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US4440739A Expired / Lapsed US ⏱️ 0.0 years remaining

Radioactive diagnostic agent and non-radioactive carrier therefor

Assignee: Nihon Medi Physics Co Ltd
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Filing: 1981-11-25
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Granted: 1984-04-03
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Expires: 2001-11-25
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Abstract

Abstract A 99mTc-labeled radioactive diagnostic agent being useful for visualization and dynamic inspection of hepatobiliary ducts and having a high stability and no material toxicity, which comprises 99mTc in the form of pertechnetate and a non-radioactive carrier, the non-radioactive carrier comprising an N-pyridoxyl- alpha -amino acid of the formula: <IMAGE> wherein R1 and R2 are each an atom or an atomic group present in the alpha -amino acid residue encompassed by the dotted line and R3, R4, R5 and R6 are each a hydrogen atom, a halogen atom, a C1-C10 alkyl group or a C1-C10 alkyl group substituted with at least one hydrophilic group or its salt, and a reducing agent for pertechnetate.

Inventors

  • 👤 Makoto Azuma
  • 👤 Masaaki Hazue

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 21:01
CPC Classifications
A; A61; A61K; A61K51/00; C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/63; C07D213/65; C07D213/66; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K2123/00

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 87 words
A non-radioactive carrier comprising an N-pyridoxyl-α-amino acid of the formula: ##STR5## wherein R 1 and R 2 are each an atom or an atomic group present in the α-amino acid residue encompassed by the dotted line and R 3 , R 4 , R 5 and R 6 are each a hydrogen atom, a halogen atom, a C 1 -C 10 alkyl group or a C 1 -C 10 alkyl group substituted with at least one hydrophilic group or its salt, and a reducing agent for pertechnetate.
Claim 2
Dependent Claim 87 words
A non-radioactive carrier comprising an N-pyridoxyl-α-amino acid of the formula: ##STR5## wherein R 1 and R 2 are each an atom or an atomic group present in the α-amino acid residue encompassed by the dotted line and R 3 , R 4 , R 5 and R 6 are each a hydrogen atom, a halogen atom, a C 1 -C 10 alkyl group or a C 1 -C 10 alkyl group substituted with at least one hydrophilic group or its salt, and a reducing agent for pertechnetate.
Claim 3
Dependent Claim 36 words
The non-radioactive carrier according to claim 1, wherein the N-pyridoxyl-α-amino acid is the one of the formula (I) wherein R 3 and R 5 are each hydrogen, R 4 is hydroxymethyl and R 6 is methyl.
Claim 4
Dependent Claim 39 words
The non-radioactive carrier according to claim 1, wherein the N-pyridoxyl-α-amino acid is the one of the formula (I) wherein R 2 , R 3 and R 5 are each hydrogen, R 4 is hydroxymethyl and R 6 is methyl.
Claim 5
Dependent Claim 53 words
The non-radioactive carrier according to claim 1, wherein the N-pyridoxyl-α-amino acid is the one of the formula (I) wherein R 1 is hydrogen, methyl, isopropyl, 1-methylpropyl, 2-methylpropyl, 2-carboxyethyl, hydroxymethyl, 1-hydroxyethyl, benzyl or 4-hydroxybenzyl, R 2 , R 3 and R 5 are each hydrogen, R 4 is hydroxymethyl and R 6 is methyl.
Claim 6
Dependent Claim 67 words
The non-radioactive carrier according to claim 1, wherein the N-pyridoxyl-α-amino acid is an N-pyridoxyl-tryptophan derivative of the formula: ##STR6## wherein R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are each a hydrogen atom, a halogen atom, a C 1 -C 5 alkyl group or a C 1 -C 5 alkyl group substituted with at least one hydrophilic group.
Claim 7
Dependent Claim 43 words
The non-radioactive carrier according to claim 5, wherein the N-pyridoxyl-tryptophan derivative is the one of the formula (II) wherein R 7 , R 8 , R 9 , R 11 and R 12 are each hydrogen and R 10 is hydrogen or methyl.
Claim 8
Dependent Claim 17 words
The non-radioactive carrier according to claim 1, wherein the reducing agent for pertechnetate is a stannous salt.
Claim 9
Dependent Claim 33 words
The non-radioactive carrier according to claim 1, wherein the reducing agent for pertechnetate is contained in an amount of 0.001 to 1 mol per 1 mol of the N-pyridoxyl-α-amino acid or its salt.
Claim 10
Dependent Claim 15 words
The non-radioactive carrier according to claim 1, which is in the form of aqueous solution.
Claim 11
Dependent Claim 23 words
The non-radioactive carrier according to claim 9, wherein the concentration of the N-pyridoxyl-α-amino acid or its salt is not less than 20 mmol/liter.
Claim 12
Dependent Claim 103 words
A 99m Tc-labeled radioactive diagnostic agent which comprises 99m Tc in the form of pertechnetate and the non-radioactive carrier comprising an N-pyridyl-α-amino acid of the formula: ##STR7## wherein R 1 and R 2 are each an atom or an atomic group present in the α-amino acid residue encompassed by the dotted line and R 3 , R 4 , R 5 and R 6 are each a hydrogen atom, a halogen atom, a C 1 -C 10 alkyl group or a C 1 -C 10 alkyl group substituted with at least one hydrophilic group or its salt, and a reducing agent for pertechnetate.
Claim 13
Dependent Claim 103 words
A 99m Tc-labeled radioactive diagnostic agent which comprises 99m Tc in the form of pertechnetate and the non-radioactive carrier comprising an N-pyridyl-α-amino acid of the formula: ##STR7## wherein R 1 and R 2 are each an atom or an atomic group present in the α-amino acid residue encompassed by the dotted line and R 3 , R 4 , R 5 and R 6 are each a hydrogen atom, a halogen atom, a C 1 -C 10 alkyl group or a C 1 -C 10 alkyl group substituted with at least one hydrophilic group or its salt, and a reducing agent for pertechnetate.
Claim 14
Dependent Claim 52 words
The 99m Tc-labeled radioactive diagnostic agent according to claim 11, prepared by contacting an aqueous solution containing 99m Tc, the radioactivity of which is 0.1 to 50 mCi in a volume of 0.5 to 5 ml aqueous solution at the time of administration, in the form of pertechnetate with the non-radioactive carrier.

References Cited (Backward Citations)

US3740418A Cited
US4256726A Cited
US4215045A Cited
US4298591A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-04-03 1987-10-03 1988-04-03 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-04-03 1991-10-03 1992-04-03 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-04-03 1995-10-03 1996-04-03 $7700.00 Window Closed / Lapsed

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