发明公开
EP1080078A1 HETEROCYCLIC COMPOUNDS AND METHODS TO TREAT CARDIAC FAILURE AND OTHER DISORDERS
有权
HETEROZYCLISCHE衍生物对心力衰竭等疾病的治疗
- 专利标题: HETEROCYCLIC COMPOUNDS AND METHODS TO TREAT CARDIAC FAILURE AND OTHER DISORDERS
- 专利标题(中): HETEROZYCLISCHE衍生物对心力衰竭等疾病的治疗
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申请号: EP99924412.2申请日: 1999-05-21
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公开(公告)号: EP1080078A1公开(公告)日: 2001-03-07
- 发明人: MAVUNKEL, Babu, J. , LIU, David, Y. , SCHREINER, George, F. , LEWICKI, John, A. , PERUMATTAM, John, J.
- 申请人: SCIOS INC.
- 申请人地址: 820 West Maude 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: 820 West Maude Avenue Sunnyvale, CA 94086 US
- 代理机构: Fisher, Adrian John
- 优先权: US86531P 19980522; US128137 19980803; US275176 19990324
- 国际公布: WO9961426 19991202
- 主分类号: C07D235/06
- IPC分类号: C07D235/06 ; C07D401/06 ; C07D401/14 ; C07D209/08 ; C07D403/06 ; A61K31/445 ; A61K31/40 ; A61K31/41
摘要:
Compounds of formulae α or β, and the pharmaceutically acceptable salts thereof, wherein each of Z?1 and Z2¿ is independently CR4 or N; where each R4 is independently H or is alkyl (1-6C) or aryl, each of said alkyl or aryl optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR¿2?, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or =O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R?1¿ is formula (I); wherein X1 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0 or 2; Z3 is CH or N; X2 is CH, CH¿2? or an isostere thereof; and Ar consists of one or two phenyl moieties directly coupled to X?2¿ optionally substituted by halo, nitro, alkyl(1-6C), alkenyl(1-6C), alkynyl(1-6C), CN or CF¿3?, or by RCO, COOR, CONR2, NR2, OR, SR, OOCR or NROCR wherein R is H or alkyl(1-6C) or by phenyl, itself optionally substituted by the foregoing substituents; R?2¿ is H, or is alkyl(1-6C) or aryl, each or said alkyl or aryl optionally including one heteroatome which is O, S or N, and optionally substituted by one or more of halo, OR, SR, NR¿2?, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl(1-6C), alkynyl(1-6C), or by one or more CN or =O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R?3¿ is H, halo, NO¿2?, alkyl(1-6C), alkenyl(1-6C), alkynyl(1-6C), CN, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl(1-6C) are disclosed. These compounds are selective inhibitors of p38α kinase.
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