Patents by Inventor Gong-Xin He
Gong-Xin He has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 8354421Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: June 26, 2008Date of Patent: January 15, 2013Assignee: Korea Research Insitute of Chemical TechnologyInventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu
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Patent number: 8268802Abstract: 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)(Type: GrantFiled: May 5, 2009Date of Patent: September 18, 2012Assignee: Gilead Sciences, Inc.Inventors: 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
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Patent number: 8088754Abstract: 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.Type: GrantFiled: February 18, 2009Date of Patent: January 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Xiaoqin Cheng, Gary P. Cook, Gong-Xin He, Choung U. Kim, John C. Rohloff, Jianying Wang, Zheng-Yu Yang
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Patent number: 7803788Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: GrantFiled: April 28, 2008Date of Patent: September 28, 2010Assignee: Gilead Sciences, Inc.Inventors: Mark W. Becker, Harlan H. Chapman, Tomas Cihlar, Eugene J. Eisenberg, Gong-Xin He, Michael R. Kernan, William A. Lee, Ernest J. Prisbe, John C. Rohloff, Mark L. Sparacino
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Patent number: 7649015Abstract: 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.Type: GrantFiled: April 25, 2003Date of Patent: January 19, 2010Assignee: Gilead Sciences, Inc.Inventors: 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
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Publication number: 20090291922Abstract: 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)(Type: ApplicationFiled: May 5, 2009Publication date: November 26, 2009Applicant: Gilead Sciences, Inc.Inventors: 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
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Patent number: 7553825Abstract: 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)Type: GrantFiled: December 29, 2004Date of Patent: June 30, 2009Assignee: Gilead Sciences, Inc.Inventors: 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
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Publication number: 20090149400Abstract: 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)(Type: ApplicationFiled: February 18, 2009Publication date: June 11, 2009Applicant: Gilead Sciences, Inc.Inventors: 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
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Publication number: 20090075939Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Inventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu
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Publication number: 20080227754Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: ApplicationFiled: April 28, 2008Publication date: September 18, 2008Inventors: Mark W. Becker, Harlan H. Chapman, Tomas Cihlar, Eugene J. Eisenberg, Gong-Xin He, Michael R. Kernan, William A. Lee, Ernest J. Prisbe, John C. Rohloff, Mark L. Sparacino
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Patent number: 7390791Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: GrantFiled: March 11, 2004Date of Patent: June 24, 2008Assignee: Gilead Sciences, Inc.Inventors: Mark W. Becker, Harlan H. Chapman, Tomas Cihlar, Eugene J. Eisenberg, Gong-Xin He, Michael R. Kernan, William A. Lee, Ernest J. Prisbe, John C. Rohloff, Mark L. Sparacino
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Publication number: 20070190523Abstract: The invention relates to methods and compositions for identifying compounds having therapeutic activity against human immunodeficiency virus (HIV).Type: ApplicationFiled: November 6, 2003Publication date: August 16, 2007Inventors: Gabriel Birkus, James Chen, Xiaowu Chen, Tomas Cihlar, Eugene Eisenberg, Marcos Hatada, Gong-Xin He, Choung Kim, William Lee, Martin McDermott, Sundaramoorthi Swaminathan
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Publication number: 20070010489Abstract: 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.Type: ApplicationFiled: April 25, 2003Publication date: January 11, 2007Inventors: 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
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Publication number: 20060030545Abstract: 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,Type: ApplicationFiled: June 29, 2005Publication date: February 9, 2006Inventors: Xiaoqin Cheng, Gary Cook, Manoj Desai, Edward Doerffler, Gong-Xin He, Choung Kim, William Lee, John Rohloff, Jianying Wang, Zheng-Yu Yang
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Publication number: 20060024659Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: ApplicationFiled: February 24, 2004Publication date: February 2, 2006Inventors: Mark Becker, Harlan Chapman, Tomas Cihlar, Eugene Eisenberg, Gong-Xin He, Michael Kernan, William Lee, Ernest Prisbe, John Rohloff, Mark Sparacino
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Publication number: 20050239054Abstract: 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.Type: ApplicationFiled: December 22, 2003Publication date: October 27, 2005Inventors: 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
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Publication number: 20050222090Abstract: 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,Type: ApplicationFiled: December 29, 2004Publication date: October 6, 2005Inventors: Xiaqin Cheng, Gary Cook, Manoj Desai, Edward Doerffler, Gong-Xin He, Choung Kim, William Lee, John Rohloff, Jianying Wang, Zheng-Yu Yang
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Publication number: 20050209197Abstract: 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.Type: ApplicationFiled: April 25, 2003Publication date: September 22, 2005Inventors: 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 Williams, Lianhong Xu, Zheng-Yu Yang, Richard Yu, Jiancun Zhang, Lijun Zhang
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Publication number: 20050159392Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: ApplicationFiled: January 6, 2005Publication date: July 21, 2005Inventors: Mark Becker, Harlan Chapman, Tomas Cihlar, Eugene Eisenberg, Gong-Xin He, Michael Kernan, William Lee, Ernest Prisbe, John Rohloff, Mark Sparacino
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Publication number: 20050124583Abstract: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.Type: ApplicationFiled: January 6, 2005Publication date: June 9, 2005Inventors: Mark Becker, Harlan Chapman, Tomas Clhlar, Eugene Elsenberg, Gong-Xin He, Michael Kernan, William Lee, Ernest Prisbe, John Rohloff, Mark Sparacino