TH17364A - - Google Patents

Abstract

Compounds with the formula as follows: R1-X-R2-Y (I), where X is Ser-Asp-Ala-Ab-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp- Leu-. Lys-Glu-Lys-Lys-Glu-Val-Glu-Glu-Ala-Glu or nuptials or fragments of these sequences. Biologically active R1 is Ac or Z, where Ac is the acetic group, and Z is (chemical formula), which Ac and X signify above, R2 is Asn or Asp.

Claims (2)

1. Compounds with the following formula: R1-X-R2Y (I), where X is Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu- Ile-Thr-Thr-Lys-Asp-Leu-. Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu- Ala-Glu, R1 is Ao or Z, where Ac is the azetic group and Z is (chemical formula), which Ac and X have the following meanings: As defined above, R2 is Asp or R3, R3 is Asn, and Y is -OH, provided that when R3 is present, R2 equals R3. 2. The compound of claim 1 where R1 is Z, R3 is Asn, R2 is Asn, and Y is -OH 3. Compound with formula: X2 - Val-Glu-Glu-Ala-Glu, R2 (II) where R2 is Asp or R3 and which X2 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, Se r-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-Val, Ala-Ala-Val-Asp-Thr-Ser-Ser- Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys- Glu-Lys-Lys-Glu-Val, Asp-Ala- Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu- Lys-Lys-Glu- Val, Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile- Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Gly-Ser- Asp-Ala- Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu- Lys-Lys-Glu-Val, Lys-Gly-Ser-Asp- Ala-Ala-Val-Asp-Thr-Ser-Ser- Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-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, which z can be replaced with the following formula (chemical formula), where R3 Is Asn, and X3 is Glu, Ala-Glu, Glu-Ala-Glu, Glu-G. lu-Alu-Glu, Val-Glu-Glu-Ala-Glu, or X4 -Val, Glu-Glu-Ala- Glu, where X4 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, lie- 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-Val, Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys- Asp-Leu-Lys-Glu-Lys-Lys-Glu- Val, Asp-Ala-Ala-Val-Asp-Thr-Ser- Ser-Glu-Ile-Thr-Thr-Lys -Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Ser- Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu- Lys -Glu-Lys-Lys-Glu-Val, provided that when R2 is Asn, X2 is Gly-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu- Ile-Thr-Thr-Lys. -Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Lys-Gly-Ser- Asp-Ala-Ala- Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp - Leu-Lys-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 condition ahead R2 = R3 when Z is present only 4. Compound of claim 3, X2 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 or Asp-Leu-Lys-Glu. -Lys- Lys-Glu-Val. 5. Compound of claim 3, which X2 is 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-Il e-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, or Ser-Ser-Glu-Ile-Thr-Thr-Lys- Asp-Leu-Lys-Glu-Lys-Lys- Glu-Val. 6. Compound of claim 3, where X2 is 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-Val, Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu -Ile- Thr-Thr-Lys- Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, Asp-Ala-Ala-Val- Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys - Asp-Leu-Lys-Glu-Lys-Lys- Glu-Val, or Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr- Thr-Lys- Asp-Leu- Lys-Glu-Lys-Lys-Glu-Val, 7. Clause 3 Compound of which X2 is Gly-Ser-Asp-Ala-Ala- Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-. Thr-Lys-Asp-Leu-Lys-Glu-Lys- Lys-Glu-Val. 8. Compound of Clause 3 of which X2 is Lys- Gly-Ser-Asp-Ala- Ala-Val-Asp-Thr. -Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu- -Lys-Lys-Glu-Val. 9. Compound of claim 3, where R2 = R3 X2 is Z- Gly. -Ser-Asp- Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys- Glu-Lys-Lys-Glu-Val, which Z is replaceable. With this formula, R3 is Asn, X3 is Glu, Ala-Glu, Glu-Alu-Glu, Glu-Glu- Ala-Glu or Val-Glu-Glu-Ala-Glu. 1 0. Clause 3 claim compound. Which X2 is Z-Ser-Asp-Ala-Ala-Val-Asp- Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val, which Z can be represented by (chemical formula), where R3 is Asn and X3 is X4-Val-Glu-Glu-Ala-Glu, where X4 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 or Asp-Leu-Lys-Glu-Lys-Lys- Glu-Val.1 1. Compound of Clause 3 of which X2 is Z-Ser-Asp-Ala-Ala-Val- Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-. Lys-Lys- Glu-Val, Z is represented by the following formula (chemical formula) where R3 is Asn and X3 is X4-Val-Glu-Glu-Ala-Glu, where X4 is 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 or Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu. -Lys-Lys-Glu-Val.1 2. Compound of Clause 3, X2 is Z-Ser-Asp-Ala-Ala- Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-. Lys- Lys-Glu-Val, Z is represented by the following formula (chemical formula) where R3 is Asn and X3 is X4-Val-Glu-Glu-Ala-Glu, where X4 is 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-Val, Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr -Thr-Lys-Asp-Leu-Lys- Glu-Lys-Lys-Glu-Val, Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile- Thr-Thr-Lys-Asp-Leu -Lys-Glu-Lys-Lys-Glu-Val or Ser-Asp-Ala- Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu- Lys -Lys-Glu-Val.