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Last Updated: April 19, 2024

Claims for Patent: 4,596,675


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Summary for Patent: 4,596,675
Title: Novel thiopeptolide substrates for vertebrate collagenase
Abstract:The disclosure relates to novel synthetic thiopeptolide substrates having high activity for the enzyme collagenase. These substrates have the following amino acid sequences: wherein R=H or N-protecting group, X=Leu, Ile, Phe, Val, Gln, Ala, Y=Leu, Ile, Phe, Val, Ala, Z=Leu, Ile, Phe, Val, Gln, Ala, and R.sub.1 =terminal amide, carboxyl or ester group.
Inventor(s): Weingarten; Harold I. (University City, MO), Feder; Joseph (University City, MO)
Assignee: Monsanto Company (St. Louis, MO)
Application Number:06/780,116
Patent Claims:1. A thiopeptolide having activity as a substrate for vertebrate collagenase selected from the group consisting of:

wherein

R=H or N-protecting group,

X=Leu, Ile, Phe, Val, Gln, Ala,

Y=Leu, Ile, Phe, Val, Ala,

Z=Leu, Ile, Phe, Val, Gln, Ala,

R.sub.1 =terminal amide, carboxyl or ester group,

and the pharmaceutically acceptable salts thereof.

2. The thiopeptolide of claim 1 in which

X=Leu or Ala,

Y=Leu, and

Z=Leu, Ala or Phe.

3. The thiopeptolide of claim 2 having the structure

4. The thiopeptolide of claim 2 having the structure

5. The thiopeptolide of claim 2 having the structure

6. The thiopeptolide of claim 2 having the structure

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