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Details for Patent: 5,182,370

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Details for Patent: 5,182,370

Title: Paramagnetic chelates
Abstract:Comounds having the formula ##STR1## wherein: a is 2 or 3; b is an integer from 0 to 4; Me.sup.(a+) is an ion of an element of atomic number from 57 to 70 or an ion of a transition metal of atomic number 21-29, 42 or 44; E.sup.(b+) is one or more physiologically biocompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units; S is the group --A--O--R wherein: A is --(CH.sub.2).sub.m --; --CH.sub.2 --C(CH.sub.3).sub.2 --; m is an integer from 1 to 5; R is H; linear or branched alkyl of 1 to 8 carbon atoms, said carbon atoms being unsubstituted or substituted by one or more hyroxy group; aralkyl of 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, amino, hydroxy or trifluoromethyl; (poly)-oxa-alkyl of 1 to 10 oxygen atoms and from 3 to 30 carbon atoms; R.sub.1 is R.sub.2 or --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; --(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.2 ; hydroxy-arylalkyl radical in which the aryl radical is unsubstituted or substituted by hydroxy; R.sub.2 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; with the proviso that when R.sub.1 is --CH.sub.2 COOZ or --CH(CH.sub.3)COOZ, R.sub.2 is other than --CH.sub.2 COOZ and --CH(CH.sub.3)--COOZ ##STR2## wherein: R.sub.3 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; a monovalent radical having the structure S--CH--COOZ; X is a direct chemical bond; --O--; --S--; --NH--; --N--CH.sub.2 COOZ; --N--CH(CH.sub.3)COOZ; n is the integer 2 or 3, with the proviso that when X is a direct chemical bond, n is 1, 2 or 3; Z is H or a negative charge; with the proviso that, unless R represents a trifluoromethyl substituted phenyl or R.sub.1 is R.sub.2, Me.sup.(a+) is different from Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+) and Mn.sup.(2+) and with the proviso that when R.sub.1 is R.sub.2 every molecule can contain not more than 500 nitrogen atoms.
Inventor(s): Felder; Ernst (Vitale, CH), Fumagalli; Luciano (Milan, IT), Uggeri; Fulvio (Milan, IT), Vittadini; Giorgio (Milan, IT)
Assignee: Bracco Industria Chimica S.p.A. (Milan, IT)
Filing Date:Dec 13, 1989
Application Number:07/450,225
Claims:1. A compound having the formula ##STR48## wherein: a is 2 or 3;

b is an integer from 0 to 4;

Me.sup.(a+) is an ion of an element of atomic number from 57 to 70 or an ion of a transition metal of atomic number 21-29, 42 or 44;

E.sup.(b+) is one or more physiologically bicompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units;

S is the group --A--O--R wherein:

A is --(CH.sub.2).sub.m --; --CH.sub.2 --C(CH.sub.3).sub.2 --;

m is an integer from 1 to 5;

R is H; linear or branched alkyl of 1 to 8 carbon atoms, said carbon atoms being unsubstituted or substituted by one or more hydroxy group; aralkyl of 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, amino, hydroxy or trifluoromethyl; (poly)-oxa-alkyl of 1 to 10 oxygen atoms and from 3 to 30 carbon atoms;

R.sub.1 is R.sub.2 or --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; --(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.2 ; hydroxy-arylalkyl radical in which the aryl radical is unsubstituted or substituted by hydroxy;

R.sub.2 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ with the proviso that when R.sub.1 is --CH.sub.2 COOZ or --CH(CH.sub.3)COOZ, R.sub.2 is other than --CH.sub.2 COOZ and --CH(CH.sub.3)COOZ; ##STR49## wherein: R.sub.3 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; a monovalent radical having the structure S--CH--COOZ;

X is a direct chemical bond; --O--; --S--; --NH--; --N--CH.sub.2 COOZ; --N--CH(CH.sub.3)COOZ;

n is the integer 2 or 3, with the proviso that when X is a direct chemical bond, n is 1, 2 or 3;

Z is H or a negative charge;

with the proviso that, unless R represents a trifluoromethyl substituted phenyl or R.sub.1 is R.sub.2, Me.sup.(a+) is different from Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+) and Mn.sup.(2+) and with the proviso that when R.sub.1 is R.sub.2 every molecule can contain not more than 500 nitrogen atoms.

2. A complex salt of a substituted .alpha.-amino propionic acid of formula ##STR50## wherein: a is 2 or 3;

b is an integer from 0 to 4;

Me.sup.(a+) is an ion of an element of atomic number 57-63 or 65-70 or an ion of a transition metal of atomic number 21-24, 27-29, 42 or 44;

E.sup.(b+) is one or more physiologically biocompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units;

S is:

1. --CH.sub.2 OR.sub.5 ;

2. --C(CH.sub.3).sub.2 --CH.sub.2 OR.sub.5 ; wherein R.sub.5 is

(a) phenyl;

(b) benzyl;

(c) 1-8 carbon alkyl;

(d) dihydroxy substituted lower alkyl;

(e) --H;

(f) (CH.sub.2 CH.sub.2 O).sub.p CH.sub.3 wherein p is an integer number between 1 and 5;

and R.sub.4 is --(CH.sub.2).sub.n --X--(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.2 wherein X is:

(a) a direct chemical bond;

(b) --O--;

(c) N--CH.sub.2 COOZ; and n is 1, 2 or 3 when X is a direct bond or the integer 2 or 3;

Z is H or a negative charge.

3. A complex salt according to claim 1 wherein the complexed ion is a member selected from the group consisting of La.sup.(3+), Sm.sup.(3+), Eu.sup.(3+), Dy.sup.(3+), Ho.sup.(3+), Yb.sup.(3+), Tb.sup.(3+), Nd.sup.(3+) and Er.sup.(3+).

4. A complex salt according to claim 1 wherein the complexed ion is Dy.sup.(3+).

5. The sodium salt of the complex dysprosium compound of 3-phenyl-methoxy-2-N-[2'-N'-[2"-N",N"-bis-(carboxymethyl)-aminoethyl]-N'-( carboxymethyl)-aminoethyl]-N-(carboxymethyl)aminopropionic acid.

6. The N-methylglucamine salt of the complex dysprosium compound of 3-phenyl-methoxy-2-N-[2'-N'-[2"-N",N"-bis-(carboxymethyl)aminoethyl]-N'-(c arboxymethyl)-aminoethyl]-N-(carboxymethyl)amino=propionic acid.

7. The N-methylglucamine salt of the complex dysprosium compound of 3-hydroxy-2-N-[2'-N'-[2"-N",N"-bis-(carboxymethyl)-aminoethyl]-N'-(carboxy methyl)-aminoethyl]-N-(carboxymethyl)aminopropionic acid.
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