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1. 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。

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

WO2004050277A1 CONTROL SYSTEM, COMPUTER PROGRAM PRODUCT, DEVICE AND METHOD 审中-公开
标题翻译：控制系统，计算机程序产品，设备和方法
公开(公告)号：WO2004050277A1
公开(公告)日：2004-06-17
申请号：PCT/SE2003/001857
申请日：2003-11-28
申请人： ABB AB , ISRAELSSON TAMPE, Stefan , KOLLBERG, Sten , ERIKSSON, Jan-Erik , LINDBERG, Carl-Fredrik , MOLANDER, Mats , LÖFGREN, Peter , TALLBÄCK, Göte , BEL FDHILA, Rebei , SAMUELSSON, Bertil
发明人： KOLLBERG, Sten , ERIKSSON, Jan-Erik , LINDBERG, Carl-Fredrik , MOLANDER, Mats , LÖFGREN, Peter , TALLBÄCK, Göte , BEL FDHILA, Rebei , SAMUELSSON, Bertil
IPC分类号： B22D11/115
CPC分类号： B22D11/115 , B22D11/16
摘要： Control system for regulating the flow of liquid metal in a device for casting a metal, comprising detection means to measure a process variable, a control unit to evaluate the data from the detection means and means to automatically vary at least one process parameter in order to optimize casting conditions. The detection means measure a characteristic of the meniscus at least two points on the meniscus instantaneously throughout the casting process.
摘要翻译：用于调节用于铸造金属的装置中的液态金属的流动的控制系统，包括用于测量过程变量的检测装置，用于评估来自检测装置的数据的控制单元和自动地改变至少一个过程参数的装置，以便优化铸造条件。检测装置在整个铸造过程中瞬间测量弯液面上至少两个点的弯月面的特征。

4. 发明申请

WO2004026896A3 HCV NS-3 SERINE PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2004026896A3
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010595
申请日：2003-09-23
申请人： MEDIVIR AB , OSCARSSON, Karin , SAMUELSSON, Bertil
发明人： OSCARSSON, Karin , SAMUELSSON, Bertil
IPC分类号： C07K7/06
摘要： Compounds possessing novel P1 amino acid replacements of the formulae (I) or (II) where R 1 is a peptidic or peptidomimetic recognition sequence P2-Pn targeting the S2- Sn pockets of HCV NS-3 serine protease, where n is 3-6, which recognition sequence is peptide bonded to formula (I); R 2 is H, C 1 -C 3 alkyl; R 3 is C 1 -C 3 alkyl, optionally substituted with 1-3 halo atoms or -SH; R 4 is =O, halo, amino or -OH; R 5 is C 1 -C 6 alkyl, C 0 -C 3 -alkylaryl, C 0 -C 3 -alkylhet, C 0 -C 3 -alkylcycloC 3 -C 6 -alkyl, any of which can be optionally substituted with hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, amino, halo, carboxy, cyano, azido, mercapto, nitro, C 0 -C 3 -alkylaryl, C 0 -C 3 -alkylhet, C 0 -C 3 -alkylcycloalkyl; R 6 is H C 1 -C 3 alkyl or cyclises with the nominal N-terminal to form a macrocycle; with the proviso that if R 4 is =O, then the alkyl moiety of R 5 as alkylaryl or alkylhet is C 1 -C 3 alkanyl or C 2 -C 3 alkenyl; have utility as HCV NS-3 serine protease inhibitors.

5. 发明申请

WO2010034789A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2010034789A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/062407
申请日：2009-09-24
申请人： Medivir AB , IVANOV, Vladimir , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , KAHNBERG, Pia , WÄHLING, Horst
发明人： IVANOV, Vladimir , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , KAHNBERG, Pia , WÄHLING, Horst
IPC分类号： C07D491/048 , A61K31/496 , A61P19/00
CPC分类号： C07D491/048
摘要： Compounds of the formula II, wherein R 3 is C 1 -C 3 alkyl or C 3 -C 6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R 3 is C 3 -C 6 cycloalkyl it may alternatively be gem substituted with fluoro; R 4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A 1 is CH or N, A 2 is CR 6 R 7 or NR 6 , provided at least one of A 1 and A 2 comprises N; n is 0 or 1 such that the ring containing A 1 and A 2 is a saturated, nitrogen-containing ring of 5 or 6 ring atoms; R 6 is H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 3 alkyl-O-C 1 -C 3 alkyl, or when A 2 is C, R 6 can also be C 1 -C 4 alkoxy or F; R 7 is H, C 1 -C 4 alkyl or F; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：其中R 3为C 1 -C 3烷基或C 3 -C 6环烷基，其中R 3为C 3 -C 6环烷基时，任选被一个或两个甲基和/或氟，三氟甲基或甲氧基取代，被氟取代; R4是甲基或氟; m为0,1或2; E是任选被甲基或氟取代的键或噻唑基; A1是CH或N，A2是CR6R7或NR6，条件是A1和A2中的至少一个包括N; n为0或1，使得含有A 1和A 2的环是5或6个环原子的饱和的含氮环; R6是H，C1-C4烷基，C1-C4卤代烷基，C1-C3烷基-O-C1-C3烷基，或当A2是C时，R6也可以是C1-C4烷氧基或F; R 7为H，C 1 -C 4烷基或F; 或其药学上可接受的盐，N-氧化物或其水合物，可用于治疗组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

6. 发明申请

WO2007068474A1 (2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：（2,5-DIOXOIMIDAZOLIDIN-I-YL）-N-羟基 - 乙酰胺作为金属蛋白酶抑制剂
公开(公告)号：WO2007068474A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/012019
申请日：2006-12-13
申请人： MEDIVIR AB , JIANGSU HENGRUI MEDICINE COMPANY LIMITED , WALLBERG, Hans , XU, Ming, Hua , LIN, Guo, Qiang , LEI, Xin, Sheng , SUN, Piaoyang , PARKES, Kevin , JOHNSON, Tony , SAMUELSSON, Bertil
发明人： WALLBERG, Hans , XU, Ming, Hua , LIN, Guo, Qiang , LEI, Xin, Sheng , SUN, Piaoyang , PARKES, Kevin , JOHNSON, Tony , SAMUELSSON, Bertil
IPC分类号： C07D233/74 , C07D233/78 , C07D233/76
CPC分类号： C07D233/78 , C07D233/76
摘要： The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).
摘要翻译：本发明提供式（I）化合物，其中变量如说明书中所定义。本发明的化合物是金属蛋白酶MMP-12的抑制剂，其它可用于治疗阻塞性气道疾病如慢性阻塞性肺疾病（COPD）。

7. 发明申请

WO2006084688A1 HIV protease inhibitors 审中-公开
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：WO2006084688A1
公开(公告)日：2006-08-17
申请号：PCT/EP2006/001135
申请日：2006-02-09
申请人： MEDIVIR AB , EKEGREN Jenny , HALLBERG, Anders , WALLBERG, Hans , SAMUELSSON, Bertil , KANNAN, Mahalingan
发明人： EKEGREN Jenny , HALLBERG, Anders , WALLBERG, Hans , SAMUELSSON, Bertil , KANNAN, Mahalingan
IPC分类号： C07C271/22 , C07C311/06 , C07C275/24 , C07D213/42 , C07D241/12 , C07D333/58 , C07D317/58 , C07D261/08 , A61K31/18 , A61K31/17 , A61K31/325 , A61K31/38 , A61K31/42 , A61K31/44 , A61K31/495
CPC分类号： C07D213/42 , C07C271/22 , C07C275/24 , C07C311/06 , C07C2602/08 , C07D241/12 , C07D261/08 , C07D263/52 , C07D303/48 , C07D307/33 , C07D317/58 , C07D333/58
摘要： Compounds of the formula (I): Wherein R1, R2, X and N are as defined in the specification; E is N, CH; A1 and A" are terminal groups as defined in the specification. The compounds have utility as HIV-I protease inhibitors.
摘要翻译：式（I）化合物：其中R1，R2，X和N如说明书中所定义; E为N，CH; A1和A“是本说明书中定义的末端基团，该化合物可用作HIV-1蛋白酶抑制剂。

8. 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。

9. 发明申请

WO2004026896A2 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：WO2004026896A2
公开(公告)日：2004-04-01
申请号：PCT/EP0310595
申请日：2003-09-23
申请人： MEDIVIR AB , OSCARSSON KARIN , SAMUELSSON BERTIL
发明人： OSCARSSON KARIN , SAMUELSSON BERTIL
IPC分类号： A61K38/00 , C07K7/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Compounds possessing novel P1 amino acid replacements of the formulae (I) or (II) where R is a peptidic or peptidomimetic recognition sequence P2-Pn targeting the S2- Sn pockets of HCV NS-3 serine protease, where n is 3-6, which recognition sequence is peptide bonded to formula (I); R is H, C1-C3 alkyl; R is C1-C3 alkyl, optionally substituted with 1-3 halo atoms or -SH; R is =O, halo, amino or -OH; R is C1-C6 alkyl, C0-C3-alkylaryl, C0-C3-alkylhet, C0-C3-alkylcycloC3-C6-alkyl, any of which can be optionally substituted with hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 alkoxy C1-C6 alkyl, C1-C6 alkanoyl, amino, halo, carboxy, cyano, azido, mercapto, nitro, C0-C3-alkylaryl, C0-C3-alkylhet, C0-C3-alkylcycloalkyl; R is H C1-C3 alkyl or cyclises with the nominal N-terminal to form a macrocycle; with the proviso that if R4 is =O, then the alkyl moiety of R5 as alkylaryl or alkylhet is C1-C3 alkanyl or C2-C3 alkenyl; have utility as HCV NS-3 serine protease inhibitors.
摘要翻译：具有式（I）或（II）的新型P1氨基酸替代物的化合物，其中R 1是针对HCV NS-3丝氨酸蛋白酶的S2-Sn袋的肽或拟肽识别序列P2-Pn，其中n为3 -6，其识别序列是肽键合到式（I）上; R 2是H，C 1 -C 3烷基; R 3是任选被1-3个卤素原子或-SH取代的C 1 -C 3烷基; R 4是= O，卤素，氨基或-OH; R 5是C 1 -C 6烷基，C 0 -C 3烷基芳基，C 0 -C 3烷基，C 0 -C 3烷基环C 3 -C 6烷基，其中任何一个可以任选地被羟基，C 1 -C 6烷基，C 1 -C 6 烷氧基，C1-C6卤代烷基，C1-C6烷氧基C1-C6烷基，C1-C6烷酰基，氨基，卤素，羧基，氰基，叠氮基，巯基，硝基，C0-C3-烷基芳基，C0-C3-烷基，C0-C3 烷基环烷基; R 6为H-C 1 -C 3烷基，或以标称N末端环化形成大环; 条件是如果R4为= O，则R5为烷基芳基或烷基的烷基部分为C1-C3烷基或C2-C3烯基; 具有HCV NS-3丝氨酸蛋白酶抑制剂的功效。

10. 发明申请

WO2010034790A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2010034790A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/062408
申请日：2009-09-24
申请人： MEDIVIR AB , ODÉN, Lourdes, Salvadore , JOHANSSON, Per-Olof , KAHNBERG, Pia , NILSSON, Magnus , SAMUELSSON, Bertil , GRABOWSKA, Urszula
发明人： ODÉN, Lourdes, Salvadore , JOHANSSON, Per-Olof , KAHNBERG, Pia , NILSSON, Magnus , SAMUELSSON, Bertil , GRABOWSKA, Urszula
IPC分类号： C07D491/048 , A61K31/496 , A61P19/00
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R 1 forms an ethynyl bond and R 2 is H or C 3 -C 6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF 3 , OMe or halo; R 3 is C 1 -C 3 alkyl or C 3 -C 6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R 3 is C 3 -C 6 cycloalkyl it may alternatively be gem subsituted with fluoro; R 4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, A 1 is CH or N, A 2 is CR 6 R 7 or NR 6 , provided at least one of A 1 and A 2 comprises N; n is 0 or 1 such that the ring containing A 1 and A 2 is a saturated, nitrogen-containing ring of 5 or 6 ring atoms; R 6 is H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 3 alkyl-O-C 1 -C 3 alkyl, or when A 2 is C, R 6 can also be C 1 -C 4 alkoxy or F; R 7 is H, C 1 -C 4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R1形成乙炔基，R2是H或任选被一个或两个独立地选自甲基，CF 3，OMe或卤素的取代基取代的C 3 -C 6环烷基; R 3是C 1 -C 3烷基或C 3 -C 6环烷基，当R 3是C 3 -C 6环烷基时，它们任选被一个或两个甲基和/或氟，三氟甲基或甲氧基取代，也可以被氟取代; R4是甲基或氟; m为0,1或2; E是键，A1是CH或N，A2是CR6R7或NR6，条件是A1和A2中的至少一个包括N; n为0或1，使得含有A 1和A 2的环是5或6个环原子的饱和的含氮环; R6是H，C1-C4烷基，C1-C4卤代烷基，C1-C3烷基-O-C1-C3烷基，或当A2是C时，R6也可以是C1-C4烷氧基或F; R7是H，C1-C4烷基或F或其药学上可接受的盐，N-氧化物或其水合物，可用于治疗组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨骼转移。

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