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公开(公告)号：US5663298A
公开(公告)日：1997-09-02
申请号：US730348
申请日：1996-10-15
申请人： Tamio Mizukami , Akira Asai , Yoshinori Yamashita , Ritsuko Katahira , Atsuhiro Hasegawa , Keiko Ochiai , Shiro Akinaga
发明人： Tamio Mizukami , Akira Asai , Yoshinori Yamashita , Ritsuko Katahira , Atsuhiro Hasegawa , Keiko Ochiai , Shiro Akinaga
CPC分类号： C07K5/06026 , A61K38/00
摘要： The present invention relates to UCK14 compounds having antitumor activity which are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or --COOC(CH.sub.3).sub.3 ; and R.sup.2 and R.sup.3 are taken together to form --CH.sub.2 --, or each R.sup.2 and R.sup.3 independently are hydrogen,and pharmaceutically acceptable salts thereof.
摘要翻译： 本发明涉及具有抗肿瘤活性的UCK14化合物，其由下式表示：其中R 1为氢或-COOC（CH 3）3; 并且R 2和R 3一起形成-CH 2 - ，或每个R 2和R 3独立地是氢，及其药学上可接受的盐。
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公开(公告)号：US5407930A
公开(公告)日：1995-04-18
申请号：US217023
申请日：1994-03-24
IPC分类号： C07D501/00 , C07D501/36 , C07D501/46 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention relates to a compound represented by the structural formula I: ##STR1## its pharmaceutically acceptable salt or ester, or its crystalline, which is a novel optically active compound useful as a curing agent for bacterial infections, a process for production thereof and a use thereof.
摘要翻译： 本发明涉及由结构式I表示的化合物：其药学上可接受的盐或酯或其结晶，其是可用作细菌感染的固化剂的新型光学活性化合物， 其制备方法及其用途。
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公开(公告)号：US5403835A
公开(公告)日：1995-04-04
申请号：US476439
申请日：1990-06-07
IPC分类号： C07D501/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention relates to a compound represented by the structural formula: ##STR1## or its pharmaceutically acceptable salt or ester, which is a novel optically active compound useful as a curing agent for bacterial infections, a process for production thereof and a use thereof.
摘要翻译： PCT No.PCT / JP89 / 01155 Sec。 371日期1990年6月7日 102（e）日期1990年6月7日PCT提交1989年11月13日PCT公布。 出版物WO91 / 07410 1991年5月30日的日期。本发明涉及由结构式表示的化合物或其药学上可接受的盐或酯，其是可用作细菌固化剂的新型光学活性化合物 感染，其生产方法及其用途。
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44.发明授权
公开(公告)号：US5084453A
公开(公告)日：1992-01-28
申请号：US265458
申请日：1988-10-13
申请人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
发明人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
IPC分类号： A61K31/545 , C07D235/28 , C07D263/46 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/36 , C07D277/40 , C07D277/56 , C07D285/12 , C07D285/125 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125 , Y02P20/55
摘要： The present invention relates to a compound having the formula: ##STR1## wherein R is a hydrogen atom, a carboxyl-protecting group or a negative charge and Q is a hydrogen atom, a halogen atom, a hydroxyl group, an acetoxy group, a carbamoyl group, an azide group, a substituted or unsubstituted quarternary ammonio group or a substituted or unsubstituted heterocyclic thio group having at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or a non-toxic salt or physiologically hydrolyzable non-toxic ester thereof; a process for producing it; and an antibacterial agent comprising it as an active ingredient.Further, the present invention also relates to a compound having the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or an amino-protecting group, and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a carboxyl-protecting group, or a salt thereof; and a process for producing it.
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公开(公告)号：US4117435A
公开(公告)日：1978-09-26
申请号：US801999
申请日：1977-05-31
申请人： Yukio Hishida , Yuichi Asai , Toshikatsu Kondo , Akira Asai , Atsuo Sakaida , Chiaki Miyazawa
发明人： Yukio Hishida , Yuichi Asai , Toshikatsu Kondo , Akira Asai , Atsuo Sakaida , Chiaki Miyazawa
摘要： A flap-armature electromagnet comprises a U-shaped yoke, a pole core, a coil, a flap-armature, a compression spring and a coil spring. The flap-armature is rockingly supported on the yoke by means of projections formed at the upper rear end of the yoke and notches formed at both sides of the flap-armature. Each end of the coil spring is connected to each of the projections for pressing the flap-armature on a rocking axis of the flap-armature.
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46.发明授权STAT3 inhibitor containing quinolinecarboxamide derivative as active ingredient 有权含有喹啉甲酰胺衍生物的STAT3抑制剂作为活性成分公开(公告)号：US08466290B2
公开(公告)日：2013-06-18
申请号：US13003441
申请日：2009-07-10
申请人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Takane Yokotagawa , Osamu Takahashi , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
发明人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Takane Yokotagawa , Osamu Takahashi , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , A61K31/4709 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides a STATS inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and R1 to R8 and R34 each represent H, halogen, alkyl, phenyl, furyl, thienyl, or the like), or a pharmacologically acceptable salt thereof.
摘要翻译： 本发明提供含有作为活性成分的式（I）所示的喹啉甲酰胺衍生物的STATS抑制剂（式中，W表示键或亚烷基链; X表示O，S或NR34; R1〜R8 和R 34各自表示H，卤素，烷基，苯基，呋喃基，噻吩基等）或其药理学上可接受的盐。
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公开(公告)号：US20120302524A1
公开(公告)日：2012-11-29
申请号：US13519707
申请日：2010-12-28
申请人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Osamu Takahashi , Yoshiaki Masuda , Ayumu Muroya , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
发明人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Osamu Takahashi , Yoshiaki Masuda , Ayumu Muroya , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
IPC分类号： A61K31/4245 , C07D413/14 , A61K31/4439 , C07F7/10 , A61K31/695 , A61K31/454 , A61K31/5377 , A61K31/496 , A61K31/4709 , A61K31/498 , C07D513/04 , A61K31/4545 , A61K31/541 , A61K31/437 , C07D487/04 , A61K31/55 , A61P35/00 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04
摘要： Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
摘要翻译： 提供具有STAT3抑制活性并可用作抗癌剂的1,3,4-恶二唑-2-甲酰胺化合物。 提供由式（I）表示的1,3,4-恶二唑-2-甲酰胺化合物或其药学上可接受的盐（在该式中，Ar表示呋喃基等; R 1表示氢原子等; -X-Y表示二苯基等二芳基）。
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公开(公告)号：US07676350B2
公开(公告)日：2010-03-09
申请号：US11778367
申请日：2007-07-16
CPC分类号： G06F17/11
摘要： In an optimum design method comprising a first solution determining step of solving an optimization problem of a first evaluation function for a state variable vector with a design variable vector being as a parameter, and a second solution determining step of solving an optimization problem of a second evaluation function for the design variable vector and the state variable vector thus obtained, the second solution determining step includes the steps of computing a gradient vector of the second evaluation function for the design variable vector, computing a first coefficient based on a value of a norm of the gradient vector, computing a search vector based on the first coefficient, computing a second coefficient, and updating the design variable vector based on the second coefficient. The second coefficient computing step includes the first solution determining step, the first solution determining step is executed as an iterative method based on the gradient vector, and the state variable vector is not initialized during iteration. The optimum design method is precisely adaptable for structural changes.
摘要翻译： 一种最优设计方法，包括：第一解决方案确定步骤，用于以设计变量向量作为参数来求解用于状态变量向量的第一评估函数的优化问题;以及第二解决方案确定步骤，用于求解第二 第二解决方案确定步骤包括以下步骤：计算用于设计变量向量的第二评估函数的梯度向量，基于规范的值计算第一系数;对于设计变量向量和状态变量向量的评估函数， 的梯度向量，基于第一系数计算搜索向量，计算第二系数，并且基于第二系数更新设计变量向量。 第二系数计算步骤包括第一解决方案确定步骤，基于梯度向量作为迭代方法执行第一解决方案确定步骤，并且在迭代期间不初始化状态变量向量。 最佳设计方法适用于结构变化。
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49.发明申请METHOD FOR DETERMINATION OF RECOGNITION SPECIFICITY OF VIRUS FOR RECEPTOR SUGAR CHAIN 审中-公开用于确定受体糖链的病毒识别特异性的方法公开(公告)号：US20090269734A1
公开(公告)日：2009-10-29
申请号：US12427636
申请日：2009-04-21
申请人： Yasuo SUZUKI , Akira Asai , Takashi Suzuki , Ilpal Jwa , Takeomi Murata , Taiichi Usui , Sou Takeda , Kohei Yamada , Toshitada Noguchi
发明人： Yasuo SUZUKI , Akira Asai , Takashi Suzuki , Ilpal Jwa , Takeomi Murata , Taiichi Usui , Sou Takeda , Kohei Yamada , Toshitada Noguchi
CPC分类号： G01N33/548 , G01N33/56983
摘要： A method in which the recognition specificity of a virus for a receptor sugar chain can be easily determined with a simple instrument or apparatus is provided. In a method for determining the recognition specificity of a virus for a receptor sugar chain or for determining the change in a host infected in accordance with the mutation of virus comprising, a sample of the virus is brought into contact with a support having a polymer with sialo-oligosaccharide immobilized on the surface thereof; and the degree of binding therein is assayed to determine the recognition specificity of said virus for said receptor sugar chain and to determine the change in a host range. The method is suitable for the surveillance of virus.
摘要翻译： 提供了利用简单的仪器或装置容易地确定病毒对受体糖链的识别特异性的方法。 在用于确定受体糖链病毒的识别特异性或根据病毒突变感染的宿主的变化的方法中，使病毒样品与具有聚合物的载体接触， 唾液酸寡糖固定在其表面上; 并测定其中的结合程度以确定所述病毒对所述受体糖链的识别特异性并确定宿主范围的变化。 该方法适用于病毒监控。
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公开(公告)号：US07587375B2
公开(公告)日：2009-09-08
申请号：US11075593
申请日：2005-03-09
CPC分类号： G06F17/11
摘要： The solution of a constrained optimization problem is easily solved by linearly approximating a point of interest to a first hypersurface given as a constraint and finding the extreme value of the objective function by moving a point r along a curved line having second-order osculation with the geodetic line of a hypersurface S(r)=c and passing through the point r.
摘要翻译： 约束优化问题的解可以通过线性近似给定为约束的第一超曲面的兴趣点来容易地解决，并且通过沿着具有二阶交调的曲线沿着具有二阶交变的曲线移动点r来找到目标函数的极值 超表面S（r）= c并通过点r的大地测量线。
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