Thiazepine and oxazepine inhibitors of hiv-1 integrase

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 513/04 (2006.01) A61K 31/55 (2006.01) A61P 31/18 (2006.01) C07D 498/04 (2006.01) C07D 498/14 (2006.01) C07D 513/14 (2006.01)

Patent

CA 2372791

The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti- integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO2, lower ester or carboxylic acid; X-Y is CH2-S, S-CH2, CH2-O, CH2-S(O), S(O)-CH2, CH2-CH2, CH2-CH2-CH2, or CH2-CH2-CH2-CH2; R4 is H or hydroxy; R5 is H, phenyl, or alkylamine; W is S or O; and R6 is H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH2, CH2CH2, or C=O.

L'invention des composés non catéchol, tels que des thiazolothiazépines, qui sont des inhibiteurs anti-intégrase, ainsi que leurs analogues et leurs dérivés. Ces composés, qui sont utiles pour traiter l'infection à VIH, comprennent des composés (I), (II), (III) ou des sels pharmaceutiquement acceptables représentés dans laquelle A représente thiazole, benzène, naphtalène, pyridine, pyrimidine, pyrazine, ou quinoline; R représente un ou plusieurs éléments parmi H, halogène, alkyle inférieur, alcoxy inférieur, NO¿2?, ester inférieur ou acide carboxylique; X-Y représente CH¿2?-S, S-CH¿2?, CH¿2?-O, CH¿2?-S(O), S(O)-CH¿2?, CH¿2?-CH¿2?, CH¿2?-CH¿2?-CH¿2?, ou CH¿2?-CH¿2?-CH¿2?-CH¿2?; R¿4? représente H ou hydroxy; R¿5? représente H, phényle ou alkylamine; W représente S ou O; et R¿6? représente H, amine ou alkyle substitué ou non substitué; et Z représente S, O, CH¿2?, CH¿2?CH¿2? ou C=O.

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