-
公开(公告)号:US09453000B2
公开(公告)日:2016-09-27
申请号:US12671873
申请日:2008-08-28
Applicant: 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
Inventor: 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: C07D471/04 , A61K31/437 , C07D487/04 , C07D498/04 , C07D403/10 , A61P25/28 , C07D403/04
CPC classification number: C07D403/10 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: 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:US08268848B2
公开(公告)日:2012-09-18
申请号:US13237205
申请日:2011-09-20
Applicant: Taro Terauchi , Ayumi Takemura , Takashi Doko , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Carsten Beuckmann , Yuji Kazuta
Inventor: Taro Terauchi , Ayumi Takemura , Takashi Doko , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Carsten Beuckmann , Yuji Kazuta
IPC: A01N43/54 , A61K31/505
CPC classification number: C07D401/12 , C07D239/34
Abstract: A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: wherein Q represents —CH— or a nitrogen atom, R1a and R1b each independently represent a C1-6 alkyl group and the like, R1c represents a hydrogen atom and the like, R2a, R2b, R2c and R2d each independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group and the like, R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom and the like, and R3d represents a hydrogen atom and the like.
Abstract translation: 由下式(A)表示的环丙烷化合物或其药学上可接受的盐具有食欲肽受体拮抗作用,因此具有治疗食欲肽受体拮抗作用有效的睡眠障碍的潜在用途,例如失眠症:其中Q表示 -CH-或氮原子,R1a和R1b各自独立地表示C1-6烷基等,R1c表示氢原子等,R2a,R2b,R2c和R2d各自独立地表示氢原子,卤素原子 C 1-6烷基等,R 3a,R 3b和R 3c各自独立地表示氢原子,卤素原子等,R 3d表示氢原子等。
-
公开(公告)号:US08048878B2
公开(公告)日:2011-11-01
申请号:US12403565
申请日:2009-03-13
Applicant: Teiji Kimura , Koki Kawano , Eriko Doi , Noritaka Kitazawa , Mamoru Takaishi , Koichi Ito , Toshihiko Kaneko , Takeo Sasaki , Takehiko Miyagawa , Hiroaki Hagiwara , Yu Yoshida
Inventor: Teiji Kimura , Koki Kawano , Eriko Doi , Noritaka Kitazawa , Mamoru Takaishi , Koichi Ito , Toshihiko Kaneko , Takeo Sasaki , Takehiko Miyagawa , Hiroaki Hagiwara , Yu Yoshida
IPC: C07D491/02 , C07D265/36 , C07D498/02 , C07D295/00 , A61K31/535 , A61K31/50 , A61K31/44 , A01N43/60
CPC classification number: C07D471/04 , C07D487/04
Abstract: 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.
Abstract translation: 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。
-
公开(公告)号:US20070117839A1
公开(公告)日:2007-05-24
申请号:US11594150
申请日:2006-11-08
Applicant: Teiji Kimura , Koki Kawano , Eriko Doi , Noritaka Kitazawa , Mamoru Takaishi , Koichi Ito , Toshihiko Kaneko , Takeo Sasaki , Takehiko Miyagawa , Hiroaki Hagiwara , Yu Yoshida
Inventor: Teiji Kimura , Koki Kawano , Eriko Doi , Noritaka Kitazawa , Mamoru Takaishi , Koichi Ito , Toshihiko Kaneko , Takeo Sasaki , Takehiko Miyagawa , Hiroaki Hagiwara , Yu Yoshida
IPC: C07D455/02 , A61K31/4745
CPC classification number: C07D471/04 , C07D487/04
Abstract: 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.
Abstract translation: 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代表可被1至3个取代基取代的苯基或吡啶基; R 1和R 2各自表示C 1-6烷基,羟基等; Z 1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,氧原子或亚氨基的取代基取代,所述取代基可以被选自取代基 A1组; 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:US20090062529A1
公开(公告)日:2009-03-05
申请号:US12200731
申请日:2008-08-28
Applicant: 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
Inventor: 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: C07D487/04 , C07D498/04
CPC classification number: C07D403/10 , C07D401/14 , C07D403/14 , C07D409/14
Abstract: 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.
Abstract translation: 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:US20120165339A1
公开(公告)日:2012-06-28
申请号:US13330972
申请日:2011-12-20
Applicant: Taro Terauchi , Ayumi Takemura , Yuji Kazuta , Fumihiro Ozaki , Takashi Doko , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Carsten Beuckmann
Inventor: Taro Terauchi , Ayumi Takemura , Yuji Kazuta , Fumihiro Ozaki , Takashi Doko , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Carsten Beuckmann
IPC: A61K31/501 , A61K31/444 , A61K31/443 , A61K31/4439 , A61K31/44 , A61K31/4196 , A61K31/427 , A61K31/428 , A61K31/42 , A61K31/4184 , A61K31/415 , A61K31/165 , C07D237/16 , C07D413/12 , C07D401/12 , C07D405/12 , C07D213/75 , C07D285/08 , C07D417/12 , C07D275/03 , C07D261/14 , C07D249/08 , C07D231/56 , C07D231/18 , C07C233/60 , A61P25/20 , A61K31/50
CPC classification number: C07D231/20 , C07C235/40 , C07D213/55 , C07D213/65 , C07D213/68 , C07D213/69 , C07D213/75 , C07D231/12 , C07D233/60 , C07D235/12 , C07D237/16 , C07D237/20 , C07D239/42 , C07D241/18 , C07D253/065 , C07D261/14 , C07D261/20 , C07D271/10 , C07D275/03 , C07D277/24 , C07D277/36 , C07D277/46 , C07D285/08 , C07D285/135 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.
Abstract translation: 由下式(I)表示的环丙烷衍生物或其药学上可接受的盐具有食欲素受体抑制作用,因此作为典型的例子,包括失眠引起的睡眠障碍或睡眠障碍引起的睡眠障碍或睡眠不适, :其中A1,A2和A3各自独立地表示芳基,杂环基等,R1,R2和R3各自独立地表示氢原子,C1-6烷基等,X表示氧原子或 类似,L表示键或类似物。
-
公开(公告)号:US20110065696A1
公开(公告)日:2011-03-17
申请号:US12950670
申请日:2010-11-19
Applicant: 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
Inventor: 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: A61K31/437 , C07D471/04 , C07D487/04 , C07D498/04 , A61K31/519 , A61K31/4439 , A61K31/5383 , A61P25/00 , A61P25/28
CPC classification number: C07D403/10 , C07D401/14 , C07D403/14 , C07D409/14
Abstract: 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.
Abstract translation: 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 A&BGR引起的疾病
-
公开(公告)号:US20110009619A1
公开(公告)日:2011-01-13
申请号:US12671873
申请日:2008-08-28
Applicant: 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
Inventor: 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: C07D487/04 , C07D471/04 , C07D498/04
CPC classification number: C07D403/10 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: 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.
Abstract translation: 公开了由式(I)表示的化合物或其药理学上可接受的盐,其作为由A&bgr诱导的疾病的治疗或预防剂是有效的,其中Ar1表示可被C1- 6烷基等; Ar 2表示可被C 1-6烷氧基取代的苯基等; X1表示双键等; Het表示可以被C 1-6烷基等取代的三唑基等。
-
公开(公告)号:US20120095031A1
公开(公告)日:2012-04-19
申请号:US13237205
申请日:2011-09-20
Applicant: Taro Terauchi , Ayumi Takemura , Takashi Doko , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Carsten Beuckmann , Yuji Kazuta
Inventor: Taro Terauchi , Ayumi Takemura , Takashi Doko , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Carsten Beuckmann , Yuji Kazuta
IPC: A61K31/506 , A61P25/20 , A61K31/505 , C07D401/12 , C07D239/34
CPC classification number: C07D401/12 , C07D239/34
Abstract: A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: wherein Q represents —CH— or a nitrogen atom, R1a and R1b each independently represent a C1-6 alkyl group and the like, R1c represents a hydrogen atom and the like, R2a, R2b, R2c and R2d each independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group and the like, R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom and the like, and R3d represents a hydrogen atom and the like.
Abstract translation: 由下式(A)表示的环丙烷化合物或其药学上可接受的盐具有食欲肽受体拮抗作用,因此具有治疗食欲肽受体拮抗作用有效的睡眠障碍的潜在用途,例如失眠症:其中Q表示 -CH-或氮原子,R1a和R1b各自独立地表示C1-6烷基等,R1c表示氢原子等,R2a,R2b,R2c和R2d各自独立地表示氢原子,卤素原子 C 1-6烷基等,R 3a,R 3b和R 3c各自独立地表示氢原子,卤素原子等,R 3d表示氢原子等。
-
公开(公告)号:US07935815B2
公开(公告)日:2011-05-03
申请号:US12200731
申请日:2008-08-28
Applicant: 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
Inventor: 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: C07D491/00 , C07D513/00 , C07D515/00 , C07D265/36 , C07D498/02 , C07D487/00 , C07D513/02 , C07D515/02 , C07D401/00
CPC classification number: C07D403/10 , C07D401/14 , C07D403/14 , C07D409/14
Abstract: 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.
Abstract translation: 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 A&BGR引起的疾病
-
-
-
-
-
-
-
-
-