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1. 发明申请

US20070105784A1 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.

2. 发明申请

US20100331355A1 Substituted Quinolines for the Treatment of Cancer 审中-公开
标题翻译：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

3. 发明授权

US07728000B2 Substituted quinolines for the treatment of cancer 失效
标题翻译：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。

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