| 摘要 |
1,173,437. Pentacosa peptide. SANDOZ Ltd. 9 Dec., 1966 [12 Jan., 1966], No. 55296/66. Heading C2C. The pentacosa peptides H-D-Ser-Tyr-Ser- Nle - X - His - Phe - Arg - Thy - Gly - Lys - Pro- Val - Gly - Lys - Lys - Lys - Lys - Pro - Val - Lys- Val-Tyr-Pro-ValNH 2 , where X is Glu (OH) or Glu (NH 2 ), and their acid addition salts and complexes with heavy metals are prepared by removing the protecting groups from N-R<SP>1</SP>-DSer - Tyr - Ser - Nle - Glu (NH 2 ) or Glu (OtBu)- (Trit)His - Phe-Arg -Try- Gly- # - N - R - Lys - Pro- Val - Gly - # - H - Lys - # - N - R - Lys - #- N - H - Lys - # - N - R - Lys - Pro - Val - # - NR - Lys - Val - Tyr - Pro - Val - NH 2 , where R=BOC or carbo-t-amyloxy and R<SP>1</SP>= Trityl, BOC or carbo-t-amyloxy, and forming the salts or complexes. The following starting materials and intermediates are prepared: BOC - Tyr - Ser - Nle- OMe, H - Tyr - Ser - Nle - OMe, HCl; BOCD - Ser - OMe and -NHNH 2 ; BOC - D - Ser- Tyr - Ser - Nle - OMe and -NH.NH 2 and -N 3 ; (BOC) - Glu (NH 2 ) - His - Phe - OMe; Trit- Glu (NH 2 ) - (Trit) His Phe OMe and -NHNH 2 ; (Trit) Glu (NH 2 ) - (Trit) His - Phe - Arg - Try- Gly - BOC - Lys - Pro OH; (Trit) Glu (NH 2 ). (Trit) His - Phe Arg - Try - Gly - (BOC) Lys Pro OCP, HCl; (Trit) - Glu (NH 2 ) - (Trit) His- Phe - Arg - Try - Gly - (BOC) Lys - Pro - Val- Gly (BOC) Lys (BOC) Lys (BOO) - Lys - (BOC) Lys - Pro - Val - (BOC) Lys - Val - Tyr - Pro- Val NH 2 and the N - unprotected heneicosa peptide. Pharmaceutical compositions comprise the pentacosa peptides of the invention and a suitable carrier. The compositions may be formulated for enteral and parenteral administration. Reference has been directed by the Comptroller to Specification 1,119,353. |
