Nr3b1 nuclear receptor binding 3-substituted pyrazoles

A method for prevention or treatment of a NR3B1 receptor protein or NR3B1 receptor protein homologue mediated disease or condition in a mammal comprising administration of a therapeutically effective amount of a compound according to formula (1), or pharmaceutical acceptable salts or solvates thereof,

• wherein:
• R1 is phenyl, substituted phenyl, C5 to C6 heteroaryl, C5 to C6 substituted heteroaryl, napthyl or substituted napthyl,
• R2 is H, C1 to C8 alkyl, C1 to C7 acyl, C1 to C7 substituted acyl, C1 to C8 substituted alkyl, C7 to C12 alkylphenyl, C7 to C12 substituted phenylalkyl, C3 to C8 cycloalkyl, C3 to C8 substituted cycloalkyl, C5 to C6 heteroaryl, or [C5 to C6]-heteroaryl-(C1 to C6)-alkyl, and
• R3 is H, C1 to C8 alkl, C1 to C8 substituted alkyl, C7 to C12 alkylphenyl, C7 to C12 substituted phenylalkyl, halogen, C1 to C8 alkoxy, furanyl, substituted furanyl, thiazyl, substituted thiazyl, carboxy, ester, amide or C1 to C8 aminoacyl
• wherein the prevention or treatment is directly or indirectly accomplished through the binding of said compound to the NR3B1 receptor protein or to the NR3B1 receptor protein homologue.

A method for

• i. regulating physiologies that are influenced by estrogenic response pathways in a mammal comprising modulating the activity of the NR3B1 receptor;
• ii. treating in a mammal a disease which is directly or indirectly affected by estrogen levels,
• iii. treating cancer, osteoporosis, obesity, lipid disorders or a cardiovascular disorder or influencing fertility and reproductive health in a mammal;
• and/or
• iv. modulating the expression of a gene directly or indirectly controlled by NR3B1 in tissues of a mammal,
• wherein said method comprises administering to a mammal in need of such regulation, treatment and/or modulation an effective amount of a compound according to formula (1), or pharmaceutical acceptable salts or solvates thereof,
• wherein:
• R1 is phenyl, substituted phenyl, C5 to C6 heteroaryl, C5 to C6 substituted heteroaryl, napthyl or substituted napthyl,
• R2 is H, C1 to C8 alkyl, C1 to C7 acyl, C1 to C7 substituted acyl, C1 to C8 substituted alkyl, C7 to C12 alkylphenyl, C7 to C12 substituted phenylalkyl, C3 to C8 cycloalkyl, C3 to C8 substituted cycloalkyl, C5 to C6 heteroaryl, or [C5 to C6]-heteroaryl-(C1 to C6)-alkyl, and
• R3 is H, C1 to C8 alkyl, C1 to C8 substituted alkyl, C7 to C12 alkylphenyl, C7 to C12 substituted phenylalkyl, halogen, C1 to C8 alkoxy, furanyl, substituted furanyl, thiazyl, substituted thiazyl, carboxy, ester, amide or C1 to C8 aminoacyl.

A pharmaceutical composition comprising a compound according to formula (1), or pharmaceutical acceptable salts or solvates thereof,

• wherein:
• R1 is phenyl, substituted phenyl, C5 to C6 heteroaryl, C5 to C6 substituted heteroaryl, napthyl or substituted napthyl,
• R2 is H, C1 to C8 alkyl, C1 to C7 acyl, C1 to C7 substituted acyl, C1 to C8 substituted alkyl, C7 to C12 alkylphenyl, C7 to C12 substituted phenylalkyl, C3 to C8 cycloalkyl, C3 to C8 substituted cycloalkyl, C5 to C6 heteroaryl, or [C5 to C6]-heteroaryl-(C1 to C6)-alkyl, and
• R3 is H, C1 to C8 alkyl, C1 to C8 substituted alkyl, C7 to C12 alkylphenyl, C7 to C12 substituted phenylalkyl, halogen, C1 to C8 alkoxy, furanyl, substituted furanyl, thiazyl, substituted thiazyl, carboxy, ester, amide or C1 to C8 aminoacyl;
• together with a pharmaceutical carrier.