The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

The invention provides compounds of formulae I, II, III, and IV:

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and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.