公开(公告)号：US20090291922A1

公开(公告)日：2009-11-26

申请号：US12436004

申请日：2009-05-05

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

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

IPC分类号： A61K31/675 ,  C07D473/16 ,  A61K31/52 ,  C07F9/02

CPC分类号： C07F9/65616 ,  Y02P20/55

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.

公开(公告)号：US08268802B2

公开(公告)日：2012-09-18

申请号：US12436004

申请日：2009-05-05

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

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

IPC分类号： C07F9/6561 ,  A61K31/675 ,  A61P31/20

CPC分类号： C07F9/65616 ,  Y02P20/55

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.

公开(公告)号：US08088754B2

公开(公告)日：2012-01-03

申请号：US12388295

申请日：2009-02-18

申请人： Xiaoqin Cheng ,  Gary P. Cook ,  Gong-Xin He ,  Choung U. Kim ,  John C. Rohloff ,  Jianying Wang ,  Zheng-Yu Yang

发明人： Xiaoqin Cheng ,  Gary P. Cook ,  Gong-Xin He ,  Choung U. Kim ,  John C. Rohloff ,  Jianying Wang ,  Zheng-Yu Yang

IPC分类号： C07F9/6561 ,  A61K31/675 ,  A61P31/20

CPC分类号： C07F9/65616 ,  Y02P20/55

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)); and pharmaceutically acceptable salts thereof.

摘要翻译： 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：Y1A和Y1B独立地为Y1; RX1和RX2独立为RX; Y1是ΟO，-O（RX），≡S，-N（RX），-N（O）（RX），-N（ORX），-N（O）（ORX） RX）（RX））; 及其药学上可接受的盐。

公开(公告)号：US07553825B2

公开(公告)日：2009-06-30

申请号：US11026303

申请日：2004-12-29

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

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

IPC分类号： C07F9/6561 ,  A61K31/675 ,  A61P31/20

CPC分类号： C07F9/65616 ,  Y02P20/55

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.

公开(公告)号：US20090149400A1

公开(公告)日：2009-06-11

申请号：US12388295

申请日：2009-02-18

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

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

IPC分类号： A61K31/675 ,  C07F9/6512 ,  A61K31/7056 ,  A61P31/12

CPC分类号： C07F9/65616 ,  Y02P20/55

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.

公开(公告)号：US07649015B2

公开(公告)日：2010-01-19

申请号：US10423496

申请日：2003-04-25

申请人： Murty N. Arimili ,  Xiaowu Chen ,  Maria Fardis ,  Gong-Xin He ,  Haolun Jin ,  Choung U. Kim ,  William A. Lee ,  Kuei-Ying Lin ,  Hongtao Liu ,  Richard L. Mackman ,  Michael L. Mitchell ,  Hyung-Jung Pyun ,  Mark Sparacino ,  Sundaramoorthi Swaminathan ,  Jianying Wang ,  Matthew A. Williams ,  Lianhong Xu ,  Zheng-Yu Yang ,  Richard H. Yu ,  Jiancun Zhang ,  Lijun Zhang

发明人： Murty N. Arimili ,  Xiaowu Chen ,  Maria Fardis ,  Gong-Xin He ,  Haolun Jin ,  Choung U. Kim ,  William A. Lee ,  Kuei-Ying Lin ,  Hongtao Liu ,  Richard L. Mackman ,  Michael L. Mitchell ,  Hyung-Jung Pyun ,  Mark Sparacino ,  Sundaramoorthi Swaminathan ,  Jianying Wang ,  Matthew A. Williams ,  Lianhong Xu ,  Zheng-Yu Yang ,  Richard H. Yu ,  Jiancun Zhang ,  Lijun Zhang

IPC分类号： A61K31/343 ,  C07F9/28

CPC分类号： A61K31/66 ,  A61K31/675 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D231/20 ,  C07D233/42 ,  C07D239/49 ,  C07D239/80 ,  C07D243/04 ,  C07D265/18 ,  C07D307/68 ,  C07D401/06 ,  C07D403/06 ,  C07D471/14 ,  C07D491/04 ,  C07F9/4006 ,  C07F9/58 ,  C07F9/645 ,  C07F9/6506 ,  C07F9/650905 ,  C07F9/650947 ,  C07F9/6512 ,  C07F9/65128 ,  C07F9/65335 ,  C07F9/65515 ,  C07F9/65583 ,  C07F9/6561 ,  C12N9/16 ,  C12Q1/18 ,  C12Q1/37 ,  C12Q1/44 ,  C40B40/04 ,  G01N33/5038 ,  G01N2333/16 ,  G01N2500/04

摘要： Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.

摘要翻译： 公开了具有用作治疗剂和其它工业目的的具有HIV蛋白酶抑制性质的膦酸酯取代的化合物。 组合物抑制HIV蛋白酶活性和/或可用于治疗AIDS和其它抗病毒感染以及用于检测HIV蛋白酶的测定。

公开(公告)号：US20060030545A1

公开(公告)日：2006-02-09

申请号：US11170247

申请日：2005-06-29

申请人： Xiaoqin Cheng ,  Gary Cook ,  Manoj Desai ,  Edward Doerffler ,  Gong-Xin He ,  Choung Kim ,  William Lee ,  John Rohloff ,  Jianying Wang ,  Zheng-Yu Yang

发明人： Xiaoqin Cheng ,  Gary Cook ,  Manoj Desai ,  Edward Doerffler ,  Gong-Xin He ,  Choung Kim ,  William Lee ,  John Rohloff ,  Jianying Wang ,  Zheng-Yu Yang

IPC分类号： A61K31/675 ,  C07F9/6512

CPC分类号： C07F9/65616 ,  Y02P20/55

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 is RX; RX2 is alkenyl of 2 to 18 carbon atoms or alkynyl of 2 to 18 carbon atoms; 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; or pharmaceutically acceptable salts thereof.

公开(公告)号：US20070010489A1

公开(公告)日：2007-01-11

申请号：US10511998

申请日：2003-04-25

申请人： Murty Arimilli ,  Mark Becker ,  Clifford Bryant ,  James Chen ,  Xiaowu Chen ,  Azar Dastgah ,  Maria Fardis ,  Gong-Xin He ,  Haolun Jin ,  Choung Kim ,  William Lee ,  Christopher Lee ,  Kuei-Ying Lin ,  Hongtao Liu ,  Richard Mackman ,  Michael Mitchell ,  Peter Nelson ,  Hyung-Jung Pyun ,  Tanisha Rowe ,  Mark Sparacino ,  Sundaramoorthi Swaminathan ,  James Tario ,  Jianying Wang ,  Matthew Wiliams ,  Lianhong Xu ,  Zheng-Yu Yang ,  Richard Yu ,  Jiancun Zhang ,  Lijun Zhang

发明人： Murty Arimilli ,  Mark Becker ,  Clifford Bryant ,  James Chen ,  Xiaowu Chen ,  Azar Dastgah ,  Maria Fardis ,  Gong-Xin He ,  Haolun Jin ,  Choung Kim ,  William Lee ,  Christopher Lee ,  Kuei-Ying Lin ,  Hongtao Liu ,  Richard Mackman ,  Michael Mitchell ,  Peter Nelson ,  Hyung-Jung Pyun ,  Tanisha Rowe ,  Mark Sparacino ,  Sundaramoorthi Swaminathan ,  James Tario ,  Jianying Wang ,  Matthew Wiliams ,  Lianhong Xu ,  Zheng-Yu Yang ,  Richard Yu ,  Jiancun Zhang ,  Lijun Zhang

IPC分类号： A61K31/663 ,  C07F9/6515 ,  C07F9/6512

CPC分类号： A61K31/66 ,  A61K31/675 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D231/20 ,  C07D233/42 ,  C07D239/49 ,  C07D239/80 ,  C07D243/04 ,  C07D265/18 ,  C07D307/68 ,  C07D401/06 ,  C07D403/06 ,  C07D471/14 ,  C07D491/04 ,  C07F9/4006 ,  C07F9/58 ,  C07F9/645 ,  C07F9/6506 ,  C07F9/650905 ,  C07F9/650947 ,  C07F9/6512 ,  C07F9/65128 ,  C07F9/65335 ,  C07F9/65515 ,  C07F9/65583 ,  C07F9/6561 ,  C12N9/16 ,  C12Q1/18 ,  C12Q1/37 ,  C12Q1/44 ,  C40B40/04 ,  G01N33/5038 ,  G01N2333/16 ,  G01N2500/04

摘要： Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit 5 HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.

摘要翻译： 公开了具有用作治疗剂和其它工业目的的具有HIV蛋白酶抑制性质的膦酸酯取代的化合物。 该组合物抑制5种HIV蛋白酶活性和/或用于治疗AIDS和其它抗病毒感染以及用于检测HIV蛋白酶的测定。

公开(公告)号：US20050239054A1

公开(公告)日：2005-10-27

申请号：US10740694

申请日：2003-12-22

申请人： Murty Arimilli ,  Mark Becker ,  Gabriel Birkus ,  Clifford Bryant ,  James Chen ,  Xiaowu Chen ,  Tomas Cihlar ,  Azar Dastgah ,  Eugene Eisenberg ,  Maria Fardis ,  Marcos Hatada ,  Gong-Xin He ,  Haolun Jin ,  Choung Kim ,  William Lee ,  Christopher Lee ,  Kuei-Ying Lin ,  Hongtao Liu ,  Richard MacKman ,  Martin McDermott ,  Michael Mitchell ,  Peter Nelson ,  Hyung-Jung Pyun ,  Tanisha Rowe ,  Mark Sparacino ,  Sundaramoorthi Swaminathan ,  James Tario ,  Jianying Wang ,  Matthew Williams ,  Lianhong Xu ,  Zheng-Yu Yang ,  Richard Yu ,  Jiancun Zhang ,  Lijun Zhang

发明人： Murty Arimilli ,  Mark Becker ,  Gabriel Birkus ,  Clifford Bryant ,  James Chen ,  Xiaowu Chen ,  Tomas Cihlar ,  Azar Dastgah ,  Eugene Eisenberg ,  Maria Fardis ,  Marcos Hatada ,  Gong-Xin He ,  Haolun Jin ,  Choung Kim ,  William Lee ,  Christopher Lee ,  Kuei-Ying Lin ,  Hongtao Liu ,  Richard MacKman ,  Martin McDermott ,  Michael Mitchell ,  Peter Nelson ,  Hyung-Jung Pyun ,  Tanisha Rowe ,  Mark Sparacino ,  Sundaramoorthi Swaminathan ,  James Tario ,  Jianying Wang ,  Matthew Williams ,  Lianhong Xu ,  Zheng-Yu Yang ,  Richard Yu ,  Jiancun Zhang ,  Lijun Zhang

IPC分类号： C12N9/99 ,  A61K31/4155 ,  A61K31/66 ,  A61K31/665 ,  A61K31/675 ,  A61P31/18 ,  A61P43/00 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D231/20 ,  C07D233/42 ,  C07D239/48 ,  C07D239/80 ,  C07D243/04 ,  C07D265/18 ,  C07D307/68 ,  C07D401/06 ,  C07D403/06 ,  C07D471/14 ,  C07D491/04 ,  C07F20060101 ,  C07F9/02 ,  C07F9/38 ,  C07F9/40 ,  C07F9/44 ,  C07F9/58 ,  C07F9/62 ,  C07F9/645 ,  C07F9/6506 ,  C07F9/6509 ,  C07F9/6512 ,  C07F9/653 ,  C07F9/6533 ,  C07F9/655 ,  C07F9/6558 ,  C07F9/6561 ,  C07F9/6584 ,  C12N9/16 ,  C12Q1/18 ,  C12Q1/37 ,  C12Q1/44 ,  C12Q1/70 ,  G01N33/04 ,  G01N33/50

CPC分类号： A61K31/66 ,  A61K31/675 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D231/20 ,  C07D233/42 ,  C07D239/49 ,  C07D239/80 ,  C07D243/04 ,  C07D265/18 ,  C07D307/68 ,  C07D401/06 ,  C07D403/06 ,  C07D471/14 ,  C07D491/04 ,  C07F9/4006 ,  C07F9/58 ,  C07F9/645 ,  C07F9/6506 ,  C07F9/650905 ,  C07F9/650947 ,  C07F9/6512 ,  C07F9/65128 ,  C07F9/65335 ,  C07F9/65515 ,  C07F9/65583 ,  C07F9/6561 ,  C12N9/16 ,  C12Q1/18 ,  C12Q1/37 ,  C12Q1/44 ,  C40B40/04 ,  G01N33/5038 ,  G01N2333/16 ,  G01N2500/04 ,  G01N2500/20

摘要： Methods are provided for identifying anti-HIV therapeutic compounds substituted with carboxyl ester or phosphonate ester groups. Libraries of such compounds are screened optionally using the novel enzyme GS-7340 Ester Hydrolase. Compositions and methods relating to GS-7340 Ester Hydrolase also are provided.

摘要翻译： 提供了用于鉴定被羧基酯或膦酸酯基取代的抗HIV治疗化合物的方法。 可以使用新型GS-7340酯水解酶来筛选这些化合物的文库。 还提供了与GS-7340酯水解酶有关的组合物和方法。

公开(公告)号：US20050222090A1

公开(公告)日：2005-10-06

申请号：US11026303

申请日：2004-12-29

申请人： Xiaqin Cheng ,  Gary Cook ,  Manoj Desai ,  Edward Doerffler ,  Gong-Xin He ,  Choung Kim ,  William Lee ,  John Rohloff ,  Jianying Wang ,  Zheng-Yu Yang

发明人： Xiaqin Cheng ,  Gary Cook ,  Manoj Desai ,  Edward Doerffler ,  Gong-Xin He ,  Choung Kim ,  William Lee ,  John Rohloff ,  Jianying Wang ,  Zheng-Yu Yang

IPC分类号： A61K31/66 ,  A61K31/675 ,  C07F9/44 ,  C07F9/6561

CPC分类号： C07F9/65616 ,  Y02P20/55

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.