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    Heteroaryl-cyclic acetals
    1.
    发明授权
    Heteroaryl-cyclic acetals 有权
    杂芳基环缩醛

    公开(公告)号：US07479501B2

    公开(公告)日：2009-01-20

    申请号：US09871564

    申请日：2001-05-31

    申请人： Alan Collis ,  Frank Halley ,  Iain McLay

    发明人： Alan Collis ,  Frank Halley ,  Iain McLay

    IPC分类号： A61K31/4439 ,  C07D405/14

    CPC分类号： C07D409/14 ,  C07D405/14 ,  C07D413/14

    摘要： Compounds of formula (I) are described in which Het is a five or six membered heteroaromatic ring of the formula in which one of R1 and R2 is optionally substituted heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X1 is a bond, X3 and X4 are each independently N or C and X2 and X5 are independently CH, N, NH, O or S; or X3 and X4 are C, one of X1, X2 and X5 is N and the others are N or CH; but excluding compounds in which X1 is a bond, one of X2 and X5 is N and the other is NH and X3 and X4 are both C; R3 represents a group -L1-R6; R4 represents hydrogen, alkyl or hydroxyalkyl; or R3 and R4, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R5 represents hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.

    摘要翻译： 描述式（I）的化合物，其中Het是下式的五或六元杂芳族环，其中R 1和R 2中的一个是任选取代的杂芳基，另一个是任选取代的杂芳基或任选取代的芳基; X1是键，X3和X4各自独立地是N或C，X2和X5独立地是CH，N，NH，O或S; 或X3和X4为C，X1，X2和X5之一为N，其余为N或CH; 但不包括X1为键的化合物，X2和X5之一为N，另一个为NH，X3和X4均为C; R3表示基团-L1-R6; R4表示氢，烷基或羟烷基; 或者R 3和R 4在连接到相同的碳原子时可与所述碳原子一起形成环烷基，环烯基或杂环烷基环或基团C-CH 2; R5代表氢或烷基; m为零或整数1或2; 和N-氧化物及其前药; 和式（I）化合物及其N-氧化物的药学上可接受的盐和溶剂合物及其前药。 这些化合物是TNF抑制剂，可用作药物。

    Heteroaryl-cyclic acetals
    2.
    发明申请
    Heteroaryl-cyclic acetals 有权
    杂芳基环缩醛

    公开(公告)号：US20050090501A1

    公开(公告)日：2005-04-28

    申请号：US09871564

    申请日：2001-05-31

    申请人： Alan Collis ,  Frank Halley ,  Iain McLay

    发明人： Alan Collis ,  Frank Halley ,  Iain McLay

    IPC分类号： A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P11/06 ,  A61P19/02 ,  A61P27/02 ,  A61P35/00 ,  A61P43/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D45/04

    CPC分类号： C07D409/14 ,  C07D405/14 ,  C07D413/14

    摘要： Compounds of formula (I) are described in which Het is a five or six membered heteroaromatic ring of the formula in which one of R1 and R2 is optionally substituted heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X1 is a bond, X3 and X4 are each independently N or C and X2 and X5 are independently CH, N, NH, O or S; or X3 and X4 are C, one of X1, X2 and X5 is N and the others are N or CH; but excluding compounds in which X1 is a bond, one of X2 and X5 is N and the other is NH and X3 and X4 are both C; R3 represents a group -L1-R6; R4 represents hydrogen, alkyl or hydroxyalkyl; or R3 and R4, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R5 represents hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.

    摘要翻译： 描述式（I）的化合物，其中Het是下式的五或六元杂芳族环，其中R 1和R 2中的一个是任选取代的杂芳基和 另一个是任选取代的杂芳基或任选取代的芳基; X 1是一个键，X 3和X 4各自独立地是N或C和X 2和X 5个独立的是CH，N，NH，O或S; 或X 3和X 4是C，X 1，X 2和X 5之一 为N，其余为N或CH; 但不包括其中X 1是一个键的化合物，X 2和X 5之一是N，另一个是NH和X 3＆lt; 4＆gt;和＆lt; 4＆gt;都是C; R 3表示基团-L 1→6→6; R 4表示氢，烷基或羟烷基; 或R 3和R 4，当连接到相同的碳原子时，可与所述碳原子一起形成环烷基，环烯基或杂环烷基环或C-CH 3基， SUB> 2 R 5表示氢或烷基; m为零或整数1或2; 和N-氧化物及其前药; 和式（I）化合物及其N-氧化物的药学上可接受的盐和溶剂合物及其前药。 这些化合物是TNF抑制剂，可用作药物。