公开(公告)号：US08178552B2

公开(公告)日：2012-05-15

申请号：US12536342

申请日：2009-08-05

Applicant: Piotr Pawel Graczyk ,  Paschalis Dimopoulos ,  Afzal Khan ,  Gurpreet Singh Bhatia ,  Christopher Neil Farthing

Inventor： Piotr Pawel Graczyk ,  Paschalis Dimopoulos ,  Afzal Khan ,  Gurpreet Singh Bhatia ,  Christopher Neil Farthing

IPC: C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  A01N43/42 ,  A61K31/44

CPC classification number: C07D471/04

Abstract: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.

Abstract translation: 本发明提供式（I）的化合物; 或其药学上可接受的盐，使用式（I）化合物或其药学上可接受的盐在抑制c-Jun N-末端激酶（JNK）活性中的用途以及在医药中的用途，特别是在治疗神经变性 疾病，炎性疾病和/或自身免疫性疾病。 本发明还提供制备所述式（I）化合物或其药学上可接受的盐以及含有它们的组合物的方法。

公开(公告)号：US07951802B2

公开(公告)日：2011-05-31

申请号：US12536354

申请日：2009-08-05

Applicant: Piotr Pawel Graczyk ,  Paschalis Dimopoulos ,  Christopher Neil Farthing ,  Gurpreet Singh Bhatia ,  Afzal Khan

Inventor： Piotr Pawel Graczyk ,  Paschalis Dimopoulos ,  Christopher Neil Farthing ,  Gurpreet Singh Bhatia ,  Afzal Khan

IPC: A61K31/535 ,  A61K31/497 ,  A61K31/44 ,  C07D413/14 ,  C07D401/14 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.

Abstract translation: 本发明提供式（I）的化合物; 或其药学上可接受的盐在抑制c-Jun N-末端激酶（JNK）活性，特别是在治疗神经变性疾病，炎性疾病和/或自身免疫疾病中。 本发明还提供了制备式（I）化合物或其药学上可接受的盐和含有它们的组合物的方法。

公开(公告)号：US07652137B2

公开(公告)日：2010-01-26

申请号：US10548162

申请日：2004-03-05

Applicant: Piotr Pawel Graczyk ,  Afzal Khan ,  Gurpreet Singh Bhatia

Inventor： Piotr Pawel Graczyk ,  Afzal Khan ,  Gurpreet Singh Bhatia

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.

Abstract translation: 本发明提供式（I）的新型取代的氮杂二氢吲哚中间体及其合成方法。 提供了用于制备5-取代的7-氮杂吲哚和5-取代的7-氮杂吲哚的新的取代的氮杂二氢吲哚中间体（I）。

公开(公告)号：US07645769B2

公开(公告)日：2010-01-12

申请号：US11499334

申请日：2006-08-04

Applicant: Afzal Khan ,  Darren Peter Medland ,  Gurpreet Singh Bhatia

Inventor： Afzal Khan ,  Darren Peter Medland ,  Gurpreet Singh Bhatia

IPC: C07D471/04 ,  A61K31/4375

CPC classification number: C07D471/04

Abstract: The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.

Abstract translation: 本发明提供新颖的式I化合物及其在抑制c-Jun N-末端激酶中的用途。 本发明进一步提供这些化合物在药物中的用途，特别是在预防和/或治疗与凋亡和/或炎症相关的神经变性疾病中的用途。

公开(公告)号：US08501733B2

公开(公告)日：2013-08-06

申请号：US13055830

申请日：2009-07-24

Applicant: Takafumi Motoki ,  Toshihiko Kaneko ,  Noboru Yamamoto ,  Afzal Khan

Inventor： Takafumi Motoki ,  Toshihiko Kaneko ,  Noboru Yamamoto ,  Afzal Khan

IPC: C07D513/10 ,  A61K31/547

CPC classification number: C07D513/10

Abstract: A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

Abstract translation: 由通式（I）表示的化合物或其药学上可接受的盐具有Abeta产生抑制作用或BACE1抑制作用，可用作由Abeta引起的神经变性疾病的预防或治疗剂，并以阿尔茨海默病 型痴呆症。

公开(公告)号：US08158620B2

公开(公告)日：2012-04-17

申请号：US12355154

申请日：2009-01-16

Applicant: Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Kunitoshi Takeda ,  Yoichi Kita ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

Inventor： Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Kunitoshi Takeda ,  Yoichi Kita ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

IPC: C07D513/02 ,  C07D279/08 ,  A61K31/542

CPC classification number: A61K31/542 ,  C07D279/08 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

Abstract translation: 由通式表示的化合物或其药学上可接受的盐或其溶剂化物，其中环A是C 6-14芳基等，L是-NReCO-等（其中Re是氢原子或 环）B是C 6-14芳基等，X是C 1-3亚烷基等，Y是单键等，Z是C 1-3亚烷基等，R 1 和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

公开(公告)号：US07432375B2

公开(公告)日：2008-10-07

申请号：US10548163

申请日：2004-03-05

Applicant: Piotr Graczyk ,  Afzal Khan ,  Gurpreet Bhatia ,  Yoichi Iimura

Inventor： Piotr Graczyk ,  Afzal Khan ,  Gurpreet Bhatia ,  Yoichi Iimura

IPC: C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC classification number: C07D471/04

Abstract: The present invention provides novel compounds of formula (I) and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.

Abstract translation: 本发明提供新的式（I）化合物及其在抑制c-Jun N-末端激酶中的用途。 本发明进一步提供这些化合物在药物中的用途，特别是在预防和/或治疗与凋亡和/或炎症相关的神经变性疾病中的用途。

公开(公告)号：USD523386S1

公开(公告)日：2006-06-20

申请号：US29242420

申请日：2005-11-10

Applicant: Afzal Khan

Designer： Afzal Khan

公开(公告)号：US08946210B2

公开(公告)日：2015-02-03

申请号：US13333238

申请日：2011-12-21

Applicant: Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Yoichi Kita ,  Kunitoshi Takeda ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

Inventor： Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Yoichi Kita ,  Kunitoshi Takeda ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

IPC: C07D239/14 ,  A61K31/5415

CPC classification number: A61K31/542 ,  C07D279/08 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

Abstract translation: 由通式表示的化合物或其药学上可接受的盐或其溶剂化物，其中环A是C 6-14芳基等，L是-NReCO-等（其中Re是氢原子或 环）B是C 6-14芳基等，X是C 1-3亚烷基等，Y是单键等，Z是C 1-3亚烷基等，R 1 和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

公开(公告)号：US20110152253A1

公开(公告)日：2011-06-23

申请号：US13055830

申请日：2009-07-24

Applicant: Takafumi Motoki ,  Toshihiko Kaneko ,  Noboru Yamamoto ,  Afzal Khan

Inventor： Takafumi Motoki ,  Toshihiko Kaneko ,  Noboru Yamamoto ,  Afzal Khan

IPC: A61K31/547 ,  C07D513/10 ,  A61P25/28

CPC classification number: C07D513/10

Abstract: A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

Abstract translation: 由通式（I）表示的化合物或其药学上可接受的盐具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。