专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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。

4. 发明申请

WO2010107384A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010107384A1
公开(公告)日：2010-09-23
申请号：PCT/SE2010/050307
申请日：2010-03-19
申请人： MEDIVIR AB , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , JOHANSSON, Per-Ola , LUNDGREN, Stina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , WIKTELIUS, Daniel , WÄHLING, Horst
发明人： AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , JOHANSSON, Per-Ola , LUNDGREN, Stina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , WIKTELIUS, Daniel , WÄHLING, Horst
IPC分类号： C07D213/81 , A61K31/166 , A61K31/18 , A61K31/402 , A61K31/426 , A61K31/44 , A61K31/4439 , A61K31/444 , A61P25/28 , C07C237/34 , C07C311/08 , C07D207/08 , C07D277/28 , C07D401/06 , C07D417/12
CPC分类号： C07C311/08 , C07C237/34 , C07C2601/02 , C07C2601/04 , C07D207/08 , C07D213/81 , C07D277/28 , C07D401/06 , C07D417/12
摘要： A compound of formula (I) N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR 1 Or N; formula (A) or formula (B) D is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, G is NR 10 or O Q is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 Cycloalkyl, aryl or heterocyclyl; W is H, C 1 -C 6 alkyl, C 3 -C 6 Cycloalkyl, CH 2 F, CHF 2 or CF 3 ; one of X' and X" is H or CH 3 , the other is C 1 -C 3 alkyl, F, OH, NRaRb, CF 3 or N 3 ; or X' and X" are both F; Y is NRd or O; Z is O, NRa, CHRd, CF 2 or S(=0)r or a bond; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：式（I）的化合物N-氧化物，加成盐，季胺金属络合物立体化学异构形式及其代谢物，其中A是CR 1或N; 式（A）或式（B）D是H，C1-C6烷基，C2-C6链烯基，C2-C6炔基，G是NR10或OQ是C1-C6烷基，C2-C6链烯基，C2-C6炔基，C3-C6环烷基，芳基或杂环基 ; W是H，C 1 -C 6烷基，C 3 -C 6环烷基，CH 2 F，CHF 2或CF 3; X'和X“之一是H或CH3，另一个是C 1 -C 3烷基，F，OH，NR a R b，CF 3或N 3;或X'和X”均为F; Y为NRd或O; Z是O，NR a，CHR d，CF 2或S（= O）r或键; 其他变量如规范中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

5. 发明申请

WO2010042030A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010042030A1
公开(公告)日：2010-04-15
申请号：PCT/SE2009/051105
申请日：2009-10-05
申请人： MEDIVIR AB , LUNDBERG, Stina , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , HAMMER, Kristin , JOHANSSON, Per-Ola , LINDSTRÖM, Stefan , ROSENQUIST, Åsa , SAMUELSSON, Bertil , BÄCK, Marcus , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , BJÖRKLUND, Katarina
发明人： LUNDBERG, Stina , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , HAMMER, Kristin , JOHANSSON, Per-Ola , LINDSTRÖM, Stefan , ROSENQUIST, Åsa , SAMUELSSON, Bertil , BÄCK, Marcus , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , BJÖRKLUND, Katarina
IPC分类号： C07D213/75 , A61K31/195 , A61K31/455 , A61P25/28 , C07C229/38 , C07D207/26 , C07D263/20 , C07D279/02 , C07D285/06
CPC分类号： C07D213/81 , C07C233/78 , C07C237/34 , C07C309/66 , C07C311/08 , C07C311/16 , C07D207/27 , C07D263/22 , C07D277/28 , C07D279/02 , C07D285/10 , C07D295/26 , C07D401/12 , C07D417/12
摘要： A compound of formula (I): N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR 1 or N; D is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or Q is C 2 -C 6 alkenyl, C 2 -Cealkynyl, aryl or heterocyclyl; W is H, Ci-Cealkyl, C 2 -C 6 alkenyl, haloC 1 -C 3 alkyl, hydroxyC 1 -C 3 alkyl, C 3 -C 6 Cy cloalkyl, aryl or heterocyclyl; one of X' and X" is H or CH 3 , the other is C 1 -C 3 alkyl, F, OH, NRaRb, CF 3 or N 3 ; or X' and X" are both F; Y is a bond, CH 2 , NRa, O, CH 2 CH 2 , CH 2 NRa, CH 2 O or S(=O) r ; Z is O, S(=O) r or NRa; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：式（I）的化合物：N-氧化物，加成盐，季胺金属络合物立体化学异构形式及其代谢物，其中A是CR 1或N; D是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或Q是C 2 -C 6烯基，C 2 -C 6炔基，芳基或杂环基; W是H，C 1 -C 6烷基，C 2 -C 6烯基，卤代C 1 -C 3烷基，羟基C 1 -C 3烷基，C 3 -C 6环烷基，芳基或杂环基; X'和X“之一是H或CH3，另一个是C 1 -C 3烷基，F，OH，NR a R b，CF 3或N 3;或X'和X”均为F; Y是键，CH2，NRa，O，CH2CH2，CH2NRa，CH2O或S（= O）r; Z是O，S（= O）r或NR a; 其他变量如规范中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式