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公开(公告)号:US06555565B2
公开(公告)日:2003-04-29
申请号:US10047816
申请日:2002-01-15
申请人: Junji Matsui , Naoki Tarui , Yu Momose , Ken-ichi Naruo
发明人: Junji Matsui , Naoki Tarui , Yu Momose , Ken-ichi Naruo
IPC分类号: A61K31427
CPC分类号: A61K31/427 , A61K31/422 , A61K31/425 , A61K31/4439
摘要: An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.
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公开(公告)号:US6087384A
公开(公告)日:2000-07-11
申请号:US272747
申请日:1999-03-15
申请人: Junji Matsui , Naoki Tarui , Yu Momose , Ken-ichi Naruo
发明人: Junji Matsui , Naoki Tarui , Yu Momose , Ken-ichi Naruo
IPC分类号: A61K31/422 , A61K31/425 , A61K31/427 , A61K31/4439 , A61K31/444 , C07D413/02 , C07D413/14 , C07D417/02 , C07D417/14 , A01K31/426 , A01K31/427
CPC分类号: A61K31/427 , A61K31/422 , A61K31/425 , A61K31/4439
摘要: An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: --CO--, --CH(OH)-- or --NR.sup.3 -- where R.sup.3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R.sup.1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R.sup.1 ; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.
摘要翻译: 一种凋亡抑制剂,其包含下式化合物:其中R表示可被取代的烃基或可被取代的杂环基; Y表示式-CO-,-CH(OH) - 或-NR 3 - ,其中R 3表示可被取代的烷基; m为0或1; n为0,1或2; X表示CH或N; A表示化学键或碳原子数为1〜7的二价脂肪族烃基; Q表示氧或硫; R1表示氢或烷基; 环E可以具有另外1至4个取代基,其可以与R 1组合形成环; L和M分别表示氢或可以相互结合形成化学键; 或其盐,或具有胰岛素敏感性增强活性的化合物。
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公开(公告)号:US06399639B1
公开(公告)日:2002-06-04
申请号:US09519274
申请日:2000-03-07
申请人: Junji Matsui , Naoki Tarui , Yu Momose , Ken-ichi Naruo
发明人: Junji Matsui , Naoki Tarui , Yu Momose , Ken-ichi Naruo
IPC分类号: A61K31427
CPC分类号: A61K31/427 , A61K31/422 , A61K31/425 , A61K31/4439
摘要: An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.
摘要翻译: 一种凋亡抑制剂,其包含下式化合物:其中R表示可被取代的烃基或可被取代的杂环基; Y表示式-CO-,-CH(OH) - 或-NR 3 - ,其中R 3表示可被取代的烷基; m为0或1; n为0,1或2; X表示CH或N; A表示化学键或碳原子数为1〜7的二价脂肪族烃基; Q表示氧或硫; R1表示氢或烷基; 环E可以具有另外1至4个取代基,其可以与R 1组合形成环; L和M分别表示氢或可以相互结合形成化学键; 或其盐,或具有胰岛素敏感性增强活性的化合物。
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公开(公告)号:US20050228020A1
公开(公告)日:2005-10-13
申请号:US11142885
申请日:2005-06-01
申请人: Masaomi Miyamoto , Junji Matsui , Hiroaki Fukumoto , Naoki Tarui
发明人: Masaomi Miyamoto , Junji Matsui , Hiroaki Fukumoto , Naoki Tarui
IPC分类号: A61K31/135 , A61K31/14 , A61K31/165 , A61K31/40 , A61K31/4164 , A61K31/4453 , A61P25/00 , A61P25/16 , A61P25/28 , A61P43/00 , C07C207/04 , C07C217/60 , C07C235/34 , C07D295/096 , C07D521/00 , A61K31/445
CPC分类号: C07D295/096 , A61K31/135 , A61K31/14 , A61K31/165 , A61K31/40 , A61K31/4164 , A61K31/4453 , C07C207/04 , C07C217/60 , C07C235/34 , C07C2602/10 , C07D231/12 , C07D233/56 , C07D249/08
摘要: An excellent β secretase inhibitor is provided, which comprises a compound of the general formula: wherein Ar is an aromatic group; X is a divalent group selected from —O—, —S—, —CO—, —SO—, —SO2—, —NR8—, CONR8—, —SO2NR8—, and —COO— (wherein R8 is hydrogen, etc.), a divalent C1-6 aliphatic hydrocarbon group which may contain one or two of these divalent groups, or a bond; Y is a divalent group selected from —O—, —S—, —CO—, —SO—, —SO2—, —NR8—, —CONR8—, —SO2NR8—, and —COO—, or a divalent C1-6 aliphatic hydrocarbon group which may contain one or two of these divalent groups; R1 and R2 are hydrogen, a hydrocarbon group, etc., respectively; and A is a ring which may be further substituted, or a salt thereof.
摘要翻译: 提供了优异的β分泌酶抑制剂,其包含通式如下的化合物:其中Ar为芳族基团; X是选自-O - , - S - , - CO - , - SO - , - SO 2 - , - NR 8 - ,CONR - , - SO 2 - , - COO-(其中R 8为氢等) ,可以含有一个或两个这些二价基团的二价C 1-6脂族烃基或键; Y是选自-O - , - S - , - CO - , - SO - , - SO 2 - , - NR 8 - , - CONR 2 - SO 2 - , - SO 2 - , - COO-或二价C 1-6 - 脂族基 可以含有一个或两个这些二价基团的烃基; R 1和R 2分别为氢,烃基等; A是可以被进一步取代的环,或其盐。
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公开(公告)号:US20090318365A1
公开(公告)日:2009-12-24
申请号:US12455563
申请日:2009-06-02
申请人: Chieko Kitada , Taiji Asami , Naoko Nishizawa , Tetsuya Ohtaki , Naoki Tarui , Hirokazu Matsumoto , Jiro Noguchi , Hisanori Matsui
发明人: Chieko Kitada , Taiji Asami , Naoko Nishizawa , Tetsuya Ohtaki , Naoki Tarui , Hirokazu Matsumoto , Jiro Noguchi , Hisanori Matsui
摘要: The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivatives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.
摘要翻译: 本发明提供了一种转氨酶衍生物,其中包含转氨酶的氨基酸被替代的化学取代基修饰,导致转氨酶衍生物,具有优异的血液稳定性和显示出癌转移抑制作用或癌生长抑制作用。
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公开(公告)号:US20070072865A1
公开(公告)日:2007-03-29
申请号:US10570270
申请日:2004-08-26
申请人: Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
发明人: Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
IPC分类号: A61K31/498 , C07D498/04 , C07D491/04 , C07D487/04
CPC分类号: C07D487/04 , C07D513/04
摘要: The present invention provides a compound represented by the formula: wherein R1 is an acyl group, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.
摘要翻译: 本发明提供由下式表示的化合物:其中R 1是酰基,R 2是可以被取代的烃基,等等,R SUP > 3为可以被取代的烃基等,R 4为可以被取代的烃基等,n为0〜4,X为 氧原子,硫原子等,或其盐。 本发明还提供具有TGR23拮抗剂活性的化合物,因此可用于预防和治疗癌症。
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公开(公告)号:US07091247B2
公开(公告)日:2006-08-15
申请号:US10312015
申请日:2001-06-28
申请人: Naoki Tarui , Takashi Santo , Hiroyuki Watanabe , Kazuyoshi Aso , Tetsuo Miwa , Shiro Takekawa
发明人: Naoki Tarui , Takashi Santo , Hiroyuki Watanabe , Kazuyoshi Aso , Tetsuo Miwa , Shiro Takekawa
IPC分类号: A61K31/166 , C07C233/64 , C07C237/28
CPC分类号: C07D213/40 , C07C237/42 , C07C311/16 , C07C311/46 , C07C323/41 , C07C335/32 , C07D207/14 , C07D207/38 , C07D209/20 , C07D209/42 , C07D211/26 , C07D211/58 , C07D213/56 , C07D213/70 , C07D231/12 , C07D233/56 , C07D241/04 , C07D249/08 , C07D285/06 , C07D295/13 , C07D295/192 , C07D307/54 , C07D317/58 , C07D333/20 , C07D333/38 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要: A novel biphenyl compound having GPR 14 antagonistic activity. It is a compound represented by the formula (I): wherein R1 represents hydrogen, etc.; X represents 1 to 12 spacers; A represents amino, etc., R2 and R3 each represents a hydrocarbon group, etc.; and rings B and C each represents an optionally further substituted benzene ring, or a salt thereof.
摘要翻译: 具有GPR 14拮抗活性的新型联苯化合物。 它是由式(I)表示的化合物:其中R 1表示氢等; X表示1〜12个间隔物; A表示氨基等,R 2和R 3各自表示烃基等; 环B和C各自表示任选进一步取代的苯环或其盐。
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公开(公告)号:US20090270625A1
公开(公告)日:2009-10-29
申请号:US12476619
申请日:2009-06-02
申请人: Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
发明人: Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
IPC分类号: C07D471/04
CPC分类号: C07D471/04
摘要: The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; — --- represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.
摘要翻译: 本发明旨在提供具有神经激肽2(NK2)受体拮抗作用的喹啉衍生物,其涉及式(I)表示的化合物,其中R1为氢原子等; R2是氢原子,任选具有取代基的烃基等; R3是未取代的(即不存在),氢原子等; R 4和R 5相同或不同,各自为氢原子,任选具有取代基的烃基等; R6是(任选具有取代基的环状基团) - 羰基等; R 7,R 8,R 9和R 10相同或不同,各自为氢原子,卤素等; 或R 7和R 8,R 8和R 9,并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数, ---表示未取代(即不存在)或单键; < img id =“CUSTOM-CHARACTER-00001”he =“2.79mm”wi =“7.03mm”file =“US20090270625A1-20091029-P00001.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键,或其盐等。
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公开(公告)号:US20090258893A1
公开(公告)日:2009-10-15
申请号:US12476626
申请日:2009-06-02
申请人: Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
发明人: Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
IPC分类号: A61K31/437 , C07D471/04 , A61P1/00
CPC分类号: C07D471/04
摘要: The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.
摘要翻译: 本发明旨在提供具有神经激肽2(NK2)受体拮抗作用的喹啉衍生物,其涉及式(I)表示的化合物,其中R1为氢原子等; R2是氢原子,任选具有取代基的烃基等; R3是未取代的(即不存在),氢原子等; R 4和R 5相同或不同,各自为氢原子,任选具有取代基的烃基等; R6是(任选具有取代基的环状基团) - 羰基等; R 7,R 8,R 9和R 10相同或不同,各自为氢原子,卤素等; 或R 7和R 8,R 8和R 9,并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数, “img id =”CUSTOM-CHARACTER-00001“he =”0.68mm“wi =”3.13mm“file =”US20090258893A1-20091015-P00001.TIF“img-content =”character“img-format =”tif“/> 表示未取代的(即不存在)或单键; < img id =“CUSTOM-CHARACTER-00002”he =“1.02mm”wi =“3.13mm”file =“US20090258893A1-20091015-P00002.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键,或其盐等。
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公开(公告)号:US20080220445A1
公开(公告)日:2008-09-11
申请号:US11664086
申请日:2005-09-30
申请人: Naoki Tarui
发明人: Naoki Tarui
CPC分类号: C12Q1/37 , C12N9/6478 , G01N33/573 , G01N2333/96472 , G01N2500/00
摘要: The present invention provides a screening method for a compound inhibiting a transmembrane enzyme activity by binding to a transmembrane region of the enzyme, characterized by using (a) a protein having a part or all of an amino acid sequence of the enzyme, comprising a region comprising an active center and a part or all of a transmembrane region of the transmembrane enzyme, and optionally (b) a protein having a part of an amino acid sequence of the transmembrane enzyme, comprising the region comprising the active center and lacking the above-mentioned part or all of the transmembrane region, and measuring the binding of a test substance to each protein and the enzyme activity of each protein, as well as a kit for screening comprising the above-mentioned protein of (a) and (b). Also, the present invention provides a β-secretase selective inhibitor comprising a β-secretase inhibiting substance binding to a transmembrane region of the enzyme, and particularly an inhibitor for prophylaxis and/or treatment of Alzheimer's disease, Down syndrome or Age-Associated Memory Impairment.
摘要翻译: 本发明提供了通过与酶的跨膜区结合来抑制跨膜酶活性的化合物的筛选方法,其特征在于使用(a)具有部分或全部所述酶的氨基酸序列的蛋白质,所述蛋白质包含区域 其包含所述跨膜酶的活性中心和部分或全部跨膜区,以及任选地(b)具有所述跨膜酶的氨基酸序列的一部分的蛋白质,所述蛋白质包含所述活性中心并且缺少所述跨膜酶的区域, 上述部分或全部的跨膜区,测定被检物质与各蛋白质的结合以及各蛋白质的酶活性,以及包含上述(a)和(b)的蛋白质的筛选试剂盒。 此外,本发明提供了一种β-分泌酶选择性抑制剂,其包含结合酶的跨膜区的β-分泌酶抑制物质,特别是用于预防和/或治疗阿尔茨海默氏病,唐氏综合征或年龄相关记忆障碍的抑制剂 。
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