PYRAZOLINE DERIVATIVES AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS

摘要

The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I), in which the substituents are as defined in the specification; to compounds of formula (I) for use as androgen receptor modulators. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.;

主权项

1. A compound of formula (I) in free form or in pharmaceutically acceptable salt form,wherein
R1 is C1-C3alkyl; R2 is halogen; R3 is cyano; R4 is selected from amino, halogen, hydroxy, C1-C3alkyl, halogen-C1-C3alkyl, hydroxy-C1-C3alkyl, C3-C6cycloalkyl, C1-C3alkoxy, halogen-C1-C3alkoxy, C1-C3alkoxy-C1-C3alkoxy, C3-C6cycloalkyl-C1-C3alkoxy, C3-C6cycloalkoxy; or R4 is selected from a (═O), (═S) or (═N(R8)) group; R5 is selected from hydrogen, amino, halogen, hydroxy, C1-C3alkyl, halogen-C1-C3alkyl, hydroxy-C1-C3alkyl, C3-C6cycloalkyl, C1-C3alkoxy, halogen-C1-C3alkoxy, C3-C6cycloalkoxy; or R5 is selected from a (═O), (═S) or (═N(R′8)) group; R6 is selected from hydrogen, amino, halogen, hydroxy, C1-C3alkyl, halogen-C1-C3alkyl, C3-C6cycloalkyl, C1-C3alkoxy, halogen-C1-C3alkoxy, C3-C6cycloalkoxy; R7 is selected from hydrogen, halogen, halogen-C1-C3alkyl; or R6 and R7 together with the carbon to which they are attached form a —C(═O)— or —C(═S)— group; R8 and R′8 are independently selected from hydrogen, hydroxy; provided R5, R6, and R7 are not all hydrogen.