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28 条记录 (耗时 0.025 秒)

    2-alkynyladenosines as antihypertensive agents
    1.
    发明授权
    2-alkynyladenosines as antihypertensive agents 失效
    2-炔基腺苷作为抗高血压药

    公开(公告)号：US4956345A

    公开(公告)日：1990-09-11

    申请号：US282892

    申请日：1988-12-12

    申请人： Tadashi Miyasaka ,  Akira Matsuda ,  Toichi Abiru ,  Haruhiko Machida

    发明人： Tadashi Miyasaka ,  Akira Matsuda ,  Toichi Abiru ,  Haruhiko Machida

    IPC分类号： C07H19/167 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P9/12 ,  C07H19/067 ,  C07H19/16

    CPC分类号： C07H19/16

    摘要： A 2-alkynyladenosine represented by general formula [I]: ##STR1## wherein n is an integer of from 2 to 15, has been found to have excellent properties as an antihypertensive agent. On the basis of this finding, the present invention has provided an antihypertensive agent comprising an antihypertensive effective amount of a compound of the above formula [I] and a pharmaceutically acceptable carrier. The present invention also discloses a novel compound 2-alkynyladenosine of formula [I] shown above wherein n is 6 to 15.

    摘要翻译： 由通式[I]表示的2-炔基腺苷：其中n为2〜15的整数，已被发现具有作为抗高血压剂的优异的性质。 基于该发现，本发明提供了包含抗高血压有效量的上述式[I]的化合物和药学上可接受的载体的抗高血压药。 本发明还公开了上述式[I]的新化合物2-炔基腺苷，其中n为6至15。

    Semiconductor device
    6.
    发明授权
    Semiconductor device 失效
    半导体器件

    公开(公告)号：US5500619A

    公开(公告)日：1996-03-19

    申请号：US121470

    申请日：1993-09-16

    申请人： Tadashi Miyasaka

    发明人： Tadashi Miyasaka

    IPC分类号： H03K17/0812 ,  H03K17/082 ,  H03K17/16 ,  H03K17/687

    CPC分类号： H03K17/0822 ,  H03K17/08128 ,  H03K17/0828 ,  H03K17/163 ,  H03K17/168

    摘要： A semiconductor device includes a main insulated gate type switching element having a gate electrode and controllable by a gate voltage applied to the gate electrode, a current detecting insulated gate type switching element connected in parallel to the main insulated gate type switching element, a detecting resistor for detecting a current flowing in the current detecting insulated gate type switching element, a gate controlling element capable of controlling the gate voltage by a drop voltage in the detecting resistor, and a gate control relieving element for relieving a varying speed of the gate voltage varied based on an operation of the gate controlling element.

    摘要翻译： 一种半导体器件包括：具有栅电极且可由施加到栅电极的栅极电压控制的主绝缘栅型开关元件，与主绝缘栅型开关元件并联连接的电流检测绝缘栅型开关元件，检测电阻器 用于检测在电流检测绝缘栅型开关元件中流动的电流，能够通过检测电阻器中的下降电压来控制栅极电压的栅极控制元件和用于缓和栅极电压变化速度的栅极控制释放元件 基于门控制元件的操作。

    Snubber circuit for a power semiconductor device
    7.
    发明授权
    Snubber circuit for a power semiconductor device 失效
    用于功率半导体器件的缓冲电路

    公开(公告)号：US5343098A

    公开(公告)日：1994-08-30

    申请号：US623347

    申请日：1990-12-07

    申请人： Tadashi Miyasaka

    发明人： Tadashi Miyasaka

    IPC分类号： H03K17/16 ,  H03K17/0814 ,  H03K17/73 ,  H03K17/60 ,  H03K5/00

    CPC分类号： H03K17/08146

    摘要： A snubber circuit, for absorbing voltage spikes applied to a power semiconductor device used as a switching means, utilizes the junction capacitance of a directly connected semiconductor device, thereby avoiding the need for a separate high-voltage capacitor. Embodiments shown use either a MOSFET or a bipolar transistor with a resistor connected in parallel between the gate (base) and the source (emitter) of the MOSFET (or bipolar transistor.) The snubber circuit of the present invention may also be a module integrally formed on a radiating base of the power semiconductor device.

    摘要翻译： 用于吸收施加到用作开关装置的功率半导体器件的电压尖峰的缓冲电路利用直接连接的半导体器件的结电容，从而避免需要单独的高压电容器。 所示的实施例使用MOSFET或双极晶体管，其电阻器与栅极（基极）和MOSFET（或双极晶体管）的源极（发射极）并联连接。本发明的缓冲电路也可以是一体的模块 形成在功率半导体器件的辐射基底上。

    6-substituted acyclopyrimidine nucleoside derivatives and antiviral agents containing the same as active ingredient thereof
    8.
    发明授权
    6-substituted acyclopyrimidine nucleoside derivatives and antiviral agents containing the same as active ingredient thereof 失效
    6-取代的环丙基嘧啶核苷衍生物和含有它的活性成分的抗病毒剂

    公开(公告)号：US5112835A

    公开(公告)日：1992-05-12

    申请号：US449930

    申请日：1989-11-21

    申请人： Tadashi Miyasaka ,  Hiromichi Tanaka ,  Erik D. A. De Clercq ,  Masanori Baba ,  Richard T. Walker ,  Masaru Ubasawa

    发明人： Tadashi Miyasaka ,  Hiromichi Tanaka ,  Erik D. A. De Clercq ,  Masanori Baba ,  Richard T. Walker ,  Masaru Ubasawa

    IPC分类号： C07D239/54 ,  C07D239/60

    CPC分类号： C07D239/54 ,  C07D239/60

    摘要： 6-substitutted acyclopyrimidine nucleoside derivatives represented by the following general formula I: ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom or a group of alkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl; R.sup.2 represents a group of arylthio, alkylthio, cycloalkylthio, aryl sulfoxide, alkyl sulfoxide, cycloalkyl sulfoxide, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy; R.sup.3 represents a hydroxyalkyl group of which alkyl portion may contain an oxygen atom; X represents an oxygen or sulfur atom or amino group; Y represents an oxygen or sulfur atom; and A represents .dbd.N-- or --NH-- or pharmaceutically acceptable salts thereof, processes for their preparation and antiviral agents containing them as active ingredients.

    摘要翻译： PCT No.PCT / JP89 / 00347 Sec。 371日期：一九八九年十一月二十一日 102（e）1989年11月21日PCT PCT 1989年3月31日PCT公布。 出版物WO89 / 09213 日期：1989年10月5日，由以下通式I表示的6-取代的阿卡吡啶核苷衍生物：其中R 1表示氢或卤原子或烷基，烯基，炔基，烷基羰基，芳基羰基，芳基羰基烷基，芳硫基或芳烷基 ; R2代表芳硫基，烷硫基，环烷硫基，芳基亚砜，烷基亚砜，环烷基亚砜，烯基，炔基，芳烷基，芳基羰基，芳基羰基烷基或芳氧基; R3表示烷基部分可含有氧原子的羟烷基; X表示氧或硫原子或氨基; Y表示氧或硫原子; 并且A表示= N-或-NH-或其药学上可接受的盐，其制备方法和含有它们作为活性成分的抗病毒剂。

    Camptothecin derivatives and process for preparing same
    10.
    发明授权
    Camptothecin derivatives and process for preparing same 失效
    喜树碱衍生物及其制备方法

    公开(公告)号：US4473692A

    公开(公告)日：1984-09-25

    申请号：US413879

    申请日：1982-09-01

    申请人： Tadashi Miyasaka ,  Seigo Sawada ,  Kenichiro Nokata ,  Masahiko Mutai

    发明人： Tadashi Miyasaka ,  Seigo Sawada ,  Kenichiro Nokata ,  Masahiko Mutai

    IPC分类号： C07D491/22 ,  C07D491/147 ,  A61K31/47

    CPC分类号： C07D491/22

    摘要： New Camptothecin derivatives possessing high anti-tumor activity with slight toxicity, represented by the general formula: ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group, R.sup.2 for a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, a carboxymethyl group or an acyloxymethyl group, and R.sup.3 is the grouping --XR' (where R' is a hydrogen atom, an alkyl group or an acyl group and X is an oxygen atom or a sulfur atom), a nitro group, an amino group, an alkylamino group, an acylamino group or a halogen atom, with the proviso that when both of R.sup.1 and R.sup.2 are hydrogen atoms, R.sup.3 should not be a hydroxyl group, methoxy group or acetoxy group. These new camptothecin derivatives are prepared by treating a 5-R.sup.1 -7-R.sup.2 -camptothecin derivative with a peroxidant and then reacting the resultant 5-R.sup.1 -7-R.sup.2 -camptothecin-1-oxide with an active hydrogen compound under irradiation of UV-rays or by catalytically hydrogenating the ring B of camptothecin in a solvent, treating the resultant tetrahydro product with an acylating agent, introducing a nitro group into the 10-position of the acylated product by the reaction with nitric acid, splitting off the acyl group in the 10-nitro product by hydrolysis and treating the hydrolyzed tetrahydro product with an oxidizing agent for dehydrogenation, and if desired, reducing the nitro group in the resulting product to an amino group and modifying the amino group by N-alkylation, N-acylation or by diazotization followed by hydrolysis or the Sandmeyer reaction, before or after the oxidation of the 10-nitro-tetrahydro product.

    摘要翻译： 新的喜树碱衍生物具有高毒性的抗肿瘤活性，由以下通式表示：其中R1是氢原子，烷基，羟基，烷氧基或酰氧基，R2代表氢原子 ，烷基，芳烷基，羟甲基，羧甲基或酰氧基甲基，R3为分组-XR'（其中R'为氢原子，烷基或酰基，X为氧 原子或硫原子），硝基，氨基，烷基氨基，酰氨基或卤素原子，条件是当R 1和R 2均为氢原子时，R 3不应为羟基，甲氧基 基团或乙酰氧基。 这些新的喜树碱衍生物通过用过氧化物处理5-R1-7-R2-喜树碱衍生物，然后使所得的5-R1-7-R2-喜树碱-1-氧化物与活性氢化合物在UV- 或通过在溶剂中催化氢化喜树碱的环B，用酰化剂处理所得的四氢产物，通过与硝酸的反应将硝基引入到酰化产物的10-位，将酰基分成 该10-硝基产物通过水解和用脱氢的氧化剂处理水解的四氢产物，如果需要，将所得产物中的硝基还原成氨基并通过N-烷基化，N-酰化或 通过重氮化随后水解或Sandmeyer反应，在10-硝基 - 四氢产物的氧化之前或之后。