Imidazole derivatives and their use as farnesyl protein transferase inhibitors

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United States of America Patent

PATENT NO 6410539
SERIAL NO

09509476

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention relates to a compound of Formula (1) wherein Ar.sup.1 represent (A) or (B) or (C); R.sup.1 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkanoyl; R.sup.12 and R.sup.13 are independently hydrogen or C.sub.1-4 alkyl; Ar.sup.2 is phenyl or heteroaryl; p is 0 or 1; Ar.sup.3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R.sup.2 and --(CH.sub.2).sub.n R.sup.3 are attached to ring carbon atoms; R.sup.2 is a group of Formula (II) or R.sup.2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R.sup.3 is phenyl or heteroaryl; provided that: when n is 0, Ar.sup.3 is substituted by R.sup.2 in the 4-position and --(CH.sub.2).sub.n R.sup.3 in the 3- or 5-position; and when n is 1 or 2, Ar.sup.3 is substituted by R.sup.2 in the 3- or 5-position and --(CH.sub.2).sub.n R.sup.3 in the 4-position; and R.sup.5 -R.sup.9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.

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Patent Owner(s)

Patent OwnerAddress
ASTRAZENECA UK LIMITED15 STANHOPE GATE LONDON W1K 1LN
ZENECA PHARMA SA OF LE GAILEN1 RUE DES CHAUFFOURS BOITE POSTAKLE 124 F-95022 CERGY CEDEX

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Arnould, Jean-Claude Reims, FR 20 129

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