公开(公告)号：EP1293503A1

公开(公告)日：2003-03-19

申请号：EP01930192.8

申请日：2001-05-17

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  Merck Patent GmbH

发明人： TOBE, Takahiko ,  SUGANE, Takashi ,  HAMAGUCHI, Wataru ,  SHIMADA, Itsuro ,  MAENO, Kyoichi ,  MIYATA, Junji ,  KIMIZUKA, Tetsuya ,  SUZUKI, Takeshi ,  KOHARA, Atsuyuki ,  MORITA, Takuma ,  ARLT, Michael ,  GREINER, Hartmut

IPC分类号： C07D249/08 ,  C07D249/12 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  C07D405/12 ,  C07D405/04 ,  A61K31/41

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

摘要翻译： 本发明涉及具有活性抑制甘氨酸转运体并用作药物的三唑衍生物和新的三唑衍生物。 本发明的三唑衍生物具有优异的抑制甘氨酸转运蛋白的活性，可用作痴呆，精神分裂症，认知障碍或涉及各种疾病如阿尔茨海默病，帕金森病或亨廷顿病等的认知障碍或痉挛的治疗剂 涉及诸如神经变性疾病和脑血管障碍等疾病。 特别地，药物对于改善痴呆等的学习障碍是有用的。

公开(公告)号：EP0696586A1

公开(公告)日：1996-02-14

申请号：EP94913822.6

申请日：1994-04-26

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： NODA, Ichio ,  IWATA, Masahiro ,  SAKAMOTO, Shuichi ,  KOSHIYA, Kazuo ,  MORITA, Takuma ,  KOHARA, Atsuyuki

IPC分类号： C07D307/52 ,  C07D333/20 ,  C07D333/24 ,  C07D409/06 ,  C07D413/06 ,  C07D407/06 ,  A61K31/34 ,  A61K31/40 ,  A61K31/445 ,  A61K31/55

CPC分类号： C07D409/06 ,  C07D307/52 ,  C07D307/54 ,  C07D333/20 ,  C07D333/24 ,  Y02P20/55

摘要： A serine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having an anti-PCP(phencyclidine) activity and being useful as a psychotropic, wherein X represents sulfur or oxygen; Y represents nitrogen or CH; R¹ and R² represent each independently hydrogen, lower alkyl or an amino-protecting group, or R¹ and R² may be combined together to form 4- to 9-membered nitrogenous cycloalkyl; R³ represents hydrogen, carboxy, protected carboxy, aralkyl, or lower alkyl which may be hydroxylated; R⁴ represents hydrogen or hydroxy; R⁵ represents hydrogen or lower alkyl; A represents lower alkylene; B represents (1) an (un)saturated 4-to 10-membered nitrogenous cycloalkyl group which may be substituted by lower alkyl or aralkyl, or (2) a bicyclic nitrogenous hydrocarbon ring group comprising a 4- to 8-membered nitrogenous cycloalkyl group and a benzene ring fused together; and ... represents a single or a double bond.

摘要翻译： 由通式（I）表示的丝氨酸衍生物或其药学上可接受的盐，具有抗PCP（苯环利定）活性，可用作精神药物，其中X表示硫或氧; Y表示氮或CH; R 1和R 2各自独立地表示氢，低级烷基或氨基保护基，或者R 1和R 2可以组合在一起形成4-至9-元含氮环烷基; R 3表示氢，羧基，保护的羧基，芳烷基或可被羟基化的低级烷基; R 4表示氢或羟基; R 5表示氢或低级烷基; A表示低级亚烷基; B表示（1）可被低级烷基或芳烷基取代的（未）饱和的4至10元含氮环烷基，或（2）包含4-至8-元含氮环烷基的双环含氮环烃基 和苯环稠合在一起; 和...表示单键或双键。

公开(公告)号：EP0921123A1

公开(公告)日：1999-06-09

申请号：EP97928516.0

申请日：1997-06-30

申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.

发明人： KIMURA, Takenori ,  MURAKAMI, Takeshi ,  OHMORI, Junya ,  MORITA, Takuma ,  TSUKAMOTO, Shin-ichi

IPC分类号： C07D333/24 ,  C07D413/04 ,  C07D409/04 ,  C07D417/04 ,  C07D413/14 ,  C07D487/04 ,  A61K31/38 ,  A61K31/41 ,  A61K31/415 ,  A61K31/55

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/24 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

摘要： A thiophene derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof
(each symbol in the above formula means as follows,

R 1 : formula -A 1 -X 1 -R 3 ,
R 2 : formula -A 2 -X 2 -R 4 or does not exist,
B ring: 1) 4- to 10-membered nitrogen-containing cycloalkyl ring,
or 2) 5- or 6-membered nitrogen-containing unsaturated heterocycle,
Ar ring: an aryl ring which may have a substituent, or a 5- or 6-membered aromatic heterocycle or an 8- to 10-membered aromatic bicyclic heterocycle, which contains 1 to 4 of one or more types of hetero atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom,
A 1 , A 2 and A 3 : the same or different from one another, and each represents a bond or a lower alkylene group,
X 1 and X 2 : the same or different from each other, and each represents a bond or a formula -O-, -S-, -NR 5 -,

R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 and R 13 : the same or different from one another, and each represents a hydrogen atom or a lower alkyl group, and
R 3 and R 4 : the same or different from each other, and each represents a hydrogen atom, a cyclic imido group which may have a substituent and may be condensed with a benzene ring, or a lower alkyl group, a cycloalkyl group, an aryl group or an aralkyl group, which may respectively have a substituent,
with the proviso that, when Ar ring is thiazole ring, either one of A 1 and A 2 is a lower alkylene group, and when Ar ring is a benzene ring, a case in which R 1 and R 2 is methyl group or a halogen group and the other is a hydrogen atom is excluded).

摘要翻译： 由以下通式（I）表示的噻吩衍生物或其药学上可接受的盐（上式中的每个符号表示如下：R1：式-A1-X1-R3，R2：式-A2-X2- R4或不存在，B环：1）4-至10-元含氮环烷基环，或2）5-或6-元含氮不饱和杂环，Ar环：可具有取代基的芳基环， 或5-或6-元芳族杂环或8至10元芳族双环杂环，其含有1至4个选自氮原子，氧原子和 硫原子，A1，A2和A3：彼此相同或不同，并且各自表示键或低级亚烷基X1和X2：彼此相同或不同，并且各自表示键或式-O - ， - S - ， - NR5-， R5，R6，R7，R8，R9，R10，R11，R12和R13彼此相同或不同， 氢原子或低级烷基，R 3和R 4彼此相同或不同，各自表示氢原子，可以具有取代基并可与苯环缩合的环状酰亚胺基或低级烷基 基团，环烷基，芳基或芳烷基，其可以分别具有取代基，条件是当Ar环是噻唑环时，A1和A2中的任一个是低级亚烷基，当Ar环是 苯环，R1和R2为甲基或卤素基，另一个为氢原子的情况除外）。