NOVEL 4 (5)-IMIDAZOLE HAVING AROMATASE INHIBITIVE ACTIVITY
申请公布号:JPH032168(A)
申请号:JP19900080548
申请日期:1990.03.28
申请公布日期:1991.01.08
发明人:ARUTO YOHANESU KARUYARAINEN;REINO ORABI PERUKONEN;MARUYAARIISA SEDERUBARU;MATSUCHI ANTERO REHEDE;RISUTO ARUBO SAKARI RAMUMINTAUSUTA;ARUYA REENA KARUYARAINEN;ARUYA MARUKETSUTA KARAPUDASU
分类号:C07D233/56;A61K31/415;A61K31/4164;A61P35/00;A61P43/00;C07D233/54;C07D233/58;C07D233/64
主分类号:C07D233/56
摘要:Novel imidazole derivatives of the formula <CHEM> wherein R1, R2, R min 1 and R min 2, which can be the same or different, are H, CH3, C2H5, C3H7, OCH3, OH, CH2OH, NO2, NH2, CN, CF3, CHF2, CH2F or halogen; R min is H or <CHEM> where R3 is H, CH3 or halogen; R4 is H, R5 is H or OH, R6 is H or OH and R7 is H or R4 and R6 together form a bond or R5 and R7 together form a bond; X and Y, which can be the same or different, are a bond, a straight C1-2-alkyl or the corresponding alkenyl and z is 0 to 2 and <CHEM> wherein R1, R2, R min 1, R min 2 and R min are as defined before, R4 is H or OH and R5 is H or R4 and R5 together form a bond and y is 0 to 4, and their non-toxic salts exhibit aromatase and desmolase inhibiting properties. Very selective aromatase inhibiting compounds are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer.
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