Water-soluble polysaccharides and diagnostic radio-labelled derivates thereof

Claim 2

A compound characterized in whole or in part by: (a) a water-soluble polysaccharide moiety having an average of at least 0.25 anionic group per monosaccharide unit, and (b) at .least one chelating group derived from the group consisting of amino acids, substituted cyclic acid anhydrides, and carbon disulfide.

Claim 3

A metal-binding compound for preparing a radiopharmaceutical for diagnosing blood clots characterized in whole or in part by: (a) a water-soluble polysaccharide moiety having an average of at least 0.25 anionic group per monosaccharide unit, and (b) at least one chelating group derived from the group consisting of amino acids, substituted cyclic acid anhydrides, and carbon disulfide.

Claim 4

A metal-binding compound for preparing a radiopharmaceutical for diagnosing blood clots characterized in whole or in part by: (a) a water-soluble polysaccharide moiety having an average of at least 0.25 anionic group per monosaccharide unit, and (b) at least one chelating group derived from the group consisting of amino acids, substituted cyclic acid anhydrides, and carbon disulfide.

Claim 5

The compound according to any preceding Claim further characterized by the feature that said polysaccharide moiety is derived from the group consisting of homopolysaccharides selected from dextran sulfates and heteropolysaccharides selected from the group consisting of chondroitin sulfates A and C, dermatan sulfate, keratan sulfates I and II, heparan sulfate, and heparin.

Claim 6

The compound according to any preceding Claim further characterized by the feature that said chelating group is derived from the group consisting of diethylenetriamine pentaacetic acid, ethylenediaminetetraacetic acid, cyclohexyldiamine tetraacetic acid, diethylenetriamine pentamethylenephosphonic acid, carbon disulfide, and substituted succinic anhydrides.

Claim 7

The compound according to any preceding Claim further characterized by the feature that said compound has the formula: wherein: a and b are numbers having a value from about 5 to 50 and b is less than or equal to a; R is the residue of heparin salt devoid its NHS0 3 - groups; n is a number having a value of 1 to 50; and K is a coordinating ligand selected from the groups consisting of: (a) (CH 2 )̵N(R 1 ) 2 in which: each R 1 is independently selected from the group consisting of (1) hydrogen, (2) (̵CH 2 )̵ p Y, in which Y is -H, -CH 3 , and p is an integer of 1 to 3, and M is hydrogen, an alkali metal ion, ammonim ion or a lower alkyl group having l,to 4 carbon atoms, with the proviso that K contains no more than 4 nitrogen atoms and no nitrogen atom in K has more than one (̵CH 2 ) p Y groups in which Y is -H or -C H 3 ; in which: p and R l are as defined in a), q is 0 or 1 to 3, and R 2 is a divalent group having 2 to 6 carbon atoms, of which one carbon atoms can be replaced by -O-, -S-, or -NH-, which atoms are necessary in order to form a ring with -CH(̵CH 2 )̵ q CH-, the ring having 5 to 8 nuclear atoms that can be saturated or unsaturated and optionally substituted by (̵CH 2 ) q Y groups in which Y is as defined in a) and q is 0 or 1 to 4; in which: t is an integer of 0 or 1, p is an integer of 1 to 3, R 3 is a group selected from -OH, -SH, (d) CH 2 O R 4 in which: r and s are independently integers of 1 to 4, and R 4 is hydrogen or lower alkyl of 1 to 4 carbon atoms; in which: r, p, and t are integers of 1 to 4, 1 R 5 is a lower alkyl group having 1 to 4 carbon atoms; in which: R 6 is alkylene or alkenylene having 1 to 4 carbon atoms, M is as defined in (a), and A is in which R 4 and Z are as defined in (d) and (e) respectively; and in which: R 7 is (̵CH 2 )̵ q Y in which q is 0 or 1 to 4 and Y and M are as defined in (a).

Claim 8

A radiopharmaceutical compound for diagnosing blood clots characterized in that it is the reaction product of: (a) the compound according to any preceding Claim, and (b) a radioactive tracer metal compound selected from lll In, 99 m T c, 5l C r, 68 Ga , and a reduced pertechnetate compound.

Claim 9

The compound according to any preceding Claim further characterized by the feature that said metal-binding compound is derived from heparin.

Claim 10

The compound according to any preceding Claim further characterized by the feature that said metal-binding compound is derived from a heparin amine moiety formed by the removal of 10 to 100% of the N-sulfate groups of a heparin salt.

Claim 11

A compound characterized in whble or in part by being the reaction product of: (a) a compound comprising in whole or in part: (1) a water-soluble polysaccharide moiety having an average of at least 0.25 anionic group per monosaccharide unit, and (2) at least one chelating group, and (b) a radioactive tracer metal compound.

Claim 12

A compound characterized in whble or in part by being the reaction product of: (a) a compound comprising in whole or in part: (1) a water-soluble polysaccharide moiety having an average of at least 0.25 anionic group per monosaccharide unit, and (2) at least one chelating group, and (b) a radioactive tracer metal compound.

Claim 13

A compound according to any one of the preceding claims for use in diagnosing formed , and forming, blood clots in a vascular system.