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US 8,940,273 B2Granted
Tricarbonyl complexes with tridentate chelators for myocardium imaging
AssigneeMallinckrodt Inc.
InventorsIsabel Rego Santos, Antonio Manuel Rocha Paulo
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Abstract
Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
Claims21
A compound comprising Formula (I), (II), or (III):
- wherein,
- n is an integer selected from 1 or 2, and
- at least one of R1, R2, R3, and R4 is a linear group of the type —Rx—O—RY or a macrocyclic ether group,
- and each of the other three R groups is independently hydrogen;
- a linear or branched, saturated or unsaturated C1 to C9 alkyl;
- a saturated or unsaturated carbocyclic group;
- a saturated or unsaturated heterocyclic or heteroaliphatic group with one or more atoms selected from O, N and S, wherein said carbocyclics, heterocyclics and heteroaliphatics are optionally substituted by one or more linear or branched, saturated or unsaturated C1 to C9 alkyls;
- an ether group —Rx—O—RY or [(CH2)xO]y(CH2)z (x=2-3, y=3-8, z=2-5),
- wherein Rx and RY are independently linear or branched, saturated or unsaturated C1 to C9 alkyl, or saturated or unsaturated carbocyclics, any of which alkyl and/or carbocyclic groups may be substituted or unsubstituted, and
- provided that when the tridentate chelator is of the type of formula (I), when R1 is —Rx—O—RY wherein RY is substituted, and R2, R3, and R4 are each hydrogen, RY is not substituted apically by a further tris(pyrazolyl)methane moiety;
- and
- when R1 is —Rx—O—RY and R2, R3, and R4 are each hydrogen, R1 cannot be —CH2—O—CH2—(p-tBu-C6H4).
9 more elements
A compound comprising Formula (I):
- wherein,
- at least one of R1, R2, R3, and R4 is a linear or macrocyclic ether group of the type —Rx—O—RY or [(CH2)xO]y (CH2)z (x=2-3, y=3-8, z=2-5), respectively,
- and each of the other three R groups is independently hydrogen;
- a linear or branched, saturated or unsaturated C1 to C9 alkyl;
- a saturated or unsaturated carbocyclic group;
- a saturated or unsaturated heterocyclic or heteroaliphatic group with one or more atoms selected from O, N and S, wherein said carbocyclics, heterocyclics and heteroaliphatics are optionally substituted by one or more linear or branched, saturated or unsaturated C1 to C9 alkyls;
- an ether group —Rx—O—RY or [(CH2)xO]y(CH2)z (x=2-3, y=3-8, z=2-5),
- wherein Rx and RY are independently linear or branched, saturated or unsaturated C1 to C9 alkyl, or saturated or unsaturated carbocyclics, any of which alkyl and/or carbocyclic groups may be substituted or unsubstituted,
- provided that when R1 is —Rx—O—RY wherein RY is substituted, and R2, R3, and R4 are each H, RY is not substituted apically by a further tris(pyrazolyl)methane moiety;
- and when R1 is —Rx—O—RY and R2, R3, and R4 are each H, R1 cannot be —CH2—O—CH2—(p-tBu-C6H4).
7 more elements
A compound comprising Formula (II):
- wherein,
- n is an integer selected from 1 or 2, and
- at least one of R1, R2, R3, and R4 is a linear or macrocyclic ether group of the type —Rx—O—RY or [(CH2)xO]y(CH2)z (x=2-3, y=3-8, z=2-5), respectively,
- and each of the other three R groups is independently hydrogen;
- a linear or branched, saturated or unsaturated C1 to C9 alkyl;
- a saturated or unsaturated carbocyclic group;
- a saturated or unsaturated heterocyclic or heteroaliphatic group with one or more atoms selected from O, N and S, wherein said carbocyclics, heterocyclics and heteroaliphatics are optionally substituted by one or more linear or branched, saturated or unsaturated C1 to C9 alkyls;
- an ether group —Rx—O—RY or [(CH2)xO]y(CH2)z (x=2-3, y=3-8, z=2-5),
- wherein Rx and RY are independently linear or branched, saturated or unsaturated C1 to C9 alkyl, or saturated or unsaturated carbocyclics, any of which alkyl and/or carbocyclic groups may be substituted or unsubstituted.
6 more elements
A compound comprising Formula (III):
- wherein,
- n is an integer selected from 1 or 2, and
- at least one of R1, R2, R3, and R4 is a linear or macrocyclic ether group of the type —Rx—O—RY or [(CH2)xO]y(CH2)z (x=2-3, y=3-8, z=2-5), respectively,
- and each of the other three R groups is independently hydrogen;
- a linear or branched, saturated or unsaturated C1 to C9 alkyl;
- a saturated or unsaturated carbocyclic group;
- a saturated or unsaturated heterocyclic or heteroaliphatic group with one or more atoms selected from O, N and S, wherein said carbocyclics, heterocyclics and heteroaliphatics are optionally substituted by one or more linear or branched, saturated or unsaturated C1 to C9 alkyls;
- an ether group —Rx—O—RY or [(CH2)xO]y(CH2)z (x=2-3, y=3-8, z=2-5),
- wherein Rx and RY are independently linear or branched, saturated or unsaturated C1 to C9 alkyl, or saturated or unsaturated carbocyclics, any of which alkyl and/or carbocyclic groups may be substituted or unsubstituted.
6 more elements
Dependencies are inferred from the claim text.