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    4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES
    1.
    发明授权
    4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 有权
    4-苯基-6-取代的嘧啶-2-碳腈衍生物

    公开(公告)号：EP1928842B1

    公开(公告)日：2009-11-18

    申请号：EP06806788.3

    申请日：2006-09-21

    申请人： N.V. Organon

    发明人： RANKOVIC, Zoran ,  CAI, Jiaqiang

    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

    CPC分类号： C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12

    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.

    摘要翻译： 本发明涉及式（I）的4-苯基-6-取代的 - 嘧啶-2-腈衍生物，其中R表示1-3个独立选自以下的任选取代基：（C 1-4） - 烷基（任选被一个或多个卤素取代） ，（C 1-4）烷氧基（任选被一个或多个卤素取代）和卤素; X是NR1，O或S; R1是H或（C1-4）烷基; Y是被选自OH，（C1-4）烷氧基，NR2R3的基团取代的（C1-4）烷基，苄基或（C2-6）烷基，含有1或2个选自下列的杂原子的4-8元饱和杂环： O，S和NR 4以及包含1-4个N原子的5或6元芳族杂环基; 或R1和Y与它们所键合的氮一起形成5-8元饱和杂环，任选地包含选自O，S，NR4和NO的另外的杂原子; 该环任选地被NR 2 R 3或1至4个（C 1-3）烷基取代; R2和R3独立地为H或（C1-4）烷基; 或者R 2和R 3与它们所键合的氮一起形成4-8元饱和杂环，任选地包含另外的选自O，S和NR 4的杂原子; （C1-6）烷基，（C3-6）环烷基，（C3-6）环烷基（C1-4）烷基，（C1-4）烷氧基 - （C1-4）烷基，苄基，酰胺基 - C1-4）烷基，（C1-6）烷氧基羰基（C1-4）烷基或羧基（C1-4）烷基; 或其药学上可接受的盐，包含其的药物组合物，以及这些4-苯基-6-取代的 - 嘧啶-2-腈衍生物在制备用于治疗组织蛋白酶K和组织蛋白酶的药物中的用途 S相关疾病，例如 骨质疏松症，动脉粥样硬化，炎症和免疫紊乱如类风湿性关节炎和慢性疼痛。

    4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES
    2.
    发明公开
    4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 有权
    4-苯基-6-取代的嘧啶-2- CARBONITRILDERIVATE

    公开(公告)号：EP1928842A1

    公开(公告)日：2008-06-11

    申请号：EP06806788.3

    申请日：2006-09-21

    申请人： N.V. Organon

    发明人： RANKOVIC, Zoran ,  CAI, Jiaqiang

    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

    CPC分类号： C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12

    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.

    6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS
    3.
    发明授权
    6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS 有权
    作为钙调蛋白抑制剂的6-苯基-1H-咪唑并[4,5-C]吡啶-4-碳腈衍生物

    公开(公告)号：EP2178873B1

    公开(公告)日：2010-12-22

    申请号：EP08786128.2

    申请日：2008-07-14

    申请人： N.V. Organon

    发明人： CAI, Jiaqiang ,  RANKOVIC, Zoran ,  JONES, Philip, Stephen ,  BENNETT, David, Jonathan ,  FRADERA, Xavier

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P19/00 ,  A61P17/00 ,  A61P29/00

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such asatherosclerosis,obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer,and chronic pain, such as neuropathic pain.

    摘要翻译： 本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，包含其的药物组合物，以及涉及这些衍生物用于 制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫紊乱如类风湿性关节炎，牛皮癣，癌症和慢性疼痛如神经性疼痛的药物。