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公开(公告)号:US5378697A
公开(公告)日:1995-01-03
申请号:US903610
申请日:1992-06-24
IPC分类号: A61K31/54 , A61P31/04 , C07D501/24 , C07D507/00 , C07D513/04 , C07D519/00
CPC分类号: C07D513/04
摘要: The syn isomer of a compound of the formula ##STR1## in the R or S form or a mixture of R and S forms and their non-toxic, pharmaceutically acceptable acid addition salts wherein the substituents are defined as in the specification having antibacterial activity and their preparation.
摘要翻译: 具有R或S形式的式I化合物的顺式异构体或R和S形式的混合物及其无毒的药学上可接受的酸加成盐,其中取代基如本说明书中具有抗菌活性 和他们的准备。
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公开(公告)号:US06313305B1
公开(公告)日:2001-11-06
申请号:US08900366
申请日:1997-07-21
申请人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin d'Ambrieres , Daniel Humbert , Christophe Dini
发明人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin d'Ambrieres , Daniel Humbert , Christophe Dini
IPC分类号: C07D28508
CPC分类号: C07D501/00 , C07C45/63 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , Y02P20/55
摘要: A compound having the formula selected from the group consisting of wherein either R3p and R4p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R2p is selected from the group consisting of —CN, —F, Br and I and R1p and R5p are hydrogen or R5p is —F and R1p and R2p are hydrogen or R1p and R2p are F and R5p is hydrogen, or R4p and R5p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R3p is selected from the group consisting of F and —CN and R1p and R2p are hydrogen, R8 is hydrogen or an amine protective group and R10 is the remainder in which the hydroxy or amino are protected wherein R′1 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, —CN, carboxy and alkoxy carbonyl of 1 to 4 carbon atoms.
摘要翻译: 具有选自R3p和R4p中的式的化合物是相同的,并且选自-OH,被保护的-OH和1至8个碳原子的酰氧基,R2p选自-CN, -F,Br和I,R1p和R5p是氢或R5p是-F,R1p和R2p是氢或R1p,R2p是F,R5p是氢,或R4p和R5p是相同的,选自-OH, 保护的-OH和1至8个碳原子的酰氧基,R3p选自F和-CN,R1p和R2p是氢,R8是氢或胺保护基,R10是其中羟基或氨基 被保护,其中R'1选自1至4个碳原子的烷基,-CN,羧基和1至4个碳原子的烷氧基羰基。
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公开(公告)号:US5763617A
公开(公告)日:1998-06-09
申请号:US769488
申请日:1996-12-18
申请人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
发明人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
IPC分类号: C07C45/63 , C07C45/67 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07D277/40 , C07D277/46 , C07D285/08 , C07D409/12 , C07D417/12 , C07D501/00 , C07D501/24
CPC分类号: C07D501/00 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07C45/63 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , Y02P20/55
摘要: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an integral salt or their salts with organic or mineral acids wherein the substituents are as defined in the application and having antibacterial properties.
摘要翻译: (R)或(S)中的顺式异构体以(R)或(S)形式或(R,S)形式的式(I)异构体的化合物或其混合物形式或其混合物, 混合物,其形式为整体盐或其与有机或无机酸的盐,其中取代基如本申请中所定义并具有抗菌性质。
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公开(公告)号:US5712266A
公开(公告)日:1998-01-27
申请号:US453923
申请日:1995-05-30
申请人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
发明人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
IPC分类号: C07C45/63 , C07C45/67 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07D277/40 , C07D277/46 , C07D285/08 , C07D409/12 , C07D417/12 , C07D501/00 , C07D501/24
CPC分类号: C07D501/00 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07C45/63 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , Y02P20/55
摘要: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are defined as in the application having anti-bacterial properties.
摘要翻译: (R)或(S)中的顺式异构体以(R)或(S)形式或(R,S)形式的式(I)异构体的化合物或其混合物形式或其混合物, 混合物,以内盐的形式或其与有机或无机酸的盐形式,其中取代基如本申请中所定义,具有抗细菌性质。
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公开(公告)号:US5728828A
公开(公告)日:1998-03-17
申请号:US453990
申请日:1995-05-30
申请人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
发明人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
IPC分类号: C07C45/63 , C07C45/67 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07D277/40 , C07D277/46 , C07D285/08 , C07D409/12 , C07D417/12 , C07D501/00 , C07D501/24
CPC分类号: C07D501/00 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07C45/63 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , Y02P20/55
摘要: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are as set forth below.
摘要翻译: (R)或(S)中的顺式异构体以(R)或(S)形式或(R,S)形式的式(I)异构体的化合物或其混合物形式或其混合物, 混合物,以内盐的形式或其与有机或无机酸的盐形式,其中取代基如下所述。
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公开(公告)号:US5883248A
公开(公告)日:1999-03-16
申请号:US903460
申请日:1997-07-30
申请人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
发明人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert , Christophe Dini
IPC分类号: C07C45/63 , C07C45/67 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07D277/40 , C07D277/46 , C07D285/08 , C07D409/12 , C07D417/12 , C07D501/00 , C07D501/24
CPC分类号: C07D501/00 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07C45/63 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , Y02P20/55
摘要: Novel intermediates of the formula ##STR1## wherein the substituents are defined in the specification.
摘要翻译: 式中的取代基在本说明书中定义的新颖的中间体
+ TR + TR 。 -
公开(公告)号:US5455238A
公开(公告)日:1995-10-03
申请号:US989235
申请日:1992-12-11
申请人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert
发明人: Jozsef Aszodi , Jean-Francois Chantot , Patrick Fauveau , Solange Gouin D'Ambrieres , Daniel Humbert
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07C45/63 , C07C45/67 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/48 , C07C59/64 , C07C69/734 , C07C205/44 , C07C229/40 , C07C239/08 , C07C239/20 , C07C255/56 , C07C255/57 , C07C291/02 , C07C311/27 , C07C311/35 , C07C323/52 , C07C323/56 , C07D277/20 , C07D277/40 , C07D277/42 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/24 , C07D501/46 , C07D501/56 , C07D519/06
CPC分类号: C07D501/00 , C07C205/44 , C07C239/20 , C07C255/56 , C07C255/57 , C07C45/63 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07C59/64 , C07C69/734 , Y02P20/55
摘要: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## in the form of an internal salt or a non-toxic, pharmaceutically acceptable acid addition salt wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are individually defined in the specification, R.sub.4 is --OH or alkoxy of 1 to 8 carbon atoms, A and A' are individually selected from the group consisting of hydrogen, an equivalent of an alkali metal or alkaline earth metal, magnesium, ammonium and an organic amine, or one or two of --COOA or --COOA' ARE --CO.sub.2 --, the wavy line means --CH.sub.2 R.sub.6 can be in the E or Z position, R.sub.6 in the quaternary ammonium form is selected from the group consisting of ##STR2## X is defined as in the specification with the proviso that when R.sub.3 is --OH or alkoxy of 1 to 8 carbon atoms, at least one R.sub.1, R.sub.2 and R.sub.5 is other than hydrogen having antibacterial properties.
摘要翻译: (R)或(S)中的顺式异构体以内盐或无毒的药学上可接受的酸加成盐的形式或其混合物形式,其中R1,R2,R3 R 5为-OH或碳原子数为1〜8的烷氧基,A和A'分别选自氢,当量碱金属或碱土金属,镁,铵 和有机胺,或-COO&上拉和A或-COO&上升和A'ARE-CO 2 - 中的一种或两种,波浪线表示-CH 2 R 6可以在E或Z位,季铵形式的R6选自 组成的组
X如本说明书中所定义,条件是当R3为-OH或1至8个碳原子的烷氧基时,至少有一个R1,R2和 R5不是具有抗菌性的氢。 -
公开(公告)号:US5538963A
公开(公告)日:1996-07-23
申请号:US313745
申请日:1994-09-27
IPC分类号: A61K31/54 , A61P31/04 , C07D501/24 , C07D507/00 , C07D513/04 , C07D519/00
CPC分类号: C07D513/04
摘要: The syn isomer of a compound of the formula ##STR1## in the R or S form or a mixture of R and S forms wherein selected from the group consisting of ##STR2## and their non-toxic, pharmaceutically acceptable acid addition salts wherein the substituents are defined as in the specification having antibacterial activity and their preparation.
摘要翻译: 具有R或S形式的式I化合物的顺式异构体或R和S形式的混合物,其选自由下列组成的组及其无毒的药学上可接受的酸加成物 盐,其中取代基如本说明书中所定义,具有抗菌活性及其制备。
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公开(公告)号:US5936083A
公开(公告)日:1999-08-10
申请号:US625910
申请日:1996-04-01
IPC分类号: C07D501/00 , C07D501/22 , C07D501/24 , C07D501/56
CPC分类号: C07D501/00
摘要: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R us selected from the group consisting of ##STR2## R and R' are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, CO.sub.2 --Q, ##STR3## CH.sub.2 --SQ, Q and Q' are individually hydrogen or alkyl of 1 to 4 carbon atoms, P, P' and P" are individually alkyl of 1 to 4 carbon atoms optionally substituted by one of the substituents R and R' the dotted line indicating that P and P' can optionally form with the nitrogen atom to which they are linked a heterocycle with 5 or 6 links, R.sub.b and R.sub.c are individually selected from the group consisting of an equivalent of an alkali metal, an alkaline earth metal, magnesium, ammonium and an amine organic base or A and A' are the remainder of an easily cleavable ester group or CO.sub.2 A is CO.sub.2 --and the wavy line indicates that CH.sub.2 R.sub.1 is in the E or Z position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.
摘要翻译: 选自R或S形式的式的化合物的顺式异构体或R,S混合物形式的化合物,其中R us选自R和R'的化合物分别选自 由氢,1-4个碳原子的烷基,1-4个碳原子的烷氧基,卤素,CO2-Q,CH2-SQ,Q和Q'分别是氢或1-4个碳原子的烷基,P, P'和P“分别是1至4个碳原子的烷基,任选被一个取代基R和R'取代,虚线表示P和P'可以任选地与它们连接的氮原子一起形成杂环与 5或6链,Rb和Rc分别选自碱金属,碱土金属,镁,铵和胺有机碱的当量,A和A'是易裂解酯基的剩余部分 或CO 2 A是CO 2 - 而波浪线表示CH 2 R 1在E或Z位置a 它们具有抗菌活性的无毒的,药学上可接受的酸加成盐。
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公开(公告)号:US5416080A
公开(公告)日:1995-05-16
申请号:US80572
申请日:1993-06-21
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D417/14 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/24 , C07D501/36 , C07D501/46 , C07D501/56
CPC分类号: C07D501/00 , Y02P20/55
摘要: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein the substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.
摘要翻译: 选自由R或S形式的式I的化合物的顺式异构体或R,S混合物形式的化合物的化合物,其中取代基如说明书中所定义, 具有抗菌活性的有毒的,药学上可接受的酸加成盐。
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