Anti-angiogenesis methods
    3.
    发明申请
    Anti-angiogenesis methods 审中-公开
    抗血管生成方法

    公开(公告)号:US20050119278A1

    公开(公告)日:2005-06-02

    申请号:US10930065

    申请日:2004-08-30

    摘要: A method for inhibiting cell proliferation, cell migration, or tube formation induced by an angiogenic factor. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: wherein A is H or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

    摘要翻译: 一种抑制血管生成因子诱导的细胞增殖,细胞迁移或管形成的方法。 该方法包括向有需要的受试者施用有效量的下式化合物:其中A为H或其中n为0,1,2或3; Ar 1,Ar 2和Ar 3各自独立地是苯基,噻吩基,呋喃基,吡咯基,吡啶基或嘧啶基; R 1,R 2,R 3,R 4,R 5,和/或R 3中的每一个 >和R 6独立地是R,硝基,卤素,C(O)OR,C(O)SR,C(O)NRR',(CH 2) (CH 2)m,或(CH 2)m SR,(CH 2 2)m, C(O)OR(CH 2 CH 2)m C(O)OR(CH 2) ,(CH 2 CH 2)m CHO,(CH 2 CH 2)m CH或NOR,或R 1, 1个和R 2个在一起,R 3和R 4一起,或者R 5和R 5 一起是O(CH 2)2 O,其中R和R'各自独立地是H,烷基,芳基, 杂芳基,环基或杂环基; m为0,1,2,3,4,5或6,n为0,1,2或3。

    Cancer treatment
    5.
    发明申请
    Cancer treatment 审中-公开
    癌症治疗

    公开(公告)号:US20050209252A1

    公开(公告)日:2005-09-22

    申请号:US11132756

    申请日:2005-05-18

    摘要: This invention relates to a method for treating cancer including administrating to a subject in need thereof an effective amount of a compound of the formula: wherein, A is H or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, (CH2)mC(O)N(OR)R′, N(OR)R′, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

    摘要翻译: 本发明涉及一种治疗癌症的方法,包括向有需要的受试者施用有效量的下式化合物:其中A为H或Ar 1,Ar 2的每一个 R 3和R 3独立地是苯基,噻吩基,呋喃基,吡咯基,吡啶基或嘧啶基; R 1,R 2,R 3,R 4,R 5,和/或R 3中的每一个 >和R 6独立地是R,硝基,卤素,C(O)OR,C(O)SR,C(O)NRR',(CH 2) (CH 2)m,或(CH 2)m SR,(CH 2 2)m, C(O)OR(CH 2 CH 2)m C(O)OR(CH 2) ,(CH 2 CH 2)m CHO,(CH 2 CH 2)m CH,或CH 2,(CH 3) C(O)N(OR)R',N(OR)R'或R 1和R 2' 一起,R 3和R 4一起,或者R 5和R 6一起是O(CH 其中R和R'各自独立地是H或C 1〜C 6, 烷基; m为0,1,2,3,4,5或6,n为0,1,2或3。

    Cancer chemotherapy
    6.
    发明申请
    Cancer chemotherapy 审中-公开
    癌症化疗

    公开(公告)号:US20070149554A1

    公开(公告)日:2007-06-28

    申请号:US11643103

    申请日:2006-12-21

    摘要: A method for treating cancer, which includes administrating to a subject in need thereof an effective amount of a chemotherapeutic agent and an effective amount of a compound of the formula: in which, A is H or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, (CH2)mC(O)N(OR)R′, N(OR)R′, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

    摘要翻译: 一种治疗癌症的方法,其包括向有需要的受试者施用有效量的化学治疗剂和有效量的下式化合物:其中A为H或Ar 1 / Ar 2,Ar 3和Ar 3独立地是苯基,噻吩基,呋喃基,吡咯基,吡啶基或嘧啶基; R 1,R 2,R 3,R 4,R 5,和/或R 3中的每一个 >和R 6独立地是R,硝基,卤素,C(O)OR,C(O)SR,C(O)NRR',(CH 2) (CH 2)m,或(CH 2)m SR,(CH 2 2)m, C(O)OR(CH 2 CH 2)m C(O)OR(CH 2) ,(CH 2 CH 2)m CHO,(CH 2 CH 2)m CH,或CH 2,(CH 3) C(O)N(OR)R',N(OR)R'或R 1和R 2' 一起,R 3和R 4一起,或者R 5和R 6一起是O(CH 其中R和R'各自独立地是H或C 1〜C 6, 烷基; m为0,1,2,3,4,5或6,n为0,1,2或3。

    Angiogenesis inhibitors
    7.
    发明申请
    Angiogenesis inhibitors 审中-公开
    血管生成抑制剂

    公开(公告)号:US20070142449A1

    公开(公告)日:2007-06-21

    申请号:US11648952

    申请日:2007-01-03

    摘要: A method for treating an angiogenesis-related disorder or cancer. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: Each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC)O)OR, (CH2)mCHO, (CH2)mCH═NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

    摘要翻译: 一种治疗血管生成相关病症或癌症的方法。 该方法包括向有需要的受试者施用有效量的下式化合物:Ar 1,Ar 2和Ar 3中的每一个, 独立地是苯基,噻吩基,呋喃基,吡咯基,吡啶基或嘧啶基; R 1,R 2,R 3,R 4,R 5,和/或R 3中的每一个 >和R 6独立地是R,硝基,卤素,C(O)OR,C(O)SR,C(O)NRR',(CH 2) (CH 2)m,或(CH 2)m SR,(CH 2 2)m, N,NRR',(CH 2 CH 2)m CN,(CH 2 CH 2)m C(O)OR ,(CH 2 CH 2)m CHO,(CH 2 CH 2)m CH或NOR,或R 1, 1个和R 2个在一起,R 3和R 4一起,或者R 5和R 5 一起是O(CH 2 CH 2)m O,其中R和R'各自独立地是H或C 1 -C 6烷基, C 1 -C 6烷基; m为0,1,2,3,4,5或6,n为0,1,2或3。

    Methods of treating sepsis
    8.
    发明授权
    Methods of treating sepsis 失效
    治疗败血症的方法

    公开(公告)号:US06943186B2

    公开(公告)日:2005-09-13

    申请号:US10350794

    申请日:2003-01-24

    摘要: The present invention features a method for treating sepsis. The method includes administrating to a subject in need thereof an effective amount of a fused pyrazolyl compound of formula (I): A is H, C1˜C6 alkyl, or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, pyridinyl, thienyl, furyl, or pyrrolyl; and each of R1, R2, R3, R4, R5, and R6, independently, is XYZ; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)1-6O; in which X is a bond or C1˜C6 alkylene, Y is a bond, O, S, OC(O), OC(O)(CH2)1-6C(O)O, C(O)O, C(O)S, C(O)NH, C(O)NC1˜C6 alkyl, NH, or NC1˜C6 alkyl, and Z is H, halogen, CN, NO2, or C1˜C6 alkyl; and provided that one of R3 and R4 is not H.

    摘要翻译: 本发明的特征在于一种治疗败血症的方法。 该方法包括向有需要的受试者施用有效量的式(I)的稠合吡唑基化合物:A是H,C 1 -C 6烷基,或 其中n为0,1,2或3; Ar 1,Ar 2和Ar 3各自独立地是苯基,吡啶基,噻吩基,呋喃基或吡咯基; 并且R 1,R 2,R 3,R 4,R 5, SUB>和R 6独立地是XYZ; 或R 1和R 2共同在一起,R 3和R 4一起,或R 5, / SUB和R 6一起是O(CH 2)2 - 其中X是一个键或C 1 -C 6亚烷基,Y是一个键,O,S,OC(O),OC(O)(CH

    Preferential inhibition of release of pro-inflammatory cytokines
    9.
    发明授权
    Preferential inhibition of release of pro-inflammatory cytokines 失效
    优先抑制促炎细胞因子的释放

    公开(公告)号:US07754751B2

    公开(公告)日:2010-07-13

    申请号:US11080384

    申请日:2005-03-15

    CPC分类号: A61K31/4162 A61K31/415

    摘要: A method for preferentially inhibiting release of pro-inflammatory cytokines over release of anti-inflammatory cytokines using a fused pyrazolyl compound of formula (I): A is R or in which R is H, alkyl, aryl, cyclyl, heteroaryl, or heterocyclyl; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is R′, nitro, halogen, —C(O)—OR′, —C(O)—SR′, —C(O)—NR′R″, —(CH2)mOR′, —(CH2)mSR′, —(CH2)mNR′R″, —(CH2)mCN, —(CH2)mC(O)—OR′, —(CH2)mC(O)H, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are —O(CH2)nO—, in which each of R′ and R″, independently, is H, alkyl, cyclyl, aryl, heteroaryl, heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6; and n is 1, 2, or 3. This invention also covers a method of inhibiting activity of NF-κB with such a compound.

    摘要翻译: 使用式(I)的稠合吡唑基化合物优先抑制促炎细胞因子释放超过抗炎细胞因子释放的方法:A是R或其中R是H,烷基,芳基,环基,杂芳基或杂环基; Ar 1,Ar 2和Ar 3各自独立地是苯基,噻吩基,呋喃基或吡咯基; R 1,R 2,R 3,R 4,R 5和R 6各自独立地是R',硝基,卤素,-C(O)-OR', - C(O)-SR' “(CH 2)m R”, - (CH 2)m SRR', - (CH 2)m NR R', - (CH 2)m CN, - (CH 2)m C(O) (O)H,或R 1和R 2一起,R 3和R 4一起,或者R 5和R 6一起是-O(CH 2)n O-,其中R'和R“各自独立地是H,烷基,环基,芳基 ,杂芳基,杂环基; m为0,1,2,3,4,5或6; 并且n为1,2或3.本发明还涵盖了用这种化合物抑制NF-κB活性的方法。

    Angiogenesis inhibitors
    10.
    发明授权
    Angiogenesis inhibitors 有权
    血管生成抑制剂

    公开(公告)号:US07166293B2

    公开(公告)日:2007-01-23

    申请号:US10147445

    申请日:2002-05-16

    IPC分类号: A01N25/00 A01N25/32

    摘要: A method for treating an angiogenesis-related disorder. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: Each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

    摘要翻译: 一种治疗血管生成相关病症的方法。 该方法包括向有需要的受试者施用有效量的下式化合物:Ar 1,Ar 2和Ar 3中的每一个, 独立地是苯基,噻吩基,呋喃基,吡咯基,吡啶基或嘧啶基; R 1,R 2,R 3,R 4,R 5,和/或R 3中的每一个 >和R 6独立地是R,硝基,卤素,C(O)OR,C(O)SR,C(O)NRR',(CH 2) (CH 2)m,或(CH 2)m SR,(CH 2 2)m, C(O)OR(CH 2 CH 2)m C(O)OR(CH 2) ,(CH 2 CH 2)m CHO,(CH 2 CH 2)m CH或NOR,或R 1, 1个和R 2个在一起,R 3和R 4一起,或者R 5和R 5 一起是O(CH 2 CH 2)m O,其中R和R'各自独立地是H或C 1 -C 6烷基, C 1 -C 6烷基; m为0,1,2,3,4,5或6,n为0,1,2或3。