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US4028318A Expired / Lapsed US ⏱️ 0.0 years remaining

Chromogenic enzyme substrates

Assignee: Phadia AB
•
Filing: 1975-11-14
•
Granted: 1977-06-07
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Expires: 1995-11-14
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Abstract

Abstract Chromogenic substrates for serine proteases, represented by the formula: R.sub.1 -A.sub.1 -A.sub.2 -Gly-Arg-NH-R.sub.2 or its salts, where R 1 is hydrogen or alkanoyl having from 1 to 12 carbon atoms or cyclohexylcarbonyl or benzoyl or benzoyl substituted with one or two halogen atoms, methylamine or phenyl groups or benzene sulphonyl or toluenesulphonyl, R 2 is nitrophenyl or naphthyl or nitronaphthyl or methoxynaphthyl or quinolyl or nitroquinolyl, A 1 is a single bond or one of the amino acids Gly, Ala, Val, Leu, Ileu, Pro, Met, Phe or Tyr, and A 2 is one of the amino acids Glu, Gln, Asp, or Asn.

Inventors

  • 👤 Leif Erik Aurell
  • 👤 Karl Goran Claeson

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-30 21:55
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0819; C07K5/10; C07K5/1002; C07K5/1005; C07K5/101; C12; C12Q; C12Q1/00; C12Q1/34; C12Q1/37; C12Q1/56; C12Q2337/00; C12Q2337/10; C12Q2337/12; C12Q2337/30; G; G01; G01N; G01N2333/00; G01N2333/90; G01N2333/914; G01N2333/948; G01N2333/95; G01N2333/964; G01N2333/96425; G01N2333/96427; G01N2333/9643; G01N2333/96433; G01N2333/96441; G01N2333/96444; G01N2333/968; G01N2333/974; G01N2333/976; Y; Y10; Y10S; Y10S530/00; Y10S530/802; Y10S930/00; Y10S930/01; Y10S930/28

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 132 words
New chromogenic substrates for serine proteases, specially suitable for diagnostic determination of factor Xa, which are represented by the following general formula: R.sub.1 -A.sub.1 -A.sub.2 -Gly-Arg-NH-R.sub.2 or its salts, where R 1 is selected from the group consisting of hydrogen, alkanoyl having from 1 to 12 carbon atoms, cyclohexylcarbonyl, benzoyl, benzoyl substituted with one or two halogen atoms, methylamine or phenyl groups, benzene sulphonyl and toluenesulphonyl; R 2 is selected from the group consisting of nitrophenyl, naphthyl, nitronaphthyl, methoxynaphthyl, quinolyl and nitroquinolyl; A 1 is selected from the group consisting of a single bond, and the amino acids selected from the group consisting of Gly, Ala, Val, Leu, Ileu, Pro, Met, Phe and Tyr; and A 2 is selected from the group consisting of the amino acids Glu, Gln, Asp, and Asn.
Claim 2
Dependent Claim 132 words
New chromogenic substrates for serine proteases, specially suitable for diagnostic determination of factor Xa, which are represented by the following general formula: R.sub.1 -A.sub.1 -A.sub.2 -Gly-Arg-NH-R.sub.2 or its salts, where R 1 is selected from the group consisting of hydrogen, alkanoyl having from 1 to 12 carbon atoms, cyclohexylcarbonyl, benzoyl, benzoyl substituted with one or two halogen atoms, methylamine or phenyl groups, benzene sulphonyl and toluenesulphonyl; R 2 is selected from the group consisting of nitrophenyl, naphthyl, nitronaphthyl, methoxynaphthyl, quinolyl and nitroquinolyl; A 1 is selected from the group consisting of a single bond, and the amino acids selected from the group consisting of Gly, Ala, Val, Leu, Ileu, Pro, Met, Phe and Tyr; and A 2 is selected from the group consisting of the amino acids Glu, Gln, Asp, and Asn.
Claim 3
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Ileu-Glu-Gly-Arg-p-nitroanilide.
Claim 4
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is H-Phe-Glu-Gly-Arg-p-nitroanilide.
Claim 5
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Leu-Glu-Gly-Arg-p-nitroamilide.
Claim 6
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Val-Glu-Gly-Arg-p-nitroanilide.
Claim 7
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Leu-Asp-Gly-Arg-p-nitroanilide.
Claim 8
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Ileu-Glu-Gly-Arg-2-naphthylamide.
Claim 9
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Ileu-Glu-Gly-Arg-4-methoxy-2-naphthylamide.
Claim 10
Dependent Claim 10 words
The chromogenic substrate according to claim 1, which is benzoyl-Ileu-Gln-Gly-Arg-p-Nitroanilide.

References Cited (Backward Citations)

US3896103A Cited
US3778426A Cited
US3884896A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-06-06 1980-12-06 1981-06-07 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-06-06 1984-12-06 1985-06-07 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-06-06 1988-12-06 1989-06-07 $7700.00 Window Closed / Lapsed

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