Heterocyclic derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2071375

Compounds of the formula: Image wherein R1 is carboxy or protected carboxy, R2 is hydrogen, lower alkyl or halogen, R3 is aryl or ar(lower)alkyl, each of which may have suitable substituent(s), [substituted carbamoyl](lower)alkyl, or:a group of the formula: Image in which Image is heterocyclic group containing nitrogen atom, and n is 0 or 1, R11 is hydrogen or lower alkyl, A is lower alkylene which may be substituted by oxo, or lower alkenylene, Q is carbonyl or lower alkylene, Image in which R4 is hydrogen or lower alkyl, and R5 is hydrogen, lower alkyl or Y-Z-R3. Y is bond or lower alkylene, Z is lower alkylene, lower alkenylene, -O- or Image in which R6 is hydrogen, lower alkyl, ar(lower)alkyl which may have suitable sub- stituent(s) or amino protective group, and pharmaceutically acceptables salts thereof. Pharma- ceutical compositions containing same, the preparation of these compounds and a method of treating or pre- venting testosteron 5.alpha.-reductase mediated diseases are also disclosed. The compounds according to the inven- tion are particularly useful for treating alopecia, acnes, prostatism, and the like.

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