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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
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。
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公开(公告)号:EP0757985A1
公开(公告)日:1997-02-12
申请号:EP95917462.4
申请日:1995-04-26
发明人: OHMORI, Junya , MAENO, Kyoichi , HIDAKA, Kazuyuki , NAKATO, Kazuhiro , SAKAMOTO, Shuichi , TSUKAMOTO, Shin-ichi
IPC分类号: C07D207/14 , A61K31/40
CPC分类号: C07D207/14
摘要: N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D 3 and/or D 4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof.
(wherein each symbol in the formula has the following meaning,
R 1 : hydrogen, lower alkyl, aralkyl, or cycloalkyl or cycloalkyl-lower alkyl having 3 to 8 ring atoms,
R 2 : bicyclic or tricyclic bridged hydrocarbon ring of 4 to 16 ring atoms which may have lower alkyl,
R 3 : lower alkoxy, amino or mono- or di-lower alkylamino,
R 4 : hydrogen, halogen, lower alkyl which may have hydroxyl, lower alkoxy, cyano, nitro, amino, mono- or di-lower alkylamino, acyl or a group represented by -S(O) m -R 5 ,
R 5 : lower alkyl, amino or mono- or di-lower alkylamino,
m: 0, 1 or 2,
X: a bond or a group represented by -O-, -S(O) n -, -NH- or -CONH-, and
n: 0, 1 or 2,
with the proviso that, when R 1 is cycloalky, the cases wherein X is -CONH-, R 3 is lower alkoxy and R 4 is halogen are excluded.)摘要翻译: 具有对多巴胺D3和/或D4受体具有强效和选择性拮抗作用并且可用作精神药物,精神分裂症治疗剂等的由以下通式(I)表示的N-(3-吡咯烷基)苯甲酰胺衍生物,或 其药学上可接受的盐或其药物制剂。 (其中式中的每个符号具有以下含义:R 1:氢,低级烷基,芳烷基或具有3至8个环原子的环烷基或环烷基 - 低级烷基,R 2:双环或三环桥连 具有4至16个环原子的烃环,其可具有低级烷基,R 3:低级烷氧基,氨基或单 - 或二 - 低级烷基氨基,R 4:氢,卤素,可具有羟基的低级烷基,低级烷氧基 ,氰基,硝基,氨基,一或二低级烷基氨基,酰基或由-S(O)m R 5表示的基团,R 5:低级烷基,氨基或单 - 或二 - 低级烷基氨基,m :0,1或2,X:由-O - , - S(O)n-,-NH-或-CONH-表示的键或基团,n:0,1或2,条件是, 当R 1为环烷基时,其中X为-CONH-,R 3为低级烷氧基且R 4为卤素的情况除外)
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公开(公告)号:EP0696585B1
公开(公告)日:1998-12-16
申请号:EP94913821.8
申请日:1994-04-26
发明人: NIIGATA, Kunihiro , TAKAHASHI, Takumi , MARUYAMA, Tatsuya , SUZUKI, Takayuki , MAENO, Kyoichi , ONDA, Kenichi , KONTANI, Toru , NOSHIRO, Osamu , KOIKE, Reiko , SHIMAYA, Akiyoshi , IRIE, Jun
IPC分类号: C07D271/06 , C07D413/14 , A61K31/41 , A61K31/44
CPC分类号: C07D271/07 , C07D413/14
摘要: A bisoxadiazolidinedione derivative of general formula (I) useful as an insulin-sensitivity improver, a pharmaceutically acceptable salt thereof, and a medicinal composition thereof, wherein (a) and (b) may be the same or different from each other and each represent an optionally substituted phenylene group, and L represents: (1) an oxygen atom, (2) a group of formula (II) (R1 being a hydrogen atom or a lower alkyl group), (3) a group of the formula: -S(O)¿n?- (n being 0, 1 or 2), (4) a group of the formula: -CO-, (5) a group of formula (III) or (IV) (R?2¿ being a hydrogen atom or a lower alkyl group), or (6) an alkylene or alkenylene group which may be substituted and interrupted by an oxygen atom and/or a sulfur atom, and the like.
摘要翻译: 用作胰岛素敏感性改进剂的通式(I)的双恶二唑烷二酮衍生物,其药学上可接受的盐及其药用组合物,其中(a)和(b)可以彼此相同或不同,并且各自表示 (1)氧原子,(2)式(II)的基团(R 1为氢原子或低级烷基),(3)下式的基团:-S (O)n - (n为0,1或2),(4)式-CO-的基团,(5)式(III)或(IV)的基团 氢原子或低级烷基),或(6)可以被氧原子和/或硫原子取代和插入的亚烷基或亚烯基等。
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公开(公告)号:EP1167369A1
公开(公告)日:2002-01-02
申请号:EP00915350.3
申请日:2000-04-05
发明人: HAYASHIBE, Satoshi , ITAHANA, Hirotsune , OKADA, Masamichi , KOHARA, Atsuyuki , MAENO, Kyoichi , YAHIRO, Kiyoshi , SHIMADA, Itsuro , TANABE, Kazuhito , NEGORO, Kenji , KAMIKUBO, Takashi , SAKAMOTO, Shuichi
IPC分类号: C07D513/04 , A61K31/429 , A61K31/5383 , A61K31/454 , A61K31/4439 , A61K31/435 , A61P43/00 , A61P25/28 , A61P9/10
CPC分类号: C07D513/04 , A61K31/429
摘要: Novel thiazolo[3,2-a]benzimidazol derivatives represented by general formula (1), which act specifically on metabotropic glutamate receptors and are useful as drugs; and novel compounds useful as intermediates for the synthesis of the derivatives wherein, R 1 is optionally substituted carbamoyl, carbonyl, oxy, amino, carbonylamino, or the like; R 2 is hydrogen, lower alkyl, or the like; and R 3 , R 4 and R 5 are each independently hydrogen, lower alkyl, or the like.
摘要翻译: 由通式(1)表示的新型噻唑并[3,2-a]苯并咪唑衍生物,其特异性作用于代谢型谷氨酸受体并可用作药物; 以及用作合成衍生物中间体的新型化合物,其中R1是任选取代的氨基甲酰基,羰基,氧基,氨基,羰基氨基等; R2是氢,低级烷基等; 并且R3,R4和R5各自独立地为氢,低级烷基等。
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公开(公告)号:EP0696585A1
公开(公告)日:1996-02-14
申请号:EP94913821.8
申请日:1994-04-26
发明人: NIIGATA, Kunihiro , TAKAHASHI, Takumi , MARUYAMA, Tatsuya , SUZUKI, Takayuki , MAENO, Kyoichi , ONDA, Kenichi , KONTANI, Toru , NOSHIRO, Osamu , KOIKE, Reiko , SHIMAYA, Akiyoshi , IRIE, Jun
IPC分类号: C07D271/06 , C07D413/14 , A61K31/41 , A61K31/44
CPC分类号: C07D271/07 , C07D413/14
摘要: A bisoxadiazolidinedione derivative of general formula (I) useful as an insulin-sensitivity improver, a pharmaceutically acceptable salt thereof, and a medicinal composition thereof, wherein (a) and (b) may be the same or different from each other and each represent an optionally substituted phenylene group, and L represents: (1) an oxygen atom, (2) a group of formula (II) (R¹ being a hydrogen atom or a lower alkyl group), (3) a group of the formula: -S(O) n - (n being 0, 1 or 2), (4) a group of the formula: -CO-, (5) a group of formula (III) or (IV) (R² being a hydrogen atom or a lower alkyl group), or (6) an alkylene or alkenylene group which may be substituted and interrupted by an oxygen atom and/or a sulfur atom, and the like.
摘要翻译: 用作胰岛素敏感性改进剂的通式(I)的双恶二唑烷二酮衍生物,其药学上可接受的盐及其药用组合物,其中(a)和(b)可以彼此相同或不同,并且各自表示 (1)氧原子,(2)式(II)的基团(R 1为氢原子或低级烷基),(3)下式的基团:-S (O)n-(n为0,1或2),(4)式-CO-的基团,(5)式(III)或(IV)的基团(R 2为氢原子或 低级烷基)或(6)可被氧原子和/或硫原子取代和插入的亚烷基或亚烯基等。
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