Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

A compound of formula (I)

• wherein
• R1 and R2 are each independently selected from the group consisting of H and halogen;
• (i) R3 is selected from the group consisting of H and C1-4 alkyl and
• R4 is selected from the group consisting of
• C1-6-alkyl optionally substituted with OH;
• —(CH2)n—R5, where n is 1 to 3 and R5 is a 3 to 7 membered alicycle;
• 4 to 7 membered unsubstituted saturated alicycle or unsubstituted heterocycle comprising one heteroatom selected from the group consisting of nitrogen, sulfur, and oxygen;
• 5 membered partially unsaturated heterocycle or aromatic heterocycle comprising 1 to 3 heteroatom(s) selected from the group consisting of nitrogen and oxygen, and being optionally substituted with one or two substituents selected from the group consisting of halogen, CN, C1-4-alkyl, C1-3-(per)haloalkyl, OH, C1-3-alkoxy, C(O)N(C1-3-alkyl)2, and 6 membered saturated heterocycle comprising 1 to 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur and being optionally substituted with one or two substituent(s) independently selected from the group consisting of halogen, CN, C1-4-alkyl, C1-3-(per)haloalkyl, OH, and C1-3-alkoxy;
• 5 membered unsubstituted unsaturated or aromatic heterocycle comprising 1 to 3 heteroatom(s) independently selected from the group consisting of nitrogen, sulfur, and oxygen;
• 5 membered unsaturated or aromatic heterocycle comprising 1 to 3 heteroatom(s) independently selected from the group consisting of nitrogen and oxygen, and being optionally substituted with one or two substituent(s) independently selected from the group consisting of halogen, CN, C1-4-alkyl, C1-3-(per)haloalkyl, OH, C1-3-alkoxy, C(O)N(C1-3-alkyl)2, and 6 membered saturated heterocycle containing 1 to 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur and being optionally substituted with one or two substituent(s) independently selected from the group consisting of halogen, CN, C1-4-alkyl, C1-3-(per)haloalkyl, OH, and C1-3-alkoxy;
• phenyl, 6 membered unsaturated, or aromatic heterocycle comprising 1 to 3 heteroatom(s) independently selected from the group consisting of nitrogen, sulfur, and oxygen, and being optionally substituted with one to five substituent(s) independently selected from the group consisting of halogen, CN, C1-4-alkyl, C1-3-(per)haloalkyl, OH, oxo, C1-3-alkoxy, morpholino, C(O)N(C1-3-alkyl)2 and a 6 membered saturated heterocycle with 1 to 3 heteroatom(s) selected from the group consisting of nitrogen, oxygen and sulfur, optionally substituted with C1-4-alkyl;
• and
• 6 membered saturated heterocycle comprising 1 to 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur and being optionally substituted with one to three substituent(s) independently selected from the group consisting of halogen, CN, C1-4-alkyl, C1-3-(per)haloalkyl, OH, oxo, and C1-3-alkoxy, or two adjacent substituents may form a 5 or 6 membered saturated fused ring;
• or
• (ii) R3 and R4 form together with the nitrogen atom they are attached to a group selected from a 4 to 7 membered saturated heterocycle comprising said nitrogen atom and optionally one additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur including sulfonyl, and being optionally substituted with a substituent selected from the group consisting of halogen, CN, methyl, C1-3-(per)haloalkyl, OH, oxo, C1-3-alkoxy and a 4 to 7 membered alicycle or saturated heterocycle with 1 to 3 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, optionally substituted with C1-4-alkyl;
• or
• (iii) R3 and R4 form together with the nitrogen atom they are attached to a group selected from a 4 to 7 membered saturated heterocycle comprising said nitrogen atom and said saturated heterocycle forms a fused or spirocycle ring with a 4 to 7 membered saturated or unsaturated alicycle or heterocycle with 1 to 3 heteroatoms selected from the group nitrogen, oxygen and sulfur;
• provided that only one of hydrogens H1 and H2 is present at the same time, and the position of the double bonds in the pyrazole ring to which the hydrogens H1 and H2 are attached is determined based on which of the hydrogen H1 and H2 is present
• or a pharmaceutically acceptable salt thereof.