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US5679642A
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Peptide-chelator conjugates
Assignee: Bracco Suisse SA
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Filing: 1996-09-13
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Granted: 1997-10-21
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Expires: 2016-09-13
Abstract
Abstract Peptide-chelator conjugates are provided that when labelled with a traceable metal are useful for diagnostic imaging of sites of inflammation. The peptide component is an antagonist of the naturally occurring tetrapeptide tuftsin while the chelator component serves as a labelling site for metals, in particular radionuclide metals such as technetium-99m.
Inventors
- 👤 Anne Goodbody
- 👤 Alfred Pollak
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 07:50
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/088; A61K2123/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
145 words
A peptide-chelator conjugate useful for imaging sites of inflammation, comprising a metal chelator coupled to the N-terminus of a peptide consisting of the sequence Thr-Lys-Pro-Pro-Arg (SEQ ID NO:2). wherein the metal chelator has a general formula: ##STR5## wherein R 1 and R 2 , and together form a 5- or 6-membered heterocyclic ring which is optionally fused to a 5- or 6-membered ring wherein either ring is optionally substituted with groups selected from alkyl, alkoxy, carboxyl, halogen, hydroxyl and a linking group; R 3 is selected from H; alkyl; and alkyl substituted by a group selected from amino, aminoacyl, carboxyl, guanidinyl, hydroxyl, thiol, phenyl, phenolyl, indolyl and imidazolyl; R 4 is selected from hydroxyl, alkoxy, and a linking group; and T represents H or a sulfur protecting group; with the proviso that R 1 and R 2 do not form a pyridine or pyrrolindine ring.
Claim 2
Dependent Claim
145 words
A peptide-chelator conjugate useful for imaging sites of inflammation, comprising a metal chelator coupled to the N-terminus of a peptide consisting of the sequence Thr-Lys-Pro-Pro-Arg (SEQ ID NO:2). wherein the metal chelator has a general formula: ##STR5## wherein R 1 and R 2 , and together form a 5- or 6-membered heterocyclic ring which is optionally fused to a 5- or 6-membered ring wherein either ring is optionally substituted with groups selected from alkyl, alkoxy, carboxyl, halogen, hydroxyl and a linking group; R 3 is selected from H; alkyl; and alkyl substituted by a group selected from amino, aminoacyl, carboxyl, guanidinyl, hydroxyl, thiol, phenyl, phenolyl, indolyl and imidazolyl; R 4 is selected from hydroxyl, alkoxy, and a linking group; and T represents H or a sulfur protecting group; with the proviso that R 1 and R 2 do not form a pyridine or pyrrolindine ring.
Claim 3
Dependent Claim
20 words
A peptide-chelator conjugate according to claim 1, wherein the metal chelator and the peptide are coupled by a linking group.
Claim 4
Dependent Claim
18 words
A peptide-chelator conjugate according to claim 2, wherein the linking group is one or more amino acid residues.
Claim 5
Dependent Claim
20 words
A peptide-chelator conjugate according to claim 1, wherein the peptide is coupled to the metal chelator at R 4 .
Claim 6
Dependent Claim
24 words
A peptide-chelator conjugate according to claim 1, wherein the peptide is coupled to the metal chelator by a linking group at R 4 .
Claim 7
Dependent Claim
18 words
A peptide-chelator conjugate according to claim 5, wherein the linking group is one or more amino acid residues.
Claim 8
Dependent Claim
22 words
A peptide-chelator conjugate according to claim 5, wherein the linking group is selected from -Gly-, -Gly-Asp-Gly-(SEQ ID NO:3) and -Ser-Gly-Asp-Gly-(SEQ ID NO:6).
Claim 9
Dependent Claim
22 words
A peptide-chelator conjugate according to claim 1, in a form complexed with a diagnostically useful metal or an oxide or nitride thereof.
Claim 10
Dependent Claim
22 words
A peptide-chelator conjugate according to claim 1, in a form complexed with a diagnostically useful metal or an oxide or nitride thereof.
Claim 11
Dependent Claim
51 words
A method of imaging a site of inflammation in a mammal comprising the step of administering a diagnostically effective amount of a composition comprising the peptide-chelator conjugate as claimed in claim 1, the peptide chelator conjugate in a form complexed with a diagnostically useful metal or an oxide or nitride thereof.
References Cited (Backward Citations)
WO1980002141A1
Cited
US4390528A
Cited
US4729848A
Cited
US5175343A
Cited
US5187264A
Cited
US5082930A
Cited
US4914226A
Cited
US4965250A
Cited
US5091514A
Cited
US4965392A
Cited
US5047400A
Cited
US5021567A
Cited
US5202451A
Cited
US5202109A
Cited
US5071965A
Cited
EP0352218A2
Cited
US4957736A
Cited
US4986979A
Cited
US5196515A
Cited
US5248764A
Cited
US5028593A
Cited
WO1991003200A1
Cited
US5043423A
Cited
US5175257A
Cited
EP0454302A2
Cited
US5112595A
Cited
WO1992013572A1
Cited
US5112594A
Cited
WO1992019235A2
Cited
WO1992019274A1
Cited
WO1993010823A1
Cited
US5220000A
Cited
WO1993015770A1
Cited
WO1993017719A1
Cited
WO1993021962A1
Cited
EP0569132A1
Cited
WO1993021957A1
Cited
WO1993025244A1
Cited
US5433816A
Cited
WO1995013832A1
Cited
US5480970A
Cited
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 2000-10-20 | 2001-04-21 | 2001-10-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2004-10-20 | 2005-04-21 | 2005-10-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2008-10-20 | 2009-04-21 | 2009-10-21 | $7700.00 | Window Closed / Lapsed |