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filingDate 1987-04-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 1989-09-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32cdbd8059b085589e47380e96f7a6c0
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publicationDate 1989-09-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-4870188-A
titleOfInvention Vinyl substituted radiohalogen conjugates for protein labeling
abstract Vinyl radiohalogenated small molecules as shown in formulas I and II: ##STR1## wherein *X is a radiohalogen, C═C is a double bonded set of sp 2 hybridized carbon atoms, and substituents R 1 , R 2 , and Y are as defined below. R 1 and R 2 are substituents independently selected from among hydrogen; alkyl or substituted alkyl, provided that any sp 2 or sp carbon atom substituted on the alkyl is separated from C═C by at least one fully substituted sp 3 carbon atom; aryl or substituted aryl, provided that the aryl is bonded directly to C═C; heteroalkyl, provided, first, that no heteroatom of the heteroalkyl bonds directly to C═C and, second, that any sp 2 or sp hybridized carbon bonded to a heteroatom of the heteroalkyl is not bonded directly to or otherwise conjugated with C═C and, third, that where a single sp 3 carbon intervenes between C═C and an sp 2 or sp carbon bonded to a heteroatom that intervening sp 3 carbon must be fully substituted; heteroaryl, provided that a heteroatom of the heteroaryl is not bonded directly with C 50 C; mixed alkylaryl, provided first, that no heteroatom is bonded to C═C and, second that either an aryl moiety of the mixed alkylaryl is directly bonded to C═C or that any aryl moiety is separated from C═C by at least one sp 3 carbon atom and, where only one sp 3 hybridized carbon atom intervenes between C═C and an aryl moiety, that intervening sp 3 carbon must be fully substituted. Y is substituent containing any of the groups described above for R 1 and R 2 , except that Y cannot be hydrogen, and bearing a functional group suitable for binding to protein under conditions that preserve the biological activity of the protein. The compounds of formulas I and II can be coupled to proteins such as monoclonal antibodies ot provide reagents for diagnostic and therapeutic applications. n Also metalated precursors of compounds I and II, as well as radiophormaceutical reagent kits containing any of the subject small molecules.
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