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公开(公告)号:US06489331B1
公开(公告)日:2002-12-03
申请号:US09719570
申请日:2001-04-09
申请人: Junichi Shimada , Yoshihisa Ohta , Kotaro Takasaki , Miho Suda , Hideaki Kusaka , Hiroshi Yano , Satoshi Nakanishi , Yuzuru Matsuda
发明人: Junichi Shimada , Yoshihisa Ohta , Kotaro Takasaki , Miho Suda , Hideaki Kusaka , Hiroshi Yano , Satoshi Nakanishi , Yuzuru Matsuda
IPC分类号: A61K3152
CPC分类号: C07D487/14 , A61K31/505 , A61K31/519 , Y10S514/866
摘要: A medicament for the therapeutic treatment of diabetes which comprises as an active ingredient a compound represented by the general formula (I): wherein R1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, R3 represents a hydrogen atom, a lower alkyl group or a substituted or unsubstituted aralkyl group, X1 and X2 independently represent a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and the symbol “n” represents an integer of from 0 to 3, or a physiologically acceptable salt thereof.
摘要翻译: 一种用于治疗糖尿病的药物,其包含作为活性成分的由通式(I)表示的化合物:其中R 1表示氢原子,低级烷基,取代或未取代的芳基或取代或未取代的芳族 杂环基,R2表示氢原子,低级烷基,取代或未取代的芳烷基,取代或未取代的芳基或取代或未取代的芳香族杂环基,R3表示氢原子,低级烷基或取代 或未取代的芳烷基,X 1和X 2独立地表示氢原子,低级烷基,取代或未取代的芳烷基或取代或未取代的芳基,符号“n”表示0〜3的整数,或 其生理上可接受的盐。
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公开(公告)号:US07005430B2
公开(公告)日:2006-02-28
申请号:US10149423
申请日:2000-12-22
申请人: Kimihisa Ueno , Akira Ogawa , Yoshihisa Ohta , Yuji Nomoto , Kotaro Takasaki , Hideaki Kusaka , Hiroshi Yano , Chiharu Nakagawa , Satoshi Nakanishi
发明人: Kimihisa Ueno , Akira Ogawa , Yoshihisa Ohta , Yuji Nomoto , Kotaro Takasaki , Hideaki Kusaka , Hiroshi Yano , Chiharu Nakagawa , Satoshi Nakanishi
IPC分类号: C07D487/14 , C07D473/24 , C07D473/22 , A61K31/519 , A61P3/10
CPC分类号: C07D487/14
摘要: A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C═O or N═C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y-Z represents R1aN—C═O and R2 represents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, —NR7R8, —CO2H, a lower alkoxycarbonyl group, —COHal, —CONR9R10 or —CHO, V2 may represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.
摘要翻译: 由式(I)表示的稠合嘌呤衍生物:化学式id =“CHEM-US-00001”num =“000”
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公开(公告)号:US20060252780A1
公开(公告)日:2006-11-09
申请号:US10554254
申请日:2004-04-23
申请人: Takao Nakajima , Kimihisa Ueno , Yuji Nomoto , Yuichi Matsumoto , Hiroshi Yano , Satoshi Nakanishi , Kotaro Takasaki , Hideaki Kusaka
发明人: Takao Nakajima , Kimihisa Ueno , Yuji Nomoto , Yuichi Matsumoto , Hiroshi Yano , Satoshi Nakanishi , Kotaro Takasaki , Hideaki Kusaka
IPC分类号: A61K31/519 , C07D487/14
CPC分类号: C07D487/14
摘要: A fused pyrimidine derivative is presented. The derivatie has an insulin secretion stimulating activity represented by Formula (I): {wherein R1 represents a hydrogen atom, lower alkyl, or the like; n represents an integer of 0 to 3; and X1 and X2 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like; and formula (II): represents formula (III): [wherein X—Y—Z represents R2C═CR3—NR4 (wherein R2, R3 and R4 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like)]}, or a pharmaceutically acceptable salt thereof.
摘要翻译: 提出了一种稠合的嘧啶衍生物。 衍生物具有由式(I)表示的胰岛素分泌刺激活性:其中R 1表示氢原子,低级烷基等; n表示0〜3的整数, X 1和X 2可以相同或不同,各自表示氢原子,低级烷基等; 和式(II):表示式(III):[其中XYZ表示R 2 C-CR 3 -NR 4(其中R' O 2,R 3和R 4可以相同或不同,各自表示氢原子,低级烷基等)]}, 或其药学上可接受的盐。
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公开(公告)号:US20060046992A1
公开(公告)日:2006-03-02
申请号:US10519630
申请日:2003-06-25
申请人: Daisuke Machii , Koji Suzuki , Tsutomu Matsumura , Hitoshi Arai , Miho Iwase , Hiroshi Yano , Satoshi Nakanishi , Fumiko Ogino , Kotaro Takasaki , Hideaki Kusaka
发明人: Daisuke Machii , Koji Suzuki , Tsutomu Matsumura , Hitoshi Arai , Miho Iwase , Hiroshi Yano , Satoshi Nakanishi , Fumiko Ogino , Kotaro Takasaki , Hideaki Kusaka
IPC分类号: A61K31/519 , C07D487/04
CPC分类号: C07D471/04 , A61K31/437 , A61K31/445 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/55 , C07D487/04
摘要: The present invention provides a compound represented by formula (I): [wherein X—Y-Z represents R5N—C═O (wherein R5 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted lower alkenyl, or substituted or unsubstituted lower alkynyl), etc; R1 and R2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, etc; and R3 and R4 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, etc], or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供由式(I)表示的化合物:[其中XYZ表示R 5 NCO(其中R 5表示氢原子,取代或未取代的低级烷基,取代的 或未取代的芳烷基,取代或未取代的低级烯基,或取代或未取代的低级炔基)等; R 1和R 2可以相同或不同,各自表示氢原子,取代或未取代的低级烷基等; R 3和R 4可以相同或不同,各自表示氢原子,取代或未取代的低级烷基等]或其药学上可接受的盐。
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公开(公告)号:US20070191402A1
公开(公告)日:2007-08-16
申请号:US10514119
申请日:2003-05-16
申请人: Hiroki Ishiguro , Yuko Saeki , Seiji Sugimoto , Masahiro Matsubara , Kimihisa Ueno , Kiyotoshi Mori , Satoshi Nakanishi , Hiroshi Yano
发明人: Hiroki Ishiguro , Yuko Saeki , Seiji Sugimoto , Masahiro Matsubara , Kimihisa Ueno , Kiyotoshi Mori , Satoshi Nakanishi , Hiroshi Yano
IPC分类号: A61K31/519 , A61K31/53 , C07D487/12 , G01N33/53
CPC分类号: C12Q1/32 , A61K31/53 , A61K31/5377 , A61K31/55 , C07D487/14 , G01N33/56966 , G01N2333/90209 , G01N2500/00
摘要: The present invention provides a screening method of a substance which inhibits binding of a condensed purine derivative to a pancreatic β cell or a treated product of the cell, a substance which inhibits binding of a condensed purine derivative to a protein capable of the condensed purine derivative, and a substance which inhibits the expression or enzymatic activity of a protein capable of a condensed purine derivative, which comprises using the condensed purine derivative and a pancreatic β cell or a treated product of the cell or a protein capable of binding to the condensed purine derivative.
摘要翻译: 本发明提供了抑制冷凝的嘌呤衍生物与胰腺β细胞或细胞的处理产物的结合的物质的筛选方法,抑制结合的嘌呤衍生物与能够产生缩合嘌呤衍生物的蛋白质结合的物质 以及抑制能够结合嘌呤衍生物的蛋白质的表达或酶活性的物质,其包括使用稠合的嘌呤衍生物和胰β细胞或能够结合浓缩的嘌呤的细胞或蛋白质的处理产物 衍生物。
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公开(公告)号:US07524852B2
公开(公告)日:2009-04-28
申请号:US10516750
申请日:2003-06-06
申请人: Hitoshi Arai , Tsutomu Matsumura , Hiroshi Ishida , Yosuke Yamaura , Seiji Aratake , Etsuo Ohshima , Koji Yanagawa , Motoki Miyama , Koji Suzuki , Ari Kawabe , Satoshi Nakanishi , Katsuya Kobayashi , Takashi Sato , Ichiro Miki , Kimihisa Ueno , Shinya Fujii , Miho Iwase
发明人: Hitoshi Arai , Tsutomu Matsumura , Hiroshi Ishida , Yosuke Yamaura , Seiji Aratake , Etsuo Ohshima , Koji Yanagawa , Motoki Miyama , Koji Suzuki , Ari Kawabe , Satoshi Nakanishi , Katsuya Kobayashi , Takashi Sato , Ichiro Miki , Kimihisa Ueno , Shinya Fujii , Miho Iwase
IPC分类号: C07D487/04 , A61K31/519 , A61P29/00
CPC分类号: C07D263/58 , C07D471/04 , C07D487/04
摘要: [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, —C(═O)—, —SO2—, —OC(═O)— or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.
摘要翻译: [其中m和n可以相同或不同,并且各自表示1〜3的整数,其中m + n为4以下; R1表示-NR4R5(其中R4和R5可以相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的芳烷基等); R2表示上述式(II),式(IV)等; A表示单键,-C(-O) - , - SO 2 - , - OC(-O) - 等; 并且R 3表示取代或未取代的低级烷基,取代或未取代的环烷基,取代或未取代的芳烷基等〕上式(I)表示的双环嘧啶衍生物或其季铵盐,或其药学上可接受的盐等, 被提供。 它们具有对TARC和/或MDC的功能的抗炎活性或调节活性,并且可用于治疗和/或预防与T细胞相关的疾病,例如过敏性疾病,自身免疫疾病或移植排斥反应。
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公开(公告)号:US4990693A
公开(公告)日:1991-02-05
申请号:US465892
申请日:1990-01-16
申请人: Satoshi Nakanishi , Koji Yamada , Katsuhiko Ando , Isao Kawamoto , Toru Yasuzawa , Hiroshi Sano , Noriaki Hirayama , Hiroshi Kase , Joji Goto , Etsuyo Shimizu
发明人: Satoshi Nakanishi , Koji Yamada , Katsuhiko Ando , Isao Kawamoto , Toru Yasuzawa , Hiroshi Sano , Noriaki Hirayama , Hiroshi Kase , Joji Goto , Etsuyo Shimizu
CPC分类号: C12R1/645 , C07C35/48 , C07C45/58 , C07C47/46 , C07D303/48 , C12P17/02 , C12P7/02 , C12P7/24
摘要: Novel physiologically active substances KS-504a, KS-504b and KS-504d having a vasodilative activity and a novel physiologically active substance KS-504e having an activity to inhibit histamine secretion are produced by culturing a microorganism of the genus Mollisia.
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公开(公告)号:US20070037834A1
公开(公告)日:2007-02-15
申请号:US10516750
申请日:2003-06-06
申请人: Hitoshi Arai , Tsutomu Matsumura , Hiroshi Ishida , Yosuke Yamaura , Seiji Aratake , Etsuo Ohshima , Koji Yanagawa , Motoki Miyama , Koji Suzuki , Ari Kawabe , Satoshi Nakanishi , Katsuya Kobayashi , Takashi Sato , Ichiro Miki , Kimihisa Ueno , Shinya Fujii , Miho Iwase
发明人: Hitoshi Arai , Tsutomu Matsumura , Hiroshi Ishida , Yosuke Yamaura , Seiji Aratake , Etsuo Ohshima , Koji Yanagawa , Motoki Miyama , Koji Suzuki , Ari Kawabe , Satoshi Nakanishi , Katsuya Kobayashi , Takashi Sato , Ichiro Miki , Kimihisa Ueno , Shinya Fujii , Miho Iwase
IPC分类号: A61K31/519 , C07D487/02
CPC分类号: C07D263/58 , C07D471/04 , C07D487/04
摘要: [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, —C(═O)—, —SO2—, —OC(═O)— or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like]Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.
摘要翻译: [其中m和n可以相同或不同,并且各自表示1〜3的整数,其中m + n为4以下; R 1表示-NR 4 R 5(其中R 4,R 5和R 5) 可以相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的芳烷基等); R 2表示上述式(II),式(IV)等; A表示单键,-C(-O) - , - SO 2 - , - OC(-O) - 等; 和R 3表示取代或未取代的低级烷基,取代或未取代的环烷基,取代或未取代的芳烷基等〕由上式(I)表示的双环嘧啶衍生物或其季铵盐或药学上可接受的盐 可接受的盐等。 它们具有对TARC和/或MDC的功能的抗炎活性或调节活性,并且可用于治疗和/或预防与T细胞相关的疾病,例如过敏性疾病,自身免疫疾病或移植排斥反应。
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公开(公告)号:US20090298928A1
公开(公告)日:2009-12-03
申请号:US12534775
申请日:2009-08-03
申请人: Masato Iino , Satoshi Yamaki , Satoshi Nakanishi , Masahiro Tajima , Ryuji Ueno
发明人: Masato Iino , Satoshi Yamaki , Satoshi Nakanishi , Masahiro Tajima , Ryuji Ueno
IPC分类号: A61K31/351 , A61P17/00
CPC分类号: C07D319/06 , A61K8/365 , A61K8/37 , A61K8/4973 , A61K8/498 , A61K9/0014 , A61K9/06 , A61K47/10 , A61Q5/006 , A61Q7/00 , C07C69/734 , C07D317/30
摘要: Provided is a composition for scalp and hair treatment, comprising a menthol derivative and a prostaglandin compound having two hetero atoms at the 15 position. The composition of the present invention is effective not only for preventing dandruff and itchy scalp but also for preventing or treating hair loss, baldness, or hair thinness.
摘要翻译: 本发明提供一种用于头皮和头发处理的组合物,其包含薄荷醇衍生物和在15位具有两个杂原子的前列腺素化合物。 本发明的组合物不仅有效防止头皮屑和瘙痒的头皮,而且有效地防止或治疗脱发,秃发或毛发的变细。
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公开(公告)号:US5161743A
公开(公告)日:1992-11-10
申请号:US763515
申请日:1991-09-20
申请人: Hideto Takeda , Kazuyoshii Sugaya , Ryoichi Tada , Oyuki Ogawa , Hisanori Kobayashi , Satoshi Nakanishi
发明人: Hideto Takeda , Kazuyoshii Sugaya , Ryoichi Tada , Oyuki Ogawa , Hisanori Kobayashi , Satoshi Nakanishi
CPC分类号: F02M61/08 , F02M51/0675 , F02M51/0678 , F02M61/06
摘要: An electromagnetic fuel injection valve for use in an internal combustion engine includes a valve body provided with a valve seat and a valve member having an abutting part moved within the valve body by an electromagnetic actuator between a closed position where the abutting part abuts against the valve seat to interrupt supply of fuel to the engine and an open position where the abutting portion is spaced from the valve seat to permit supply of the fuel to the engine. The valve member has a metering portion which cooperates with the valve seat to define therebetween a fuel metering gap when the valve member is in the open position. The abutting part of the valve member is located downstream of the metering portion with reference to a flow direction of the fuel so that the metering portion is always immersed in the fuel when the valve member is in the closed position.
摘要翻译: 一种用于内燃机的电磁燃料喷射阀包括一阀体,该阀体设置有阀座和阀构件,该阀体具有一抵靠部件,该抵接部件通过电磁致动器在阀体内移动, 以阻止向发动机供应燃料和打开位置,其中抵接部分与阀座间隔开以允许向发动机供应燃料。 阀构件具有计量部分,其在阀构件处于打开位置时与阀座配合以在其间限定燃料计量间隙。 阀构件的邻接部分相对于燃料的流动方向位于计量部分的下游,使得当阀构件处于关闭位置时,计量部分总是浸入燃料中。
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