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    POLYMERS AND THEIR USE AS FLUORESCENT LABELS
    5.
    发明申请
    POLYMERS AND THEIR USE AS FLUORESCENT LABELS 审中-公开

    公开(公告)号：US20100129800A1

    公开(公告)日：2010-05-27

    申请号：US12452626

    申请日：2008-07-09

    申请人： Juan Aymami Bofarull ,  Fernando Albericio Palomera ,  Anna Maria Avino Andres ,  Josep Farrera Sinfreu ,  Miriam Royo Exposito ,  Isabel Navarro Munoz ,  Ramon Eritja Casadella

    发明人： Juan Aymami Bofarull ,  Fernando Albericio Palomera ,  Anna Maria Avino Andres ,  Josep Farrera Sinfreu ,  Miriam Royo Exposito ,  Isabel Navarro Munoz ,  Ramon Eritja Casadella

    IPC分类号： C12Q1/68 ,  C07D471/04 ,  C07D219/08 ,  C07H21/04 ,  C08G69/00

    CPC分类号： C08G73/0273 ,  C08G73/028 ,  C08G79/04

    摘要： The present invention relates to a polymer composed by two to ten monomers of formula (I) as well as to a process for its preparation and its use as fluorophore wherein: X is a radical of formula (II) wherein —R5 is an electron pair or a (C1-C3)-alkyl radical; —Ra and —Rb are radicals independently selected from the group consisting of H, (C1-C4)-alKyI, (C1-C4)-alkoxy, (C1-C4)-alkylamino, phenyl, F, Cl, Br, amino, hydroxy, and nitro or —Ra and —Rb are fused forming with the carbon atoms to which they are attached a ring of formula (III) with the condition that (I) when —R5 is an electron pair, a is a N═C double bond, and Ra and Rb are fused forming the ring (III), said ring being a biradical selected from (IIIa) and (IIIb), thus, radical (II) is (IIa) or (IIb) respectively (II) when —R5 is a (C1-C3)-alkyl radical, a is a N—C single bond and Ra and Rb are fused forming the ring (III), said ring being a biradical (a), thus, the radical (II) is (IIc) R1-R4 and R7-R18 represent radicals, same or different, selected for the group consisting of H1 (C1-C4)-alkyl, (C1-C4)-alky-lamiπo, phenyl, F, Cl, Br, amino, hydroxy, and nitro; p is an integer from 0 to 1; R6 is a biradical selected from the group consisting of —CO—; —CONH(CH2)mCO—; and —CO[NHCHR″CO]m—, wherein —R″ are side chains radicals, same or different, corresponding to natural aminoacids; and m is an integer from 1 to 3; Z is a triradical of formula (IV) wherein r is an integer from 0 to 1; v is an integer from O to 1; Z′ is a triradical selected from —CH2— and nitrogen; Z″ is H, with the proviso that: (a) when Z′ is nitrogen, forming an amide bound with R6, then is hydrogen and v is an integer from O to 1, and (b) when Z″ is —NH—, forming an amide group with R6, then Z1 is —CH2 and v=O or of formula (V) wherein Z″ is selected from —CH3 and —CH2NH—, Z1v is selected from H and NH, Zv is selected from S and O atom, W is an integer from 0 to 1, with the proviso that (c) when R6 is bound to Z′″ then Z′″ is —CH2NH—, Z1v is hydrogen and w is 0; and (d) when Z1v is —NH— forming an amide bound with R6, Z′″ is —CH3 and w is 1; and and wherein the monomers of formula (I) are linked through the triradical Z, forming an amide or phosphate bound.

    Antitumor 1,2-Diphenylpyrrole Compounds and their Preparation Process
    7.
    发明申请
    Antitumor 1,2-Diphenylpyrrole Compounds and their Preparation Process 审中-公开
    抗肿瘤剂1,2-二苯基吡咯化合物及其制备方法

    公开(公告)号：US20120196915A1

    公开(公告)日：2012-08-02

    申请号：US13387634

    申请日：2010-07-28

    申请人： Ramon Mangues Bafalluy ,  Isolda Casanova Rigalt ,  Fernando Albericio Palomera ,  Mercedes Álvarez ,  Svetlana Savina

    发明人： Ramon Mangues Bafalluy ,  Isolda Casanova Rigalt ,  Fernando Albericio Palomera ,  Mercedes Álvarez ,  Svetlana Savina

    IPC分类号： A61K31/402 ,  A61P35/00 ,  C07D207/325

    CPC分类号： C07D207/333 ,  C07D207/335

    摘要： The present invention relates to a new series of 1,2-diphenylpyrroles of formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable solvates, having antitumor activity, wherein R1 and R2 are individually selected from the group consisting of halogen, optionally substituted O(C1-C4)alkyl and optionally substituted (C1-C4)alkyl; and R3 is selected from the group consisting of H, (C1-C4)alkyl, CONH2 and (C═NH)NH2. It also relates to a process for preparing them, to pharmaceutical compositions containing them, and to their use for the treatment of cancer, in particular lung carcinoma, colorectal carcinoma, breast carcinoma and/or prostate carcinoma.

    摘要翻译： 本发明涉及新的一系列式（I）的1,2-二苯基吡咯或其药学上可接受的盐或其药学上可接受的溶剂化物，其具有抗肿瘤活性，其中R1和R2分别选自卤素，任选地 取代的O（C 1 -C 4）烷基和任选取代的（C 1 -C 4）烷基; 并且R 3选自H，（C 1 -C 4）烷基，CONH 2和（C = NH）NH 2。 它还涉及其制备方法，含有它们的药物组合物及其用于治疗癌症，特别是肺癌，结肠直肠癌，乳腺癌和/或前列腺癌的用途。