A61K49/08

MALIGNANT TUMOR TARGET PEPTIDE

The present invention provides a peptide comprising the amino acid sequence of any of the formulas (I-(III) below: (I) an amino acid sequence of (X1)[D]P[D](X2)[D] wherein X1 is W or F, X2 is S or T, and each amino acid symbol immediately followed by symbol [D] is a D form of the amino acid, (II) an amino acid sequence of P[D]T[D](X).sub.n F[D] wherein (X).sub.n is any amino acid in the number of n selected independently of each other, n is an integer of 0-4, and the symbol [D] is as defined above, (III) an amino acid sequence that is a Retro-inverso of the amino acid sequence of any of the aforementioned (I) and the aforementioned (II);
and a conjugate containing the peptide and a functional part.

NITROGEN-CONTAINING MACROCYCLIC CONJUGATES AS RADIOPHARMACEUTICALS

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

Imaging compositions

In one aspect, compositions are described herein. In some embodiments, a composition described herein comprises, consists of, or consists essentially of an MRI-active or MRI-sensitive polymer or oligomer formed from (i) a non-alkoxylated and non-alkenoxylated citric acid, citrate, or ester/amide of citric acid, and optionally an alkoxylated or alkenoxylated citric acid, citrate, or ester/amide of citric acid, (ii) a polyol/polyamine such as a diol/diamine, (iii) a monomer comprising an MRI contrast agent, and (iv) an amino acid monomer. The polymer or oligomer may be photoluminescent and MRI-sensitive. In another aspect, imaging methods utilizing the compositions described herein are described. In another aspect, scaffolds, grafts, and films comprising, consisting of, or consisting essentially of the compositions described herein are described.

NEW CONTRAST AGENT FOR USE IN MAGNETIC RESONANCE IMAGING

The present invention relates to a new class of compounds of general formula (I), the Gd.sup.3+ chelate complexes thereof, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents. Formula (I)

##STR00001##

Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilizing the radiolabelled compounds of the invention.

Collagen imaging compositions

Compounds and methods for imaging and/or assessing collagen are described. The compounds can include collagen binding peptides.

Targeted contrast agents comprising a hydrazide functional group
10286090 · 2019-05-14 · ·

Described herein is a contrast agent for administration to a subject. The contrast agent includes a targeting portion that includes a hydrazide functional group; a metal ion bound to a metal-complexable portion; and a linker joining the targeting portion and the metal-complexable portion of the contrast agent. The portion that is not bound to a metal ion localizes the contrast agent to necrotic tissue in the subject.

Long-lived gadolinium based tumor targeted imaging and therapy agents

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt thereof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

Composition Intended to Vectorise an Anti-Cancer Agent
20190099496 · 2019-04-04 ·

A composition in the form of a water-in-oil emulsion comprising: from 20% to 40% (v/v) of aqueous phase, in the form of droplets, comprising an anti-cancer agent and a densifying agent chosen from the complexes of nonionic macrocyclic chelate with a paramagnetic metal, from 60% to 80% (v/v) of lipid phase comprising an iodized oil and at least one surfactant of formula (I) in a proportion, by weight of surfactant relative to the total volume of the composition, of 0.3% to 5%, formula (I) of said surfactant being the following:

##STR00001##

in which: s is 0 or 1, m is an integer from 2 to 30, R.sub.1 represents a group of formula (II)

##STR00002## in which n is an integer from 4 to 10, o is an integer from 1 to 4, p is an integer from 3 to 7, q is an integer from 2 to 10, and r is 0 or 1, R.sub.2 represents a hydrogen atom or is identical to R.sub.1, and each R.sub.3 independently represents a hydrogen atom or is identical to R.sub.1.

Gadolinium complex comprising DO3A-tranexamic acid conjugate

The present disclosure relates to a magnetic resonance imaging (MRI) contrast agent containing a gadolinium complex, and more specically, to a DO3A-tranexamic acid compound having a structure of a chemical formula 1, or an ester compound thereof, and gadolinium complexes thereof. The DO3A-tranexamic acid compound or the ester compound thereof may be used to prepare gadolinium complexes. The gadolinium complexes exhibit thermodynamic and kinetic stabilities, and show the relaxation rate equal to that of the clinical contrast agent which is currently commercially available. Therefore, the gadolinium complexes can be widely used as an MRI contrast agent.