7-substituted 4-aza cholanic acid derivatives and their use

Details 7-substituted 4-aza cholanic acid derivatives and their use 7-substituted 4-aza cholanic acid derivatives and their use

C - Chemistry, Metallurgy

07

J

C07J 73/00 (2006.01) A61K 31/58 (2006.01) C07C 59/353 (2006.01) C07C 69/00 (2006.01) C07C 69/716 (2006.01) C07C 235/74 (2006.01) C07C 255/31 (2006.01) C07D 207/34 (2006.01) C07D 213/60 (2006.01) C07D 215/16 (2006.01) C07D 307/56 (2006.01) C07D 333/26 (2006.01) C07J 9/00 (2006.01)

Patent

CA 2200885

Compounds of formula (I) wherein: the dotted line indicates that a double bond may be present or absent; R1 is H, methyl or ethyl; R2 is .alpha.- or .beta.- C1-10 straight or branched alkyl; R3 is CO2H, CN, CO2R4, COHNR4, or CON(R4)2; R4 is H, C1-10 straight or branched alkyl, aryl, heteroaryl, or aralkyl; Aryl is phenyl, substituted phenyl, naphthyl, or biphenyl; Heteroaryl is pyridil, pyrrolyl, thienyl, furanyl or quinolinyl; and Aralkyl is C1-10 alkyl substituted with one to three phenyl or substituted phenyl moieties; and their pharmaceutically acceptable salts are described. These compounds are 5.alpha.- reductase type 1 inhibitors. They may be used for treating conditions associated with an excess of DHT, either alone or in combination with other 5.alpha.-reductase inhibitors.

Composés de formule (I) dans laquelle la ligne en pointillés indique qu'une double liaison peut être présente ou absente; R?1¿ représente H, méthyle ou éthyle; R?2¿ représente .alpha.- ou .beta.-alkyle C¿1?-C¿10? linéaire ou ramifié, R?3¿ représente CO¿2?H, CN, CO¿2?R?4¿, COHNR?4¿, CON(R?4¿)¿2?; R?4¿ représente H, alkyle C¿1?-C¿10? droit ou ramifié, aryle, hétéroaryle ou aralkyle; l'aryle peut être phényle, phényle substitué, naphtyle ou biphényle; l'hétéroaryle est pyridyle, pyrrolyle, thiényle, furanyle ou quinolinyle; et l'aralkyle est alkyle C¿1?-C¿10? substitué par une à trois fractions phényle ou phényle substituées. L'invention porte également sur les sels pharmacocompatibles desdits composés qui sont des inhibiteurs de type 1 de la 5.alpha.-réductase. Ils peuvent s'utiliser seuls ou en association avec d'autres inhibiteurs de la 5.alpha.-réductase pour le traitement d'états liés à un excès de dihydrotestostérone (DHT).

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