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：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：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：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：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：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：US20090181945A1

公开(公告)日：2009-07-16

申请号：US12403565

申请日：2009-03-13

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

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

IPC分类号： A61K31/4375 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/437 ,  A61K31/55 ,  A61K31/4178 ,  A61K31/5365 ,  A61K31/4985 ,  A61P25/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing Aβ40 and Aβ42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ such as Alzheimer's disease or Down's syndrome.

摘要翻译： 本发明涉及一种新型的两种环状肉桂酰胺化合物和包含该化合物作为活性成分的药剂。 由通式（I）表示的两种环状肉桂酰胺化合物：其中表示单键或双键; Ar 1表示可被1〜3个取代基取代的苯基或吡啶基; R1和R2各自表示C1-6烷基，羟基等; Z1表示亚甲基或亚乙烯基，其可以被1或2个选自取代基组A1，氧原子或可被选自取代基组A1的取代基取代的亚氨基取代基取代; 并且p，q和r各自表示0〜2的整数，其具有降低Abeta40和Abeta42产生的作用，因此特别可用作由Abeta如阿尔茨海默病或阿尔茨海默病引起的神经变性疾病的预防或治疗剂 唐氏综合症。

公开(公告)号：US20080070902A1

公开(公告)日：2008-03-20

申请号：US11596723

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 ,  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： A61K31/4164 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/535 ,  A61K31/55 ,  A61P25/28 ,  A61P3/00 ,  A61P43/00 ,  C07D233/66 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

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.

摘要翻译： 本发明涉及由式（I）表示的化合物：（其中Ar 1代表可被1至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至3个取代基取代的苯基; X 1表示（1）-C≡C-或（2）双键等，其可以 被取代; R 1和R 2表示例如可以被取代的C 1-6烷基或C 3-8环烷基）或其药理学上可接受的盐 以及作为药剂的用途。

公开(公告)号：US08048878B2

公开(公告)日：2011-11-01

申请号：US12403565

申请日：2009-03-13

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

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

IPC分类号： C07D491/02 ,  C07D265/36 ,  C07D498/02 ,  C07D295/00 ,  A61K31/535 ,  A61K31/50 ,  A61K31/44 ,  A01N43/60

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing Aβ40 and Aβ42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ such as Alzheimer's disease or Down's syndrome.

摘要翻译： 本发明涉及一种新型的两种环状肉桂酰胺化合物和包含该化合物作为活性成分的药剂。 由通式（I）表示的两个环状肉桂酰胺化合物：其中表示单键或双键; Ar 1表示可被1〜3个取代基取代的苯基或吡啶基; R1和R2各自表示C1-6烷基，羟基等; Z1表示亚甲基或亚乙烯基，其可以被1或2个选自取代基组A1，氧原子或可被选自取代基组A1的取代基取代的亚氨基取代基取代; p，q和r各自表示0〜2的整数，其具有降低A＆bgr 40和A＆bgr 42生成的效果，因此特别可用作由A＆bgr引起的神经变性疾病的预防或治疗剂。 如阿尔茨海默病或唐氏综合症。