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    POLYMERS AND THEIR USE AS FLUORESCENT LABELS
    1.
    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.

    Substituted quinolines for the treatment of cancer
    2.
    发明申请
    Substituted quinolines for the treatment of cancer 失效

    公开(公告)号：US20070105784A1

    公开(公告)日：2007-05-10

    申请号：US10580140

    申请日：2004-11-18

    申请人： Juan Aymami Bofarull ,  Miquel Coll Capella ,  Amadeo Llebaria Soldevila ,  Isabel Navarro Munoz

    发明人： Juan Aymami Bofarull ,  Miquel Coll Capella ,  Amadeo Llebaria Soldevila ,  Isabel Navarro Munoz

    IPC分类号： A61K38/04 ,  A61K31/7076 ,  A61K31/4745 ,  C07D471/02 ,  C07H21/02

    CPC分类号： C07D471/04 ,  A61K38/00 ,  C07K5/06026

    摘要： Compounds of formula G1-L-G2, where -G1 is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from (CH2)rNR′″(CH2)s and —(CH2)rNR′″(CH2)SNR″″(CH2)t—, —R′″ and —R″″ are radicals, same or different, selected from the group consisting of H and (C1-C3)-alkyl; r, s and t are an integer from 1 to 3 and, -G2 is H or a radical structurally close to -G1, are intercalators. They are compounds which intercalate between DNA base pairs, and are useful as therapeutic agents against cancer, as assess by an in vitro test of cytotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G1 is bonded to -L- through a carbonyl amino and -L- is —(CH2)3NCH3(CH2)3 or —(CH2)2NCH3(CH2)SNCH3(CH2)2— where s=2 or 3. -G1 is a radical selected from (IIa) y (IIb); -G2 is a radical selected from H, a radical of formula (IIa), a radical of formula (IIb), the N-radical of 1,8-naphthalimide, the C4-radical of 2-phenylquinoline, and the C9-radical of acridine.

    Substituted Quinolines for the Treatment of Cancer
    5.
    发明申请
    Substituted Quinolines for the Treatment of Cancer 审中-公开
    替代喹啉治疗癌症

    公开(公告)号：US20100331355A1

    公开(公告)日：2010-12-30

    申请号：US12760408

    申请日：2010-04-14

    申请人： Juan Aymami Bofarull ,  Miquel Coll Capella ,  Amadeo Llebaria Soldevila ,  Isabel Navarro Muñoz

    发明人： Juan Aymami Bofarull ,  Miquel Coll Capella ,  Amadeo Llebaria Soldevila ,  Isabel Navarro Muñoz

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P35/00

    CPC分类号： C07D471/04 ,  A61K38/00 ,  C07K5/06026

    摘要： Compounds of formula G1-L-G2, where G1, is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from —(CH2)rNR′″(CH2)s— and —(CH2)rNR′″(CH2)sNR″″(CH2)t—, —R′″ and —R″″ are radicals, same or different, selected from the group consisting of H and (C1-C3)-alkyl; r, s and t are an integer from 1 to 3 and -G2 is H or a radical structurally close to -G1, are intercalators. They are compounds which intercalate between DNA base pairs, and are useful as therapeutic agents against cancer, as assess by an in vitro test of citotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G1 is bonded to -L- through a carbonyl amino and -L- is —(CH2)3NCH3(CH2)3— or —(CH2)2NCH3(CH2)sNCH3(CH2)2— where s=2 or 3.-G1 is a radical selected from (IIa) and (IIb); -G2 is a radical selected from H, a radical of formula (IIa), a radical of formula (IIb), the N-radical of 1,8-naphthalimide, the C4-radical of 2-phenylquinoline and the C9-radical of acridine.

    摘要翻译： 式G1-L-G2的化合物，其中G1是结构上接近隐斜体的基团-L-是单个共价键或共价连接双基，其选自 - （CH 2）r NR'“（CH 2）s - 和 - （ CH2）rNR“”（CH2）sNR“”（CH2）t-，-R'“和-R”“是相同或不同的选自H和（C1-C3） - 烷基的基团; r，s和t是1至3的整数，-G 2是H或结构上接近-G1的基团是嵌入剂。 它们是插入DNA碱基对之间的化合物，并且可用作抗癌剂的治疗剂，如用人类白血病细胞Jurkat E6-1和人类癌细胞GLC-4的体外试验的体外试验评价的。 优选的化合物是其中-G1通过羰基氨基与-L-是 - （CH2）3NCH3（CH2）3-或 - （CH2）2NCH3（CH2）sNCH3（CH2）2-键合的那些化合物，其中s = 2或3 -G1是选自（IIa）和（IIb）的基团; -G2是选自H，式（IIa）的基团，式（IIb）的基团，1,8-萘酰亚胺的N-基，2-苯基喹啉的C4-基和C9-基的基团 吖啶

    Substituted quinolines for the treatment of cancer
    6.
    发明授权
    Substituted quinolines for the treatment of cancer 失效
    用于治疗癌症的取代喹啉

    公开(公告)号：US07728000B2

    公开(公告)日：2010-06-01

    申请号：US10580140

    申请日：2004-11-18

    申请人： Juan Aymami Bofarull ,  Miquel Coll Capella ,  Amadeo Llebaria Soldevila ,  Isabel Navarro Muñoz

    发明人： Juan Aymami Bofarull ,  Miquel Coll Capella ,  Amadeo Llebaria Soldevila ,  Isabel Navarro Muñoz

    IPC分类号： A61K31/4745 ,  C07D471/04

    CPC分类号： C07D471/04 ,  A61K38/00 ,  C07K5/06026

    摘要： Compounds of formula G1-L-G2, where -G1 is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from (CH2)rNR′″(CH2)s and —(CH2)rNR′″(CH2)sNR″″(CH2)t—, —R′″ and —R″″ are radicals, same or different, selected from the group consisting of H and (C1-C3)-alkyl; r, s and t are an integer from 1 to 3 and, -G2 is H or a radical structurally close to -G1, are intercalators. They are compounds which intercalate between DNA base pairs, and are useful as therapeutic agents against cancer, as assess by an in vitro test of cytotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G1 is bonded to -L- through a carbonyl amino and -L- is —(CH2)3NCH3(CH2)3 or —(CH2)2NCH3(CH2)sNCH3(CH2)2— where s =2 or 3. -G1 is a radical selected from (IIa) y (IIb); -G2 is a radical selected from H, a radical of formula (IIa), a radical of formula (IIb), the N-radical of 1,8-naphthalimide, the C4-radical of 2-phenylquinoline, and the C9-radical of acridine.

    摘要翻译： 式G1-L-G2的化合物，其中-G1是结构上靠近隐斜体的基团，-L-是选自（CH 2）r NR“ - （CH 2）s和 - （CH 2）2的单共价键或共价连接双基， （CH 2）n - ， - （CH 2）t - ， - R''和-R“”是相同或不同的选自H和（C 1 -C 3） - 烷基的基团; r，s和t是1至3的整数，-G 2是H或结构上接近-G1的基团是嵌入剂。 它们是插入DNA碱基对之间的化合物，并且可用作抗癌剂的治疗剂，如用人类白血病细胞Jurkat E6-1和人类癌细胞GLC-4的细胞毒性的体外试验评估。 优选的化合物是其中-G1通过羰基氨基与-L-是 - （CH2）3NCH3（CH2）3或 - （CH2）2NCH3（CH2）sNCH3（CH2）2-键合的那些化合物，其中s = 2 或3. -G1是选自（IIa）y（IIb）的基团; -G2是选自H，式（IIa）的基团，式（IIb）的基团，1,8-萘二甲酰亚胺的N-基，2-苯基喹啉的C 4 - 基团和C 9 - 基团 的吖啶。