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1. 发明申请

WO1995018109A1 NOVEL ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 审中-公开
标题翻译：新颖的2,4-二吡啶衍生物及其制备方法
公开(公告)号：WO1995018109A1
公开(公告)日：1995-07-06
申请号：PCT/KR1994000178
申请日：1994-12-20
申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , SON, Jong, Chan , LEE, Ill, Young , BAE, Byung, Il , HAN, Jeong, Sik , CHOI, Joong, Kwon , CHAE, Yung, Bok
发明人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
IPC分类号： C07D239/60
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: R represents an unsubstituted or substituted alkyl group represented by CH2CH=CR R or an unsubstituted or substituted propargyl group represented by CH2CCR wherein R , R and R are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C1-10 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 represents a halogen atom, an optionally substituted C1-5 alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl group or a benzyl group; R and R represent independently a hydrogen or halogen atom, or a hydroxy, C1-3 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.
摘要翻译：新颖的具有良好抗病毒活性的2,4-嘧啶二酮化合物及其药学上可接受的盐，具体由式（I）表示，其中：R 1表示由CH 2 CH = CR 5表示的未取代或取代的烷基， 6>或由CH 2 CCR 7表示的未取代或取代的炔丙基，其中R 5，R 6和R 7各自独立地为氢原子; 羟基，叠氮基，氰基，任选取代的氨基，任选取代的膦酰基，任选取代的苯基，C 3-10杂芳基，C 1-3烷氧基或苄氧基; C2-10烷基或烯基; 环丙基; 任选取代的苯基; C3-10杂芳基; C1-10酯基; 或任选取代的C 1-10烷基酰胺基; R 2表示卤素原子，任选取代的C 1-5烷基，C 3-6环烷基，C 2-8烯基，C 2-8炔基或苄基; R 3和R 4独立地表示氢或卤素原子，或羟基，C 1-3烷基，氟甲基，C 1-3烷氧基，氨基，C 2-6烷基酯或C 2-7烷基酰胺基团。 A表示氧或硫原子; Z表示氧或硫原子; 羰基; 氨基; 或任选被至少一个选自卤素原子和氰基，羟基，叠氮基，氨基，C 1-3烷基酰胺，C 1-4酯和硝基取代的亚甲基。

2. 发明申请

WO2009085797A1 PROCESSES FOR PREPARING HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：制备HIV逆转录酶抑制剂的方法
公开(公告)号：WO2009085797A1
公开(公告)日：2009-07-09
申请号：PCT/US2008/087106
申请日：2008-12-17
申请人： GILEAD SCIENCES, INC. , KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , GUO, Hongyan , HEUMANN, Stacey , LEE, Ill Young , MITCHELL, Michael , PFEIFFER, Steven , SON, Jong Chan
发明人： GUO, Hongyan , HEUMANN, Stacey , LEE, Ill Young , MITCHELL, Michael , PFEIFFER, Steven , SON, Jong Chan
IPC分类号： C07D239/54
CPC分类号： C07D239/54
摘要： Compounds of Formula (I): can be prepared by a multi-step process from compounds of Formula (II): wherein G is Cl, Br or I.
摘要翻译：式（I）化合物：可以通过式（II）化合物的多步法制备：其中G是Cl，Br或I.

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。

5. 发明申请

WO1997043266A1 ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：有用的2,4-二吡啶衍生物及其制备方法
公开(公告)号：WO1997043266A1
公开(公告)日：1997-11-20
申请号：PCT/KR1997000084
申请日：1997-05-15
申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , SAMJIN PHARMACEUTICAL CO., LTD. , 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
发明人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , SAMJIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D239/54
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 R is hydrogen or a C1-10 alkyl group optionally having a substituent selected from the group consisting of aryl, hydroxy, C1-10 alkoxy and C2-5 alkylcarbonyloxy groups; R is hydrogen or a C1-10 alkyl group optionally having an aryl substituent; R and R are each hydrogen or a C1-3 alkyl group; and A is oxygen or a carbonyl group.
摘要翻译：对HIV-1具有高抗病毒活性和低毒性的式（I）的6-芳氧基和6-芳基羰基2,4-嘧啶二酮衍生物可用于治疗AIDS，其中R 1是氢或任选地是C 1-10烷基具有选自芳基，羟基，C 1-10烷氧基和C 2-5烷基羰基氧基的取代基; R 2是氢或任选具有芳基取代基的C 1-10烷基; R 3和R 4各自为氢或C 1-3烷基; A是氧或羰基。

6. 发明申请

WO2010085128A3 PROCESSES FOR PREPARING HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：制备HIV逆转录酶抑制剂的过程
公开(公告)号：WO2010085128A3
公开(公告)日：2010-11-25
申请号：PCT/KR2010000464
申请日：2010-01-26
申请人： KOREA RES INST CHEM TECH , HEUMANN STACEY , LEVINS CHRISTOPHER M , PFEIFFER STEVEN , TANG DONALD , SON JONG CHAN
发明人： HEUMANN STACEY , LEVINS CHRISTOPHER M , PFEIFFER STEVEN , TANG DONALD , SON JONG CHAN
IPC分类号： C07D239/54 , A61K31/505 , A61P31/18
CPC分类号： C07D239/545 , A61K31/505 , C07C255/57 , C07C275/50 , C07D233/60 , C07D239/54 , C07D239/553
摘要： Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.
摘要翻译：公开了一种制备抑制HIV感染HIV细胞中HIV复制的HIV逆转录酶抑制剂的方法，以及其中使用的新型中间体化合物。

7. 发明申请

WO2010085128A2 PROCESSES FOR PREPARING HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：制备HIV逆转录酶抑制剂的方法
公开(公告)号：WO2010085128A2
公开(公告)日：2010-07-29
申请号：PCT/KR2010/000464
申请日：2010-01-26
申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , HEUMANN, Stacey , LEVINS, Christopher, M. , PFEIFFER, Steven , TANG, Donald , SON, Jong Chan
发明人： HEUMANN, Stacey , LEVINS, Christopher, M. , PFEIFFER, Steven , TANG, Donald , SON, Jong Chan
IPC分类号： C07D239/54 , A61K31/505 , A61P31/18
CPC分类号： C07D239/545 , A61K31/505 , C07C255/57 , C07C275/50 , C07D233/60 , C07D239/54 , C07D239/553
摘要： Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.
摘要翻译：公开了一种制备抑制HIV感染细胞中HIV复制的HIV逆转录酶抑制剂的方法及其中所用的新型中间体化合物。

8. 发明申请

WO2009005674A3 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：WO2009005674A3
公开(公告)日：2009-09-24
申请号：PCT/US2008007925
申请日：2008-06-26
申请人： GILEAD SCIENCES INC , KOREAN RES INST OF CHEMICAL TE , 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 , A61K31/506 , A61K31/513 , A61P31/18 , C07D239/553 , C07D401/04 , C07D403/04
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，溶剂合物，酯和/或膦酸盐，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。

9. 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.

10. 发明申请

WO2008016522A2 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：WO2008016522A2
公开(公告)日：2008-02-07
申请号：PCT/US2007016703
申请日：2007-07-24
申请人： GILEAD SCIENCES INC , KOREA RES INST CHEM TECH , 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
CPC分类号： C07D401/06 , C07D239/54 , C07D403/06 , C07D413/06
摘要： The invention is related to com ounds 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.
摘要翻译：本发明涉及式（I），（II）或（III）的化合物; 或其药学上可接受的盐，溶剂合物，酯和/或膦酸盐，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。

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