利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

145 条记录 (耗时 0.042 秒)

    Compounds containing short aminoalcohol chains and metal complexes for medical imaging
    69.
    发明专利
    Compounds containing short aminoalcohol chains and metal complexes for medical imaging 有权

    公开(公告)号：JP2009513574A

    公开(公告)日：2009-04-02

    申请号：JP2008534029

    申请日：2006-10-09

    申请人： ゲルベGuerbet

    发明人： マール ポール

    IPC分类号： C07D471/08 ,  A61K49/00 ,  A61K51/00 ,  C07D257/02 ,  C07F5/00

    CPC分类号： A61K49/085 ,  A61K49/10 ,  A61K49/103 ,  A61K49/106 ,  A61K49/14 ,  A61K51/0402 ,  A61K51/0478 ,  A61K51/0482 ,  C07D257/02 ,  C07D471/08 ,  C07D487/04

    摘要： Polyaza compounds (I) and their isomers, enantiomers and/or diastereomers and salts, are new. Polyaza compounds (I) of formula (IIa), (IIb) and (VIa) or linear polyaza compounds (Vb) of formula (R5-CH(X5)-N(CHX4R4)-CH(K16)-CH(K15 )-N(CH(R3)(X3))-CH(K14)-CH(K13)-N(CHX2R2)-CH(R1)-X1), and their isomers, enantiomers and/or diastereomers and salts of (VIa) and (VIb), are new. R1-R5COOH, P(O)(OH)2 or R6-P(O)-OH, preferably COOH; R6H or 1-3C alkyl; X1-X5L-Y1; L : 1-3C alkyl, preferably (CH2)n; n : 1-3; Y1-CONH2, CO-NR7R8 or NR7-CO-R8; R7, R7H or 1-6C (hydroxy)alkyl, preferably -CH2-CH2-OH, CHOH-CH2OH, -CH-(CH2OH)2, -(CH2)m-(CHOH)p-CH2OH or -C(CH2OH)3; m : 1-3; p : 1-4; D, E, F1CH or N; either K1-K20H, -(CH2)j-CH3 or -(CH2)i-OH, preferably H; or K3K5, K4K5, K3K6, K4K6, K7K9, K7K10, K8K9, K8K10, K13K14, K15K16, K17K18, K19K203-6C ring; j : 0-3; and i : 1-3. Provided that the sum of m and p is 2-5. Independent claims are included for: (1) a multimer, preferably dimer or trimer, of (II) or (VI); (2) vectorized compound comprising (II) or (VI) coupled to a biovector by an intermediate optionally of a bridging group; (3) a complex compound or multimer or a vectorized compound having a metal ion (M); (4) lipidic pharmaceutical composition comprising the compound, multimer, vectorized product or complex bound to a lipidic nanoparticule; (5) diagnostic composition for magnetic resonance imaging comprising the compound, multimer, vectorized product or complex; and (6) preparation of the metal complex of (IIa) comprising reacting an ester compound of formula (RaOOC-CHQ-(CH2)n-COORa) with a fused macrocycle of formula (IV) to obtain a hexaacid of formula (V), optionally hydrolyzing or hydrogenating the ester groups of (V) to obtain the hexaacid of formula (Va), reacting a salt or an oxide of the metal to be complexed with (Va), to obtain the complex or its base salts and reacting amino alcohol groups of formula NHR7R8 with the complex, in the presence of a carboxylic acid group activating agent to obtain the triamide of formula (IIa). M : metal ion of atomic number 21-29, 42-44 or 58-70, preferably Gd, Mn or Fe, or radionuclide e.g. 99>Tc, 117>Sn, 111>In, 97>Ru, 67>Ga, 68>Ga, 89>Zr, 177>Lu, 47>Sc, 105>Rh, 188>Re, 60>Cu, 62>Cu, 64>Cu, 67>Cu, 90>Y, 159>Gd, 149>Pr or 166>Ho; X1-X3-(CH2)n-CO-NR7R8; n : 1-3; Q = halo (preferably Br), 1-3C alkyl sulfonate, tosylate or triflate; and RaH, 1-3C alkyl or benzyl. [Image] [Image]

    Synthesis of cyclen derivatives
    70.
    发明专利
    Synthesis of cyclen derivatives 审中-公开

    公开(公告)号：JP2008538371A

    公开(公告)日：2008-10-23

    申请号：JP2008507582

    申请日：2006-04-18

    申请人： ジーイー・ヘルスケア・アクスイェ・セルスカプ

    发明人： アクセルソン，オスカー ,  オルソン，アンドレアス

    IPC分类号： C07D257/02 ,  C07D20060101

    CPC分类号： C07D257/02

    摘要： 【課題】 ＤＯ３Ａ−トリ−ｔ−ブチルエステル（１，４，７，１０−テトラアザシクロドデカン−１，４，７−三酢酸トリ−ｔ−ブチルエステル）のような保護ＤＯ３Ａの改良製造方法を提供する。
    【解決手段】 上記化合物を塩として製造する。 この方法は、ＤＯ３Ａ−トリ−ｔ−ブチルエステルを高純度の塩として得る仕上げ処理を含む。 具体的には、（１）シクレンを活性化酢酸エステルからなるアルキル化剤と反応させて、保護ＤＯ３Ａを含む混合物を形成し、（２）上記混合物のｐＨを９．０±０．５に調節し、（３）上記混合物に塩を添加し、（４）沈殿した生成物を回収する。
    【選択図】 なし