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    PROCESS FOR PREPARING CYCLOALKYL-SUBSTITUTED PIPERAZINE COMPOUNDS
    1.
    发明申请
    PROCESS FOR PREPARING CYCLOALKYL-SUBSTITUTED PIPERAZINE COMPOUNDS 审中-公开
    制备环丙基取代的哌嗪化合物的方法

    公开(公告)号：US20110301350A1

    公开(公告)日：2011-12-08

    申请号：US13058658

    申请日：2009-02-13

    申请人： Waldemar Pfrengle ,  Markus Frank ,  Thorsten Pachur ,  Guenther Huchler

    发明人： Waldemar Pfrengle ,  Markus Frank ,  Thorsten Pachur ,  Guenther Huchler

    IPC分类号： C07D295/135 ,  C07D295/155

    CPC分类号： C07D295/14

    摘要： The present invention relates to a process for preparing compounds of general formula I wherein m, n, o, R1, R2 and R3 are defined as mentioned hereinafter, the enantiomers thereof and the diastereomers thereof, which are particularly suitable for preparing compounds of general formula II wherein m, o, R1, R2, R3 and R4 are defined as mentioned hereinafter. The compounds of general formula II have B1-antagonistic properties.

    摘要翻译： 本发明涉及一种制备通式I化合物的方法，其中m，n，o，R 1，R 2和R 3如下文所定义，其对映体和非对映体特别适用于制备通式 其中m，o，R 1，R 2，R 3和R 4如下文所述定义。 通式II的化合物具有B1拮抗性质。

    Process for the stereoselective preparation of bicyclic heterocycles
    5.
    发明授权
    Process for the stereoselective preparation of bicyclic heterocycles 有权
    双环杂环立体选择性制备方法

    公开(公告)号：US08263768B2

    公开(公告)日：2012-09-11

    申请号：US13057871

    申请日：2009-07-23

    申请人： Markus Ostermeier ,  Stefan Braith ,  Juergen Daeubler ,  Guenther Huchler ,  Waldemar Pfrengle

    发明人： Markus Ostermeier ,  Stefan Braith ,  Juergen Daeubler ,  Guenther Huchler ,  Waldemar Pfrengle

    IPC分类号： C07D239/72 ,  C07D241/00

    CPC分类号： C07D241/08 ,  C07D471/20

    摘要： The present invention relates to a process for the stereoselective preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.

    摘要翻译： 本发明涉及具有有价值的药理学特性，特别是对信号的抑制作用的通式（I）化合物及其盐特别是其生理上可接受的盐与无机或有机酸和碱的立体选择性制备方法。 由酪氨酸激酶介导的转导，其用于治疗疾病，特别是肿瘤疾病以及良性前列腺增生（BPH），肺和气道疾病的用途。

    Process for the preparation of chiral 8-(-3-aminopiperidin-1-yl) xanthines
    10.
    发明授权
    Process for the preparation of chiral 8-(-3-aminopiperidin-1-yl) xanthines 有权
    手性8-（ - 3-氨基哌啶-1-基）黄嘌呤的制备方法

    公开(公告)号：US07820815B2

    公开(公告)日：2010-10-26

    申请号：US11267235

    申请日：2005-11-04

    申请人： Waldemar Pfrengle ,  Thorsten Pachur ,  Thomas Nicola ,  Adil Duran

    发明人： Waldemar Pfrengle ,  Thorsten Pachur ,  Thomas Nicola ,  Adil Duran

    IPC分类号： C07D473/06 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07B2200/07 ,  C07D473/04 ,  C07D473/06

    摘要： The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof where X is a leaving group selected from halogens and sulphonic ester acid residues, and R1 to R3 are as defined herein, to obtain a compound of the formula (II) and deprotecting the obtained compound of the formula (II) to obtain the product xanthines.

    摘要翻译： 本发明涉及制备对映体纯的8-（3-氨基哌啶-1-基） - 黄嘌呤的改进方法。 该方法包括使式（III）的化合物与3-（苯二甲酰亚氨基）哌啶或其对映异构体反应，其中X是选自卤素和磺酸酯酸残基的离去基团，并且R 1至R 3如本文所定义，以获得 式（II）的化合物和所得到的式（II）的化合物脱保护，得到产物黄嘌呤。