发明授权
- 专利标题: PIPERIDINE/PIPERAZINE-TYPE INHIBITORS OF P38 KINASE
- 专利标题(中): 哌啶基/哌嗪型的P38KINASE抑制剂
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申请号: EP01989111.8申请日: 2001-11-20
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公开(公告)号: EP1353905B1公开(公告)日: 2007-01-10
- 发明人: DUGAR, Sundeep , PERUMATTAM, John , TESTER, Richland , LU, Qing , MCENROE, Glenn
- 申请人: SCIOS INC.
- 申请人地址: 749 North Mary Avenue Sunnyvale, CA 94086 US
- 专利权人: SCIOS INC.
- 当前专利权人: SCIOS INC.
- 当前专利权人地址: 749 North Mary Avenue Sunnyvale, CA 94086 US
- 代理机构: Fisher, Adrian John
- 优先权: US252196P 20001120
- 国际公布: WO2002046158 20020613
- 主分类号: C07D211/18
- IPC分类号: C07D211/18 ; C07D513/04 ; C07D471/04 ; C07D207/40 ; A61K31/445 ; A61P29/00
摘要:
The invention is directed to inhibition of p38-α kinase using compounds of the formula (1) and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein: Ar1 is an aryl group substituted with 0-5 non-interfering substituents, wherein two adjacent noninterfering substituents can form a fused aromatic or nonaromatic ring; L?1 and L2¿ are linkers; each R1 is independently a noninterfering substitutent; Z?1 is CR2¿ or N wherein R2 is hydrogen or a noninterfering substituent; m is 0-4; each of n and p is an integer from 0-2 wherein the some of n and p is 0-3; Ar2 is a substantially planar, monocyclic or polycyclic aromatic moiety having one or more optional ring heteroatoms, said moiety being optionally substituted with one or more optional ring heteroatoms, said moiety being optionally substituted with one or more non-interfering substituents, two or more of which may form a fused ring; Z is W¿1?-COXjY wherein Y is COR?3¿ or an isotere thereof; R3 is a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; wherein the smallest number of covalent bonds is the compound separating the atom of Ar1 bonded to L2 to the atom of Ar2 bonded to L1 is at least 6, where each of said bonds has a bond length of 1.2 to 2.0 angstroms; and/or wherein the distance in space between the atom of Ar1 bonded to L2 and the atom of Ar2 bonded to L1 is 4.5-24 angstroms; with the proviso that the protion of the compound represented by Ar2-Z is not formula (2) wherein formula (3) represents a singel or double bond; n is 0-3; one Z2 is CA or CRA and the other is CR, CR¿2?, NR or N; A is Wi-COXjY wherein Y is COR or an isostere thereof, each of W and X is a spacer of 2-6Å, and each of i and j is independently 0 ot 1; Z?3¿ is NR or O; and each R independently hydrogen or a mominterfering substituent.
公开/授权文献
- EP1353905A2 PIPERIDINE/PIPERAZINE-TYPE INHIBITORS OF P38 KINASE 公开/授权日:2003-10-22
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