US4244865A
Expired / Lapsed
US
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α hydroxy tripeptide substrates
Assignee: Abbott Laboratories
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Filing: 1979-12-03
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Granted: 1981-01-13
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Expires: 1999-12-03
Abstract
Abstract This invention relates to the synthesis and use of novel α hydroxy tripeptide substrates which are useful in the quantitative determination of proteolytic enzymes such as thrombin and trypsin. In use, the disclosed substrates are hydrolyzed by a proteolytic enzyme to yield a moiety that can be evaluated spectrophotometrically to indicate the quantity of enzyme present.
Inventors
- 👤 Akhtar Ali
- 👤 Robert G. Hiltibran
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 22:41
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06139; C07K5/06165; C12; C12Q; C12Q1/00; C12Q1/34; C12Q1/37
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
113 words
A chromogenic substrate for the quantitative determination of proteolytic enzymes which split peptide bonds on the carboxyl side of arginine and lysine of the formula: ##STR10## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl (C 1 -C 4 ) straight chain or branched and benzyl; R 2 is selected from the group consisting of paranitroanilide, nitrophenyl, methylnitrophenyl, dinitrophenyl, naphthyl and nitronaphthyl; A 1 is selected from the group of L amino acids consisting of glycine, alanine, valine, leucine, proline, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroglycine, histidine, arginine, phenylalanine, tyrosine, tryptophan, cysteine, pipercolic acid and methionine; and A 2 is either L-arginine or L-lysine.
Claim 2
Dependent Claim
113 words
A chromogenic substrate for the quantitative determination of proteolytic enzymes which split peptide bonds on the carboxyl side of arginine and lysine of the formula: ##STR10## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl (C 1 -C 4 ) straight chain or branched and benzyl; R 2 is selected from the group consisting of paranitroanilide, nitrophenyl, methylnitrophenyl, dinitrophenyl, naphthyl and nitronaphthyl; A 1 is selected from the group of L amino acids consisting of glycine, alanine, valine, leucine, proline, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroglycine, histidine, arginine, phenylalanine, tyrosine, tryptophan, cysteine, pipercolic acid and methionine; and A 2 is either L-arginine or L-lysine.
Claim 3
Dependent Claim
101 words
A chromogenic substrate for the quantitative determination of proteolytic enzymes which split peptide bonds on the carboxyl side of arginine and lysine of the formula: ##STR11## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl (C 1 -C 4 ) straight chain or branched and benzyl; R 2 is selected from the group consisting of paranitroanilide, nitrophenyl, methylnitrophenyl, dinitrophenyl, naphthyl and nitronaphthyl; A 1 is selected from the group of L-amino acids consisting of glycine, alanine, valine, leucine, proline, isoleucine, threonine, aspartic acid, asparagine, glutamic acid, phenylalanine and methionine; and A 2 is either L-arginine or L-lysine.
Claim 4
Dependent Claim
101 words
A chromogenic substrate for the quantitative determination of proteolytic enzymes which split peptide bonds on the carboxyl side of arginine and lysine of the formula: ##STR11## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl (C 1 -C 4 ) straight chain or branched and benzyl; R 2 is selected from the group consisting of paranitroanilide, nitrophenyl, methylnitrophenyl, dinitrophenyl, naphthyl and nitronaphthyl; A 1 is selected from the group of L-amino acids consisting of glycine, alanine, valine, leucine, proline, isoleucine, threonine, aspartic acid, asparagine, glutamic acid, phenylalanine and methionine; and A 2 is either L-arginine or L-lysine.
Claim 5
Dependent Claim
94 words
A chromogenic substrate for the quantitative determination of proteolytic enzymes which split peptide bonds on the carboxyl side of arginine and lysine of the formula: ##STR12## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl (C 1 -C 4 ) straight chain or branched and benzyl; R 2 is selected from the group consisting of paranitroanilide and nitrophenyl; A 1 is selected from the group of L amino acids consisting of glycine, alanine, valine, proline, isoleucine, aspartic acid, glutamic acid and phenylalanine; and A 2 is either L-arginine or L-lysine.
Claim 6
Dependent Claim
94 words
A chromogenic substrate for the quantitative determination of proteolytic enzymes which split peptide bonds on the carboxyl side of arginine and lysine of the formula: ##STR12## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl (C 1 -C 4 ) straight chain or branched and benzyl; R 2 is selected from the group consisting of paranitroanilide and nitrophenyl; A 1 is selected from the group of L amino acids consisting of glycine, alanine, valine, proline, isoleucine, aspartic acid, glutamic acid and phenylalanine; and A 2 is either L-arginine or L-lysine.
Claim 7
Dependent Claim
8 words
The chromogenic substrate according to claim 3 glycolic-L-prolyl-L-arginyl-p-nitroanilide.
Claim 8
Dependent Claim
8 words
The chromogenic substrate according to claim 3 L-α-hydroxyisocaproic-L-prolyl-L-arginyl-p-nitroanilide.
Claim 9
Dependent Claim
8 words
The chromogenic substrate according to claim 3 D-α-hydroxyisocaproic-L-prolyl-L-arginyl-p-nitroanilide.
Claim 10
Dependent Claim
8 words
The chromogenic substrate according to claim 3 L-α-hydroxy-β-phenylpropionic-L-prolyl-L-arginyl-p-nitroanilide.
Claim 11
Dependent Claim
8 words
The chromogenic substrate according to claim 3 D-α-hydroxy-β-phenylpropionic-L-prolyl-L-arginyl-p-nitroanilide.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-01-13 | 1984-07-14 | 1985-01-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-01-13 | 1988-07-14 | 1989-01-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-01-13 | 1992-07-14 | 1993-01-13 | $7700.00 | Window Closed / Lapsed |