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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:US5621095A
公开(公告)日:1997-04-15
申请号:US594764
申请日:1996-01-31
申请人: Jean-Fran.cedilla.ois Chantot , Solange Gouin d'Ambrieres , Daniel Humbert , Jean-Georges Teutsch
发明人: Jean-Fran.cedilla.ois Chantot , Solange Gouin d'Ambrieres , Daniel Humbert , Jean-Georges Teutsch
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 their non-toxic, pharmaceutically acceptable acid addition salts and having antibacterial activity and their preparation wherein the substituents are defined as in the specification.
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,其中其无毒的,药学上可接受的酸加成盐并具有抗菌活性及其制备,其中定义了取代基 如说明书中所述。
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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: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: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:US4294845A
公开(公告)日:1981-10-13
申请号:US34431
申请日:1979-04-30
IPC分类号: A61K31/335 , A61K31/357 , A61P3/04 , A61P9/00 , C07C39/367 , C07D319/08
CPC分类号: C07D319/08 , C07C39/367
摘要: Novel racemic mixtures or optically active isomers of 1,3-benzodioxins of the formula ##STR1## wherein R.sub.1 ' is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.4, aluminum, non-toxic, pharmaceutically acceptable amines, alkyl of 1 to 5 carbon atoms, 2,3-dihydroxypropanyl, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl and dialkylaminoalkyl with alkyls of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl and R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen and halogen, and the non-toxic, pharmaceutically acceptable acid addition salts where R.sub.1 ' is dialkylaminoalkyl, with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously having hypolipemic activity and their preparation.
摘要翻译: 下式的1,3-苯并二恶英的新型外消旋混合物或光学活性异构体其中R1'选自氢,碱金属,碱土金属,-NH4,铝,无毒,药学上可接受的 胺,1至5个碳原子的烷基,2,3-二羟基丙酰基,(2,2-二甲基-1,3-二氧戊环-4-基)甲基和具有1至4个碳原子的烷基的二烷基氨基烷基,R2选自 由氢和1至5个碳原子的烷基组成的组,R3选自氢,1至5个碳原子的烷基和苯基,R4和R5分别选自氢和卤素,和 无毒,药学上可接受的酸加成盐,其中R1'是二烷基氨基烷基,条件是R2和R3不同时具有降血脂活性及其制备。
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