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1. 发明申请

WO2009007397A1 NEW POLYMERS AND THEIR USE AS FLUORESCENT LABELS 审中-公开
标题翻译：新型聚合物及其作为荧光标签使用
公开(公告)号：WO2009007397A1
公开(公告)日：2009-01-15
申请号：PCT/EP2008/058922
申请日：2008-07-09
申请人： CRYSTAX PHARMACEUTICALS, S.L. , AYMAMÍ BOFARULL, Juan , ALBERICIO PALOMERA, Fernando , AVIÑÓ ANDRÉS, Anna Maria , FARRERA SINFREU, Josep , ROYO EXPÓSITO, Míriam , NAVARRO MUÑOZ, Isabel , ERITJA CASADELLÀ, Ramón
发明人： AYMAMÍ BOFARULL, Juan , ALBERICIO PALOMERA, Fernando , AVIÑÓ ANDRÉS, Anna Maria , FARRERA SINFREU, Josep , ROYO EXPÓSITO, Míriam , NAVARRO MUÑOZ, Isabel , ERITJA CASADELLÀ, Ramón
IPC分类号： C08G73/02 , C08G79/02 , C09K11/06
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 -R 5 is an electron pair or a (C 1 -C 3 )-alkyl radical; -R a and -R b are radicals independently selected from the group consisting of H, (C 1 -C 4 )-alKyI, (C 1 -C 4 )-alkoxy, (C 1 -C 4 )-alkylamιno, phenyl, F, Cl, Br, amino, hydroxy, and nitro or -R a and -R b are fused forming with the carbon atoms to which they are attached a ring of formula (III) with the condition that (I) when -R 5 is an electron pair, a is a N=C double bond, and R a and R b 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 -R 5 is a (C 1 -C 3 )-alkyl radical, ais a N-C single bond and R a and R b are fused forming the ring (III), said ring being a biradical (a), thus, the radical (II) is (IIc) R 1 -R 4 and R 7 -R 18 represent radicals, same or different, selected fro the group consisting of H 1 (C 1 -C 4 )-alkyl,, (C 1 -C 4 )-alkylamiπo, phenyl, F, Cl, Br, amino, hydroxy, and nitro; p is an integer from 0 to 1; R 6 is a biradical selected from the group consisting of -CO-; -CONH(CH 2 ) m CO-; 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 O to 1; v is an integer from O to 1; Z' is a triradical selected from -CH 2 - and nitrogen; Z" is H, with the proviso that: (a) when Z' is nitrogen, forming an amide bound with R 6 , then is hydrogen and v is an integer from O to 1, and (b) when Z" is -NH-, forming an amide group with R 6 , then Z1 is -CH 2 - and v= O or of formula (V) wherein Z" is selected from -CH 3 and -CH 2 NH-, Z lv is selected from H and NH, Z v is selected from S and O atom, W is an integer from 0 to 1, with the proviso that (c) when R 6 is bound to Z"' then Z"' is -CH 2 NH-, Z ιv is hydrogen and w is 0; and (d) when Z ιv is -NH- forming an amide bound with R 6 , Z'" is - CH 3 and w is 1; and and wherein the monomers of formula (I) are linked through the triradical Z, forming an amide or phosphate bound.
摘要翻译：本发明涉及由2至10个式（I）单体组成的聚合物，以及其制备方法及其作为荧光团的用途。其中：X是式（II）的基团，其中-R5是电子对或（C1-C3） - 烷基; -R a和-R b是独立地选自H，（C 1 -C 4） - 烷基，（C 1 -C 4） - 烷氧基，（C 1 -C 4） - 烷基氨基，苯基，F，Cl，Br，氨基，羟基和硝基或-Ra和-Rb与其连接的式（III）的环与碳原子稠合形成，条件是当-R5是电子对时，（I），a是N = C双键，并且R a和R b熔合形成环（III），所述环为选自（IIIa）和（IIIb）的双原子。因此，当-R5是（C1-C3） - 烷基时，基团（II）分别为（IIa）或（IIb），即NC单键，Ra和Rb稠合形成环（III），所述环是双原子（a），因此，基团（II）是（IIc）R 1 -R 4和R 7 -R 18表示相同或不同的选自H1（C1-C4） - 烷基，（C 1 -C 4） - 烷基氨基，苯基，F，Cl，Br，氨基，羟基和硝基; p是从0到1的整数; R6是选自-CO-的一个双原子; -CONH（CH 2）mCO-; 和-CO [NHCHR'CO] m - ，其中-R“是对应于天然氨基酸的侧链基团，相同或不同; m是1至3的整数; Z是式（IV）的三元组，其中 r为0至1的整数; v为0至1的整数; Z'为选自-CH 2 - 和氮的三元组; Z“为H，条件是：（a）当Z'为氮时，形成与R6结合的酰胺，然后是氢，v是从0到1的整数，和（b）当Z“是-NH-时，与R6形成酰胺基，则Z1是-CH2-，v = 0或其中Z“选自-CH 3和-CH 2 NH-，Z 1v选自H和NH，Zv选自S和O原子，W是0至1的整数，条件是（c ）当R 6与Z“'结合时，Z”'是-CH 2 NH-，Z 2 v是氢，w是0; 和（d）当Z？v是-NH-形成与R6结合的酰胺时，Z'“是-CH 3，w是1;并且其中式（I）的单体通过三元Z连接，形成酰胺或磷酸盐结合。

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