Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

The present invention provides a radiopharmaceutical composition comprising the following four components: (i) a radio-labelled compound; (ii) ethanol; (iii) a stabilizer of the radio-labelled compound; and (iv) a cyclodextrin.

The present invention also provides a radiopharmaceutical composition comprising: (i) a radio-labelled compound; (ii) a stabilizer of the radio-labelled compound, wherein the stabilizer comprises: ascorbic acid, aspartic acid, cysteine, maleic acid, gentisic acid, glutathione, glutamic acid, mannitol, nicotinamide, calcium chloride, N-t-butyl-alpha-phenylnitrone (PBN), tartaric acid, para-aminobenzoic acid (pABA), chloride ions or salts or combinations thereof; and (iii) a cyclodextrin.

The present invention provides .sup.18F-labeled amino acids or derivatives thereof having formula (I) and methods of making same, which can be suitable for PET imaging: ##STR00001##

The present invention provides a set of novel isobaric chemical tags, also referred herein as SUGAR (Isobaric Multiplex Reagents for Carbonyl Containing Compound). These labeling tags are compact and easy to synthesize at high yield and purity in just a few steps using commercially available starting materials. The tagging reagents of the present invention comprise: a) a reporter group, having at least one atom that is optionally isotopically labeled; b) a balancing group, also having at least one atom that is optionally isotopically labeled, and c) an aldehyde, ketone, or carboxylic acid reactive group. The multiplex SUGAR tags are able to react with an aldehyde, ketone, or carboxylic acid group of the molecule to be tagged, which offers the capability for labeling and quantitation of glycans, proteins/peptides, and fatty acids.

Methods are provided for the prognosis, diagnosis and treatment of various pathological states, including cancer, chemotherapy resistance and dementia associated with Alzheimer's disease. The methods provided herein are based on the discovery that various proteins with a high level of sialylation are shown herein to be associated with disease states, such as, cancer, chemotherapy resistance and dementia associated with Alzheimer's disease. Such methods provide a lysosomal exocytosis activity profile comprising one or more values representing lysosomal exocytosis activity. Also provided herein, is the discovery that low lysosomal sialidase activity is associated with various pathological states. Thus, the methods also provide a lysosomal sialidase activity profile, comprising one or more values representing lysosomal sialidase activity. A lysosomal sialidase activity profile is one example of a lysosomal exocytosis activity profile.

Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula:

##STR00001##

The compounds are useful for treating inflammatory and autoimmune diseases.

Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula:

##STR00001##

The compounds are useful for treating inflammatory and autoimmune diseases.

The present invention relates to a compound represented by the following General Formula (1) or a salt thereof.

##STR00001##

In General Formula (1), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R.sup.1 and R.sup.2 may be bonded to each other to form a ring. R.sup.3 and R.sup.4 may be bonded to each other to form a ring. R.sup.1 and/or R.sup.2 may be bonded to a 6-membered ring to which —NR.sup.1R.sup.2 is bonded to form a ring. R.sup.3 and/or R.sup.4 may be bonded to a 6-membered ring to which —NR.sup.3R.sup.4 is bonded to form a ring. R.sup.5 represents —.sup.11CH.sub.3, a linear or branched alkyl group which may have a substituent or the like. R.sup.6 represents —F, —.sup.18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.

The present invention relates to a compound represented by the following General Formula (1) or a salt thereof.

##STR00001##

In General Formula (1), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R.sup.1 and R.sup.2 may be bonded to each other to form a ring. R.sup.3 and R.sup.4 may be bonded to each other to form a ring. R.sup.1 and/or R.sup.2 may be bonded to a 6-membered ring to which —NR.sup.1R.sup.2 is bonded to form a ring. R.sup.3 and/or R.sup.4 may be bonded to a 6-membered ring to which —NR.sup.3R.sup.4 is bonded to form a ring. R.sup.5 represents —.sup.11CH.sub.3, a linear or branched alkyl group which may have a substituent or the like. R.sup.6 represents —F, —.sup.18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.

The present disclosure provides a method for preparing a deuterated organic compound in good yield even though a reduced amount of benzene-D6 is used by using a solvent comprising a benzene-based compound not substituted with deuterium or partially substituted with deuterium.