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    Phosphonic acid derivatives and the treating agents of diseases related hyperphosphatemia
    3.
    发明授权
    Phosphonic acid derivatives and the treating agents of diseases related hyperphosphatemia 失效
    膦酸衍生物和疾病相关高磷血症的治疗剂

    公开(公告)号：US07691898B2

    公开(公告)日：2010-04-06

    申请号：US11664830

    申请日：2005-10-05

    申请人： Hiroshi Tomiyama ,  Masayuki Yokota ,  Kazuo Tokuzaki ,  Ryoko Tomita

    发明人： Hiroshi Tomiyama ,  Masayuki Yokota ,  Kazuo Tokuzaki ,  Ryoko Tomita

    IPC分类号： A61K31/381 ,  C07D333/46 ,  C07F9/30

    CPC分类号： C07F9/6541 ,  C07F9/3834 ,  C07F9/3882 ,  C07F9/3891 ,  C07F9/59 ,  C07F9/6539 ,  C07F9/65517 ,  C07F9/655345 ,  C07F9/655354 ,  C07F9/6558 ,  C07F9/65586

    摘要： This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is —(CH2)(n+1)—, —(CH2)—O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R1˜R7, wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle, R1, R2 and R3 are not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, R8 and R9 are may be the same or different and are substituents, R10 is an alkyl group, n and m are 0-10 and o is 0-2.

    摘要翻译： 本发明涉及一系列具有抗高磷酸血症活性的新型膦酸衍生物。 其中：A选自 - （CH 2）n - ， - CO - ， - （CH 2）n -CO-（CH 2）m - ， - （CH 2）n -C CS-（CH 2）m-或支链亚烷基， B环和C环选自苯环，萘环，薁环或杂环或稠合杂环化合物，D是 - （CH 2）（n + 1） - ， - （CH 2）-O-（CH 2）m - ， - （CH2）-S（O）o-（CH2）m-，-CF3或 - （CH2）n-NR10-（CH2）m-，其中D环与构成C环的碳原子连接，E 选自氧原子或硫原子，P为膦原子，R1〜R7，其中R1和R2，R4和R5与邻位碳原子连接在一起形成5〜7元饱和或不饱和烃环，或5 如果B环是苯环并且可以相同或不同，并且是取代基，则R 6，R 6和R 3不是氢原子，R 8和R 9可以相同或不同，并且是取代基R 10 是烷基，n和m是0-10，o是0-2。

    PREPARATION METHOD FOR ANTITUMOR DRUG AP26113
    6.
    发明申请
    PREPARATION METHOD FOR ANTITUMOR DRUG AP26113 审中-公开

    公开(公告)号：US20180071324A1

    公开(公告)日：2018-03-15

    申请号：US15822092

    申请日：2017-11-24

    申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.

    发明人： Xuenong XU

    IPC分类号： A61K31/675

    CPC分类号： A61K31/675 ,  C07F9/6558 ,  C07F9/65583

    摘要： Disclosed is a preparation method for an antitumor drug AP26113 (I). The method comprises the following preparation steps: cyclizing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and N,N-dimethylamino acrylate, condensing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and 4-(dimethyl phosphitylate)aniline, and chlorinating N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and a chlorinating agent, sequentially, so as to prepare AP26113 (I). The preparation method adopts easily-obtained raw materials, causes few side reactions, and is economical, environmentally friendly, and suitable for industrial production.

    Five-membered heterocyclic compounds
    10.
    发明授权
    Five-membered heterocyclic compounds 失效
    五元杂环化合物

    公开(公告)号：US07368578B2

    公开(公告)日：2008-05-06

    申请号：US10527426

    申请日：2003-09-09

    申请人： Yu Momose ,  Nobuyuki Takakura ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    发明人： Yu Momose ,  Nobuyuki Takakura ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    IPC分类号： C07D263/02 ,  C07D263/00 ,  C07D263/30 ,  C07D261/00 ,  C07D261/04 ,  C07D261/06 ,  A01N43/76 ,  A01N43/80

    CPC分类号： C07D263/32 ,  C07F9/6558 ,  C07F9/65583

    摘要： The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic action and a hypolipidemic action, and which is useful as an agent for the prophylaxis or treatment of obesity, diabetes mellitus, hyperlipidemia, impaired glucose tolerance, hypertension and the like.

    摘要翻译： 本发明提供由下式表示的化合物：其中R 1是任选取代的5元杂环基; X，Y和V相同或不同，各自为键，氧原子，硫原子等; Q为碳原子数为1〜20的二价烃基; 环A是任选进一步具有1至3个取代基的芳环; Z是 - （CH 2）n - - - - - - - - 1 - （CH 2） （n为0〜8的整数，Z 1为键，氧原子，硫原子等）; n为0〜8的整数。 环B是任选进一步具有1至3个取代基的含氮杂环; W是碳原子数为1〜20的键或二价烃基; R 2是氢原子，氰基，-PO（OR 9）（OR 10）（R 10） SUP＆gt;和R 10相同或不同，各自为氢原子或任选取代的烃基，R 9和R 10为 任选地键合以形成任选取代的环）等，或其盐，其具有优异的脂肪组织重量减少作用，降血糖作用和降血脂作用，并且其可用作预防或治疗 肥胖症，糖尿病，高脂血症，葡萄糖耐量降低，高血压等。