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    Agent for potentiating nerve growth factor activity containg 1,2-ethanediol derivate or salt thereof
    16.
    发明公开
    Agent for potentiating nerve growth factor activity containg 1,2-ethanediol derivate or salt thereof 失效
    含有活性物质对促进神经生长因子和其盐1,2-乙二醇衍生物

    公开(公告)号：EP1223169A1

    公开(公告)日：2002-07-17

    申请号：EP02004782.5

    申请日：1995-10-20

    申请人： TOYAMA CHEMICAL CO., LTD.

    发明人： Ono, Satoshi ,  Maekawa, Mutsuko ,  Narita, Hirokazu ,  Hirata, Kazunari

    IPC分类号： C07D333/54 ,  C07D307/79 ,  C07D417/12 ,  C07C217/10 ,  A61K31/38 ,  A61K31/34 ,  A61K31/495 ,  A61K31/44 ,  A61K31/535 ,  A61K31/40

    CPC分类号： C07D307/79 ,  C07C217/10 ,  C07D333/54 ,  C07D409/12 ,  C07D453/02 ,  C07D471/08 ,  Y02P20/55

    摘要： A remedy for diseases caused by degeneration of central nervous system, comprising a 1,2-ethanediol derivative represented by the following general formula or its salt:
    wherein R 1 represents a substituted or unsubstituted phenyl, naphthyl, indanyl, indenyl, tetrahydronaphthyl or heterocyclic group; R 2 represents a hydrogen atom, a C 1-6 alkyl group or a hydroxyl-protecting group; R 3 represents a hydrogen atom or a C 1-6 alkyl group; nR 4 's may be the same as or different from one another and each represents a hydrogen atom or a C 1-6 alkyl group; nR 5' s may be the same as or different from one another and each represents a hydrogen atom or a C 1-6 alkyl group; R 6 represents a substituted or unsubstituted amino or nitrogen-containing heterocyclic group or an ammonio group; and n represents 0 or an integer of 1 to 6, provided that the following 1,2-ethanediol derivative represented by general formula or its salt:
    wherein nR 1a 'S may be the same as or different from one another and each represents a fluorine, chlorine, bromine or iodine atom, C 1-6 alkyl, C 1-6 alkoxy or phenyl group; R 2a represents a hydrogen atom or a hydroxyl-protecting group; R 6a represents a C 1-6 alkyl-substituted amino group or a pyrrolyl, pyrrolidinyl, piperidyl, piperazinyl, imidazolyl, pyrazolyl, pyridyl, tetrahydropyridyl, pyrimidinyl, morpholinyl, thiomorpholinyl, quinolyl, quinolidinyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, quinuclidinyl, thiazolyl, tetrazolyl, thiadiazolyl, pyrrolinyl, imidazolinyl, imidazolidinyl, pyrazolinyl, pyrazolidinyl, purinyl, indazolyl, furyl, thienyl, benzothienyl, pyranyl, isobenzofuranyl, oxazolyl, benzofuranyl, indolyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, quinoxalyl, dihydroquinoxalinyl, 2,3-dihydrobenzothienyl, 2,3-dihydrobenzopyrrolyl, 2,3-dihydro-4H-1-thianaphthyl, 2,3-dihydrobenzofuranyl, benzo[b]dioxanyl, imidazo[2,3-a]pyridyl, benzo[b]piperazinyl, chromenyl, isothiazolyl, isoxazolyl, thiadiazolyl, oxadiazolyl, pyridazinyl, isoindolyl or isoquinolyl group; and n represents an integer of 1 to 5, is excluded.

    摘要翻译： 一种用于由中枢神经系统的变性引起的疾病的补救，含有下述通式化合物或其盐表示的1,2-乙二醇衍生物： worin - [R <1> darstellt一个substituiertem奥德unsubstituiertem苯基，萘基，茚满基，茚基 基，四氢或杂环基团; [R <2>代表氢原子，C 1-6烷基或羟基保护基; [R <3> darstellt氢原子或C 1-6烷基; NR <4>“可以彼此相同或彼此不同，并且各自darstellt氢原子或C 1-6烷基; NR <5“>可以彼此相同或彼此不同，并且各自darstellt氢原子或C 1-6烷基; [R <6> darstellt一个substituiertem奥德unsubstituiertem氨基或杂环基团或在铵基的含氮; 和n darstellt 0或1至6的整数，条件做了以下的1,2-乙二醇衍生物由通式或其盐表示： worin NR <1A>“可以彼此相同或彼此不同 并且各自表示氟，氯，溴或碘原子，C 1-6烷基，C 1-6烷氧基或苯基; [R <2A>代表氢原子或羟基保护基; [R <6A>表示一个C 1-6烷基取代的氨基或吡咯基，吡咯烷基，哌啶基，哌嗪基，咪唑基，吡唑基，吡啶基，四氢吡啶基，嘧啶基，吗啉基，硫代吗啉基，喹啉基，quinolidinyl，四氢喹啉基，四氢异喹啉，奎宁环基，噻唑基，四唑基 ，噻二唑基，吡咯啉基，咪唑啉基，咪唑烷基，吡唑啉基，吡唑烷基，嘌呤基，吲唑基，呋喃基，噻吩基，苯并噻吩基，吡喃基，异苯并呋喃基，恶唑基，苯并呋喃基，吲哚基，苯并咪唑基，苯并恶唑基，苯并噻唑基，喹喔啉基，dihydroquinoxalinyl，2,3-二氢苯并噻吩，2- ，3- dihydrobenzopyrrolyl，2,3-二氢-4H-1- thianaphthyl，2,3-二氢苯并呋喃基，benzoÄbÜdioxanyl，imidazoÄ2,3-aÜpyridyl，benzoÄbÜpiperazinyl，色烯，异噻唑基，异恶唑基，噻二唑基，恶二唑基，哒嗪基，异吲哚基或异喹啉基; 和n darstellt为1整数以5，被排除在外。

    PROCESS FOR THE PREPARATION OF SALMETEROL AND ITS SALTS
    20.
    发明公开
    PROCESS FOR THE PREPARATION OF SALMETEROL AND ITS SALTS 审中-公开
    DESZESS ZUR HERSTELLUNG VON SALMETEROL UND DESSEN SALZE

    公开(公告)号：EP2641893A1

    公开(公告)日：2013-09-25

    申请号：EP13154981.8

    申请日：2006-10-17

    申请人： Generics [UK] Limited

    发明人： GORE, Vinayak, G. ,  GAIKWAD, Avinash, C. ,  GADAKAR, Maheshkumar, Suryakant ,  SHUKLA, Vinay, Kumar

    IPC分类号： C07C213/08 ,  C07C217/10 ,  C07C43/172 ,  C07C41/16 ,  C07C43/174

    CPC分类号： C07C217/10 ,  C07C41/16 ,  C07C43/174 ,  C07C213/08 ,  Y02P20/55

    摘要： The present invention relates to processes for the preparation of 4-hydroxy-α'-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol 1-hydroxy-2-naphthoate (salmeterol xinafoate) (12a), the preparation of 4-hydroxy-α'-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol (salmeterol) (11), the preparation of protected N-[6-(4-phenylbutoxy)hexyl]amine intermediates (7), and the preparation of 6-substituted (4-phenylbutoxy)hexane intermediates (5), shown below, wherein X is a leaving group and Pg is a protecting group.

    摘要翻译： 本发明涉及制备4-羟基-5' - [[[（6-苯基丁氧基）己基]氨基]甲基] -1,3-苯二甲醇1-羟基-2-萘甲酸盐（沙美特罗昔萘酸盐）的方法， （12a），制备4-羟基 - ±[ - [[[（6-（4-苯基丁氧基）己基]氨基]甲基] -1,3-苯二甲醇（沙美特罗）（11） 6-（4-苯基丁氧基）己基]胺中间体（7）和6-取代的（4-苯基丁氧基）己烷中间体（5）的制备，其中X是离去基团，Pg是保护基团。