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1. 发明申请

WO2007006714A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2007006714A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063950
申请日：2006-07-06
申请人： MEDIVIR AB , KANGASMETSA, Jussi , HISCOCK, Stephen , JOHNSON, Tony , SAMUELSSON, Bertil , TOZER, Matt , GRABOWSKA, Urszula
发明人： KANGASMETSA, Jussi , HISCOCK, Stephen , JOHNSON, Tony , SAMUELSSON, Bertil , TOZER, Matt , GRABOWSKA, Urszula
IPC分类号： C07D487/04 , A61K31/407 , A61P19/10
CPC分类号： C07D487/04
摘要： Compounds of the formula II wherein R 1 and R 1, are halo; or one of R 1 and R 1, is halo, and the other is is H; R 2 is R 4 , -C(=O)R 4 ; -OC(=O)R 4 , -S(=O) n R 4 , -S(=O)nNRdRe; R 3 is H, -OR 4 , -SR 4 ; R 3' is H; or R 3 and R 3' together define =O; R 4 is -C 1 C 6 alkyl, -C 0 -C 3 alkylenecarbocyclyl or -C 0 -C 3 alkyleneheterocyclyl, any of which is optionally substituted with up to three substituents selected from R 7 ; R 5 is -C 1 C 5 alkyl, -CH 2 CR 5" C 3 -C 4 -cycloalkyl; R 5' is H; or R 5 and R 5' together with the carbon to which they are attached define C 4 -C 6 -cycloalkyl; R 5" is H, C 1 C 2 alkyl, C 1 C 2 haloalkyl, hydroxyl, OC 1 C 2 alkyl, fluoro; E is -C(=O)-, -S(=O) m -, -NRaS(=O) m -, -NRaC(=O)-, -OC(=O)-, -CRbRc-; R 6 is a stable, optionally substituted, monocyclic or bicyclic carbocycle or heterocycle, wherein the, or each, ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepisn K, such as osteoporosis, osteoarthritis, rhuematoid arthritis or bone metastases.
摘要翻译：其中R 1和R 2的式II化合物是卤素; 或R 1和R 2中的一个为卤素，另一个为H; R 2是R 4，-C（= O）R 4; -OC（= O）R 4，-S（= O）n R 4，-S（= O）n NR d Re; R 3是H，-OR 4，-SR 4; R 3'是H; 或R 3和R 3'一起定义= O; R 4是-C 1 -C 6烷基，-C 0 -C 3 -C 3 亚烷基环丙基或-C 0 -C 3亚烷基杂环基，其中任何一个任选被至多三个选自R 7的取代基取代; R 5是-C 1 -C 5烷基，-CH 2 CH 2，5“ > C 3 -C 4 - 环烷基; R 5'是H;或R 5和R SUP > 5'与它们所连接的碳一起定义为C 4 -C 6 - 环烷基; R 5“是 H，C 1 -C 2烷基，C 1 -C 2卤代烷基，羟基，OC 1，氟; C 1 -C 6烷基，氟; E是-C（= O） - ， - S（= O）m - ， - NR a（= O）m - ， - NR a C（= O） - ， -OC（= O） - ， - CR b R c-; R 6是稳定的，任选取代的单环或双环碳环或杂环，其中环或每个环具有4,5或6个环原子和0至3个选自S，O的杂原子和 N; 可用于治疗特征为导管骨K不适当表达或活化的疾病，如骨质疏松症，骨关节炎，类型性关节炎或骨转移。

2. 发明申请

WO2008114054A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2008114054A1
公开(公告)日：2008-09-25
申请号：PCT/GB2008/050193
申请日：2008-03-18
申请人： MEDIVIR AB , KANGASMETSA, Jussi , PARKES, Kevin , TOZER, Matt , JOHNSON, Tony , GRABOWSKA, Urszula , ODEN, Lourdes , SUND, Christian , NILSSON, Magnus , IVANOV, Vladimir , KAHNBERG, Pia
发明人： KANGASMETSA, Jussi , PARKES, Kevin , TOZER, Matt , JOHNSON, Tony , GRABOWSKA, Urszula , ODEN, Lourdes , SUND, Christian , NILSSON, Magnus , IVANOV, Vladimir , KAHNBERG, Pia
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
CPC分类号： C07D491/04
摘要： Compounds of the formula (II): wherein R 2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R 3 is H, methyl or fluoro; R 4 is C 1 -C 6 alkyl; E is a bond or thiazolyl, optionally substituted with methyl or fluoro; n is 0 or 1; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsinK, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式（II）的化合物：其中R 2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟代亮氨酸或3-甲氧基缬氨酸; R 3是H，甲基或氟; R 4是C 1 -C 6烷基; R 4是C 1 -C 6烷基; E是任选被甲基或氟取代的键或噻唑基; n为0或1; 或其药学上可接受的盐，N-氧化物或其水合物; 可用于治疗特征为组织蛋白酶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。

3. 发明申请

WO2005066180A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2005066180A1
公开(公告)日：2005-07-21
申请号：PCT/GB2005/050003
申请日：2005-01-06
申请人： MEDIVIR AB , NILSSON, Magnus , ZHOU, Xiao-Xiong , ODEN, Lourdes , CLASSON, Bjorn , NOREN, Rolf , GRABOWSKA, Urszula , JACKSON, Philip , FALLON, Philip , CARR, Andrew , LILEY, Mark , TOZER, Matt , JOHNSON, Tony , DIAZ, Victor , CRESPO, Laia , KANGASMETSA, Jussi , BONNAUD, Thierry
发明人： NILSSON, Magnus , ZHOU, Xiao-Xiong , ODEN, Lourdes , CLASSON, Bjorn , NOREN, Rolf , GRABOWSKA, Urszula , JACKSON, Philip , FALLON, Philip , CARR, Andrew , LILEY, Mark , TOZER, Matt , JOHNSON, Tony , DIAZ, Victor , CRESPO, Laia , KANGASMETSA, Jussi , BONNAUD, Thierry
IPC分类号： A61K31/407 , C07D491/04
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula (II) wherein one of R 1 and R 2 is halo and the other is H or halo; R 3 is C 1 -C 4 straight or branched chain, optionally fluorinated, alkyl; R 4 is H; or R 3 together with R 4 and the adjoining backbone carbon defines: a spiro-C 5 -C 7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl; or optionally bridged with a methylene group; or a C 4 -C 6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(=O) 2 ; where Ra is H, C 1 -C 4 alkyl or CH 3 C(=O); R 5 is independently selected from H or methyl; E is -C(=O)-, -S(=O) m -, -NR 5 S(=O) m -, -NR 5 C(=O)-, -OC(=O)-, R 6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：其中R 1和R 2之一为卤素且另一个为H或卤素的式（II）化合物; R 3是C 1 -C 4直链或支链，任选氟化的烷基; R 4是H; 或R 3与R 4一起，相邻的主链碳定义：任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O，NR a，S，S（= O）2的杂原子的C 4 -C 6饱和杂环; 其中R a是H，C 1 -C 4烷基或CH 3 C（= O）; R 5独立地选自H或甲基; E是-C（= O） - ， - S（= O）m - ， - NR 5 S（= O）m - ， - NR 5 C（= O） - ， - OC（= O） - ，R 6是稳定的，任选取代的单环或双环碳环或hetorocycle; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

4. 发明申请

WO2008049832A1 FURANONE DERIVATIVES AS CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译：呋喃酮衍生物作为CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2008049832A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061335
申请日：2007-10-23
申请人： MEDIVIR AB , LILEY, Mark , JOHNSON, Tony , TOZER, Matt , GRABOWSKA, Urszula
发明人： LILEY, Mark , JOHNSON, Tony , TOZER, Matt , GRABOWSKA, Urszula
IPC分类号： C07D417/12 , A61K31/495 , A61P35/00 , A61P19/00 , C07K5/06
CPC分类号： C07D417/12
摘要： Compounds of the Formula (Il) wherein R 1 is H, OH, F R 2 is -CH 2 CH(CH 3 ) 2 , -CH 2 C(CH 3 ) 3 or -CH(CH 3 )(CH 2 CH 3 ); R 2' is H; or R 2 and R 2' together with the adjacent C atom defines cyclohexyl; and pharmaceutically acceptable salts, hydrates and N-oxides thereof have utility in the treatment of disorders characterised by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：其中R 1是H，OH，FR 2的式（II）化合物是-CH 2 CH（CH 3）（CH 3）3或-CH（CH 3 ）（CH _{2 CH _{3 ）; R 2是H; 或R 2和R 2'与相邻的C原子一起定义为环己基; 其药学上可接受的盐，水合物和N-氧化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。}}

5. 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）。

6. 发明申请

WO2012044673A1 POWER MONITORING DEVICE SIMULATION USING A DATABASE PROFILE GENERATED FROM REAL TIME-VALUE DATA 审中-公开
标题翻译：使用实时数据生成的数据库配置文件进行电力监控设备的仿真
公开(公告)号：WO2012044673A1
公开(公告)日：2012-04-05
申请号：PCT/US2011/053659
申请日：2011-09-28
申请人： SCHNEIDER ELECTRIC USA, INC. , LLOYD, Chad, Andrew , JOHNSON, Tony , MCQUILLAN, Jayme
发明人： LLOYD, Chad, Andrew , JOHNSON, Tony , MCQUILLAN, Jayme
IPC分类号： G05B23/02
CPC分类号： G05B23/0213
摘要： A system and methods for using data from an external database compiled from real device used for testing and simulation of a system. The system includes an external database interface to access an external database. The external database includes a plurality of categories of time-value data collected from an electrical device. An importer converts one of plurality of categories of time-value data to a corresponding topic of a common data format. A device profiler is coupled to the importer to create a device profile including the converted topic. A database profiler creates a database profile representing a system including a device defined by the device profile and including the category of time-value data.
摘要翻译：用于从用于测试和模拟系统的实际设备编译的外部数据库中使用数据的系统和方法。该系统包括一个用于访问外部数据库的外部数据库接口。外部数据库包括从电气设备收集的多个类别的时间值数据。导入器将多个类别的时间值数据中的一个转换为公共数据格式的相应主题。设备分析器耦合到导入器以创建包括转换的主题的设备简档。数据库分析器创建表示包括由设备配置文件定义并且包括时间值数据类别的设备的系统的数据库配置文件。

7. 发明申请

WO2011086053A1 TRICYCLIC HETEROCYCLIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：三元杂环化合物，组合物及其使用方法
公开(公告)号：WO2011086053A1
公开(公告)日：2011-07-21
申请号：PCT/EP2011/050239
申请日：2011-01-11
申请人： F. HOFFMANN-LA ROCHE AG , BABU, Srinivasan , BERGERON, Phillippe , DRAGOVICH, Peter , DYKE, Hazel Joan , GIBBONS, Paul , GRADL, Stefan , HANAN, Emily , HURLEY, Christopher , JOHNSON, Tony , KOEHLER, Michael , KULAGOWSKI, Janusz Josef , LABADIE, Sharada Shenvi , LYSSIKATOS, Joseph P. , MENDONCA, Rohan , PULK, Rebecca , WARD, Stuard , WASZKOWYCZ, Bohdan , ZAK, Mark
发明人： BABU, Srinivasan , BERGERON, Phillippe , DRAGOVICH, Peter , DYKE, Hazel Joan , GIBBONS, Paul , GRADL, Stefan , HANAN, Emily , HURLEY, Christopher , JOHNSON, Tony , KOEHLER, Michael , KULAGOWSKI, Janusz Josef , LABADIE, Sharada Shenvi , LYSSIKATOS, Joseph P. , MENDONCA, Rohan , PULK, Rebecca , WARD, Stuard , WASZKOWYCZ, Bohdan , ZAK, Mark
IPC分类号： C07D471/14 , C07D487/10 , A61K31/437 , A61P11/06 , A61P17/06 , A61P19/02 , A61P37/00 , A61P37/06
CPC分类号： C07D471/14 , C07D487/10
摘要： The invention provides novel compounds of formula (I) having the general formula, wherein R 1 , R 2 , R 3 , X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要翻译：本发明提供具有以下通式的新的式（I）化合物：其中R 1，R 2，R 3，X和Y如本文所述。因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

8. 发明申请

WO2012027702A1 PYRIDYL-AMINE FUSED AZADECALIN MODULATORS 审中-公开
标题翻译：吡啶胺混合阿扎他林调节剂
公开(公告)号：WO2012027702A1
公开(公告)日：2012-03-01
申请号：PCT/US2011/049408
申请日：2011-08-26
申请人： CORCEPT THERAPEUTICS, INC. , CLARK, Robin , JOHNSON, Tony , HUNT, Hazel , MCDONALD, Ian
发明人： CLARK, Robin , JOHNSON, Tony , HUNT, Hazel , MCDONALD, Ian
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
摘要翻译：本发明提供了一类新颖的吡啶基 - 胺稠合的十九烷基化合物和使用该化合物作为糖皮质激素受体调节剂的方法。

9. 发明申请

WO2007063330A3 BAG 审中-公开
公开(公告)号：WO2007063330A3
公开(公告)日：2007-06-07
申请号：PCT/GB2006/004506
申请日：2006-12-04
申请人： TRI-BAG LIMITED , SMITH, Wendy , MYERS, Chris , JOHNSON, Tony , PROBEREZNY, Ken
发明人： MYERS, Chris , JOHNSON, Tony , PROBEREZNY, Ken
IPC分类号： A45C5/14 , A63B55/08
摘要： Apparatus (1) comprising a bag (22) having a base (6) adapted to receive a ground rolling device (100), said ground rolling device (100) being detachably connectable to the base (6) and comprising an axle (16) provided with a wheel (17a, 17b) at or adjacent each end such that when the ground rolling device (100) is connected to the base (6) the wheels (17a, 17b) project laterally from either side of the base (6).

10. 发明公开

EP1966153A1 (2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：（2,5-二氧代咪唑烷-1-基）-N- hydroxyacetamides ALS金属蛋白酶
公开(公告)号：EP1966153A1
公开(公告)日：2008-09-10
申请号：EP06840975.4
申请日：2006-12-13
申请人： Medivir AB
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).

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