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    Quinazoline derivatives as kinase inhibitors
    1.
    发明公开
    Quinazoline derivatives as kinase inhibitors 审中-公开
    喹唑啉衍生物作为激酶抑制剂

    公开(公告)号：EP1964839A2

    公开(公告)日：2008-09-03

    申请号：EP08075237.1

    申请日：2001-08-17

    申请人： MILLENNIUM PHARMACEUTICALS, INC. ,  KYOWA HAKKO KOGYO CO., LTD.

    发明人： Pandey, Anjali ,  Scarborough, Robert, M. ,  Matsuno, Kenji ,  Ichimura, Michio ,  Nomoto, Yuji ,  Ide, Shinichi ,  Tsukuda, Eiji ,  Irie, Junko ,  Oda, Shoji

    IPC分类号： C07D403/12 ,  C07D239/94 ,  C07D401/12 ,  A61P35/00 ,  A61K31/517

    CPC分类号： C07D239/94 ,  A61K31/517 ,  C07D401/12 ,  C07D403/12

    摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    摘要翻译： 本发明涉及对激酶的磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐，其抑制这些激酶的活性。 本发明还涉及抑制激酶并通过抑制激酶的磷酸化来治疗哺乳动物的疾病状态的方法。 本发明的一个特定方面提供了抑制PDGF受体的磷酸化以阻碍异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管性 重建，癌症和肾小球硬化。

    Quinazoline derivatives as kinase inhibitors
    2.
    发明公开
    Quinazoline derivatives as kinase inhibitors 审中-公开
    Quinazolinderivate als Kinasehemmer

    公开(公告)号：EP2277877A1

    公开(公告)日：2011-01-26

    申请号：EP10182322.7

    申请日：2001-08-17

    申请人： MILLENNIUM PHARMACEUTICALS, INC. ,  Kyowa Hakko Kogyo Co., Ltd

    发明人： Pandey, Anjali ,  Scarborough, Carroll ,  Matsuno, Kenji ,  Ichimura, Michio ,  Nomoto, Yuji ,  Ide, Schinichi ,  Tsukuda, Eiji ,  Irie, Junko ,  Oda, Shoji

    IPC分类号： C07D403/12 ,  C07D239/94 ,  C07D401/12 ,  A61P35/00 ,  A61K31/517

    CPC分类号： C07D239/94 ,  A61K31/517 ,  C07D401/12 ,  C07D403/12

    摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinase and treating disese states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    摘要翻译： 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制激素和治疗哺乳动物中的二恶烷状态的方法。 在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及用于预防或治疗细胞增殖性疾病如动脉硬化，血管 重建，癌症和肾小球硬化。

    Tricyclic compounds and intermediates thereof
    5.
    发明公开
    Tricyclic compounds and intermediates thereof 失效
    Tricyclische Verbindungen und ihre Zwischenprodukte。

    公开(公告)号：EP0497201A1

    公开(公告)日：1992-08-05

    申请号：EP92101012.0

    申请日：1992-01-22

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Kumazawa, Toshiaki ,  Yanase, Masashi ,  Harakawa, Hiroyuki ,  Obase, Hiroyuki ,  Oda, Shoji ,  Shirakura, Shiro ,  Yamada, Koji ,  Kubo, Kazuhiro

    IPC分类号： C07D313/12 ,  C07D491/04 ,  C07C233/58 ,  C07D223/20 ,  C07D337/12 ,  C07D471/04 ,  C07D513/04 ,  C07D213/56

    CPC分类号： C07D491/04 ,  C07C233/65 ,  C07C2603/32 ,  C07D223/20 ,  C07D313/12 ,  C07D337/12 ,  Y10S514/824

    摘要： Disclosed is a tricyclic compound represented by the formula (I):

    wherein each of R¹, R², R³ and R⁴ independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR⁹R¹⁰CO₂R¹¹ (wherein each of R⁹, R¹⁰ and R¹¹ independently represents hydrogen or C1-6 alkyl) or CONR¹²R¹³ (wherein each of R¹² and R¹³ independently represents hydrogen or C1-6 alkyl); R⁵ represents hydrogen or C1-6 alkyl; each of R⁶, R⁷ and R⁸ independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y¹-Y² represents CH₂-O, CH₂-S(O) n , (wherein n represents 0, 1, or 2), CH₂CH₂, CH=CH or CON(R¹⁴) (wherein R¹⁴ represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

    摘要翻译： 公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6 烷氧基，C 1-6烷硫基，氨基，C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 1， （其中R 9，R 1，O和R 1各自独立地表示氢或C 1-6烷基）或CONR 1 2 R 1（3）其中R 1和R 2各自独立地表示氢或C 1-6烷基）。 R 5表示氢或C 1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y 1 -Y 2表示CH 2 -O，CH 2 -S（O）n，（其中n表示0,1或2），CH 2 CH 2，CH = CH或CON（R 1 4） （其中R 1 4代表氢或C 1-6烷基），Z代表氧或硫，或其药学上可接受的盐。 该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。