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

公开(公告)号：US07667041B2

公开(公告)日：2010-02-23

申请号：US11136355

申请日：2005-05-25

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

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

IPC: C07D401/00 ,  A61K31/54

CPC classification number: C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090203697A1

公开(公告)日：2009-08-13

申请号：US12301421

申请日：2007-05-18

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

Inventor： 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: A61K31/5377 ,  A61K31/4353 ,  A61K31/4439 ,  C07D413/10 ,  C07D455/02 ,  C07D401/10 ,  C07D413/14 ,  C07D401/14

CPC classification number: C07D249/08 ,  C07D401/10 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14 ,  C07D471/04

Abstract: 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 a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like; Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group or the like; X1 represents —CR3═CR4— (wherein R3 and R4 respectively represent a C1-6 alkyl group or the like); and R1 and R2 respectively represent a C1-6 alkyl group or the like.)

Abstract translation: 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烷基等取代的三唑基等，Ar 2表示可被C 1-6烷氧基等取代的苯基等） ; X1表示-CR3-CR4-（其中R3和R4分别表示C1-6烷基等），R1和R2分别表示C1-6烷基等）。

公开(公告)号：US20090181945A1

公开(公告)日：2009-07-16

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

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：US20080207900A1

公开(公告)日：2008-08-28

申请号：US12037315

申请日：2008-02-26

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

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

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: 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.

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

公开(公告)号：US20080070902A1

公开(公告)日：2008-03-20

申请号：US11596723

申请日：2005-05-25

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

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

IPC: 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 classification number: C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

Abstract: 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.

Abstract translation: 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：US06579881B2

公开(公告)日：2003-06-17

申请号：US09859517

申请日：2001-05-18

Applicant: Noritaka Kitazawa ,  Kohshi Ueno ,  Keiko Takahashi ,  Teiji Kimura ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Makoto Komatsu ,  Manabu Matsunaga ,  Atsuhiko Kubota

Inventor： Noritaka Kitazawa ,  Kohshi Ueno ,  Keiko Takahashi ,  Teiji Kimura ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Makoto Komatsu ,  Manabu Matsunaga ,  Atsuhiko Kubota

IPC: A61K31435

CPC classification number: C07D231/12 ,  C07D211/26 ,  C07D211/74 ,  C07D217/04 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D491/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5876981A

公开(公告)日：1999-03-02

申请号：US733232

申请日：1996-10-17

Applicant: Chi-Huey Wong ,  Teiji Kimura

Inventor： Chi-Huey Wong ,  Teiji Kimura

IPC: C12P19/14 ,  C12P19/26 ,  C12N9/38 ,  C12P19/04 ,  C12P19/18

CPC classification number: C12P19/26 ,  C12P19/14

Abstract: .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.

Abstract translation: 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。

公开(公告)号：US4408372A

公开(公告)日：1983-10-11

申请号：US198726

申请日：1980-10-20

Applicant: Teiji Kimura ,  Shigeru Kimura

Inventor： Teiji Kimura ,  Shigeru Kimura

IPC: F16C11/06 ,  F16B17/00 ,  F16B21/07 ,  H04R1/02 ,  A44B21/00

CPC classification number: F16B21/073 ,  Y10T24/45775

Abstract: A coupler for joining two objects comprises an insertion member attached fast to one of the objects and a reception member attached fast to the other object and used for admitting the insertion member into fast engagement therewith. The insertion member is provided with a setting portion for fast attachment to the aforementioned one object and a shaft extended from the setting portion and possessed of a radially expanded engaging portion at the leading end thereof. The reception member is provided with two generally semicylindrical shells connected to each other through a thin-walled hinge portion and adapted to form one cylindrical shape upon being closed onto each other along the matched edges thereof and a plurality of resilient engaging pieces regularly spaced in the longitudinal direction on the inner wall of each of the shells.

Abstract translation: 用于连接两个物体的联接器包括快速附接到物体之一的插入构件和快速附接到另一物体的接收构件，并用于允许插入构件与其快速接合。 插入构件设置有用于快速附接到上述一个物体的设置部分和从设置部分延伸并且在其前端具有径向扩张的接合部分的轴。 接收构件设置有两个通常半圆柱形壳体，通过薄壁铰链部分相互连接，并且适于在沿其匹配边缘彼此闭合时形成一个圆柱形形状，并且多个弹性接合件在该 每个壳体的内壁上的纵向方向。

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