Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

The present invention relates to a cycloaddition process comprising the step of reacting a halogenated aliphatic 1,3-dipole compound with a (hetero)cycloalkyne according to Formula (1): Preferably, the (hetero)cycloalkyne according to Formula (1) is a (hetero)cyclooctyne. The invention also relates to the cycloaddition products obtainable by the process according to the invention. The invention further relates to halogenated aliphatic 1,3-dipole compounds, in particular to halogenated aliphatic 1,3-dipole compounds comprising N-acetylgalactosamine-UDP (GalNAc-UDP), and to halogenated 1,3-dipole compounds comprising (peracylated) N-acetylglucosamine (GlcNAc), N-acetylgalactosamine (GalNAc), N-acetylmannosamine (ManNAc) and N-acetyl neuraminic acid (NeuNAc). ##STR00001##

The present invention relates to a cycloaddition process comprising the step of reacting a halogenated aliphatic 1,3-dipole compound with a (hetero)cycloalkyne according to Formula (1): Preferably, the (hetero)cycloalkyne according to Formula (1) is a (hetero)cyclooctyne. The invention also relates to the cycloaddition products obtainable by the process according to the invention. The invention further relates to halogenated aliphatic 1,3-dipole compounds, in particular to halogenated aliphatic 1,3-dipole compounds comprising N-acetylgalactosamine-UDP (GalNAc-UDP), and to halogenated 1,3-dipole compounds comprising (peracylated) N-acetylglucosamine (GlcNAc), N-acetylgalactosamine (GalNAc), N-acetylmannosamine (ManNAc) and N-acetyl neuraminic acid (NeuNAc). ##STR00001##

A method for detecting phospholipase D (PLD) activity in a cell, comprising: (i) stimulating endogenous PLD in said cell for said PLD to catalyze a transphosphatidylation reaction between phosphatidylcholine or a derivative thereof and an exogenous functionalized alcohol to form a phosphatidyl alcohol, wherein the functionalized alcohol possesses a first functional group that can react with and form a bond to a functionalized detectable label having a second functional group reactive with the first functional group, and said phosphatidyl alcohol contains said first functional group in available form; (ii) reacting said phosphatidyl alcohol with said functionalized detectable label under conditions where said functionalized detectable label reacts, via its second functional group, with the first functional group to form a linkage between said detectable label and said phosphatidyl alcohol so as to form a labeled phosphatidyl alcohol containing said detectable label; and (iii) detecting said labeled phosphatidyl alcohol.

A method for detecting phospholipase D (PLD) activity in a cell, comprising: (i) stimulating endogenous PLD in said cell for said PLD to catalyze a transphosphatidylation reaction between phosphatidylcholine or a derivative thereof and an exogenous functionalized alcohol to form a phosphatidyl alcohol, wherein the functionalized alcohol possesses a first functional group that can react with and form a bond to a functionalized detectable label having a second functional group reactive with the first functional group, and said phosphatidyl alcohol contains said first functional group in available form; (ii) reacting said phosphatidyl alcohol with said functionalized detectable label under conditions where said functionalized detectable label reacts, via its second functional group, with the first functional group to form a linkage between said detectable label and said phosphatidyl alcohol so as to form a labeled phosphatidyl alcohol containing said detectable label; and (iii) detecting said labeled phosphatidyl alcohol.

The present invention includes novel compounds containing heterocycles or azaheterocycles and fused phenylene or aza and cyano substituted variants thereof. These compounds may be useful as host materials for phosphorescent electroluminescent devices.

This disclosure relates to trans-cyclooctene compounds and methods of using the same in bioorthogonal labeling experiments.

This disclosure relates to trans-cyclooctene compounds and methods of using the same in bioorthogonal labeling experiments.

The present disclosure describes functional oligomers or functional polymers. The functional oligomers or functional polymers may contain functional groups, e.g., OH and/or CHO. The functional oligomers or functional polymers may be obtained from hydrolyzing certain copolymers and may be soluble in commercially available solvents. The copolymers may be thermosetting polymers. The functional oligomers and functional polymers may be useful for recycling thermosetting polymers and may be useful as starting materials for preparing additional oligomers or polymers.