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US 8,044,081 B2Granted
Aminoderivative of biotin and their conjugates with macrocyclic chelating agents
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsGiovanni Paganelli, Marco Chinol, Mauro Ginanneschi
Life of this patent
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Abstract
Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.
Claims6
A complex of a compound of formula (I)
- where:
- Q is a —(CH2)n— group, in which n is an integer from 4 to 12, in which case R′ does not exist, or Q is selected from the group consisting of —(CH2)a—CH(R′)—(CH2)b— where a and b are independently 0 or h, wherein h is an integer from 4 to 12, R′ is as defined here below, or Q is cyclohexyl, phenyl, in which case R′ is a substituent on the cyclohexyl or phenyl ring;
- R is hydrogen or -Λ, where -Λ is a formula (II) macrocycle
- where the various Ys, which may be the same or different, are selected from the group consisting of hydrogen, a C2 alkyl group, straight or branched C3-C4 alkyl, —(CH2)m—COOH, where m is an integer from 1 to 3;
- X is hydrogen or the —CH2—U group, where U is selected from methyl, ethyl, p-aminophenyl, or X is the —(CHW)o—Z group, where o is an integer from 1 to 5, W is hydrogen, methyl or ethyl, Z is a heterocyclic group with 5 or 6 members containing one or more heteroatoms selected from O, N—R1, R1 being a hydrogen, C1-C2 alkyl group, or a straight or branched C3-C4 alkyl group, and S;
- or Z is selected from —NH2, —NH—C(═NH)—NH2, or —S—R2 where R2 is a C1 or C2 alkyl group or a straight or branched C1-C4 alkyl group;
- p is the integer 2 or 3;
- R′ is selected from the group consisting of hydrogen, a C1-C2 alkyl group, a straight or branched C3-C4 alkyl, —(CH2)q-T, where T is selected from the group consisting of S—CH3, —OH, or —COOH, and q is the integer 1 or 2;
- R″ has the same meaning as R, with the following conditions:
- if R is -Λ, R″ is hydrogen;
- if R is hydrogen R″ is -Λ, or R and R″ are (CH2)r-Λ(for R), where r is an integer from 4 to 12, and -Λ (for R″) respectively, Q being a —(CH2)n— group where n is an integer from 4 to 12
- with a radioisotope.
9 more elements
Dependencies are inferred from the claim text.