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    AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
    24.
    发明申请
    AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS 审中-公开

    公开(公告)号：WO2009114512A1

    公开(公告)日：2009-09-17

    申请号：PCT/US2009/036635

    申请日：2009-03-10

    Applicant: INCYTE CORPORATION ,  RODGERS, James, D. ,  SHEPARD, Stacey ,  LI, Yun-Long ,  ZHOU, Jiacheng ,  LIU, Pingli ,  MELONI, David ,  XIA, Michael

    Inventor： RODGERS, James, D. ,  SHEPARD, Stacey ,  LI, Yun-Long ,  ZHOU, Jiacheng ,  LIU, Pingli ,  MELONI, David ,  XIA, Michael

    IPC: C07D487/04 ,  A61K31/437 ,  A61P35/00

    CPC classification number: C07D487/04 ,  B60Q3/76 ,  B60Q3/80 ,  Y10S362/80 ,  Y10S362/802

    Abstract: The method includes the steps of performing in-vitro liver, intestinal and/or expressed enzyme assays with selected ethnobotanical substances, for both humans and a variety of animal species, to produce an array of resulting chemical entities, such as metabolites, for the human and the animals. Comparisons are then made between the chemical entities from the human in-vitro studies and the animal in-vitro studies to determine the closest match. The animal with the closest match is then used for an in-vivo study. If a match is present between the animal in-vivo results and the human in-vitro results, the matched chemical entity is isolated or synthesized and then further tested to determine the suitability of the matched chemical entity as a treatment drug.

    Abstract translation: 该方法包括以下步骤：对人和各种动物物种进行用选定的人造植物物质进行体外肝，肠和/或表达的酶测定，以产生所得化学物质的阵列，例如代谢物 和动物。 然后在人类体外研究的化学实体和动物体外研究之间进行比较，以确定最接近的匹配。 然后将最接近匹配的动物用于体内研究。 如果在动物体内结果与人体外结果之间存在匹配，则匹配的化学实体被分离或合成，然后进一步测试以确定匹配的化学实体作为治疗药物的适合性。

    NOVEL STEROID 5 a -REDUCTASE
    26.
    发明申请
    NOVEL STEROID 5 a -REDUCTASE 审中-公开

    公开(公告)号：WO2006122214A3

    公开(公告)日：2007-12-27

    申请号：PCT/US2006018147

    申请日：2006-05-10

    Applicant: HEALTH RESEARCH INC ,  UNIV NORTH CAROLINA ,  MOHLER JAMES L ,  TITUS MARK ,  KOZYREVA OLGA ,  FORD O'HARRIS III ,  KAWINSKI ELSBIETA ,  LI YUN

    Inventor： MOHLER JAMES L ,  TITUS MARK ,  KOZYREVA OLGA ,  FORD O'HARRIS III ,  KAWINSKI ELSBIETA ,  LI YUN

    IPC: C12N9/02

    CPC classification number: C12Q1/26 ,  C07K2319/21 ,  C07K2319/40 ,  C12N9/001 ,  C12N2799/022 ,  G01N33/57434

    Abstract: The invention provides an isolated, novel steroid 5a-reductase enzyme termed SRD5AIIL The protein has an estimated molecular weight of 37 kDa and is capable of converting testosterone to dihydrotestosterone at a pH of about 7.0. Also provided is a method for identifying inhibitors of SRD5 AIII by contacting SRD5 AIII with a test compound and measuring the activity of the enzyme. A reduced activity relative to a control indicates that the test compound is an inhibitor of SRD5AIII. A method is also provided for detecting androgen stimulated prostate cancer or recurrent prostate cancer in an individual. The method comprises obtaining a prostate biopsy from an individual and determining the level of expression of SRD5ADI gene or protein relative to a normal control. An increased expression of SRD5AIII relative to the control is indicative of androgen stimulated prostate cancer or recurrent prostate cancer.

    Abstract translation: 本发明提供了一种称为SRD5AIIL的分离的新型类固醇5a-还原酶。该蛋白质具有37kDa的估计分子量，并且能够在约7.0的pH下将睾酮转化为二氢睾酮。 还提供了通过将SRD5AIII与测试化合物接触并测量酶的活性来鉴定SRD5AIII的抑制剂的方法。 相对于对照的降低的活性表明测试化合物是SRD5AIII的抑制剂。 还提供了用于检测个体中激素刺激的前列腺癌或复发性前列腺癌的方法。 该方法包括从个体获得前列腺活检，并确定SRD5ADI基因或蛋白质相对于正常对照的表达水平。 SRD5AIII相对于对照的增加的表达指示雄激素刺激的前列腺癌或复发性前列腺癌。

    NEW CALIX ARENE COMPOUNDS, THEIR PROCESS OF PREPARATION AND THEIR USE, PARTICULARLY AS ENZYMATIC MIMES
    30.
    发明申请
    NEW CALIX ARENE COMPOUNDS, THEIR PROCESS OF PREPARATION AND THEIR USE, PARTICULARLY AS ENZYMATIC MIMES 审中-公开
    新的CALIX ARENE化合物，其制备方法及其用途，特别是作为酶制剂

    公开(公告)号：WO2004085442A2

    公开(公告)日：2004-10-07

    申请号：PCT/EP2004/003140

    申请日：2004-03-24

    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITE RENE DESCARTES-PARIS V ,  UNIVERSITE DU HAVRE ,  REINAUD, Olivia ,  JABIN, Ivan ,  DARBOST, Ulrich ,  XU-LI, Yun ,  REDON, Sophie

    Inventor： REINAUD, Olivia ,  JABIN, Ivan ,  DARBOST, Ulrich ,  XU-LI, Yun ,  REDON, Sophie

    IPC: C07D498/22

    CPC classification number: C07D498/22

    Abstract: The present invention relates to new calix arene compounds of formula (1). It also relates to their process of preparation. The present invention also relates to complexes between a compound of formula (1) and an element chosen among a metal, an actinide, a radioelement, a cationic guest or an anionic guest. The present invention also relates to a pharmaceutical composition comprising a compound of formula (I) in association with a pharmaceutically acceptable carrier. The present invention also relates to a process of preparation of water-soluble compounds, comprising a reaction of nitration or sulfonation, and optionally a reaction of sulfonation or nitration, particularly of compounds of formula (1), and also to the compounds such as obtained.

    Abstract translation: 本发明涉及式（1）的新型杯芳烃化合物。 它也涉及他们的准备过程。 本发明还涉及式（1）化合物与选自金属，act系元素，放射性元素，阳离子客体或阴离子客体的元素之间的络合物。 本发明还涉及包含式（I）化合物和药学上可接受的载体的药物组合物。 本发明还涉及一种制备水溶性化合物的方法，该方法包括硝化或磺化反应，和任选的磺化或硝化反应，特别是式（1）化合物的反应，还涉及例如获得的化合物

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