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1. 发明申请

WO2002070516A2 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO2002070516A2
公开(公告)日：2002-09-12
申请号：PCT/EP2002/002328
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： LINDSTRÖM, Stefan , SAHLBERG, Christer , WALLBERG, Hans , KALYANOV, Genaidy , ODÉN, Lourdes , NAESLUND, Lotta
IPC分类号： C07D407/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of Formula (I), where; R 1 is O, S; R 2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R 3 is H, C 1 -C 3 alkyl, R 4 -R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, haloC 1 -C 6 alkyl, C 1 -C 6 alkanoyl, haloC 1 -C 6 alkanoyl, C 1 -C 6 alkoxy, haloC 1 -C 6 alkoxy, C 1 -C 6 alkyloxy-C 1 -C 6 alkyl, haloC 1 -C 6 alkyloxy-C 1 -C 6 alkyl hydroxy-C 1 -C 6 alkyl, amino-C 1 -C 6 alkyl, carboxy-C 1 -C 6 alkyl, cyano-C 1 -C 6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CHR 8 ) n- -D-(CHR 8 ) m -; D is -NR 9 -, -O-, -S-, -S(=O)- or -S(=O)2-; R 8 is independently H, C 1 -C 3 alkyl, halo substitutedC 1 -C 3 alkyl;R 9 is H, C 1 -C 3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式（I）的化合物，其中; R1为O，S; R2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R3是H，C1-C3烷基，R4-R7独立地选自H，C1-C6烷基，C2-C6烯基，C2-C6炔基，卤代C 1 -C 6烷基，C 1 -C 6烷酰基，卤代C 1 -C 6烷酰基， C6烷氧基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基-C 1 -C 6烷基，卤代C 1 -C 6烷氧基-C 1 -C 6烷基羟基-C 1 -C 6烷基，氨基-C 1 -C 6烷基，羧基-C 1 -C 6烷基， C 1 -C 6烷基，氨基，羧基，氨基甲酰基，氰基，卤素，羟基，酮基; X是 - （CHR 8）n -D-（CHR 8）m - ; D是-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O） R8独立地是H，C1-C3烷基，卤素取代的C1-C3烷基; R9是H，C1-C3烷基; n和m独立地为0,1或2; 和其前药和药学上可接受的盐，可用作HIV-1逆转录酶的抑制剂，特别是药物逃逸突变体。

2. 发明授权

EP1373261B1 CYCLOPROPAHETEROCYCLES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 有权
标题翻译： CYCLOPROPAHETEROCYCLEN比非核苷逆转录酶抑制剂
公开(公告)号：EP1373261B1
公开(公告)日：2011-05-04
申请号：EP02748329.6
申请日：2002-03-04
申请人： Medivir AB
发明人： LINDSTRÖM, Stefan , SAHLBERG, Christer , WALLBERG, Hans , KALYANOV, Genaidy , ODEN, Lourdes , NAESLUND, Lotta
IPC分类号： C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/35 , A61P31/18 , C07D405/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of Formula (I), where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CHR8)n--D-(CHR8)m-; D is -NR9-, -O-, -S-, -S(=O)- or -S(=O)2-; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl;R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.

3. 发明公开

EP1373261A2 CYCLOPROPAHETEROCYCLES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 有权
标题翻译： CYCLOPROPAHETEROCYCLEN比非核苷逆转录酶抑制剂
公开(公告)号：EP1373261A2
公开(公告)日：2004-01-02
申请号：EP02748329.6
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： LINDSTRÖM, Stefan , SAHLBERG, Christer , WALLBERG, Hans , KALYANOV, Genaidy , ODEN, Lourdes , NAESLUND, Lotta
IPC分类号： C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/35 , A61P31/18 , C07D405/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of Formula (I), where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CHR8)n--D-(CHR8)m-; D is -NR9-, -O-, -S-, -S(=O)- or -S(=O)2-; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl;R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.

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