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    Process for preparation of pyridine derivatives
    2.
    发明授权
    Process for preparation of pyridine derivatives 有权
    吡啶衍生物的制备方法

    公开(公告)号：US07288658B2

    公开(公告)日：2007-10-30

    申请号：US10888912

    申请日：2004-07-09

    申请人： Wolfgang Goehring ,  Peter John Harrington ,  Lewis M Hodges ,  David A Johnston ,  Goesta Rimmler

    发明人： Wolfgang Goehring ,  Peter John Harrington ,  Lewis M Hodges ,  David A Johnston ,  Goesta Rimmler

    IPC分类号： C07D401/02 ,  C07D213/02

    CPC分类号： C07D213/82 ,  C07D213/85

    摘要： The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/═O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

    摘要翻译： 本发明涉及制备下式化合物的方法，其中取代基如本文所述，其包括以下步骤：a）使式的化合物与式的化合物反应以形成式b的化合物：b）将OH / -O式XIV / XIVa化合物的功能通过选自POCl 3，PBr 3，MeI和（F 3）的离去基团的试剂转化成离去基团P， 其中P为卤素或三氟甲磺酸酯;其中P为卤素或三氟甲磺酸酯; c）通过使化合物XV与HR 2反应形成式的化合物，用R 2取代离去基团P，并且d）在选自以下的酸性介质中水解腈官能团 H 2 SO 4，HCl和乙酸，以形成式I的化合物。式I化合物是制备治疗活性化合物的有价值的中间体，其具有NK- 1拮抗剂活性。

    [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph
    5.
    发明授权
    [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph 有权
    [6,7-双（2-甲氧基 - 乙氧基） - 喹唑啉-4-基] - （3-乙炔基 - 苯基）胺盐酸盐多晶型

    公开(公告)号：US07148231B2

    公开(公告)日：2006-12-12

    申请号：US10771217

    申请日：2004-02-03

    申请人： Andre Gerard Bubendorf ,  Michael Hennig ,  Pirmin Hidber ,  Goesta Rimmler ,  Franziska Rohrer

    发明人： Andre Gerard Bubendorf ,  Michael Hennig ,  Pirmin Hidber ,  Goesta Rimmler ,  Franziska Rohrer

    IPC分类号： A61K31/505 ,  C07D239/04

    CPC分类号： A61K31/517 ,  C07D239/94

    摘要： The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.

    摘要翻译： 本发明涉及[6,7-双（2-甲氧基 - 乙氧基） - 喹唑啉-4-基] - （3-乙炔基 - 苯基）胺盐酸盐的新型多晶型物。 与先前已知的[6,7-双（2-甲氧基 - 乙氧基） - 喹唑啉-4-基] - （3-乙炔基 - 苯基）胺盐酸盐形式相比，该多晶型物显示出优异的性能。 [6,7-双（2-甲氧基 - 乙氧基） - 喹唑啉-4-基] - （3-乙炔基 - 苯基）胺盐酸盐是酪氨酸激酶的抑制剂，可用于治疗癌症。 还公开了制备和使用新型多晶型物的方法，以及含有新型多晶型物的药物组合物。

    Process for preparation of pyridine derivatives
    6.
    发明申请
    Process for preparation of pyridine derivatives 有权
    吡啶衍生物的制备方法

    公开(公告)号：US20050014792A1

    公开(公告)日：2005-01-20

    申请号：US10888912

    申请日：2004-07-09

    申请人： Wolfgang Goehring ,  Peter Harrington ,  Lewis Hodges ,  David Johnston ,  Goesta Rimmler

    发明人： Wolfgang Goehring ,  Peter Harrington ,  Lewis Hodges ,  David Johnston ,  Goesta Rimmler

    IPC分类号： C07D213/82 ,  C07D213/85 ,  A61K31/4545 ,  A61K31/4439 ,  C07

    CPC分类号： C07D213/82 ,  C07D213/85

    摘要： The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/═O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

    摘要翻译： 本发明涉及制备下式化合物的方法，其中取代基如本文所述，其包括以下步骤：a）使式的化合物与式的化合物反应以形成式b的化合物：b）将OH / =式XIV / XIVa化合物的O官能团与含有离去基团的试剂选自POCl 3，PBr 3，MeI和（F3CSO 2）2 O形成离子基团P，以形成下式的化合物其中P为卤素或三氟甲磺酸酯; c）通过使化合物XV与HR 2反应，将R 2取代离去基团P以形成式的化合物，和d）在选自H 2 SO 4，HCl和乙酸的酸性介质中水解腈官能团，形成 式I化合物式I化合物是制备具有NK-1拮抗剂活性的治疗活性化合物的有价值的中间体。