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1. 发明申请

WO2004021969A2 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：WO2004021969A2
公开(公告)日：2004-03-18
申请号：PCT/EP2003/009872
申请日：2003-09-05
申请人： MEDIVIR AB , ANTONOV, Dmitry , SUND, Christian , LINDSTRÖM, Stefan , SAHLBERG, Christer
发明人： ANTONOV, Dmitry , SUND, Christian , LINDSTRÖM, Stefan , SAHLBERG, Christer
IPC分类号： A61K
CPC分类号： C07D213/73 , C07D213/65 , C07D307/93 , C07D311/94 , C07D333/78 , C07D335/06 , C07D405/12 , Y02P20/582
摘要： A compound of the formula (Y): where; R 1 is O, S; R 2 is a nitrogen-containing heterocycle; R 3 is H, C l -C 3 alkyl; X is -(CR 8 R 8 ') n -D-(CR 8 R 8 ') m -; D is a bond, -NR 9 -, -O-, -S-, -S(=O)- or -S(=O) 2 -; n and m are independently 0, 1 or 2, R 8 and R 8 ' are independently H, C 1 -C 3 alkyl, haloC 1 -C 3 alkyl, hydroxy, or R 8 and R 8 ' together with their adjacent C atom is -C(=O)-; R 9 is independently H, C 1 -C 3 alkyl; E is CH 2 -, -CHOH-, -C(=O)-, -NR 9 -, -O-, -S-, -S(=O) 2 -; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q ≤ 2; R 10 is an optionally substituted carbocycle or heterocycle; R 11 is independently H, C 1 -C 3 alkyl, halo substituted C l -C 3 alkyl, hydroxy; have utility as HIV antivirals.
摘要翻译：式（Y）的化合物：其中; R1为O，S; R2是含氮杂环; R3是H，C1-C3烷基; X是 - （CR8R8'）n-D-（CR8R8'）m-; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O） n和m独立地为0,1或2，R 8和R 8'独立地为H，C 1 -C 3烷基，卤代C 1 -C 3烷基，羟基或R 8和R 8'与它们相邻的C原子一起为-C（= O） - ; R9独立地为H，C1-C3烷基; E是CH 2 - ， - CHOH - ， - C（= O） - ， - NR 9 - ， - O - ， - S - ， - S（= O） n和m独立地为0,1或2; p和q独立地为0,1或2，其中p + q <= 2; R 10是任选取代的碳环或杂环; R 11独立地为H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基，羟基; 具有艾滋病毒抗病毒药物的作用。

2. 发明申请

WO2005066131A1 NON-NUCLEOTIDE 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：WO2005066131A1
公开(公告)日：2005-07-21
申请号：PCT/SE2004/002034
申请日：2004-12-30
申请人： MEDIVIR AB , SUND, Christian , ROUE, Nathalie , LINDSTRÖM, Stefan , ANTONOV, Dmitry , SAHLBERG, Christer , JANSSON, Katarina
发明人： SUND, Christian , ROUE, Nathalie , LINDSTRÖM, Stefan , ANTONOV, Dmitry , SAHLBERG, Christer , JANSSON, Katarina
IPC分类号： C07D213/75
CPC分类号： C07D409/12 , C07D405/12 , C07D405/14 , C07D409/14
摘要： Compounds of the formula Z: where; A is CH or N; R 1 is a substituent to a carbon atom in the ring containing A selected from -S(=O) p Ra, where Ra is -C 1 -C 4 alkyl, -ORx, -NRxRx, -NHNRxRx, - NHNHC(=O)ORx, -NRxOH; -C(=O)-Rb, where Rb is -CT-C4-alkyl, ORx, -NRxRx, -NHNRxRx, -NHC 1 -C 3 -alkyl-C(=O)Orx -NRxRc, where Rc is H, C 1 -C 4 alkyl, -NRxRx; -C(=0)Rd, -CN, S(=O)pRx where Rd is Rd is C1-C4-alkyl, -ORx, -NRxRx C 1 -C 3 -alkyl-O-Cl-C3alkylC(=O)ORx, -C 1 -C 3 -alkyl-COORx; -C 1 -C 3 alkyl-OH or C 1 -C 4 alkyl ethers or esters thereof (O-C l -C 3 alkyl)q-O-Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C 1 -C 4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, -S(=O),- or -CH 2 -, where r is 0, 1 or 2; R 3 -R 7 are substituents as defined in the specification; X is -(CR 8 R 8 ')n-D-(CR 8 R 8 ')m-; D is a bond, -NR 9 -, -0-, -S-, -S(=0)- or -S(=0) 2 -; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
摘要翻译：式Z的化合物：其中; A是CH或N; R 1是含有选自-S（= O）p R a的A的环中的碳原子的取代基，其中R a是-C 1 -C 4烷基，-OR x，-NR x R x，-NHNR x R x，-NH NH（= O）OR x， NRxOH; -C（= O）-R b，其中R b是-C 1 -C 4 - 烷基，OR x，-NR x R x，-NHNR x R x，-NHC 1 -C 3 - 烷基-C（= O）OR x -NR x R c，其中R c是H， C4烷基，-NRxRx; -C（= O）R d，-CN，S（= O）p R x其中Rd是Rd是C 1 -C 4 - 烷基，-OR x，-NR x R x C 1 -C 3烷基-O-C 1 -C 3烷基C（= O）OR x， -C 1 -C 3 - 烷基 - COORx; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯（O-Cl-C 3烷基）q-O-Rx具有1-3个杂原子的5或6元芳环p为1或2; R x独立地选自H，C 1 -C 4烷基或乙酰基; 或一对Rx可与相邻的N原子一起形成环; L是-O - ， - S（= O）， - 或-CH 2 - ，其中r是0,1或2; R3-R7是说明书中定义的取代基; X是 - （CR8R8'）n-D-（CR8R8'）m-; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O）其药学上可接受的盐和前药具有作为HIV抗病毒剂的效用。

3. 发明申请

WO2010024772A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010024772A1
公开(公告)日：2010-03-04
申请号：PCT/SE2009/050976
申请日：2009-08-28
申请人： Medivir AB , SAHLBERG, Christer , SUND, Christian , WIKTELIUS, Daniel , BELDA, Oscar
发明人： SAHLBERG, Christer , SUND, Christian , WIKTELIUS, Daniel , BELDA, Oscar
IPC分类号： C07C237/22 , A61K38/05 , A61P27/06 , A61P9/04 , A61P9/12 , C07D213/04 , C07D275/02
CPC分类号： C07D213/30 , C07C237/22 , C07C255/60 , C07C2601/02 , C07D277/24
摘要： The invention provides compounds of the formula (I wherein Q is trifluoromethyl, C 3 -C 6 cycloalkyl, phenyl, p-fluorophenyl, pyridyl, thiazolyl, furyl, thienyl or C 3 -C 6 cycloalkylethynyl; R 3 is C 1 -C 6 alkyl; R 4 is C 1 -C 6 alkyl; W is cyano or fluoro; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.
摘要翻译：本发明提供式（I）化合物，其中Q为三氟甲基，C 3 -C 6环烷基，苯基，对氟苯基，吡啶基，噻唑基，呋喃基，噻吩基或C3-C6环烷基乙炔基; R3为C1-C6烷基; R4为C1-C6烷基; W为氰基或氟;或其药学上可接受的盐，水合物或N-氧化物。本发明的化合物是天冬氨酰蛋白酶如肾素的抑制剂，并且其它可用于治疗与RAS活性相关的病症，例如高血压，心力衰竭和肾功能不全。

4. 发明申请

WO2009053277A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2009053277A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/063802
申请日：2008-10-14
申请人： MEDIVIR AB , SUND, Christian , SAHLBERG, Christer , BELDA, Oscar
发明人： SUND, Christian , SAHLBERG, Christer , BELDA, Oscar
IPC分类号： C07C237/00 , A61K31/16 , C07D213/74 , C07D265/30
CPC分类号： C07D213/74 , C07C237/06 , C07C237/08 , C07C237/10 , C07C243/28 , C07C271/16 , C07C311/08 , C07C311/18 , C07D265/30
摘要： The invention provides compounds of the formula (I) wherein A is selected from the partial structures A1, A2 and A3; Ry and Ry' are both hydrogen, or Ry and Ry' together with the nitrogen atom to which they are attached form a cyclic amine such as morpholine, piperidine, piperazine or pyrrolidine; L is NHNH, CH 2 NH, O or S; Y is NH, NHNH, NHC(=O), S(=O) 2 NH, NHS(=O) 2 , CH 2 , CH 2 NH, O, S or S(=0) p ; Q is aryl or heterocyclyl; Z is O, S, NRa or S(=0) p ; m is O, 1 or 2; n is O, 1, 2 or 3; p is independently 1 or 2; q is 0 or 1; Ra is H or C 1 -C 4 alkyl; R1 is hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkylC 0 -C 3 alkyl, arylC 0 -C 3 alkyl or heterocyclylC 0 -C 3 alkyl, R 4'' is H or C 1 -C 6 alkyl; or R 4' and R 4'' together with the carbon atom to which they are attached define a C 3 -C 6 cycloalkyl; W is H, C 1 -C 6 alkyl, C 3 -C 7 ycycloalkyl, aryl or heterocyclyl; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.
摘要翻译：本发明提供式（I）化合物，其中A选自部分结构A1，A2和A3; Ry和Ry'都是氢，或者Ry和Ry'与它们所连接的氮原子一起形成环胺，如吗啉，哌啶，哌嗪或吡咯烷; L是NHNH，CH 2 NH，O或S; Y是NH，NHNH，NHC（= O），S（= O）2NH，NHS（= O）2，CH2，CH2NH，O，S或S（= O）p; Q是芳基或杂环基; Z是O，S，NR a或S（= O）p; m为O，1或2; n是0,1,2或3; p独立地为1或2; q为0或1; R a是H或C 1 -C 4烷基; R 1是氢，C 1 -C 6烷基，C 3 -C 7环烷基C 0 -C 3烷基，芳基C 0 -C 3烷基或杂环基C 0 -C 3烷基，R 4“是H或C 1 -C 6烷基; 或R 4'和R 4“与它们所连接的碳原子一起定义为C 3 -C 6环烷基; W是H，C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂环基; 或其药学上可接受的盐，水合物或N-氧化物。本发明的化合物是天冬氨酰蛋白酶如肾素的抑制剂，并且其它可用于治疗与RAS活性有关的病症，例如高血压，心力衰竭和肾功能不全。

5. 发明申请

WO2008119772A1 AMIDE DERIVATIVES AS INHIBITORS OF ASPARTYL PROTEASES 审中-公开
标题翻译：作为ASPARTYL蛋白抑制剂的酰胺衍生物
公开(公告)号：WO2008119772A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053765
申请日：2008-03-28
申请人： MEDIVIR AB , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , ROSENQUIST, Åsa , SAMUELSSON, Bertil , SAHLBERG, Christer , SUND, Christian , BELDA, Oscar , IVANOV, Vladimir , ODEN, Lourdes , NORÉN, Rolf
发明人： KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , ROSENQUIST, Åsa , SAMUELSSON, Bertil , SAHLBERG, Christer , SUND, Christian , BELDA, Oscar , IVANOV, Vladimir , ODEN, Lourdes , NORÉN, Rolf
IPC分类号： C07C311/08 , A61K31/18 , A61P9/12 , A61P9/04 , A61P27/06 , A61P13/12 , C07C309/66 , C07C311/07 , C07C255/57
CPC分类号： C07C311/08 , C07C255/57 , C07C309/66 , C07C311/07 , C07C2601/02 , C07C2601/08
摘要： The invention provides compounds of the formula (I). N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein W is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, aryl or heterocyclyl; Q is aryl or heterocyclyl; A is a five or six membered saturated, partially unsaturated or aromatic ring; D is formula (II) or formula (III); and the other variables are as defined in the specification. The compounds of the invention are inhibitors of aspartyl proteases such as renin and BACE and are among other things useful for the treatment and/or prophylaxis of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency and for the treatment and or prophylaxis of conditions associated with BACE activity such as of Alzheimer's disease.
摘要翻译：本发明提供式（I）化合物。 N-氧化物，加成盐，季胺，金属配合物，立体化学异构形式及其代谢物，其中W是H，C 1 -C 6烷基，C 1 -C 6烷基， 3个-C 6环烷基，芳基或杂环基; Q是芳基或杂环基; A是五或六元饱和，部分不饱和或芳环; D是式（II）或式（III）; 其他变量如规范中所定义。本发明的化合物是天冬氨酰蛋白酶如肾素和BACE的抑制剂，并且用于治疗和/或预防与RAS活性有关的病症，例如高血压，心力衰竭和肾功能不全以及治疗和/或预防与诸如阿尔茨海默氏病之类的BACE活性相关的病症。

6. 发明申请

WO2008107365A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2008107365A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052416
申请日：2008-02-28
申请人： MEDIVIR AB , BELDA, Oscar , SUND, Christian , IVANOV, Vladimir , WIKTELIUS, Daniel , SAHLBERG, Christer , SAMUELSSON, Bertil , ROSENQUIST, Åsa , WÅNGSELL, Fredrik , KVARNSTRÖM, Ingemar
发明人： BELDA, Oscar , SUND, Christian , IVANOV, Vladimir , WIKTELIUS, Daniel , SAHLBERG, Christer , SAMUELSSON, Bertil , ROSENQUIST, Åsa , WÅNGSELL, Fredrik , KVARNSTRÖM, Ingemar
IPC分类号： A61K31/44 , C07D213/40 , C07C237/12 , C07D213/38
CPC分类号： C07D307/33 , C07C237/22 , C07C255/60 , C07D213/38 , C07D213/40
摘要： The invention provides compounds of the formula I wherein Q is aryl or heterocyclyl any of which is optionally substituted; Z is O, S, NRa or S(=O) p ; Y is NH, NHNH, CH 2 NH, O, S or S(=O) p ; n is 0, 1, 2 or 3; m is 0, 1 or 2; p is 1 or 2; Ra is H or C 1 -C 4 alkyl; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkanediylC 3 -C 7 cycloalkyl, C 0 -C 3 alkanediylaryl or C 0 - C3alkanediylheterocyclyl; R 2 is hydrogen or C 1 -C 6 alkyl; X' is hydrogen, fluoro, hydroxy, amino or C 1 -C 6 alkoxy; X" is hydrogen, or when X' is fluoro, then X" may also be fluoro; R 3 is C 1 -C 6 alkyl; R 4' is C 1 -C 6 alkyl; R 4" is H or C 1 -C 6 alkyl; or R 4' and R 4" together with the carbon atom to which they are attached define a C 3 -C 6 cycloalkyl; W is C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, aryl or heterocyclyl any of which is optionally substituted; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.
摘要翻译：本发明提供式I化合物，其中Q是任选被取代的芳基或杂环基; Z是O，S，NR a或S（= O）p。 Y是NH，NHNH，CH 2 NH，O，S或S（= O）p; n为0,1,2或3; m为0,1或2; p为1或2; R a是H或C 1 -C 4烷基; R 1是氢，C 1 -C 6烷基，C 0 -C 3 - 烷二基C 3 -C 7环烷基，C 0 -C 3烷二基芳基或C 0 < / C3-烷二基杂环基; R 2是氢或C 1 -C 6烷基; R 2是氢或C 1 -C 6烷基; X'是氢，氟，羟基，氨基或C 1 -C 6烷氧基; X“是氢，或者当X'是氟时，X”也可以是氟; R 3是C 1 -C 6烷基; R 3是C 1 -C 6烷基; R 4是C 1 -C 6烷基; R 4是C 1 -C 6烷基; R 4是H或C 1 -C 6烷基;或R 4'和R“ 4“与它们所连接的碳原子一起定义为C 3 -C 6环烷基; W是C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂环基，其中任何一个任选地被取代; 或其药学上可接受的盐，水合物或N-氧化物。本发明的化合物是天冬氨酰蛋白酶如肾素的抑制剂，并且其它可用于治疗与RAS活性有关的病症，例如高血压，心力衰竭和肾功能不全。

7. 发明申请

WO2007006707A1 1- [2' , 3' -DIDEOXY-3' C- (HYDROXYMETHYL) - BETA-D-ERYTHRO-PENTOFURANOSYL] CYTOSINE DERIVATIVES AS HIV INHIBITORS 审中-公开
标题翻译：作为艾滋病毒抑制剂的1- [2'，3'-二氧代-3'C-（羟甲基） - β-D-呋喃基 - 戊氧羰基]胞嘧啶衍生物
公开(公告)号：WO2007006707A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063919
申请日：2006-07-05
申请人： MEDIVIR AB , ZHOU, Xiao-Xiong , SAHLBERG, Christer
发明人： ZHOU, Xiao-Xiong , SAHLBERG, Christer
IPC分类号： C07D493/04 , A61K31/513 , A61P31/18
CPC分类号： C07D493/04
摘要： Compounds of the formula (I) wherein: R 1 is independently H 1 -OR 3 , -NHR 4 ; C 1 -C 4 alkyl; or, when n is 2, adjacent R 1 together define an olefin ic bond; R 2 is H; or when the gem R 1 is C 1 -C 4 alkyl, that R 2 may also be C 1 -C 4 alkyl; or when the gem R 1 is -OR 3 , that R 2 may also be -C(=O)OH or a pharmaceutically acceptable ester thereof; R 3 is independently H, or a pharmaceutically acceptable ester thereof; R 4 is independently H or a pharmaceutically acceptable amide thereof; R 5 and R6 are H or an amine prodrug moiety n is 1 , 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.
摘要翻译：式（I）的化合物其中：R 1独立地是H 1 - ， - 3， - NHR 4， ; C 1 -C 4烷基; 或者当n为2时，相邻的R 1一起限定了烯烃键; R 2是H; 或者当R 1是C 1 -C 4烷基时，R 2也可以是C 1 -C 4烷基， C 1 -C 4烷基; 或当Gem R 1为-OR 3时，R 2还可以是-C（= O）OH或药学上可接受的酯物; R 3独立地为H或其药学上可接受的酯; R 4独立地是H或其药学上可接受的酰胺; R 5和R 6是H或胺前体药物部分n是1,2或3; 及其药学上可接受的盐; 在治疗或预防艾滋病毒方面具有实用价值，特别是逆转录酶突变体，其允许通过ATP或焦磷酸盐介导的切除从核心DNA链上切除核苷或磷酸核苷酸。

8. 发明申请

WO2013095275A1 NOVEL HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译：新型丙型肝炎病毒抑制剂
公开(公告)号：WO2013095275A1
公开(公告)日：2013-06-27
申请号：PCT/SE2012/051426
申请日：2012-12-19
申请人： MEDIVIR AB
发明人： AYESA, Susana , BELDA, Oscar , BJÖRKLUND, Catarina , NILSSON, Magnus , RUSSO, Francesco , SAHLBERG, Christer , WIKTELIUS, Daniel
IPC分类号： C07D413/14 , A61K31/4178 , A61K31/4192 , A61K31/427 , A61K31/4439 , A61K31/4523 , A61K31/496 , A61K31/5377 , A61K31/5386 , A61K31/553 , A61P31/14 , C07D403/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D401/14
CPC分类号： C07D495/10 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
摘要： The invention provides compounds of formula (I): wherein Rings A and A' are independently 5-membered optionally substituted aromatic heterocycles; Q is C(=O)NR 1 R 1' or formula U is C(R 4 ) 2 , O, S, S(=O) 2 , C(R 4 ) 2 C(R 4 ) 2 , CH 2 O, OCH 2 , CH 2 S, SCH 2 , CH 2 S(=O) 2 , S(=O)CH 2 or C=C(R u ) 2 ; X is CH 2 , CHR 12 , CR 12 R 12 , O, S, S(=O) 2 or NR x ; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
摘要翻译：本发明提供式（I）化合物：其中环A和A'独立地是5元任选取代的芳族杂环; Q是C（= O）NR1R1'或式U是C（R4）2，O，S，S（= O）2，C（R4）2C（R4）2，CH2O，OCH2，CH2S，SCH2，CH2S = O）2，S（= O）CH 2或C = C（Ru）2; X是CH 2，CHR 12，CR 12 R 12，O，S，S（= O）2或NR x; m为0,1,2或3; n为0,1,2或3; 其他变量如权利要求中所定义，其用于治疗或预防丙型肝炎病毒感染以及相关方面。

9. 发明申请

WO2003020705A1 UREA AND THIOUREA DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：尿素和硫脲衍生物作为非核苷酸逆转录酶抑制剂
公开(公告)号：WO2003020705A1
公开(公告)日：2003-03-13
申请号：PCT/EP2002/002346
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： SAHLBERG, Christer , ANTONOV, Dmitry , WALLBERG, Hans , NOREEN, Rolf
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D213/85
摘要： Compounds of the 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 -(CR 8 R 9 ) n -, R 8 and R 9 are independently H, C 1 -C 3 alkyl, OH or R 8 and R 9 together are =0, n is 1, 2 or 3, 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R 1是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 - （CR 8 R 9）n - ， - R 8和R 9独立地为H，C 1 -C 3烷基，OH或R 8和R 9一起为= 0，n为1,2或3，并且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。

10. 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。

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