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1. 发明申请

WO2008016522A3 HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
公开(公告)号：WO2008016522A3
公开(公告)日：2008-02-07
申请号：PCT/US2007/016703
申请日：2007-07-24
申请人： GILEAD SCIENCES, INC. , KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , GUO, Hongyan , KIM, Choung, U. , KIM, Hae, Soo , LEE, Chong-kyo , LEE, III Young , MITCHELL, Michael, L. , SON, Jong, Chan , XU, Lianhong
发明人： GUO, Hongyan , KIM, Choung, U. , KIM, Hae, Soo , LEE, Chong-kyo , LEE, III Young , MITCHELL, Michael, L. , SON, Jong, Chan , XU, Lianhong
IPC分类号： C07D239/54 , C07D401/06 , C07D403/06 , C07D413/06 , A61K31/513 , A61P31/00
摘要： The invention is related to compounds of Formula (I), (II), or (III); 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.

2. 发明申请

WO2010009047A1 PYRIDONE DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：吡喃酮衍生物作为非核苷酸逆转录酶抑制剂
公开(公告)号：WO2010009047A1
公开(公告)日：2010-01-21
申请号：PCT/US2009/050400
申请日：2009-07-13
申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , KIM, Choung, U. , MITCHELL, Michael, L. , SON, Jong, Chan
发明人： KIM, Choung, U. , MITCHELL, Michael, L. , SON, Jong, Chan
IPC分类号： C07D213/64 , C07D213/70 , C07D213/71 , A61K31/4412 , A61P31/18
CPC分类号： C07D213/64 , C07D213/70 , C07D213/71
摘要： The present invention relates to 2-pyridone derivatives of Formula (I) or (IV) as herein described, compositions containing such compounds, synthetic processes for making such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译：本发明涉及如本文所述的式（I）或（IV）的2-吡啶酮衍生物，含有这些化合物的组合物，用于制备这些化合物的合成方法，以及包括施用这些化合物的治疗方法。

3. 发明申请

WO2009005674A2 NOVEL HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：新型HIV逆转录酶抑制剂
公开(公告)号：WO2009005674A2
公开(公告)日：2009-01-08
申请号：PCT/US2008/007925
申请日：2008-06-26
申请人： GILEAD SCIENCES, INC. , KOREAN RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , GUO, Hongyan , KIM, Choung, U. , LEE, Ill, Young , MITCHELL, Michael, L. , RHODES, Gerry , SON, Jong, Chan , XU, Lianhong
发明人： GUO, Hongyan , KIM, Choung, U. , LEE, Ill, Young , MITCHELL, Michael, L. , RHODES, Gerry , SON, Jong, Chan , XU, Lianhong
IPC分类号： C07D239/54 , C07D401/04 , C07D403/04 , C07D239/553 , A61K31/506 , A61K31/513 , A61P31/18
CPC分类号： A61K31/513 , A61K31/496 , A61K31/536 , A61K31/551 , A61K31/66 , A61K31/7048 , A61K31/7072 , A61K31/708 , A61K39/39558 , A61K45/06 , C07D239/54 , C07D239/545 , C07D239/553 , C07D239/60 , C07D401/04 , C07D403/04
摘要： 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.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物，酯和/或膦酸酯，含有这些化合物的组合物，以及包括给予这些化合物的治疗方法

4. 发明公开

EP2167476A2 NOVEL HIV REVERSE TRANSCRIPTASE INHIBITORS 有权
标题翻译：新的HIV逆转录酶抑制剂
公开(公告)号：EP2167476A2
公开(公告)日：2010-03-31
申请号：EP08779769.2
申请日：2008-06-26
申请人： Korea Research Institute Of Chemical Technology
发明人： GUO, Hongyan , KIM, Choung U. , LEE, Ill, Young , MITCHELL, Michael, L. , RHODES, Gerry , SON, Jong, Chan , XU, Lianhong
IPC分类号： C07D239/54 , C07D401/04 , C07D403/04 , C07D239/553 , A61K31/506 , A61K31/513 , A61P31/18
CPC分类号： A61K31/513 , A61K31/496 , A61K31/536 , A61K31/551 , A61K31/66 , A61K31/7048 , A61K31/7072 , A61K31/708 , A61K39/39558 , A61K45/06 , C07D239/54 , C07D239/545 , C07D239/553 , C07D239/60 , C07D401/04 , C07D403/04
摘要： 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.

5. 发明授权

EP1159271B1 ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
标题翻译： ANIVIRALE 2.4嘧啶二酮衍生物及其生产工艺
公开(公告)号：EP1159271B1
公开(公告)日：2004-08-25
申请号：EP00908087.0
申请日：2000-03-03
申请人： Korea Research Institute of Chemical Technology
发明人： SON, Jong, Chan , SHIN, Seun, Shil , KIM, Shin, Keol , LEE, Chong, Kyo , KIM, Hae, Soo
IPC分类号： C07D239/04 , A61K31/495 , A61P31/18
CPC分类号： C07D239/54 , C07D239/545 , C07D239/62 , C07D239/66 , C07D401/06
摘要： 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C¿6-10? aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-6 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O-(C1-6 alkyl)-substituted oximino, C-1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethyl, C1-6 alkoxymethyl, C1-6 acyloxymethyl, carbamoyloxymethyl, aminomethyl, N-(C1-3 alkyl) aminomethyl, N,N-di(C1-3 alkyl) aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl) amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl) carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a tetrahydropyridyl or piperidyl group optionally substituted with a C1-6 alkyl or C1-6 alkoxycarbonyl group; a tetrahydropyranyl group; or a tetrahydrofuryl group; R?2¿ is hydrogen, halogen, nitro, cyano, C¿1-3? alkoxycarbonyl, C1-3 alkylamino, di(C1-3 alkyl) amino, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl, C1-6 alkyl, C3-6 cycloalkyl or benzyl; R?3 and R4¿ are each independently hydrogen, halogen, hydroxy, cyano, nitro, amino, acetamido, trifluoroacetamido, azido, C¿1-3? alkyl, C1-3 alkyl substituted with one or more halogen atoms, C1-3 alkoxycarbonyl, carbamoyl, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl or C1-3 alkoxy; A is O or S; and Z is O, S, C=O, NH or CH2.

6. 发明公开

EP2044037A2 HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：反抑制剂HIV酶
公开(公告)号：EP2044037A2
公开(公告)日：2009-04-08
申请号：EP07836229.0
申请日：2007-07-24
申请人： Gilead Sciences, Inc. , Korea Research Institute Of Chemical Technology
发明人： GUO, Hongyan , KIM, Choung U. , KIM, Hae Soo , LEE, Chong-Kyo , LEE, III Young , MITCHELL, Michael L. , SON, Jong, Chan , XU, Lianhong , KIRSCHBERG, Thorsten, A.
IPC分类号： C07D239/54
CPC分类号： C07D401/06 , C07D239/54 , C07D403/06 , C07D413/06
摘要： The invention is related to compounds of Formula (I), (II), or (III); 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.

7. 发明公开

EP1159271A1 ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
标题翻译： ANIVIRALE 2.4嘧啶二酮衍生物及其生产工艺
公开(公告)号：EP1159271A1
公开(公告)日：2001-12-05
申请号：EP00908087.0
申请日：2000-03-03
申请人： Korea Research Institute of Chemical Technology
发明人： SON, Jong, Chan , SHIN, Seun, Shil , KIM, Shin, Keol , LEE, Chong, Kyo , KIM, Hae, Soo
IPC分类号： C07D239/04 , A61K31/495
CPC分类号： C07D239/54 , C07D239/545 , C07D239/62 , C07D239/66 , C07D401/06
摘要： 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C¿6-10? aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-6 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O-(C1-6 alkyl)-substituted oximino, C-1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethyl, C1-6 alkoxymethyl, C1-6 acyloxymethyl, carbamoyloxymethyl, aminomethyl, N-(C1-3 alkyl) aminomethyl, N,N-di(C1-3 alkyl) aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl) amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl) carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a tetrahydropyridyl or piperidyl group optionally substituted with a C1-6 alkyl or C1-6 alkoxycarbonyl group; a tetrahydropyranyl group; or a tetrahydrofuryl group; R?2¿ is hydrogen, halogen, nitro, cyano, C¿1-3? alkoxycarbonyl, C1-3 alkylamino, di(C1-3 alkyl) amino, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl, C1-6 alkyl, C3-6 cycloalkyl or benzyl; R?3 and R4¿ are each independently hydrogen, halogen, hydroxy, cyano, nitro, amino, acetamido, trifluoroacetamido, azido, C¿1-3? alkyl, C1-3 alkyl substituted with one or more halogen atoms, C1-3 alkoxycarbonyl, carbamoyl, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl or C1-3 alkoxy; A is O or S; and Z is O, S, C=O, NH or CH2.

8. 发明公开

EP0912526A1 ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 失效
标题翻译：抗病毒2.4嘧啶二酮衍生物和工艺及其
公开(公告)号：EP0912526A1
公开(公告)日：1999-05-06
申请号：EP97920976.0
申请日：1997-05-15
申请人： Korea Research Institute of Chemical Technology , Samjin Pharmaceutical Co., Ltd.
发明人： SON, Jong, Chan , LEE, Ill, Young , KIM, Hyun, Sook , KIM, Jin, Chel , CHO, Eui, Hwan , CHUNG, Sun, Gan , KIM, Joung, Young , LEE, Soon, Hwan , KWON, Ho, Seok , LEE, Jae, Weung
IPC分类号： A61K31 , A61P31 , C07D239
CPC分类号： C07D239/54
摘要： 6-aryloxy and 6-arylcarbonyl 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against HIV-1 and low toxicity are useful for treating AIDS, wherein R1 is hydrogen or a C¿1-10? alkyl group optionally having a substituent selected from the group consisting of aryl, hydroxy, C1-10 alkoxy and C2-5 alkylcarbonyloxy groups; R?2¿ is hydrogen or a C¿1-10? alkyl group optionally having an aryl substituent; R?3 and R4¿ are each hydrogen or a C¿1-3? alkyl group; and A is oxygen or a carbonyl group.

9. 发明公开

EP0736015A1 NOVEL ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 失效
标题翻译：新的抗病毒2.4嘧啶二酮衍生物及其制造方法
公开(公告)号：EP0736015A1
公开(公告)日：1996-10-09
申请号：EP95903455.0
申请日：1994-12-20
申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
发明人： SON, Jong, Chan , LEE, Ill, Young , BAE, Byung, Il , HAN, Jeong, Sik , CHOI, Joong, Kwon , CHAE, Yung, Bok
IPC分类号： C07D239 , A61K31 , A61P31
CPC分类号： C07D239/54 , C07D239/60
摘要： Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by formula (I) wherein: R1 represents an unsubstituted or substituted alkyl group represented by CH¿2?CH=CR?5R6¿ or an unsubstituted or substituted propargyl group represented by CH¿2?C CR?7¿ wherein R?5, R6 and R7¿ are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C¿1-10? carbonyloxy, hydroxy, azido, cyano, optionally substituted amino, optionally substituted phosphonyl, optionally substituted phenyl, C3-10 heteroaryl, C1-3 alkoxy or benzyloxy radical; a C2-10 alkyl or alkenyl group; a cyclopropyl group; an optionally substituted phenyl group; a C3-10 heteroaryl group; a C1-10 ester group; or an optionally substituted C1-10 alkylamide group; R?2¿ represents a halogen atom, an optionally substituted C¿1-5? alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl group or a benzyl group; R?3 and R4¿ represent independently a hydrogen or halogen atom, or a hydroxy, C¿1-3? alkyl, fluoromethyl, C1-3 alkoxy, amino, C2-6 alkylester or C2-7 alkylamide group; A represents an oxygen or sulfur atom; Z represents an oxygen or sulfur atom; a carbonyl group; an amino group; or a methylene group optionally substituted with at least one selected from the group consisting of a halogen atom, and a cyano, hydroxy, azido, amino, C1-3 alkylamide, C1-4 ester, and nitro groups.

10. 发明授权

EP2167476B1 NOVEL HIV REVERSE TRANSCRIPTASE INHIBITORS 有权
标题翻译：新的HIV逆转录酶抑制剂
公开(公告)号：EP2167476B1
公开(公告)日：2015-02-25
申请号：EP08779769.2
申请日：2008-06-26
申请人： Korea Research Institute Of Chemical Technology
发明人： GUO, Hongyan , KIM, Choung U. , LEE, Ill, Young , MITCHELL, Michael, L. , RHODES, Gerry , SON, Jong, Chan , XU, Lianhong
IPC分类号： C07D239/54 , C07D401/04 , C07D403/04 , C07D239/553 , A61K31/506 , A61K31/513 , A61P31/18
CPC分类号： A61K31/513 , A61K31/496 , A61K31/536 , A61K31/551 , A61K31/66 , A61K31/7048 , A61K31/7072 , A61K31/708 , A61K39/39558 , A61K45/06 , C07D239/54 , C07D239/545 , C07D239/553 , C07D239/60 , C07D401/04 , C07D403/04

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