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Specific chromogenic enzyme substrates

Assignee: Chromogenix AB
•
Filing: 1977-11-16
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Granted: 1980-06-10
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Expires: 1997-11-16
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Abstract

Abstract Chromogenic or fluorogenic enzyme substrates for serine proteases containing the amino acid sequence Ile-A-Gly-Arg wherein A is Asp or Glu substituted in the carboxylic group by esterification or amidation, a method of preparation thereof, and use thereof.

Inventors

  • 👤 Karl G. Claeson
  • 👤 Leif E. Aurell
  • 👤 Leif R. Simonsson

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 03:44
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/10; C07K5/1002; C07K5/1005; C07K5/101; C12; C12Q; C12Q1/00; C12Q1/56; C12Q2337/00; C12Q2337/10; C12Q2337/12; Y; Y10; Y10S; Y10S530/00; Y10S530/802; Y10S930/00; Y10S930/01; Y10S930/28

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 98 words
Chromogenic or fluorogenic enzyme substrates for serine proteases containing the amino acid sequence -Ile-A-Gly-Arg- wherein A is Asp or Glu substituted in the carboxylic group by esterification or amidation wherein the esters contain a short chain alkyl or hydroxy alkyl or alkyl-substituted aminoalkyl or cycloalkyl group containing a total of 2-6 carbon atoms, and the amides contain a mono or di-substituted short chain alkyl or hydroxy alkyl or alkyl-substituted aminoalkyl group containing a total of 1-6 carbon atoms, or a heterocyclic group in which the amido nitrogen forms part of a piperidine, a morpholine or a piperazine ring.
Claim 2
Dependent Claim 98 words
Chromogenic or fluorogenic enzyme substrates for serine proteases containing the amino acid sequence -Ile-A-Gly-Arg- wherein A is Asp or Glu substituted in the carboxylic group by esterification or amidation wherein the esters contain a short chain alkyl or hydroxy alkyl or alkyl-substituted aminoalkyl or cycloalkyl group containing a total of 2-6 carbon atoms, and the amides contain a mono or di-substituted short chain alkyl or hydroxy alkyl or alkyl-substituted aminoalkyl group containing a total of 1-6 carbon atoms, or a heterocyclic group in which the amido nitrogen forms part of a piperidine, a morpholine or a piperazine ring.
Claim 3
Dependent Claim 34 words
The substrate of claim 1 represented by the formula R 1 -Ile-A-Gly-Arg-NH-R 2 wherein R 1 is acyl and R 2 is a group which gives a chromophore or fluorescent compound upon enzymatic hydrolysis.
Claim 4
Dependent Claim 10 words
The substrate of claim 2 wherein R 1 is acetyl.
Claim 5
Dependent Claim 10 words
The substrate of claim 2 wherein R 1 is benzoyl.
Claim 6
Dependent Claim 18 words
The substrate of claim 2 wherein R 2 is p-nitrophenyl or β-naphthyl or 4 methoxy-β-naphthyl or salt thereof.
Claim 7
Dependent Claim 16 words
The substrate of claim 1 wherein A is Asp or Glu substituted with a methoxy group.
Claim 8
Dependent Claim 16 words
The substrate of claim 1 wherein A is Asp or Glu substituted with an ethoxy group.
Claim 9
Dependent Claim 16 words
The substrate of claim 1 wherein A is Asp or Glu substituted with an isopropoxy group.
Claim 10
Dependent Claim 16 words
The substrate of claim 1 wherein A is Asp or Glu substituted with a cyclohexoxy group.
Claim 11
Dependent Claim 16 words
The substrate of claim 1 wherein A is Asp or Glu substituted with a dimethylaminoethoxy group.
Claim 12
Dependent Claim 18 words
The substrate of claim 1 wherein A is Asp or Glu substituted with CONHCH(CH 3 ) 2 .
Claim 13
Dependent Claim 14 words
The substrate of claim 1 wherein A is Asp or Glu substituted with ##STR6##
Claim 14
Dependent Claim 20 words
The substrate of claim 1 wherein A is Asp or Glu substituted with CON(CH 2 CH 2 OH) 2 .
Claim 15
Dependent Claim 25 words
The substrate of any of claims 6-13 represented by the formula R 1 -Ile-A-Gly-Arg-NH-R 2 wherein R 1 is benzoyl and R 2 is p-nitrophenyl.

References Cited (Backward Citations)

US4028318A Cited
US4070245A Cited
US4061625A Cited
US4137225A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-06-10 1983-12-10 1984-06-10 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-06-10 1987-12-10 1988-06-10 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-06-10 1991-12-10 1992-06-10 $7700.00 Window Closed / Lapsed

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