Contrast agents and compositions for radiological imaging, and radiological imaging method utilizing same

• US 5,545,397 A
• Filed: 11/18/1994
• Issued: 08/13/1996
• Est. Priority Date: 10/23/1991
• Status: Expired due to Fees

• Current Assignee: Boron Biologicals Incorporated, Guerbet
• Original Assignee: Boron Biologicals Incorporated, Guerbet
• Inventors: Meyer, Dominique, Spielvogel, Bernard F.
• Primary Examiner(s): Burn, Brian M.
• Application Number:
  US08/341,767
• Time in Patent Office: 634 Days
• Field of Search: 424/5, 424/9.4, 423/287, 423/292, 423/294
• US Class Current: 424/9.4
• CPC Class Codes: A61K 49/0433 containing an organic halogenated X-ray contrast-enhancing agent
• CPC Class Codes: C01B 35/06 Boron halogen compounds
• CPC Class Codes: C07C 215/10 with one amino group and at least two hydroxy groups bound to the carbon skeleton
• CPC Class Codes: C07F 5/022 without C-boron linkages
• CPC Class Codes: C07F 9/067 Polyphosphazenes containing the structure [P=N-n] cyclic compounds C07F9/65812
• CPC Class Codes: C07F 9/5357 Polyphosphazenes containing the structure [P=N-]n cyclic phosphazenes C07F9/65812
• CPC Class Codes: C07F 9/65812 Cyclic phosphazenes [P=N-]n, n>=3
• CPC Class Codes: C08G 79/00 Macromolecular compounds obtained by reactions forming a linkage containing atoms other than silicon, sulfur, nitrogen, oxygen, and carbon with or without the latter elements in the main chain of the macromolecule

Abstract

Contrast agent for X-ray imaging, consisting of a halogenated, especially iodinated or brominated, derivative of boron, having characteristics necessary for its use in X-ray imaging. The contrast agent may be used for imaging a corporeal situs by radiological techniques, comprising delivery to the corporeal situs of an imagingly effectively amount of a physiologically acceptable composition comprising the boron reagent. A variety of illustrative boron reagents is described, including vectorised boron derivatives, e.g., boron derivatives encapsulated within liposomes, fixed on or bonded to macromolecules or polymers, etc. The contrast agents, formulations, and method of the present invention may be employed for a wide variety of radiological imaging applications, e.g., excretory urography, angiocardiography, aortography, etc.

Claims

1. A method of imaging a corporeal situs using x-ray imaging means, comprising delivering to the corporeal situs an imagingly effective amount of a physiologically acceptable contrast medium formulation containing a radiopacity-imparting boron compound, and thereafter visualizing the corporeal situs with said x-ray imaging means, wherein the boron compound comprises a compound selected from the group consisting of iodinated boron salts of the formula:

space="preserve" listing-type="equation">M.sub.x B.sub.n H.sub.n-y I.sub.y

wherein;

M is a monovalent or divalent cation;

x is 1 when M is divalent and 2 when M is monovalent;

n is 3 to 14; and

y is 1 to 14,

and derivatives thereof.

2. A method according to claim 1, wherein the boron compound comprises a compound selected from the group consisting of iodinated boron salts of the formula:

space="preserve" listing-type="equation">M.sub.x B.sub.n H.sub.n-y I.sub.y

wherein;

M is an alkali metal or alkaline earth metal;

x is 1 when M is divalent and 2 when M is monovalent;

n is 10 to 12; and

y is 2 to 12,

and derivatives thereof.

3. A method according to claim 1, wherein M is selected from the group consisting of lithium, sodium, magnesium, and cesium.