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公开(公告)号:US20110009619A1
公开(公告)日:2011-01-13
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: C07D487/04 , C07D471/04 , C07D498/04
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.
摘要翻译: 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。
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公开(公告)号:US07935815B2
公开(公告)日:2011-05-03
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: C07D491/00 , C07D513/00 , C07D515/00 , C07D265/36 , C07D498/02 , C07D487/00 , C07D513/02 , C07D515/02 , C07D401/00
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 A&BGR引起的疾病
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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
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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.
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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。
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公开(公告)号:US20090048213A1
公开(公告)日:2009-02-19
申请号:US11878556
申请日:2007-07-25
申请人: Teiji Kimura , Koki Kawano , Noritaka Kitazawa , Nobuaki Sato , Toshihiko Kaneko , Koichi Ito , Mamoru Takaishi , Ikuo Kushida
发明人: Teiji Kimura , Koki Kawano , Noritaka Kitazawa , Nobuaki Sato , Toshihiko Kaneko , Koichi Ito , Mamoru Takaishi , Ikuo Kushida
IPC分类号: A61K31/675 , C07D401/02 , C07F9/06 , A61K31/5377 , C07D221/04 , A61K31/5365 , A61P25/28 , C07D498/04 , A61K31/4439 , A61K31/435 , C07D413/02 , A61K31/454
CPC分类号: C07D401/10 , C07F9/65583 , C07F9/6561
摘要: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
摘要翻译: 本发明提供了最合适的肉桂酰胺化合物的前药。 前药由式(I)表示,其中R a和R b各自表示C 1-6烷基等; Xa表示甲氧基或氟原子; Y表示膦酰基等; A表示环状内酰胺衍生物。
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公开(公告)号:US07737141B2
公开(公告)日:2010-06-15
申请号:US11878556
申请日:2007-07-25
申请人: Teiji Kimura , Koki Kawano , Noritaka Kitazawa , Nobuaki Sato , Toshihiko Kaneko , Koichi Ito , Mamoru Takaishi , Ikuo Kushida
发明人: Teiji Kimura , Koki Kawano , Noritaka Kitazawa , Nobuaki Sato , Toshihiko Kaneko , Koichi Ito , Mamoru Takaishi , Ikuo Kushida
IPC分类号: A61K31/535 , A61K31/44 , C07D413/14 , C07D221/02
CPC分类号: C07D401/10 , C07F9/65583 , C07F9/6561
摘要: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
摘要翻译: 本发明提供了最合适的肉桂酰胺化合物的前药。 前药由式(I)表示,其中R a和R b各自表示C 1-6烷基等; Xa表示甲氧基或氟原子; Y表示膦酰基等; A表示环状内酰胺衍生物。
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公开(公告)号:US06825192B1
公开(公告)日:2004-11-30
申请号:US09913444
申请日:2001-08-15
申请人: Koichi Ito , Noritaka Kitazawa , Satoshi Nagato , Akiharu Kajiwara , Tatsuto Fukushima , Shinji Hatakeyama , Takahisa Hanada , Masataka Ueno , Kohshi Ueno , Koki Kawano
发明人: Koichi Ito , Noritaka Kitazawa , Satoshi Nagato , Akiharu Kajiwara , Tatsuto Fukushima , Shinji Hatakeyama , Takahisa Hanada , Masataka Ueno , Kohshi Ueno , Koki Kawano
IPC分类号: C07D25306
CPC分类号: C07D271/113 , A61K31/53 , A61K31/5395 , A61K31/549 , C07D249/12 , C07D285/16 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要: The present invention provides a hetrodiazinon compound having 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, which is represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A represents O, S or a group represented by the formula NR3 (wherein R3 represents hydrogen atom or a lower alkyl group); R1 and R2 are the same as or different from each other and each represents an optionally substituted (hetero)aryl group etc.; and R4 and R5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, a (hetero)aryl group etc.
摘要翻译: 本发明提供由下式(I)表示的具有2-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体拮抗作用的hetrodiazinon化合物,其药理学上可接受的盐或水合物 其中A表示O,S或由式NR 3表示的基团(其中R 3表示氢原子或低级烷基); R 1和R 2相同或不同 彼此各自表示任选取代的(杂)芳基等; R 4和R 5彼此相同或不同,各自表示氢原子,羟基,卤素原子,腈基,硝基,低级烷基,(杂)芳基等。
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公开(公告)号:US06737425B1
公开(公告)日:2004-05-18
申请号:US09743358
申请日:2001-01-29
申请人: Noboru Yamamoto , Makoto Komatsu , Yuichi Suzuki , Koki Kawano , Teiji Kimura , Koichi Ito , Satoshi Nagato , Yoshihiko Norimine , Tetsuhiro Niidome , Tetsuyuki Teramoto , Yoichi Iimura , Shinji Hatakeyama
发明人: Noboru Yamamoto , Makoto Komatsu , Yuichi Suzuki , Koki Kawano , Teiji Kimura , Koichi Ito , Satoshi Nagato , Yoshihiko Norimine , Tetsuhiro Niidome , Tetsuyuki Teramoto , Yoichi Iimura , Shinji Hatakeyama
IPC分类号: A61K31497
CPC分类号: C07D213/64 , C07D213/57 , C07D215/20 , C07D217/02 , C07D233/54 , C07D239/34 , C07D239/80 , C07D295/15 , C07D317/64 , C07D333/24 , C07D333/38
摘要: The invention provides an N,N-substituted cyclic amine compound represented by the following formula (VIII): wherein A represents an aryl group etc.; E represents a group represented by the formula —CO— or a group represented by the formula —CHOH—; G represents an oxygen atom etc.; J represents an aryl group which may be substituted; R1 represents a lower alkyl group etc.; Alk represents a linear or branched lower alkylene group; n, v, w, x and y are independent of each other and each represents 0 or 1; and p represents 2 or 3, or a pharmacologically acceptable salt thereof. The compound of the present invention or a salt thereof is effective to treat a disease against which calcium antagonism is effective. The disease may include acute ischemic stroke, cerebral apoplexy, cerebral infarction, head trauma, cerebral nerve cell death, Alzheimer disease, Parkinson disease, amyotrophic lateral sclerosis, Huntington disease, cerebral circulatory metabolism disturbance, cerebral function disturbance, pain, spasm, schizophrenia, migraine, epilepsy, maniac-depressive psychosis, nerve degenerative diseases, cerebral ischemia, AIDS dementia complications, edema, anxiety disorder (generalized anxiety disorder) and diabetic neuropathy.
摘要翻译: 本发明提供由下式(VIII)表示的N,N-取代的环胺化合物:其中A表示芳基等; E表示由式-CO-表示的基团或由式-CHOH-表示的基团; G表示氧原子等。 J表示可被取代的芳基; R 1表示低级烷基等。 Alk表示直链或支链低级亚烷基; n,v,w,x和y彼此独立,各自表示0或1; 和p表示2或3,或其药理学上可接受的盐。 本发明的化合物或其盐可有效治疗钙拮抗作用有效的疾病。 该疾病可能包括急性缺血性脑卒中,脑中风,脑梗塞,头部创伤,脑神经细胞死亡,阿尔茨海默病,帕金森病,肌萎缩性侧索硬化,亨廷顿病,脑循环代谢障碍,脑功能障碍,疼痛,痉挛,精神分裂症, 偏头痛,癫痫,疯子抑郁精神病,神经退行性疾病,脑缺血,艾滋病痴呆并发症,水肿,焦虑症(广泛性焦虑症)和糖尿病性神经病变。
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公开(公告)号:US06667412B1
公开(公告)日:2003-12-23
申请号:US09914349
申请日:2001-08-27
申请人: Yuichi Suzuki , Noboru Yamamoto , Koki Kawano , Teiji Kimura , Koichi Ito , Satoshi Nagato , Yoshihiko Norimine , Yoichi Iimura
发明人: Yuichi Suzuki , Noboru Yamamoto , Koki Kawano , Teiji Kimura , Koichi Ito , Satoshi Nagato , Yoshihiko Norimine , Yoichi Iimura
IPC分类号: C07C25536
CPC分类号: C07D295/145 , C07C255/36 , C07C255/41 , C07D295/14
摘要: The present invention provides a novel nitrile compound useful as an intermediate for the production of, for example, N,N-substituted cyclic amine derivatives or phenylacetonitrile derivatives that are useful as a medicine. Specifically it provides a nitrile carboxylic acid compound, nitrile ester compound and nitrile alcohol compound. That is, it provides a nitrile compound represented by the following formula (I): wherein R1 and R2 means substituents; m means 0 or an integer of from 1 to 6; n means 0 or an integer of from 1 to 5; and R3 means carboxyl group, a lower alkoxycarbonyl group or hydroxymethyl group.
摘要翻译: 本发明提供了可用作制备例如可用作药物的N,N-取代的环胺衍生物或苯乙腈衍生物的中间体的新型腈化合物。 具体地说,它提供了一种腈羧酸化合物,腈酯化合物和腈醇化合物。 也就是说,它提供由下式(I)表示的腈化合物:其中R 1和R 2表示取代基; m表示0或1〜6的整数; n表示0或1至5的整数; R 3表示羧基,低级烷氧基羰基或羟甲基。
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