abstract |
Pyrazolopyrimidines of formula (I) including the stereolsomers and the pharmaceutically acceptable acid addition salt forms, where R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy, or C1-6alkylthio; R3 is hydrogen, C1-6 alkyl or C1-6 alkylsulfonyl, C1-6 alkylsulfoxy and C1-6alkylthio; R4 is hydrogen, mono or di (C3-6 cycloalkyl) methyl, C3-6 cycloalkyl C3-6 alkenyl hydroxyalkyl C1-6, C1-6alkylcarbonyloxy C1-6alkyl, or C1-6alkyloxy C1-6alkyl; R5 is alkyl. C1-8, mono or di (C3-6 cycloalkyl) methyl Ar CH2, C1-6 alkyloxy C1-6 alkyl, hydroxy C1-6 alkyl, C3-6 alkenyl, and thienylmethyl, furanylmethyl, C1-6 alkylthio C1-6 alkyl, morpholinyl mono or di (C1-6alkyl) aminoC1-6alkyl, di (C1-6alkyl) amino with C1-6alkylcarbonyl C1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula -ALK-O-CO-Ar1; or R4 and R5 together with the dehydrogen atom to which they are attached can form a pyrrolidinyl, piperidinyl group with homopiperidinyl or morpholinyl, having antagonistic properties of the CRF receptor, a process for its preparation, pharmaceutical compositions containing said compounds as useful active ingredients to treat disorders related to CRF hypersecretion, such as depression, anxiety, substance abuse, a procedure for its preparation, intermediates thereof and a procedure for its preparation. |