公开(公告)号：US20160002224A1

公开(公告)日：2016-01-07

申请号：US14769159

申请日：2014-03-10

Applicant: John J. ACTON, III ,  Rajan ANAND ,  Ashok ARASAPPAN ,  Qun DANG ,  Iyassu SEBHAT ,  Zhifa PU ,  Takao SUZUKI ,  MERCK SHARP & DOHME CORP.

Inventor： John J. Acton, III ,  Rajan Anand ,  Ashok Arasappan ,  Qun Dang ,  Iyassu Sebhat ,  Zhifa Pu ,  Takao Suzuki

IPC: C07D471/04 ,  A61K31/404 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/4439 ,  A61K31/366 ,  A61K31/397 ,  C07D209/08 ,  C07D401/10

CPC classification number: C07D471/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/404 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D209/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D413/04 ,  C07D413/10 ,  C07D493/04 ,  C07D519/00 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

公开(公告)号：US20140206681A1

公开(公告)日：2014-07-24

申请号：US14160587

申请日：2014-01-22

Applicant: RONALD M. KIM ,  Jian Liu ,  Xiaolei Gao ,  Sobhana Babu Boga ,  Deodialsingh Guiadeen ,  Joseph A. Kozlowski ,  Wensheng Yu ,  Rajan Anand ,  Younong Yu ,  Oleg B. Selyutin ,  Ying-Duo Gao ,  Hao Wu ,  Shilan Liu ,  Chundao Yang ,  Hongjian Wang

Inventor： RONALD M. KIM ,  Jian Liu ,  Xiaolei Gao ,  Sobhana Babu Boga ,  Deodialsingh Guiadeen ,  Joseph A. Kozlowski ,  Wensheng Yu ,  Rajan Anand ,  Younong Yu ,  Oleg B. Selyutin ,  Ying-Duo Gao ,  Hao Wu ,  Shilan Liu ,  Chundao Yang ,  Hongjian Wang

IPC: C07D471/04 ,  A61K31/4985 ,  A61K31/506 ,  C07D487/04 ,  A61K31/5383 ,  A61K31/519 ,  A61K31/5365 ,  A61K45/06 ,  C07D498/04 ,  C07D455/02

CPC classification number: C07D491/048 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  A61K45/06 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  Y02A50/411 ,  Y02A50/463

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

Abstract translation: 本发明提供了根据式I的Bruton's酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐或包含这些化合物的药物组合物及其在治疗中的用途。 特别地，本发明涉及Btk抑制剂化合物在治疗Btk介导的病症中的用途。

公开(公告)号：US20140155404A1

公开(公告)日：2014-06-05

申请号：US14176781

申请日：2014-02-10

Applicant: Chu-Biao Xue ,  Genfeng Cao ,  Taisheng Huang ,  Lihua Chen ,  Ke Zhang ,  Anlai Wang ,  David J. Meloni ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

Inventor： Chu-Biao Xue ,  Genfeng Cao ,  Taisheng Huang ,  Lihua Chen ,  Ke Zhang ,  Anlai Wang ,  David J. Meloni ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

IPC: C07D401/14 ,  C07D417/14 ,  A61K31/496 ,  C07D471/04 ,  A61K31/506 ,  A61K31/502

CPC classification number: C07D401/14 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K45/06 ,  C07D401/06 ,  C07D417/14 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

Abstract translation: 本发明涉及式I化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。 在一些实施方案中，本发明的化合物对CCR5是选择性的。 该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。

公开(公告)号：US07307086B2

公开(公告)日：2007-12-11

申请号：US11125647

申请日：2005-05-10

Applicant: Chu-Biao Xue ,  Changsheng Zheng ,  Ganfeng Cao ,  Hao Feng ,  Michael Xia ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

Inventor： Chu-Biao Xue ,  Changsheng Zheng ,  Ganfeng Cao ,  Hao Feng ,  Michael Xia ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

IPC: C07D471/02 ,  A61K31/47

CPC classification number: C07D471/04 ,  C07D217/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.

Abstract translation: 本发明涉及式I化合物：其是趋化因子受体的调节剂。 本发明的化合物及其组合物可用于治疗与趋化因子受体表达和/或活性相关的疾病。

公开(公告)号：US20050267146A1

公开(公告)日：2005-12-01

申请号：US11125647

申请日：2005-05-10

Applicant: Chu-Biao Xue ,  Changsheng Zheng ,  Ganfeng Cao ,  Hao Feng ,  Michael Xia ,  Rajan Anand ,  Joseph Glenn ,  Brian Metcalf

Inventor： Chu-Biao Xue ,  Changsheng Zheng ,  Ganfeng Cao ,  Hao Feng ,  Michael Xia ,  Rajan Anand ,  Joseph Glenn ,  Brian Metcalf

IPC: A61K31/47 ,  A61K31/4745 ,  C07D217/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/02 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D217/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.

Abstract translation: 本发明涉及式I化合物：其是趋化因子受体的调节剂。 本发明的化合物及其组合物可用于治疗与趋化因子受体表达和/或活性相关的疾病。

公开(公告)号：US20160194330A1

公开(公告)日：2016-07-07

申请号：US14655572

申请日：2013-12-20

Applicant: Amjad ALI ,  Michael Man-Chu LO ,  Yeon-Hee LIM ,  Andrew STAMFORD ,  Rongze KUANG ,  Paul TEMPEST ,  Younong YU ,  Michael BERLIN ,  Pauline TING ,  Gang ZHOU ,  Tao YU ,  Christopher BOYCE ,  Joseph Michael KELLY ,  Jayaram TAGAT ,  Junying ZHENG ,  Xianhai HUANG ,  Wei ZHOU ,  Jae-Hun KIM ,  Nicolas ZORN ,  Dong XIAO ,  Gioconda V. GALLO ,  Walter WON ,  Heping WU ,  Rajan ANAND ,  MERCK SHARP & DOHME CORP.

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC: C07D487/04 ,  C07D487/18 ,  C07D487/08 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Abstract translation: 公开了式A化合物（结构表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：US08680104B2

公开(公告)日：2014-03-25

申请号：US13564434

申请日：2012-08-01

Applicant: Chu-Biao Xue ,  Genfeng Cao ,  Taisheng Huang ,  Lihua Chen ,  Ke Zhang ,  Anlai Wang ,  David J. Meloni ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

Inventor： Chu-Biao Xue ,  Genfeng Cao ,  Taisheng Huang ,  Lihua Chen ,  Ke Zhang ,  Anlai Wang ,  David J. Meloni ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

IPC: A61K31/497

CPC classification number: C07D401/14 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K45/06 ,  C07D401/06 ,  C07D417/14 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

Abstract translation: 本发明涉及式I化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。 在一些实施方案中，本发明的化合物对CCR5是选择性的。 该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。

公开(公告)号：US08268826B2

公开(公告)日：2012-09-18

申请号：US12422517

申请日：2009-04-13

Applicant: Chu-Biao Xue ,  Ganfeng Cao ,  Taisheng Huang ,  Lihua Chen ,  Ke Zhang ,  Anlai Wang ,  David Meloni ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

Inventor： Chu-Biao Xue ,  Ganfeng Cao ,  Taisheng Huang ,  Lihua Chen ,  Ke Zhang ,  Anlai Wang ,  David Meloni ,  Rajan Anand ,  Joseph Glenn ,  Brian W. Metcalf

IPC: A61P29/00 ,  A61P31/12 ,  A61P37/00 ,  C07D237/28 ,  C07D401/14 ,  A61K31/502 ,  C07D403/14 ,  A61K31/501

CPC classification number: C07D401/14 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K45/06 ,  C07D401/06 ,  C07D417/14 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

Abstract translation: 本发明涉及式I化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。 在一些实施方案中，本发明的化合物对CCR5是选择性的。 该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。

公开(公告)号：US20100151839A1

公开(公告)日：2010-06-17

申请号：US12336526

申请日：2008-12-16

Applicant: Udhayakumar Krishnamurthy ,  Rajan Anand ,  Basker Kothandam

Inventor： Udhayakumar Krishnamurthy ,  Rajan Anand ,  Basker Kothandam

IPC: H04M3/42

CPC classification number: H04M3/42 ,  H04M1/575 ,  H04M1/663 ,  H04M3/02 ,  H04M3/42051 ,  H04M3/428 ,  H04M3/436 ,  H04M2203/2011 ,  H04M2203/2038 ,  H04M2242/06

Abstract: Devices, systems and methods are disclosed which enable a user of a communications device to receive a notification of a priority and a context of a call before answering the call. A caller records a short phrase to be played on the callee's device either in place of ringing or following a predetermined amount of rings controlled by the callee's preferences. Among the callee's preferences is a selection of priority, such as among low, high, and critical. When callee's communications device is in any of these modes, every incoming call is intercepted giving the caller the opportunity to provide a short phrase for the context of the call and choose a priority level. This short phrase is played on the callee's communications device if the specified priority of the call matches or exceeds the current mode set on the callee's communications device, and the callee may answer. If the specified priority of the call falls below the current mode set, then the short phrase and priority are saved, but the call is ignored. Optional device configuration allows a special tone, vibration pattern, or beep to occur on the callee's communications device indicating a call has been ignored. The recorded phrase can then be reviewed on demand. The above solution can also be extended to provide a quick glimpse into the voicemail, either in place of the current tone indicating a voicemail has arrived, or immediately following.

Abstract translation: 公开了设备，系统和方法，其使通信设备的用户能够在应答呼叫之前接收到呼叫的优先级和上下文的通知。 来电者在被叫方的设备上记录要播放的短语，以代替铃声或者遵循由受访者喜好控制的预定量的铃声。 被调查者的偏好是优先选择，例如低，高和关键。 当被呼叫者的通信设备处于任何这些模式时，每个来电都被截取，给予呼叫者提供呼叫上下文的短语并选择优先级。 如果呼叫的指定优先级匹配或超过被叫方通信设备上设置的当前模式，则被叫方通信设备上会播放该短语，被叫方可以应答。 如果呼叫的指定优先级低于当前模式设置，则保存短语和优先级，但忽略该呼叫。 可选设备配置允许被叫方通信设备上发生特殊音调，振动模式或蜂鸣声，表示呼叫已被忽略。 录制的短语可以根据需要进行审查。 上述解决方案也可以扩展，以便快速浏览语音邮件，或者代替当前语音信号，指示语音邮件已经到达或紧随其后。

公开(公告)号：US20090197887A1

公开(公告)日：2009-08-06

申请号：US12422517

申请日：2009-04-13

Applicant: Chu-Biao XUE ,  Ganfeng CAO ,  Taisheng HUANG ,  Lihua CHEN ,  Ke ZHANG ,  Anlai WANG ,  David MELONI ,  Rajan ANAND ,  Joseph GLENN ,  Brian W. METCALF

Inventor： Chu-Biao XUE ,  Ganfeng CAO ,  Taisheng HUANG ,  Lihua CHEN ,  Ke ZHANG ,  Anlai WANG ,  David MELONI ,  Rajan ANAND ,  Joseph GLENN ,  Brian W. METCALF

IPC: A61K31/498 ,  C07D401/14 ,  A61K31/506 ,  A61P31/18 ,  A61P37/00 ,  C07K14/71

CPC classification number: C07D401/14 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K45/06 ,  C07D401/06 ,  C07D417/14 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

Abstract translation: 本发明涉及式I化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。 在一些实施方案中，本发明的化合物对CCR5是选择性的。 该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。