| 摘要 |
The present invention relates to new pyrazole derivatives possessing an amide group substituted with an amino acid or one of its derivatives at position 3 and variously substituted in positions 1, 2, 4 or 5 of the pyrazole ring, to a process for preparing these and to pharmaceutical compositions containing the said pyrazole derivatives as an active ingredient. The novel compounds are capable of binding to neurotensin receptor and are capable of beng useful in pathological states associated with dysfunction of the dopaminergic systems. The novel compounds comprise a 3-amidopyrazole of formula I: <See fig. I> in which: X is hydrogen; X' is a C3-C7 cycloalkyl group; or X and X', together with the carbon atom to which they are linked, form a C3-C12 cycloalkyl group optionally substituted by a C1-C3 alkyl; R1 represents: a phenyl group substituted by Ra, R'a and R"a wherein Ra, R'a and R"a each independently represent a hydrogen atom, a halogen atom, a hydroxyl, a linear or branched C1-C4 alkyl group, a C1-C4 alkoxy group, a trifluoromethyl group, a trifluoromethoxy group, a nitro group, a carboxyl group or an amino group; a tetrahydronaphthyl group; a naphthyl group substituted by Ra, R'a and R"a as defined above; or a quinolyl or isoquinolyl group optionally substituted by Ra, R'a and R"a as defined above; R represents hydrogen or linear or branched C1-C4 alkyl; n represents 0, 1, 2 or 3; Z represents a hydroxyl group; a C1-C6 alkoxy group; an oxygen atom substituted with a carboxylic acid-protecting group, wherein the carboxylic acid-protecting group is selected from the group consisting of tert-butyl, benzyl, benzyl substituted with a halogen atom, C1-C6 alkyl, trifluoromethyl, trifluoromethoxy or carboxyl; an amino group; or a nitrogen atom substituted with a carboxyalkyl in which the alkyl is a linear or branched C1-C6 group; RIV represents a hydrogen atom, a halogen atom or a C1-C6 alkyl; RV represents: a phenyl group substituted by R5, R'5 and R"5, where R5, R'5 and R"5 each independently represent a hydrogen atom, a halogen atom, a linear or branched C1-C4 alkyl, a hydroxyl, a C1-C4 alkoxy, a nitro, a trifluoromethyl, a trifluoromethoxy, a cyano, an amino, a carboxyl, a C1-C4 carboxyalkyl or a phenyl; a naphthyl group unsubstituted or substituted with a C1-C4 alkyl; a pyridyl group; a styryl group unsubstituted or substituted with a C1-C4 alkyl; or alternatively RIV and RV considered together represent: a group <IMG> in which the phenyl group substitutes the pyrazole at position 5 and the group -(CH2)i - in which i = 1 to 3 substitutes the pyrazole at position 4; W1 W2 and W3 substitute the benzene ring and independently represent hydrogen, a halogen or a hydroxyl group; or one of its possible salts with organic or inorganic acids or with inorganic or organic bases.
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