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US 2003/0198597 A1Published application
Novel macrocyclic activatible magnetic resonance imaging contrast agents
OwnerThomas J. Meade, Douglas A. Bakaninventors
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Abstract
The invention relates to novel magnetic resonance imaging contrast agents and methods of detecting physiological signals or substances.
Claims31
A chelate having the formula:
- 11
- wherein
- each Q is independently selected from the group consisting of nitrogen, oxygen or sulfur;
- A—B is a structure selected from the group consisting of —CR2—CR2—, —CR═CR—, —CR2—CR2—CR2—, —CR═CR—CR2— and —CR2—CR═CR—;
- X1 and X2 are independently selected from the group consisting of CR2COO−, CR2COOH, CR2(BM), CR(CR2COO−)2, CR(CR2COO−)(BM), CR(CR2COOH)2 and CR(CR2COOH)(BM), wherein BM is a blocking moiety;
- and
- each R is independently selected from the group consisting of hydrogen, alkyl, aryl, alcohol, amine, amido, nitro, ether, ester, ketone, imino, aldehyde, alkoxy, carbonyl, halogen, sulfur containing moiety, phosphorus containing moiety, targeting moiety, blocking moiety, or, together with an adjacent R group forms an alkyl or aryl group;
- wherein either:
- a) X1 or X2 comprises a BM;
- or
- b) at least one R comprises a BM.
8 more elements
A chelate having the formula:
- 12
- wherein
- each Q is independently selected from the group consisting of nitrogen, oxygen or sulfur;
- A—B is a structure selected from the group consisting of —CR2—CR2—, —CR═CR—, —CR2—CR2—CR2—, —CR═CR—CR2— and —CR2—CR═CR—;
- X3, X4, X5, X6 and X7 are independently selected from the group consisting of —(CR2)nCOO−, —(CR2)nCOOH, (CR2)n(BM), —CR(CR2COO−)2, —CR(CR2COO−) (BM), —CR(CR2COOH)2 and —CR(CR2COOH)(BM), —(CR2)n-CR((CR2)m-COOH)2, —(CR2)n-CR((CR2)m-COO−)2, —(CR2)m-CR[((CR2)m-COOH))((CR2)m-BM), —(CR2)n-C(CR2)m-COOH)3;
- and —C((CR2)n-COOH)3, wherein BM is a blocking moiety;
- each R is independently selected from the group consisting of hydrogen, alkyl, aryl, alcohol, amine, amido, nitro, ether, ester, ketone, imino, aldehyde, alkoxy, carbonyl, halogen, sulfur containing moiety, phosphorus containing moiety, blocking moiety, or, together with an adjacent R group forms an alkyl or aryl group;
- wherein optionally two of X3—X7 are joined to form —CR2—CR2—, —CR═CR—, —CR2—CR2—CR2— or —CR═CR—CR2—;
- and
- wherein either:
- a) X3, X4, X5, X6 or X7 comprises a BM;
- or
- b) at least one R comprises a BM.
10 more elements
A chelate having the formula:
- 13
- wherein
- each Q is independently selected from the group consisting of nitrogen, sulfur or oxygen;
- each Z is —(CR2)n- wherein n is at least 1 and R is a substitution group;
- at least two of X8—X10 are selected from the group consisting of hydrogen, R, blocking moiety, —(CR2)nCOO−, —(CR2)nCOOH, (CR2)n(BM), —CR(CR2COO−)2, —CR(CR2COO−)(BM), —CR(CR2COOH)2 and —CR(CR2COOH)(BM), —(CR2)n-CR((CR2)m-COOH)2, —(CR2)n-CR((CR2)m-COO−)2, —(CR2)m-CR[((CR2)m-COOH))((CR2)m-BM), —(CR2)n-C(CR2)m-COOH)3;
- and —C((CR2)n-COOH)3;
- wherein at least one R or X comprises a blocking moiety.
4 more elements
A chelate having the formula:
- 14
- wherein
- A and B are selected from the group consisting of CR2—CR2, CR═CR, CR2—CR2—CR2, CR═CR—CR2, and CR2—CR═CR;
- each Q is independently selected from the group consisting of nitrogen, sulfur or oxygen;
- each R is independently selected from the group consisting of hydrogen, alkyl, aryl, alcohol, amine, amido, nitro, ether, ester, ketone, imino, aldehyde, alkoxy, carbonyl, halogen, sulfur containing moiety, phosphorus containing moiety, blocking moiety, or, together with an adjacent R group forms an alkyl or aryl group, or together with an non adjacent R group forms an alkyl or aryl group;
- wherein X11—X16 are selected from the group consisting of hydrogen, R, blocking moiety, —(CR2)nCOO−, —(CR2)nCOOH, (CR2)n(BM), —CR(CR2COO−)2, —CR(CR2COO−)(BM), —CR(CR2COOH)2 and —CR(CR2COOH)(BM), —(CR2)n-CR((CR2)m-COOH)2, —(CR2)n-CR((CR2)m-COO−)2, —(CR2)m-CR[((CR2)m-COOH))((CR2)m-BM), —(CR2)n-C(CR2)m-COOH)3;
- and —C((CR2)n-COOH)3;
- wherein optionally two of X1—X7 are joined to form a C1-5 alkyl group;
- wherein either:
- a) X11, X12, X13, X14, X15 or X16 comprises a BM;
- or
- b) at least one R comprises a BM.
9 more elements
A chelate having the formula:
- 15
- wherein
- A and B are selected from the group consisting of CR2—CR2, CR═CR, CR2—CR2—CR2, CR═CR—CR2, and CR2—CR═CR;
- each Q is independently selected from the group consisting of nitrogen, sulfur or oxygen;
- each R is independently selected from the group consisting of hydrogen, alkyl, aryl, alcohol, amine, amido, nitro, ether, ester, ketone, imino, aldehyde, alkoxy, carbonyl, halogen, sulfur containing moiety, phosphorus containing moiety, blocking moiety, or, together with an adjacent R group forms an alkyl or aryl group, or together with an non adjacent R group forms an alkyl or aryl group;
- wherein each of X23 are independently selected from the group consisting of hydrogen, R, blocking moiety, —(CR2)nCOO−, —(CR2)nCOOH, (CR2)n(BM), —CR(CR2COO−)2, —CR(CR2COO−)(BM), —CR(CR2COOH)2 and —CR(CR2COOH)(BM), —(CR2)n-CR((CR2)m-COOH)2, —(CR2)n-CR((CR2)m-COO−)2, —(CR2)m-CR[((CR2)m-COOH))((CR2)m-BM), —(CR2)n-C(CR2)m-COOH)3;
- and —C((CR2)n-COOH)3;
- wherein optionally two of X17—X23 are joined to form a C1-10 alkyl group;
- wherein either:
- a) X17, X18, X19, X20, X21, X22 or X23 comprises a BM;
- or
- b) at least one R comprises a BM.
9 more elements
Dependencies are inferred from the claim text.