公开(公告)号：EP1070711A2

公开(公告)日：2001-01-24

申请号：EP00306196

申请日：2000-07-20

申请人： SANKYO CO

发明人： KIMURA TOMIO ,  AOKI KAZUMASA ,  NAKAO AKIRA ,  USHIYAMA SHIGERU ,  SHIMOZATO TAKAICHI ,  OHKAWA NOBUYUKI

IPC分类号： A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P29/00 ,  C07D401/04 ,  C07D401/14 ,  C07D451/02 ,  C07D453/02 ,  C07D455/02 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/4427

CPC分类号： C07D451/02 ,  C07D401/04 ,  C07D401/14 ,  C07D453/02 ,  C07D455/02 ,  C07D471/04

摘要： Compounds of formula (I): wherein: A is a pyrrole ring; R is an optionally substituted aryl or heteroaryl group; R is an optionally substituted nitrogen-containing heteroaryl group; R represents a group of the formula -X-R , wherein X is a single bond or an optionally substituted alkylene, alkenylene or alkynylene group, and R is a substituted cycloalkyl group, a substituted aryl group, a substituted heterocyclyl group, an optionally substituted nitrogen-containing heterocyclyl group, a substituted heteroaryl group, an optionally substituted nitrogen-containing heteroaryl group, or -NR R , wherein each of R and R is a hydrogen atom or an alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl group; PROVIDED THAT said substituents R and R are bonded to the two atoms of said pyrrole ring which are adjacent to the atom of the pyrrole ring to which said substituent R is bonded­ have excellent inhibitory activity against the production of inflammatory cytokines.

摘要翻译： 式（I）化合物：其中：A是吡咯环; R 1是任选取代的芳基或杂芳基; R 2是任选取代的含氮杂芳基; R 3表示式-XR 4的基团，其中X是单键或任选取代的亚烷基，亚烯基或亚炔基，并且R 4是取代的环烷基，取代的芳基， 取代的杂环基，任选取代的含氮杂环基，取代的杂芳基，任选取代的含氮杂芳基或-NRR，其中R和R各自为氢原子或烷基，烯基，炔基，芳烷基 或烷基磺酰基; 提供所述取代基R 1和R 3与所述吡咯环的两个与所述取代基R 2所键合的吡咯环的原子相邻的原子结合的化合物具有优异的抗生产抑制活性 炎性细胞因子。

公开(公告)号：EP1031572A4

公开(公告)日：2001-09-19

申请号：EP98953051

申请日：1998-11-13

申请人： SANKYO CO

发明人： KIMURA TOMIO ,  KAWARA AKIHIRO ,  NAKAO AKIRA ,  SUZUKI KEISUKE ,  USHIYAMA SHIGERU ,  SHIMOZATO TAKAICHI

IPC分类号： C07D409/14 ,  C07D411/14 ,  C07D417/14 ,  A61K31/44 ,  A61K31/54 ,  C07D413/14

CPC分类号： C07D409/14 ,  C07D411/14 ,  C07D417/14

摘要： Object: to provide compounds having an inhibitory effect on the production of inflammatory cytokines. Constitution: compounds having general formula (I), pharmacologically acceptable salts thereof or derivatives of the same, wherein A: single bond, oxygen, sulfur, CO, SO, SO2, C(R?9)(R10) [R9, R10¿: H, OH, halogeno, alkyl], N(R11), C=NOR11 [R11: H, alkyl]; D: single bond, C(R?12)(R13) [R12, R13¿: H, OH, halogeno, alkyl]; R1: optionally substituted pyridyl; R2: optionally substituted phenyl; R3: halogeno, alkyl, haloalkyl, alkoxy, haloalkoxy; R?4, R5, R6, R7, R8¿: H, alkyl; k: 0-3; and m: 1, 2.

摘要翻译： 目的：提供对炎性细胞因子产生具有抑制作用的化合物。 组成：具有通式（I）的化合物，其药理学上可接受的盐或其衍生物，其中A为单键，氧，硫，CO，SO，SO 2，C（R 9）（R 10）[R 9，R 10 ：H，OH，卤素，烷基]，N（R11），C = NOR11 [R11：H，烷基]; D：单键，C（R 12）（R 13）[R 12，R 13：H，OH，卤代，烷基]; R1：任选取代的吡啶基; R2：任选取代的苯基; R3：卤代，烷基，卤代烷基，烷氧基，卤代烷氧基; R 4，R 5，R 6，R 7，R 8：H，烷基; k：0-3; 和m：1，2。

公开(公告)号：EP1069110A4

公开(公告)日：2004-09-01

申请号：EP99910822

申请日：1999-04-02

申请人： SANKYO CO

发明人： KIMURA TOMIO ,  MIYAZAKI SHOUJIRO ,  UEDA KEIJI ,  TANZAWA KAZUHIKO ,  USHIYAMA SHIGERU ,  TAKASAKI WATARU

IPC分类号： A61K31/18 ,  C07C311/29 ,  C07C311/46 ,  C07D209/46 ,  C07D209/48 ,  C07D209/60 ,  C07D209/66 ,  C07D217/24 ,  C07D233/78 ,  C07D239/54 ,  C07D239/70 ,  C07D239/96 ,  C07D275/06 ,  C07D277/34 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D473/04 ,  C07D475/02 ,  C07D495/04 ,  A61K31/505 ,  A61P35/00

CPC分类号： C07D209/48 ,  C07C311/29 ,  C07D209/66 ,  C07D233/78 ,  C07D239/54 ,  C07D239/70 ,  C07D239/96 ,  C07D275/06 ,  C07D277/34 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D473/04 ,  C07D475/02 ,  C07D495/04

摘要： Compounds having a matrix metaloproteinase-13 inhibitory activity and an aggrecanase inhibitory activity. They are compounds represented by general formula (I) or pharmacologically acceptable salts, esters, or other derivatives thereof wherein R1 is H or NHOH; R2 is H, optionally substituted alkyl, cycloalkyl, or -AR6 (wherein A is O, -S(O)¿m?-, or alkylene optionally interrupted by -N(R?9¿)-; and R6 is a group represented by formula (II), (III), or (IV) [wherein X is O, S, -N(R10)-, or -C(R11)(R12)-; Y is O, CO, -S(O)¿n?-, -N(R?10¿)-, or -C(R?11)(R12)-; R7 and R8¿ each is H, alkyl, COOH, optionally substituted alkyl, etc.; R?9, R10, R11, and R12¿ each is H, alkyl, etc.; and m and n each is 0 to 2]); R3 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, or optionally substituted alkynyl; R4 is optionally substituted (hetero)arylene; and R5 is optionally substituted alkyl or optionally substituted (hetero)aryl.