PRODRUGS OF INHIBITORS OF CATHEPSIN S
    1.
    发明申请
    PRODRUGS OF INHIBITORS OF CATHEPSIN S 审中-公开
    。OF OF。。。。。。。。。。。。。

    公开(公告)号:WO2008028301A1

    公开(公告)日:2008-03-13

    申请号:PCT/CA2007/001584

    申请日:2007-09-07

    CPC classification number: C07C317/48 C07C2601/02

    Abstract: The present invention provides compounds of formula (I) which are prodrugs of inhibitors of cathepsin S and as such are useful in the prevention and treatment of cathepsin S dependent diseases and conditions including, but not limited to, chronic obstructive pulmonary disease (COPD) and pain.

    Abstract translation: 本发明提供式(I)化合物,其为组织蛋白酶S抑制剂的前药,因此可用于预防和治疗组织蛋白酶S依赖性疾病和病症,包括但不限于慢性阻塞性肺病(COPD)和 疼痛。

    PROCESS FOR THE PREPARATION OF BENZOPHENTHIONES AND BENZOPHENONES
    8.
    发明申请
    PROCESS FOR THE PREPARATION OF BENZOPHENTHIONES AND BENZOPHENONES 审中-公开
    制备苯并噻唑和苯并噻唑的方法

    公开(公告)号:WO1995031435A1

    公开(公告)日:1995-11-23

    申请号:PCT/GB1995001101

    申请日:1995-05-16

    Inventor: ZENECA LIMITED

    CPC classification number: C07C45/27 C07C45/42 C07C45/518 C07C325/02

    Abstract: A process comprising the reaction of an optionally substituted benzene with thiophosgene in the presence of a Friedel-Crafts catalyst for the preparation of the equivalent optionally substituted benzophenthione and benzophenthiones of formula (I), in which X is H, halogen, alkyl, alkoxy, CN, or dialkylamino. The benzophenthiones are converted into the equivalent benzophenone derivatives by hydrolysis or by oxidation.

    Abstract translation: 一种方法,包括在Friedel-Crafts催化剂存在下与任选取代的苯与硫光气的反应,用于制备式(I)的当量任选取代的二苯并噻吩和苯并噻二唑,其中X为H,卤素,烷基,烷氧基, CN或二烷基氨基。 苯并噻吩通过水解或氧化转化为相应的二苯甲酮衍生物。

    METHOD FOR PRODUCING ALPHA-KETOALDEHYDE COMPOUND
    10.
    发明申请
    METHOD FOR PRODUCING ALPHA-KETOALDEHYDE COMPOUND 审中-公开
    生产α-羟基乙酸的方法

    公开(公告)号:WO2013018626A1

    公开(公告)日:2013-02-07

    申请号:PCT/JP2012/068899

    申请日:2012-07-19

    Inventor: HAGIYA, Koji

    Abstract: An object of the present invention is to provide a new method for producing an ALPHA-ketoaldehyde compound from a 2-oxo-primary alcohol compound. The present invention provides a method for producing an ALPHA-ketoaldehyde compound including a step of oxidizing a 2-oxo-primary alcohol compound in the presence of platinum, a platinum compound, iron or an iron compound. The 2-oxo-primary alcohol compound is preferably a compound represented by the formula (1a), and the ALPHA-ketoaldehyde compound is preferably a compound represented by the formula (2a), wherein Ra is a C1-C6 alkyl group which may have a substituent or a C6-C20 aryl group which may have a substituent.

    Abstract translation: 本发明的目的是提供从2-氧代 - 伯醇化合物制备ALPHA-酮醛化合物的新方法。 本发明提供了一种制备ALPHA-酮醛化合物的方法,包括在铂,铂化合物,铁或铁化合物存在下氧化2-氧代 - 伯醇化合物的步骤。 2-氧代 - 伯醇化合物优选为式(1a)表示的化合物,ALPHA-酮醛化合物优选为式(2a)表示的化合物,其中,R a为可具有式 取代基或可具有取代基的C6-C20芳基。

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