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1. 发明申请

WO2006081664A1 ALTERNATIVE UPLOCK RELEASE ASSEMBLY 审中-公开
标题翻译：替代性UPLOCK RELEASE ASSEMBLY
公开(公告)号：WO2006081664A1
公开(公告)日：2006-08-10
申请号：PCT/CA2006/000139
申请日：2006-02-03
申请人： HÉROUX-DEVTEK INC. , GAGNON, Marc-Olivier , PELLETIER, Marc-André , THERRIEN, Eric
发明人： GAGNON, Marc-Olivier , PELLETIER, Marc-André , THERRIEN, Eric
IPC分类号： B64C25/26 , E05B57/00 , E05B17/20 , E05B15/12
CPC分类号： B64C1/1407 , B64C25/16 , B64C25/26 , E05B51/02
摘要： A new alternative uplock release assembly is provided. The assembly comprises a pivot pin having a first end and a second end and an internal bore, a release system operatively connected to the first end of the pivot pin, said release system comprising a cylinder and a piston, said piston having a piston head and an elongated member passing longitudinally through said bore, said cylinder having a pressure port through which a pressure source can be fed. The assembly further comprises a hooking member, a torque member rotatably mounted at the second end of the pivot pin, a biasing system operatively connected to the torque member, said biasing system having a bias cylinder and a biasing means located within the bias cylinder. When biasing force is applied to the torque member, an interlocking means to enable the rotatable interconnection between the torque member and the hooking member in a locked and first position, and an engaging means to interconnect the torque member with a link member. When torque is applied to the link member, the torque is transferred, via the engaging means and interlocking means, to the hooking member forcing the hooking member to rotate around the pivot pin. During alternative operation, pressure is fed through the pressure port, the piston counteracts the biasing force, thereby translating the torque member longitudinally over the pivot pin sufficiently to decouple the torque member and the hooking member from the said locked and first position, to an unlocked and second position enabling the hooking member to rotate around the pivot pin.
摘要翻译：提供了一种新的可选择的上锁释放组件。组件包括具有第一端和第二端以及内孔的枢轴销，可操作地连接到枢转销的第一端的释放系统，所述释放系统包括气缸和活塞，所述活塞具有活塞头和细长构件纵向通过所述孔，所述圆筒具有压力端口，压力源可以通过该压力端口供给。所述组件还包括钩构件，可转动地安装在所述枢转销的第二端处的扭矩构件，与所述扭矩构件可操作地连接的偏置系统，所述偏置系统具有偏置气缸和位于偏置气缸内的偏置装置。当向扭矩构件施加偏置力时，能够在扭转构件和钩挂构件之间在锁定和第一位置中的可旋转互连的互锁装置以及将扭矩构件与连杆构件互连的接合装置。当扭矩施加到连杆构件时，扭矩通过接合装置和互锁装置传递到使挂钩构件围绕枢转销旋转的钩构件。在替代操作期间，压力通过压力端口进入，活塞抵消偏压力，从而使扭矩构件在枢轴销上纵向平移，足以将扭矩构件和钩挂构件从所述锁定和第一位置解耦到解锁以及第二位置，使得所述钩构件能够围绕所述枢转销旋转。

2. 发明申请

WO2008104077A1 SMALL MOLECULE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASES (PRMTS) 审中-公开
标题翻译：蛋白质亚甲基转移酶的小分子抑制剂（PRMTS）
公开(公告)号：WO2008104077A1
公开(公告)日：2008-09-04
申请号：PCT/CA2008/000384
申请日：2008-02-28
申请人： METHYLGENE INC. , WAHHAB, Amal , THERRIEN, Eric , ALLAN, Martin , MANKU, Sukhdev
发明人： WAHHAB, Amal , THERRIEN, Eric , ALLAN, Martin , MANKU, Sukhdev
IPC分类号： C07D231/14 , A61K31/415 , A61K31/435 , A61P31/00 , A61P35/00 , A61P37/00 , C07D211/26 , C07D231/22 , C07D235/18 , C07D401/00 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
CPC分类号： C07D409/04 , C07D211/26 , C07D231/14 , C07D231/22 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.
摘要翻译：本发明涉及可用作具有选自式（I），式（II）和式（III）的式的蛋白质精氨酸甲基转移酶的抑制剂的化合物，以及外消旋混合物，非对映异构体，对映异构体和互变异构体以及N 氧化物，水合物，溶剂化物，药学上可接受的盐，前药和复合物。所述化合物可用作PRMT和/或CARM-1的抑制剂。本发明还涉及包含这些化合物的组合物及其使用方法。

3. 发明申请

WO2006102760A1 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2006102760A1
公开(公告)日：2006-10-05
申请号：PCT/CA2006/000483
申请日：2006-03-31
申请人： METHYLGENE INC. , LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DÉZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
发明人： LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DÉZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
IPC分类号： C07D417/04 , A61K31/18 , A61K31/166 , A61K31/195 , A61K31/34 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/505 , C07C237/38 , C07C311/21 , C07C323/33 , C07C323/60 , C07D207/16 , C07D209/30 , C07D209/42 , C07D211/22 , C07D215/38 , C07D217/12 , C07D235/04 , C07D239/08 , C07D241/40 , C07D277/82 , C07D285/12 , C07D317/46 , C07D319/14 , C07D333/32 , C07D403/06 , C07D409/06 , C07D413/04
CPC分类号： C07D209/14 , C07C237/22 , C07C309/51 , C07C311/13 , C07C311/29 , C07C311/46 , C07C311/51 , C07C311/59 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/60 , C07C2601/14 , C07C2603/32 , C07D209/42 , C07D209/46 , C07D213/30 , C07D213/32 , C07D213/40 , C07D213/70 , C07D213/89 , C07D215/40 , C07D235/14 , C07D239/38 , C07D241/52 , C07D277/82 , C07D285/12 , C07D285/135 , C07D295/185 , C07D307/42 , C07D307/81 , C07D317/58 , C07D333/16 , C07D333/24 , C07D333/34 , C07D401/06 , C07D405/12 , C07D409/06 , C07D409/12
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I); wherein Y, L, Z, W, X, Q, R 1 , R 2 and R 3 are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地，本发明提供式（I）的化合物; 其中Y，L，Z，W，X，Q，R 1，R 2和R 3均如说明书中所定义。

4. 发明申请

WO2007143822A1 SULFAMIDE AND SULFAMATE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：磺酰胺和磺酰胺衍生物作为脱乙酰壳多糖酶抑制剂
公开(公告)号：WO2007143822A1
公开(公告)日：2007-12-21
申请号：PCT/CA2007/001024
申请日：2007-06-14
申请人： METHYLGENE INC. , SMIL, David , LEIT, Silvana , AJAMIAN, Alain , ALLAN, Martin , CHANTIGNY, Yves, André , DEZIEL, Robert , THERRIEN, Eric , WAHHAB, Amal , MANKU, Sukhdev
发明人： SMIL, David , LEIT, Silvana , AJAMIAN, Alain , ALLAN, Martin , CHANTIGNY, Yves, André , DEZIEL, Robert , THERRIEN, Eric , WAHHAB, Amal , MANKU, Sukhdev
IPC分类号： C07D277/46 , A61K31/185 , A61K31/417 , A61K31/4184 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/47 , A61K31/4709 , C07D215/40 , C07D233/64 , C07D235/14 , C07D271/06 , C07D277/28 , C07D307/06 , C07D401/12 , C07D417/02
CPC分类号： C07D215/38 , C07C307/06 , C07C2603/32 , C07C2603/74 , C07D209/14 , C07D215/42 , C07D215/48 , C07D223/26 , C07D233/61 , C07D235/14 , C07D249/08 , C07D261/14 , C07D263/56 , C07D263/60 , C07D271/06 , C07D271/10 , C07D273/01 , C07D277/46 , C07D277/56 , C07D277/82 , C07D285/12 , C07D307/85 , C07D401/12 , C07D405/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I), and racemic and scalemic mixtures, diastereomers and enantiomers thereof: (I) or an N-oxide, hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof, wherein Y, L, Z, W, M, R a , R b and R c are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地说，本发明提供式（I）化合物及其外消旋和可饱和的混合物，非对映异构体和对映体：（I）或其N-氧化物，水合物，溶剂合物，药学上可接受的盐，前药或复合物，其中Y， L，Z，W，M，R a，R b和R c如本说明书中所定义。

5. 发明申请

WO2005058826A8 NEW 5,6-DIHYDROPYRIN-2-ONE COMPOUNDS USEFUL AS INHIBITORS OF THROMBIN 审中-公开
标题翻译：新的5,6-DIHYDROPYRIN-2-ONE化合物作为硫蛋白抑制剂有用
公开(公告)号：WO2005058826A8
公开(公告)日：2005-10-27
申请号：PCT/SE2004001878
申请日：2004-12-15
申请人： ASTRAZENECA AB , BERGGREN KRISTINA , DAVIDSSON OEJVIND , FJELLSTROEM OLA , GUSTAFSSON DAVID , HANESSIAN STEPHEN , INGHARDT TORD , NAAGAARD MATS , NILSSON INGEMAR , THERRIEN ERIC , VAN OTTERLO WILLEM
发明人： BERGGREN KRISTINA , DAVIDSSON OEJVIND , FJELLSTROEM OLA , GUSTAFSSON DAVID , HANESSIAN STEPHEN , INGHARDT TORD , NAAGAARD MATS , NILSSON INGEMAR , THERRIEN ERIC , VAN OTTERLO WILLEM
IPC分类号： C07D211/98 , A61K31/4412 , A61P7/02
CPC分类号： C07D211/98
摘要： There is provided a compound of formula (I) wherein R , R , R , R , R , R , R , R , A, G and L have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competetive inhibitors of trypsin-like proteases, such as trombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e,g. conditions, such as thrombo-embolisms, where inhibition of trombin is required or desired, and/or conditions wherea anticoagulant thererapy is indicated).
摘要翻译：提供式（I）化合物，其中R 1，R 2a，R 2b，R 3a，R 3b，R 4，R 5，R 6， A，G和L具有说明书中给出的含义，哪些化合物可用作胰蛋白酶样蛋白酶如凝血酶的竞争抑制剂的前体药物，因此特别是在治疗其中凝血酶的抑制是有益的（例如，需要或期望抑制凝血酶的条件，例如血栓栓塞，和/或表示抗凝血剂的条件）。

6. 发明申请

WO2005075424A1 NEW PYRIDIN-2-ONE COMPOUNDS USEFUL AS INHIBITORS OF THROMBIN 审中-公开
标题翻译：新的吡啶-2-酮化合物作为硫蛋白抑制剂有用
公开(公告)号：WO2005075424A1
公开(公告)日：2005-08-18
申请号：PCT/SE2005/000124
申请日：2005-02-02
申请人： ASTRAZENECA AB , BAYRAKDARIAN, Malken , BERGGREN, Kristina , DAVIDSSON, Öjvind , FJELLSTRÖM, Ola , GUSTAFSSON, David , HANESSIAN, Stephen , INGHARDT, Tord , NILSSON, Ingemar , NÅGÅRD, Mats , SIMARD, Daniel , THERRIEN, Eric
发明人： BAYRAKDARIAN, Malken , BERGGREN, Kristina , DAVIDSSON, Öjvind , FJELLSTRÖM, Ola , GUSTAFSSON, David , HANESSIAN, Stephen , INGHARDT, Tord , NILSSON, Ingemar , NÅGÅRD, Mats , SIMARD, Daniel , THERRIEN, Eric
IPC分类号： C07D211/86
CPC分类号： C07D413/12 , C07D211/98 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： There is provided a compound of formula I, wherein the dashed line, R 1 , R 2 , R 3a , R 3b , A, D, E, G and L have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).
摘要翻译：提供了式I化合物，其中虚线R 1，R 2，R 3a，R 3b，A，D，E，G和L具有说明书中给出的含义，哪些化合物可用作或用作胰蛋白酶样蛋白酶的竞争性抑制剂如凝血酶的前药，因此特别是用于治疗凝血酶抑制是有益的条件（例如，血栓 - 栓塞，其中需要或期望抑制凝血酶，和/或表示抗凝治疗的条件）。

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