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1. 发明申请

WO2007006716A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2007006716A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063952
申请日：2006-07-06
申请人： MEDIVIR AB , TICKLE, David , PARKES, Kevin , TOZER, Matt , GRABOWSKA, Urszula
发明人： TICKLE, David , PARKES, Kevin , TOZER, Matt , GRABOWSKA, Urszula
IPC分类号： C07D471/04 , A61K31/407 , A61P19/00
CPC分类号： C07D471/04
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 5 straight or branched chain, optionally fluorinated, alkyl or -CH 2 CR 5 C 3 -C 4 -Cycloalkyl; R 4 is H; R 5 is H, C 1 -C 2 alkyl, C 1 -C 2 haloalkyl, hydroxyl, OC 1 -C 2 alkyl, fluoro; R 6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle wherein the or each ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; Rb is haloalkyl; Rc is H or C 1 -C 4 alkyl; and pharmaceutically acceptable salts, hydrates or 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和R 2中的一个为卤素且另一个为H或卤素的式（II）化合物; R 3是C 1 -C 5直链或支链，任选氟化的烷基或-CH 2 O 2， CR ^{5 C _{3 -C _{4 - 环烷基; R 4是H; R 5是H，C 1 -C 2烷基，C 1 -C 2烷基，C 1 -C 2烷基，C 1 -C 2烷基，卤代烷基，羟基，OC 1 -C 2烷基，氟; R 6是一个稳定的，任选取代的单环或双环的碳环或hetorocycle，其中该环或每个环具有4,5或6个环原子和0至3个选自S，O和N的杂原子; Rb是卤代烷基; R c是H或C 1 -C 4烷基; 其药学上可接受的盐，水合物或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。}}}

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

WO2011070541A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2011070541A1
公开(公告)日：2011-06-16
申请号：PCT/IB2010/055738
申请日：2010-12-10
申请人： MEDIVIR UK LIMITED , AYESA, Susana , CARLQUIST, Peter , ERSMARK, Karolina , GRABOWSKA, Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KAHNBERG, Pia , KLASSON, Björn , LIND, Peter , ODÉN, Lourdes , PARKES, Kevin , WIKTELIUS, Daniel
发明人： AYESA, Susana , CARLQUIST, Peter , ERSMARK, Karolina , GRABOWSKA, Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KAHNBERG, Pia , KLASSON, Björn , LIND, Peter , ODÉN, Lourdes , PARKES, Kevin , WIKTELIUS, Daniel
IPC分类号： C07D231/40 , A61K31/16 , A61K31/415 , A61K31/426 , A61P9/10 , A61P11/06 , A61P17/06 , A61P21/04 , A61P37/02 , A61P37/08 , C07C237/14 , C07D277/46
CPC分类号： C07K5/06078 , A61K38/05 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D231/40 , C07D277/46 , C07D405/12 , C07K5/06034 , C07K5/0606 , C07K5/06139
摘要： Compounds of the formula (I) wherein R 1a is H; and R 1b is C 1 -C 6 alkyl, Carbocyclyl or Het; or R 1a and R 1b together define a saturated cyclic amine with 3-6 ring atoms; R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a branched C 5 -C 10 alkyl chain, C 2 -C 4 haloalkyl or -CH 2 C 3 -C 7 cycloalkyl; R 4 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkylamino or C 1 -C 6 dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译：式（I）的化合物，其中R 1a是H; 并且R 1b是C 1 -C 6烷基，碳环或Het; 或R 1a和R 1b一起限定具有3-6个环原子的饱和环胺; R2a和R2b独立地为H，卤素，C1-C4烷基，C1-C4卤代烷基或C1-C4烷氧基，或R2a和R2b与它们所连接的碳原子一起形成C 3 -C 6环烷基; R3是支链C 5 -C 10烷基链，C 2 -C 4卤代烷基或-CH 2 C 3 -C 7环烷基; R 4是C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷基氨基或C 1 -C 6二烷基氨基; 用于预防或治疗以组织蛋白酶S不适当表达或活化为特征的病症。

4. 发明申请

WO2011070539A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2011070539A1
公开(公告)日：2011-06-16
申请号：PCT/IB2010/055732
申请日：2010-12-10
申请人： MEDIVIR UK LIMITED , AYESA, Susana , ERSMARK, Karolina , GRABOWSKA, Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KAHNBERG, Pia , KLASSON, Björn , LIND, Peter , LUNDGREN, Stina , ODÉN, Lourdes , PARKES, Kevin , WIKTELIUS, Daniel
发明人： AYESA, Susana , ERSMARK, Karolina , GRABOWSKA, Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KAHNBERG, Pia , KLASSON, Björn , LIND, Peter , LUNDGREN, Stina , ODÉN, Lourdes , PARKES, Kevin , WIKTELIUS, Daniel
IPC分类号： C07D231/40 , A61K31/27 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/42 , A61K31/426 , A61P9/10 , A61P11/06 , A61P17/06 , A61P21/04 , A61P37/02 , A61P37/08 , C07C271/20 , C07D233/88 , C07D261/14 , C07D277/46 , C07D405/12
CPC分类号： C07K5/06078 , A61K38/05 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D231/40 , C07D277/46 , C07D405/12 , C07K5/06034 , C07K5/0606 , C07K5/06139
摘要： Compounds of Formula (II) wherein R 1a is H; and R 1b is C 1 -C 6 alkyl, Carbocyclyl or Het; or R 1a and R 1b together define a saturated cyclic amine with 3-6 ring atoms; R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a branched C 5 -C 10 alkyl chain, C 2 -C 4 haloalkyl or -CH 2 C 3 -C 7 cycloalkyl; R 4' is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译：式（II）的化合物，其中R 1a是H; 并且R 1b是C 1 -C 6烷基，碳环或Het; 或R1a和R1b一起限定具有3-6个环原子的饱和环胺; R2a和R2b独立地为H，卤素，C1-C4烷基，C1-C4卤代烷基或C1-C4烷氧基，或R2a和R2b与它们所连接的碳原子一起形成C 3 -C 6环烷基; R3是支链C 5 -C 10烷基链，C 2 -C 4卤代烷基或-CH 2 C 3 -C 7环烷基; R 4'是C 1 -C 6烷基，C 1 -C 6卤代烷基或氧杂环丁烷-3-基。用于预防或治疗以组织蛋白酶S不适当表达或活化为特征的病症。

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

WO2011070131A1 5-AMINO- 4-HYDROXYPENTOYL AMIDES 审中-公开
标题翻译： 5-氨基-4-羟基苯甲酸
公开(公告)号：WO2011070131A1
公开(公告)日：2011-06-16
申请号：PCT/EP2010/069328
申请日：2010-12-10
申请人： TIBOTEC PHARMACEUTICALS , MEDIVIR AB , KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
发明人： KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
IPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04 , A61K31/506 , A61P31/18
CPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04
摘要： HIV inhibitors of formula (I) wherein R 1 is halo, C 1-4 alkoxy, trifluoromethoxy; R 2 is a group of formula (A); R 3 is a group of formula (B); R 4 is a group of formula (C); n is 0 or 1; A is CH or N; R 5 and R 6 are hydrogen, C 1-4 alkyl, halo; R 7 and R 8 are C 1-4 alkyl or C 1-4 alkoxyC 1-4 alkyl; R 9 is C 1-4 alkyl, cyclopropyl, trifluoromethyl, C 1-4 alkoxy, or dimethylamino; R 10 is hydrogen, C 1-4 alkyl, cyclopropyl, trifluoromethyl, C 1-4 alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.
摘要翻译：式（I）的HIV抑制剂，其中R 1是卤素，C 1-4烷氧基，三氟甲氧基; R2是式（A）的基团; R3是式（B）的基团; R4是式（C）的基团; n为0或1; A是CH或N; R5和R6是氢，C1-4烷基，卤素; R 7和R 8是C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 9为C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; R 10是氢，C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; 其药学上可接受的加成盐和溶剂合物; 含有这些化合物作为活性成分的药物组合物和制备所述化合物的方法

7. 发明申请

WO2011076248A1 MULTI-POINT CONTACTS WITH PRESSURE DATA ON AN INTERACTIVE SURFACE 审中-公开
标题翻译：在交互式表面上的压力数据的多点联系
公开(公告)号：WO2011076248A1
公开(公告)日：2011-06-30
申请号：PCT/EP2009/067680
申请日：2009-12-21
申请人： PROMETHEAN LIMITED , PEARCE, Nigel , PARKES, Kevin , SMITH, Barry
发明人： PEARCE, Nigel , PARKES, Kevin , SMITH, Barry
IPC分类号： G06F3/048 , G06F3/041
CPC分类号： G06F3/0412 , G06F3/0416 , G06F3/04883
摘要： There is disclosed a method and apparatus for controlling a software application running on a computer system including an interactive display adapted to detect at least two contact points on the surface of the interactive display, the method comprising: detecting at least two contact points; determining pressure data associated with at least one of said contact points; and defining a condition of the software application in dependence on said detected at least two contact points and said at least one determined pressure value.
摘要翻译：公开了一种用于控制在计算机系统上运行的软件应用的方法和装置，包括适于检测交互式显示器表面上的至少两个接触点的交互式显示器，所述方法包括：检测至少两个接触点; 确定与所述接触点中的至少一个相关联的压力数据; 以及根据所述检测到的至少两个接触点和所述至少一个确定的压力值来定义所述软件应用的状况。

8. 发明申请

WO2021207343A1 MALT1 INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：WO2021207343A1
公开(公告)日：2021-10-14
申请号：PCT/US2021/026152
申请日：2021-04-07
申请人： RHEOS MEDICINES, INC. , MEDIVIR AB
发明人： CLASSON, Björn , PARKES, Kevin , BEISEL, Hans-Georg , LUNDGREN, Stina , ODÉN, Lourdes, Salvador , ERSMARK, Karolina , KARLSTRÖM, Sofia , ENGSTRÖM, Olof , DECHRISTOPHER, Brian, Addison , BARBE, Guillaume
IPC分类号： A61K31/519 , A61P29/00 , A61P35/00
摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification which are potent inhibitors of the enzyme MALT1 and are useful in the treatment of autoimmune disorders and diseases and as an immunooncology approach to the treatment of cancer, especially bladder cancer, colon cancer, hepatocellular cancer and small cell or non-small cell lung cancer.

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