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    • 5. 发明申请
    • Substituted Quinolines for the Treatment of Cancer
    • 替代喹啉治疗癌症
    • US20100331355A1
    • 2010-12-30
    • US12760408
    • 2010-04-14
    • Juan Aymami BofarullMiquel Coll CapellaAmadeo Llebaria SoldevilaIsabel Navarro Muñoz
    • Juan Aymami BofarullMiquel Coll CapellaAmadeo Llebaria SoldevilaIsabel Navarro Muñoz
    • A61K31/437C07D471/04A61P35/00
    • C07D471/04A61K38/00C07K5/06026
    • 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.
    • 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
    • 6. 发明授权
    • Substituted quinolines for the treatment of cancer
    • 用于治疗癌症的取代喹啉
    • US07728000B2
    • 2010-06-01
    • US10580140
    • 2004-11-18
    • Juan Aymami BofarullMiquel Coll CapellaAmadeo Llebaria SoldevilaIsabel Navarro Muñoz
    • Juan Aymami BofarullMiquel Coll CapellaAmadeo Llebaria SoldevilaIsabel Navarro Muñoz
    • A61K31/4745C07D471/04
    • C07D471/04A61K38/00C07K5/06026
    • 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.
    • 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。