首页> 外国专利> Compound, composition, use of a compound, and methods for inhibiting telomerase in vitro or in vivo, for regulating cell proliferation in vitro or in vivo, and for treating a proliferative condition.

Compound, composition, use of a compound, and methods for inhibiting telomerase in vitro or in vivo, for regulating cell proliferation in vitro or in vivo, and for treating a proliferative condition.

机译:化合物,组合物,化合物的用途以及在体外或体内抑制端粒酶,在体外或体内调节细胞增殖以及治疗增殖性疾病的方法。

摘要

"COMPOUND, COMPOSITION, USE OF A COMPOUND, AND METHODS FOR INHIBITING IN VITRO OR IN VIVO TELOMERASE, FOR REGULATING IN VITRO OR IN VIVO CELL PROLIFERATION, AND FOR TREATMENT OF A PROLIFERATIVE CONDITION". This invention belongs to certain acridone and acridine compounds of Formula (1) that inhibit telomerase, regulate cell proliferation, etc. and / or treat cancer, proliferative conditions, etc .; where: (a) K is = o, L is -H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J 1 is a 2 or 3 substituent; R 2 is a 6 or 7 substituent; They are each a group of the formula -N (R 2 N 3) - W, wherein: R 2 N 2 is a nitrogen substituent and is hydrogen, C 1 -C 7 alkyl, C 3 -C 20 heterocyclyl or C 5 -C 20 aryl and is optionally substituted; and W is C 1 -C 7 alkyl, C 3 -C 20 heterocyclyl or C 5 -C 20 aryl and is optionally substituted; and wherein, when K is a 9-substituent, K is a group of Formula -N (R 2 N 3) - q, where: R 2 N 4 is an amino substituent and is hydrogen, C 1-1. C1-7 alkyl, C1-3 heterocyclyl or C1-5 aryl; and Q is C 1 -C 7 alkyl, C 3 -C 20 heterocyclyl or C 5 -C 20 aryl and is optionally substituted; and their pharmaceutically acceptable salts, esters, amides, solvates, hydrates and protected forms. The present invention also pertains to pharmaceutical compositions comprising such compounds and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, etc. and / or cancer treatment, proliferative conditions, etc.
机译:“化合物,组合物,化合物的使用以及体外或体内端粒酶抑制,体外或体内细胞增殖调控以及增殖条件的治疗方法”。本发明属于某些式(1)的a啶酮和a啶化合物,它们可抑制端粒酶,调节细胞增殖等和/或治疗癌症,增殖性疾病等。其中:(a)K为= o,L为-H,α单键,β为双键,γ为单键(ac啶酮); (b)K是9个取代基,L不存在,α是双键,β是单键,γ是双键(ac啶);或其中J 1是2或3个取代基;和R 2为6或7取代基;它们各自是式-N(R 2 N 3)-W的基团,其中:R 2 N 2是氮取代基并且是氢,C 1 -C 7烷基,C 3 -C 20杂环基或C 5- C 20芳基并且是任选取代的; W是C 1 -C 7烷基,C 3 -C 20杂环基或C 5 -C 20芳基,并且是任选取代的;其中,当K为9个取代基时,K为式-N(R 2 N 3)-q的基团,其中:R 2 N 4为氨基取代基,为氢,C 1-1。 C1-7烷基,C1-3杂环基或C1-5芳基; Q是C 1 -C 7烷基,C 3 -C 20杂环基或C 5 -C 20芳基,并且是任选取代的;及其药学上可接受的盐,酯,酰胺,溶剂化物,水合物和保护形式。本发明还涉及包含此类化合物的药物组合物以及此类化​​合物和组合物在体外和体内在抑制端粒酶,调节细胞增殖等和/或癌症治疗,增殖性疾病等中的用途。

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