Fluoro linkers and their use as linkers for enzyme-activated drug conjugates

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United States of America Patent

APP PUB NO 20050107543A1
SERIAL NO

10486477

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention provides compounds or formula (1) R.sub.1--HN--CH.sub.2--CF.sub.2--(CH.sub.2).sub.l--CR.sub.3R.sub.4--CO--R-.sub.2, wherein: l is 0, 1 or 2, R.sub.1 is a labile amino protecting group, R.sub.2 is hydroxy group or the residue or an activated ester or halogen atom; R.sub.3 and R.sub.4 are independently hydrogen atom or C.sub.1-C.sub.4 alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.

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Patent Owner(s)

Patent OwnerAddress
PHARMACIA ITALIA S P AVIA ROBERT KOCH 1 2 20152 MILAN

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Angelucci, Francesco Milan, IT 32 523
Caruso, Michele Milan, IT 51 428
Faiardi, Daniela Pavia, IT 10 39
Pesenti, Enrico Milan, IT 20 417
Scolaro, Alessandra Milan, IT 18 89
Suarato, Antonino Milan, IT 46 647

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