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公开(公告)号:US20090270361A1
公开(公告)日:2009-10-29
申请号:US12383502
申请日:2009-03-25
申请人: Mitsuhiro Ito , Naoki Tomita , Tomohiro Kaku , Tomohiko Suzaki
发明人: Mitsuhiro Ito , Naoki Tomita , Tomohiro Kaku , Tomohiko Suzaki
IPC分类号: A61K31/4155 , C07D231/12 , A61K31/415 , A61K31/4439 , C07D401/12 , C07D403/10 , A61P35/00
CPC分类号: C07D231/12 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/12
摘要: The present invention aims to provide a novel pyrazole derivative and a pharmaceutical agent containing the same. The present invention provides a compound represented by the formula (I′) wherein R1′ is (1) a hydrogen atom, (2) a group via a carbon atom, (3) a group via a nitrogen atom, (4) a group via an oxygen atom or (5) a group via a sulfur atom; R2′ is an aromatic ring group optionally having substituent(s); R3′ is (1) a hydrogen atom, (2) a group via a carbon atom, (3) a group via a nitrogen atom, (4) a group via an oxygen atom or (5) a group via a sulfur atom; R4′ is a cyanophenyl group optionally having substituent(s); X′ is (1) —Y′—CR5′R6′-Z′- wherein R5′ and R6′ are the same or different and each is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom or a group via a sulfur atom, or —CR5′R6′— is —C(alkylidene)-; Y′ is a bond, —COCO—, —CONH—, —COCONH— or —O—; and Z′ is a bond, —CH2—, —CONH—, —O—, —OCH2—, —S—, —SO—, —SO2—, —CON(C6H5)— or (2) —CO(CONH)n— wherein n is 0 or 1, (3) —NHCO—, (4) —CONH—, (5) —O—, (6) —CH═CH— or (7) —O(C1-3 alkylene)O—; (excluding the compounds indicated to be excluded from the specification), or a salt thereof.
摘要翻译: 本发明的目的在于提供一种新的吡唑衍生物和含有它们的药剂。 本发明提供由式(I')表示的化合物,其中R 1'为(1)氢原子,(2)通过碳原子的基团,(3)通过氮原子的基团,(4) 通过氧原子或(5)经由硫原子的基团; R2'是任选具有取代基的芳环基团; R 3'为(1)氢原子,(2)经由碳原子的基团,(3)经由氮原子的基团,(4)经由氧原子的基团或(5)经由硫原子的基团; R4'是任选具有取代基的氰基苯基; X'为(1)-Y'-CR5'R6'-Z'-,其中R5'和R6'相同或不同,各自为氢原子,经由碳原子的基团,经由氮原子的基团, 一个经由氧原子或一个经由硫原子的基团,或-CR 5'R 6' - 是-C(亚烷基) - ; Y'是键,-COCO - , - CONH-,-COCONH-或-O-; 并且Z'为键,-CH 2 - , - CONH - , - O - , - OCH 2 - , - S - , - SO - , - SO 2 - , - CON(C 6 H 5) - 或(2)-CO 其中n为0或1,(3)-NHCO-,(4)-CONH-,(5)-O-,(6)-CH-CH-或(7)-O(C1-3亚烷基) O-; (不包括表示从说明书中排除的化合物)或其盐。
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公开(公告)号:US08470859B2
公开(公告)日:2013-06-25
申请号:US12446960
申请日:2007-10-22
申请人: Masato Yoshida , Tomohiko Suzaki , Yasuhisa Kohara , Haruhiko Kuno , Hiroshi Nagabukuro , Reiko Saikawa , Yuuichi Okabe , Shigemitsu Imai
发明人: Masato Yoshida , Tomohiko Suzaki , Yasuhisa Kohara , Haruhiko Kuno , Hiroshi Nagabukuro , Reiko Saikawa , Yuuichi Okabe , Shigemitsu Imai
IPC分类号: C07D213/78 , A61K31/44
CPC分类号: C07D213/82 , C07D401/06 , C07D405/06 , C07D409/06
摘要: Provided are an iminopyridine derivative having a selective α1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an α1D adrenergic receptor antagonistic action. An α1D adrenergic receptor antagonist containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an α1D adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.
摘要翻译: 提供具有选择性α1D肾上腺素能受体拮抗作用并可用作预防或治疗下尿路疾病等的药物的亚氨基吡啶衍生物和具有α1D肾上腺素能受体拮抗作用的化合物的筛选方法。 含有由下式表示的化合物的α1D肾上腺素能受体拮抗剂:其中每个符号如说明书中所定义,或其盐,以及筛选具有α1D肾上腺素能受体拮抗作用的药物用于预防或治疗 下尿路疾病,其中包括测量膀胱出口梗阻大鼠膀胱平滑肌张力。
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公开(公告)号:US20090270359A1
公开(公告)日:2009-10-29
申请号:US12199008
申请日:2008-08-27
申请人: Mitsuhiro ITO , Tomohiko SUZAKI , Satoshi YAMAMOTO
发明人: Mitsuhiro ITO , Tomohiko SUZAKI , Satoshi YAMAMOTO
IPC分类号: A61K31/415 , C07D231/12 , C07D413/08 , A61K31/5377 , C07D413/14
CPC分类号: C07D231/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/10 , C07D417/14 , C07D495/04
摘要: The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) wherein R1 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R2 is a phenyl group having cyano (the phenyl group may further have substituent(s) other than cyano); R3 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R4 is a cyclic group optionally having substituent(s); and X is methylene optionally having substituent(s), or CO, or a salt thereof.
摘要翻译: 本发明提供了一种新的吡唑衍生物和含有该衍生物的雄激素受体拮抗剂。 本发明提供由式(I')表示的化合物,其中R 1是氢原子,经由碳原子的基团,经由氮原子的基团,经由氧原子的基团,或经由硫原子的基团; R2是具有氰基的苯基(苯基可以进一步具有除氰基以外的取代基); R3是氢原子,通过碳原子的基团,经由氮原子的基团,经由氧原子的基团,或经由硫原子的基团; R4是任选具有取代基的环状基团; 并且X是任选具有取代基的亚甲基,或CO或其盐。
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公开(公告)号:US20100227846A1
公开(公告)日:2010-09-09
申请号:US12675748
申请日:2008-08-27
申请人: Mitsuhiro Ito , Tomohiko Suzaki , Satoshi Tamamoto
发明人: Mitsuhiro Ito , Tomohiko Suzaki , Satoshi Tamamoto
IPC分类号: A61K31/4155 , C07D231/12 , A61P35/00 , C07D403/06 , C07D401/06 , A61K31/4439 , C07D417/06 , A61K31/427 , C07D413/10 , A61K31/5377
CPC分类号: C07D231/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/10 , C07D417/14 , C07D495/04
摘要: The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) wherein R1 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R2 is a phenyl group having cyano (the phenyl group may further have substituent(s) other than cyano); R3 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R4 is a cyclic group optionally having substituent(s); and X is methylene optionally having substituent(s), or CO, or a salt thereof.
摘要翻译: 本发明提供了一种新的吡唑衍生物和含有该衍生物的雄激素受体拮抗剂。 本发明提供由式(I')表示的化合物,其中R 1是氢原子,经由碳原子的基团,经由氮原子的基团,经由氧原子的基团,或经由硫原子的基团; R2是具有氰基的苯基(苯基可以进一步具有除氰基以外的取代基); R3是氢原子,通过碳原子的基团,经由氮原子的基团,经由氧原子的基团,或经由硫原子的基团; R4是任选具有取代基的环状基团; 并且X是任选具有取代基的亚甲基,或CO或其盐。
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公开(公告)号:US20100016315A1
公开(公告)日:2010-01-21
申请号:US12446960
申请日:2007-10-22
申请人: Masato Yoshida , Tomohiko Suzaki , Yasuhisa Kohara , Haruhiko Kuno , Hiroshi Nagabukuro , Reiko Saikawa , Yuuichi Okabe , Shigemitsu Imai
发明人: Masato Yoshida , Tomohiko Suzaki , Yasuhisa Kohara , Haruhiko Kuno , Hiroshi Nagabukuro , Reiko Saikawa , Yuuichi Okabe , Shigemitsu Imai
IPC分类号: A61K31/5377 , C07D213/78 , A61K31/44 , C07D413/10 , A61P13/02 , C12Q1/02
CPC分类号: C07D213/82 , C07D401/06 , C07D405/06 , C07D409/06
摘要: Provided are an iminopyridine derivative having a selective α1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an α1D adrenergic receptor antagonistic action. An α1D adrenergic receptor antagonist containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an α1D adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.
摘要翻译: 提供具有选择性α1D肾上腺素能受体拮抗作用并可用作预防或治疗下尿路疾病等的药物的亚氨基吡啶衍生物和具有α1D肾上腺素能受体拮抗作用的化合物的筛选方法。 含有由下式表示的化合物的α1D肾上腺素能受体拮抗剂:其中每个符号如说明书中所定义,或其盐,以及筛选具有α1D肾上腺素能受体拮抗作用的药物用于预防或治疗 下尿路疾病,其中包括测量膀胱出口梗阻大鼠膀胱平滑肌张力。
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公开(公告)号:US06357390B1
公开(公告)日:2002-03-19
申请号:US09423590
申请日:1999-11-11
IPC分类号: A01K6100
CPC分类号: H05C1/04
摘要: An electric screen device for preventing creatures from intruding into a water channel, which comprises a pair of opposed electrode assemblies disposed on opposite sides of a water intake channel, and a dc pulse applying device 13 for applying dc pulses between the electrode assemblies. In such electric screen device, the product of the peak value of the intensity of an electric field produced between the electrode assemblies by the dc pulse applying device and the body length of creatures to be prevented from intrusion into the water channel is not less than 0.1 V, the dc pulse applying time is within the range of 2-200 msec, and the duty factor of the dc pulse is not more than 0.5.
摘要翻译: 一种用于防止生物侵入水通道的电动屏幕装置,其包括设置在进水通道的相对侧上的一对相对的电极组件,以及用于在电极组件之间施加直流脉冲的直流脉冲施加装置13。 在这种电动屏幕装置中,通过直流脉冲施加装置在电极组件之间产生的电场强度的峰值与防止入侵到水通道的生物的身体长度的乘积不小于0.1 V,直流脉冲施加时间在2-200毫秒的范围内,直流脉冲的占空比不大于0.5。
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公开(公告)号:US4469572A
公开(公告)日:1984-09-04
申请号:US241651
申请日:1981-03-09
申请人: Yasuo Kimoto , Masahiko Yamamoto , Katsunori Tamiya , Yoshihito Sakai , Akio Komura , Shoichi Honda , Hidehiko Maehata , Hiroshi Kamada , Tomohiko Suzaki , Tomoya Inoue
发明人: Yasuo Kimoto , Masahiko Yamamoto , Katsunori Tamiya , Yoshihito Sakai , Akio Komura , Shoichi Honda , Hidehiko Maehata , Hiroshi Kamada , Tomohiko Suzaki , Tomoya Inoue
摘要: The present invention discloses a method of continuously processing a ribbonlike material. The method is characterized by comprising a preliminary polishing step in which surface defects of a material pulled out from an uncoiler are removed and the surface of the material is semi-finished by abrasion in combination with electrolytic polishing, a final polishing step in which the surface of the material is mirror-finished by abrasion in combination with electrolytic polishing, a washing and drying step in which the material is washed and dried with extraneous matter on the surface of the material washingly removed, a surface inspection step in which the thus finished surface of the material is inspected as to surface roughness and defects, a surface protection step in which a protective film is applied to the finished surface of the material, and a press step in which the material is cut into a predetermined size.According to the present invention, processes of mirror-finishing the surface of a ribbonlike material pulled out from an uncoiler and cutting such material into a predetermined size are continuously performed in an efficient and automatic manner.
摘要翻译: 本发明公开了一种连续处理带状材料的方法。 该方法的特征在于包括初步抛光步骤,其中从开卷机拉出的材料的表面缺陷被去除并且材料的表面通过与电解抛光相结合的磨蚀而半成品,最终研磨步骤,其中表面 的材料通过与电解抛光结合的磨损进行镜面抛光,洗涤和干燥步骤,其中材料在被清除的材料的表面上用外来物质洗涤和干燥,表面检查步骤,其中这样完成的表面 检查材料的表面粗糙度和缺陷,将保护膜施加到材料的成品表面的表面保护步骤,以及将材料切割成预定尺寸的压制步骤。 根据本发明,从开卷机拉出的带状材料的表面的镜面精加工和将这种材料切割成预定尺寸的方法以有效和自动的方式连续进行。
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公开(公告)号:US4421624A
公开(公告)日:1983-12-20
申请号:US244619
申请日:1981-03-17
申请人: Yasuo Kimoto , Masahiko Yamamoto , Katsunori Tamiya , Yoshihito Sakai , Akio Komura , Shoichi Honda , Hidehiko Maehata , Hiroshi Kamada , Tomohiko Suzaki , Tomoya Inoue
发明人: Yasuo Kimoto , Masahiko Yamamoto , Katsunori Tamiya , Yoshihito Sakai , Akio Komura , Shoichi Honda , Hidehiko Maehata , Hiroshi Kamada , Tomohiko Suzaki , Tomoya Inoue
摘要: The present application discloses an equipment for continuously processing a band-shape material comprising transverse sliding shafts disposed on a base table, a basal board which freely slides transversely along said transverse sliding shafts, transverse-feeding means by which said basal board is quickly and/or slowly moved transversely, vertical sliding shafts disposed on said basal board, a tool of abrasion in combination with elctrolytic polishing which freely slides vertically along said vertical sliding shafts, vertical-feeding means by which said tool is moved vertically against said basal board and a polishing head which is disposed on said tool and composed of electrodes for electrolysis and abrasive matters for abrasion and by which continuously sent band-shape material is polished. In the case a band-shape material being conveyed is continuously polished for many hours, worn-out abrasive matters may be exchanged without interrupting the conveyance of said band-shape material, improving the working efficiency thereby.
摘要翻译: 本申请公开了一种用于连续加工带状材料的设备,包括设置在基台上的横向滑动轴,沿着所述横向滑动轴横向滑动的基板,横向进给装置,所述基板快速地和/ 或横向缓慢移动,设置在所述基板上的垂直滑动轴,与所述垂直滑动轴垂直滑动的电解抛光组合的磨损工具,垂直进给装置,所述工具垂直于所述基板移动, 抛光头,其设置在所述工具上,由用于电解的电极和磨料用磨料构成,并且连续送出的带状材料被抛光。 在输送的带状材料连续抛光多个小时的情况下,可以更换磨损的磨料,而不会中断所述带状材料的输送,从而提高工作效率。
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