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49 条记录 (耗时 0.026 秒)

    Perhydroisoindole derivatives and preparation
    2.
    发明授权
    Perhydroisoindole derivatives and preparation 失效
    全氢异吲哚衍生物及其制备方法

    公开(公告)号：US5463077A

    公开(公告)日：1995-10-31

    申请号：US313120

    申请日：1994-10-11

    申请人： Daniel Achard ,  Serge Grisoni ,  Jean-Luc Malleron ,  Jean-Francois Peyronel ,  Michel Tabart

    发明人： Daniel Achard ,  Serge Grisoni ,  Jean-Luc Malleron ,  Jean-Francois Peyronel ,  Michel Tabart

    IPC分类号： C07D209/44 ,  C07D403/06 ,  C07D409/06 ,  C07D209/04

    CPC分类号： C07D403/06 ,  C07D209/44 ,  C07D409/06 ,  Y02P20/55

    摘要： This ivention relates to novel perhydroisoindole derivatives having formula (I), ##STR1## wherein the symbols R, which are the same or different, are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical, R' is a phenyl radical optionally 2-substituted by a C.sub.1-2 alkylk or alkyloxy radical, R" is a fluorine atom or a hydroxy radical, and R'" is a hydrogen atom, or else R' and R'" are hydroxy radicals, or R" and R'" together form a bond, and R.sup.o is a hydrogen atom or a protective radical; salts thereof whereever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.

    摘要翻译： PCT No.PCT / FR93 / 00351 Sec。 371日期：1994年10月11日 102（e）日期1994年10月11日PCT提交1993年4月8日PCT公布。 出版物WO93 / 21154 日本公开日1993年10月28日。本说明书涉及具有式（I），其中符号R相同或不同的式（I）的新型全氢异吲哚衍生物是任选被2-或3-取代的苯基 卤素原子或甲基，R'是任选被C 1-2烷基或烷氧基取代的苯基，R“是氟原子或羟基，R”'是氢原子，或 其中R'和R“'是羟基，或者R”和R“'一起形成键，而Ro是氢原子或保护基; 其盐适用; 及其制备。 这些产品是用于制备具有P物质拮抗剂活性的衍生物的合成中间体。

    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them
    4.
    发明授权
    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them 失效

    公开(公告)号：US5021420A

    公开(公告)日：1991-06-04

    申请号：US375934

    申请日：1989-07-06

    申请人： Marie-Iherese Comte ,  Claude Gueremy ,  Jean-Luc Malleron ,  Serge Mignani ,  Jean-Francois Peyronel ,  Alain Truchon

    发明人： Marie-Iherese Comte ,  Claude Gueremy ,  Jean-Luc Malleron ,  Serge Mignani ,  Jean-Francois Peyronel ,  Alain Truchon

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P43/00 ,  C07D275/06 ,  C07D417/00 ,  C07D417/06 ,  C07D417/14 ,  C07D513/06

    CPC分类号： C07D275/06 ,  C07D417/06 ,  C07D417/14 ,  C07D513/06

    摘要： This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

    3-(1-Halo-2-oxoethyl)cephalosporin intermediates
    5.
    发明授权
    3-(1-Halo-2-oxoethyl)cephalosporin intermediates 失效
    3-（1-卤代-2-氧代乙基）头孢菌素中间体

    公开(公告)号：US4554350A

    公开(公告)日：1985-11-19

    申请号：US522261

    申请日：1983-08-11

    申请人： Pierre Le Roy ,  Daniel Farge ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    发明人： Pierre Le Roy ,  Daniel Farge ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/24

    CPC分类号： C07D501/24

    摘要： New cephalosporin derivatives of the formula: ##STR1## in which R is an amino-protecting radical, R' is a protected carboxyl radical, Hal is a halogen atom, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or R.sub.a is a protected carboxyl radical and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms, or C.sub.1 -C.sub.4 alkyl radicals, or together form a C.sub.2 -C.sub.5 alkylene radical, and n=0 or 1, their isomeric forms and mixtures thereof, are useful for the preparation of cephalosporins which have antibacterial properties.

    摘要翻译： 下式的新型头孢菌素衍生物：其中R为氨基保护基，R'为被保护的羧基，Hal为卤素原子，Ra，Rb和Rc为氢原子，或Ra为被保护的羧基 和相同或不同的R b和R c是氢原子或C 1 -C 4烷基，或一起形成C 2 -C 5亚烷基，n = 0或1，它们的异构形式及其混合物可用于 制备具有抗菌性能的头孢菌素。

    Cephalosporin derivatives, their preparation and compositions containing them
    6.
    发明授权
    Cephalosporin derivatives, their preparation and compositions containing them 失效
    头孢菌素衍生物，它们的制备和含有它们的组合物

    公开(公告)号：US4508717A

    公开(公告)日：1985-04-02

    申请号：US522359

    申请日：1983-08-11

    申请人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    发明人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    IPC分类号： C07D501/20 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/24 ,  C07D501/36

    CPC分类号： C07D501/00

    摘要： Cephalosporin derivatives of the formula: ##STR1## in which A is a single bond or a radical --CH.sub.2 --, --NH-- or --NHCO--, attached to the 3-position or 4-position of the pyridinio radical, R is a methyl, carboxymethyl, carbamoylmethyl, benzyl or allyl radical, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or alternatively R.sub.a is carboxyl and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms or alkyl radicals, or together form an alkylene radical, and n equals 0 or 1, in their syn form, and also their addition salts with acids, metal salts and addition salts with nitrogen-containing bases are antibacterial agents having a broad spectrum of activity.

    摘要翻译： 下式的头孢菌素衍生物：其中A是单键或者连接到吡啶基的3-位或4-位的基团-CH 2 - ， - NH-或-NHCO-，R 是甲基，羧甲基，氨基甲酰基甲基，苄基或烯丙基，Ra，Rb和Rc是氢原子，或者Ra是羧基，Rb和Rc相同或不同，是氢原子或烷基，或一起形成亚烷基 自由基，n等于0或1，并且它们与酸，金属盐和与含氮碱的加成盐的加成盐也是具有广谱活性的抗菌剂。

    3-Formylmethyl-cephalosporins
    7.
    发明授权
    3-Formylmethyl-cephalosporins 失效
    3-甲酰甲基头孢菌素

    公开(公告)号：US4415735A

    公开(公告)日：1983-11-15

    申请号：US322963

    申请日：1981-11-19

    申请人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel

    IPC分类号： C07D501/14 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/20 ,  C07D501/24 ,  C07D501/26 ,  C07D501/60

    CPC分类号： C07D501/24

    摘要： The invention provides new cephalosporins of the general formula: ##STR1## in which n=0 or 1, R.sub.4 is an amine-protecting radical, R.sup.a.sub.5 and R.sup.b.sub.5, which are identical or different, are hydrogen atoms or alkyl radicals, or form an alkylene radical of 2 or 3 carbon atoms, R.sup.c.sub.5 is a hydrogen atom or an acid-protecting radical and R.sub.2 is an acid-protecting radical or a radical which can easily be removed by an enzymatic method. The compounds of formula (I) are in the form of a 3-oxoethyl-bicyclooct-2-ene or -bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane if n=0, and in the form of a 3-oxoethylbicyclooct-2-ene or a 3-oxoethylidenebicyclooctane if n=1. They are useful as intermediates for the preparation of pharmaceutically active cephalosporins.

    摘要翻译： 本发明提供了新的头孢菌素，其通式如下：其中n = 0或1，R4是胺保护基，Ra5和Rb5相同或不同，为氢原子或烷基，或 形成2或3个碳原子的亚烷基，Rc5是氢原子或酸保护基，R2是酸保护基或可以通过酶法容易地除去的基团。 如果n = 0，式（I）化合物是3-氧代乙基 - 双环辛烯-2-烯或二环辛烯-3-烯或3-氧代亚乙基双环辛烷的形式，并且为3-氧代乙基双环辛-2 如果n = 1，则为3-烯亚乙基双环辛烷。 它们可用作制备药学活性头孢菌素的中间体。

    Oxacephalosporins and anti-bacterial composition containing same
    8.
    发明授权
    Oxacephalosporins and anti-bacterial composition containing same 失效
    含有类孢菌素和抗菌组合物

    公开(公告)号：US4399135A

    公开(公告)日：1983-08-16

    申请号：US322962

    申请日：1981-11-19

    申请人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D501/24 ,  C07D505/00 ,  C07D498/04

    CPC分类号： C07D505/00

    摘要： New oxacephalosporins of the general formula (I), in which R is optionally N-oxidised pyridyl, pyrimidin-2-yl, substituted pyridazin-3-yl, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 4-position, substituted 1-alkyl-1,3,4-triazol-5-yl or 1,2,4-triazol-5-yl, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 1-position, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 2-position, substituted or unsubstituted 2-alkyl-2,5-dihydro-5-oxo-1,2,4-triazin-3-yl, 1-amino-1,2-dihydro-2-oxo-pyrimidin-4-yl, substituted 1,3,4-thiadiazol-5-yl or tetrazol-5-yl substituted in the 1-position, R' is a substituted 2-(2-aminothiazol-4-yl)-acetyl radical or an .alpha.-carboxyarylacetyl radical and R" is a hydrogen atom or a methoxy radical in the 7.alpha.-position, and also their salts, their preparation and the medicaments in which they are present. ##STR1##

    摘要翻译： 通式（I）的新型硫代氨基甲酸酯，其中R为任选的N-氧化吡啶基，嘧啶-2-基，取代的哒嗪-3-基，5,6-二氧代-1,4,5,6-四氢-1 在4-取代的1-烷基-1,3,4-三唑-5-基或1,2,4-三唑-5-基中取代的2,4-三嗪-3-基， 在1-位上取代的二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，5,6-二氧代-1,4,5,6-四氢-1,2， 2-取代或未取代的2-烷基-2,5-二氢-5-氧代-1,2,4-三嗪-3-基，1-氨基-1,2 - 二氢-2-氧代 - 嘧啶-4-基，在1-位取代的取代的1,3,4-噻二唑-5-基或四唑-5-基是取代的2-（2-氨基噻唑-5-基） 4-基） - 乙酰基或α-羧基芳基乙酰基，R“是7α-位中的氢原子或甲氧基，以及它们的盐，它们的制备方法及其存在的药物。 （一）

    Oxacephalosporins
    9.
    发明授权
    Oxacephalosporins 失效
    牛蒡子

    公开(公告)号：US4369315A

    公开(公告)日：1983-01-18

    申请号：US323113

    申请日：1981-11-19

    申请人： Daniel Farge ,  Pierre Le Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre Le Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D501/24 ,  C07D505/00 ,  C07D498/04

    CPC分类号： C07D505/00

    摘要： New oxacephalosporins of the general formula ##STR1## in which R.sub.1 is a protective radical and (a) R.sub.4 is a substituted 2-(2-aminothiazol-4-yl)-acetyl radical of which the amine group is protected, or an .alpha.-carboxyarylacetyl radical, and R" is hydrogen or methoxy in the 7.alpha.-position, or alternatively(b) R.sub.4 is a protective radical and R" is hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, in the form of a bicyclooct-2-ene or bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane, are useful as intermediates for the preparation of pharmaceutically active oxacephalosporins.

    摘要翻译： 其中R 1为保护基的通式为（IMA）（Ⅰ）的新型硫代吗啡，（a）R4为被保护的胺基的取代的2-（2-氨基噻唑-4-基） - 乙酰基，或 一个α-羧基芳基乙酰基，R“是7个α-位的氢或甲氧基，或者（b）R4是保护基，R”是7位中的氢或甲氧基或7位中的氢 以双环-2-烯或双环辛烯-3-烯或3-氧代亚乙基双环辛烷的形式的β-位可用作制备药学活性的硫氰酸头孢菌素的中间体。