公开(公告)号：EP1516877A1

公开(公告)日：2005-03-23

申请号：EP04015656.4

申请日：2000-03-15

申请人： AXYS PHARMACEUTICALS, INC.

发明人： Martichonok, Valeri ,  Burgess-Henry, Jana ,  Graupe, Michael ,  Link, John O. ,  McDowell, Robert S. ,  McGrath, Mary E. ,  Mossman, Craig J. ,  Patterson, John W. ,  Saunders, Oliver L. ,  Zipfel, Sheila M. ,  Martelli, Arnold J. ,  Lai, Justine ,  Aldous, David J. ,  Halley, Frank ,  Pickett, Stephen D. ,  Thurairatnam, Sukanthini ,  Timm, Andreas P.

IPC分类号： C07D263/56 ,  A61K31/42 ,  C07D263/34 ,  C07D413/12 ,  A61K31/44 ,  C07D213/40 ,  C07D209/14 ,  C07D307/81 ,  A61P37/00 ,  A61P9/00

CPC分类号： C07D413/12 ,  A61K31/42 ,  A61K31/44 ,  A61K45/06 ,  C07D209/14 ,  C07D213/40 ,  C07D217/04 ,  C07D221/08 ,  C07D233/64 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D263/56 ,  C07D307/14 ,  C07D307/81 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07F7/1856 ,  A61K2300/00

摘要： The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making; according to Formal (I) in which: A comprises a heteromonocyclic ring containing 5 to 6 ring member atoms or a fused heteropolycyclic ring system containing 8 to 14 ring member atoms, wherein each ring contains 5 to 7 ring member atoms, X 1 is a ring member carbon atom and each ring member other than X 1 is a carbon atom or a heteroatom, with the proviso that (i) at least one ring member atom is a heteroatom and (ii) when A is a heteromonocyclic radical containing 5 ring member atoms, no more than two of the ring member atoms comprising A are heteroatoms; n is 0, 1, 2 or 3; X 1 is =C- or -CH-; X 2 is a bond or a divalent group of Formula (a) or (b); R 1 - R 8 = as in the application.

摘要翻译： 本发明涉及新型烷酰基取代的杂环衍生物，它们是半胱氨酸蛋白酶抑制剂; 其药学上可接受的盐和N-氧化物; 它们作为治疗剂的用途及其制备方法; 根据Formal（I），其中：A包含含有5至6个环成员原子的杂单环或含有8至14个环成员原子的稠合杂多环系，其中每个环含有5至7个环成员原子，X 1， 是环成员碳原子，除X 1之外的每个环成员是碳原子或杂原子，条件是（i）至少一个环原子是杂原子，和（ii）当A是异单环基团时 含有5个环成员原子，不超过两个包含A的环成员原子是杂原子; n为0,1,2或3; X 1 = C或-CH-; X 2为式（a）或（b）的键或二价基团; R 1 -R 8 =如申请中所述。