公开(公告)号：US20130005741A1

公开(公告)日：2013-01-03

申请号：US13610005

申请日：2012-09-11

申请人： Keith John HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory T. STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING

发明人： Keith John HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory T. STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING

IPC分类号： C07D401/04 ,  A61P37/08 ,  A61P11/06 ,  A61P11/02 ,  A61P3/10 ,  A61P27/02 ,  A61P27/14 ,  A61P11/00 ,  A61P9/10 ,  A61P3/06 ,  A61K31/506 ,  A61P17/00

CPC分类号： C07D403/04

摘要： The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrimidine compound of formula (I): or an enantiomer thereof, or an ester prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.

摘要翻译： 本发明涉及式（I）的2,6-取代-4-单取代氨基嘧啶化合物或其对映异构体或其酯前药或其药学上可接受的盐，或包含这种化合物的药物组合物。 本发明还包括通过施用药学有效量的这种化合物来治疗患者的方法。

公开(公告)号：US20120245199A1

公开(公告)日：2012-09-27

申请号：US13488541

申请日：2012-06-05

申请人： Yong Mi CHOI-SLEDESKI ,  Thaddeus R. NIEDUZAK ,  Gregory B. POLI ,  Patrick Wai-Kwok SHUM ,  Gregory T. STOKLOSA ,  Zhicheng ZHAO

发明人： Yong Mi CHOI-SLEDESKI ,  Thaddeus R. NIEDUZAK ,  Gregory B. POLI ,  Patrick Wai-Kwok SHUM ,  Gregory T. STOKLOSA ,  Zhicheng ZHAO

IPC分类号： A61K31/437 ,  A61P29/00 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.

摘要翻译： 本发明涉及用于治疗和改善炎性疾病的化合物和组合物。 具体地说，本发明涉及具有类胰蛋白酶抑制活性的化合物及其中间体，包含这些化合物的药物组合物，以及治疗患有可通过施用类胰蛋白酶抑制剂而改善的疾病或病症的受试者的方法。

公开(公告)号：US20120245161A1

公开(公告)日：2012-09-27

申请号：US13488539

申请日：2012-06-05

申请人： Yong Mi CHOI-SLEDESKI ,  Guyan LIANG ,  Thaddeus R. NIEDUZAK ,  Gregory B. POLI ,  Patrick Wai-Kwok SHUM ,  Gregory T. STOKLOSA ,  Zhicheng ZHAO

发明人： Yong Mi CHOI-SLEDESKI ,  Guyan LIANG ,  Thaddeus R. NIEDUZAK ,  Gregory B. POLI ,  Patrick Wai-Kwok SHUM ,  Gregory T. STOKLOSA ,  Zhicheng ZHAO

IPC分类号： A61K31/454 ,  C07D413/14 ,  A61K31/5377 ,  A61P11/00 ,  A61K31/4545 ,  C07D498/06 ,  A61K31/5383 ,  C07D401/06 ,  C07D401/14

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D498/14

摘要： The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of the formula wherein R1, R2, R4 and R5 are as described herein. More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted indolyl-piperidinyl benzylamines.

摘要翻译： 本发明公开并要求一系列下式的取代的吲哚基 - 哌啶基苄胺其中R 1，R 2，R 4和R 5如本文所述。 更具体地，本发明的化合物是β-葡聚糖酶的抑制剂，因此可用作药剂。 此外，本发明还公开了制备取代的吲哚基 - 哌啶基苄胺的方法。

公开(公告)号：US20130005728A1

公开(公告)日：2013-01-03

申请号：US13610027

申请日：2012-09-11

申请人： Keith J. HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING ,  David STEFANY ,  Charles GARDNER

发明人： Keith J. HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING ,  David STEFANY ,  Charles GARDNER

IPC分类号： C07D403/04 ,  A61K31/5377 ,  A61K31/506 ,  C07D401/04 ,  A61P37/08 ,  A61P11/06 ,  A61P11/02 ,  A61P17/00 ,  A61P27/02 ,  A61P27/14 ,  A61P11/00 ,  A61P9/10 ,  A61P3/06 ,  A61P3/10 ,  C07D413/04

CPC分类号： C07D403/04

摘要： The present invention is directed to a substituted pyrimidine compound of formula (I) or an enantiomer thereof, or a prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.

摘要翻译： 本发明涉及式（I）的取代嘧啶化合物或其对映异构体或其前药或药学上可接受的盐，或包含该化合物的药物组合物。 本发明还包括通过施用药学有效量的这种化合物来治疗患者的方法。

公开(公告)号：US09064186B2

公开(公告)日：2015-06-23

申请号：US13991721

申请日：2010-12-09

申请人： Xiaohui Xie ,  Xiao Zeng ,  Yingfei Liu ,  Yanming Zou ,  Kongqiao Wang ,  Zhicheng Zhao ,  Anni Cai

发明人： Xiaohui Xie ,  Xiao Zeng ,  Yingfei Liu ,  Yanming Zou ,  Kongqiao Wang ,  Zhicheng Zhao ,  Anni Cai

IPC分类号： G06K9/68 ,  G06K9/62 ,  G06K9/00

CPC分类号： G06K9/6202 ,  G06K9/00751 ,  G06K9/00765

摘要： An example apparatus is caused to receive a video sequence of a plurality of frames, and perform a number of operations as each of at least some of the frames is received but before all of the frames are received. The apparatus is caused to calculate a score for the frame, and compare the score for the frame to a predefined threshold. The apparatus is caused to cause output of the frame as a key frame in an instance in which the frame is received within a specified period of time and the score for the frame is above the predefined threshold. Otherwise, in an instance in which none of the scores for frames received within the specified period of time is above the predefined threshold, the apparatus is caused to cause output of one of the frames received within the specified period of time as a key frame.

摘要翻译： 使得示例设备接收多个帧的视频序列，并且在接收到至少一些帧中的每一个之后但在接收到所有帧之前执行多个操作。 使该装置计算该帧的分数，并将该帧的得分与预定义的阈值进行比较。 导致该装置在帧的指定时间段内接收帧的情况下将帧的输出作为关键帧，并且帧的分数高于预定阈值。 否则，在指定时间段内接收到的帧的分数都不高于预定义阈值的情况下，使装置将指定时间段内接收到的一个帧的输出作为关键帧。

公开(公告)号：US20130251274A1

公开(公告)日：2013-09-26

申请号：US13991721

申请日：2010-12-09

申请人： Xiaohui Xie ,  Xiao Zeng ,  Yingfei Liu ,  Yanming Zou ,  Kongqiao Wang ,  Zhicheng Zhao ,  Anni Cai

发明人： Xiaohui Xie ,  Xiao Zeng ,  Yingfei Liu ,  Yanming Zou ,  Kongqiao Wang ,  Zhicheng Zhao ,  Anni Cai

IPC分类号： G06K9/62

CPC分类号： G06K9/6202 ,  G06K9/00751 ,  G06K9/00765

摘要： An example apparatus is caused to receive a video sequence of a plurality of frames, and perform a number of operations as each of at least some of the frames is received but before all of the frames are received. The apparatus is caused to calculate a score for the frame, and compare the score for the frame to a predefined threshold. The apparatus is caused to cause output of the frame as a key frame in an instance in which the frame is received within a specified period of time and the score for the frame is above the predefined threshold. Otherwise, in an instance in which none of the scores for frames received within the specified period of time is above the predefined threshold, the apparatus is caused to cause output of one of the frames received within the specified period of time as a key frame.

摘要翻译： 使得示例设备接收多个帧的视频序列，并且在接收到至少一些帧中的每一个之后但在接收到所有帧之前执行多个操作。 使该装置计算该帧的分数，并将该帧的得分与预定义的阈值进行比较。 导致该装置在帧的指定时间段内接收帧的情况下将帧的输出作为关键帧，并且帧的分数高于预定阈值。 否则，在指定时间段内接收到的帧的分数都不高于预定义阈值的情况下，使装置将指定时间段内接收到的一个帧的输出作为关键帧。

公开(公告)号：US20120142735A1

公开(公告)日：2012-06-07

申请号：US13396111

申请日：2012-02-14

申请人： Yong- Mi CHOI-SLEDESKI ,  Charles J. GARDNER ,  Guyan LIANG ,  Gregory B. POLI ,  Patrick Wai-Kwok SHUM ,  Grzegory T. STOKLOSA ,  Zhicheng ZHAO

发明人： Yong- Mi CHOI-SLEDESKI ,  Charles J. GARDNER ,  Guyan LIANG ,  Gregory B. POLI ,  Patrick Wai-Kwok SHUM ,  Grzegory T. STOKLOSA ,  Zhicheng ZHAO

IPC分类号： A61K31/454 ,  A61P25/00 ,  A61P29/00 ,  A61P27/02 ,  A61P1/00 ,  A61P11/06 ,  A61P37/08 ,  A61P11/00 ,  A61P1/16 ,  A61P17/02 ,  A61P17/00 ,  A61P9/10 ,  A61P3/10 ,  A61P35/00 ,  A61P1/04 ,  A61P31/12 ,  A61P19/02 ,  A61P17/06 ,  C07D401/06

CPC分类号： C07D401/06 ,  A61K31/454 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention extends to a compound of formula I: or a pharmaceutically acceptable salt of said compound, or a pharmaceutical composition comprising the compound of formula I and a pharmaceutically acceptable carrier. The invention is also directed to the use of a compound of formula I as an inhibitor of tryptase and for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by an inhibitor of tryptase. The invention further includes methods for the preparation of a compound of formula I.

摘要翻译： 本发明延伸到式I化合物：或所述化合物的药学上可接受的盐，或包含式I化合物和药学上可接受的载体的药物组合物。 本发明还涉及式I化合物作为类胰蛋白酶抑制剂的用途，并且用于治疗患有需要由类胰蛋白酶抑制剂改善的生理条件或受其影响的患者。 本发明还包括制备式I化合物的方法。