发明公开
EP1928842A1 4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES
有权
4-苯基-6-取代的嘧啶-2- CARBONITRILDERIVATE
- 专利标题: 4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES
- 专利标题(中): 4-苯基-6-取代的嘧啶-2- CARBONITRILDERIVATE
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申请号: EP06806788.3申请日: 2006-09-21
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公开(公告)号: EP1928842A1公开(公告)日: 2008-06-11
- 发明人: RANKOVIC, Zoran , CAI, Jiaqiang
- 申请人: N.V. Organon
- 申请人地址: Kloosterstraat 6 5349 AB Oss NL
- 专利权人: N.V. Organon
- 当前专利权人: N.V. Organon
- 当前专利权人地址: Kloosterstraat 6 5349 AB Oss NL
- 代理机构: van Wezenbeek, Petrus M.G.F.
- 优先权: EP05108810 20050923
- 国际公布: WO2007039470 20070412
- 主分类号: C07D239/42
- IPC分类号: C07D239/42 ; C07D239/34 ; C07D239/38 ; C07D239/36 ; C07D403/04 ; C07D401/04 ; C07D403/12 ; C07D401/12 ; A61K31/505 ; A61K31/506 ; A61P19/10 ; A61P9/10
摘要:
The invention relates to 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula (I) wherein R represents 1-3 optional substituents independently selected from (C1-4)- alkyl (optionally substituted with one or more halogens), (C1-4)alkyloxy (optionally substituted with one or more halogens) and halogen; X is NR1, O or S; R1 is H or (C1-4)alkyl; Y is (C1-4)alkyl, benzyl or (C2-6)alkyl, substituted with a group selected from OH, (C1-4)alkyloxy, NR2R3, a 4-8 membered saturated heterocyclic ring comprising 1 or 2 heteroatoms selected from O, S and NR4, and a 5 or 6-membered aromatic heterocyclic group comprising 1-4 N atoms; or R1 and Y form together with the nitrogen to which they are bonded a 5-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S, NR4 and NO; the ring being optionally substituted with NR2R3 or with 1 to 4 (C1-3)alkyl groups; R2 and R3 are independently H or (C1-4)alkyl; or R2 and R3 form together with the nitrogen to which they are bonded a 4-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S and NR4; R4 is H, (C1-6)alkyl,(C3-6) cycloalkyl, (C3-6)cycloalkyl(C1-4)alkyl, (C1-4)alkyloxy-(C1-4)alkyl, benzyl, amido- (C1-4)alkyl, (C1-6)alkyloxycarbonyl(C1-4)alkyl or carboxy(C1-4)alkyl; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the preparation of a medicament for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.
公开/授权文献
- EP1928842B1 4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 公开/授权日:2009-11-18
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