C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 73/00 (2006.01) A61K 31/58 (2006.01)
Patent
CA 2107102
- 76 - ABSTRACT 1. Compounds represented by the formula Image wherein R1 denotes a hydrogen atom or a lower alkyl group; R2 denotes a hydrogen atom, a halogen atom, or a hydroxyl, mercapto or amino group which may optionally be acylated or lower alkylated; R3, R4, R5 and R6 denote one of the following (a) to (d): (a) R3 and R5 each denote a hydrogen atom, and R4 and R6 each denote a hydrogen atom, a halogen atom or a lower alkyl group, (b) R3 and R6 each denote a hydrogen atom, and R4 and R5 combine to denote a single bond, a methylene group or a dihalomethylene group, (c) R3 and R4 combine to denote an oxo group or a methylene group, and R5 and R6 each denote a hydrogen atom, (d) R3 denotes an acyloxy group, R4 and R5 combine to denote a single bond, and R6 denotes a hydro- gen atom; A denotes C=O, CH2, C=CH2 or C=CH-lower alkyl; B denotes O, NH or N-lower alkyl; X does not exist, or denotes C=O or CH2; n denotes 2 or 3 when X does not exist, or denotes 1 or 2 when X denotes C=O or CH2; and the broken line between the 1- and 2-positions of the steroid skeleton means that a double bond may - 77 - optionally exist there. These compounds have an aroma- tase inhibition action and are useful for prophylaxis or treatment of diseases caused by excess of estrogens, for example, breast cancer, uterine cancer, prostatic hyper- trophy, etc.
Honma Seijiro
Iwashita Shigeki
Kawachi Tomoko
Koizumi Naoyuki
Matsui Teruaki
Smart & Biggar
Teikoku Hormone Mfg. Co. Ltd.
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