公开(公告)号：US4889858A

公开(公告)日：1989-12-26

申请号：US180104

申请日：1988-02-17

申请人： Hitoshi Uno ,  Mikio Kurokawa ,  Fuminori Sato ,  Shunsuke Naruto ,  Yoshinobu Masuda

发明人： Hitoshi Uno ,  Mikio Kurokawa ,  Fuminori Sato ,  Shunsuke Naruto ,  Yoshinobu Masuda

IPC分类号： C07D313/12 ,  C07D401/12 ,  C07D409/12

CPC分类号： C07D401/12 ,  C07D313/12 ,  C07D409/12

摘要： The present invention relates to compounds represented by the general formula (I): ##STR1## wherein R.sub.1 is H or methoxy, R.sub.2 is H, methoxy, OH or F, R.sub.3 is H or F, R.sub.4 is H or F at 7-, 8- or 9-position, and .circle.Ar is a benzene, thiophene or pyridine ring, provided that (i) at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, (ii) R.sub.2 or R.sub.3 is F when R.sub.4 is F, (iii) R.sub.1, R.sub.3 and R.sub.4 are H when R.sub.2 is methoxy or OH, (iv) R.sub.2 and R.sub.3 are not simultaneously F, and (v) R.sub.2 and R.sub.3 are H or F, and both R.sub.1 and R.sub.4 are H when .circle.Ar is a thiophene or pyridine ring, or a physiologically acceptable acid addition salt thereof. The compounds of the present invention have an excellent protective effect against cerebral anoxia and some of them have also an inhibitory effect on lipid peroxidation of mitochondrial membrane of brain and an anti-convulsant activity and are useful as an agent for prevention or treatment of cerebral diseases caused by hypoxia in mammals including human.

公开(公告)号：US3948928A

公开(公告)日：1976-04-06

申请号：US340195

申请日：1973-03-12

申请人： Haruki Nishimura ,  Masanao Shimizu ,  Hitoshi Uno ,  Tetsuo Hirooka ,  Yoshinobu Masuda ,  Mikio Kurokawa

发明人： Haruki Nishimura ,  Masanao Shimizu ,  Hitoshi Uno ,  Tetsuo Hirooka ,  Yoshinobu Masuda ,  Mikio Kurokawa

IPC分类号： A61K31/42 ,  C07D261/20

CPC分类号： A61K31/42 ,  C07D261/20

摘要： 3-Substituted-1,2-benzisoxazole derivative of the following formula: ##SPC1##Wherein R.sub.1 is hydrogen, hydroxy, nitro, alkyl, alkoxy, halogen or amino; R.sub.2 is hydroxyamino, amino, hydrazino, mono- or di- alkyl substituted amino, aralkylamino, acyloxyamino, morpholino, piperazine which is unsubstituted or substituted with alkyl, aralkyl or aryl at 4 position, or pyrrolidino, or R.sub.2 may combine with imino group and form together with the adjacent carbon atom a heterocyclic ring such as imidazoline or tetrahydropyrimidine; and n is an integer of 0 to 3, and its pharmaceutically acceptable acid addition salt, and preparation thereof. The present compounds show valuable pharmacological properties, such as anti-reserpine activity, central nervous depressing activity, anti-hypertensive activity and l-dopa potentiating activity.

摘要翻译： 3-取代的1,2-苯并异恶唑衍生物：

公开(公告)号：US4172896A

公开(公告)日：1979-10-30

申请号：US912857

申请日：1978-06-05

申请人： Hitoshi Uno ,  Mikio Kurokawa ,  Yoshinobu Masuda

发明人： Hitoshi Uno ,  Mikio Kurokawa ,  Yoshinobu Masuda

IPC分类号： C07D261/20 ,  C07D263/56 ,  A61K31/42

CPC分类号： C07D263/56 ,  C07D261/20

摘要： Methane-sulfonamide derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group: --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y,and an alkali metal salt thereof, and a process for the preparation of said methane-sulfonamide derivatives. Said compounds have an excellent anticonvulsant activity and are useful as anticonvulsants for controlling convulsions and seizures in patients with epilepsy.

摘要翻译： 下式的甲磺酰胺衍生物：其中R 1是氢或卤素原子，R 2和R 3相同或不同，各自为氢或具有1至3个碳原子的直链或支链烷基， 的X和Y是碳原子，另一个是氮原子，条件是：-CH 2 SO 2 NR 2 R 3基团与X和Y中的任一个的碳原子键合，及其碱金属盐，以及制备所述 甲磺酰胺衍生物。 所述化合物具有优异的抗惊厥活性，可用作控制癫痫患者惊厥和癫痫发作的抗惊厥药。

公开(公告)号：US5128354A

公开(公告)日：1992-07-07

申请号：US499444

申请日：1990-06-25

申请人： Yoshinobu Masuda ,  Toshiaki Kadokawa ,  Mikio Kurokawa ,  Kayoko Zushi ,  Yoshiaki Ochi

发明人： Yoshinobu Masuda ,  Toshiaki Kadokawa ,  Mikio Kurokawa ,  Kayoko Zushi ,  Yoshiaki Ochi

IPC分类号： A61K31/42 ,  C07D261/20

CPC分类号： A61K31/42 ,  C07D261/20

摘要： The present invention provides an agent for treating ischemic brain damage comprising 3-sulfamoylmethyl-1,2-benzisoxazole or its alkali metal salt as an active ingredient. This agent can be used for the prevention and/or treatment of cerebral ischemia-induced intracranial diseases or various symptoms associated therewith in mammals including human beings.

公开(公告)号：US6008679A

公开(公告)日：1999-12-28

申请号：US730058

申请日：1996-10-15

申请人： Yoshinobu Masuda

发明人： Yoshinobu Masuda

IPC分类号： H01L21/822 ,  H01L27/04 ,  H03F1/26 ,  H03F3/343 ,  H03F3/45 ,  H03K3/353 ,  H03K3/3565 ,  H03K5/08 ,  H03K3/295

CPC分类号： H03K3/3565

摘要： A Schmitt trigger circuit has an input device and an amplifier. The input device has a current adder device having a P-type current mirror circuit and a N-type current mirror circuit connected in parallel. The P-type current mirror circuit has a positive constant current source for converting an external input signal to a positive constant current and a first output current control transistor for controlling an output current from the positive constant current source. The N-type current mirror circuit has a negative constant current source for converting the external input signal to a negative constant current and a second output current control transistor for controlling an output current from the negative constant current source. The amplifier amplifies the output signal from the input device and generates the feed-back control signal to be used for controlling and driving the first output current control transistor and the second output current control transistor.

摘要翻译： 施密特触发电路具有输入装置和放大器。 输入装置具有并联连接的P型电流镜电路和N型电流镜电路的电流加法器装置。 P型电流镜电路具有用于将外部输入信号转换为正恒定电流的正恒流源和用于控制来自正恒流源的输出电流的第一输出电流控制晶体管。 N型电流镜电路具有用于将外部输入信号转换为负的恒定电流的负的恒定电流源和用于控制来自负的恒定电流源的输出电流的第二输出电流控制晶体管。 放大器放大来自输入装置的输出信号，并产生用于控制和驱动第一输出电流控制晶体管和第二输出电流控制晶体管的反馈控制信号。

公开(公告)号：US07892821B2

公开(公告)日：2011-02-22

申请号：US11307692

申请日：2006-02-17

申请人： Setsuo Watanabe ,  Yoshinobu Masuda ,  Shuji Inagaki

发明人： Setsuo Watanabe ,  Yoshinobu Masuda ,  Shuji Inagaki

IPC分类号： C12M1/00 ,  C12M3/00 ,  C12M1/22 ,  B01L3/00

CPC分类号： C12M41/00 ,  C12M23/04

摘要： A culture chamber which cultivates a culture object by using a culture liquid has a culture space part which houses the culture object together with the culture liquid, an introducing part (an introducing port) which introduces the culture liquid into the culture space part, a discharging part (a discharging port) which discharges the culture liquid from the culture space part, and a flow arrangement part (a vertical wall, a small space part). The flow arrangement part is formed in a side of the introducing part of the culture space part, and causes a liquid flow, which reaches to the discharging part, to the culture liquid introduced into the culture space part from the introducing part by diffusing from inner wall surfaces of the culture space part toward a direction which intersects a virtual line connecting the introducing part and the discharging part.

摘要翻译： 通过培养液培养培养物的培养室具有将培养物与培养液一起容纳的培养空间部分，将培养液引入培养空间部的引入部（引入口），放出 从培养空间部排出培养液的部分（排出口），流动配置部（垂直壁，小空间部）。 流动布置部分形成在培养空间部分的引入部分的一侧，并且通过从内部扩散而导致从引入部分引入到培养空间部分的培养液到达排出部分的液体流动 培养空间部分的壁表面朝与连接引入部分和排出部分的虚拟线相交的方向。

公开(公告)号：US4499085A

公开(公告)日：1985-02-12

申请号：US490223

申请日：1983-04-29

申请人： Yoshinobu Masuda

发明人： Yoshinobu Masuda

IPC分类号： A61K31/34 ,  A61K31/40 ,  A61K31/557 ,  A61K47/48 ,  C07C405/00 ,  A61K31/70

CPC分类号： B82Y5/00 ,  A61K31/34 ,  A61K31/40 ,  A61K31/557 ,  A61K47/48969 ,  C07C405/00

摘要： The invention provides a new method for the treatment of anoxia of brain cells using a PGI.sub.1 derivative of the formula: ##STR1## wherein R.sub.1 represents hydrogen or lower alkyl and R.sub.2 represents 2-methylhexyl, 3-propylcyclopentyl, 3-butylcyclopentyl or 4-propylcyclohexyl, a PGI.sub.2 derivative of the formula: ##STR2## wherein R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents 2-methylhexyl, cyclopentyl, 3-propylcyclopentyl, or cyclohexyl, a PGI.sub.2 derivative of the formula: ##STR3## wherein R.sub.5 represents lower alkyl and R.sub.6 represents pentyl, 1-methylpentyl, 1-methyl-5-chloropentyl, 2-methyl-5-chloropentyl, 3-ethylcyclopentyl, 3-propylcyclopentyl, 3-butylcyclopentyl, 3-(2-chloroethyl)cyclopentyl, cyclohexyl, 4-ethylcyclohexy, or cyclohexylmethyl or a PGE.sub.1 derivative of the formula: ##STR4## wherein X represents methylene or carbonyl and (i) when X represents methylene, Y represents ethylene or trans-vinylene, R.sub.7 represents carboxy or lower alkoxycarbonyl and R.sub.8 represents 2-methylhexyl or 1-cyclohexylethyl and (ii) when X represents carbonyl, Y represents ethylene, R.sub.7 represents carboxyl, lower alkoxycarbonyl, glycoloyl or hydroxymethyl and R.sub.8 represents 2-methylhexyl, cyclopentyl, 3-propylcyclopentyl, or 3-butylcyclopentyl or a cyclodextrin clathrate or non-toxic salt thereof.

摘要翻译： 本发明提供了一种使用下式的PGI1衍生物治疗脑细胞的新方法：其中R1代表氢或低级烷基，R2代表2-甲基己基，3-丙基环戊基，3-丁基环戊基或 4-丙基环己基，下式的PGI 2衍生物：其中R 3表示氢或低级烷基，R 4表示2-甲基己基，环戊基，3-丙基环戊基或环己基，具有下式的PGI 2衍生物：＆lt; IMAGE＆gt; （III）其中R5代表低级烷基，R6表示戊基，1-甲基戊基，1-甲基-5-氯戊基，2-甲基-5-氯戊基，3-乙基环戊基，3-丙基环戊基，3-丁基环戊基，3-（2- （IV）其中X表示亚甲基或羰基，（i）当X表示亚甲基时，Y表示亚乙基或反式亚乙烯基，R 7表示亚乙基或反式亚乙烯基，R 7表示亚乙基， 表示羧基或低级烷氧基羰基，R 8表示2- 甲基己基或1-环己基乙基，和（ii）当X表示羰基时，Y表示乙烯，R7表示羧基，低级烷氧基羰基，乙酰氧基或羟甲基，R8表示2-甲基己基，环戊基，3-丙基环戊基或3-丁基环戊基或环糊精包合物或 无毒盐。

公开(公告)号：US4812475A

公开(公告)日：1989-03-14

申请号：US935153

申请日：1986-11-25

申请人： Yoshinobu Masuda

发明人： Yoshinobu Masuda

IPC分类号： C08B37/16 ,  A61K31/40 ,  A61K31/403 ,  A61K31/557 ,  A61K47/40 ,  A61P3/00 ,  A61P9/00 ,  A61P25/28 ,  A61P43/00 ,  C07C35/08 ,  C07C35/17 ,  C07C51/08 ,  C07C61/08 ,  C07C405/00 ,  C07D209/52 ,  C07D309/12 ,  C07F9/40

CPC分类号： C07F9/4018 ,  A61K31/40 ,  A61K31/557 ,  C07C309/00 ,  C07C35/08 ,  C07C35/17 ,  C07C405/00 ,  C07C51/08 ,  C07C61/08 ,  C07D209/52 ,  C07D309/12

摘要： The invention relates to a new method for the treatment of anoxia of brain cells using a PGI.sub.1 derivative of the formula: ##STR1## (wherein R represents an alkyl group of 1 to 4 carbon atoms.) or cyclodextrin clathrates thereof, or non-toxic salts thereof.

摘要翻译： 本发明涉及使用下式的PGI1衍生物治疗脑细胞缺氧的新方法：其中R表示1至4个碳原子的烷基或其环糊精包合物，或 无毒盐。

公开(公告)号：US20070020750A1

公开(公告)日：2007-01-25

申请号：US11307692

申请日：2006-02-17

申请人： Setsuo Watanabe ,  Yoshinobu Masuda ,  Shuji Inagaki

发明人： Setsuo Watanabe ,  Yoshinobu Masuda ,  Shuji Inagaki

IPC分类号： C12M3/00

CPC分类号： C12M41/00 ,  C12M23/04

摘要： A culture chamber which cultivates a culture object by using a culture liquid has a culture space part which houses the culture object together with the culture liquid, an introducing part (an introducing port) which introduces the culture liquid into the culture space part, a discharging part (a discharging port) which discharges the culture liquid from the culture space part, and a flow arrangement part (a vertical wall, a small space part). The flow arrangement part is formed in a side of the introducing part of the culture space part, and causes a liquid flow, which reaches to the discharging part, to the culture liquid introduced into the culture space part from the introducing part by diffusing from inner wall surfaces of the culture space part toward a direction which intersects a virtual line connecting the introducing part and the discharging part.

摘要翻译： 使用培养液培养培养物的培养室具有将培养物与培养液一起容纳的培养空间部，将培养液引入培养空间部的导入部（引入口），放出 从培养空间部排出培养液的部分（排出口），流动配置部（垂直壁，小空间部）。 流动布置部分形成在培养空间部分的引入部分的一侧，并且通过从内部扩散而导致从引入部分引入到培养空间部分的培养液到达排出部分的液体流动 培养空间部分的壁表面朝与连接引入部分和排出部分的虚拟线相交的方向。

公开(公告)号：US06342515B1

公开(公告)日：2002-01-29

申请号：US09582433

申请日：2000-06-26

申请人： Yoshinobu Masuda ,  Yoshiaki Ochi

发明人： Yoshinobu Masuda ,  Yoshiaki Ochi

IPC分类号： A61K3142

CPC分类号： A61K31/423 ,  A61K31/42 ,  Y10S514/878 ,  Y10S514/879

摘要： The present invention provides a medicament for neurodegenerative diseases comprising zonisamide or an alkali metal salt thereof as an active ingredient. The present medicament can be used in the prevention and treatment of neurodegenerative diseases such as Parkinson's disease, Huntington's disease, choreic syndrome and dystonic syndrome in mammals (including human).

摘要翻译： 本发明提供了包含唑尼沙胺或其碱金属盐作为活性成分的神经变性疾病的药物。 本发明的药物可用于预防和治疗哺乳动物（包括人）中的帕金森病，亨廷顿舞蹈症，乔治综合征和肌张力障碍综合征等神经变性疾病。