US4518528A
Expired / Lapsed
US
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α Amino fluoro ketones
Assignee: Prototek Inc
•
Filing: 1984-02-06
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Granted: 1985-05-21
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Expires: 2004-02-06
Abstract
Abstract Novel alpha amino fluoro ketones, a method of their synthesis and a method for irreversibly inhibiting proteases is disclosed.
Inventors
- 👤 David W. Rasnick
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:59
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/06; C07K5/00; C07K5/02; C07K5/04; C07K5/06; C07K5/06191; C07K5/08; C07K5/0827; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
74 words
A composition of matter, comprising an αamino fluoro ketone compound of the structural formulae: ##STR6## wherein R 1 and R 2 are independently selected from the group of hydrogen; alkyl of 1-6 carbons; substituted alkyl of 1-6 carbons; aryl; alkylaryl where the alkyl group is of 1-4 carbons; n is an integer from 1-4 inclusive; X is a peptide end-blocking group; and Y is an amino acid or peptide chain of 1-6 amino acids.
Claim 2
Dependent Claim
74 words
A composition of matter, comprising an αamino fluoro ketone compound of the structural formulae: ##STR6## wherein R 1 and R 2 are independently selected from the group of hydrogen; alkyl of 1-6 carbons; substituted alkyl of 1-6 carbons; aryl; alkylaryl where the alkyl group is of 1-4 carbons; n is an integer from 1-4 inclusive; X is a peptide end-blocking group; and Y is an amino acid or peptide chain of 1-6 amino acids.
Claim 3
Dependent Claim
26 words
The composition of matter according to claim 1, wherein substituted alkyl is a hydroxy, amino, quanidino, carboxy, or mercapto substituent on an alkyl having 1-6 carbons.
Claim 4
Dependent Claim
23 words
The composition of matter according to claim 1, wherein X is acetyl, benzoyl, carbobenzoxy, glutaryl, t-butoxycarbonyl, succinyl, methoxysuccinyl, D-Pro, D-Val, D-Leu, or D-Phe.
Claim 5
Dependent Claim
16 words
The composition of matter according to claim 1, wherein X is benzoyl, t-butoxycarbonyl, methoxysuccinyl, or carbobenzoxy.
Claim 6
Dependent Claim
13 words
The composition of matter according to claim 1 wherein R 2 is H.
Claim 7
Dependent Claim
22 words
The composition of matter according to claim 1 wherein Y is an amino acid or peptide chain of from 1-4 amino acids.
Claim 8
Dependent Claim
15 words
The composition of matter according to claim 1, wherein said compound is Bz-AlaCH 2 F.
Claim 9
Dependent Claim
15 words
The composition of matter according to claim 1, wherein said compound is Z-Phe-AlaCH 2 F.
Claim 10
Dependent Claim
15 words
The composition of matter according to claim 1, wherein said compound is Boc-ProCHFCO 2 Et.
Claim 11
Dependent Claim
15 words
The composition of matter according to claim 1, wherein said compound is Boc-AlaCHFCO 2 -t-butyl.
Claim 12
Dependent Claim
15 words
The composition of matter according to claim 1, wherein said compound is MeOSuc-Ala-Ala-ProAlaCH 2 F.
Claim 13
Dependent Claim
15 words
The composition of matter according to claim 1, wherein said compound is MeOSuc-Phe-Ala-PhePhe-Val-LeuCH 2 F.
References Cited (Backward Citations)
US4153688A
Cited
US4438270A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-05-20 | 1988-11-19 | 1989-05-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-05-20 | 1992-11-19 | 1993-05-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-05-20 | 1996-11-19 | 1997-05-21 | $7700.00 | Window Closed / Lapsed |