药物输送装置和检测接触的方法_2

文档序号:8268222阅读:来源:国知局

[0028]其中在又一个实施方案中,所述药学活性化合物包括至少一种人胰岛素或人胰岛素类似物或衍生物、胰高血糖素样肽(glucagon-like peptide, GLP-1)或其类似物或衍生物、或毒蜥外泌肽-3 (exedin-3)或毒蜥外泌肽_4 (exedin-4)或毒蜥外泌肽_3或毒蜥外泌肽-4的类似物或衍生物。
[0029]胰岛素类似物例如Gly (A21)、Arg (B31)、Arg (B32)人胰岛素;Lys(B3)、Glu (B29)人胰岛素;Lys(B28)、Pro(B29)人胰岛素;Asp (B28)人胰岛素;人胰岛素,其中B28位的脯氨酸被替换为Asp、Lys, Leu、Val或Ala且其中B29位的赖氨酸可以替换为Pro ;Ala(B26)人胰岛素;Des(B28-B30)人胰岛素;Des(B27)人胰岛素jPDes(B30)人胰岛素。
[0030]膜岛素衍生物例如B29-N-肉?蓮酸-des (B30)人膜岛素;B29_N_掠桐酰-des(B30)人胰岛素;B29-N-肉豆蘧酰人胰岛素;B29_N_棕榈酰人胰岛素;Β28_Ν_肉豆蘧酰LysB28ProB29人胰岛素;Β28_Ν_棕榈酰_LysB28ProB29人胰岛素;B30_N_肉豆蘧酰-ThrB29LysB30 人胰岛素;B30_N_ 棕榈酰 _ThrB29LysB30 人胰岛素;B29_N_(N-棕榈酰-T-谷氨酰)-des(B30)人胰岛素;B29-N-(N-石胆酰-T-谷氨酰)-des(B30)人胰岛素;B29_N_ (ω -竣基十七酸)_des (B30)人膜岛素和B29-N- (ω -竣基十七酸)人膜岛素。
[0031]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-GIy-GIu-GIy-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-GIn-Met-GIu-GIu-GIu-AIa-Va1-Arg-Leu-Phe-1Ie-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2o
[0032]毒蜥外泌肽-4衍生物例如选自下述化合物列表:
[0033]H- (Lys) 4_des Pro36, des Pro37 毒蜥外泌肽 _4 (1-39) -NH2,
[0034]H- (Lys) 5_des Pro36, des Pro37 毒蜥外泌肽 _4 (1-39) -NH2,
[0035]des Pro36 [Asp28]毒晰外泌妝 _4 (1-39),
[0036]des Pro36 [IsoAsp28]毒晰外泌妝 _4 (1-39),
[0037]des Pro36 [Met (O) 14,Asp28]毒蜥外泌肽 _4 (1-39),
[0038]des Pro36 [Met (O) 14,IsoAsp28]毒晰外泌妝 _4 (1-39),
[0039]des Pro36 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0040]des Pro36 [Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0041 ]des Pro36 [Met (O) 14 Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0042]des Pro36[Met(0) 14 Trp (02)25, IsoAsp28]毒蜥外泌肽 _4 (1-39);或
[0043]des Pro36 [Asp28]毒晰外泌妝 _4 (1-39),
[0044]des Pro36 [IsoAsp28]毒晰外泌妝 _4 (1-39),
[0045]des Pro36 [Met (O) 14,Asp28]毒晰外泌妝 _4 (1-39),
[0046]des Pro36 [Met (O) 14,IsoAsp28]毒晰外泌妝 _4 (1-39),
[0047]des Pro36 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0048]des Pro36 [Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0049]des Pro36 [Met (O) 14 Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0050]des Pro36 [Met (O) 14 Trp (02) 25,IsoAsp28]毒蜥外泌肽-4 (1-39),
[0051]其中-Lys6_NH2基团可以结合于毒蜥外泌肽_4衍生物的C端;
[0052]或下述序列的毒蜥外泌肽-4衍生物:
[0053]H- (Lys) 6~des Pro36 [Asp28]毒晰外泌妝 _4 (1-39)-Lys6_NH2,
[0054]des Asp28 Pro36, Pro37, Pro38 毒蜥外泌肽 _4 (1-39) -NH2,
[0055]H- (Lys) 6_des Pro36, Pro38 [Asp28]毒晰外泌妝-4 (1-39) -NH2,
[0056]H-Asn- (Glu) 5des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0057]des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0058]H- (Lys) 6_des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0059]H-Asn - (Glu) 5~des Pro36, Pro37, Pro38 [Asp28]毒晰外泌肽-4(l-39)-(Lys)6-NH2,
[0060]H- (Lys) 6_des Pro36 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39) -Lys6-NH2,
[0061 ]H-des Asp28 Pro36, Pro37, Pro38 [Trp (02) 25]毒蜥外泌肽 _4 (1-39) -NH2,
[0062]H-(Lys) 6_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒晰外泌肽-4(1-39)-ΝΗ2,
[0063]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒晰外泌肽-4(1-39)-ΝΗ2,
[0064]des Pro36, Pro37, Pro38 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0065]H-(Lys) 6_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒晰外泌肽-4(l-39)-(Lys)6-NH2,
[0066]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒晰外泌肽-4(l-39)-(Lys)6-NH2,
[0067]H- (Lys) 6_des Pro36 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -Lys6_NH2,
[0068]des Met (0) 14 Asp28 Pro36, Pro37, Pro38 毒蜥外泌肽 _4 (1-39) -NH2,
[0069]H- (Lys) 6-desPro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0070]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒晰外泌肽-4(1-39)-ΝΗ2,
[0071 ] des Pro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
当前第2页1 2 3 4 
网友询问留言 已有0条留言
  • 还没有人留言评论。精彩留言会获得点赞!
1