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US 4,908,475 AGranted
Intermediates for preparing 1,6-dicarba-vasopressin compounds
AssigneeSmithKline Beckman Corporation
InventorsJames F. Callahan, William F. Huffman, Kenneth A. Newlander, Nelson C. F. Yim
Life of this patent
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Abstract
New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by a Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
Claims5
A chemical compound having the formula:
- ##STR17## in which:
- * is to indicate D isomer, L isomer or a D, L mixture;
- m is an integer of from 2-4;
- n is 0 or 1;
- R and R.sup.1 are, each, hydrogen or a carboxy protecting group;
- and
- R.sup.2 is hydrogen or an amino protecting group.
4 more elements
Dependencies are inferred from the claim text.