Claims
- 1. A compound comprising an amino acid sequence having an N-terminal blocking group and a C-terminal Asp residue connected to an electronegative leaving group, wherein said amino acid sequence correspond to the sequence Ala-Tyr-Val-His-Asp, residues 112 to 116 of Seq. I.D. No. 3.
- 2. A compound according to claim 1 having the formula:
- Z--Q.sub.2 -Asp-Q.sub.1
- where Z is an N-terminal protecting group;
- Q.sub.2 is such that the sequence Q.sub.2 -Asp corresponds to the sequence Ala-Tyr-Val-His-Asp, residues 112 to 116 of Seq. I.D. No. 3; and Q.sub.1 is an electronegative leaving group.
- 3. The compound according to claim 2 wherein Z is C.sub.1 -C.sub.6 alkyl, benzyl, acetyl, C.sub.1 -C.sub.6 alkoxycarbonyl, benzyloxycarbonyl or C.sub.1 -C.sub.6 alkyl carbonyl.
- 4. The compound according to claim 2 wherein Z is t-butoxycarbonyl, acetyl or benzyloxycarbonyl.
- 5. The compound according to claim 2 wherein Q.sub.1 is an aldehyde, a diazomethyl ketone or a halomethyl ketone.
- 6. The compound according to claim 2 wherein Q.sub.1 is fluoromethyl ketone.
- 7. A pharmaceutical composition comprising a physiologically acceptable carrier and a compound of the formula:
- Z--Q.sub.2 -Asp-Q.sub.1
- where Z is an N-terminal protecting group;
- Q.sub.2 is 0 to 4 amino acids such that Q.sub.2 -Asp corresponds to the sequence Ala-Tyr-Val-His-Asp, residues 112 to 116 of Seq. I.D. No. 3; and
- Q.sub.1 is an electronegative leaving group.
- 8. The composition according to claim 7 wherein Z is C.sub.1 -C.sub.6 alkyl, benzyl, acetyl, C.sub.1 -C.sub.6 alkoxycarbonyl, benzyloxycarbonyl or C.sub.1 -C.sub.6 alkoxycarbonyl, benzyloxycarbonyl or C.sub.1 -C.sub.6 alkyl carbonyl.
- 9. The composition according to claim 7 wherein Z is t-butoxycarbonyl, acetyl or benzyloxycarbonyl.
- 10. The composition according to claim 7 wherein Q.sub.1 is an aldehyde, a diazomethyl ketone or a halomethyl ketone.
- 11. The composition according to claim 7 wherein Q.sub.1 is fluoromethyl ketone.
CROSS REFERENCE TO RELATED APPLICATIONS
This application is a division of application Ser. No. 08/203,716, now U.S. Pat. No. 5,416,013, filed Feb. 28, 1998 which in turn is a continuation of application Ser. No. 07/750,644, filed on Aug. 30, 1991, now abandoned.
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Divisions (1)
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203716 |
Feb 1994 |
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Continuations (1)
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750644 |
Aug 1991 |
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