- 专利标题: ANTI-PROLIFERATIVE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE THEREOF
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申请号: US12436004申请日: 2009-05-05
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公开(公告)号: US20090291922A1公开(公告)日: 2009-11-26
- 发明人: Xiaoqin Cheng , Gary P. Cook , Manoj C. Desai , Edward Doerffler , Gong-Xin He , Choung U. Kim , William A. Lee , John C. Rohloff , Jianying Wang , Zheng-Yu Yang
- 申请人: Xiaoqin Cheng , Gary P. Cook , Manoj C. Desai , Edward Doerffler , Gong-Xin He , Choung U. Kim , William A. Lee , John C. Rohloff , Jianying Wang , Zheng-Yu Yang
- 申请人地址: US CA Foster City
- 专利权人: Gilead Sciences, Inc.
- 当前专利权人: Gilead Sciences, Inc.
- 当前专利权人地址: US CA Foster City
- 主分类号: A61K31/675
- IPC分类号: A61K31/675 ; C07D473/16 ; A61K31/52 ; C07F9/02
摘要:
Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ═O, —O(RX), ═S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ═O, —O(R4), ═S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4)(R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, —SC(R3b)(N(R4)(R4)), —N(R4)C(R3b)R4, —N(R4)C(R3b)OR4, —N(R4)C(R3b) (N(R4)(R4)), W3 or —R5W3; R3d is —C(R3b)R4, —C(R3b)OR4, —C(R3b)W3, —C(R3b)OW3 or —C(R3b)(N(R4)(R4)); R4 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; R5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W3 is W4 or W5; W4 is R6, —C(R3b)R6, —C(R3b)W5, —SOM2R6, or —SOM2W5, wherein R6 is R4 wherein each R4 is substituted with 0 to 3 R3 groups; W5 is carbocycle or heterocycle wherein W5 is independently substituted with 0 to 3 R2 groups; and M2 is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
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