| 摘要 |
<p>1532574 Tripeptides and tetrapeptides G D SEARLE & CO 4 Feb 1977 [5 Feb 1976] 04791/77 Heading C3H [Also in Division C2] A compound of formula wherein A is H, an N-terminal amino protecting group or a group of formula B-W, wherein B is hydrogen or an N-terminal protecting group and W is Trp or D-Trp; R is H or C 1-6 alkyl; X is Met, D-Met, Nle or D-Nle; Y is a D or DL radical of formula wherein R<SP>1</SP> is C 1-6 alkyl or C 6-7 alkyl (cycloalkyl) or Y is a radical of formula and non-toxic pharmacologically acceptable acid addition salts thereof. In the Examples, compounds (I) prepared are: TRIPEPTIDES: Boc-Met-Asp-T wherein T is D-Ala-NH 2 , DL-2-aminoheptanamide, DL-2-amino-3-cyclopentylpropionamide, DL-2- amino-5-methylhexanamide, DL-Nhe-NH 2 , 2- amino-2-propionamide, DL-2-aminobutanamide D-Val-NH 2 , D-Leu-NH 2 , D-Ala-NH n -C 3 H 7 , N<SP>1</SP>- propyl - 2 - amino - 2 - methylpropionamide; HMet-Asp-T; Boc-Met-Asp-DL-Nva-NH 2 ; Boc- Nle-Asp-D-Ala-NH 2 ; H-Nle-Asp-DL-NH 2 . TETRAPEPTIDES: Boc-Trp-Met-Asp-T; H-Trp-Met-Asp-T; Z-Trp-Met-Asp-DL-Nva- NH 2 ; H-Trp-Met-Asp-DL-Nva-NH 2 ; Boc-Trp- Nle-Asp-D-Ala-NH 2 ; H-Trp-Nle-Asp-D-Ala- NH 2 . Dipeptide intermediates isolated are Z-Asp- (OBz)-T, H-Asp-T. Pharmaceutical compositions, which may be in the form of a tablet, capsule, suppository or solution for parenteral administration and are preferably in unit dosage of 1 to 5 mg. of peptide I, comprises a peptide I in association with a pharmacologically-acceptable carrier. Pharmaceutical compositions exemplified are Boc-Trp-Met-Asp-D-Ala-NH 2 plus (89) lactose, corn starch, polyvinyl pyrrolidone, magnesium stearate (tablet), (90) corn starch, lactose, talc (gelatin capsule), (91) ethanol, sesame oil (solutions), (92) theobroma oil (corn butter) (suppository).</p> |
