公开(公告)号：US20080139556A1

公开(公告)日：2008-06-12

申请号：US11567421

申请日：2006-12-06

Applicant: Raymond W. KOSLEY ,  Bruce Baron ,  Patrick Jimonet ,  John G. Jurcak ,  Stephen J. Shimshock ,  Xu-yang Zhao ,  Rosy Sher ,  Paul J. Mueller ,  Jennifer Beall ,  Matthieu Barrague ,  Joseph W. Guiles

Inventor： Raymond W. KOSLEY ,  Bruce Baron ,  Patrick Jimonet ,  John G. Jurcak ,  Stephen J. Shimshock ,  Xu-yang Zhao ,  Rosy Sher ,  Paul J. Mueller ,  Jennifer Beall ,  Matthieu Barrague ,  Joseph W. Guiles

IPC: A61K31/5377 ,  C07D221/00 ,  C07D295/00 ,  A61K31/445 ,  A61P25/00 ,  A61K31/496 ,  A61K31/453 ,  A61K31/454

CPC classification number: C07D401/12 ,  C07D211/96 ,  C07D405/12 ,  C07D409/14

Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.

Abstract translation: 公开了一种用于结合FKBP蛋白的组合物，以及治疗与神经元变性相关的病症的方法，其中所述组合物包含式I化合物，其中R 1，R 2，R 2 R 3和X如本文所定义。

公开(公告)号：US07777042B2

公开(公告)日：2010-08-17

申请号：US11567421

申请日：2006-12-06

Applicant: Raymond W. Kosley, Jr. ,  Bruce Baron ,  Patrick Jimonet ,  John G. Jurcak ,  Stephen J. Shimshock ,  Xu-Yang Zhao ,  Rosy Sher ,  Paul J. Mueller ,  Jennifer Beall ,  Matthieu Barrague ,  Joseph W. Guiles

Inventor： Raymond W. Kosley, Jr. ,  Bruce Baron ,  Patrick Jimonet ,  John G. Jurcak ,  Stephen J. Shimshock ,  Xu-Yang Zhao ,  Rosy Sher ,  Paul J. Mueller ,  Jennifer Beall ,  Matthieu Barrague ,  Joseph W. Guiles

IPC: A61K31/535 ,  C07D211/30

CPC classification number: C07D401/12 ,  C07D211/96 ,  C07D405/12 ,  C07D409/14

Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.

Abstract translation: 公开了一种用于结合FKBP蛋白质的组合物以及治疗与神经元变性相关的病症的方法，其中所述组合物包含式I化合物，其中R 1，R 2，R 3和X如本文所定义。

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。

公开(公告)号：US08354405B2

公开(公告)日：2013-01-15

申请号：US12647059

申请日：2009-12-24

Applicant: Antonio Almario Garcia ,  Matthieu Barrague ,  Philippe Burnier ,  Cécile Enguehard ,  Zhongli Gao ,  Pascal George ,  Alain Gueiffier ,  Adrien Tak Li ,  Frédéric Puech ,  Roy Vaz ,  Qiuxia Zhao

Inventor： Antonio Almario Garcia ,  Matthieu Barrague ,  Philippe Burnier ,  Cécile Enguehard ,  Zhongli Gao ,  Pascal George ,  Alain Gueiffier ,  Adrien Tak Li ,  Frédéric Puech ,  Roy Vaz ,  Qiuxia Zhao

IPC: C07D487/04 ,  C07D237/00 ,  C07D413/14 ,  A61K31/5025 ,  A61K31/5355 ,  A61P25/30 ,  A61P25/00

CPC classification number: C07D487/04

Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.

Abstract translation: 本发明涉及对应于通式（I）的6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物：其中R2，R3，R7，R8，A，L和B 如本文所定义。 还公开了其制备方法及其治疗用途。

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：US20130012516A1

公开(公告)日：2013-01-10

申请号：US13617678

申请日：2012-09-14

Applicant: Antonio ALMARIO GARCIA ,  Matthieu BARRAGUE ,  Philippe BURNIER ,  Cécile ENGUEHARD ,  Zhongli GAO ,  Pascal GEORGE ,  Alain GUEIFFIER ,  Adrien Tak LI ,  Frédéric PUACH ,  Roy VAZ ,  Qiuxia ZHAO

Inventor： Antonio ALMARIO GARCIA ,  Matthieu BARRAGUE ,  Philippe BURNIER ,  Cécile ENGUEHARD ,  Zhongli GAO ,  Pascal GEORGE ,  Alain GUEIFFIER ,  Adrien Tak LI ,  Frédéric PUACH ,  Roy VAZ ,  Qiuxia ZHAO

IPC: A61K31/5025 ,  A61P25/30 ,  A61P25/20 ,  C07D487/04 ,  C07D471/10

CPC classification number: C07D487/04

Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.

Abstract translation: 本发明涉及对应于通式（I）的6-环氨基-3-（吡啶-4-基）咪唑并[ⅰ，2-b]哒嗪衍生物：其中R2，R3，R7，R8，A，L和B 如本文所定义。 还公开了其制备方法及其治疗用途。

公开(公告)号：US20100179154A1

公开(公告)日：2010-07-15

申请号：US12647059

申请日：2009-12-24

Applicant: Antonio ALMARIO GARCIA ,  Matthieu BARRAGUE ,  Philippe BURNIER ,  Cécile ENGUEHARD-GUEIFFIER ,  Zhongli GAO ,  Pascal GEORGE ,  Alain GUEIFFIER ,  Adrien Tak LI ,  Frédéric PEUCH ,  Roy VAZ ,  Qiuxia ZHAO

Inventor： Antonio ALMARIO GARCIA ,  Matthieu BARRAGUE ,  Philippe BURNIER ,  Cécile ENGUEHARD-GUEIFFIER ,  Zhongli GAO ,  Pascal GEORGE ,  Alain GUEIFFIER ,  Adrien Tak LI ,  Frédéric PEUCH ,  Roy VAZ ,  Qiuxia ZHAO

IPC: A61K31/5025 ,  C07D487/04 ,  A61P25/00 ,  A61P25/30

CPC classification number: C07D487/04

Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.

Abstract translation: 本发明涉及对应于通式（I）的6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物：其中R2，R3，R7，R8，A，L和B 如本文所定义。 还公开了其制备方法及其治疗用途。

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：US20070254937A1

公开(公告)日：2007-11-01

申请号：US11368566

申请日：2006-03-06

Applicant: John Jurcak ,  Matthieu Barrague ,  Timothy Gillespy ,  Michael Edwards ,  Kwon Musick ,  Philip Weintraub ,  Yan Du ,  Ramalinga Dharanipragada ,  Ashfaq Parkar

Inventor： John Jurcak ,  Matthieu Barrague ,  Timothy Gillespy ,  Michael Edwards ,  Kwon Musick ,  Philip Weintraub ,  Yan Du ,  Ramalinga Dharanipragada ,  Ashfaq Parkar

IPC: A61K31/415 ,  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。