Disclosed herein is an oligonucleotide conjugate or complex thereof, comprising a modified oligonucleotide having sequence independent antiviral activity against hepatitis B, a liver targeting agent, and a linker connecting the liver targeting agent to a 3′ end and/or a 5′ end of the modified oligonucleotide or complex thereof. The oligonucleotide conjugate may be incorporated into a pharmaceutical composition for treating a liver disease or disorder such as hepatitis B.

The present disclosure provides a single dose form composition to optimize the relationship between the ‘Tolate-Cobalamin’ and ‘Choline-Betaine’ pathways. Single dose form compositions disclosed herein ensure an adequate intake of the rate limiting compounds that have been demonstrated to reduce the efficiency of this vital metabolic axis, and methods of use thereof.

Compounds derived from celecoxib and valdecoxib, and methods of use thereof, are disclosed. The compounds are useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The compounds contain a radioactive agent which permits imaging. The compounds concentrate at sites of increased cyclooxygenase expression, such as areas of increased COX-2 expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections, assessing efficacy of diagnosis and treatment of rheumatoid arthritis, and assessing the need for treatment with opioid drugs.

The present disclosure relates to compounds according to Formula I. These compounds display very good binding affinities to the PSMA binding sites. They comprise a radioactive isotope or a chelating moiety that can be labeled with a radioactive metal such as [.sup.68Ga]or [.sup.177Lu]. The present disclosure also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or a complex thereof, or a pharmaceutically acceptable salt thereof.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

Aspects of the present disclosure relate to local delivery of pentaaza macrocyclic ring complexes to the intestines and methods of using the same. Certain disclosed dosage forms, including oral dosage forms suitable for local delivery and characterized by low systemic oral bioavailability, are therapeutically effective to relieve symptoms of inflammatory diseases of the lower gastrointestinal tract (e.g. small intestine, colon, and/or rectum) while minimizing systemic toxicity.

It is an object of the present invention to provide a conjugate of a biotin-modified dimer and a phthalocyanine dye, which is used in photoimmunotherapy. The present invention provides a conjugate of a compound represented by the following formula (1) or a salt thereof and a phthalocyanine dye:

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wherein the meaning of each of symbols is as defined in the specification.

A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt, is disclosed. Compositions comprising the compound and methods of use are also disclosed. Those dimeric Evans Blue derivatives, denoted as N(tEB)2, reversibly bind two molecules of albumin via the two albumin binding regions of each NtEB in the dimer, resulting in significantly increased binding affinity to albumin and extended circulation half-life in vivo. Further, when the N(tEB)2 is conjugated to a peptide therapeutic, the in situ formation of the complex of N(tEB)2 with two albumin molecules resulted in increased resistance of the peptide therapeutic from proteolysis.

##STR00001## ##STR00002## ##STR00003## ##STR00004##

Compositions for delivering a drug to a subject having: a plurality of self-assembled supramolecular nanoparticles (SMNPs), each of the plurality of self-assembled supramolecular nanoparticles (SMNPs) having: a plurality of binding components, each having a plurality of binding regions; a plurality of cores that are suitable to at least provide some mechanical structure to the plurality of self-assembled supramolecular nanoparticles (SMNPs), the plurality of cores comprising at least one core binding element adapted to bind to the binding regions to form a first inclusion complex; a plurality of terminating components, each having a single terminating binding element that binds to remaining binding regions of one of said plurality of binding components by forming a second inclusion complex; the drug; and a reporter agent, and methods of use thereof.

An amorphous form of a chelating agent is provided, in particular wherein the chelating agent comprises ethylenediaminetetraacetic acid/edetic acid (EDTA), diethylenetriaminepentaacetic acid/pentetic acid (DTPA), nitrilotriacetic acid (NTA), amino tris(methylenephosphonic acid) (ATMP), ethylenediamine tetramethylene phosphonic acid (EDTMP), 1-hydroxyethane 1,1-diphosphonic acid (HEDP), ethylenediaminedisuccinic acid (EDDS), iminodisuccinic acid (IDS), hydroxamic acid, oxalic acid, galactaric acid, metaphosphoric acid, or phytic acid, or a salt of any one or more of the above acids, or a mixture of two or more of any of the above acids or salts thereof.

A process for preparing an amorphous form of a chelating agent comprises the steps of: a) Dissolving the chelating agent in a suitable solvent; b) Optionally purifying the solution; c) Isolating an amorphous form of the chelating agent; d) Optionally post drying or conditioning the amorphous form of the chelating agent.