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

机译:抗癌组合物,特别是用于治疗黑素瘤的抗癌组合物,其包含具有L-m-肌氨酸残基的肽作为活性剂和环糊精磺烷基醚作为载体,具有高生物利用度

摘要

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.
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。

著录项

  • 公开/公告号CH693558A5

    专利类型

  • 公开/公告日2003-10-15

    原文格式PDF

  • 申请/专利权人 PTC PHARMA AG;

    申请/专利号CH19980001643

  • 发明设计人 MEHLEM FRANCESCO;

    申请日1998-08-06

  • 分类号A61K38/06;A61K38/07;A61K38/08;A61P35/00;

  • 国家 CH

  • 入库时间 2022-08-21 23:42:43

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