Tetrahydrocarbazole derivatives with improved biological action and improved solubility as ligands of G-Protein coupled receptors (GPCRs)

摘要

Disclosed is a tetrahydrocarbazole compound of the formula (I) in which: X1 is S or S+-O-, X2 and X3 are independently of one another O or geminally linked H2 (the remaining substituents are defined herein); and a physiologically tolerated salt of the compound of the formulae (I), where the salt is obtained by neutralising the bases with inorganic or organic acids or by neutralising the acids with inorganic or organic bases, where the compound of the formula (I) and its salt may be in the form of a racemate, in the form of a pure enantiomer and/or diastereomer or in the form of a mixture of these enantiomers and/or diastereomers, in the form of a tautomer, a solvate and hydrate thereof and a polymorphic form thereof. Also disclosed is a pharmaceutical composition which comprises a pharmacologically active amount of at least one of the above compounds, wherein the composition additionally comprises at least one pharmaceutically acceptable carrier, and optionally comprises at least one further pharmacologically active substance. Further disclosed is the use of a compound as defined above for producing a medicament for the treatment or prophylaxis of pathological conditions mediated by G-protein coupled receptors or of pathological conditions which can be treated by modulation of this receptor. The use of the medicament for the treatment of benign or malignant neoplastic diseases, in male fertility control, in hormone therapy, in hormone replacement therapy, for the treatment and/or control of female sub- or infertility, for controlled ovarian stimulation in in vitro fertilization, for female contraception, and for protection from side effects due to chemotherapy is additionally disclosed.