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    2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof
    2.
    发明授权
    2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof 失效
    2-苯甲酰基咪唑并吡啶衍生物，其制备和治疗用途

    公开(公告)号：US07902219B2

    公开(公告)日：2011-03-08

    申请号：US12336989

    申请日：2008-12-17

    申请人： Jean-Francois Peyronel ,  Youssef El-Ahmad

    发明人： Jean-Francois Peyronel ,  Youssef El-Ahmad

    IPC分类号： A61K31/437 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention is related to a compound of formula (I) wherein R1, R2, R3, R4 and X are as defined herein, or an acid-addition salt thereof, its preparation and therapeutic use in the treatment or prevention of diseases involving the Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.

    摘要翻译： 本发明涉及其中R 1，R 2，R 3，R 4和X如本文所定义的式（I）化合物或其酸加成盐，其在治疗或预防涉及 Nurr-1核受体，也称为NR4A2，NOT，TINUR，RNR-1和HZF3。

    Derivatives of perhydroisoindole and preparation thereof
    4.
    发明授权
    Derivatives of perhydroisoindole and preparation thereof 失效
    全氢异吲哚的衍生物及其制备

    公开(公告)号：US5508433A

    公开(公告)日：1996-04-16

    申请号：US146142

    申请日：1993-11-17

    申请人： Daniel Achard ,  Serge Grisoni ,  Stephen Hanessian ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Michel Tabart ,  Alain Truchon

    发明人： Daniel Achard ,  Serge Grisoni ,  Stephen Hanessian ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Michel Tabart ,  Alain Truchon

    IPC分类号： C07D209/44 ,  C07D209/48

    CPC分类号： C07D209/44

    摘要： This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R.sub.2 are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, R.sub.3 is a halogen atom or a hydroxy radical, R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.

    摘要翻译： PCT No.PCT / FR92 / 00430 Sec。 371日期：1993年11月17日 102（e）日期1993年11月17日PCT提交日期：1992年5月15日PCT公布。 出版物WO92 / 20654 本发明涉及式（I）的全氢异吲哚衍生物，其中基团R是氢原子或一起形成键，符号R2是可被卤素取代的苯基 原子或位置2或3中的甲基，R3是卤素原子或羟基，R4是H或卤素，如果R3是卤素，以其异构体形式或其混合物，以及它们存在时也可以是它们的盐，以及 的制备。 本发明的衍生物作为P物质拮抗剂是特别有意义的。

    3-vinyl-cephalosporins and their preparations
    5.
    发明授权
    3-vinyl-cephalosporins and their preparations 失效
    3-乙烯基头孢菌素及其制剂

    公开(公告)号：US4622393A

    公开(公告)日：1986-11-11

    申请号：US610175

    申请日：1984-05-14

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

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

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D253/07 ,  C07D501/24

    CPC分类号： C07D253/065 ,  C07D253/07

    摘要： New 3-vinylcephalosporins of the general formula (I), ##STR1## in which n=0 or 1, R.sub.1 is a radical of the general formula (II), ##STR2## in which R.sub.4 is hydrogen or a protective radical and R.sub.5 represents a radical of the general formula (IIa) ##STR3## in which R.sup.a.sub.5 and R.sup.b.sub.5 are hydrogen or alkyl or together form an alkylene radical and R.sup.c.sub.5 is hydrogen or a protective radical, R.sub.2 is hydrogen, a protective radical or a radical which can easily be removed by an enzymatic method, and R.sub.3 is a halogen atom or a radical R'.sub.3 SO.sub.2 O-- or R".sub.3 CO--O--, in which radicals R'.sub.3 and R".sub.3 are substituted or unsubstituted alkyl or phenyl radicals, or alternatively R.sub.1 is a hydrogen atom or a radical of the general formula (II) in which R.sub.4 is defined as above and R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl or a protective radical, and R.sub.2 is defined as above, or R.sub.1 is hydrogen or a variously substituted acyl radical and R.sub.2 is hydrogen or a protective radical, and R.sub.3 is a halogen atom.These new products are useful as intermediates for the preparation of antibiotic cephalosporins.

    摘要翻译： 通式（I）的新的3-乙酰头孢菌素，其中n = 0或1的其中R 1是通式（II）的基团，其中R 4是氢或 保护基，R 5表示通式（IIa）（IIa）的基团，其中Ra5和Rb5为氢或烷基或一起形成亚烷基，Rc5为氢或保护基，R2为氢， 保护基或可以通过酶法容易地除去的基团，R3是卤素原子或基团R'3SO2O-或R'3CO-O-，其中基团R'3和R'3被取代 或未取代的烷基或苯基，或者R 1是氢原子或通式（II）的基团，其中R 4如上定义，R 5是氢，烷基，乙烯基，氰基甲基或保护基，并且R 2被定义 如上所述，或R 1为氢或各种取代的酰基，R 2为氢或保护基，R 3为卤素原子。 这些新产品可用作制备抗生素头孢菌素的中间体。

    Cephalosporin derivatives
    6.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4503220A

    公开(公告)日：1985-03-05

    申请号：US408674

    申请日：1982-08-16

    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： C07D501/18 ,  C07F9/6561 ,  C07D501/14 ,  A61K31/545

    CPC分类号： C07F9/65613

    摘要： 3-Vinylcephalosporin derivatives of the formula: ##STR1## in which the symbols R.sub.1 are phenyl radicals or radicals --OZ.sub.1 (it being possible for Z.sub.1 to be alkyl, 2,2,2-trichloroethyl or optionally substituted phenyl or benzyl, or for the radicals Z.sub.1 to form an alkylene radical), R.sub.2 is a radical which can be removed by an enzymatic method, or a protecting radical, and R.sub.3 and R.sub.4 are optionally substituted alkyl, or phenyl, or together form a saturated 5-membered or 6-membered heterocyclic ring optionally containing another hetero-atom, are new, crystallizable intermediates useful for the preparation of anti-bacterial cephalosporins.

    摘要翻译： 其中符号R1是苯基或基团-OZ1（Z1可以是烷基，2,2,2-三氯乙基或任选取代的苯基或苄基）的下式的3-乙烯基头孢菌素衍生物： 或基团Z 1形成亚烷基），R 2为可通过酶法或保护基除去的基团，且R 3和R 4为任选取代的烷基或苯基，或一起形成饱和的5元环 或任选含有另一个杂原子的6元杂环是可用于制备抗菌头孢菌素的新的可结晶中间体。

    Cephalosporin derivatives, and pharmaceutical compositions containing them
    7.
    发明授权
    Cephalosporin derivatives, and pharmaceutical compositions containing them 失效
    头孢菌素衍生物和含有它们的药物组合物

    公开(公告)号：US4496560A

    公开(公告)日：1985-01-29

    申请号：US408676

    申请日：1982-08-16

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

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

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D501/20 ,  C07D501/24 ,  C07D505/00 ,  A61K31/545

    CPC分类号： C07D505/00

    摘要： New cephalosporin derivatives, of the formula: ##STR1## in which R.sub.1 is a heterocyclic, phenyl, p-hydroxyphenyl, phenoxy or dichlorophenylthio radical and R.sub.2 is a hydrogen atom, or R.sub.1 is phenyl or p-hydroxyphenyl and R.sub.2 is an amino radical, R.sub.3 is hydrogen, phenyl, substituted phenyl, alkylthio or substituted amino or a radical of the structure --A--R'.sub.3, which A is --CH.sub.2 --, --NH-- or --NHCO-- and R'.sub.3 is a substituted pyridinio radical, R is a carboxyl radical or a carboxylato radical if R.sub.3 is a --AR'.sub.3 radical and X is a sulphur or oxygen atom, the said alkyl moieties or radicals containing 1 to 4 carbon atoms each in their D, L and D,L forms, where these exist, and their salts are narrow-spectrum anti-bacterial agents which are active against gram-positive bacteria.

    摘要翻译： 新的头孢菌素衍生物，其结构式如下：其中R1是杂环，苯基，对羟基苯基，苯氧基或二氯苯硫基，R2是氢原子，或R1是苯基或对羟基苯基，R2是 氨基，R3是氢，苯基，取代的苯基，烷硫基或取代的氨基或结构-A-R'3的基团，其中A是-CH 2 - ， - NH-或-NHCO-，R'3是取代的 吡啶基，R为羧基或羧基，如果R3为-AR'3基，X为硫或氧原子，则所述烷基部分或含有1至4个碳原子的基团各自为D，L和D L形式，其中存在这些盐，其盐是对革兰氏阳性细菌具有活性的窄谱抗菌剂。

    Oxacephalosporins
    8.
    发明授权
    Oxacephalosporins 失效
    牛蒡子

    公开(公告)号：US4370478A

    公开(公告)日：1983-01-25

    申请号：US323112

    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: ##STR1## in which either R.sub.1 is hydrogen or a protective radical, R.sub.4 is hydrogen or substituted 2-(2-aminothiazol-4-yl)-acetyl or .alpha.-carboxyarylacetyl, of which the amine and acid groups are free or protected, and R" is hydrogen or methoxy in the 7.alpha.-position, or R.sub.1 is a protective radical, R.sub.4 is a radical which can easily be removed and R" is hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, and R.sub.2 is a radical --O SO.sub.2 --R.sub.3 or --O CO--R'.sub.3 (R.sub.3 and R'.sub.3 being substituted or unsubstituted alkyl radicals, or phenyl radicals) or a halogen atom, are useful as intermediates for the preparation of antimicrobial oxacephalosporins.

    摘要翻译： 新的通式为：其中R 1为氢或保护基的式（Ⅰ）的化合物，R4为氢或取代的2-（2-氨基噻唑-4-基） - 乙酰基或α-羧基芳基乙酰基，其中 胺和酸基是游离的或被保护的，并且R“在7α-位中是氢或甲氧基，或者R1是保护基，R4是可以容易地除去的基团，R”是氢或甲氧基， 7个α位或7位β-中的氢，R2是-O-SO 2 -R 3或-OCO-R'3（R3和R'3是取代或未取代的烷基或苯基）或 卤素原子，可用作制备抗微生物头孢菌素的中间体。

    Oxacephalosporins
    9.
    发明授权
    Oxacephalosporins 失效
    牛蒡子

    公开(公告)号：US4369314A

    公开(公告)日：1983-01-18

    申请号：US322951

    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 oxacephalosporin derivative of the general formula: ##STR1## in which R.sub.1 is a protective radical, R.sub.2 is either a radical of the general formula: ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an .alpha.-carboxyarylacetyl radical and R" is hydrogen or methoxy in the 7.alpha.-position, or alternatively R.sub.2 is a protective radical and R" is either hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, and R.sub.3 and R.sub.4 are optionally substituted alkyl, or phenyl, or form a heterocyclic ring with the nitrogen atom, their E and Z forms and mixtures thereof and also their preparation.These new products are useful as intermediates for the preparation of biologically active oxacephalosporins.

    摘要翻译： （I）其中R1是保护基团的新的类似于以下通式的式（II）的新的类鞘氨醇衍生物：R2是以下通式的基团：其中R 5是氢，烷基，乙烯基，保护基 羧基烷基或保护基，R 6为保护基]或α-羧基芳基乙酰基，R“为7位上的氢或甲氧基，或者R2为保护基，R”为氢或甲氧基 7个β-位中的7个α-位或氢，R3和R4是任选取代的烷基或苯基，或与氮原子，它们的E和Z形式及其混合物形成杂环，以及它们的制备。 这些新产品可用作制备生物活性的羟基头孢菌素的中间体。