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    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    55.
    发明授权
    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
    醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法

    公开(公告)号：US06841562B2

    公开(公告)日：2005-01-11

    申请号：US10659095

    申请日：2003-09-10

    申请人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： A61P31/04 ,  C07D211/60 ,  C07D401/06 ,  C07D409/14 ,  A61K31/44 ,  C07D215/12 ,  C07D215/18

    CPC分类号： C07D401/06 ,  C07D211/60 ,  C07D409/14 ,  Y02P20/55

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中R 1a是氢，卤素，羟基，氨基，烷基氨基，二烷基氨基，羟基氨基，烷氧基氨基或烷基烷氧基氨基，R 1b是氢，或者R 1a和R 1b形成氧代，R 2是羧基，羧甲基或羟甲基， 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基，或与任选被卤素或三氟甲基取代的环烷硫基（3至7个成员）或与杂芳硫基（ 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基或R3是被苯基或杂芳基取代的炔丙基，被苯基或杂芳基取代 R4是烷基，烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基，其各种异构体形式，分别或混合物，和 它们的盐，它们的制备方法和中间体以及含有它们的组合物。 这些新型衍生物是有效的抗菌剂。

    Process for the preparation of 4, 10 beta- diacetoxy-2 alpha-benzoyloxy-5 beta, 20-epoxy-1, 13 alpha-dihydroxy-9-oxo-19-norcyclopropa [g] tax-11-ene
    56.
    发明申请
    Process for the preparation of 4, 10 beta- diacetoxy-2 alpha-benzoyloxy-5 beta, 20-epoxy-1, 13 alpha-dihydroxy-9-oxo-19-norcyclopropa [g] tax-11-ene 失效
    制备4,10β-二乙酰氧基-2α-苯甲酰氧基-5β，20-环氧-1,13α-二羟基-9-氧代-19-降胆[g] tax-11-烯的方法

    公开(公告)号：US20040248969A1

    公开(公告)日：2004-12-09

    申请号：US10824030

    申请日：2004-04-14

    申请人： Aventis Pharma S.A.

    发明人： Eric Didier ,  Guy Amouret

    IPC分类号： A61K031/337 ,  C07D35/14

    CPC分类号： C07D305/14

    摘要： There is disclosed a process for the preparation of 4 -acetoxy-2null-benzoyloxy-5null,20-epoxy-1,13null-dihydroxy-9 -oxo-19-norcyclopropanullgnull tax-11-ene from 4-acetoxy-2null-benzoyloxy-5null,20-epoxy-1,13null-dihydroxy-9-oxo-7null-(trifluoromethyl sulfonyloxy) tax-11-ene by reaction with a molecular sieve in sulfolane.

    摘要翻译： 公开了一种从4-乙酰氧基-2α制备4-乙酰氧基-2α-苯甲酰氧基-5β，20-环氧-1,13α-二羟基-9-氧代-19-降胆固醇[g] tax-11-烯的方法 苯并氧基-5βa，20-环氧-1,13α-二羟基-9-氧代-7a-（三氟甲基磺酰氧基）tax-11-烯与分子筛在环丁砜中反应。

    Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors
    57.
    发明申请
    Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors 审中-公开
    新型吲哚衍生物，作为药物和药物组合物的制备，特别是作为KDR抑制剂

    公开(公告)号：US20040242559A1

    公开(公告)日：2004-12-02

    申请号：US10830826

    申请日：2004-04-23

    申请人： Aventis Pharma S.A.

    发明人： Antonio Ugolini ,  Herve Bouchard

    IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/416 ,  C07D43/14

    CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D405/14

    摘要： The invention relates to compounds of formula (I): 1 in which R1 represents pyrazolyl or indazolyl, R2 and R3 especially represent H, halogen, hydroxyl, nitro, cyano, R4, nullOR4, nullCOR4, nullOC(nullO)R4, nullC(nullO)OR4, nullC(nullO)OH, nullN(R5)C(nullO)R4, nullN(R5)C(nullO)OR4, nullS(O)nR4, nullS(O)nOR4, nullN(R5)SO2R4, nullNY1Y2, nullC(nullO)NY1Y2, nullN(R5)C(nullO)NY1Y2, nullS(O)nNY1Y2 and nullOC(nullO)NY1Y2, R4 especially represents alkyl, alkenyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl, R5 especially represents H, alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, Y1 and Y2 especially represent H, alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylcarboxyl, heteroaryl and heteroarylcarboxy, which are optionally substituted, or Y1 and Y2 form with N an amino ring, n represents 0 to 2, all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products, especially as KDR inhibitors.

    摘要翻译： 本发明涉及式（I）化合物：其中R1表示吡唑基或吲唑基，R2和R3特别表示H，卤素，羟基，硝基，氰基，R4，-OR4，-COR4，-OC（= O）R4， -C（= O）OR 4，-C（= O）OH，-N（R 5）C（= O）R 4，-N（R 5）C（= O）OR 4，-S（O）n R 4， O）nOR 4，-N（R 5）SO 2 R 4，-NY 1 Y 2，-C（= O）NY 1 Y 2，-N（R 5）C（= O）NY 1 Y 2，-S（O）n NY 1 Y 2和-OC（= O） 尤其代表烷基，烯基，环烷基，芳基，杂芳基和杂环烷基，R 5尤其代表H，烷基，烯基，环烷基，杂环烷基，芳基和杂芳基，Y 1和Y 2特别表示H，烷基，烯基，环烷基，杂环烷基，芳基，芳基羧基， 杂芳基和杂芳基羧基，其任选被取代，或Y 1和Y 2与N一个氨基环形成，n表示0至2，所有这些基团任选被取代，这些产物是所有异构形式和盐，作为药用产品，特别是 作为KDR抑制剂。