Functionalized vinyl azoles and their use

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 233/60 (2006.01) A61K 31/41 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 249/08 (2006.01) C07D 401/06 (2006.01) C07D 405/02 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07D 495/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2097824

Pharmaceutical compositions that contain vinylazoles having general formula (I) (see formula I) are disclosed, as well as new vinylazoles having general formula (Ia), contained within the scope of formula (I). In the formulas, X stands for an N atom or for a CH group; Y stands for a S atom or for a CH=CH group; Z stands for a cyano group, a fluorine, chlorine or bromine atom; and R1 or R2 stand for a carboxyl group that may be esterified, for a carboxylic acid amide group that may be substituted, for an aldehyde group, for an alkyl or aryl ketone group, for a sulfonamide group that may be substituted, or for a nitrile group; whereas the other group represented by R1 or R2 stands for a hydrogen atom, a lower alkyl group of a cycloalkyl group, an aryl group that may be substituted; an aralkyl group, a carboxyl group that may be esterified, a carboxylic acid amide group that may be substituted, an aldehyde group, an alkyl or aryl ketone group or a nitrile group. The compounds having general formulas (I) or (Ia) are effective inhibitors of estrogen biosynthesis (aromatase inhibitors) and are useful for treating diseases medicated by or dependent on estrogens. Processes for producing the compounds having general formula (I) are also disclosed.

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