Patent US3971736A successfully refreshed from Google Patents.
US3971736A
Expired / Lapsed
US
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Cathepsin in D inhibitors
Assignee: Merck and Co Inc
•
Filing: 1975-01-21
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Granted: 1976-07-27
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Expires: 1995-01-21
Abstract
Abstract Hexa- and heptapeptides of formula W-[X-Pro-Phe-Phe-Y-Z]nH prepared by standard synthetic peptide techniques are anti-inflammatory, anti-rheumatoid arthritic and anti-ulcer agents.
Inventors
- 👤 Arthur F. Wagner
- 👤 Frederick W. Holly
- 👤 Tsau-Yen Lin
- 👤 Tsung-Ying Shen
- 👤 Ralph F. Hirschmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 18:47
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/06; C07K9/00; C07K9/001; C07K9/005; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
69 words
A compound of the formula: W-[X-Pro-Phe-Phe-Y-Z].sub.n H or pharmaceutically acceptable acid addition salt thereof, wherein n is 1, 2 or 3; W is hydrogen; an amino acid residue in the D- or L- configuration selected from pyroglutamyl, prolyl, valvyl, or glycyl; indole-3-acetyl; isovaleryl; dansyl; D-glucuronyl; t-butyloxycarbonyl; cholyl; or 2-deoxy-2-acetamidoglucopyranosyl; X is D-phenylalanine; Y is L-proline or L-valine; and Z is D-leucine, D-tryptophan, D-phenylalanine, D-nor-leucine, D-allo-i-leucine, D-alanine, D-proline or D-valine.
Claim 2
Dependent Claim
69 words
A compound of the formula: W-[X-Pro-Phe-Phe-Y-Z].sub.n H or pharmaceutically acceptable acid addition salt thereof, wherein n is 1, 2 or 3; W is hydrogen; an amino acid residue in the D- or L- configuration selected from pyroglutamyl, prolyl, valvyl, or glycyl; indole-3-acetyl; isovaleryl; dansyl; D-glucuronyl; t-butyloxycarbonyl; cholyl; or 2-deoxy-2-acetamidoglucopyranosyl; X is D-phenylalanine; Y is L-proline or L-valine; and Z is D-leucine, D-tryptophan, D-phenylalanine, D-nor-leucine, D-allo-i-leucine, D-alanine, D-proline or D-valine.
Claim 3
Dependent Claim
9 words
The compound of claim 1, wherein n is 1.
Claim 4
Dependent Claim
38 words
A compound of claim 1 W [X-Pro-Phe-Phe-Y-Z].sub.n H wherein n is 1, 2 or 3; W is D- or L-pyroglutamyl, or t-butyloxycarbonyl; X is D-phenylalanine; Y is L-proline or L-valine; and Z is D-leucine, D-tryptophan, D-phenylalanine or D-nor-leucine.
Claim 5
Dependent Claim
9 words
The compound of claim 3, wherein n is 1.
Claim 6
Dependent Claim
8 words
The compound of claim 3 of formula: Pyroglu-DPhe-Pro-Phe-Phe-Val-D-Trp.
Claim 7
Dependent Claim
8 words
The compound of claim 3 of formula: Pyroglu-DPhe-Pro-Phe-Phe-Val-DPhe.
Claim 8
Dependent Claim
8 words
The compound of claim 3 of formula; Pyroglu-DPhe-Pro-Phe-Phe-Val-DLeu.
Claim 9
Dependent Claim
8 words
The compound of claim 3 of formula: Boc-DPhe-Pro-Phe-Phe-Val-DTrp.
Claim 10
Dependent Claim
8 words
The compound of claim 3 of formula: Boc-DPhe-Pro-Phe-Phe-Val-DNle.
Claim 11
Dependent Claim
8 words
The compound of claim 3 of formula: Boc-DPhe-Pro-Phe-Phe-Val-DPhe.
References Cited (Backward Citations)
US3840513A
Cited
US3867364A
Cited
US3840516A
Cited
US3819486A
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US3878185A
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US3869347A
Cited
US3885012A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-07-27 | 1980-01-26 | 1980-07-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-07-27 | 1984-01-26 | 1984-07-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-07-27 | 1988-01-26 | 1988-07-27 | $7700.00 | Window Closed / Lapsed |