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US 5,512,656 AGranted
Thymosin alpha-1 derivatives
AssigneeAlpha-1 Biomedicals, Inc.
InventorSu-Sun Wang
Life of this patent
Estimating the term…
Abstract
A compound of the formula R.sub.1 -X-R.sub.2 -Y (I) wherein X is Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Ly s-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu, or a biologically active derivative or fragment thereof; R.sub.1 is Ac or Z, wherein Ac is an acetyl group and Z is ##STR1## wherein Ac and X and are defined above; R.sub.2 is Asn or Asp; R.sub.3 is Asn or Asp; Y is --OH or --NH.sub.2 ; with the proviso that when R.sub.1 is Ac and R.sub.2 is Asn, Y is -NH.sub.2. The invention also applies to novel intermediates and precursors of compounds of formula (I) above.
Claims12
A compound of the formula:
- R.sub.1 -X-R.sub.2 -Y (I)
- wherein X is Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Ly s-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu, R.sub.1 is Ac or Z, wherein Ac is an acetyl group and Z is ##STR6## wherein Ac and X are as defined above;
- R.sub.2 is Asp or R.sub.3 ;
- R.sub.3 is Asn;
- and Y is --OH;
- with the proviso that only when R.sub.3 is present does R.sub.2 equal R.sub.3.
3 more elements
The compound, comprised of the formula:
- X.sub.2 -Val-Glu-Glu-Ala-Glu-R.sub.2 (II)
- wherein R.sub.2 is Asp or R.sub.3 ;
- and wherein X.sub.2 is Val, Glu-Val, Lys-Glu-Val, Lys-Lys-Glu-Val, Glu-Lys-Lys-Glu-Val, Lys-Glu-Lys-Lys-Glu-Val, Leu-Lys-Glu-Lys-Lys-Glu-Val, Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Va l, Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Gl u-Val, Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Ly s-Glu-Val, Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Ly s-Lys-Glu-Val, Gly-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Gl u-Lys-Lys-Glu-Val, Lys-Gly-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Ly s-Glu-Lys-Lys-Glu-Val, or Z-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu- Lys-Lys-Glu-Val, wherein Z is represented by the formula:
- ##STR7## wherein R.sub.3 is Asn, and X.sub.3 is Glu, Ala-Glu, Glu-Ala-Glu, Glu-Glu-Ala-Glu, Val-Glu-Glu-Ala-Glu, or X.sub.4 -Val-Glu-Glu-Ala-Glu, wherein X.sub.4 is Val, Glu-Val, Lys-Glu-Val, Lys-Lys-Glu-Val, Glu-Lys-Lys-Glu-Val, Lys-Glu-Lys-Lys-Glu-Val, Leu-Lys-Glu-Lys-Lys-Glu-Val, Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Va l, Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Gl u-Val, Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Ly s-Glu-Val, Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Ly s-Lys-Glu-Val;
- with the proviso that when R.sub.2 is Asn, X.sub.2 is Gly-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Gl u-Lys-Lys-Glu-Val, Lys-Gly-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Ly s-Glu-Lys-Lys-Glu-Val, or Z-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu- Lys-Lys-Glu-Val, and with the further proviso that R.sub.2 =R.sub.3 only when Z is present.
2 more elements
Dependencies are inferred from the claim text.