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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:US06579881B2
公开(公告)日:2003-06-17
申请号:US09859517
申请日:2001-05-18
申请人: Noritaka Kitazawa , Kohshi Ueno , Keiko Takahashi , Teiji Kimura , Atsushi Sasaki , Koki Kawano , Tadashi Okabe , Makoto Komatsu , Manabu Matsunaga , Atsuhiko Kubota
发明人: Noritaka Kitazawa , Kohshi Ueno , Keiko Takahashi , Teiji Kimura , Atsushi Sasaki , Koki Kawano , Tadashi Okabe , Makoto Komatsu , Manabu Matsunaga , Atsuhiko Kubota
IPC分类号: A61K31435
CPC分类号: C07D231/12 , C07D211/26 , C07D211/74 , C07D217/04 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D491/04 , C07D513/04
摘要: A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.
摘要翻译: 由下式表示的1,4-取代环状胺衍生物或其药理学上可接受的盐:其中A,B,C,D,T,Y和Z各自表示次甲基或氮键; R1,R2,R3,R4和R5各自表示取代基; n表示0或1〜3的整数, m表示0或1〜6的整数, p表示1〜3的整数。这些化合物具有5-羟色胺拮抗作用。 因此,它们在临床上可用作药物,特别是用于治疗,改善和预防痉挛性麻痹。 它们也可用作改善肌强直的中枢肌肉松弛剂。
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公开(公告)号:US07071201B2
公开(公告)日:2006-07-04
申请号:US09846259
申请日:2001-05-02
申请人: Noritaka Kitazawa , Kohshi Ueno , Keiko Takahashi , Teiji Kimura , Atsushi Sasaki , Koki Kawano , Tadashi Okabe , Makoto Komatsu , Manabu Matsunaga , Atsuhiko Kubota
发明人: Noritaka Kitazawa , Kohshi Ueno , Keiko Takahashi , Teiji Kimura , Atsushi Sasaki , Koki Kawano , Tadashi Okabe , Makoto Komatsu , Manabu Matsunaga , Atsuhiko Kubota
IPC分类号: A61K31/435 , A61K31/55 , C07D211/68 , C07D401/00
CPC分类号: C07D231/12 , C07D211/26 , C07D211/74 , C07D217/04 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D491/04 , C07D513/04
摘要: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
摘要翻译: 下式的新化合物:其中A,B,C,D,T,Y和Z代表每个次甲基或氮; R 1,R 2,R 3,R 4和R 5, 表示取代基; n表示0或1〜3的整数, m表示0或1〜6的整数, p表示1〜3的整数, 及其药理学上可接受的盐。 该化合物具有5-羟色胺拮抗作用,并且在临床上可用作药物,特别是用于治疗,改善和预防痉挛性麻痹或中枢肌肉松弛剂以改善肌强直。
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公开(公告)号:US06448243B1
公开(公告)日:2002-09-10
申请号:US09367227
申请日:1999-08-11
申请人: Noritaka Kitazawa , Kohshi Ueno , Keiko Takahashi , Teiji Kimura , Atsushi Sasaki , Koki Kawano , Tadashi Okabe , Makoto Komatsu , Manabu Matsunaga , Atsuhiko Kubota
发明人: Noritaka Kitazawa , Kohshi Ueno , Keiko Takahashi , Teiji Kimura , Atsushi Sasaki , Koki Kawano , Tadashi Okabe , Makoto Komatsu , Manabu Matsunaga , Atsuhiko Kubota
IPC分类号: C07D40100
CPC分类号: C07D231/12 , C07D211/26 , C07D211/74 , C07D217/04 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D491/04 , C07D513/04
摘要: A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
摘要翻译: 由下式表示的新的1,4-取代环胺衍生物或其药理学上可接受的盐:(其中A,B,C,D,T,Y和Z表示次甲基或氮; R1,R2,R3,R4 R5表示取代基,n表示0或1〜3的整数,m表示0或1〜6的整数,p表示1〜3的整数。)该化合物具有5-羟色胺拮抗作用,临床有用 作为药物,特别是用于治疗,改善和预防痉挛性麻痹或用于改善肌强直的中枢肌肉松弛剂。
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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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公开(公告)号:US5801180A
公开(公告)日:1998-09-01
申请号:US904260
申请日:1997-07-31
申请人: Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
发明人: Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
IPC分类号: C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04
CPC分类号: C07D235/06 , C07D215/42 , C07D231/12 , C07D233/56 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D239/96 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/12 , C07D471/04 , C07D491/04
摘要: The present invention provides a nitrogenous heterocyclic compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof which is useful for various ischemic heart diseases and the like: ##STR1## �in formula (1), ring A represents a benzene ring, a pyridine ring or a cyclohexane ring; ring B represents a pyridine ring, a pyrimidine ring or an imidazole ring, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent each a hydrogen atom, a halogen atom or a group such as a lower alkoxy group; R.sup.5 represents a group represented by the formula --NR.sup.11 R.sup.12 (wherein R.sup.11 and R.sup.12 represent each a hydrogen atom or a group such as a lower alkyl group) or the like; and R.sup.6 represents a group represented by the formula ##STR2## (wherein R.sup.19 represents a hydrogen atom, a lower alkyl group or the like; R.sup.20, R.sup.21 and R.sup.22 represent each a hydrogen atom, a halogen atom, a hydroxyl group or the like; and r represents 0 or an integer of 1 to 8)!.
摘要翻译: 本发明提供由以下通式(1)表示的含氮杂环化合物或其药理学上可接受的盐,其可用于各种缺血性心脏病等:(1)[式(1)中,环A 表示苯环,吡啶环或环己烷环; 环B表示吡啶环,嘧啶环或咪唑环,R1,R2,R3和R4分别表示氢原子,卤素原子或低级烷氧基等基团。 R5表示由式-NR11R12表示的基团(其中R11和R12各自表示氢原子或低级烷基等基团)等; R 6表示氢原子,低级烷基等,R 20,R 21,R 22分别表示氢原子,卤素原子,羟基等。 和r表示0或1〜8的整数)]。
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公开(公告)号:US5876981A
公开(公告)日:1999-03-02
申请号:US733232
申请日:1996-10-17
申请人: Chi-Huey Wong , Teiji Kimura
发明人: Chi-Huey Wong , Teiji Kimura
摘要: .beta.-Galactosides are synthesized using a transglycosylation reaction catalyzed by .beta.-galactosidase. The reaction employs a carbohydrate donor having a glycosidic leaving group attached to its anomeric carbon and an oxo group attached to the C-6 carbon. Strong leaving groups are preferred over weak leaving groups. The method can be carried out in aqueous solution without organic solvents to give the transglycosylation product in high yields and high regioselectivity. The synthesis of lactosamine using this methodology with galactose oxidase (GO) and .beta.-galactosidase has been accomplished. (FIG. 3). The methodology affords simple reaction conditions and minimal purification steps. In addition, the intermediate substrates maintain high stability, the process affords high yields and the enzymes and reagents employed are commercially available with high stability and low costs.
摘要翻译: β-半乳糖苷是使用由β-半乳糖苷酶催化的转糖基化反应合成的。 该反应采用具有与其端基异构碳连接的糖苷离去基团和与C-6碳连接的氧代基团的碳水化合物供体。 强离去基团优于弱离去基团。 该方法可以在没有有机溶剂的水溶液中进行,以高收率和高区域选择性得到转糖基化产物。 已经完成了使用该方法与半乳糖氧化酶(GO)和β-半乳糖苷酶合成乳糖胺。 (图3)。 该方法提供简单的反应条件和最小的纯化步骤。 此外,中间基材保持高稳定性,该方法提供高产率,所用的酶和试剂可以高稳定性和低成本商购。
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