Back to results
US 5,627,286 AGranted
Heteroatom-bearing ligands and metal complexes thereof
AssigneeBracco International B.V.
InventorsKondareddiar Ramalingam, Natarajan Raju
Life of this patent
Estimating the term…
Abstract
Novel compounds containing a heteroatom-bearing bridge and novel complexes of these compounds with metals. The novel compounds and complexes are useful in diagnostic and therapeutic methods.
Claims12
A compound of the following formula Ia, Ib or Ic:
- ##STR63## where Q is the group --(C(RR)).sub.m1 --Y.sup.1 --(C(RR)).sub.m2 --(Y.sup.2 --(C(RR)).sub.m3).sub.n --, where Y.sup.1 is --O--, --S--, --SO--, --SO.sub.2 --, or --Se-- and Y.sup.2 is independently --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --Se--;
- n is an integer selected from 0 or 1;
- and m1, m2 and m3 are integers independently selected from 0 to 4, provided that the sum of ml and m2 is greater than zero;
- with the proviso that if the compound is of the formula Ic, Y.sup.1 is --SO.sub.2 --, and n=0, then either m1=0 or m2=0;
- all R and R* groups are independently:
- (i) R.sup.2 ;
- (ii) halogen;
- (iii) --OR.sup.2 ;
- (iv) --C(O)--OR.sup.2 ;
- (v) --C(O)--N(R.sup.2).sub.2 ;
- (vi) --N(R.sup.2).sub.2 ;
- (vii) -alkyl--C(O)--OR.sup.2 ;
- (viii) -alkyl--C(O)--N(R.sup.2).sub.2 ;
- (ix) -alkyl-N(R.sup.2).sub.2 ;
- (x) -aryl-C(O)--OR.sup.2 ;
- (xi) -aryl-C(O)--N(R.sup.2).sub.2 ;
- (xii) -aryl-N(R.sup.2).sub.2 ;
- (xiii) acyl;
- (xiv) acyloxy;
- (xv) heterocyclo;
- (xvi) hydmxyalkyl;
- (xvii) --SO.sub.2 --R.sup.2 ;
- (xviii) -alkyl-SO.sub.2 --R.sup.2 ;
- (xix) -(A)p-R.sup.3, where A is a linking group, p is 0 or a positive integer, and R.sup.3 is a bioactivc moiety;
- or
- (xx) two R groups, or an R group and an R* group, taken together with the 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 (xix) above;
- with the proviso that a carbon atom bearing an R group is not directly bonded to more than one heteroatom;
- R.sup.1 is hydrogen, a thiol protecting group, or the group --(A)p-R.sup.3 defined above;
- and
- R.sup.2 is independently hydrogen, alkyl, alkenyl, allkynyl, or aryl.
27 more elements
A compound of the following formula Ia':
- ##STR64## where Z.sup.1 and Z.sup.2 are R* groups and Z.sup.3 is an R group, where one, two or all three of Z.sup.1, Z.sup.2 and Z.sup.3 are -(A)p-R.sup.3 groups.
A compound which is:
- (R)-3,3,9,9-tetramethyl-6-[(2-nitro-1H-imidazol-1-yl)methyl]-5-oxa-4,8-diaz aundecane-2,10-dione dioxime;
- or
- (S)-3,3,9,9-tetramethyl-6-[(2-nitro-1H-imidazol-1-yl)methyl]-5-oxa-4,8-diaz aundecane-2,10-dione dioxime.
A compound having the following formula Ia, Ib or Ic:
- ##STR65## where Q is the group --(C(RR)).sub.m1 --Y.sup.1 (C(RR)).sub.m2 --(Y.sup.2 --(C(RR)).sub.m3).sub.m-, where Y.sup.1 is --O--, and Y.sup.2 is independently --NR--, --O--, --S--, --SO--, --S.sub.2 -- or --Se--;
- n is an integer selected from 0 or 1;
- and m1, m2 and m3 are integers independently selected from 0 to 4, provided that the sum of m1 and m2 is greater than zero;
- all R and R* groups are independently:
- (i) R.sup.2 ;
- (ii) halogen;
- (iii) OR.sup.2 ;
- (iv) C(O)--OR.sup.2 ;
- (v) --C(O)--N(R.sup.2).sub.2 ;
- (vi) --N(R.sup.2).sub.2 ;
- (vii) -alkyl-C(O)--OR.sup.2 ;
- (viii) -alkyl-C(O)--N(R.sup.2).sub.2 ;
- (ix) -alkyl-N(R.sup.2).sub.2 ;
- (x) -aryl-C(O)--OR.sup.2 ;
- (xi) -aryl-C(O)--N(R.sup.2).sub.2 ;
- (xii) -aryl-N(R.sup.2).sub.2 ;
- (xiii) acyl;
- (xiv) acyloxy;
- (xv) heterocyclo;
- (xvi) hydroxyalkyl;
- (xvii) -SO.sub.2 --R.sup.2 ;
- (xviii) -alkyl-SO.sub.2 --R.sup.2 ;
- (xix) -(A)p-R.sup.3, where A is a linking group, p is 0 or a positive integer, and R.sup.3 is a bioactive moiety;
- or
- (xx) two R groups, taken together with the one or more atom to which they are bonded, form a saturated or unsaturated, or fused, carbocyclic or heterocyclic ring which may be unsubstituted or substituted by one or more groups selected from the groups (i) to (xix) above;
- with the proviso that a carbon atom bearing an R group is not directly bonded to more than one heteroatom;
- R.sup.1 is hydrogen;
- a thiol protecting group;
- or the group -(A)p-R.sup.3 defined above;
- and
- R.sup.2 is independently hydrogen, alkyl, alkenyl, alkynyl, or aryl.
28 more elements
Dependencies are inferred from the claim text.