Compounds with hydroxycarbonyl-halogenoalkyl side chains

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Details

C514S412000, C514S443000, C514S456000, C514S520000, C514S570000, C544S105000, C548S452000, C549S023000, C549S049000

Reexamination Certificate

active

10281990

ABSTRACT:
The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1):in whichR1represents a hydrogen atom, etc.,R2represents a C1–C7halogenoalkyl group, etc.,m represents an integer of 2 to 14, andn represents an integer of 2 to 7,or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

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West, Anthony R., Solid State Chemistry and its Applications, Wiley, New York, 1988, pp. 358 & 365.
Vippagunta et al., Advanced Drug Delivery Reviews 48: 3-26, 2001.

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