Back to results
US 6,660,246 B1Granted
Ligands and metal complexes thereof
AssigneeBracco International B.V.
InventorsDavid P. Nowotnik, Palaniappa Nanjappan
Life of this patent
Estimating the term…
Abstract
Novel compounds of the formula and novel complexes of these compounds with metals are useful in diagnostic and therapeutic methods.
Claims7
A compound of the following formula I:
- where
- Q is the group —(C(RR))m1—(Y1)n—(C(RR))m2—(Y2—(C(RR))m3)n1—, where Y1 and Y2 are each independently —NR—, —O—, —S—, —SO—, —SO2— or —Se—;
- n and n1 are each independently 0 or 1;
- and m1, m2 and m3 are each independently 0 or an integer from 1 to 4;
- provided that m1 and m2 are not both 0, that m1+m2+n+n1 is less than 6 and that a carbon atom bearing an R group is not directly bonded to more than one heteroatom;
- each R and R* group is independently:
- (i) R1;
- (ii) alkoxy;
- (iii) hydroxy;
- (iv) halogen;
- (v) haloalkyl;
- (vi) —OR1;
- (vii) —C(O)—OR1;
- (viii) —C(O)—N(R1)2;
- (ix) —N(R1)2—;
- (x) —N(R1)—COR1;
- (xi) -alkyl-C(O)—OR1;
- (xii) -alkyl-C(O)—N(R1)2;
- (xiii) -alkyl-N(R1);
- (xiv) -alkyl-N(R1)—COR1;
- (xv) -aryl-C(O)—OR1;
- (xvi) -aryl-C(O)—N(R1)2;
- (xvii) -aryl-N(R1)2;
- (xviii) -aryl-N(R1)—COR1;
- (xix) nitrile;
- (xx) acyl;
- (xxi) acyloxy;
- (xxii) heterocyclo;
- (xxiii) hydroxyalkyl;
- (xxiv) alkoxyalkyl;
- (xxv) hydroxyaryl;
- (xxvi) arylalkyl;
- (xxvii) —SO2—R1;
- (xxviii) -alkyl-SO2—R1;
- (xxix) —(A)p—R1, where A is a linking group which is bound to Ra via a carbon, oxygen, nitrogen or sulfur group, p is 0 or a positive integer, and Ra is a bioactive moiety or a reactive group which forms a covalent bond to a bioactive moiety;
- or
- (xxx) two of the groups, taken together with one or more atoms to which they are bonded, form a saturated or unsaturated, spiro or fused, carbocyclic or heterocyclic ring which may be unsubstituted or substituted by one or more groups selected from the groups (i) to (xxix) above;
- each R1 is independently hydrogen, alkyl, alkenyl, alkynyl or aryl;
- and
- G1 and G2 are each independently —OH or —N(R2)2, provided that at least one of G1 and G2 is —N(R2)2, where each R2 is independently hydrogen, alkyl, aryl, acyl or —(A)p—Ra, further provided;
- each alkyl is substituted or unsubstituted and has 1 to 12 carbon atoms;
- each alkoxy is substituted or unsubstituted and has 1 to 12 carbon atoms;
- each alkenyl is substituted or unsubstituted and has 2 to 10 carbon atoms;
- each alkenyl is substituted or unsubstituted and has 2 to 10 carbon atoms;
- each cycloalkyl is substituted or unsubstituted and is a 2- to 3-ring system where each ring contains 3 to 7 carbon atoms;
- each aryl is substituted or unsubstituted and is a homocyclic aromatic group which contains 1 or 2 rings where each ring contains 6 to 12 carbon atoms;
- each heterocycl is substituted 1 or 2 is where or unsaturated, aromatic or non-aromatic cyclic group containing at least one oxygen, nitrogen or sulfur atom;
- and
- each bioactive moiety is a group selected from the list consisting of a group which can function a s a metabolic substrate, catalyst or inhibitor;
- a group which can preferentially be taken up at a selected biological site;
- a group which contains reactive groups for coupling to a protein;
- or a group which can preferentially localize at a selected biological site.
49 more elements
Dependencies are inferred from the claim text.