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US3884896A Expired / Lapsed US ⏱️ 0.0 years remaining

New substrates for diagnostic use, with high susceptibility to thrombin and other proteolytic

Assignee: Saab Bofors AB
•
Filing: 1973-04-24
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Granted: 1975-05-20
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Expires: 1993-04-24
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Abstract

Abstract A substrate suitable for diagnostic use, with high susceptibility to proteolytic enzymes of the type peptide peptidohydrolases, such as thrombin, plasmin, trypsin, which substrate is represented by the formula: OR SALTS THEREOF, WHERE R1 is hydrogen, an alkyl-carbonyl having 1-12 carbon atoms, a omega -aminoalkyl-carbonyl having 1-12 carbon atoms in a straight chain, cyclohexyl-carbonyl a omega cyclohexylalkyl-carbonyl having 1-6 carbon atoms in a straight chain, 4-amino ethyl-cyclohexyl-carbonyl, benzoyl, benzoyl substituted with one or more substituents selected from halogen atoms, methyl, amino and phenyl groups, a omega -phenyl-alkylcarbonyl having 1-6 carbon atoms in a straight chain, benzenesulphonyl, 4-toluenesulphonyl or N -benzoyl-phenylalanyl; R2 is phenyl, benzyl, 4-hydroxybenzyl, 4-methoxybenzyl or 4methylbenzyl; R3 is a straight, branched or cyclic alkyl having 3-8 carbon atoms, phenyl, or benzyl; n is 3 or 4; R4 is hydrogen or guanyl; and R5 is phenyl, nitrophenyl, methylnitrophenyl, dinitrophenyl, naphthyl, nitronaphthyl, quinolyl or nitroquinolyl.

Inventors

  • 👤 Gustaf Erik Birger Blomback
  • 👤 Margareta Blomback
  • 👤 Karl Goran Claeson
  • 👤 Lars-Gundro Svendsen

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-30 03:57
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06034; C07C; C07C271/00; C07C271/06; C07C271/08; C07C271/10; C07C271/22; C07K5/06043; C07K5/06052; C07K5/08; C07K5/0802; C07K5/0812; C07K5/10; C07K5/1002; C07K5/1016; C12; C12Q; C12Q1/00; C12Q1/34; C12Q1/37; C12Q1/56; C12Q2337/00; C12Q2337/10; C12Q2337/12; G; G01; G01N; G01N2333/00; G01N2333/90; G01N2333/914; G01N2333/948; G01N2333/968; G01N2333/974; G01N2333/976; Y; Y10; Y10S; Y10S530/00; Y10S530/802; Y10S930/00; Y10S930/01; Y10S930/13

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 19 words
SUBSTRATE WITH HIGH SUSCEPTIBILITY TO PROTEOLYTIC ENZYMES OF THE TYPE PEPTIDE PEPTIDOHYDROLASES, WHICH SUBSTRATE IS REPRESENTED BY THE FORMULA:
Claim 2
Dependent Claim 19 words
SUBSTRATE WITH HIGH SUSCEPTIBILITY TO PROTEOLYTIC ENZYMES OF THE TYPE PEPTIDE PEPTIDOHYDROLASES, WHICH SUBSTRATE IS REPRESENTED BY THE FORMULA:
Claim 3
Dependent Claim 27 words
The substrate of claim 1 wherein R1 is selected from the group consisting of hydrogen, acetyl, n-octanoyl, 4-aminobutyryl, 6-aminohexanoyl, cyclohexyl-carbonyl, 2-cyclohexylacetyl, 4-aminoethyl-cyclohexyl-carbonyl, benzoyl, p-methylbenzoyl, p-aminobenzoyl, 3-phenylpropionyl, 4-toluenesulphonyl.
Claim 4
Dependent Claim 9 words
The substrate of claim 1 wherein R1 is benzoyl.
Claim 5
Dependent Claim 9 words
The substrate of claim 1 wherein R1 is hydrogen.
Claim 6
Dependent Claim 9 words
The substrate of claim 1 wherein R2 is benzyl.
Claim 7
Dependent Claim 9 words
The substrate of claim 1 wherein R2 is phenyl.
Claim 8
Dependent Claim 13 words
The substrate of claim 1 wherein n is 3 and R4 is quanyl.
Claim 9
Dependent Claim 13 words
The substrate of claim 1 wherein n is 4 and R4 is hydrogen.
Claim 10
Dependent Claim 9 words
The substrate of claim 1 wherein R5 is p-nitrophenyl.
Claim 11
Dependent Claim 9 words
The substrate of claim 1 wherein R5 is naphthyl.
Claim 12
Dependent Claim 9 words
The substrate of claim 1 wherein R5 is 4-nitronaphthyl
Claim 13
Dependent Claim 9 words
The substrate of claim 1 wherein R2 is hydroxybenzyl.
Claim 14
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoyl-phenylalanyl-valyl-arginine-p-nitroanilide or the HCl salt thereof.
Claim 15
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoyl-phenylalanyl-leucyl-arginine-p-nitroanilide or the HCl salt thereof.
Claim 16
Dependent Claim 15 words
The substrate of claim 1 in which is N -benzoyl-phenylalanyl-isoleucyl-arginine-p-nitroanilide or the HCl salt thereof.
Claim 17
Dependent Claim 13 words
The substrate of claim 1 which is phenylalanylphenylalanyl-arginine-p-nitroanilide or the HCl salt thereof.
Claim 18
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoyl-D-phenylalanyl-valyl-arginine-p-nitroanilide or the HCl salt thereof.
Claim 19
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoyl-D,L-phenylglycinyl-valyl-arginine-p-nitroanilide or the HCl salt thereof.
Claim 20
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoylphenylalanyl-valyl-arginine-2-naphthylamide or the HCl salt thereof.
Claim 21
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoyl-phenylalanyl-valyl-arginine-4-nitro-1-naphthylamide or the HCl salt thereof.
Claim 22
Dependent Claim 14 words
The substrate of claim 1 which is N -benzoylphenylalanyl-valyl-lysyl-p-nitroanilide or the HCl salt thereof.

References Cited (Backward Citations)

No citation records indexed.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1978-05-19 1978-11-18 1979-05-20 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1982-05-19 1982-11-18 1983-05-20 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1986-05-19 1986-11-18 1987-05-20 $7700.00 Window Closed / Lapsed

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