公开(公告)号：US08008491B2

公开(公告)日：2011-08-30

申请号：US12140632

申请日：2008-06-17

Applicant: John Ziqi Jiang ,  Jack Roger Koehl ,  Shujaath Mehdi ,  Neil Moorcroft ,  Kwon Yon Musick ,  Philip Marvin Weintraub ,  Paul Robert Eastwood

Inventor： John Ziqi Jiang ,  Jack Roger Koehl ,  Shujaath Mehdi ,  Neil Moorcroft ,  Kwon Yon Musick ,  Philip Marvin Weintraub ,  Paul Robert Eastwood

IPC: C07D403/04 ,  C07D209/04

CPC classification number: C04B35/632 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  C07D209/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D471/04 ,  C07D487/08

Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract translation: 本发明涉及一系列式I的取代的氮杂 - 吲哚衍生物：其中R，R 1，R 2，R 3，R 4，X和Y如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病 系统和心血管疾病。

公开(公告)号：US07928231B2

公开(公告)日：2011-04-19

申请号：US12411818

申请日：2009-03-26

Applicant: John Gerard Jurcak ,  Matthieu Barrague ,  Timothy Alan Gillespy ,  Michael Louis Edwards ,  Kwon Yon Musick ,  Philip Marvin Weintraub ,  Yan Du ,  Ramalinga M. Dharanipragada ,  Ashfaq Ahmad Parkar

Inventor： John Gerard Jurcak ,  Matthieu Barrague ,  Timothy Alan Gillespy ,  Michael Louis Edwards ,  Kwon Yon Musick ,  Philip Marvin Weintraub ,  Yan Du ,  Ramalinga M. Dharanipragada ,  Ashfaq Ahmad Parkar

IPC: C07D403/00 ,  C07D231/54

CPC classification number: C07D495/04

Abstract: Thienopyrazoles of formula I, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).

Abstract translation: 式I的噻吩并吡唑类，其制备方法，包含这些化合物的药物组合物及其在治疗能够通过抑制蛋白激酶（特别是白细胞介素-2诱导型酪氨酸激酶（ITK））调节的疾病状态的药物用途。

公开(公告)号：US07169925B2

公开(公告)日：2007-01-30

申请号：US10421511

申请日：2003-04-23

Applicant: Gregory H. Merriman ,  Philip M. Weintraub ,  Jeffrey S. Sabol ,  Ramalinga M. Dharanipragada ,  Nicholas J. Hrib ,  John G. Jurcak ,  Alexandre Gross ,  Brian Whiteley ,  Kwon Yon Musick ,  Joseph T. Klein

Inventor： Gregory H. Merriman ,  Philip M. Weintraub ,  Jeffrey S. Sabol ,  Ramalinga M. Dharanipragada ,  Nicholas J. Hrib ,  John G. Jurcak ,  Alexandre Gross ,  Brian Whiteley ,  Kwon Yon Musick ,  Joseph T. Klein

IPC: C07D403/12 ,  C07D401/00

CPC classification number: A61K31/381 ,  A61K31/40 ,  A61K31/405 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

Abstract: This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.

Abstract translation: 本发明公开了一种用于治疗过敏，哮喘，鼻炎，皮炎，B细胞淋巴瘤，肿瘤和与细菌，鼻病毒或呼吸道合胞病毒（RSV）感染相关的疾病的新一类吲哚衍生物。 现在已经发现，本发明的化合物能够调节T辅助细胞Th1 / Th2，从而能够抑制白细胞介素-4（IL-4）信号，IL-4释放或IL的转录 -4生产。

公开(公告)号：US20080255350A1

公开(公告)日：2008-10-16

申请号：US12140632

申请日：2008-06-17

Applicant: John Z. JIANG ,  Jack Roger KOEHL ,  Shujaath MEHDI ,  Neil MOORCROFT ,  Kwon Yon MUSICK ,  Philip Marvin WEINTRAUB ,  Paul Robert EASTWOOD

Inventor： John Z. JIANG ,  Jack Roger KOEHL ,  Shujaath MEHDI ,  Neil MOORCROFT ,  Kwon Yon MUSICK ,  Philip Marvin WEINTRAUB ,  Paul Robert EASTWOOD

IPC: C07D403/04 ,  C07D417/04 ,  C07D401/04 ,  C07D471/04

CPC classification number: C04B35/632 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  C07D209/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D471/04 ,  C07D487/08

Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract translation: 本发明涉及一系列式I的取代的氮杂 - 吲哚衍生物：其中R 1，R 2，R 2，R 3， R 4，X和Y如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病 系统和心血管疾病。

公开(公告)号：US20120202795A1

公开(公告)日：2012-08-09

申请号：US13449711

申请日：2012-04-18

Applicant: Philip M. WEINTRAUB ,  Paul R. EASTWOOD ,  Shujaath MEHDI ,  David W. STEFANY ,  Kwon Yon MUSICK ,  Neil MOORCROFT ,  Sungtaek LIM ,  John Z. JIANG ,  Hartmut RUTTEN ,  Stefan PEUKERT ,  Uwe SCHWAHN

Inventor： Philip M. WEINTRAUB ,  Paul R. EASTWOOD ,  Shujaath MEHDI ,  David W. STEFANY ,  Kwon Yon MUSICK ,  Neil MOORCROFT ,  Sungtaek LIM ,  John Z. JIANG ,  Hartmut RUTTEN ,  Stefan PEUKERT ,  Uwe SCHWAHN

IPC: A61K31/4412 ,  C07D217/24 ,  C07D413/10 ,  C07D401/10 ,  C07D401/04 ,  C07D413/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  A61K31/506 ,  C07D491/113 ,  C07D417/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/551 ,  A61K31/497 ,  A61P25/00 ,  A61P25/28 ,  A61P9/10 ,  A61P9/00 ,  A61K31/472 ,  A61K31/444 ,  C07D213/64

CPC classification number: C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract translation: 本发明涉及一系列式I的2,3,5-取代吡啶酮衍生物：其中R，R 1，R 2，R 3和R 4如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病 系统和心血管疾病。

公开(公告)号：US07518000B2

公开(公告)日：2009-04-14

申请号：US11368566

申请日：2006-03-06

Applicant: John Gerald Jurcak ,  Matthieu Barrague ,  Timothy Alan Gillespy ,  Michael Louis Edwards ,  Kwon Yon Musick ,  Phillip Marvin Weintraub ,  Yan Du ,  Ramalinga M. Dharanipragada ,  Ashfaq Ahmed Parkar

Inventor： John Gerald Jurcak ,  Matthieu Barrague ,  Timothy Alan Gillespy ,  Michael Louis Edwards ,  Kwon Yon Musick ,  Phillip Marvin Weintraub ,  Yan Du ,  Ramalinga M. Dharanipragada ,  Ashfaq Ahmed Parkar

IPC: C07D495/02 ,  C07D231/54

CPC classification number: C07D495/04

Abstract: Thienopyrazoles of formula I, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).

Abstract translation: 式I的噻吩并吡唑类，其制备方法，包含这些化合物的药物组合物及其在治疗能够通过抑制蛋白激酶（特别是白细胞介素-2诱导型酪氨酸激酶（ITK））调节的疾病状态的药物用途。

公开(公告)号：US08173682B2

公开(公告)日：2012-05-08

申请号：US11535127

申请日：2006-09-26

Applicant: Philip M. Weintraub ,  Paul R. Eastwood ,  Shujaath Mehdi ,  David W. Stefany ,  Kwon Yon Musick ,  Neil Moorcroft ,  Sungtaek Lim ,  John Z. Jiang ,  Hartmut Rutten ,  Stefan Peukert ,  Uwe Schwahn

Inventor： Philip M. Weintraub ,  Paul R. Eastwood ,  Shujaath Mehdi ,  David W. Stefany ,  Kwon Yon Musick ,  Neil Moorcroft ,  Sungtaek Lim ,  John Z. Jiang ,  Hartmut Rutten ,  Stefan Peukert ,  Uwe Schwahn

IPC: A61K31/4436 ,  C07D401/14

CPC classification number: C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract translation: 本发明涉及一系列式I的2,3,5-取代吡啶酮衍生物：其中R，R 1，R 2，R 3和R 4如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病 系统和心血管疾病。

公开(公告)号：US07405300B2

公开(公告)日：2008-07-29

申请号：US10933098

申请日：2004-09-01

Applicant: John Z. Jiang ,  Jack Roger Koehl ,  Shujaath Mehdi ,  Neil David Moorcroft ,  Kwon Yon Musick ,  Philip Marvin Weintraub ,  Paul Robert Eastwood

Inventor： John Z. Jiang ,  Jack Roger Koehl ,  Shujaath Mehdi ,  Neil David Moorcroft ,  Kwon Yon Musick ,  Philip Marvin Weintraub ,  Paul Robert Eastwood

IPC: C07D403/04 ,  C07D209/04

CPC classification number: C04B35/632 ,  A61K31/404 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  C07D209/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D471/04 ,  C07D487/08

Abstract: The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract translation: 本发明涉及一系列式I的取代的吲哚衍生物：其中R 1，R 2，R 2，R 3，R 3， X和Y如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病 系统和心血管疾病。

公开(公告)号：US20100056514A1

公开(公告)日：2010-03-04

申请号：US12411818

申请日：2009-03-26

Applicant: John Gerard JURCAK ,  Matthieu BARRAGUE ,  Timothy Alan GILLESPY ,  Michael Louis EDWARDS ,  Kwon Yon MUSICK ,  Philip Marvin WEINTRAUB ,  Yan DU ,  Ramalinga M. DHARANIPRAGADA ,  Ashfaq Ahmad PARKAR

Inventor： John Gerard JURCAK ,  Matthieu BARRAGUE ,  Timothy Alan GILLESPY ,  Michael Louis EDWARDS ,  Kwon Yon MUSICK ,  Philip Marvin WEINTRAUB ,  Yan DU ,  Ramalinga M. DHARANIPRAGADA ,  Ashfaq Ahmad PARKAR

IPC: A61K31/4162 ,  C07D495/04 ,  C07D413/14 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61P11/06

CPC classification number: C07D495/04

Abstract: Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).

Abstract translation: 噻吩并吡唑类，它们的制剂，包含这些化合物的药物组合物及其药物用途，用于治疗能够通过抑制蛋白激酶（特别是白细胞介素-2诱导型酪氨酸激酶（ITK））调节的疾病状态。