公开(公告)号：US07446195B2

公开(公告)日：2008-11-04

申请号：US11505263

申请日：2006-08-16

Applicant: Yongqi Deng ,  Lianyun Zhao ,  Gerald W. Shipps, Jr. ,  Patrick J. Curran ,  M. Arshad Siddiqui ,  Rumin Zhang ,  Charles W. McNemar ,  Todd W. Mayhood ,  William T. Windsor ,  Emma M. Lees ,  David A. Parry

Inventor： Yongqi Deng ,  Lianyun Zhao ,  Gerald W. Shipps, Jr. ,  Patrick J. Curran ,  M. Arshad Siddiqui ,  Rumin Zhang ,  Charles W. McNemar ,  Todd W. Mayhood ,  William T. Windsor ,  Emma M. Lees ,  David A. Parry

IPC: C07D413/12 ,  C07D403/12 ,  C07D409/12 ,  C07D405/12

CPC classification number: C07D405/12 ,  C07D333/40 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.

Abstract translation: 描述了细胞周期蛋白依赖性激酶2的抑制剂，包括抑制剂的组合物，以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法，抑制CDK-2的方法以及治疗疾病或疾病症状的方法。

公开(公告)号：US20080139571A1

公开(公告)日：2008-06-12

申请号：US11936380

申请日：2007-11-07

Applicant: David B. Belanger ,  M. Arshad Siddiqui ,  Timothy J. Guzi ,  Patrick J. Curran ,  Praveen K. Tadikonda ,  Blake Hamann ,  Panduranga Adulla P. Reddy ,  Lianyun Zhao

Inventor： David B. Belanger ,  M. Arshad Siddiqui ,  Timothy J. Guzi ,  Patrick J. Curran ,  Praveen K. Tadikonda ,  Blake Hamann ,  Panduranga Adulla P. Reddy ,  Lianyun Zhao

IPC: A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并吡嗪化合物作为蛋白质和/或极光激酶的抑制剂，制备这些化合物的方法，包含一种或多种这样的化合物的药物组合物，制备药物制剂的方法，包括一种或多种这样的化合物 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或极光激酶相关的一种或多种疾病的方法。

公开(公告)号：US20080027063A1

公开(公告)日：2008-01-31

申请号：US11758243

申请日：2007-06-05

Applicant: Lianyun Zhao ,  Panduranga Reddy ,  Neng-Yang Shih ,  Kamil Paruch ,  Timothy Guzi ,  M. Siddiqui

Inventor： Lianyun Zhao ,  Panduranga Reddy ,  Neng-Yang Shih ,  Kamil Paruch ,  Timothy Guzi ,  M. Siddiqui

IPC: A61K31/4985 ,  A61P35/00 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并吡嗪化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种此类化合物的药物组合物，制备药物制剂的方法，包括一种或多种 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

公开(公告)号：US20070105864A1

公开(公告)日：2007-05-10

申请号：US11598188

申请日：2006-11-08

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  David Parry ,  Lianyun Zhao ,  Patrick Curran ,  David Belanger ,  Blake Hamann ,  Panduranga Reddy ,  M. Siddiqui ,  Praveen Tadikonda

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  David Parry ,  Lianyun Zhao ,  Patrick Curran ,  David Belanger ,  Blake Hamann ,  Panduranga Reddy ,  M. Siddiqui ,  Praveen Tadikonda

IPC: A61K31/498

CPC classification number: A61K31/4985 ,  A61K31/498

Abstract: The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.

Abstract translation: 本发明提供使用咪唑并[1,2-a]吡嗪化合物抑制选自AKT，检查点激酶，极光激酶，Pim-1激酶和酪氨酸激酶的蛋白激酶的方法以及治疗，预防，抑制 ，或使用这些化合物改善与蛋白激酶相关的一种或多种疾病。

公开(公告)号：US20070043045A1

公开(公告)日：2007-02-22

申请号：US11505263

申请日：2006-08-16

Applicant: Yongqi Deng ,  Lianyun Zhao ,  Gerald Shipps ,  Patrick Curran ,  M. Siddiqui ,  Rumin Zhang ,  Charles McNemar ,  Todd Mayhood ,  William Windsor ,  Emma Lees ,  David Parry

Inventor： Yongqi Deng ,  Lianyun Zhao ,  Gerald Shipps ,  Patrick Curran ,  M. Siddiqui ,  Rumin Zhang ,  Charles McNemar ,  Todd Mayhood ,  William Windsor ,  Emma Lees ,  David Parry

IPC: A61K31/5377 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/428 ,  A61K31/42 ,  A61K31/4196 ,  A61K31/4178 ,  A61K31/4025 ,  A61K31/416 ,  C07D413/02 ,  C07D405/02 ,  C07D409/02 ,  C07D417/02

CPC classification number: C07D405/12 ,  C07D333/40 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.

Abstract translation: 描述了细胞周期蛋白依赖性激酶2的抑制剂，包括抑制剂的组合物，以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法，抑制CDK-2的方法以及治疗疾病或疾病症状的方法。

公开(公告)号：US20060106023A1

公开(公告)日：2006-05-18

申请号：US11272392

申请日：2005-11-10

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Lianyun Zhao ,  Patrick Curran ,  David Belanger ,  Blake Hamann ,  Panduranga Reddy ,  M. Siddiqui

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Lianyun Zhao ,  Patrick Curran ,  David Belanger ,  Blake Hamann ,  Panduranga Reddy ,  M. Siddiqui

IPC: A61K31/506 ,  A61K31/498 ,  C07D487/02

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并[1,2-a]吡嗪化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

公开(公告)号：US09273040B2

公开(公告)日：2016-03-01

申请号：US14353488

申请日：2012-10-26

Applicant: Mark E. Layton ,  Joseph E. Pero ,  Hannah Fiji ,  Michael J. Kelly, III ,  Pablo de Leon ,  Michael A. Rossi ,  Kevin F. Gilbert ,  Anthony J. Roecker ,  Zhijian Zhao ,  Swati I P. Mercer ,  Scott Wolkenberg ,  James Mulhearn ,  Lianyun Zhao ,  Dansu Li

Inventor： Mark E. Layton ,  Joseph E. Pero ,  Hannah Fiji ,  Michael J. Kelly, III ,  Pablo de Leon ,  Michael A. Rossi ,  Kevin F. Gilbert ,  Anthony J. Roecker ,  Zhijian Zhao ,  Swati I P. Mercer ,  Scott Wolkenberg ,  James Mulhearn ,  Lianyun Zhao ,  Dansu Li

IPC: A61K31/00 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D491/107 ,  C07D493/10

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D491/107 ,  C07D493/10

Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 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 neuropathic pain disorders using the same.

Abstract translation: 公开了式（A）的化合物或其盐，其中“Het”，Ra和Rb在本文中定义，其具有用于阻断在外周和交感神经元中发现的Nav 1.7离子通道的性质。 还描述了包含式（A）化合物或其盐的药物制剂，以及使用其制备神经性疼痛障碍的方法。

公开(公告)号：US08883801B2

公开(公告)日：2014-11-11

申请号：US13818177

申请日：2011-08-22

Applicant: Lianyun Zhao ,  Duan Liu ,  Shuyi Tang ,  Amit K. Mandal ,  Umar Faruk Mansoor ,  Lalanthi Dilrukshi Vitharana ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui

Inventor： Lianyun Zhao ,  Duan Liu ,  Shuyi Tang ,  Amit K. Mandal ,  Umar Faruk Mansoor ,  Lalanthi Dilrukshi Vitharana ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui

IPC: A61K31/519 ,  C07D239/70 ,  A61K31/5377 ,  C07D487/04 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.

Abstract translation: 本发明涉及作为哺乳动物雷帕霉素靶标（mTOR）激酶的抑制剂的式（I）的吡唑并[1,5-a]嘧啶化合物，其也称为FRAP，RAFT，RAPT或SEP。 所述化合物可用于治疗其中mTOR失调的癌症和其它病症。 本发明还提供包含吡唑并[1,5-a]嘧啶化合物的药物组合物。

公开(公告)号：US08591943B2

公开(公告)日：2013-11-26

申请号：US13263193

申请日：2010-04-08

Applicant: Yongqi Deng ,  Binyuan Sun ,  Hongbo Zeng ,  Matthew Richards ,  Gerald W. Shipps, Jr. ,  Cliff C. Cheng ,  Yinyan Zhao ,  Andrew McRiner ,  Zhaoyang Meng ,  Yang Nan ,  Mehul F. Patel ,  Iwona E. Wrona ,  Panduranga Adulla Reddy ,  Brian M. Eklov ,  Shuyi Tang ,  Duan Liu ,  Amit K. Mandal ,  Lianyun Zhao ,  M. Arshad Siddiqui

Inventor： Yongqi Deng ,  Binyuan Sun ,  Hongbo Zeng ,  Matthew Richards ,  Gerald W. Shipps, Jr. ,  Cliff C. Cheng ,  Yinyan Zhao ,  Andrew McRiner ,  Zhaoyang Meng ,  Yang Nan ,  Mehul F. Patel ,  Iwona E. Wrona ,  Panduranga Adulla Reddy ,  Brian M. Eklov ,  Shuyi Tang ,  Duan Liu ,  Amit K. Mandal ,  Lianyun Zhao ,  M. Arshad Siddiqui

IPC: A61K9/127 ,  A61K39/395 ,  A61K31/554 ,  A61K31/541 ,  A61K31/5377 ,  A61K38/50 ,  A61K31/553 ,  A61K33/24 ,  A61K31/704 ,  A61K31/551 ,  A61K31/538 ,  A61K31/519

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.

Abstract translation: 本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制mTOR的方法以及使用这些化合物治疗，预防，抑制或改善与mTOR相关的一种或多种疾病的方法。

公开(公告)号：US08476278B2

公开(公告)日：2013-07-02

申请号：US12738487

申请日：2008-10-27

Applicant: Panduranga Adulla P. Reddy ,  Tzu T. Wong ,  Lianyun Zhao ,  Shuyi Tang ,  Marc A. Labroli ,  Timothy J. Guzi ,  M. Arshad Siddiqui

Inventor： Panduranga Adulla P. Reddy ,  Tzu T. Wong ,  Lianyun Zhao ,  Shuyi Tang ,  Marc A. Labroli ,  Timothy J. Guzi ,  M. Arshad Siddiqui

IPC: A61K31/496 ,  C07D417/14 ,  A61K31/427 ,  A61K31/551 ,  A61K31/5377 ,  C07D413/14 ,  C07D417/12 ,  C07D471/10

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/056 ,  C07D495/04

Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.

Abstract translation: 本发明涉及新的噻唑衍生物，包含噻唑衍生物的组合物，以及使用噻唑衍生物治疗或预防增殖性疾病，抗增殖性疾病，炎症，关节炎，中枢神经系统疾病，心血管疾病， 脱发，神经元疾病，缺血性损伤，病毒感染，真菌感染或与蛋白激酶活性相关的病症。