公开(公告)号：US20090209755A1

公开(公告)日：2009-08-20

申请号：US12355154

申请日：2009-01-16

申请人： Yuichi SUZUKI ,  Takafumi MOTOKI ,  Toshihiko KANEKO ,  Mamoru TAKAISHI ,  Tasuku ISHIDA ,  Yoichi KITA ,  Kunitoshi TAKEDA ,  Noboru YAMAMOTO ,  Afzal KHAN ,  Paschalis DIMOPOULOS

发明人： Yuichi SUZUKI ,  Takafumi MOTOKI ,  Toshihiko KANEKO ,  Mamoru TAKAISHI ,  Tasuku ISHIDA ,  Yoichi KITA ,  Kunitoshi TAKEDA ,  Noboru YAMAMOTO ,  Afzal KHAN ,  Paschalis DIMOPOULOS

IPC分类号： C07D513/02 ,  C07D279/08

CPC分类号： A61K31/542 ,  C07D279/08 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： 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.

摘要翻译： 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Aβ生产抑制作用或BACE1抑制作用，可用作预防性 或由Abeta引起并以阿尔茨海默氏型痴呆为代表的神经变性疾病的治疗剂。

公开(公告)号：US20110112138A1

公开(公告)日：2011-05-12

申请号：US13005064

申请日：2011-01-12

申请人： Teiji KIMURA ,  Noritaka KITAZAWA ,  Toshihiko KANEKO ,  Nobuaki SATO ,  Koki KAWANO ,  Koichi ITO ,  Eriko DOI ,  Mamoru TAKAISHI ,  Takeo SASAKI ,  Takehiko MIYAGAWA ,  Hiroaki HAGIWARA ,  Takashi DOKO

发明人： Teiji KIMURA ,  Noritaka KITAZAWA ,  Toshihiko KANEKO ,  Nobuaki SATO ,  Koki KAWANO ,  Koichi ITO ,  Eriko DOI ,  Mamoru TAKAISHI ,  Takeo SASAKI ,  Takehiko MIYAGAWA ,  Hiroaki HAGIWARA ,  Takashi DOKO

IPC分类号： A61K31/444 ,  C07D471/04 ,  A61P25/28

CPC分类号： C07D403/10 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.

摘要翻译： 本发明提供由式（I）表示的化合物或其药理学上可接受的盐，其中Ar 1表示可被C 1-6烷基取代的咪唑基等，Ar 2表示可以 被C 1-6烷氧基等取代，X 1表示双键等，Het表示可被C 1-6烷基取代的咪唑基等，其作为式 由A＆Bgr引起的疾病的治疗或预防剂。

公开(公告)号：US20090281310A1

公开(公告)日：2009-11-12

申请号：US12497251

申请日：2009-07-02

申请人： Teiji KIMURA ,  Koki KAWANO ,  Eriko DOI ,  Noritaka KITAZAWA ,  Kogyoku SHIN ,  Takehiko MIYAGAWA ,  Toshihiko KANEKO ,  Koichi ITO ,  Mamoru TAKAISHI ,  Takeo SASAKI ,  Hiroaki HAGIWARA

发明人： Teiji KIMURA ,  Koki KAWANO ,  Eriko DOI ,  Noritaka KITAZAWA ,  Kogyoku SHIN ,  Takehiko MIYAGAWA ,  Toshihiko KANEKO ,  Koichi ITO ,  Mamoru TAKAISHI ,  Takeo SASAKI ,  Hiroaki HAGIWARA

IPC分类号： C07D413/14 ,  C07D233/61 ,  C07D403/12 ,  C07D413/12 ,  C07D401/10 ,  C07D233/60

CPC分类号： C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

摘要： The present invention relates to a process for preparing a compound of formula (6a): wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents shown below; Ar2 represents a pyridinyl group, a pyrimidinyl group or a phenyl group which may be substituted with 1 to 3 substituents; and R11 represents a group selected from certain substituents.

摘要翻译： 本发明涉及式（6a）化合物的制备方法：其中Ar 1表示可被1〜3个取代基取代的咪唑基， Ar 2表示吡啶基，嘧啶基或可被1〜3个取代基取代的苯基; R 11表示选自某些取代基的基团。

公开(公告)号：US20100168095A1

公开(公告)日：2010-07-01

申请号：US12721952

申请日：2010-03-11

申请人： Teiji KIMURA ,  Noritaka KITAZAWA ,  Toshihiko KANEKO ,  Nobuaki SATO ,  Koki KAWANO ,  Koichi ITO ,  Eriko DOI ,  Mamoru TAKAISHI ,  Takeo SASAKI ,  Takehiko MIYAGAWA ,  Hiroaki HAGIWARA ,  Takashi DOKO

发明人： Teiji KIMURA ,  Noritaka KITAZAWA ,  Toshihiko KANEKO ,  Nobuaki SATO ,  Koki KAWANO ,  Koichi ITO ,  Eriko DOI ,  Mamoru TAKAISHI ,  Takeo SASAKI ,  Takehiko MIYAGAWA ,  Hiroaki HAGIWARA ,  Takashi DOKO

IPC分类号： A61K31/4178 ,  A61K31/5383 ,  A61K31/4985 ,  A61K31/437 ,  A61K31/4196 ,  C07D498/04 ,  C07D487/04 ,  C07D471/04 ,  C07D403/10

CPC分类号： C07D403/10 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.

摘要翻译： 本发明提供由式（I）表示的化合物或其药理学上可接受的盐，其中Ar 1表示可被C 1-6烷基取代的咪唑基等，Ar 2表示可以 被C 1-6烷氧基等取代，X 1表示双键等，Het表示可被C 1-6烷基取代的咪唑基等，其作为式 由A＆Bgr引起的疾病的治疗或预防剂。