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31 条记录 (耗时 0.036 秒)

    OXYIMINO COMPOUNDS AND THE USE THEREOF
    2.
    发明申请
    OXYIMINO COMPOUNDS AND THE USE THEREOF 有权
    OXYIMINO化合物及其用途

    公开(公告)号：US20100240703A1

    公开(公告)日：2010-09-23

    申请号：US12602441

    申请日：2008-05-30

    申请人： Moriyasu Masui ,  Hidenori Mikamiyama ,  Naoki Tsuno

    发明人： Moriyasu Masui ,  Hidenori Mikamiyama ,  Naoki Tsuno

    IPC分类号： A61K31/445 ,  C07D211/96 ,  A61P29/00 ,  A61P25/00 ,  A61P9/06 ,  A61P9/12 ,  G01N33/53

    CPC分类号： C07D211/96

    摘要： The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

    摘要翻译： 本发明涉及（式I）的氧亚氨基化合物及其药学上可接受的盐，前药和溶剂化物，其中：Y是CO或SOm; Z是氢，每个任选取代的低级烷基，低级烯基，芳基，杂环基等.R 1和R 2各自独立地为氢，各自为任选取代的低级烷基，低级烯基，环烷基，芳基，杂环基等，各X独立地为= 任选取代的低级烷基，氰基，硝基等，m为1或2，p为O，1或2，q为O或1.本发明还涉及式I的用途化合物，以治疗，预防或改善 对钙通道阻断，特别是N型钙通道的阻滞作用。 本发明的化合物特别适用于治疗疼痛。

    Oxime derivatives, hydrazone derivatives and use thereof
    3.
    发明授权
    Oxime derivatives, hydrazone derivatives and use thereof 失效
    肟衍生物，腙衍生物及其用途

    公开(公告)号：US06251949B1

    公开(公告)日：2001-06-26

    申请号：US09457672

    申请日：1999-12-09

    申请人： Moriyasu Masui ,  Norihiko Tanimoto ,  Kuniyoshi Nishida

    发明人： Moriyasu Masui ,  Norihiko Tanimoto ,  Kuniyoshi Nishida

    IPC分类号： A61K3115

    CPC分类号： C07D213/30 ,  A01N37/50 ,  A01N41/06 ,  A01N41/10 ,  A01N43/40 ,  A01N43/46 ,  A01N43/80 ,  A01N47/16 ,  C07C251/36 ,  C07C251/48 ,  C07C251/52 ,  C07C251/54 ,  C07C251/74 ,  C07C259/06 ,  C07D207/12 ,  C07D211/42 ,  C07D211/46 ,  C07D211/58 ,  C07D211/72 ,  C07D243/08 ,  C07D261/02 ,  C07D295/185 ,  C07D295/26 ,  C07D333/16 ,  C07D401/12

    摘要： Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R3 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R4 and R5, which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R4 and R5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR6 wherein R6 represents a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted alkanoyl, or an optionally substituted aroyl; Z represents an oxygen atom or a sulfur atom; and a wavy line (˜) represents the configuration of an E isomer, a Z isomer, or a mixture thereof.

    摘要翻译： 具有杀真菌活性并由通式（I）表示的化合物及其盐和水合物，其中R 1表示任选取代的芳基，任选取代的烷基等; R 2表示任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基，任选取代的杂环基等; R 3表示任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基磺酰基，任选取代的杂环基团等; R 4和R 5可以相同或不同，表示氢原子，任选取代的烷基或任选取代的烷氧基，或者R 4和R 5可以与相邻的氮原子一起形成任选取代的单环或多环; X和Y可以相同或不同，表示每个氧原子或NR 6，其中R 6表示氢原子，任选取代的烷基，任选取代的芳基，任选取代的烷酰基或任选取代的芳酰基; Z表示氧原子或硫原子; 波浪线（〜）表示E异构体，Z异构体或其混合物的构型。

    Fused aminodihydropyrimidine derivative
    4.
    发明授权
    Fused aminodihydropyrimidine derivative 有权
    熔融氨基二氢嘧啶衍生物

    公开(公告)号：US09018219B2

    公开(公告)日：2015-04-28

    申请号：US13881112

    申请日：2011-10-27

    申请人： Moriyasu Masui ,  Genta Tadano

    发明人： Moriyasu Masui ,  Genta Tadano

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D239/70 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2═X3 is CR5—CR6═CR7, N—CR6═CR7, CR5—N═CR7 or CR5—CR6═N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid β production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid β proteins.

    摘要翻译： 本发明例如提供以下化合物：其中环A为取代或未取代的碳环或取代或未取代的杂环，X1-X2 = X3为CR5-CR6 = CR7，N-CR6 = CR7，CR5-N = CR7或CR5-CR6 = N，R1是取代或未取代的烷基，取代或未取代的烯基等，R2a和R2b各自独立地为氢，取代或未取代的烷基等，R4a，R4b，R5，R6和R7各自为 独立地是氢，卤素，羟基，取代或未取代的烷基等，其药学上可接受的盐或其溶剂合物具有抑制淀粉样蛋白的作用; 生产，特别是BACE1抑制活性，并且可用作治疗由淀粉样蛋白的生产，分泌或沉积诱导的疾病的药物。 蛋白质。

    Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
    6.
    发明授权
    Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them 有权
    恶嗪衍生物和用于抑制含有它们的BACE1的药物组合物

    公开(公告)号：US08883779B2

    公开(公告)日：2014-11-11

    申请号：US14113327

    申请日：2012-04-25

    申请人： Moriyasu Masui ,  Yasunori Mitsuoka ,  Syuhei Yoshida ,  Ken-ichi Kusakabe ,  Naohiro Onodera ,  Noriyuki Kurose

    发明人： Moriyasu Masui ,  Yasunori Mitsuoka ,  Syuhei Yoshida ,  Ken-ichi Kusakabe ,  Naohiro Onodera ,  Noriyuki Kurose

    IPC分类号： C07D265/04 ,  A61K31/5355 ,  C07D413/12 ,  C07D413/14

    CPC分类号： C07D413/14 ,  C07D413/12

    摘要： The present invention provides a compound of formula (I): wherein —X═ is —CR7═ or —N═, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.

    摘要翻译： 本发明提供式（I）化合物：其中-X =是-CR 7 =或-N =，环B是取代或未取代的碳环或取代或未取代的杂环，R 1是取代或未取代的烷基等， R2a和R2b各自独立地为氢，取代或未取代的烷基等，R3和R4各自独立地为氢，卤素，取代或未取代的烷基等，R5为氢，取代或未取代的烷基等，各R6 独立地为卤素，羟基，取代或未取代的烷基等，R 7为氢，卤素，羟基，取代或未取代的烷基等，p为0〜3的整数，或其药学上可接受的盐， 抑制淀粉样蛋白 特别是抑制BACE1的作用，其可用作由淀粉样蛋白的生产，分泌和/或沉积引起的疾病的治疗或预防剂。 蛋白质。

    Process for producing carboxylic acid derivatives
    10.
    发明授权
    Process for producing carboxylic acid derivatives 失效
    制备羧酸衍生物的方法

    公开(公告)号：US5510506A

    公开(公告)日：1996-04-23

    申请号：US392852

    申请日：1995-03-27

    申请人： Akira Takase ,  Hiroyuki Kai ,  Moriyasu Masui ,  Katuhisa Masumoto ,  Akihiko Nakamura ,  Yujiro Kiyoshima ,  Mikio Sasaki

    发明人： Akira Takase ,  Hiroyuki Kai ,  Moriyasu Masui ,  Katuhisa Masumoto ,  Akihiko Nakamura ,  Yujiro Kiyoshima ,  Mikio Sasaki

    IPC分类号： C07C249/12 ,  C07C251/48 ,  C07C229/02

    CPC分类号： C07C249/12 ,  C07C251/48

    摘要： A process is disclosed to produce a carboxylic acid derivative of the general formula VIII!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and L are each as defined in the specification, characterized in that a benzyl halide is reacted with a cyano compound to give a phenylacetonitrile, which is then reacted with an alkyl nitrite in the presence of a base to give an .alpha.-hydroxyiminophenylacetonitrile, which is then reacted with an alkylating agent to give an .alpha.-alkoxyiminophenylacetonitrile, which is then hydrolyzed in the presence of a base, or is hydrated and treated with an acid, followed by hydrolysis in the presence of a base, to give an .alpha.-alkoxyiminophenylacetic acid, which is then reacted with an acid halide forming agent, or is convened into a metal salt, followed by reaction with an alkylating agent, or is reacted with a lower alcohol in the presence of an acid catalyst.According to the present invention, the reactions can be allowed to proceed under mild conditions over the whole process, and the desired carboxylic acid derivative VIII! can be produced without any facilities such as high-pressure steam equipment, high-temperature heat medium control equipment and freezing machines. In addition, there is no need to use various different solvents in the respective steps and the present process can be conducted with only one solvent, in which respect the present invention is also advantageous.

    摘要翻译： PCT No.PCT / JP94 / 01075 Sec。 371日期：1995年3月27日 102（e）1995年3月27日PCT PCT 1994年7月1日PCT公布。 出版物WO95 / 01328 日本公开1995年1月12日。公开了一种制备通式[Ⅷ]羧酸衍生物的方法：各自如说明书中所定义，其特征在于苄基卤与氰基化合物反应得到苯乙腈 然后在碱的存在下与亚硝酸烷基酯反应，得到α-羟基亚氨基苯基乙腈，然后与烷基化剂反应，得到α-烷氧基亚氨基苯基乙腈，然后在碱的存在下水解，或水合和 然后在碱的存在下水解，得到α-烷氧基亚氨基苯基乙酸，然后与酰卤化物形成试剂反应，或转入金属盐中，随后与烷基化剂反应， 或者在酸催化剂的存在下与低级醇反应。 根据本发明，可以在整个过程的温和条件下进行反应，并且可以制备所需的羧酸衍生物[Ⅷ]，无需任何设备，例如高压蒸汽设备，高温热介质控制 设备和冷冻机。 此外，在各步骤中不需要使用各种不同的溶剂，并且本发明方法可以仅使用一种溶剂进行，其中本发明也是有利的。