CN103153994B - 双环杂芳基激酶抑制剂及使用方法 - Google Patents

双环杂芳基激酶抑制剂及使用方法 Download PDF

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CN103153994B
CN103153994B CN201180036376.2A CN201180036376A CN103153994B CN 103153994 B CN103153994 B CN 103153994B CN 201180036376 A CN201180036376 A CN 201180036376A CN 103153994 B CN103153994 B CN 103153994B
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phenyl
pyrrolo
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optionally substituted
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CN103153994A (zh
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H.A.杰尔巴德
S.久赫斯特
V.S.古德菲洛
T.维曼
S.B.拉乌拉
C.J.罗思
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University of Rochester
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    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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CN201180036376.2A 2010-05-24 2011-05-24 双环杂芳基激酶抑制剂及使用方法 Active CN103153994B (zh)

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US34769410P 2010-05-24 2010-05-24
US61/347694 2010-05-24
US61/347,694 2010-05-24
PCT/US2011/037758 WO2011149950A2 (en) 2010-05-24 2011-05-24 Bicyclic heteroaryl kinase inhibitors and methods of use

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CN103153994B true CN103153994B (zh) 2016-02-10

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US (1) US8846909B2 (enExample)
EP (1) EP2576549A4 (enExample)
JP (1) JP6086326B2 (enExample)
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AU (1) AU2011258465B2 (enExample)
CA (1) CA2800176C (enExample)
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