US5480970A
Expired / Lapsed
US
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Metal chelators
Assignee: Bracco Suisse SA
•
Filing: 1993-12-22
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Granted: 1996-01-02
•
Expires: 2013-12-22
Abstract
Abstract Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.
Inventors
- 👤 Alfred Pollak
- 👤 Anne Goodbody
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 03:47
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0821; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/088
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
121 words
A compound of the general formula: ##STR2## wherein R 1 and R 2 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 a conjugating group or with a conjugating group having a targetting molecule coupled thereto; 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; any amino acid residue; and a targetting molecule; and T is H or a sulfur protecting group; with the proviso that R 1 and R 2 do not form a pyridine or pyrrolidine ring.
Claim 2
Dependent Claim
121 words
A compound of the general formula: ##STR2## wherein R 1 and R 2 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 a conjugating group or with a conjugating group having a targetting molecule coupled thereto; 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; any amino acid residue; and a targetting molecule; and T is H or a sulfur protecting group; with the proviso that R 1 and R 2 do not form a pyridine or pyrrolidine ring.
Claim 3
Dependent Claim
22 words
A compound according to claim 1, wherein the ring formed by R 1 and R 2 is a six membered heterocyclic ring.
Claim 4
Dependent Claim
19 words
A compound according to claim 1, wherein R 1 and R 2 together form a 6-carboxy substituted pyridine ring.
Claim 5
Dependent Claim
19 words
A compound according to claim 1, wherein R 1 and R 2 together form a 4-hydroxy-6-carboxy substituted pyridine ring.
Claim 6
Dependent Claim
11 words
A compound according to claim 1 wherein R 3 is H.
Claim 7
Dependent Claim
19 words
A compound according to claim 1, wherein R 3 is the side chain of a serine amino acid residue.
Claim 8
Dependent Claim
42 words
A compound according to claim 1, wherein R 1 and R 2 together form a ring selected from a 6-carboxypyridine ring and a 6-carboxy-4-hydroxypyridine ring; R 3 is a serine amino acid side chain; T is Acm; and R 4 is -Gly-OH.
Claim 9
Dependent Claim
16 words
A compound according to claim 1, wherein R 4 is selected from -Gly-OH and -Gly-targetting molecule.
Claim 10
Dependent Claim
13 words
A compound according to claim 8, wherein the targetting molecule is a peptide.
Claim 11
Dependent Claim
24 words
A compound according to claim 9, wherein the peptide has a sequence selected from: -NH-Lys-Pro-Pro-Arg-OH (SEQ. ID NO: 3) -NH-Thr-Lys-Pro-Pro-Arg-OH (SEQ. ID NO: 2)
Claim 12
Dependent Claim
35 words
A compound according to claim 9, wherein the Gly forms an amide linkage with an ε-amino Lys residue of the peptide selected from: -ε-amino Lys(-Gly-OH)-Tyr-Nleu-Phe-Leu-Nleu-formyl (SEQ. ID NO: 14) -ε-amino Lys(-Asp-Gly-OH)-Lys-Tyr-Nleu-Phe-Leu-Nleu-formyl (SEQ. ID NO: 15).
Claim 13
Dependent Claim
33 words
A compound of the general formula: ##STR3## wherein R 1 and R 2 together form a pyridine ring; R 3 is H; T is Acm; and R 4 is -Gly-ε-amino Lys (-Gly-OH) -Tyr-Nleu-Phe-Leu-Nleu-formyl.
Claim 14
Dependent Claim
33 words
A compound of the general formula: ##STR3## wherein R 1 and R 2 together form a pyridine ring; R 3 is H; T is Acm; and R 4 is -Gly-ε-amino Lys (-Gly-OH) -Tyr-Nleu-Phe-Leu-Nleu-formyl.
Claim 15
Dependent Claim
42 words
A compound of the general formula: ##STR4## wherein R 1 and R 2 together form a pyridine ring; R 3 is a serine amino acid side chain; T is Acm; and R 4 is selected from: -Gly-Lys-Pro-Pro-Arg-OH -Gly-Thr-Lys-Pro-Pro-Arg-OH -Gly-ε-amino Lys(-Gly-OH)-Tyr-Nleu-Phe-Leu-Nleu-formyl -Gly-ε-amino Lys(-Asp-Gly-OH)-Lys-Tyr-Nleu-Phe-Leu-Nleuformyl-formyl.
Claim 16
Dependent Claim
42 words
A compound of the general formula: ##STR4## wherein R 1 and R 2 together form a pyridine ring; R 3 is a serine amino acid side chain; T is Acm; and R 4 is selected from: -Gly-Lys-Pro-Pro-Arg-OH -Gly-Thr-Lys-Pro-Pro-Arg-OH -Gly-ε-amino Lys(-Gly-OH)-Tyr-Nleu-Phe-Leu-Nleu-formyl -Gly-ε-amino Lys(-Asp-Gly-OH)-Lys-Tyr-Nleu-Phe-Leu-Nleuformyl-formyl.
Claim 17
Dependent Claim
130 words
A compound of the general formula: ##STR5## wherein: R 1 and R 2 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 a conjugating group or with a conjugating group having a targetting molecule coupled thereto or a hydroxyl group; R 3 is selected from H; alkyl; and alkyl substituted by a group selected from amino, emlnoacyl, carboxyl, guanidinyl, hydroxyl, thiol, phenyl, phenolyl, indolyl end imidazolyl; R 4 selected from hydroxyl; alkoxy; any areinc acid residue; and a targetting molecule; and T is H or a sulfur protecting group; wherein the targetting molecule is a peptide having a sequence: formyl-Nleu-Leu-Phe-Nleu-Tyr-Lys-Lys-Asp-X-OH (SEQ. ID NO: 1) and X is a bond or any amino acid residue.
Claim 18
Dependent Claim
130 words
A compound of the general formula: ##STR5## wherein: R 1 and R 2 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 a conjugating group or with a conjugating group having a targetting molecule coupled thereto or a hydroxyl group; R 3 is selected from H; alkyl; and alkyl substituted by a group selected from amino, emlnoacyl, carboxyl, guanidinyl, hydroxyl, thiol, phenyl, phenolyl, indolyl end imidazolyl; R 4 selected from hydroxyl; alkoxy; any areinc acid residue; and a targetting molecule; and T is H or a sulfur protecting group; wherein the targetting molecule is a peptide having a sequence: formyl-Nleu-Leu-Phe-Nleu-Tyr-Lys-Lys-Asp-X-OH (SEQ. ID NO: 1) and X is a bond or any amino acid residue.
Claim 19
Dependent Claim
10 words
A compound according to claim 14, wherein X is -Gly-.
Claim 20
Dependent Claim
13 words
A compound having the formula: ##STR6## wherein X is a bond or -Gly-.
Claim 21
Dependent Claim
13 words
A compound having the formula: ##STR6## wherein X is a bond or -Gly-.
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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) | 1999-01-01 | 1999-07-03 | 2000-01-02 | $2000.00 | Window Closed / Lapsed |
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| 11.5 Years (Year 12) | 2007-01-01 | 2007-07-03 | 2008-01-02 | $7700.00 | Window Closed / Lapsed |