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1. 发明授权

US08859505B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US08859505B2
公开(公告)日：2014-10-14
申请号：US13704441
申请日：2011-06-16
申请人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
发明人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
IPC分类号： C07K14/81 , C07D233/60 , C07K5/065 , C07C271/22 , C07D277/56 , A61K38/55 , C07D305/08 , C07K5/062 , C07C275/18 , C07K5/078 , C07C237/22 , C07D213/81
CPC分类号： C07D233/61 , A61K38/55 , C07C231/12 , C07C235/80 , C07C237/22 , C07C271/22 , C07C275/18 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D233/60 , C07D277/56 , C07D305/08 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139
摘要： Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译：其中R 2a和R 2b独立地是H，卤素，C 1 -C 4烷基，C 1 -C 4卤代烷基或C 1 -C 4烷氧基或R 2a和R 2b与它们所连接的碳原子一起形成C 3 -C 6环烷基的式I化合物; R3是任选地被1-3个独立地选自卤素，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基的取代基取代的C 5 -C 10烷基; 或R3是具有至少2个氯或3个氟取代基的C 2 -C 4烷基链; 或R3是C3-C7环烷基甲基，任选地被1-3个独立地选自C 1 -C 4烷基，卤素，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基的取代基取代; R 4是C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，C 1 -C 6烷基氨基，C 1 -C 6二烷基氨基或 R 4是Het或碳环基，其任一个任选被1-3个取代基取代，R 4是Het，碳环基，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基或C 1 -C 6卤代烷氧基; n为1,2或3; 用于预防或治疗以组织蛋白酶S的不适当表达或活化为特征的病症。

2. 发明申请

US20130172232A1 CYSTEINE PROTEASE INHIBITORS 有权
公开(公告)号：US20130172232A1
公开(公告)日：2013-07-04
申请号：US13704441
申请日：2011-06-16
申请人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
发明人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
IPC分类号： C07K5/078 , C07K5/062 , C07K5/065
CPC分类号： C07D233/61 , A61K38/55 , C07C231/12 , C07C235/80 , C07C237/22 , C07C271/22 , C07C275/18 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D233/60 , C07D277/56 , C07D305/08 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139
摘要： Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

3. 发明授权

US08859605B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US08859605B2
公开(公告)日：2014-10-14
申请号：US13514760
申请日：2010-12-10
申请人： Susana Ayesa , Peter Carlqvist , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Pia Kahnberg , Bjorn Klasson , Peter Lind , Lourdes Oden , Kevin Parkes , Daniel Wiktelius
发明人： Susana Ayesa , Peter Carlqvist , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Pia Kahnberg , Bjorn Klasson , Peter Lind , Lourdes Oden , Kevin Parkes , Daniel Wiktelius
IPC分类号： C07C271/22 , C07D405/12 , C07D231/40 , 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 R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; 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化合物，其中R1a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. 发明授权

US07697493B2 Automatic service activation 有权
标题翻译：自动服务激活
公开(公告)号：US07697493B2
公开(公告)日：2010-04-13
申请号：US11162162
申请日：2005-08-31
申请人： Richard Ljungberg , Daniel Jonsson , Jonas Lundgren
发明人： Richard Ljungberg , Daniel Jonsson , Jonas Lundgren
IPC分类号： H04W4/00
CPC分类号： G01S5/0072
摘要： Wireless communication systems wherein services involving two or more stations in the system may be activated automatically. Data is communicated between airborne stations according to a TDMA protocol, where the data is transmitted in time slots organized in frames of a repeating frame structure. A link address is associated with at least one time slot. The stations select link addresses for transmission of data according to a self-organizing transmission algorithm. Each station broadcasts data messages of a first type at a first repetition rate and receives such corresponding messages from the other stations. At least based on the received data messages of the first type, each station determines whether a service activation criterion is fulfilled with respect to at least one other station. If the service activation criterion is fulfilled, the station starts to transmit data messages of a second type, which pertain to a service that involves the station itself and the at least one other station.
摘要翻译：可以自动激活涉及系统中两个或多个站的业务的无线通信系统。根据TDMA协议，在机载站之间传送数据，其中数据以组织在重复帧结构的帧中的时隙发送。链接地址与至少一个时隙相关联。站点根据自组织传输算法选择数据传输的链路地址。每个站以第一重复率广播第一类型的数据消息，并从其他站接收这样的相应消息。至少基于所接收到的第一类型的数据消息，每个站确定是否满足至少一个其他站的服务激活标准。如果满足服务激活标准，则站开始发送第二类型的数据消息，这涉及涉及站本身的服务和至少一个其他站。

5. 发明申请

US20060045058A1 Automatic Service Activation 有权
标题翻译：自动服务激活
公开(公告)号：US20060045058A1
公开(公告)日：2006-03-02
申请号：US11162162
申请日：2005-08-31
申请人： Richard Ljungberg , Daniel Jonsson , Jonas Lundgren
发明人： Richard Ljungberg , Daniel Jonsson , Jonas Lundgren
IPC分类号： H04Q7/24
CPC分类号： G01S5/0072
摘要： The invention relates to wireless communication systems wherein services involving two or more stations in the system may be activated automatically. Data is communicated between airborne stations (A, B) according to a TDMA protocol, where the data is transmitted in time slots organized in frames of a repeating frame structure. A link address is associated with at least one time slot, and the stations select link addresses for transmission of data according to a self-organizing transmission algorithm. Each station (A, B) broadcasts data messages of a first type (D1) at a first repetition rate and receives such corresponding messages from the other stations (A, B). At least based on the received data messages of the first type (D1), each station determines whether a service activation criterion is fulfilled with respect to at least one other station (A, B), for example by the other station being located within a limit distance (rA). If the service activation criterion is fulfilled, the station (A, B) starts to transmit data messages of a second type (D2), which pertain to a service that involves the station itself and the at least one other station (A, B).
摘要翻译：本发明涉及无线通信系统，其中系统中涉及两个或多个站的业务可以被自动激活。根据TDMA协议在空中站（A，B）之间传送数据，其中数据以重复帧结构的帧组织的时隙发送。链路地址与至少一个时隙相关联，并且站点根据自组织传输算法选择用于传输数据的链路地址。每个站（A，B）以第一重复率广播第一类型的数据消息（D SUB 1），并从其他站（A，B）接收这样的相应消息。至少基于接收到的第一类型的数据消息（D 1> 1），每个站确定是否满足关于至少一个其他站（A，B）的服务激活标准由另一站位于限制距离（r A A）之内。如果满足服务激活标准，则站（A，B）开始发送第二类型的数据消息（D＆lt; 2＆gt;），其涉及涉及站本身的服务，并且至少另一站（A，B）。

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