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1. 发明申请

WO2005073216A2 HCV NS-3 SERINE PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS-3丝氨酸蛋白酶抑制剂
公开(公告)号：WO2005073216A2
公开(公告)日：2005-08-11
申请号：PCT/SE2005/000096
申请日：2005-01-28
申请人： MEDIVIR AB , ROSENQUIST, Åsa , THORSTENSSON, Fredrik , JOHANSSON, Per-Ola , KVARNSTRÖM, Ingemar , AYESA, Susana , CLASSON, Björn , RAKOS, Lazlo , SAMUELSSON, Bertil
发明人： ROSENQUIST, Åsa , THORSTENSSON, Fredrik , JOHANSSON, Per-Ola , KVARNSTRÖM, Ingemar , AYESA, Susana , CLASSON, Björn , RAKOS, Lazlo , SAMUELSSON, Bertil
IPC分类号： C07D401/00
CPC分类号： A61K31/47 , C07C235/40 , C07C237/04 , C07C237/10 , C07C247/04 , C07C271/22 , C07C281/02 , C07C309/73 , C07C311/51 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07D207/16 , C07D215/20 , C07D215/233 , C07D245/04 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07K5/0205 , C07K5/06034 , C07K5/06052
摘要： Compounds of the formula (F) where the variables are as defined in the specification inhibit the NS3 protease of flavivirus sych as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.
摘要翻译：变量如本说明书中定义的式（F）化合物抑制黄病毒sych的NS3蛋白酶作为丙型肝炎病毒（HCV）。化合物包括杂环P2单元和更远离天然底物标称切割位点的那些抑制剂部分之间的新连接，该连接反转相对于靠近切割位点的末端侧的肽键的取向。

2. 发明申请

WO2005073195A2 HCV NS-3 SERINE PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS-3丝氨酸蛋白酶抑制剂
公开(公告)号：WO2005073195A2
公开(公告)日：2005-08-11
申请号：PCT/SE2005/000097
申请日：2005-01-28
申请人： MEDIVIR AB , ROSENQUIST, Åsa , THORSTENSSON, Fredrik , JOHANSSON, Per-Ola , KVARNSTRÖM, Ingemar , SAMUELSSON, Bertil , WALLBERG, Hans
发明人： ROSENQUIST, Åsa , THORSTENSSON, Fredrik , JOHANSSON, Per-Ola , KVARNSTRÖM, Ingemar , SAMUELSSON, Bertil , WALLBERG, Hans
IPC分类号： C07D215/00
CPC分类号： A61K31/47 , C07C235/40 , C07C237/04 , C07C237/10 , C07C247/04 , C07C271/22 , C07C281/02 , C07C309/73 , C07C311/51 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07D207/16 , C07D215/20 , C07D215/233 , C07D245/04 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07K5/0205 , C07K5/06034 , C07K5/06052
摘要： Peptidomimetic compounds are described which inhibit the NS3 protease of the hepatitis C virus (HCV). The compounds have the formula where the variable definitions are as provided in the specification. The compounds comprise a carbocyclic P2 unit in conjunction with a novel linkage to those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.
摘要翻译：描述了拟肽化合物，其抑制丙型肝炎病毒（HCV）的NS3蛋白酶。该化合物具有下式，其中变量定义如说明书中所提供。所述化合物包含碳环P2单元以及与更远离天然底物的标称切割位点的抑制剂的那些部分的新型连接，该连接反转远侧的肽键相对于切割近侧的取向站点。

3. 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。

4. 发明申请

WO2008135488A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2008135488A1
公开(公告)日：2008-11-13
申请号：PCT/EP2008/055326
申请日：2008-04-30
申请人： MEDIVIR AB , BJÖRKLUND, Catarina , KVARNSTRÖM, Ingemar , AYESA, Susana , JOHANSSON, Per-Ola , DORANGE, Ismet , ERSMARK, Karolina , SAMUELSSON, Bertil , ROSENQUIST, Åsa
发明人： BJÖRKLUND, Catarina , KVARNSTRÖM, Ingemar , AYESA, Susana , JOHANSSON, Per-Ola , DORANGE, Ismet , ERSMARK, Karolina , SAMUELSSON, Bertil , ROSENQUIST, Åsa
IPC分类号： C07D267/00 , C07D313/00 , A61P25/28 , A61K31/365
CPC分类号： C07D313/00 , C07D267/00
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 G is-O-, -S(=O) r -, -CRdRd or -NRa-; W is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, aryl or heterocyclyl; L 1 is a bond, methyleneor ethylene; L 2 is CHR 1 ;or L 1 and L 2 together form CH=CH; L 3 is a bond, C(=O) or CH 2 ; V 1 and V 2 are independently a bond, NRa, CRdRd or O; R 1 is H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 4 alkoxyC 1 -C 4 alkyl, C 1 -C 4 alkoxyC 1 -C 4 alkoxyC 1 -C 4 alkyl, C 0 -C 3 alkandiylcarbocyclyl or C 0 -C 3 alkandiylheterocyclyl; R 2b are both H, or the two R 2b together form=O; ring A is a five or six membered saturated, partially unsaturated or aromatic ring; and 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：本发明提供式（I）的化合物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G是-O-，-S（= O） > - ，-CRdRd或-NRa-; W是H，C 1 -C 6烷基，C 3 -C 6 -C 6环烷基，芳基或杂环基; L 1是键，亚甲基或亚乙基; L 2是CHR 1或L 1和L 2一起形成CH = CH; L 3是一个键，C（= O）或CH 2; V 1和V 2独立地是键，NR a，CR d R d或O; R 1是H，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷氧基，C 1 -C 4烷氧基C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， / SUB> -C _{4 烷氧基C _{1 -C _{4 烷氧基C _{1 -C ₄}}}}

5. 发明申请

WO2008119773A1 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：WO2008119773A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053767
申请日：2008-03-28
申请人： MEDIVIR AB , KVARNSTRÖM, Ingemar , BÄCK, Marcus , SANDGREN, Veronica , OSCARSON, Stefan , BJÖRKLUND, Catarina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , DORANGE, Ismet
发明人： KVARNSTRÖM, Ingemar , BÄCK, Marcus , SANDGREN, Veronica , OSCARSON, Stefan , BJÖRKLUND, Catarina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , DORANGE, Ismet
IPC分类号： C07C311/07 , C07C311/08 , C07C237/22 , C07D207/26 , C07D213/56 , A61K31/18 , A61K31/16 , A61P25/28
CPC分类号： C07C311/08 , C07C237/22 , C07C311/07 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/26 , C07D213/56
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 (II) or (III) 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：本发明提供式（I）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W是H，C 1 -C 6烷基，C 3 -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（II）或（III）其他变量如说明书中所定义。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

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。

7. 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。

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