公开(公告)号：US07618960B2

公开(公告)日：2009-11-17

申请号：US11594130

申请日：2006-11-08

申请人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Mamoru Takaishi ,  Koichi Ito ,  Toshihiko Kaneko ,  Takeo Sasaki ,  Nobuaki Sato ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Mamoru Takaishi ,  Koichi Ito ,  Toshihiko Kaneko ,  Takeo Sasaki ,  Nobuaki Sato ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D498/04 ,  A61K31/5375

CPC分类号： C07D413/10 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

摘要： The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R1, R2, R3, and R4 are the same or different and each represent a hydrogen atom or a C1-6 alkyl group; X1 represents a C1-6 alkylene group that may be substituted; Xa represents a methoxy group or a fluorine atom; Xb represents an oxygen atom or a methylene group, provided that Xb is only an oxygen atom when Xa is a methoxy group; and Ar1 represents an aryl group, pyridinyl group, aryloxy group, or pyridinyloxy group that may have a substituent such as a halogen atom; and to use of the compound or salt as a pharmaceutical agent.

摘要翻译： 本发明涉及由式（I）表示的化合物或其药理学上可接受的盐，其中R 1，R 2，R 3和R 4相同或不同，各自表示氢原子或C 1-6烷基; X 1表示可以被取代的C 1-6亚烷基; Xa表示甲氧基或氟原子; Xb表示氧原子或亚甲基，条件是当Xa为甲氧基时Xb仅为氧原子; Ar 1表示可以具有卤素原子等取代基的芳基，吡啶基，芳氧基或吡啶氧基; 并使用化合物或盐作为药剂。

公开(公告)号：US20090062529A1

公开(公告)日：2009-03-05

申请号：US12200731

申请日：2008-08-28

申请人： Teiji KIMURA ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji KIMURA ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D487/04 ,  C07D498/04

CPC分类号： C07D403/10 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

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

摘要翻译： 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表示可被取代的苯基等 具有C 1-6烷氧基，X 1表示双键等，Het表示可以被C 1-6烷基等取代的三唑基等，作为治疗或预防药物是有效的 由Abeta引起的疾病

公开(公告)号：US20070219181A1

公开(公告)日：2007-09-20

申请号：US11715440

申请日：2007-03-08

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： A61K31/553 ,  A61K31/55 ,  A61K31/5383 ,  A61K31/498 ,  A61K31/506

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烷氧基等取代的苯基，X 1表示双键等，Het表示 可被C 1-6烷基取代的咪唑基等作为由Aβ引起的疾病的治疗或预防剂有效。

公开(公告)号：US09453000B2

公开(公告)日：2016-09-27

申请号：US12671873

申请日：2008-08-28

申请人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  C07D498/04 ,  C07D403/10 ,  A61P25/28 ,  C07D403/04

CPC分类号： C07D403/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

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

公开(公告)号：US08008293B2

公开(公告)日：2011-08-30

申请号：US12522281

申请日：2008-02-27

申请人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Mamoru Takaishi ,  Koichi Ito ,  Toshihiko Kaneko ,  Takeo Sasaki ,  Nobuaki Sato ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Mamoru Takaishi ,  Koichi Ito ,  Toshihiko Kaneko ,  Takeo Sasaki ,  Nobuaki Sato ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D498/04 ,  A61K31/5375

CPC分类号： C07D498/04

摘要： The present invention relates to a compound represented by formula (I): wherein R1 represents a C1-3 alkyl group, R2 represents a hydrogen atom or a C1-3 alkyl group, Ar represents a phenyl group or the like which may be substituted with 1 to 3 substituents, X represents an oxygen atom or the like, n and m are the same or different and integers of 0 to 2, or a pharmacologically acceptable salt, and use thereof as a medicament.

摘要翻译： 本发明涉及由式（I）表示的化合物：其中R1表示C1-3烷基，R2表示氢原子或C1-3烷基，Ar表示可被基团取代的苯基等 1〜3个取代基，X表示氧原子等，n和m相同或不同，为0〜2的整数，或药理学上可接受的盐及其作为药物的用途。

公开(公告)号：US07973033B2

公开(公告)日：2011-07-05

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： C07D471/04 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/5025

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.

公开(公告)号：US20100105904A1

公开(公告)日：2010-04-29

申请号：US12301428

申请日：2007-05-18

申请人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Takehiko Miyagawa ,  Nobuaki Sato ,  Toshihiko Kaneko ,  Kogyoku Shin ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Takehiko Miyagawa ,  Nobuaki Sato ,  Toshihiko Kaneko ,  Kogyoku Shin ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Hiroaki Hagiwara

IPC分类号： C07D233/64 ,  C07D405/12 ,  C07D403/10

CPC分类号： C07D233/64 ,  C07D249/06 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/10 ,  C07D405/12

摘要： Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (In the formula, Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group; X1 represents a single bond; R1 and R2 respectively represent a C1-6 alkyl group or the like which may be substituted with a substituent such as a 5- to 14-membered aromatic heterocyclic group; and R3 represents a hydrogen atom or the like.)

摘要翻译： 公开了由下式（I）表示的化合物或其药理学上可接受的盐。 还公开了化合物或盐作为药物产品的用途。 （式中，Ar 1表示可被C 1-6烷基取代的咪唑基，Ar 2表示可被C 1-6烷氧基取代的苯基，X 1表示单键; R 1，R 2分别表示 可以被诸如5至14元芳族杂环基团的取代基取代的C 1-6烷基等; R 3表示氢原子等。

公开(公告)号：US20070117798A1

公开(公告)日：2007-05-24

申请号：US11594130

申请日：2006-11-08

申请人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Mamoru Takaishi ,  Koichi Ito ,  Toshihiko Kaneko ,  Takeo Sasaki ,  Nobuaki Sato ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Mamoru Takaishi ,  Koichi Ito ,  Toshihiko Kaneko ,  Takeo Sasaki ,  Nobuaki Sato ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： A61K31/538 ,  A61K31/5377 ,  A61K31/454 ,  C07D413/04

CPC分类号： C07D413/10 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

摘要： The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R1, R2, R3, and R4 are the same or different and each represent a hydrogen atom or a C1-6 alkyl group; X1 represents a C1-6 alkylene group that may be substituted; Xa represents a methoxy group or a fluorine atom; Xb represents an oxygen atom or a methylene group, provided that Xb is only an oxygen atom when Xa is a methoxy group; and Ar1 represents an aryl group, pyridinyl group, aryloxy group, or pyridinyloxy group that may have a substituent such as a halogen atom; and to use of the compound or salt as a pharmaceutical agent.

摘要翻译： 本发明涉及由式（I）表示的化合物或其药理学上可接受的盐，其中R 1，R 2，R 3， SUP>和R 4相同或不同，各自表示氢原子或C 1-6烷基; X 1表示可以被取代的C 1-6亚烷基; X a a表示甲氧基或氟原子; X B表示氧原子或亚甲基，条件是当X a a为甲氧基时，X B b仅为氧原子; 和Ar 1表示可以具有卤素原子等取代基的芳基，吡啶基，芳氧基或吡啶氧基; 并使用化合物或盐作为药剂。

公开(公告)号：US07687640B2

公开(公告)日：2010-03-30

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： C07D233/56 ,  A01N43/50

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：US07667041B2

公开(公告)日：2010-02-23

申请号：US11136355

申请日：2005-05-25

申请人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Kogyoku Shin ,  Takehiko Miyagawa ,  Toshihiko Kaneko ,  Koichi Ito ,  Mamoru Takaishi ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Koki Kawano ,  Eriko Doi ,  Noritaka Kitazawa ,  Kogyoku Shin ,  Takehiko Miyagawa ,  Toshihiko Kaneko ,  Koichi Ito ,  Mamoru Takaishi ,  Hiroaki Hagiwara

IPC分类号： C07D401/00 ,  A61K31/54

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 compound represented by Formula (I): (wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar2 represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X1 represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R1 and R2 represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted) or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be provided.

摘要翻译： 本发明涉及由式（I）表示的化合物：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; X1表示（1）-C≡C-或（2）可被取代的双键等; R 1和R 2表示例如C 1-6烷基或C 3-8环烷基， 可以被取代）或其药理学上可接受的盐及其作为药剂的用途。 本发明的目的是找到由A＆Bgr引起的疾病的治疗或预防剂。 根据本发明，由A＆Bgr引起的疾病的治疗或预防剂; 可以提供。