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METHOD FOR PREPARING FOR SOMATOSTATIN PEPTIDE ANALOGUES WITH TREONINE IN THE SIXTH POSITION

机译:在第六位置上用苏氨酸制备生长抑素肽类似物的方法

摘要

A compound of the formula: IMAGE wherein each A1 and A2, independently, is H, C1-12 alkyl, C7-10 phenylalkyl, R1CO (where R1 is C1-20 alkyl, C3-20 alkenyl, C3-20 alkinyl, phenyl, naphthyl, or C7-10 phenylalkyl), or R2OCO (where R2 is C1-10 alkyl or C7-10 phenylalkyl), provided that when one of A1 or A2 is R1CO or R2OCO, the other must be H; each X1 and X2, independently, is H, F, Cl, Br, OH, CH3, or CF3, provided that at least one of X1 and X2 must be H; A3 is Phe or Tyr; and A4 is OH, NH2, or NH-R3 (wherein R3 is a saturated aliphatic C1-8 alkyl); or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.
机译:式:的化合物,其中每个A1和A2独立地为H,C1-12烷基,C7-10苯基烷基,R1CO(其中R1为C1-20烷基,C3-20烯基,C3-20炔基,苯基,萘基或C7-10苯基烷基)或R2OCO(其中R2为C1-10烷基或C7-10苯基烷基),条件是当A1或A2中的一个为R1CO或R2OCO时,另一个必须为H; X1和X2各自独立地为H,F,Cl,Br,OH,CH3或CF3,条件是X1和X2中至少一个必须为H; A3是Phe或Tyr; A4为OH,NH2或NH-R3(其中R3为饱和脂族C1-8烷基);或其药学上可接受的盐。还描述了含有本发明化合物的治疗组合物及其使用方法。

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