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    • 1. 发明授权
    • Pyrazoloquinolone derivative and use thereof
    • 吡唑并喹啉衍生物及其用途
    • US07842701B2
    • 2010-11-30
    • US10589443
    • 2005-02-18
    • Shoji FukumotoTakeshi YamamotoMasanori OkaniwaToshimasa Tanaka
    • Shoji FukumotoTakeshi YamamotoMasanori OkaniwaToshimasa Tanaka
    • A61K31/437C07D471/06
    • C07D471/04
    • The present invention provides a pyarzoloquinolone derivative having kinase inhibitory activity. The derivative is represented by the formula: wherein R1 is an aryl group which may be substituted, or an aromatic heterocyclic group which may be substituted; R2 is a hydrogen atom, an amino group which may be substituted, a hydroxy group which may be substituted, or a thiol group which may be substituted; R3, R4, R5 and R6, which may be identical or different, are each (1) a hydrogen atom, (2) a nitro group, (3) a cyano group, (4) a halogen atom, (5) a hydrocarbon group which may be substituted, (6) an amino group which may be substituted, (7) a hydroxy group which may be substituted, or (8) a thiol group which may be substituted; and R3 and R4, R4 and R5, and R5 and R6 may respectively form a ring together with the adjacent carbon atom, or salt thereof.
    • 本发明提供具有激酶抑制活性的pyarzoloquinolone衍生物。 该衍生物由下式表示:其中R1是可被取代的芳基或可被取代的芳族杂环基; R2是氢原子,可被取代的氨基,可被取代的羟基,或可以被取代的硫醇基; R 3,R 4,R 5和R 6可以相同或不同,分别为(1)氢原子,(2)硝基,(3)氰基,(4)卤素原子,(5) 可以被取代的基团,(6)可以被取代的氨基,(7)可被取代的羟基,或(8)可以被取代的硫醇基; 并且R 3和R 4,R 4和R 5以及R 5和R 6可以与相邻的碳原子或其盐一起分别形成环。
    • 2. 发明申请
    • Pyrazoloquinolone Derivative And Use Thereof
    • 吡唑并喹啉衍生物及其用途
    • US20070281963A1
    • 2007-12-06
    • US10589443
    • 2005-02-18
    • Shojl FukumotoTakeshi YamamotoMasanori OkaniwaToshimasa Tanaka
    • Shojl FukumotoTakeshi YamamotoMasanori OkaniwaToshimasa Tanaka
    • A61K31/435A61P35/00C07D471/00
    • C07D471/04
    • The present invention provides a pyarzoloquinolone derivative having kinase inhibitory activity. The derivative is represented by the formula: wherein R1 is an aryl group which may be substituted, or an aromatic heterocyclic group which may be substituted; R2 is a hydrogen atom, an amino group which may be substituted, a hydroxy group which may be substituted, or a thiol group which may be substituted; R3, R4, R5 and R6, which may be identical or different, are each (1) a hydrogen atom, (2) a nitro group, (3) a cyano group, (4) a halogen atom, (5) a hydrocarbon group which may be substituted, (6) an amino group which may be substituted, (7) a hydroxy group which may be substituted, or (8) a thiol group which may be substituted; and R3 and R4, R4 and R5, and R5 and R6 may respectively form a ring together with the adjacent carbon atom, or salt thereof.
    • 本发明提供具有激酶抑制活性的pyarzoloquinolone衍生物。 该衍生物由下式表示:其中R 1为可被取代的芳基,或可被取代的芳族杂环基; R 2是氢原子,可以被取代的氨基,可被取代的羟基或可以被取代的硫醇基; R 3,R 4,R 5,R 6和R 6可以相同或不同,各自为( 1)氢原子,(2)硝基,(3)氰基,(4)卤素原子,(5)可被取代的烃基,(6)可以被取代的氨基, 7)可被取代的羟基,或(8)可被取代的硫醇基; 和R 3和R 4,R 4和R 5和R 5和/或 >和R 6可以与相邻的碳原子或其盐一起分别形成环。
    • 3. 发明授权
    • Heterocyclic compound and use thereof
    • 杂环化合物及其用途
    • US08697874B2
    • 2014-04-15
    • US13132253
    • 2009-11-30
    • Masanori Okaniwa
    • Masanori Okaniwa
    • C07D513/04A61K31/4365
    • C07D513/04
    • A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity. In formula (I), R1 represents an optionally substituted C1-6 alkyl, etc.; X represents —O— or —NR2— (wherein R2 represents a hydrogen atom or a C1-6 alkyl); Y represents a group represented by formula 2 (2i or 2ii) (wherein ring A represents an optionally substituted benzene ring; Z represents a group represented by (1) —NR3CO—W1—, (2) —NR3CO—W1—O—, (3) —NR3CO—W1—O—W2—, (4) —NR3CO—W1—S—, (5) —NR3CO—W1—NR4—, (6) —NR3COO—, (7) —NR3COO—W1—, (8) —NR3CO—CO—, or (9) —NR3CONR4— (wherein R3 and R4 each represents a hydrogen atom, etc., and W1 and W2 each represents an optionally substituted C1-6 alkylene, etc.); and R5 represents an optionally substituted five- or six-membered ring group.
    • 由式(I)表示的化合物或其盐具有强的Raf抑制活性。 在式(I)中,R 1表示任选取代的C 1-6烷基等; X表示-O-或-NR2-(其中R2表示氢原子或C1-6烷基); Y表示由式2(2i或2ii)表示的基团(其中环A表示任选取代的苯环; Z表示由(1)-NR 3 CO-W 1表示的基团,(2)-NR 3 CO-W1-O-, (3)-NR3CO-W1-O-W2-,(4)-NR3CO-W1-S-,(5)-NR3CO-W1-NR4-,(6)-NR3COO-,(7)-NR3COO-W1- ,(8)-NR 3 CO-CO-或(9)-NR 3 CONR 4 - (其中R 3和R 4各自表示氢原子等,并且W 1和W 2各自表示任选取代的C 1-6亚烷基等);和 R5表示任选取代的五元或六元环基团。
    • 8. 发明申请
    • HETEROCYCLIC COMPOUND AND USE THEREOF
    • 杂环化合物及其用途
    • US20110237620A1
    • 2011-09-29
    • US13132253
    • 2009-11-30
    • Masanori Okaniwa
    • Masanori Okaniwa
    • A61K31/437C07D513/04A61K31/444A61K31/4545A61P35/00
    • C07D513/04
    • A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity. In formula (I), R1 represents an optionally substituted C1-6 alkyl, etc.; X represents —O— or —NR2— (wherein R2 represents a hydrogen atom or a C1-6 alkyl); Y represents a group represented by formula 2 (2ii or 2ii) (wherein ring A represents an optionally substituted benzene ring; Z represents a group represented by (1) —NR3CO—W1—, (2) —NR3CO—W1—O—, (3) —NR3CO—W1—O—W2—, (4) —NR3CO—W1—S—, (5) —NR3CO—W1—NR4—, (6) —NR3COO—, (7) —NR3COO—W1—, (8) —NR3CO—CO—, or (9) —NR3CONR4— (wherein R3 and R4 each represents a hydrogen atom, etc., and W1 and W2 each represents an optionally substituted C1-6 alkylene, etc.); and R5 represents an optionally substituted five- or six-membered ring group.
    • 由式(I)表示的化合物或其盐具有强的Raf抑制活性。 在式(I)中,R 1表示任选取代的C 1-6烷基等; X表示-O-或-NR2-(其中R2表示氢原子或C1-6烷基); Y表示由式2(2ii或2ii)表示的基团(其中环A表示任选取代的苯环; Z表示由(1)-NR 3 CO-W 1表示的基团,(2)-NR 3 CO-W1-O-, (3)-NR3CO-W1-O-W2-,(4)-NR3CO-W1-S-,(5)-NR3CO-W1-NR4-,(6)-NR3COO-,(7)-NR3COO-W1- ,(8)-NR 3 CO-CO-或(9)-NR 3 CONR 4 - (其中R 3和R 4各自表示氢原子等,并且W 1和W 2各自表示任选取代的C 1-6亚烷基等);和 R5表示任选取代的五元或六元环基团。