IP Library Granted Patent US 7,390,828
Granted Patent B2
US 7,390,828 · App. 10/468,075 · Granted Jun 24, 2008

Aminoderivatives of biotin and their conjugates with macrocyclic chelating agents

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Quick Facts
Patent No.
US 7,390,828
App. No.
10/468,075
Granted
Jun 24, 2008
Kind
B2
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

Claims (11)

1. A compound of Formula (I):

where:

Q is a —(CH 2 ) n — group, where n is an integer from 4 to 12, in which case R′ does not exist, or Q is selected from the group consisting of —(CH 2 ) a —CH(R′)—(CH 2 ) 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 C 2 alkyl group, straight or branched C 3 -C 4 alkyl, —(CH 2 ) m —COOH, where m is an integer from 1 to 3;

X is hydrogen, or the —CH 2 —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—R 1 , R 1 being a hydrogen, C 1 -C 2 alkyl group, or a straight or branched C 3 -C 4 alkyl group, and S; or Z is selected from —NH 2 , —NH—C(=NH)—NH 2 , or —S—R 2 where R 2 is a C 1 or C 2 alkyl group or a straight or branched C 3 -C 4 alkyl group;

p is the integer 2 or 3

R′ is selected from the group consisting of hydrogen, a C 1 -C 2 alkyl group, a straight or branched C 3 -C 4 alkyl, —(CH 2 ) q —T, where T is selected from the group consisting of S—CH 3 , —OH, or —COOH, and q is the integer 1 or 2;

R″ has the same meanings 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 (CH 2 ) r -Λ (for R), where r is an integer from 4 to 12, and -Λ (for R″), respectively, Q being a —(CH 2 ) n — group where n is an integer from 4 to 12.

2. A composition containing a compound according to claim 1 , in a mixture with a suitable vehicle and/or excipient.

Assignments (2)
CHANGE OF ADDRESS Recorded Oct 15, 2019
From: ALFASIGMA S.P.A.
To: ALFASIGMA S.P.A.
Reel/Frame 050727/0652 →
MERGER Recorded Nov 14, 2017
From: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
To: ALFASIGMA S.P.A.
Reel/Frame 044760/0906 →