公开(公告)号：US09815813B2

公开(公告)日：2017-11-14

申请号：US15110504

申请日：2015-01-16

申请人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

发明人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC分类号： A61K31/4427 ,  C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D249/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10077276B2

公开(公告)日：2018-09-18

申请号：US15110511

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

IPC分类号： C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D401/14

摘要： The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US09938295B2

公开(公告)日：2018-04-10

申请号：US15110511

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

IPC分类号： C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

摘要： The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20170015680A1

公开(公告)日：2017-01-19

申请号：US15110511

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

IPC分类号： C07D498/10 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D498/10 ,  C07B2200/07 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

摘要： The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

摘要翻译： 其中p，q，Y1，Y2，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b，R7和R8定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。

公开(公告)号：US20170001975A1

公开(公告)日：2017-01-05

申请号：US15110504

申请日：2015-01-16

申请人： Zhuoliang CHEN ,  Michael DORE ,  Jorge Garcia FORTANET ,  Rajesh KARKI ,  Mitsunori KATO ,  Matthew J. LAMARCHE ,  Lawrence Blas PEREZ ,  Sarah WILLIAMS ,  Martin SENDZIK

发明人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC分类号： C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

摘要翻译： 本发明涉及式I化合物：其中Y1，Y2，Y3，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。

公开(公告)号：US20180362496A1

公开(公告)日：2018-12-20

申请号：US16117674

申请日：2018-08-30

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D471/04 ,  C07D409/14 ,  C07D239/48 ,  C07D487/04 ,  C07D403/04 ,  C07D249/14

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20170204080A1

公开(公告)日：2017-07-20

申请号：US15110498

申请日：2015-01-16

申请人： Christine Hiu-tung CHEN ,  Zhuoliang CHEN ,  Jorge Garcia FORTANET ,  Denise GRUNENFELDER ,  Rajesh KARKI ,  Mitsunori KATO ,  Matthew J. LAMARCHE ,  Lawrence Blas PEREZ ,  Travis Matthew STAMS ,  Sarah WILLIAMS

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC分类号： C07D401/04 ,  C07D487/04 ,  C07D403/04 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10774065B2

公开(公告)日：2020-09-15

申请号：US16117674

申请日：2018-08-30

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC分类号： C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10093646B2

公开(公告)日：2018-10-09

申请号：US15110498

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC分类号： C07D401/04 ,  C07D409/14 ,  C07D471/04 ,  C07D403/04 ,  C07D401/14 ,  C07D487/04

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US08933896B2

公开(公告)日：2015-01-13

申请号：US13280346

申请日：2011-10-25

申请人： Scott Honji ,  Masahiko Kaneko ,  Sarah Williams ,  Vincent Ball ,  Paul Millsap ,  Jan-Kristian Markiewicz

发明人： Scott Honji ,  Masahiko Kaneko ,  Sarah Williams ,  Vincent Ball ,  Paul Millsap ,  Jan-Kristian Markiewicz

IPC分类号： G06F3/041 ,  G06F3/0488

CPC分类号： G06F3/0416 ,  G06F3/04883 ,  G06F2203/04808

摘要： In an indirect interaction input device, z-information can be considered in defining a user interaction model for the device. Any measurement of displacement in a z-direction can be used, if such information is available from the input device. The pressure data can be used to define states of interaction, with transitions between these states determined by various thresholds. The device can provide raw or normalized data, and can provide state information or data defining its thresholds that specify state transitions. This information can be provided as an attribute of a contact point provided by the device. Data can be normalized across various similar devices. Applications can use the raw pressure data from the device for their own purposes, or rely on the device itself or host operating system software to interpret the pressure data according to thresholds and states.

摘要翻译： 在间接交互输入设备中，可以考虑在定义设备的用户交互模型时考虑z信息。 如果可以从输入设备获得这种信息，则可以使用z方向上的位移测量。 压力数据可以用于定义交互状态，并通过各种阈值确定这些状态之间的转换。 该设备可以提供原始或规范化的数据，并且可以提供定义其指定状态转换的阈值的状态信息或数据。 该信息可以作为由设备提供的联系点的属性来提供。 数据可以在各种类似的设备上进行归一化。 应用程序可以将设备的原始压力数据用于自己的目的，或者依靠设备本身或主机操作系统软件根据阈值和状态来解释压力数据。