具有针保护件的药物输送装置的制造方法_3

文档序号:9251644阅读:来源:国知局
)人膜岛素和B29-N- (ω -幾基十七醜)人膜岛素。
[0055]毒蜥外泌肽-4意指例如毒蜥外泌肽-4 (1-39),其是具有下述序列的肽:H His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-LyS-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-1le-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser_NH20
[0056]毒蜥外泌肽-4衍生物例如选自下述化合物列表:
[0057]H- (Lys) 4~des Pro36, des Pro37 毒嫩外泌狀 _4 (1-39) _NH2,
[0058]H- (Lys) 5~des Pro36, des Pro37 毒嫩外泌狀 _4 (1-39) _NH2,
[0059]des Pro36 [Asp28]毒嫩外泌狀-4 (1-39),
[0060]des Pro36 [IsoAsp28]毒嫩外泌狀-4 (1-39),
[0061]des Pro36[Met(0) 14,Asp28]毒蜥外泌肽-4(1-39),
[0062]des Pro36 [Met (0) 14,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0063]des Pro36 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0064]des Pro36 [Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0065]des Pro36 [Met (0) 14Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0066]des Pro36 [Met (0) 14Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39);或
[0067]des Pro36 [Asp28]毒嫩外泌狀-4 (1-39),
[0068]des Pro36 [IsoAsp28]毒嫩外泌狀-4 (1-39),
[0069]des Pro36 [Met (0) 14, Asp28]毒嫩外泌狀-4 (1-39),
[0070]des Pro36 [Met (0) 14, IsoAsp28]毒嫩外泌狀-4 (1-39),
[0071]des Pro36[Trp(02)25, Asp28]毒蜥外泌肽-4(1-39),
[0072]des Pro36 [Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0073]des Pro36 [Met (0) 14Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0074]des Pro36 [Met (0) 14Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0075]其中-Lys6-NH2基团可以结合于毒蜥外泌肽_4衍生物的C端;
[0076]或下述序列的毒蜥外泌肽-4衍生物
[0077]H- (Lys) 6~des Pro36 [Asp28]毒嫩外泌狀 _4 (1-39)-Lys6_NH2,
[0078]des Asp28Pro36, Pro37, Pro38 毒蜥外泌肽 _4 (1-39) -NH2,
[0079]H- (Lys) 6_des Pro36, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0080]H-Asn- (Glu) 5des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0081 ]des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0082]H- (Lys) 6_des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0083]H-Asn - (Glu) 5~des Pro36, Pro37, Pro38 [Asp28]毒嫩外泌肽-4 (1-39)-(Lys) 6-NH2,
[0084]H- (Lys) 6_des Pro36 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39) -Lys6-NH2,
[0085]H-des Asp28Pro36, Pro37, Pro38 [Trp (02) 25]毒蜥外泌肽 _4 (1-39) -NH2,
[0086]H-(Lys) 6_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒嫩外泌肽-4(1-39)-ΝΗ2,
[0087]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒嫩外泌肽-4(1-39)-ΝΗ2,
[0088]des Pro36, Pro37, Pro38 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0089]H-(Lys) 6_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒嫩外泌肽-4 (1-39)-(Lys) 6-NH2,
[0090]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒嫩外泌肽-4 (1-39)-(Lys) 6-NH2,
[0091 ]H- (Lys) 6_des Pro36 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -Lys6_NH2,
[0092]des Met (0) 14Asp28Pro36, Pro37, Pro38 毒蜥外泌肽 _4 (1-39) -NH2,
[0093]H- (Lys) 6-desPro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0094]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒嫩外泌肽-4(1-39)-ΝΗ2,
[0095]des Pro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0096]H_ (Lys) 6_des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒嫩外泌肽-4 (1-39)-(Lys) 6-NH2,
[0097]H-Asn-(Glu) 5des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒嫩外泌肽-4 (1-39)-(Lys) 6-NH2,
[0098]H-Lys6-des Pro36 [Met (0) 14, Trp (02) 25, Asp28]毒嫩外泌月太-4(l-39)-Lys6-NH2,
[0099]H-des Asp28Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25]毒嫩外泌肽-4(1-39)-ΝΗ2,
[0100]H- (Lys) 6-des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒蜥外泌肽 _4 (1-39)-NH2,
[0101]H-Asn-(Glu)5_des Pro36,Pro37, Pro38[Met(0)14,Trp(02)25,Asp28]毒蜥外泌肽-4(1-39)-ΝΗ2,
[0102]des Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25, Asp28]毒嫩外泌肽-4 (1-39)-(Lys) 6-NH2,
[0103]H-(Lys)6-des Pro36, Pro37, Pro38[Met(0)14, Trp(02)25, Asp28]毒蜥外泌肽-4 (Sl-39)-(Lys)6-NH2,
[0104]H-Asn-(Glu) 5-des Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25, Asp28]毒蜥外泌肽-4 (1-39)-(Lys)6-NH2 ;
[0105]或前述任一种毒蜥外泌肽-4衍生物的药学可接受盐或溶剂合物。
[0106]激素例如在Rote Liste, ed.2008,第50章中列出的垂体激素(hypophysishormones)或下丘脑激素(hypothalamus hormones)或调节性活性月太(regulatoryactive peptides)和它们的措抗剂,诸如促性腺激素(促滤泡素(Follitropin)、促黄体激素(Lutropin)、绒毛膜促性腺激素(Chor1ngonadotropin)、绝经促性素(Menotropin))、Somatropine (生长激素(Somatropin))、去氨加压素(Desmopressin)、特利加压素(Terlipressin)、戈那瑞林(Gonadorelin)、曲普瑞林(Triptorelin)、亮丙瑞林(Leuprorel
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