ESTRA-1,3,5(10)-TRIENE COMPOUNDS CONDENSED IN POSITION 16(17) WITH A PYRAZOLE RING AS INHIBITORS OF 17-HSD1

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof (I) wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17beta-HSD1 and in treatment or prevention of steroid hormone dependent dis-eases or disorders, such as steroid hormone dependent dis-eases or disorders requiring the inhibition of the 17beta-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof. 本发明涉及式(I)的化合物及其药学上可接受的盐，其中R1至R4如权利要求中所定义。本发明进一步涉及它们作为17β-HSD1抑制剂和治疗或预防类固醇激素依赖性疾病或病症的用途，例如需要抑制17β-HSD1酶和/或需要降低内源性雌二醇浓度的类固醇激素依赖性疾病或病症。本发明还涉及上述化合物的制备和包含一种或更多种上述化合物或其药学上可接受的盐作为活性成分的药物组合物。