首页>
外国专利>
Anticancer composition, especially for treating melanoma, containing peptide with L-m-sarcolysine residue(s) as active agent and cyclodextrin sulfoalkyl ether as carrier providing high bioavailability
Anticancer composition, especially for treating melanoma, containing peptide with L-m-sarcolysine residue(s) as active agent and cyclodextrin sulfoalkyl ether as carrier providing high bioavailability
In a pharmaceutical composition (A) for treating cancer diseases, containing a peptide compound (I) in delayed release form as active agent, (a) (I) is selected from six specific tri-, tetra- or pentapeptides containing at least one L-m-sarcolysine residue and (b) (A) additionally contains a cyclodextrin (II), containing at least one sulfoalkyl ether salt substituent, as auxiliary or carrier. In a pharmaceutical composition (A) for treating cancer diseases, containing at least one peptide compound (I) in delayed release form as active agent, (a) (I) is selected from L-seryl-L-p-fluorophenylalanyl-L-m-sarcolysine, L-prolyl-L-m-sarcolysyl-L-p-fluorophenylalanine (Ia), L-m-sarcolysyl-N-nitro-L-arginyl-L-norvaline, L-p-fluorophenylalanyl-L-m-sarcolysyl-L-asparagine, L-p-fluorophenylalanyl-glycyl-L-m-sarcolysyl-L-norvaline and L-m-sarcolysyl-L-arginyl-L-lysyl-L-m-sarcolysyl-L-histidine (or their lower alkyl esters and/or acid addition salts) and (b) (A) additionally contains at least one substituted cyclodextrin (II), containing at least one substituent of formula -O-R-SO3-.M+, as auxiliary or carrier. R = 2-6C alkylene; M+ = counter-ion.
展开▼
机译:在包含延迟释放形式的肽化合物(I)作为活性剂的用于治疗癌症疾病的药物组合物(A)中,(a)(I)选自含有至少一个Lm的六种特定的三肽,四肽或五肽-肌氨酸残基和(b)(A)还含有环糊精(II),其含有至少一个磺烷基醚盐取代基作为助剂或载体。在包含至少一种延迟释放形式的肽化合物(I)作为活性剂的用于治疗癌症的药物组合物(A)中,(a)(I)选自L-丝氨酰-Lp-氟苯基丙氨酰基-Lm-肌氨酸。 L-脯氨酰-Lm-糖基-Lp-氟苯丙氨酸(Ia),Lm-糖基-N-硝基-L-精氨酸-L-正缬氨酸,Lp-氟苯丙氨酰基-Lm-糖基-L-天冬酰胺,Lp-氟苯丙氨酰基-糖基-Lm -糖基-L-正缬氨酸和Lm-糖基-L-精氨酸-L-赖基-Lm-糖基-L-组氨酸(或它们的低级烷基酯和/或酸加成盐),并且(b)(A)另外包含至少一种取代的环糊精(II),其包含至少一个式-OR-SO3-.M +的取代基作为助剂或载体。 R = 2-6C亚烷基; M + =抗衡离子。
展开▼