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Last Updated: September 18, 2021

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Claims for Patent: 5,100,874

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Summary for Patent: 5,100,874
Title: Hydroxamic acid tetrapeptide derivatives
Abstract:New peptide derivatives of which utility in the treatment of such diseases as rheumatoid arthritis, peridental diseases, corneal ulcer and epidermolysis bullosa is expected. These compounds are hydroxamic acid derivatives of tetrapeptides having a specific inhibitory activity against collagenase derived from vertebrates.
Inventor(s): Odake; Shinjiro (Takaoka, JP), Okayama; Toru (Ishikawa, JP), Obata; Masami (Toyama, JP), Morikawa; Tadanori (Toyama, JP), Nagai; Yutaka (Koshigaya, JP)
Assignee: Fuji Yakuhin Kogyo Kabushiki Kaisha (Toyama, JP)
Application Number:07/392,931
Patent Claims:1. A peptidylhydroxamic acid derivative of the general formula:

wherein X.sup.1 is a residue of an .alpha.-amino acid selected from glycine and sarcosine, X.sup.2 is a residue of an amino acid selected from proline, hydroxyproline, thioproline and alaine, X.sup.3 is a residue of an amino acid selected from glutamine, glutamic acid, leucine, isoleucine and phenylalanine and X.sup.4 is a residue of an .alpha.-amino acid selected from glycine, alanine, valine, leucine and sarcosine; and the carboxyl group of .alpha.-amino acide X.sup.1 forms a peptide bond together with the amino group of .alpha.-amino acid X.sup.2, the carboxyl group of .alpha.-amino acid and acid X.sup.2 forms a peptide bond together with the amino group of .alpha.-amino acid X.sup.3, the caboxyl group of .alpha.-amino acid X.sup.3 forms a peptide bond together with the amino group of .alpha.-amino acid X.sup.4 and the carboxyl group of .alpha.- amino acid X.sup.4 forms an amido together with --NHOH; and the hydrogen atom of the amino group in said .alpha.-amino acids X.sup.1 may be replaced with a member selected from the group consisting of acetyl, benzoyl, benzyloxy, t-butyloxycarbonyl, benzyloxycarbonyl, p-aminobenzoyl, p-amino-benzyl, p-hydroxybenzoyl or a pharmaceutically acceptable salt thereof.

2. The peptidylhydroxamic acid derivative according to claim 1, wherein X.sup.1 is glycine; X.sup.2 is proline; X.sup.3 is leucine; and X.sup.4 is glycine.

3. A peptidylhydroxamic acid derivative according to claim 1, of the general formula:

wherein X.sup.1 is glycine;

X.sup.2 is proline;

X.sup.4 is alanine or leucine; and

wherein a hydrogen atom of the amino group of X.sup.1 may be replaced with a member selected from the group consisting of acetyl, benzoyl, benzyloxy, t-butyloxycarbonyl, benzyloxycarbonyl, p-aminobenzoyl, p-aminobenzyl, p-hydroxybenzoyl; or a pharmaceutically acceptable salt thereof.

4. A method of inhibiting collagenases which comprises administering to a patient in need thereof a collagenase inhibiting effective amount of the compound according to claim 1.

5. A method of inhibiting collagenases which comprises administering to a patient in need thereof a collagenase inhibiting effective amount of the compound according to claim 3.

6. The peptidylhydroxamic acid derivative according to claim 3, which has the formula:

p-aminobenzoyl-Gly-Pro-D-Leu-D-Ala-NHOH, or a pharmaceutically acceptable salt thereof.

7. The peptidylhydroxamic acid derivative according to claim 3, which has the formula:

p-hydroxybenzoyl-Gly-Pro-D-Leu-D-Ala-NHOH, or a pharmaceutically acceptable salt thereof.

8. The peptidylhydroxamic acid derivative according to claim 2, wherein X.sup.3 is D-Leu.

9. The peptidylhydroxamic acid derivative according to claim 3, wherien D.sup.3 is D-Leu and X.sup.4 is D-Ala.

10. The peptidylhydroxamic acid derivative according to claim 3, wherein X.sup.3 is D-Leu and X.sup.4 is D-Leu.

Summary for Patent: ⤷  Free Forever Trial

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan62-317364Dec 17, 1987
PCT Information
PCT FiledDecember 16, 1988PCT Application Number:PCT/JP88/01281
PCT Publication Date:June 29, 1989PCT Publication Number:WO89/05819

Details for Patent 5,100,874

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Smith And Nephew SANTYL collagenase OINTMENT;TOPICAL 101995 001 1965-06-04 ⤷  Free Forever Trial Fuji Yakuhin Kogyo Kabushiki Kaisha (Toyama, JP) 2009-03-31 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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