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    • 2. 发明授权
    • Piperazinedione compounds
    • 哌嗪二酮化合物
    • US06635649B2
    • 2003-10-21
    • US09851077
    • 2001-05-08
    • Che-Ming TengHui-Po WangEric I. C. LiOn LeeJih-Hwa GuhHuei-Ting ChenYa-Bing FanYa-Lan Chen
    • Che-Ming TengHui-Po WangEric I. C. LiOn LeeJih-Hwa GuhHuei-Ting ChenYa-Bing FanYa-Lan Chen
    • A61K31496
    • C07D401/06C07D409/14
    • Piperazinedione compounds of the formula: Each of and and independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is R3O—(Ar)—B, in which B is CH(Rc) when is a single bond, or C(Rc) when is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; each of R1 and R2, independently, is H, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; and each of Ra, Rb, Rc, Rd, and Re, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, Ra and Rb taken together are cyclyl or heterocyclyl; and, also optionally, R1 and Ra or R1 and Rb taken together are cyclyl or heterocyclyl. Also disclosed is a method for treating tumor with the above described piperazinedione compounds.
    • 哌嗪二酮化合物,分别为:< CUSTOM-CHARACTER FILE =“US06635649-20031021-P00900.TIF”ALT =“custom character”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/ >和 或双键; 当是单键,或C(R a R b)当为双键时; 当是单键或C(R )”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00005”/>是双键; Ar是杂芳基; 且R 3为H,烷基,芳基,杂芳基,C(O)R d,C(O)OR d,C(O)NR d R e或SO 2 R d; R 1和R 2各自独立地是H,C(O)R d,C(O)OR d,C(O)NR d R e或SO 2 R ; R a,R b,R c,R d和R e各自独立地是H,烷基,芳基,杂芳基,环基或杂环基。 任选地,R 5和R b一起是环基或杂环基; 并且还可任选地,R 1和R 5'或R 1和R b一起是环基或杂环基。 还公开了用上述哌嗪二酮化合物治疗肿瘤的方法。
    • 3. 发明申请
    • Anti-angiogenesis methods
    • 抗血管生成方法
    • US20050119278A1
    • 2005-06-02
    • US10930065
    • 2004-08-30
    • Che-Ming TengSheng-Chu KuoFang-Yu LeeShiow-Lin PanJih-Hwa Guh
    • Che-Ming TengSheng-Chu KuoFang-Yu LeeShiow-Lin PanJih-Hwa Guh
    • A61K31/416A61K31/4745A61K31/519A61K31/4162A61K31/4439A61K31/506
    • A61K31/4745A61K31/416A61K31/519
    • 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.
    • 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。
    • 9. 发明授权
    • Preferential inhibition of release of pro-inflammatory cytokines
    • 优先抑制促炎细胞因子的释放
    • US07754751B2
    • 2010-07-13
    • US11080384
    • 2005-03-15
    • Che-Ming TengJih-Hwa GuhShiow-Lin PanSheng-Chu KuoFang-Yu Lee
    • Che-Ming TengJih-Hwa GuhShiow-Lin PanSheng-Chu KuoFang-Yu Lee
    • A01N43/56C07D231/10C07D231/12
    • A61K31/4162A61K31/415
    • 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.
    • 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。
    • 10. 发明授权
    • Angiogenesis inhibitors
    • 血管生成抑制剂
    • US07166293B2
    • 2007-01-23
    • US10147445
    • 2002-05-16
    • Che-Ming TengSheng-Chu KuoFang Yu LeeShiow-Lin PanJih-Hwa Guh
    • Che-Ming TengSheng-Chu KuoFang Yu LeeShiow-Lin PanJih-Hwa Guh
    • A01N25/00A01N25/32
    • A61K31/4162A61K31/416A61K31/4745A61K31/519
    • 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.
    • 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。