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公开(公告)号:US5663163A
公开(公告)日:1997-09-02
申请号:US591261
申请日:1996-01-22
申请人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
发明人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
IPC分类号: C07D501/00 , C07D501/46 , A61K31/545
CPC分类号: C07D501/46 , C07D501/00
摘要: The present invention relates to new cephem compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same and anti-bacterial methods of using the same. The subject cephem compounds comprise a thiadiazine ring bonded to the cephem through an iminoacetamido chain and a pyarzolium ring bonded to the cephem through a methylene chain.
摘要翻译: 本发明涉及新的头孢烯化合物,其药学上可接受的盐,包含与其相同的抗菌方法的药物组合物。 本发明的头孢烯化合物包含通过亚氨基乙酰氨基链和通过亚甲基链键合到头孢烯上的吡哆醛环与头孢烯结合的噻二嗪环。
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公开(公告)号:US5401734A
公开(公告)日:1995-03-28
申请号:US63982
申请日:1993-05-20
申请人: Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
发明人: Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
IPC分类号: A61K31/545 , C07D501/18 , C07D501/36 , C07D501/46
CPC分类号: C07D501/46
摘要: Cephem compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,Z is N or CH,R.sup.2 is lower alkyl, mono(or di or tri)halo(lower)alkyl, lower alkenyl, lower alkynyl, phenyl, naphthyl, phenyl(lower)alkyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl,A is lower alkylene, andR.sup.5 is hydroxy or a protected hydroxy group; or pharmaceutically acceptable salts thereof show antimicrobial activities and are useful in the treatment of microbial infections.
摘要翻译: 下式化合物:其中R 1为氨基或被保护的氨基,Z为N或CH,R 2为低级烷基,单(或二或三)卤代(低级)烷基,低级烯基,低级炔基,苯基 ,萘基,苯基(低级)烷基,羧基(低级)烷基或保护的羧基(低级)烷基,R是下式的基团:其中R 3和R 4各自为低级烷基,A为低级亚烷基, R5是羟基或被保护的羟基; 或其药学上可接受的盐显示抗微生物活性,并且可用于治疗微生物感染。
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公开(公告)号:US5173485A
公开(公告)日:1992-12-22
申请号:US714995
申请日:1991-06-14
申请人: Kazuo Sakane , Kohji Kawabata , Yoshiko Inamoto
发明人: Kazuo Sakane , Kohji Kawabata , Yoshiko Inamoto
IPC分类号: C07D519/00 , C07D519/06
CPC分类号: C07D519/00
摘要: The invention relates to an antimicrobial compound of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is lower alkyl, lower alkenyl, carboxy (lower) alkyl or protected carboxy(lower)alkyl,R.sup.3 is hydrogen, lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl, protected amino(lower)alkyl or lower alkanoyl,R.sup.4 is hydrogen, lower alkyl or lower alkylthio, andZ is N or CHor a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及下式的抗微生物化合物:其中R1是氨基或被保护的氨基,R2是低级烷基,低级烯基,羧基(低级)烷基或被保护的羧基(低级)烷基, R3是氢,低级烷基,羟基(低级)烷基,保护的羟基(低级)烷基,氨基(低级)烷基,被保护的氨基(低级)烷基或低级烷酰基,R4是氢,低级烷基或低级烷硫基,Z是N 或CH或其药学上可接受的盐。
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公开(公告)号:US5162520A
公开(公告)日:1992-11-10
申请号:US826062
申请日:1992-01-27
申请人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
发明人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
IPC分类号: A61K31/425 , C07D501/18 , C07D501/38 , C07D501/46
CPC分类号: C07D501/46
摘要: The invention relates to intermediate compounds of the formula: ##STR1## wherein R.sup.3 is a lower alkyl, hydroxy(lower)alkyl or a protected hydroxy(lower)alkyl,R.sup.4 is amino or a protected amino group, andR.sup.5 is hydrogen or lower alkyl, or a salt thereof,useful in the preparation of compounds of antimicrobial activity.
摘要翻译: 本发明涉及下式的中间体化合物:其中R3是低级烷基,羟基(低级)烷基或被保护的羟基(低级)烷基,R4是氨基或被保护的氨基,R5是氢或低级烷基 ,或其盐,其可用于制备抗微生物活性化合物。
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公开(公告)号:US5109130A
公开(公告)日:1992-04-28
申请号:US658866
申请日:1991-02-22
申请人: Kazuo Sakane , Kohji Kawabata , Shinya Okuda
发明人: Kazuo Sakane , Kohji Kawabata , Shinya Okuda
IPC分类号: C07D501/00 , C07D501/46
CPC分类号: C07D501/00
摘要: The invention relates to a highly stable antibacterial agent which is crystalline 7.beta.-[2-(5 -amino-1,2,4-thiadiazol-3-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[3-amino-2-(2-hydroxyethyl)-1-pyrazolio]methyl-3-cephem-4-carboxylate hydrochloride (syn-isomer).
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公开(公告)号:US4960766A
公开(公告)日:1990-10-02
申请号:US930427
申请日:1986-11-14
申请人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
发明人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D231/12 , C07D277/28 , C07D501/00 , C07D501/18 , C07D501/36 , C07D501/40 , C07D501/46 , C07D501/56
CPC分类号: C07D501/46 , Y02P20/55
摘要: The invention relates to cephem compounds characterized by a substituted 2-pyrazoliomethyl group and a 7-(aminothiazolyl)(alkoxyimino)-acetamido group and certain derivatives thereof, to pharmaceutical compositions comprising the same and to use for treatment of infections diseases.
摘要翻译: 本发明涉及特征为取代的2-吡唑基甲基和7-(氨基噻唑基)(烷氧基亚氨基) - 乙酰胺基及其某些衍生物的头孢烯化合物,其包含该化合物并用于治疗感染性疾病。
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公开(公告)号:US4927818A
公开(公告)日:1990-05-22
申请号:US90345
申请日:1987-08-28
申请人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
发明人: Takao Takaya , Kazuo Sakane , Kenzi Miyai , Kohji Kawabata
IPC分类号: A61K31/545 , A61K31/425 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/18 , C07D501/38 , C07D501/46 , C07D501/56
CPC分类号: C07D501/46 , Y02P20/55
摘要: 7 .beta.-[2-5 amino-1, 2, 4 thiadiazol-3yl) 2(carboxy lower alkyleneoxyimino) acetamido]-3-(3-amino-2-alkyl-1-pyrazolio) methyl 3 cephem 4 carboxylates are prepared. They are antibiotics.
摘要翻译: 7β-[2-5氨基-1,2,4-噻二唑-3-基] 2(羧基低级亚烷氧基亚氨基)乙酰氨基] -3-(3-氨基-2-烷基-1-吡唑啉基)甲基3头孢烯4羧酸酯。 他们是抗生素。
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公开(公告)号:US4772682A
公开(公告)日:1988-09-20
申请号:US944229
申请日:1986-12-22
申请人: Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人: Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号: C07F9/6539 , C07D285/08 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/36 , C07D501/46 , C07F9/6561 , A61K31/545
CPC分类号: C07D285/08 , C07F9/65613
摘要: The invention relates to intermediates useful in the preparation of antimicrobial compounds, the intermediates being of the formula: ##STR1## wherein R.sup.A is --SCN or --S.sup..sym. (R.sup.3).sub.2, whereinR.sup.3 is lower alkyl, andR.sup.B is carboxy or --COO.sup..crclbar.,or a salt thereof, with the proviso that when R.sup.A is --SCN, then R.sup.B is carboxy and that when R.sup.A is --S.sup..sym. (R.sup.3).sub.2, then R.sup.B is --COO.sup..sym..
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公开(公告)号:US4654422A
公开(公告)日:1987-03-31
申请号:US785712
申请日:1985-10-09
申请人: Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人: Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号: C07F9/6539 , C07D285/08 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/36 , C07D501/46 , C07F9/6561 , C07F9/65
CPC分类号: C07D285/08 , C07F9/65613
摘要: The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is phosphono, dihalophosphoryl, di(lower) alkoxyphosphoryl, O-lower alkylphosphono, diaminophosphoryl, (amino) (hydroxy) phosphoryl or (lower alkoxy) (morpholino) phosphoryl,R.sup.2 is lower alkyl or lower alkenyl,R.sup.3 is a group of the formula: ##STR2## wherein X is hydrogen, halogen or lower alkoxy, or a group of the formula: ##STR3## wherein R.sup.4 is lower alkyl, and Y is N or CH; and pharmaceutically acceptable salts thereof.
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20.
公开(公告)号:US4567275A
公开(公告)日:1986-01-28
申请号:US619981
申请日:1984-06-12
申请人: Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人: Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号: C07C17/26 , C07D209/48 , C07D257/04 , C07D285/08 , C07D295/21 , C07D501/20
CPC分类号: C07D209/48 , C07C17/26 , C07C17/263 , C07D257/04 , C07D285/08 , C07D295/21
摘要: The cephalosporin intermediate 2-(5-amino-1,2,4, thiadiazol-3yl)glyoxylic acid has been prepared.
摘要翻译: 已经制备了头孢菌素中间体2-(5-氨基-1,2,4-噻二唑-3-基)乙醛酸。
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