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1. 发明申请

US20050038072A1 Nitrogeneous cyclic ketone derivative, process for producing the same, and use 审中-公开
标题翻译：亚硝基环酮衍生物，其制备方法和用途
公开(公告)号：US20050038072A1
公开(公告)日：2005-02-17
申请号：US10498228
申请日：2002-12-26
申请人： Masayoshi Yamaoka , Yoshinori Ikeura , Tadatoshi Hashimoto , Naoki Tarui
发明人： Masayoshi Yamaoka , Yoshinori Ikeura , Tadatoshi Hashimoto , Naoki Tarui
IPC分类号： A61P1/00 , A61P1/08 , A61P9/00 , A61P11/00 , A61P11/06 , A61P11/14 , A61P13/02 , A61P15/00 , A61P15/10 , A61P17/04 , A61P17/06 , A61P17/16 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P43/00 , C07D207/24 , C07D211/74 , C07D211/86 , C07D401/06 , C07D401/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D43/02 , A61K31/445 , A61K31/454
CPC分类号： C07D405/04 , C07D207/24 , C07D211/74 , C07D211/86 , C07D401/06 , C07D401/10 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D417/04
摘要： A novel compound represented by the formula (I): wherein rings A and B each represents an optionally substituted aromatic ring, or rings A and B may be bonded to each other through linking between bonds or substituents thereof to form a ring; ring C represents a nitrogenous saturated heterocycle optionally having one or more substituents besides the oxo (provided that 2,3-dioxopyrrolidine ring is excluded); R1 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and indicates a single bond or a double bond. It has high antagonistic activity against a tachykinin receptor, especially an SP receptor.
摘要翻译：由式（I）表示的新化合物：其中环A和B各自表示任选取代的芳环，或者环A和B可以通过键或取代基之间的连接键合而形成环; 环C表示除了氧代外，任选具有一个或多个取代基的氮饱和杂环（只要不包括2,3-二氧代吡咯烷环）; R 1表示氢，任选取代的烃基或任选取代的杂环基; 并表示单键或双键。对速激肽受体，特别是SP受体具有较高的拮抗作用。

2. 发明申请

US20060167052A1 Piperidine derivative, process for producing the same, and use 失效
标题翻译：哌啶衍生物，其制备方法和用途
公开(公告)号：US20060167052A1
公开(公告)日：2006-07-27
申请号：US10516252
申请日：2003-05-29
申请人： Yoshinori Ikeura , Tadatoshi Hashimoto , Naoki Tarui , Junya Shirai , Masayuki Yamashita
发明人： Yoshinori Ikeura , Tadatoshi Hashimoto , Naoki Tarui , Junya Shirai , Masayuki Yamashita
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D405/14 , C07D211/46 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally lo substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and 15 when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.
摘要翻译：本发明提供由下式表示的化合物：其中Ar是芳基，芳烷基或芳族杂环基，其各自可以被取代，R 1是氢原子，任选地取代烃基，酰基或任选取代的杂环基，X是氧原子或任选取代的亚氨基，Z是任选取代的亚甲基，环A是任选进一步取代的哌啶环，环B是任选取代的芳环，条件是当Z是被氧代基取代的亚甲基时，R 1不是甲基，而当Z是被甲基取代的亚甲基时，R 1是环B 是取代的芳香环或其盐，其是对速激肽受体具有优异拮抗作用的新型哌啶衍生物，并且可用作药物，特别是用于预防和/或治疗尿频和/或尿失禁

3. 发明授权

US07622487B2 Piperidine derivative, process for producing the same, and use 失效
标题翻译：哌啶衍生物，其制备方法和用途
公开(公告)号：US07622487B2
公开(公告)日：2009-11-24
申请号：US10516252
申请日：2003-05-29
申请人： Yoshinori Ikeura , Tadatoshi Hashimoto , Naoki Tarui , Junya Shirai
发明人： Yoshinori Ikeura , Tadatoshi Hashimoto , Naoki Tarui , Junya Shirai
IPC分类号： A61K31/445 , C07D403/12
CPC分类号： C07D405/14 , C07D211/46 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.
摘要翻译：本发明提供由下式表示的化合物：其中Ar是芳基，芳烷基或芳族杂环基，其各自可以被取代，R 1是氢原子，任选取代的烃基，酰基或任选取代的杂环基，X是氧原子或任选取代的亚氨基，Z是任选取代的亚甲基，环A是任选进一步取代的哌啶环，环B是任选取代的芳环，条件是当Z 是被氧基取代的亚甲基，R1不是甲基，当Z是被甲基取代的亚甲基时，环B是取代的芳香环或其盐，它是具有用于速激肽受体的优异拮抗作用，可用作药物，特别是用于预防和/或治疗尿频和/或尿失禁的药剂。

4. 发明授权

US5770590A Cyclic compounds, their prudiction and use 失效
标题翻译：循环化合物，其审慎和使用
公开(公告)号：US5770590A
公开(公告)日：1998-06-23
申请号：US717801
申请日：1996-09-23
申请人： Hideaki Natsugari , Takenori Ishimaru , Takayuki Doi , Yoshinori Ikeura , Chiharu Kimura , Naoki Tarui
发明人： Hideaki Natsugari , Takenori Ishimaru , Takayuki Doi , Yoshinori Ikeura , Chiharu Kimura , Naoki Tarui
IPC分类号： C07D471/04 , C07D471/14 , C07D498/04 , A61K31/33 , A61K31/55 , C07D245/00 , C07D487/00
CPC分类号： C07D471/04 , C07D471/14
摘要： Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C
摘要翻译：下列通式的新化合物或其盐。其中环M是具有-N = C，-CO-N或-CS-N（作为部分结构-X + E，ov）的杂环。。 + EE Y < R a和R b彼此键合形成环A，或它们相同或不同，独立地表示环M上的氢原子或取代基; 环A和环B独立地表示任选取代的杂环或杂环，并且它们中的至少一个是任选取代的杂环; R C是任选取代的杂环或杂环; R Z是任选取代的环; n表示1〜6的整数，或其盐具有优异的速激肽受体拮抗作用及其制备及药物组合物。

5. 发明申请

US20090318365A1 METASTIN DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：分子衍生物及其用途
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
IPC分类号： A61K38/08 , C07K7/06
CPC分类号： C07K14/47 , A61K38/00
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。

6. 发明申请

US20070072865A1 Bicyclic piperazine compound and use thereof 失效
标题翻译：双环哌嗪化合物及其用途
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。

7. 发明授权

US07091247B2 Biphenyl compound 失效
标题翻译：联苯化合物
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。

8. 发明申请

US20090270625A1 FUSED QUINOLINE DERIVATIVE AND USE THEREOF 失效
标题翻译：熔融喹啉衍生物及其用途
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; ＆lt; 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。

9. 发明申请

US20090258893A1 FUSED QUINOLINE DERIVATIVE AND USE THEREOF 失效
标题翻译：熔融喹啉衍生物及其用途
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; ＆lt; 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。

10. 发明申请

US20080220445A1 Method of Screening Transmembrane Enzyme Inhibitory Substance 审中-公开
标题翻译：筛选跨膜酶抑制物质的方法
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
IPC分类号： G01N33/53 , C12N9/99
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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