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    Quaternary salts of para-dialkylamino benzamide derivatives
    5.
    发明授权
    Quaternary salts of para-dialkylamino benzamide derivatives 失效
    对二烷基氨基苯甲酰胺衍生物的季盐

    公开(公告)号：US5451394A

    公开(公告)日：1995-09-19

    申请号：US111690

    申请日：1993-08-25

    申请人： Ratan K. Chaudhuri ,  Anatoly Alexander ,  Anna A. Gripp

    发明人： Ratan K. Chaudhuri ,  Anatoly Alexander ,  Anna A. Gripp

    IPC分类号： A61K8/41 ,  A61K8/44 ,  A61K8/49 ,  A61Q17/04 ,  C07C233/77 ,  C07C237/34 ,  C07D263/04 ,  C07D295/12 ,  C07D295/13 ,  C07D249/00 ,  A61K7/06 ,  A61K7/42

    CPC分类号： C07D295/13 ,  A61K8/416 ,  A61K8/445 ,  A61K8/49 ,  A61K8/4926 ,  A61Q17/04 ,  C07C237/34 ,  Y10S514/938

    摘要： This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 are each selected from the group of C.sub.1 to C.sub.4 alkyl, hydrogen and, alternatively, R.sub.1 and R.sub.2, together with the attached cationic nitrogen atom can form a 5 to 6-membered heterocyclic ring selected from the group of ##STR2## and X is an anion. These benzamide derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.

    摘要翻译： 本发明涉及具有式“IMAGE”的对二烷基氨基苯甲酰胺的不可水解的，无刺激性的毛发，皮肤和纺织品实质季铵盐，其中R'和R“各自选自C1至C2 烷基; n是2至6的整数; R是具有1至30个碳原子的烷基; R 1和R 2各自选自C 1至C 4烷基，氢和可选地，R 1和R 2与连接的阳离子氮原子一起可以形成选自下列基团的5至6元杂环： IMAGE> ，X是阴离子。 这些苯甲酰胺衍生物是活性防晒剂，其有效用量为约0.5至约10wt。 需要防止阳光对皮肤灼伤，头发损伤，褪色等有害影响的配方中的％。

    Treatment of cancers
    10.
    发明授权
    Treatment of cancers 失效
    癌症治疗

    公开(公告)号：US5891886A

    公开(公告)日：1999-04-06

    申请号：US921331

    申请日：1997-08-29

    申请人： Bruce Charles Baguley ,  Graham John Atwell ,  William Alexander Denny ,  Graeme John Finlay ,  Gordon William Rewcastle

    发明人： Bruce Charles Baguley ,  Graham John Atwell ,  William Alexander Denny ,  Graeme John Finlay ,  Gordon William Rewcastle

    IPC分类号： A61K31/473 ,  A61K31/44 ,  C07C233/77 ,  C07D219/08

    CPC分类号： A61K31/00 ,  A61K31/473

    摘要： A new treatment schedule for administration of N-�2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.

    摘要翻译： 用于施用N- [2-（二甲基氨基）乙基]吖啶-4-甲酰胺和其它相关的羧酰胺抗癌药物的新的治疗方案，其中药物以分次给药方案施用，其包含频繁间隔的两次或更多次给药，用于 例如每小时。 提及产生血浆水平的循环峰/谷的时间表。 该化合物可用于规避癌症中的多药耐药性，并且可以例如与其它细胞毒性药物，特别是非地头性II抑制剂组合使用。 包括黑色素瘤和晚期结肠癌的治疗。