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1. 发明申请

WO2011156757A1 COMBINATION OF ANTI-HCV COMPOUNDS WITH RIBAVIRIN FOR THE TREATMENT OF HCV 审中-公开
标题翻译：抗HCV化合物与RIBAVIRIN的组合用于治疗HCV
公开(公告)号：WO2011156757A1
公开(公告)日：2011-12-15
申请号：PCT/US2011/040045
申请日：2011-06-10
申请人： GILEAD SCIENCES, INC. , DELANEY, William, E., IV , LEE, William, A. , OLDACH, David, W. , ROUSSEAU, Franck
发明人： DELANEY, William, E., IV , LEE, William, A. , OLDACH, David, W. , ROUSSEAU, Franck
IPC分类号： A61K31/4196 , A61K31/501 , A61K31/662 , A61K45/06
CPC分类号： A61K45/06 , A61K31/4196 , A61K31/501 , A61K31/662 , A61K2300/00
摘要： This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
摘要翻译：本发明涉及可用于治疗丙型肝炎病毒感染的治疗分子的组合。本发明涉及方法，用途，给药方案和组合物。

2. 发明申请

WO2005066189A1 PHOSPHONATES, MONOPHOSPHONAMIDATES, BISPHOSPHONAMIDATES FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：磷酸盐，单磷酰胺，治疗病毒性疾病的双磷酰胺
公开(公告)号：WO2005066189A1
公开(公告)日：2005-07-21
申请号：PCT/US2004/043969
申请日：2004-12-29
申请人： GILEAD SCIENCES, INC. , CHENG, Xiaqin , COOK, Gary, P. , DESAI, Manoj, C. , DOERFFLER, Edward , HE, Gong-Xin , KIM, Choung, U. , LEE, William, A. , ROHLOFF, John, C. , WANG, Jianying , YANG, Zheng-Yu
发明人： CHENG, Xiaqin , COOK, Gary, P. , DESAI, Manoj, C. , DOERFFLER, Edward , HE, Gong-Xin , KIM, Choung, U. , LEE, William, A. , ROHLOFF, John, C. , WANG, Jianying , YANG, Zheng-Yu
IPC分类号： C07F9/44
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.
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。

3. 发明申请

WO2004096286A2 ANTIVIRAL PHOSPHONATE ANALOGS 审中-公开
标题翻译：抗磷酸酯类似物
公开(公告)号：WO2004096286A2
公开(公告)日：2004-11-11
申请号：PCT/US2004/013063
申请日：2004-04-26
申请人： GILEAD SCIENCES, INC. , BOOJAMARA, Constantine, G. , CANNIZZARO, Carina, E. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , FARDIS, Maria , JIN, Haolun , HIRSCHMANN, Ralph, F. , HUANG, Alan, X. , KIM, Choung, U. , KIRSCHBERG, Thorsten, A. , LEE, Christopher, P. , LEE, William, A. , MACKMAN, Richard, L. , MARKEVITCH, David, Y. , OARE, David , PRASAD, Vidya, K. , PYUN, Hyung-Jung , RAY, Adrian, S. , SHERLOCK, Rosemarie , SWAMINATHAN, Sundaramoorthi , WATKINS, Will , ZHANG, Jennifer, R.
发明人： BOOJAMARA, Constantine, G. , CANNIZZARO, Carina, E. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , FARDIS, Maria , JIN, Haolun , HIRSCHMANN, Ralph, F. , HUANG, Alan, X. , KIM, Choung, U. , KIRSCHBERG, Thorsten, A. , LEE, Christopher, P. , LEE, William, A. , MACKMAN, Richard, L. , MARKEVITCH, David, Y. , OARE, David , PRASAD, Vidya, K. , PYUN, Hyung-Jung , RAY, Adrian, S. , SHERLOCK, Rosemarie , SWAMINATHAN, Sundaramoorthi , WATKINS, Will , ZHANG, Jennifer, R.
IPC分类号： A61K47/48
CPC分类号： C07F9/65616 , A61K31/662 , A61K31/7072 , A61K31/7076 , A61K47/548 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07F9/4075 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/60 , C07F9/65037 , C07F9/650941 , C07F9/653 , C07F9/6539 , C07F9/65515 , C07F9/655354 , C07F9/6561 , C07H15/00 , C07H17/00 , C07H19/056 , C07H19/10 , C07H19/20 , C07H21/00 , Y02A50/393 , Y02A50/465
摘要： The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译：本发明涉及具有抗病毒活性的磷取代的化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

5. 发明申请

WO2003091264A3 NON NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
公开(公告)号：WO2003091264A3
公开(公告)日：2003-11-06
申请号：PCT/US2003/012926
申请日：2003-04-25
申请人： GILEAD SCIENCES, INC. , CHEN, James, M. , CHEN, Xiaowu , KIM, Choung, U. , LEE, William, A. , LEE, Christopher, P. , TARIO, James, D. , XU, Lianhong , NELSON, Peter, H.
发明人： CHEN, James, M. , CHEN, Xiaowu , KIM, Choung, U. , LEE, William, A. , LEE, Christopher, P. , TARIO, James, D. , XU, Lianhong , NELSON, Peter, H.
IPC分类号： C07F9/38
摘要： Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes.

6. 发明申请

WO2003090691A3 METHOD AND COMPOSITIONS FOR IDENTIFYING ANTI-HIV THERAPEUTIC COMPOUNDS 审中-公开
公开(公告)号：WO2003090691A3
公开(公告)日：2003-11-06
申请号：PCT/US2003/012943
申请日：2003-04-25
申请人： GILEAD SCIENCES, INC. , BIRKUS, Gabriel , CHEN, James, M. , CHEN, Xiaowu , CIHLAR, Tomas , EISENBERG, Eugene, J. , HATADA, Marcos , HE, Gong-Xin , KIM, Choung, U. , LEE, William, A. , MCDERMOTT, Martin, J. , SWAMINATHAN, Sundaramoorthi
发明人： BIRKUS, Gabriel , CHEN, James, M. , CHEN, Xiaowu , CIHLAR, Tomas , EISENBERG, Eugene, J. , HATADA, Marcos , HE, Gong-Xin , KIM, Choung, U. , LEE, William, A. , MCDERMOTT, Martin, J. , SWAMINATHAN, Sundaramoorthi
IPC分类号： C12Q1/34
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.

7. 发明申请

WO2003090690A3 CELLULAR ACCUMULATION OF PHOSPHONATE ANALOGS OF HIV PROTEASE INHIBITOR COMPOUNDS AND THE COMPOUNDS AS SUCH 审中-公开
公开(公告)号：WO2003090690A3
公开(公告)日：2003-11-06
申请号：PCT/US2003/012901
申请日：2003-04-25
申请人： GILEAD SCIENCES, INC. , ARIMILLI, Murty, N. , BECKER, Mark, M. , BRYANT, Clifford , CHEN, James, M. , CHEN, Xiaowu , DASTGAH, Azar , FARDIS, Maria , HE, Gong-Xin , JIN, Haolun , KIM, Choung, U. , LEE, William, A. , LEE, Christopher, P. , LIN, Kuei-Ying , LIU, Hongtao , MACKMAN, Richard, L. , MITCHELL, Michael, L. , NELSON, Peter, H. , PYUN, Hyung-Jung , ROWE, Tanisha, D. , SPARACINO, Mark , SWAMINATHAN, Sundaramoorthi , TARIO, James, D. , WANG, Jianying , WILLIAMS, Matthew, A. , XU, Lianhong , YANG, Zheng-Yu , YU, Richard, H. , ZHANG, Jiancun , ZHANG, Lijun
发明人： ARIMILLI, Murty, N. , BECKER, Mark, M. , BRYANT, Clifford , CHEN, James, M. , CHEN, Xiaowu , DASTGAH, Azar , FARDIS, Maria , HE, Gong-Xin , JIN, Haolun , KIM, Choung, U. , LEE, William, A. , LEE, Christopher, P. , LIN, Kuei-Ying , LIU, Hongtao , MACKMAN, Richard, L. , MITCHELL, Michael, L. , NELSON, Peter, H. , PYUN, Hyung-Jung , ROWE, Tanisha, D. , SPARACINO, Mark , SWAMINATHAN, Sundaramoorthi , TARIO, James, D. , WANG, Jianying , WILLIAMS, Matthew, A. , XU, Lianhong , YANG, Zheng-Yu , YU, Richard, H. , ZHANG, Jiancun , ZHANG, Lijun
IPC分类号： C07F9/40
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.

8. 发明申请

WO2007136650A2 METHOD AND COMPOSITIONS FOR TREATING HEMATOLOGICAL MALIGNANCIES 审中-公开
标题翻译：用于治疗血液恶性肿瘤的方法和组合物
公开(公告)号：WO2007136650A2
公开(公告)日：2007-11-29
申请号：PCT/US2007/011726
申请日：2007-05-16
申请人： GILEAD SCIENCES, INC. , CHONG, Lee, S. , LEE, William, A. , RAY, Adrian, S. , REISER, Hans, C. , TUMAS, Daniel, B. , WATKINS, William, J.
发明人： CHONG, Lee, S. , LEE, William, A. , RAY, Adrian, S. , REISER, Hans, C. , TUMAS, Daniel, B. , WATKINS, William, J.
IPC分类号： A61K31/00 , A61P35/00 , C07F9/6561
CPC分类号： C07F9/65616
摘要： A compound of formula (1), and/or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.
摘要翻译：使用式（1）的化合物和/或其盐，互变异构体或溶剂合物来治疗血液恶性肿瘤。在一个实施方案中，提供化合物1的有机酸盐，用于一般用于治疗赘生物，并且在另一个实施方案中，所述盐用碳水化合物稳定。

9. 发明申请

WO2007002912A2 ANTI-PROLIFERATIVE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE THEREOF 审中-公开
标题翻译：抗增殖化合物，组合物及其使用方法
公开(公告)号：WO2007002912A2
公开(公告)日：2007-01-04
申请号：PCT/US2006/025726
申请日：2006-06-29
申请人： GILEAD SCIENCES, INC. , CHENG, Xiaoqin , COOK, Gary, P. , DESAI, Manoj, C. , DOERFFLER, Edward , HE, Gong-xin , KIM, Choung, U. , LEE, William, A. , ROHLOFF, John, C. , WANG, Jianying , YANG, Zheng-Yu
发明人： CHENG, Xiaoqin , COOK, Gary, P. , DESAI, Manoj, C. , DOERFFLER, Edward , HE, Gong-xin , KIM, Choung, U. , LEE, William, A. , ROHLOFF, John, C. , WANG, Jianying , YANG, Zheng-Yu
IPC分类号： C07F9/6561 , A61P31/12 , A61K31/66
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: 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.
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：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。}}}}}}}

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