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    Pyridazines as interleukin-1&bgr; converting enzyme inhibitors
    5.
    发明授权
    Pyridazines as interleukin-1&bgr; converting enzyme inhibitors 失效
    哒嗪作为白细胞介素-1β转换酶抑制剂

    公开(公告)号：US06624166B1

    公开(公告)日：2003-09-23

    申请号：US08625680

    申请日：1996-04-03

    申请人： Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

    发明人： Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

    IPC分类号： C07D23724

    CPC分类号： C07D401/04 ,  C07D237/24 ,  C07D403/04

    摘要： Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.

    摘要翻译： 公开了式（I）的化合物及其药学上可接受的盐：其中R1是卤素或含有芳香醚，烷基磺酸酯，芳基磺酸酯，烷基膦酸酯，芳基膦酸酯，磷酸烷基酯 或芳基磷酸酯; R2是COOR5，C（= O）NH（CHR5）m -COOR5，NH（CHR5）mCON（R5）R6，C（= O）N（R5）R6或NH（CHR5） H或烷基; R 4是H，取代或未取代的芳基，杂芳基或烷基; R 5和R 6独立地是H，低级烷基，芳基，羟基烷基，氨基烷基，杂芳基，低级亚烷基 - 芳基，低级亚烷基 - 杂芳基或低级环烷基; m = 0-6; 含有这些化合物的药物组合物; 以及利用该化合物和组合物抑制哺乳动物中白细胞介素-1β蛋白酶活性的方法。

    Pyridazines as interleukin-1.beta. converting enzyme inhibitors
    6.
    发明授权
    Pyridazines as interleukin-1.beta. converting enzyme inhibitors 失效
    哒嗪作为白细胞介素-1β转换酶抑制剂

    公开(公告)号：US6121266A

    公开(公告)日：2000-09-19

    申请号：US444984

    申请日：1995-05-19

    申请人： Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

    发明人： Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

    IPC分类号： A61K31/50 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D237/24 ,  C07D401/04 ,  C07D403/04 ,  A61K31/4965 ,  A61K31/497

    CPC分类号： C07D401/04 ,  C07D237/24 ,  C07D403/04

    摘要： Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate;R.sub.2 is COOR.sub.5, C(.dbd.O)NH(CHR.sub.5).sub.m --COOR.sub.5, NH(CHR.sub.5).sub.m CON(R.sub.5)R.sub.6, C(.dbd.O)N(R.sub.5)R.sub.6 or NH(CHR.sub.5).sub.m OH;R.sub.3 is H or alkyl;R.sub.4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl;R.sub.5 and R.sub.6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta. protease activity in a mammal utilizing the compounds and compositions.

    摘要翻译： 公开了式（I）的化合物及其药学上可接受的盐：其中R1是卤素，或含有芳香族醚，烷基磺酸酯，芳基磺酸酯，烷基膦酸酯，芳基膦酸酯，烷基 磷酸盐或芳基磷酸盐; R2是COOR5，C（= O）NH（CHR5）m -COOR5，NH（CHR5）mCON（R5）R6，C（= O）N（R5）R6或NH（CHR5） R3是H或烷基; R4是H，取代或未取代的芳基，杂芳基或烷基; R5和R6独立地为H，低级烷基，芳基，羟基烷基，氨基烷基，杂芳基，低级亚烷基 - 芳基，低级亚烷基 - 杂芳基或低级环烷基; m = 0-6; 含有这些化合物的药物组合物; 以及利用该化合物和组合物抑制哺乳动物中白细胞介素-1β蛋白酶活性的方法。