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    N-(2,5-Diazolyl)alkyl-halogenacetanilide, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Herbizide
    71.
    发明公开
    N-(2,5-Diazolyl)alkyl-halogenacetanilide, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Herbizide 失效
    N-（2,5-二唑）烷基卤代乙酰苯胺，其制备方法和它们作为除草剂的使用过程。

    公开(公告)号：EP0019742A2

    公开(公告)日：1980-12-10

    申请号：EP80102375.5

    申请日：1980-05-02

    申请人： BAYER AG

    发明人： Stetter, Jörg, Dr. ,  Ditgens, Klaus, Dr. ,  Thomas, Rudolf, Dr. ,  Eue, Ludwig, Dr. ,  Schmidt, Robert Rudolf

    IPC分类号： C07D271/08 ,  C07D285/10 ,  C07D249/04 ,  A01N43/64 ,  A01N43/82

    CPC分类号： C07D285/10 ,  A01N43/653 ,  A01N43/82 ,  C07D249/04 ,  C07D271/08

    摘要： Neue N-(2,5-Diazolyl)-alkyl-halogenacetanilide der Formel
    in welcher

    A für Sauerstoff, Schwefel oder die Gruppierung >NH steht, worin
    R für Alkyl steht,
    R' für Wasserstoff. Alkyl oder Alkoxy steht,
    R 2 für Wasserstoff. Alkyl, Alkoxy oder Halogen steht.
    R 3 für Wasserstoff, Alkyl, Alkoxy oder Halogen steht.
    R 4 für Wasserstoff oder Alkyl steht,
    R' für Wasserstoff, Alkyl. Alkoxy, Alkylthio. Dialkylamino. Halogen. Cyano oder Alkoxycarbonyl steht und
    Z für Halogen steht,

    sowie deren Säureadditions-Salze und Metallsalz-Komplexe, mehrere Verfahren zu ihrer Herstellung sowie ihre Verwendung als Herbizide.
    Neue N-(2,5-Diazolyl)-alkyl-aniline der Formel
    in welcher R', R 2 , R 3 , R 4 , R 5 und A die oben angegebene Bedeutung haben, und ein Verfahren zur Herstellung dieser Stoffe.

    摘要翻译： 新颖的N-（2,5-二唑）的一般formmula的烷基halogenoacetanilides （I）氢，其中A darstellt氧，硫或分组> NR，worinřdarstellt烷基，R1 darstellt，烷基或烷氧基， R2 darstellt氢，烷基，卤素烷氧基或，R3 darstellt氢，烷基，烷氧基或卤素，R 4表示氢或烷基，R5 darstellt氢，烷基，烷氧基，烷硫基，二烷基氨基，卤素，氰基或烷氧基羰基和Z darstellt卤素，和酸 加成盐和金属盐复合物作为除草剂有效出色。 进一步更新颖的N-（2,5-二唑），其中R1，R2，R3，R4，R5和A的通式（II）的烷基 - 苯胺具有上述含义。

    5-SUBSTITUTED 1,1-DIOXO-¬1,2,5 THIAZOLIDINE-3-ONE DERIVATIVES AS PTPASE 1B INHIBITORS
    77.
    发明授权
    5-SUBSTITUTED 1,1-DIOXO-¬1,2,5 THIAZOLIDINE-3-ONE DERIVATIVES AS PTPASE 1B INHIBITORS 有权
    5-取代的1,1-二氧代噻唑烷-3-酮衍生物¬1,2,5ALS缝边PTP酶1B

    公开(公告)号：EP1492780B1

    公开(公告)日：2011-11-23

    申请号：EP03720412.0

    申请日：2003-04-02

    申请人： Novartis AG

    发明人： COPPOLA, Gary, Mark ,  DAVIES, John, William ,  JEWELL, Charles, Francis, Jr. ,  LI, Yu-Chin ,  WAREING, James, Richard ,  SPERBECK, Donald, Mark ,  STAMS, Travis, Mathew ,  TOPIOL, Sidney, Wolf ,  VLATTAS, Isidoros

    IPC分类号： C07D285/10 ,  A61K31/433 ,  A61P3/10 ,  C07D417/06

    CPC分类号： C07D285/10 ,  C07D417/06 ,  C07D417/10 ,  C07K5/06078

    摘要： Compounds of the formula (I) provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula (I) inhibit PTP-1 B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

    5-substituted 1,1-dioxo-[1,2,5]thiazolidine-3-one derivatives as PTPASE 1B inhibitors
    78.
    发明公开
    5-substituted 1,1-dioxo-[1,2,5]thiazolidine-3-one derivatives as PTPASE 1B inhibitors 审中-公开
    5-取代物1,1-二氧代 - [1,2,5]噻唑烷-3-酮衍生物PTPASE 1B mer

    公开(公告)号：EP2341049A1

    公开(公告)日：2011-07-06

    申请号：EP11156123.9

    申请日：2003-04-02

    申请人： Novartis AG

    发明人： Coppola, Gary Mark ,  Davies, John William ,  Jewel, Charles Francis, Jr. ,  Li, Yu-Chin ,  Wareing, James Richard ,  Sperbeck, Donald Mark ,  Stams, Travis Mathew ,  Topiol, Sidney Wolf ,  Vlattas, Isidoros

    IPC分类号： C07D285/10 ,  A61K31/433 ,  A61P3/10 ,  C07D417/06

    CPC分类号： C07D285/10 ,  C07D417/06 ,  C07D417/10 ,  C07K5/06078

    摘要： Compounds of the formula

    wherein L 1 , L 2 , L 3 , Q 1 , Q 2 , R 1 , R 2 , X, Y and Z are as decribed in the description fo the invention, provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

    摘要翻译： 其中L 1，L 2，L 3，Q 1，Q 2，R 1，R 2，X，Y和Z如本发明描述的化合物提供作为PTP酶抑制剂的药理学试剂， 特别地，式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。 因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，糖尿病，高血压和大血管和小血管缺血性疾病相关的胰岛素抵抗。 此外，本发明的化合物可用于治疗或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。