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    OXAZINE DERIVATIVE AND BACE 1 INHIBITOR CONTAINING SAME
    23.
    发明公开
    OXAZINE DERIVATIVE AND BACE 1 INHIBITOR CONTAINING SAME 审中-公开
    OXAZINDERIVAT UND BACE-1-HEMMER DAMIT

    公开(公告)号：EP2703399A1

    公开(公告)日：2014-03-05

    申请号：EP12777494.1

    申请日：2012-04-25

    申请人： Shionogi & Co., Ltd.

    发明人： MASUI, Moriyasu ,  MITSUOKA, Yasunori ,  YOSHIDA, Syuhei ,  KUSAKABE, Ken-ichi ,  ONODERA, Naohiro ,  KUROSE, Noriyuki

    IPC分类号： C07D413/12 ,  A61K31/5355 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00

    CPC分类号： C07D413/14 ,  C07D413/12

    摘要： The present invention provides a compound of formula (I):

    wherein
    -X= is -CR 7 = or -N=,
    ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle,
    R 1 is substituted or unsubstituted alkyl or the like,
    R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like,
    R 3 and R 4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like,
    R 5 is hydrogen, substituted or unsubstituted alkyl or the like,
    each R 6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R 7 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 =为-CR 7 =或-N =，环B为取代或未取代的碳环或取代或未取代的杂环，R 1为取代或未取代的烷基或 R 2a和R 2b各自独立地为氢，取代或未取代的烷基等，R 3和R 4各自独立地为氢，卤素，取代或未取代的烷基等，R 5为氢，取代或未取代的烷基或 每个R 6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，或药学上可接受的 其具有抑制淀粉样蛋白²产生的作用，特别是抑制BACE1的作用，并且其可用作由淀粉样蛋白²蛋白质的产生，分泌和/或沉积诱导的疾病的治疗或预防剂。

    FUSED AMINODIHYDROPYRIMIDINE DERIVATIVE
    24.
    发明公开
    FUSED AMINODIHYDROPYRIMIDINE DERIVATIVE 审中-公开
    稠合的氨基二氢嘧啶衍生物

    公开(公告)号：EP2634188A1

    公开(公告)日：2013-09-04

    申请号：EP11836380.3

    申请日：2011-10-27

    申请人： Shionogi & Co., Ltd.

    发明人： MASUI, Moriyasu ,  TADANO, Genta

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P43/00

    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,
    X 1 -X 2 =X 3 is CR 6 -CR 6 =CR 7 , N-CR 6 =CR 7 , CR 5 -N=CR 7 or CR 5 -CR 6 =N, R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R 4a , R 4b , R 5 , R 6 and R 7 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： 本发明提供例如以下化合物：其中环A为取代或未取代的碳环或取代或未取代的杂环，X 1 -X 2 = X 3为CR 6 -CR 6 = CR 7，N-CR 6 = CR 7，CR 5 -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 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β淀粉样蛋白产生，特别是BACE1抑制活性的作用，并且可用作治疗由生产， 淀粉样蛋白β蛋白的分泌或沉积。

    OXYIMINO COMPOUNDS AND THE USE THEREOF
    27.
    发明公开
    OXYIMINO COMPOUNDS AND THE USE THEREOF 有权
    OXYIMINO化合物及其用途

    公开(公告)号：EP2164325A1

    公开(公告)日：2010-03-24

    申请号：EP08767992.4

    申请日：2008-05-30

    申请人： Shionogi&Co., Ltd.

    发明人： TSUNO, Naoki ,  MIKAMIYAMA, Hidenori ,  MASUI, Moriyasu

    IPC分类号： A01N43/40 ,  A61K31/445

    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为氢，各自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= O， 任选取代的低级烷基，氰基，硝基等，m是1或2，p是0,1或2，q是0或1.本发明还涉及使用式I化合物治疗，预防或改善 对钙通道阻断有响应的病症，特别是N型钙通道。 本发明的化合物对于治疗疼痛特别有用。

    OXIME DERIVATIVES, HYDRAZONE DERIVATIVES, AND USE THEREOF
    28.
    发明公开
    OXIME DERIVATIVES, HYDRAZONE DERIVATIVES, AND USE THEREOF 失效
    OXIMDERIVATE，HYDRAZONDERIVATE UND DEREN ANWENDUNG

    公开(公告)号：EP0940388A1

    公开(公告)日：1999-09-08

    申请号：EP97942270.6

    申请日：1997-10-07

    申请人： SHIONOGI & CO., LTD.

    发明人： MASUI, Moriyasu ,  TANIMOTO, Norihiko ,  NISHIDA, Kuniyoshi

    IPC分类号： C07C251/36 ,  C07C251/74 ,  C07C259/06 ,  C07C327/40 ,  C07D207/12 ,  C07D211/42 ,  C07D211/58 ,  C07D261/02 ,  C07D265/30 ,  C07D279/12 ,  C07D295/18

    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 R 1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R 2 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; R 3 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; R 4 and R 5 , which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R 4 and R 5 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 NR 6 wherein R 6 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 相邻的氮原子是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地 取代的芳酰基; Z表示氧原子或硫原子; 和波浪线（SIMILAR）表示E异构体，Z异构体或其混合物的构型。

    PROCESS FOR PRODUCING $g(a)-HYDROXYIMINOPHENYLACETONITRILE
    30.
    发明公开
    PROCESS FOR PRODUCING $g(a)-HYDROXYIMINOPHENYLACETONITRILE 失效
    生产$ g（a） - 羟基亚氨基苯基乙酰丙酮的方法

    公开(公告)号：EP0658542A1

    公开(公告)日：1995-06-21

    申请号：EP94919839.4

    申请日：1994-07-01

    申请人： SHIONOGI & CO., LTD. ,  SUMITOMO CHEMICAL COMPANY LIMITED

    发明人： TAKASE, Akira ,  KAI, Hiroyuki ,  MASUI, Moriyasu ,  MASUMOTO, Katuhisa ,  NAKAMURA, Akihiko ,  KIYOSHIMA, Yujiro ,  SASAKI, Mikio

    IPC分类号： C07C255/62 ,  C07C253/30 ,  C07C323/63 ,  C07C319/20 ,  C07C253/14

    CPC分类号： C07C251/48 ,  C07C253/14 ,  C07C253/30 ,  C07C255/64

    摘要： A process for producing an α-hydroxyiminophenylacetonitrile represented by general formula [II], (wherein R¹, R², R³ and Z are each as defined in the specification) by reacting a crude nitrile containing a phenylacetonitrile represented by general formula [I], (wherein R¹, R², R³ and Z are each as defined in the specification) with an alkyl nitrite in the presence of a base, extracting the reaction mixture with water, and neutralizing the separated water layer with an acid. This process enables target α-hydroxyiminophenylacetonitriles to be readily produced in a highly pure form in high yield by extracting the reaction mass with water and neutralizing the separated water layer with an acid.

    摘要翻译： 通式[Ⅱ]代表的α-羟基亚氨基苯基乙腈的制备方法（其中R 1，R 2，R 3和Z各自如本说明书中所定义）通过使含有通式[Ⅰ]代表的苯乙腈， 其中R 1，R 2，R 3和Z各自如说明书中所定义）与亚硝酸烷基酯在碱存在下反应，用水萃取反应混合物，并用酸中和分离的水层。 通过该方法，通过用水提取反应物并用酸中和分离的水层，能够以高收率容易地以高纯度形式生产目标α-羟基亚氨基苯基乙腈。