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    Quinoline derivatives, having in particular antiviral properties, preparation and biological applications thereof
    3.
    发明授权
    Quinoline derivatives, having in particular antiviral properties, preparation and biological applications thereof 失效
    喹啉衍生物，具有特别的抗病毒性质，其制备和生物应用

    公开(公告)号：US06670377B1

    公开(公告)日：2003-12-30

    申请号：US09402858

    申请日：2001-01-16

    申请人： Khalid Mekouar ,  Jean D'Angelo ,  Didier Desmaele ,  Jean-Francois Mouscadet ,  Frèdèric Subra ,  Christian Auclair

    发明人： Khalid Mekouar ,  Jean D'Angelo ,  Didier Desmaele ,  Jean-Francois Mouscadet ,  Frèdèric Subra ,  Christian Auclair

    IPC分类号： A61K3147

    CPC分类号： C07D215/26 ,  C07D215/14 ,  C07D215/48

    摘要： The invention concerns quinoline derivatives of formula (I) in which: Ra, Rb and Rc, identical or different represent one or several substituents, themselves identical or different, in any position on the cycles, this or these substituents being selected among a —(CH2)n—Y or —CH═CH—Y group, in which Y is halogen, —OH, —OR, —COH, —COR, —COOH, COOR, —COH, —COR, —CONH2, —CON(Rx, Ry)—CH═NOH, —CO— —CH═NOH, —NH2, —N(Rx, Ry), —NO2, —PO(OR)2—SH2, —SR, —SO2R, —SO2NHR, CN, or Z(Rc) in which R is a C1-C8 alkyl, or aryl or a heterocyclic compound, Rx and Ry, identical or different are C1-C5 alkyl, an aryl or heterocyclic compound and n is nil or a whole number between 1 and 5 Rb can further represent a hydrogen, and when Y is —COOH or —COOR in Rc, Z, if it represents an aryl, comprises at least 3 substituents or the quinoline ring is trisubstituted; X is an ethylene double bond; a —(CH2)n— group in which n is a whole number between 1 and 5: or a —CH(Rd—CH(Re) group, Rd and Re, identical or different, representing a hydrogen, a halogen, hydroxy or epoxy; or a —(CH2)n, —O—C—(CH2)m—, —(CH2)n, —C(O)—O—(CH2)m, —(CH2)n, —O—(CH2)m—, (CH2)n, —N(Q)—(CH2)m—, or (CH2)n, —S(O)—(CH2)m—, group, in which n=1 to 8, m=0 to 8, t=0, 1 or 2, and Q=h, aryl or alkyl. The invention also concerns the pharmaceutically acceptable salts of these derivatives, the diastereoisomeric and the enantiomeric forms thereof. The invention is useful as medicines with HIV anti-integrase inhibiting effect.

    摘要翻译： 本发明涉及式（I）的喹啉衍生物，其中：相同或不同的R a，R b和R c表示一个或几个取代基，它们在循环中的任何位置本身相同或不同，这些或这些取代基选自 - （ CH2）nY或-CH = CH-Y基，其中Y是卤素，-OH，-OR，-COH，-COR，-COOH，COOR，-COH，-COR，-CONH2，-CON（Rx，Ry ）-CH = NOH，-CO--CH = NOH，-NH2，-N（Rx，Ry），-NO2，-PO（OR）2-SH2，-SR，-SO2R，-SO2NHR，CN或Z （Rc）其中R为C1-C8烷基或芳基或杂环化合物，Rx和Ry相同或不同，为C1-C5烷基，芳基或杂环化合物，n为零或整数为1至5 如果R代表芳基，当Y是-COOH或-COOR时，R 3可以进一步代表氢，当代表芳基时，Z包含至少3个取代基或喹啉环是三取代的; X是乙烯双键; 其中n是1至5之间的整数的 - （CH 2）n - 基团或-CH（R d-CH（Re）基团，R d和R e相同或不同，表示氢，卤素，羟基或 环氧基或 - （CH 2）n，-OC-（CH 2）m - ， - （CH 2）n，-C（O）-O-（CH 2）m - ，（CH 2）n，-O- m - ，（CH2）n，-N（Q） - （CH2）m-或（CH2）n，-S（O） - （CH2）m-，其中n = 1至8，m = 0至8，t = 0,1或2，Q = h，芳基或烷基，本发明还涉及这些衍生物的药学上可接受的盐，其非对映异构体和对映体形式。本发明可用作具有HIV抗性的药物 - 内酯酶抑制作用。

    Rhenium complexes and their pharmaceutical use
    7.
    发明授权
    Rhenium complexes and their pharmaceutical use 有权
    铼配合物及其制药用途

    公开(公告)号：US08987491B2

    公开(公告)日：2015-03-24

    申请号：US13701191

    申请日：2011-06-01

    申请人： Philippe Collery ,  Jean D'Angelo ,  Georges Morgant

    发明人： Philippe Collery ,  Jean D'Angelo ,  Georges Morgant

    IPC分类号： C07F17/00 ,  A61K31/28 ,  A61K33/24 ,  A61K45/06 ,  C07F13/00

    CPC分类号： A61K31/28 ,  A61K33/24 ,  A61K45/06 ,  C07F13/00 ,  C07F13/005 ,  A61K2300/00

    摘要： The present invention is directed to a rhenium complex of general Formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is Se; Y is NH, O or S or is a methylene group; Z is halogen; m=0, 1, or 2 and p=0, 1, or 2, provided that m and p are both different from zero when Y is NH, O or S; n=3; R′ is a phenyl group or a group of general Formula —(CH2)q—COOH wherein q=1 or 2, a pharmaceutical composition comprising a therapeutically effective amount of at least one of such rhenium complex where X is additionally S or Te, a method for preparing said rhenium complex and a method for treating a proliferative growth related-disorder using a therapeutically effective amount of at least one of said rhenium complex where X is additionally S or Te. Also claimed is the use of compounds of formula (II) in the preparation of compounds of formula (I).

    摘要翻译： 本发明涉及通式（I）的铼络合物或其药学上可接受的盐或溶剂化物，其中X为Se; Y是NH，O或S，或是亚甲基; Z是卤素; m = 0,1或2，p = 0,1或2，条件是当Y是NH，O或S时，m和p都不同于0; n = 3; R'是苯基或其中q = 1或2的通式 - （CH 2）q -COOH的基团，药物组合物包含治疗有效量的至少一种这样的铼络合物，其中X另外是S或Te， 制备所述铼配合物的方法和使用治疗有效量的至少一种所述铼配合物治疗增殖性生长相关障碍的方法，其中X另外是S或Te。 还要求保护的是式（II）化合物在制备式（I）化合物中的用途。

    RHENIUM COMPLEXES AND THEIR PHARMACEUTICAL USE
    9.
    发明申请
    RHENIUM COMPLEXES AND THEIR PHARMACEUTICAL USE 有权
    铑复合物及其药物用途

    公开(公告)号：US20130158109A1

    公开(公告)日：2013-06-20

    申请号：US13701191

    申请日：2011-06-01

    申请人： Philippe Collery ,  Jean D'Angelo ,  Georges Morgant

    发明人： Philippe Collery ,  Jean D'Angelo ,  Georges Morgant

    IPC分类号： A61K31/28 ,  A61K45/06 ,  C07F13/00

    CPC分类号： A61K31/28 ,  A61K33/24 ,  A61K45/06 ,  C07F13/00 ,  C07F13/005 ,  A61K2300/00

    摘要： The present invention is directed to a rhenium complex of general Formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is Se; Y is NH, O or S or is a methylene group; Z is halogen; m=0, 1, or 2 and p=0, 1, or 2, provided that m and p are both different from zero when Y is NH, O or S; n=3; R′ is a phenyl group or a group of general Formula —(CH2)q—COOH wherein q=1 or 2, a pharmaceutical composition comprising a therapeutically effective amount of at least one of such rhenium complex where X is additionally S or Te, a method for preparing said rhenium complex and a method for treating a proliferative growth related-disorder using a therapeutically effective amount of at least one of said rhenium complex where X is additionally S or Te. Also claimed is the use of compounds of formula (II) in the preparation of compounds of formula (I).

    摘要翻译： 本发明涉及通式（I）的铼络合物或其药学上可接受的盐或溶剂化物，其中X为Se; Y是NH，O或S，或是亚甲基; Z是卤素; m = 0,1或2，p = 0,1或2，条件是当Y是NH，O或S时，m和p都不同于0; n = 3; R'是苯基或其中q = 1或2的通式 - （CH 2）q -COOH的基团，药物组合物包含治疗有效量的至少一种这样的铼络合物，其中X另外是S或Te， 制备所述铼配合物的方法和使用治疗有效量的至少一种所述铼配合物治疗增殖性生长相关障碍的方法，其中X另外是S或Te。 还要求保护的是式（II）化合物在制备式（I）化合物中的用途。