公开(公告)号：US20180362518A1

公开(公告)日：2018-12-20

申请号：US16061815

申请日：2016-12-15

Applicant: Thomas J. GRESHOCK ,  James MULHEARN ,  Liangqin GUO ,  Ting ZHANG ,  Deping WANG ,  Ronald M. KIM ,  Mark E. LAYTON ,  Michael J. KELLY, III ,  Rajan ANAND ,  Tianying JIAN ,  Philippe NANTERMET ,  Anthony J. ROECKER ,  Walter WON ,  Gang ZHOU ,  Merck Sharp & Dohme Corp.

Inventor： Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

IPC: C07D417/12 ,  C07D285/135 ,  C07D277/52 ,  A61P11/14 ,  A61P17/04 ,  A61P25/04 ,  A61P25/02

CPC classification number: C07D417/12 ,  A61K45/06 ,  A61P11/14 ,  A61P17/04 ,  A61P25/02 ,  A61P25/04 ,  C07D277/52 ,  C07D285/135

Abstract: Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Na 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

公开(公告)号：US09676780B2

公开(公告)日：2017-06-13

申请号：US14655572

申请日：2013-12-20

Applicant: MERCK SHARP & DOHME CORP. ,  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

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 ,  A61K31/519 ,  C07D487/08 ,  C07D487/18 ,  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.

公开(公告)号：US09650375B2

公开(公告)日：2017-05-16

申请号：US14769159

申请日：2014-03-10

Applicant: Merck Sharp & Dohme Corp. ,  John J. Acton, III ,  Rajan Anand ,  Ashok Arasappan ,  Qun Dang ,  Iyassu Sebhat ,  Zhifa Pu ,  Takao Suzuki

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

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

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.

公开(公告)号：US20170044183A1

公开(公告)日：2017-02-16

申请号：US15305421

申请日：2015-04-21

Applicant: Yeon-Hee Lim ,  Zhuyan Guo ,  Amjad Ali ,  Scott D. Edmondson ,  Weiguo Liu ,  Giocanda V. Gallo-Etienne ,  Heping Wu ,  Ying-Duo Gao ,  Andrew W. Stamford ,  Younong Yu ,  Nancy J. Kevin ,  Rajan Anand ,  Deyou Sha ,  Santhosh F. Neelamkavil ,  Zahid Hussain ,  Puneet Kumar ,  Remond Moningka ,  Joseph L. Duffy ,  Jiayi Xu ,  Yu Jiang ,  Anjan Chakrabarti ,  Hiroki Sone

Inventor： Yeon-Hee Lim ,  Zhuyan Guo ,  Amjad Ali ,  Scott D. Edmondson ,  Weiguo Liu ,  Giocanda V. Gallo-Etienne ,  Heping Wu ,  Ying-Duo Gao ,  Andrew W. Stamford ,  Younong Yu ,  Nancy J. Kevin ,  Rajan Anand ,  Deyou Sha ,  Santhosh F. Neelamkavil ,  Zahid Hussain ,  Puneet Kumar ,  Remond Moningka ,  Joseph L. Duffy ,  Jiayi Xu ,  Yu Jiang ,  Anjan Chakrabarti ,  Hiroki Sone

IPC: C07D498/20 ,  C07F9/6561 ,  C07D487/10 ,  C07D498/10 ,  C07D471/10

CPC classification number: C07D498/20 ,  C07D471/10 ,  C07D487/10 ,  C07D498/10 ,  C07F9/6561

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Abstract translation: 本发明提供式（I）的化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。

公开(公告)号：US20150353570A1

公开(公告)日：2015-12-10

申请号：US14762954

申请日：2014-01-22

Applicant: Hao WU ,  Ronald M. KIM ,  Jian LIU ,  Xiaolei GAO ,  Sobhana Babu BOGA ,  Deodialsingh GUIADEEN ,  Joseph KOZLOWSKI ,  Wensheng YU ,  Rajan ANAND ,  Younong YU ,  Oleg B. Selyutin ,  Ying-Duo GAO ,  Shilan LIU ,  Chundao YANG ,  Hongjian WANG ,  MERCK SHARP & DOHME CORP.

Inventor： RONALD M. KIM ,  JIAN LIU ,  XIAOLEI GAO ,  SOBHANA BABU BOGA ,  DEODIALSINGH GUIADEEN ,  JOSEPH A. KOZLOWSKI ,  WENSHENG WU ,  RAJAN ANAND ,  YOUNONG YU ,  OLEG B. SELYUTIN ,  YING-DUO GAO ,  HAO WU ,  SHILAN LIU ,  CHUNDAO YANG ,  HONGJIAN WANG

IPC: C07D491/048 ,  C07D471/04 ,  A61K45/06 ,  A61K31/5383 ,  C07D455/02 ,  A61K31/5365 ,  A61K31/497 ,  C07D498/04

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：US09126976B2

公开(公告)日：2015-09-08

申请号：US14239452

申请日：2012-08-13

Applicant: Rajan Anand ,  Vincent J. Colandrea ,  Maud Reiter ,  Petr Vachal ,  Aaron Zwicker ,  Jonathan E. Wilson ,  Fengqi Zhang ,  Kake Zhao

Inventor： Rajan Anand ,  Vincent J. Colandrea ,  Maud Reiter ,  Petr Vachal ,  Aaron Zwicker ,  Jonathan E. Wilson ,  Fengqi Zhang ,  Kake Zhao

IPC: A61K31/498 ,  C07D241/42 ,  C07D409/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D409/06 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D241/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06

Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract translation: 具有式Ia结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

公开(公告)号：US20140221333A1

公开(公告)日：2014-08-07

申请号：US14233478

申请日：2012-07-19

Applicant: Adrianus Petrus Antonius De Man ,  Jan-Gerard Sterrenburg ,  Han C.A. Raaijmakers ,  Allard Kaptein ,  Arthura A. Oubrie ,  Johannes Bernardus Maria Rewinkel ,  Christiaan Gerardus Johannes Maria Jans ,  Jacobus C.H.M. Wijkamans ,  Tjeerd A. Barf ,  Alan B. Cooper ,  Ronald M. Kim ,  Sobhana Babu Boga ,  Hugh Y. Zhu ,  Xiaolei Gao ,  Xin Yao ,  Rajan Anand ,  Hao Wu ,  Shilan Liu ,  Chundao Yang ,  Abdul-Basit Alhassan ,  James Wang ,  Younong Yu ,  Jian Liu ,  Henry M. Vaccaro

Inventor： Adrianus Petrus Antonius De Man ,  Jan-Gerard Sterrenburg ,  Han C.A. Raaijmakers ,  Allard Kaptein ,  Arthura A. Oubrie ,  Johannes Bernardus Maria Rewinkel ,  Christiaan Gerardus Johannes Maria Jans ,  Jacobus C.H.M. Wijkamans ,  Tjeerd A. Barf ,  Alan B. Cooper ,  Ronald M. Kim ,  Sobhana Babu Boga ,  Hugh Y. Zhu ,  Xiaolei Gao ,  Xin Yao ,  Rajan Anand ,  Hao Wu ,  Shilan Liu ,  Chundao Yang ,  Abdul-Basit Alhassan ,  James Wang ,  Younong Yu ,  Jian Liu ,  Henry M. Vaccaro

IPC: C07D487/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/53 ,  A61K31/4985 ,  A61K31/541

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D513/04 ,  C07D519/00

Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

Abstract translation: 提供根据式（I）的6-5元稠合吡啶环化合物或其药学上可接受的盐，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，提供了使用元稠合的吡啶环化合物来治疗布鲁丁的酪氨酸激酶（Btk）介导的病症。

公开(公告)号：US08532631B2

公开(公告)日：2013-09-10

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 ,  H04M1/64 ,  H04B7/00

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.

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。

公开(公告)号：US20130123237A1

公开(公告)日：2013-05-16

申请号：US13812536

申请日：2012-02-23

Applicant: Rajan Anand ,  James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Lin Chu ,  Vincent J. Colandrea ,  Guizhen Dong ,  James F. Dropinski ,  Danqing Feng ,  Jacqueline D. Hicks ,  Jinlong Jiang ,  Alexander J. Kim ,  Kenneth J. Leavitt ,  Bing Li ,  Xiaoxia Qian ,  Iyassu Sebhat ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

Inventor： Rajan Anand ,  James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Lin Chu ,  Vincent J. Colandrea ,  Guizhen Dong ,  James F. Dropinski ,  Danqing Feng ,  Jacqueline D. Hicks ,  Jinlong Jiang ,  Alexander J. Kim ,  Kenneth J. Leavitt ,  Bing Li ,  Xiaoxia Qian ,  Iyassu Sebhat ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC: A61K31/5377 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/351 ,  A61K31/397 ,  A61K31/4412 ,  C07D471/04 ,  A61K31/496

CPC classification number: A61K31/5377 ,  A61K31/351 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

Abstract: Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are 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：US08150674B2

公开(公告)日：2012-04-03

申请号：US12476954

申请日：2009-06-02

Applicant: Rajan Anand ,  Paritosh Bajpay

Inventor： Rajan Anand ,  Paritosh Bajpay

IPC: G06F9/45 ,  G06F9/455

CPC classification number: G06F11/3664 ,  G06F11/3692

Abstract: A platform for the automated testing of event driven software applications is provided. A source environment is replicated to a target environment. The target environment includes a target system. A test case is defined with a target system, specific attributes and verification information. The attributes of the test case include the target system. The test case is fired. An event is simulated for the test case based on the target system and the specific attributes. The simulated event is transmitted to the target environment. The results of the test case being fired are determined based on verification information. The results are recorded to a data store.

Abstract translation: 提供了一个用于事件驱动软件应用程序的自动化测试的平台。 源环境被复制到目标环境。 目标环境包括目标系统。 测试用例由目标系统定义，具体属性和验证信息。 测试用例的属性包括目标系统。 测试用例被触发。 基于目标系统和特定属性，为测试用例模拟事件。 模拟事件被传送到目标环境。 根据验证信息确定被触发的测试用例的结果。 结果记录到数据存储。