Patent classifications
A61K51/0474
Cage-Like Bifunctional Chelators, Copper-64 Radiopharmaceuticals and PET Imaging Using the Same
Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula
##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.
THERAPEUTIC AND IMAGING AGENTS FOR TARGETING MYOCARDIAL TISSUE
Analogs and derivatives of omecamtiv mecarbil (OM), including an .sup.18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an .sup.18F-labeled analog of OM.
Compositions and methods for tumor imaging and targeting by a class of organic heptamethine cyanine dyes that possess dual nuclear and near-infrared properties
The present invention provides for heptamethine cyanine dyes that possess both nuclear and near-infrared imaging capabilities. These dyes can be used for imaging, targeting and detecting tumors in patients.
Non-invasive diagnostic agents of cancer and methods of diagnosing cancer, especially leukemia and lymphoma
The present invention is directed to novel non-invasive diagnostic tools to image cancers, especially, leukemia and non-Hodgkin's lymphomas (NHL) with minimal toxicity in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probe is capable of detecting precancerous cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and staging of NHL using non-invasively molecular imaging techniques. This novel probe will also be useful to monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of NHL. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.
IMAGING AND TREATMENT OF PATHOPHYSIOLOGIC CONDITIONS BY CERENKOV RADIATION
The present disclosure discloses methods and compositions for A administering Cerenkov radiation-induced therapy (GRIT). In an aspect, the invention encompasses a composition comprising at least two radiation-sensitive molecules. In another aspect, the invention encompasses a composition comprising a radiation-sensitive molecule and a targeting agent. In still another aspect, the invention encompasses a method for administering Gerenkov radiation-induced therapy (GRIT) to a target tissue in a subject. The method comprises administering to the subject an effective amount of a composition B comprising at least one radiation-sensitive molecule and administering to the subject an amount of a Gerenkov radiation (GR)-emitting radionuclide effective to activate the radiation-sensitive molecule, thereby administering GRIT to the target tissue in the subject.
MULTIVALENT GLYCO-COMPLEX, IMAGING AGENT AND USES THEREOF
The present disclosure relates to a multivalent glyco-complex, an imaging agent and uses thereof. The multivalent glyco-complex includes a plurality of glucose molecules, each of which connects to a central nitrogen atom through a linker, and a chelating group G. The multivalent glyco-complex can be used as an imaging agent to diagnose cancers and to evaluate the therapeutic efficacy of cancers.
Inert nanocapsules
Compounds are presented having the formula [M.sub.4L.sub.6].Math.X.sub.n, where M is a transition metal ion having 6 d-shell valence electrons, X is a counter ion and n is the number of counterions such that the total charge of the compound of formula (I) is zero, and wherein L is a 5-(5-bipyridin-2,2-yl)-2,2-bipyridine or derivative thereof. Methods of preparing the compounds and uses of the compounds to retain radiolabels are also presented.
DLL3-SPECIFIC BINDING CONSTRUCTS AND THEIR USE IN RADIOTHERAPY
The present invention relates to DLL3-specific binding constructs comprising a designed ankyrin repeat domain with binding specificity for DLL3, a connector, and a chelator capable of bonding to a radionuclide, such as Pb-212, as well as to such DLL3-specific binding constructs comprising a half-life extending moiety with binding specificity for serum albumin. The invention further relates to methods of producing such radio-labelled DLL3-specific binding constructs, pharmaceutical compositions comprising such constructs, and the use of such constructs or pharmaceutical compositions in methods for treating, imaging or diagnosing diseases, such as cancer.
Metal nuclide-loaded carbon microsphere (CMS), preparation method, and use thereof
A metal nuclide-loaded carbon microsphere (CMS), and a preparation method and a use thereof are provided. The preparation method includes: subjecting a metal ion and a small organic molecule to a reaction in an aqueous solution to obtain a complex; allowing a CMS to adsorb the complex; and subjecting the CMS adsorbing the complex to a first treatment. The metal nuclide-loaded CMS prepared by the method can stably exist in an aqueous solution at a temperature of lower than 180 C. and a pressure of lower than 10 MPa and has a metal nuclide dissolution rate of lower than 0.1% in the aqueous solution. After the prepared metal nuclide-loaded CMS is subjected to moist-heat sterilization at 121 C. for 15 min, a radionuclide release rate is still lower than 0.1%, which can significantly reduce the safety risk of the radioactive microsphere product in clinical use.
Radiolabeled anti-PD-L1 antibodies for immuno-PET imaging
Radiolabeled anti-PD-L1 antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of PD-L1 proteins in a patient or sample.