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1.发明申请
公开(公告)号：WO2005064008A1
公开(公告)日：2005-07-14
申请号：PCT/US2004/042991
申请日：2004-12-22
申请人： Gilead Sciences, Inc. , ARIMILLI, Murty N. , BECKER, Mark M. , BIRKUS, Gabriel , BRYANT, Clifford , CHEN, James M. , CHEN, Xiaowu , CIHLAR, Tomas , DASTGAH, Azar , EISENBERG, Eugene J. , FARDIS, Maria , HATADA, Marcos , HE, Gong-Xin , JIN, Haolun , KIM, Choung U. , LEE, William A. , LEE, Christopher P. , LIN, Kuei-Ying , LIU, Hongtao , MACKMAN, Richard L. , MCDERMOTT, Martin J. , 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. , BIRKUS, Gabriel , BRYANT, Clifford , CHEN, James M. , CHEN, Xiaowu , CIHLAR, Tomas , DASTGAH, Azar , EISENBERG, Eugene J. , FARDIS, Maria , HATADA, Marcos , HE, Gong-Xin , JIN, Haolun , KIM, Choung U. , LEE, William A. , LEE, Christopher P. , LIN, Kuei-Ying , LIU, Hongtao , MACKMAN, Richard L. , MCDERMOTT, Martin J. , 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： C12Q1/44
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 , C07F9/582 , C07F9/588 , C07F9/645 , C07F9/65061 , C07F9/65062 , C07F9/65067 , C07F9/650911 , C07F9/650917 , C07F9/650947 , C07F9/65121 , C07F9/65122 , C07F9/65127 , 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。 可以任选地使用新型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。
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公开(公告)号：WO2004100960A8
公开(公告)日：2005-06-30
申请号：PCT/US2004013198
申请日：2004-04-26
申请人： GILEAD SCIENCES INC , CANNIZZARO CARINA E , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , FARDIS MARIA , GIBBS CRAIG , HIRSCHMANN RALPH F , KIRSCHBERG THORSTEN A , LEE CHRISTOPHER P , LIN KUEI-YING , MACKMAN RICHARD L , NELSON PETER H , OARE DAVID , PYUN HYUNG-JUNG , RAY ADRIAN S , SHERLOCK ROSEMARIE , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL , ZHANG JENNIFER R
发明人： CANNIZZARO CARINA E , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , FARDIS MARIA , GIBBS CRAIG , HIRSCHMANN RALPH F , KIRSCHBERG THORSTEN A , LEE CHRISTOPHER P , LIN KUEI-YING , MACKMAN RICHARD L , NELSON PETER H , OARE DAVID , PYUN HYUNG-JUNG , RAY ADRIAN S , SHERLOCK ROSEMARIE , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL , ZHANG JENNIFER R
IPC分类号： A61K20060101 , A61K31/662 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07D487/04 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6503 , C07F9/6509 , C07F9/653 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/6561
CPC分类号： A61K31/662 , A61K47/548 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07D487/04 , C07F9/4075 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/60 , C07F9/65037 , C07F9/650941 , C07F9/653 , C07F9/6539 , C07F9/65515 , C07F9/655354 , C07F9/6561 , C07F9/65616
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公开(公告)号：WO2004096236A3
公开(公告)日：2005-06-30
申请号：PCT/US2004013143
申请日：2004-04-26
申请人： GILEAD SCIENCES INC , CANNIZZARO CARINA E , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , DESAI MANOJ , FARDIS MARIA , HUANG ALAN X , KIRSCHBERG THORSTEN A , LEE CHRISTOPHER P , MACKMAN RICHARD L , NELSON PETER H , PYUN HYUNG-JUNG , RAY ADRIAN S , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL , ZHANG JENNIFER R
发明人： CANNIZZARO CARINA E , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , DESAI MANOJ , FARDIS MARIA , HUANG ALAN X , KIRSCHBERG THORSTEN A , LEE CHRISTOPHER P , MACKMAN RICHARD L , NELSON PETER H , PYUN HYUNG-JUNG , RAY ADRIAN S , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL , ZHANG JENNIFER R
IPC分类号： A61K31/662 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07D487/04 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6503 , C07F9/6509 , C07F9/653 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/6561
CPC分类号： A61K31/662 , A61K47/548 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07D487/04 , C07F9/4075 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/60 , C07F9/65037 , C07F9/650941 , C07F9/653 , C07F9/6539 , C07F9/65515 , C07F9/655354 , C07F9/6561
摘要： The invention is related to phosphonate substituted compounds having immuno-modulatory 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： 本发明涉及具有免疫调节活性的膦酸酯取代的化合物，含有这些化合物的组合物，以及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。
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公开(公告)号：WO2005002626A2
公开(公告)日：2005-01-13
申请号：PCT/US2004/013283
申请日：2004-04-26
申请人： GILEAD SCIENCES, INC. , BOOJAMRA, Constantine, G. , CANNIZZARO, Carina, E. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , DESAI, Manoj , FARDIS, Maria , GIBBS, Craig, S. , HIRSCHMANN, Ralph, F. , HUANG, Alan, X. , JIN, Haolun , KIM, Choung, U. , KIRSCHBERG, Thorsten, A. , KRAWCZYK, Steven , LEE, Christopher, P. , LEE, William, A. , LIN, Kuei-Ying , MACKMAN, Richard, L. , MARKEVITCH, David, Y. , NELSON, Peter, H. , OARE, David, A. , PRASAD, Vidya, K. , PYUN, Hyung-Jung , RAY, Adrian, S. , SHERLOCK, Rosemarie , SWAMINATHAN, Sundaramoorthi , WATKINS, William, J. , ZHANG, Jennifer, R. , ZHANG, Lijun
发明人： BOOJAMRA, Constantine, G. , CANNIZZARO, Carina, E. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , DESAI, Manoj , FARDIS, Maria , GIBBS, Craig, S. , HIRSCHMANN, Ralph, F. , HUANG, Alan, X. , JIN, Haolun , KIM, Choung, U. , KIRSCHBERG, Thorsten, A. , KRAWCZYK, Steven , LEE, Christopher, P. , LEE, William, A. , LIN, Kuei-Ying , MACKMAN, Richard, L. , MARKEVITCH, David, Y. , NELSON, Peter, H. , OARE, David, A. , PRASAD, Vidya, K. , PYUN, Hyung-Jung , RAY, Adrian, S. , SHERLOCK, Rosemarie , SWAMINATHAN, Sundaramoorthi , WATKINS, William, J. , ZHANG, Jennifer, R. , ZHANG, Lijun
IPC分类号： A61K47/48
CPC分类号： C07F9/65616 , C07F9/4006 , C07F9/4465 , C07F9/5304 , C07F9/650958 , C07F9/653 , C07F9/65507 , C07F9/65515 , C07F9/65517 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.
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公开(公告)号：WO2004096233A2
公开(公告)日：2004-11-11
申请号：PCT/US2004/013060
申请日：2004-04-26
申请人： GILEAD SCIENCES, INC. , BOOJAMARA, Constantine, G. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , FARDIS, Maria , HUANG, Alan, X. , KIM, Choung, X. , KIRSCHBERG, Thorsten, A. , LEE, Christopher, P. , OARE, David , PRASAD, Vidya, K. , RAY, Adrian, S. , SWAMINATHAN, Sundaramoorthi , WATKINS, Will
发明人： BOOJAMARA, Constantine, G. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , FARDIS, Maria , HUANG, Alan, X. , KIM, Choung, X. , KIRSCHBERG, Thorsten, A. , LEE, Christopher, P. , OARE, David , PRASAD, Vidya, K. , RAY, Adrian, S. , SWAMINATHAN, Sundaramoorthi , WATKINS, Will
IPC分类号： A61K31/662
CPC分类号： A61K31/662 , A61K47/54 , C07F9/6561 , C07F9/65616
摘要： The invention is related to phosphorus substituted nucleoside 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： 本发明涉及磷取代的核苷化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。
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公开(公告)号：WO2003091264A2
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
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 , C07F9/582 , C07F9/588 , C07F9/645 , C07F9/65061 , C07F9/65062 , C07F9/65067 , C07F9/650911 , C07F9/650917 , C07F9/650947 , C07F9/65121 , C07F9/65122 , C07F9/65127 , 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： 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.
摘要翻译： 公开了具有用作治疗剂和其它工业目的的具有抗HIV性质的磷取代的咪唑化合物。 组合物抑制逆转录酶活性，并且可用于抑制这些酶以及用于检测这些酶的测定中。
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公开(公告)号：WO2008013834A1
公开(公告)日：2008-01-31
申请号：PCT/US2007/016691
申请日：2007-07-24
申请人： GILEAD SCIENCES, INC., , DESAI, Manoj, C. , LEE, Christopher, P. , LIU, Hongtao , SWAMINATHAN, Sundaramoorthi , XU, Lianhong
发明人： DESAI, Manoj, C. , LEE, Christopher, P. , LIU, Hongtao , SWAMINATHAN, Sundaramoorthi , XU, Lianhong
IPC分类号： C07D493/04 , A61P31/18
CPC分类号： C07D493/04
摘要： The present invention provides compounds of Formula (I): wherein A, X, Q, R 2 -R 6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are protease inhibitors and are useful for inhibiting the development of drug resistance in animals.
摘要翻译： 本发明提供式（I）化合物：其中A，X，Q，R 2，R 6，M和W具有本文所述的值，以及 作为包含这些化合物的组合物。 这些化合物是蛋白酶抑制剂，可用于抑制动物耐药性的发展。
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8.发明申请
公开(公告)号：WO2005064008A9
公开(公告)日：2006-09-28
申请号：PCT/US2004042991
申请日：2004-12-22
申请人： GILEAD SCIENCES INC , ARIMILLI MURTY N , BECKER MARK M , BIRKUS GABRIEL , BRYANT CLIFFORD , CHEN JAMES M , CHEN XIAOWU , CIHLAR TOMAS , DASTGAH AZAR , EISENBERG EUGENE J , FARDIS MARIA , HATADA MARCOS , HE GONG-XIN , JIN HAOLUN , KIM CHOUNG U , LEE WILLIAM A , LEE CHRISTOPHER P , LIN KUEI-YING , LIU HONGTAO , MACKMAN RICHARD L , MCDERMOTT MARTIN J , 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 , BIRKUS GABRIEL , BRYANT CLIFFORD , CHEN JAMES M , CHEN XIAOWU , CIHLAR TOMAS , DASTGAH AZAR , EISENBERG EUGENE J , FARDIS MARIA , HATADA MARCOS , HE GONG-XIN , JIN HAOLUN , KIM CHOUNG U , LEE WILLIAM A , LEE CHRISTOPHER P , LIN KUEI-YING , LIU HONGTAO , MACKMAN RICHARD L , MCDERMOTT MARTIN J , 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： C12N9/99 , C12Q1/44 , 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 , C12Q1/70 , 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 , C07F9/582 , C07F9/588 , C07F9/645 , C07F9/65061 , C07F9/65062 , C07F9/65067 , C07F9/650911 , C07F9/650917 , C07F9/650947 , C07F9/65121 , C07F9/65122 , C07F9/65127 , 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。
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公开(公告)号：WO2004096233A3
公开(公告)日：2005-06-16
申请号：PCT/US2004013060
申请日：2004-04-26
申请人： GILEAD SCIENCES INC , BOOJAMARA CONSTANTINE G , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , FARDIS MARIA , HUANG ALAN X , KIM CHOUNG X , KIRSCHBERG THORSTEN A , LEE CHRISTOPHER P , OARE DAVID , PRASAD VIDYA K , RAY ADRIAN S , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL
发明人： BOOJAMARA CONSTANTINE G , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , FARDIS MARIA , HUANG ALAN X , KIM CHOUNG X , KIRSCHBERG THORSTEN A , LEE CHRISTOPHER P , OARE DAVID , PRASAD VIDYA K , RAY ADRIAN S , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL
IPC分类号： A61K31/662 , A61K47/48 , C07F9/6561
CPC分类号： A61K31/662 , A61K47/54 , C07F9/6561 , C07F9/65616
摘要： The invention is related to phosphorus substituted nucleoside 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： 本发明涉及磷取代的核苷化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。
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公开(公告)号：WO2004096235A8
公开(公告)日：2005-02-24
申请号：PCT/US2004013121
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 , HUANG ALAN X , KIM CHOUNG X , KIRSCHBERG THORSTEN A , KRAWCZYK STEVEN , LEE CHRISTOPHER P , LIN KUEI-YING , MACKMAN RICHARD L , MARKEVITCH DAVID Y , NELSON PETER H , OARE DAVID , PRASAD VIDYA K , PYUN HYUNG-JUNG , RAY ADRIAN S , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL , ZHANG LIJUN
发明人： BOOJAMARA CONSTANTINE G , CANNIZZARO CARINA E , CHEN JAMES M , CHEN XIAOWU , CHO AESOP , CHONG LEE S , FARDIS MARIA , HUANG ALAN X , KIM CHOUNG X , KIRSCHBERG THORSTEN A , KRAWCZYK STEVEN , LEE CHRISTOPHER P , LIN KUEI-YING , MACKMAN RICHARD L , MARKEVITCH DAVID Y , NELSON PETER H , OARE DAVID , PRASAD VIDYA K , PYUN HYUNG-JUNG , RAY ADRIAN S , SWAMINATHAN SUNDARAMOORTHI , WATKINS WILL , ZHANG LIJUN
IPC分类号： A61K20060101 , A61K31/662 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07D487/04 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6503 , C07F9/6509 , C07F9/653 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/6561
CPC分类号： A61K31/662 , A61K47/548 , C07D205/04 , C07D211/58 , C07D239/94 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07D487/04 , C07F9/4075 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/60 , C07F9/65037 , C07F9/650941 , C07F9/653 , C07F9/6539 , C07F9/65515 , C07F9/655354 , C07F9/6561
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