroxy(lower)alkyl, amino(lower)alkyl, and carbamoyloxy; and n is 1 or 2.

摘要翻译： 下式的化合物：其中R 1是氨基或被保护的氨基; R 2是氢，低级烷基或羟基保护基; R 3是羧基或被保护的羧基; R 4是未取代的5,6或7元杂单环基， 杂原子，并且任选地还含有一个氧或硫原子; 或R4是由1-4个选自低级烷基，低级烷氧基，低级烷硫基，低级烷基氨基，环（低级）烷基，环（低级）烯基，卤素 ，氨基，保护的氨基，保护的羟基，氰基，硝基，羧基，羟基（低级）烷基，氨基（低级）烷基和氨基甲酰氧基; andn是1或2。

公开(公告)号：US6159961A

公开(公告)日：2000-12-12

申请号：US356684

申请日：1999-07-19

申请人： Kohji Kawabata ,  Hirofumi Yamamoto ,  Yoshiteru Eikyu ,  Shinya Okuda ,  Hisashi Takasugi

发明人： Kohji Kawabata ,  Hirofumi Yamamoto ,  Yoshiteru Eikyu ,  Shinya Okuda ,  Hisashi Takasugi

IPC分类号： C07D501/04 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/22 ,  C07D501/24 ,  C07D501/36 ,  C07D501/56 ,  C07D501/59 ,  A61L31/546

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is hydrogen or hydroxy protective group,R.sup.3 is carboxy or protected carboxy,R.sup.4 is hydrogen, lower alkenyl, acyloxy(lower)alkenyl, optionally substituted heterocyclic(lower)alkenyl, optionally substituted heterocyclic(lower)alkenylthio, optionally substituted heterocyclic(lower)alkylthio, or optionally substituted heterocyclic-thio(lower)alkylthio andR5 is halogen or lower alkyland pharmaceutically acceptable salts thereof, which is useful as a medicament for prophylactic and therapeutic treatment of infectious diseases.

摘要翻译： 下式的化合物：其中R1是氨基或被保护的氨基，R2是氢或羟基保护基，R3是羧基或保护的羧基，R4是氢，低级烯基，酰氧基（低级）烯基，任选取代的杂环（低级）烯基， 任选取代的杂环（低级）烯硫基，任选取代的杂环（低级）烷硫基，或任选取代的杂环硫代（低级）烷硫基，R 5为卤素或低级烷基及其可药用盐，其可用作预防和治疗性治疗药物 的传染病。

公开(公告)号：US5958914A

公开(公告)日：1999-09-28

申请号：US43578

申请日：1998-03-26

申请人： Kohji Kawabata ,  Hirofumi Yamamoto ,  Yoshiteru Eikyu ,  Shinya Okuda ,  Hisashi Takasugi

发明人： Kohji Kawabata ,  Hirofumi Yamamoto ,  Yoshiteru Eikyu ,  Shinya Okuda ,  Hisashi Takasugi

IPC分类号： C07D501/04 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/22 ,  C07D501/24 ,  C07D501/36 ,  C07D501/56 ,  C07D501/59

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino, R.sup.2 is hydrogen,R.sup.3 is carboxy,R.sup.4 is heterocyclic(lower)alkylthio wherein said heterocyclic group is pyrazolyl and said lower alkyl group is methyl, andR.sup.5 is halogen; and pharmaceutically acceptable salts thereof.

摘要翻译： PCT No.PCT / JP96 / 02797第 371日期：1998年3月26日 102（e）1998年3月26日PCT PCT 1996年9月27日PCT公布。 公开号WO97 / 12890 日期：1997年4月10日一种下式化合物：其中R1是氨基，R2是氢，R3是羧基，R4是杂环（低级）烷硫基，其中所述杂环基是吡唑基，所说的低级烷基是甲基，R5是卤素; 及其药学上可接受的盐。

公开(公告)号：US5594132A

公开(公告)日：1997-01-14

申请号：US684194

申请日：1991-04-12

申请人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanaka ,  Kohji Kawabata

发明人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanaka ,  Kohji Kawabata

IPC分类号： C07D501/32 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D209/48 ,  C07D213/75 ,  C07D239/42 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/12 ,  C07D501/18 ,  C07D501/22 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D209/48 ,  C07D213/75 ,  C07D239/42 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D277/587 ,  C07D285/08 ,  C07D417/12

摘要： A compound of the formula: ##STR1## in which R.sup.2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl,R.sup.3 is carboxy or a protected carboxy group,A.sup.5 is lower alkylene which may have a group of the formula: .dbd.N.about.OR.sup.6, wherein R.sup.6 is hydrogen, lower alkenyl, lower alkynyl, lower alkyl or lower alkyl substituted by one or more substituent (s) selected from carboxy, a protected carboxy group, amino, a protected amino group and a heterocyclic group, andX.sup.1 is halogen,or a salt thereof.

摘要翻译： 下式的化合物，其中R 2是低级烷氧基甲基，低级烷硫基甲基或低级链烯硫基甲基，R 3是羧基或受保护的羧基，A5是可以具有下列基团的低级亚烷基：= N DIFFERENCE OR 6，其中 R6是氢，低级烯基，低级炔基，被一个或多个选自羧基，保护的羧基，氨基，保护的氨基和杂环基的取代基取代的低级烷基或低级烷基，X 1是卤素，或 其盐。

公开(公告)号：US5252731A

公开(公告)日：1993-10-12

申请号：US831504

申请日：1992-02-05

申请人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanaka ,  Kohji Kawabata

发明人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanaka ,  Kohji Kawabata

IPC分类号： C07D209/48 ,  C07D213/75 ,  C07D239/42 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/12 ,  C07D501/18 ,  C07D501/22 ,  C07D501/24

CPC分类号： C07D209/48 ,  C07D213/75 ,  C07D239/42 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D277/587 ,  C07D285/08 ,  C07D417/12

摘要： Intermediates of the following formula are disclosed: ##STR1## wherein R.sup.1 is aryl; R.sup.2 is carboxy or protected carboxy; Z.dbd.CH.dbd.CH.sub.2, CH.sub.2 --X.sup.2, --CH.sub.2 --P.sup.+ (R.sup.7).sub.3 .X.sup.3 or CH .dbd.P(R.sup.7).sub.3 wherein X.sup.2 and X.sup.3 are each halogen and R.sup.7 is aryl.The compounds are useful as intermediates for cephalosporins.

摘要翻译： 公开了下式的中间体：其中R 1是芳基; R2是羧基或被保护的羧基; Z = CH = CH 2，CH 2 -X 2，-CH 2 -P +（R 7）3 .X 3或CH = P（R 7）3，其中X 2和X 3各自为卤素且R 7为芳基。 这些化合物可用作头孢菌素的中间体。

公开(公告)号：US5215982A

公开(公告)日：1993-06-01

申请号：US604632

申请日：1990-10-26

申请人： Kazuo Sakane ,  Kohji Kawabata ,  Yoshiko Inamoto

发明人： Kazuo Sakane ,  Kohji Kawabata ,  Yoshiko Inamoto

IPC分类号： C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D501/00 ,  C07D501/46

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： Cephem compounds of the following formula are disclosed: ##STR1## wherein R.sup.1 is amino or protected amino group. R.sup.2 is H or an organic group,R.sup.3 is H or an organic group,R.sup.4 is H, lower alkyl, carboxy, protected carboxy, amino, protected amino or carbamoyl, Z=N or CH. The compounds are useful as antimicrobial agents.

公开(公告)号：US5187160A

公开(公告)日：1993-02-16

申请号：US483646

申请日：1990-02-23

申请人： Kazuo Sakane ,  Kohji Kawabata ,  Kenzi Miyai ,  Yoshiko Inamoto

发明人： Kazuo Sakane ,  Kohji Kawabata ,  Kenzi Miyai ,  Yoshiko Inamoto

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/46

CPC分类号： C07D501/46

摘要： The invention relates to antimicrobial compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino, R.sup.2 is ethyl, propyl or lower alkenyl,R.sup.3 is COO .theta., carboxy or a protected carboxy,R.sup.4 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.5 is amino or a protected amino,X.sup..theta. is an anion, andn is 0 or 1,or,R.sup.1, R.sup.3, R.sup.5, X.sup..theta. and n are each as defined above,R.sup.2 is lower alkyl, andR.sup.4 is 3-hydroxypropyl, with proviso that(i) when R.sup.3 is COO.sup..theta., then n is 0, and(ii) when R.sup.3 is carboxy or a protected carboxy, then n is 1,or a pharmaceutically acceptable salt thereof.

公开(公告)号：US4985555A

公开(公告)日：1991-01-15

申请号：US385542

申请日：1989-07-27

申请人： Takao Takaya ,  Zenzaburo Tozuka ,  Nobuyoshi Yasuda ,  Kohji Kawabata

发明人： Takao Takaya ,  Zenzaburo Tozuka ,  Nobuyoshi Yasuda ,  Kohji Kawabata

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D213/32 ,  C07D501/18 ,  C07D501/22 ,  C07D501/59

CPC分类号： C07D213/32

摘要： The invention relates to a cephem compound of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino, R.sup.2 is hydrogen, phenyl, pyridyl which may have a lower alkyl group, or cyano, and R.sup.3 is carboxy or protected carboxy, or a salt thereof.

公开(公告)号：US4952578A

公开(公告)日：1990-08-28

申请号：US241419

申请日：1988-09-07

申请人： Kazuo Sakane ,  Kohji Kawabata ,  Kenzi Miyai ,  Yoshiko Inamoto

发明人： Kazuo Sakane ,  Kohji Kawabata ,  Kenzi Miyai ,  Yoshiko Inamoto

IPC分类号： C07D501/04 ,  A61K31/54 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/06 ,  C07D501/38 ,  C07D501/46 ,  C07D501/56 ,  C07F7/10

CPC分类号： C07D501/46

摘要： The object of the invention is a new cephem compound with antimicrobial activity used for the treatment of infectious diseases of the general formula: ##STR1## wherein R1 is amino or a protected aminoR2 is lower alkyl which may have 1 to 3 halogensR3 is COO.sup..crclbar., carboxy or a protected carboxyR4 is hydroxy(lower)alkyl or protected hydroxy(lower)alkylR5 is amino or a protected aminoR6 is hydrogen or lower alkylX.sup..crclbar. is an anion, andn is 0 or 1with proviso that(i) when R3 is COO.sup..crclbar., then n is 0, and(ii) when R3 is carboxy or a protected carboxy, then n is 1,and pharmaceutically acceptable salt thereof.

公开(公告)号：US4487927A

公开(公告)日：1984-12-11

申请号：US341621

申请日：1982-01-22

申请人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanaka ,  Kohji Kawabata

发明人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanaka ,  Kohji Kawabata

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D209/48 ,  C07D213/75 ,  C07D239/42 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/12 ,  C07D501/06 ,  C07D501/18 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/36 ,  C07F9/6561

CPC分类号： C07D209/48 ,  C07D213/75 ,  C07D239/42 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D277/587 ,  C07D285/08 ,  C07D417/12

摘要： This invention relates to novel 7-acylamino-3-vinylcephalosporanic acid derivatives of high antimicrobial activity, to processes for preparation thereof from novel intermediates, and to said intermediates of the formula: ##STR1## in which R.sub.A is a group of the formula: ##STR2## wherein R.sup.1 is amino-substituted-heterocyclic group which may have halogen, protected amino-substituted-heterocyclic group which may have halogen, or a group of the formula: ##STR3## wherein R.sup.3 is lower alkyl,R.sup.8 is aryl,A is lower alkylene which may have a substituent selected from the group consisting of amino, a protected amino group, hydroxy, oxo and a group of the formula:.dbd.N.about.OR.sup.4,whereinR.sup.4 is hydrogen, cyclo(lower)alkenyl, lower alkynyl, lower alkenyl, lower alkenyl substituted by carboxy or a protected carboxy group, lower alkyl, or lower alkyl substituted by one or more substituent(s) selected from carboxy, a protected carboxy group, amino, a protected amino group, cyano, phosphono, a protected phosphono group and a heterocyclic group which may have suitable substituent(s),R.sup.a is a protected amino group,R.sup.b is a protected carboxy group,R.sub.B is a group of the formula:--CH.sub.2 --X.sup.2, --CH.sub.2 P.sup..sym. (R.sup.7).sub.3 .multidot.X.sup.3.crclbar. or --CH.dbd.P(R.sup.7).sub.3whereinR.sup.7 is aryl, and X.sup.2 and X.sup.3 are each halogen, andR.sup.2 is carboxy or a protected carboxy group, provided that, when R.sub.A is a group of the formula:R.sup.8 --CH.dbd.N--, wherein R.sup.8 is as defined above, then R.sub.B is a group of the formula:--CH.sub.2 P.sup..sym. (R.sup.7).sub.3 .multidot.X.sup.3.crclbar. or --CH.dbd.P(R.sup.7).sub.3,whereinR.sup.7 and X.sup.3 are each as defined above, or a salt thereof.