会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明申请
    • ANTI-PROLIFERATIVE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE THEREOF
    • 抗增生化合物,组合物及其使用方法
    • WO2007002912A3
    • 2007-06-28
    • PCT/US2006025726
    • 2006-06-29
    • GILEAD SCIENCES INCCHENG XIAOQINCOOK GARY PDESAI MANOJ CDOERFFLER EDWARDHE GONG-XINKIM CHOUNG ULEE WILLIAM AROHLOFF JOHN CWANG JIANYINGYANG ZHENG-YU
    • CHENG XIAOQINCOOK GARY PDESAI MANOJ CDOERFFLER EDWARDHE GONG-XINKIM CHOUNG ULEE WILLIAM AROHLOFF JOHN CWANG JIANYINGYANG ZHENG-YU
    • C07F9/6561A61K31/66A61K31/675A61P31/12
    • C07F9/65616Y02P20/55
    • Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y 1A and Y 1B are independently Y 1 ; R X1 is R X ; R X2 is alkenyl of 2 to 18 carbon atoms or alkynyl of 2 to 18 carbon atoms; Y 1 is = O, -O(R X ), =S, -N(R X ), -N(O)(R X ), -N(OR X ), -N(O)(OR X ), or -N(N(R X )(R X )); R X is independently R 1 , R 2 , R 4 , W 3 , or a protecting group; R 1 is independently -H or alkyl of 1 to 18 carbon atoms; R 2 is independently R 3 or R 4 wherein each R 4 is independently substituted with 0 to 3 R 3 groups or taken together at a carbon atom, two R 2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R 3 groups; R 3 is R 3a , R 3b , R 3c or R 3d , provided that when R 3 is bound to a heteroatom, then R 3 is R 3c or R 3d ; R 3a is -H, -F, -Cl, -Br, -I, -CF 3 , -CN, N 3 , -NO 2 or -OR 4 ; R 3b is = O, -O(R 4 ), =S, -N(R 4 ), -N(O)(R 4 ), -N(OR 4 ), -N(O)(OR 4 ), or -N(N(R 4 )(R 4 )); 3c is -R 4 , -N(R 4 )(R 4 ), -SR 4 , -S(O)R 4 , -S(O) 2 R 4 , -S(O)(OR 4 ), -S(O) 2 (OR 4 ), -OC(R 3b )R 4 , -OC(R 3b )OR 4 , -OC(R 3b )(N(R 4 )(R 4 )), -SC(R 3b )R 4 , -SC(R 3b )OR 4 , -SC(R 3b )(N(R 4 )(R 4 )), -N(R 4 )C(R 3b )R 4 , -N(R 4 )C(R 3b )OR 4 , -N(R 4 )C(R 3b )(N(R 4 )(R 4 )), W 3 or -R 5 W 3 ; R 3d is -C(R 3b )R 4 , -C(R 3b )OR 4 , -C(R 3b )W 3 , -C(R 3b )OW 3 or -C(R 3b )(N(R 4 )(R 4 )); R 4 is -H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R 5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W 3 is W 4 or W 5 ; W 4 is R 6 , -C(R 3b )R 6 , -C(R 3b )W 5 , -SO M2 R 6 , or -SO M2 W 5 , wherein R 6 is R 4 wherein each R 4 is substituted with O to 3 R 3 groups; W 5 is carbocycle or heterocycle wherein W 5 is independently substituted with O to 3 R 2 groups; and M2 is 0, 1 or 2; or pharmaceutically acceptable salts thereof.
    • 描述了式I的化合物和组合物,其可用作抗增殖剂,特别是抗HPV,其中:Y 1A和Y 1B独立地为Y, 1 ; R X1是R X; R 2 X 2是2至18个碳原子的链烯基或2至18个碳原子的炔基; Y 1是= O,-O(R X),= S,-N(R X)X - , - N(O)( N(O,X),-N(O)(OR X)或-N(N(R' SUP> X )(R X )); R X独立地为R 1,R 2,R 4,W 3, ,或保护基团; R 1独立地是-H或1至18个碳原子的烷基; R 2独立地是R 3或R 4,其中每个R 4独立地被0至3个R 3取代, SUP> 3个或3个碳原子一起取代,2个R 2基团形成3〜8个碳环,该环可以被0〜3个R 3 组 R 3是R 3a,R 3b,R 3c或R i,R 3, 条件是当R 3与杂原子结合时,R 3是R 3c或R 3d; R 3a是-H,-F,-Cl,-Br,-I,-CF 3,-CN,N 3 - , - NO 2或-OR 4; R 3是= O,-O(R 4),= S,-N(R 4), - N(O)( (OR 4),-N(OR 4), - N(O)(OR 4)或-N(N(R' SUP> 4 )(R 4 )); (S 4),-S(R 4),-SR 4,-S(R 4) 4,-S(O)R 4,-S(O)2 R 4,-S(O)( 或(S)4),-S(O)2(OR 4),-OC(R 3b)R -OC(R 3b)或OR 4,-OC(R 3b)(N(R 3) (R 4)),-SC(R 3b)R 4,-SC(R SUP) (R 3)(R 4)(R 4)(R 4) /(S)S),-N(R 4)S(R 3b)R 4,-N(R 4) C(R 3b)或者4,-N(R 4)C(R 3) )(N(R 4)(R 4)),W 3或-R 5 W > 3 ; R 3 d 3是-C(R 3b)R 4,-C(R 3b)或 - -C(R 3b)W 3,-C(R 3b)OW 3 O, >或-C(R 3b)(N(R 4))(R 4)); R 4是-H或1至18个碳原子的烷基,2至18个碳原子的烯基或2至18个碳原子的炔基; R 5是1至18个碳原子的亚烷基,2至18个碳原子的亚烯基或2至18个碳原子的亚炔基; W 3或W 5是W 4或W 5; R 4是R 6,-C(R 3b)R 6,-C(R'), 或3个或更多个,其中,R 1,R 2,R 3,R 5, 其中R 6是R 4,其中每个R 4被0至3个R 3取代, / SUP>组 W 5是碳环或杂环,其中W 5独立地被O至3个R 2基团取代; M2为0,1或2; 或其药学上可接受的盐。
    • 3. 发明申请
    • ANTI-PROLIFERATIVE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE THEREOF
    • 抗增殖化合物,组合物及其使用方法
    • WO2007002912A2
    • 2007-01-04
    • PCT/US2006/025726
    • 2006-06-29
    • GILEAD SCIENCES, INC.CHENG, XiaoqinCOOK, Gary, P.DESAI, Manoj, C.DOERFFLER, EdwardHE, Gong-xinKIM, Choung, U.LEE, William, A.ROHLOFF, John, C.WANG, JianyingYANG, Zheng-Yu
    • CHENG, XiaoqinCOOK, Gary, P.DESAI, Manoj, C.DOERFFLER, EdwardHE, Gong-xinKIM, Choung, U.LEE, William, A.ROHLOFF, John, C.WANG, JianyingYANG, Zheng-Yu
    • C07F9/6561A61P31/12A61K31/66
    • C07F9/65616Y02P20/55
    • Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y 1A and Y 1B are independently Y 1 ; R X1 is R X ; R X2 is alkenyl of 2 to 18 carbon atoms or alkynyl of 2 to 18 carbon atoms; Y 1 is = O, -O(R X ), =S, -N(R X ), -N(O)(R X ), -N(OR X ), -N(O)(OR X ), or -N(N(R X )(R X )); R X is independently R 1 , R 2 , R 4 , W 3 , or a protecting group; R 1 is independently -H or alkyl of 1 to 18 carbon atoms; R 2 is independently R 3 or R 4 wherein each R 4 is independently substituted with 0 to 3 R 3 groups or taken together at a carbon atom, two R 2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R 3 groups; R 3 is R 3a , R 3b , R 3c or R 3d , provided that when R 3 is bound to a heteroatom, then R 3 is R 3c or R 3d ; R 3a is -H, -F, -Cl, -Br, -I, -CF 3 , -CN, N 3 , -NO 2 or -OR 4 ; R 3b is = O, -O(R 4 ), =S, -N(R 4 ), -N(O)(R 4 ), -N(OR 4 ), -N(O)(OR 4 ), or -N(N(R 4 )(R 4 )); 3c is -R 4 , -N(R 4 )(R 4 ), -SR 4 , -S(O)R 4 , -S(O) 2 R 4 , -S(O)(OR 4 ), -S(O) 2 (OR 4 ), -OC(R 3b )R 4 , -OC(R 3b )OR 4 , -OC(R 3b )(N(R 4 )(R 4 )), -SC(R 3b )R 4 , -SC(R 3b )OR 4 , -SC(R 3b )(N(R 4 )(R 4 )), -N(R 4 )C(R 3b )R 4 , -N(R 4 )C(R 3b )OR 4 , -N(R 4 )C(R 3b )(N(R 4 )(R 4 )), W 3 or -R 5 W 3 ; R 3d is -C(R 3b )R 4 , -C(R 3b )OR 4 , -C(R 3b )W 3 , -C(R 3b )OW 3 or -C(R 3b )(N(R 4 )(R 4 )); R 4 is -H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R 5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W 3 is W 4 or W 5 ; W 4 is R 6 , -C(R 3b )R 6 , -C(R 3b )W 5 , -SO M2 R 6 , or -SO M2 W 5 , wherein R 6 is R 4 wherein each R 4 is substituted with O to 3 R 3 groups; W 5 is carbocycle or heterocycle wherein W 5 is independently substituted with O to 3 R 2 groups; and M2 is 0, 1 or 2; or pharmaceutically acceptable salts thereof.
    • 描述了式I的化合物和组合物,其可用作抗增殖剂,特别是抗HPV,其中:Y 1A和Y 1B表示抗体, sup独立地是Y 1 ; R X1是R X; R X2是2至18个碳原子的链烯基或2至18个碳原子的炔基; Y 1 = O,-O(R X),= S,-N(R X), - N(O)( -N(OR X),-N(O)(OR X)或-N(N(R X) SUP> X )(R X )); R X独立地为R 1,R 2,R 4,W 3,R 4,R 4,R 4, ,或保护基团; R 1独立地为-H或1-18个碳原子的烷基; R 2独立地为R 3或R 4,其中每个R 4独立地被0至3个R 4取代, 两个R 2基团形成3至8个碳原子的环并且该环可以被0至3个R 3取代 组; R 3是R 3a,R 3b,R 3c或R 3d,其中R 3a, 条件是当R 3 3与一个杂原子结合时,则R 3是R 3c或R 3d; R 3a是-H,-F,-Cl,-Br,-I,-CF 3,-CN,N 3, - NO <2>或-OR <4>; (R 4), - N(R 4), - N(O)( -N(OR 4), - N(O)(OR 4)或-N(N(R 4) SUP> 4 )(R 4 )); 3c是-R 4,-N(R 4)(R 4),-SR 5, (O)R 4,-S(O)2 R 4,-S(O)( OR 4),-S(O)2(OR 4),-OC(R 3b)R (R(R 3)4,-OC(R 3b)OR 4,-OC(R 3b) (R 4)),-SC(R 3b)R 4,-SC(R sup) (R(R 4))(R 4)(R 4)R 4(R 4) -N(R 4)C(R 3b)R 4,-N(R 4) (R 3b)OR 4,-N(R 4)C(R 3b) )(N(R 4)(R 4))),W 3或-R 5 W 3 ; R 3d为-C(R 3b)R 4,-C(R 3b)OR, 4 -C(R 3b)W 3,-C(R 3b)OW 3-sup (R(R 4))或-C(R 3b)(N(R 4)(R 4)); R 4是-H,或1至18个碳原子的烷基,2至18个碳原子的烯基或2至18个碳原子的炔基; R 5是1-18个碳原子的亚烷基,2-18个碳原子的亚烯基或2-18个碳原子的亚炔基; W 3 是W 或W 5 ; W 4是R 6,-C(R 3b)R 6,-C(R 5) 3b)W 5,-SO 2 R 6或-SO 2 M W 组; W 5是碳环或杂环,其中W 5独立地被O至3个R 2基团取代; M2是0,1或2; 或其药学上可接受的盐。