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    Process for the synthesis of CXCR4 antagonist
    1.
    发明授权
    Process for the synthesis of CXCR4 antagonist 有权
    合成CXCR4拮抗剂的方法

    公开(公告)号：US07332605B2

    公开(公告)日：2008-02-19

    申请号：US11077896

    申请日：2005-03-11

    申请人： Jason B. Crawford ,  Gang Chen ,  David Gauthier ,  Renato Skerlj ,  Ian R. Baird ,  Trevor R. Wilson

    发明人： Jason B. Crawford ,  Gang Chen ,  David Gauthier ,  Renato Skerlj ,  Ian R. Baird ,  Trevor R. Wilson

    IPC分类号： C07D215/38

    CPC分类号： C07D401/14 ,  C07D215/40 ,  C07D401/12 ,  Y02P20/55

    摘要： This invention relates to a process for synthesizing heterocyclic pharmaceutical compound which binds to the CXCR4 chemokine receptor. In one embodiment, the process comprises: a) reacting a 5,6,7,8-tetrahydroquinolinylamine and an alkyl aldehyde bearing a phthalimide or a di-tertiary-butoxycarbonyl (di-BOC) protecting group to form an imine; b) reducing the imine to form a secondary amine; c) reacting the secondary amine with a haloalkyl substituted heterocyclic compound, to form a phthalimido-protected or di-tert-butoxycarbonyl protected tertiary amine; and d) hydrolyzing the protected amine to obtain a compound having Formula I′

    摘要翻译： 本发明涉及一种结合CXCR4趋化因子受体的杂环药物化合物的合成方法。 在一个实施方案中，该方法包括：a）使5,6,7,8-四氢喹啉基胺和带有邻苯二甲酰亚胺或二叔丁氧基羰基（二-BOC）保护基团的烷基醛反应以形成亚胺; b）还原亚胺以形成仲胺; c）使仲胺与卤代烷基取代的杂环化合物反应，形成邻苯二甲酰亚氨基保护或二叔丁氧羰基保护的叔胺; 和d）水解受保护的胺以获得具有式I'

    Chemokine receptor binding heterocyclic compounds
    3.
    发明授权
    Chemokine receptor binding heterocyclic compounds 失效
    趋化因子受体结合杂环化合物

    公开(公告)号：US06750348B1

    公开(公告)日：2004-06-15

    申请号：US09535314

    申请日：2000-03-24

    申请人： Gary Bridger ,  Renato Skerlj ,  Al Kaller ,  Curtis Harwig ,  David Bogucki ,  Trevor R. Wilson ,  Jason Crawford ,  Ernest J. McEachern ,  Bem Atsma ,  Siqiao Nan ,  Yuanxi Zhou ,  Dominique Schols

    发明人： Gary Bridger ,  Renato Skerlj ,  Al Kaller ,  Curtis Harwig ,  David Bogucki ,  Trevor R. Wilson ,  Jason Crawford ,  Ernest J. McEachern ,  Bem Atsma ,  Siqiao Nan ,  Yuanxi Zhou ,  Dominique Schols

    IPC分类号： C07D21516

    CPC分类号： C07D239/42 ,  A61K45/06 ,  C07D213/38 ,  C07D215/40 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04

    摘要： This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines. The present invention provides a compound of Formula I wherein, W is a nitrogen atom and Y is absent or, W is a carbon atom and Y═H; R1 to R7 may be the same or different and are independently selected from hydrogen or straight, branched or cyclic C1-6 alkyl; R8 is a substituted heterocyclic group or a substituted aromatic group Ar is an aromatic or heteroaromatic ring each optionally substituted at single or multiple, non-linking positions with electron-donating or withdrawing groups; n and n′ are independently, 0-2; X is a group of the formula: Wherein, Ring A is an optionally substituted, saturated or unsaturated 5 or 6-membered ring, and P is an optionally substituted carbon atom, an optionally substituted nitrogen atom, sulfur or oxygen atom. Ring B is an optionally substituted 5 to 7-membered ring. Ring A and Ring B in the above formula can be connected to the group W from any position via the group V, wherein V is a chemical bond, a (CH2)n″ group (where n″=0-2) or a C═O group. Z is, (1) a hydrogen atom, (2) an optionally substituted C1-6 alkyl group, (3) a C0-6 alkyl group substituted with an optionally substituted aromatic or heterocyclic group, (4) an optionally substituted C0-6 alkylamino or C3-7 cycloalkylamino group, (5) an optionally substituted carbonyl group or sulfonyl. These compounds further include any pharmaceutically acceptable acid addition salts and metal complexes thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof.

    摘要翻译： 本发明涉及结合趋化因子受体的新一类杂环化合物，从而抑制其天然配体的结合。 这些化合物通过结合趋化因子受体（包括CXCR4和CCR5）导致HIV感染的保护作用，从而抑制随后与这些趋化因子的结合。 本发明提供式I化合物，其中W是氮原子，Y不存在，或W是碳原子，Y = H; R 1至R 7可以相同或不同并且独立地选自 来自氢或直链，支链或环状的C 1-6烷基; R 8是取代的杂环基或取代的芳族基团Ar是芳族或杂芳族环，其各自任选在单个或多个非连接位置被取代，具有给电子或 取代基; n和n'独立地是0-2; X是下式的基团：其中环A是任选取代的饱和或不饱和的5或6元环，并且P是任选取代的碳原子， 任选取代的氮原子，硫或氧原子。 环B是任选取代的5至7元环。 上述式中的环A和环B可以通过组V从任何位置连接到基团W，其中V是化学键，（CH2）n“基团（其中n”= 0-2）或 一个C = O组。 Z为（1）氢原子，（2）任选取代的C 1-6烷基，（3）被任意取代的芳族或杂环基团取代的C 0-6烷基，（4）任选取代的C 0-6 烷基氨基或C 3-7环烷基氨基，（5）任选取代的羰基或磺酰基。 这些化合物还包括其任何药学上可接受的酸加成盐和金属络合物以及其立体异构体形式及其立体异构形式的混合物。