4,1-benzoxazepin derivatives and their use

C - Chemistry – Metallurgy – 07 – D

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C07D 267/14 (2006.01) A61K 31/55 (2006.01) A61K 31/551 (2006.01) A61K 31/553 (2006.01) A61K 31/554 (2006.01) C07D 413/02 (2006.01) C07D 413/06 (2006.01) C07D 413/12 (2006.01) C07D 417/02 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2094335

4,1-Benzoxazepin-2-one derivatives represented by the formula (I): (See formula I) wherein R1 stands for hydrogen atom or an optionally substituted hydrocarbon group; R2 and R3 independently stand for hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic group; X stands for a bond or a spacer having the chain length of 1 to 7 atoms; Y stands for an optionally esterified or thioesterified carboxyl group, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted phenyl group, an optionally substituted carbamoyl group or a N-containing heterocyclic residue having hydrogen atom capable of being deprotonated; provided that, when X is methylene and R1 is not an alkyl group having carbon atoms of more than 4, Y is neither carboxyl group nor alkoxycarbonyl group; and the ring A may optionally be substituted, or salts thereof, which are useful for inhibiting squalene synthetase and fungal growth.

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