RU99106804A - DERIVATIVES OF PIPERAZINE WITH ELECTORAL ACTION IN RELATION TO D4 RECEPTOR - Google Patents

Claims (7)

1. Piperazine derivatives of the formula I

in which R ¹ denotes unsubstituted or singly substituted with Ph or 2- or 3-thienyl pyridyl or phenyl;
R ² is Ph 'or Het;
Ph and Ph 'are, respectively, independently of each other phenyl, and both residues, respectively, can be unsubstituted or substituted once, twice or three times by F, Cl, Br, I, OH, OA, A, CF ₃ , NO ₂ , CN, COA, CONH ₂ , CONHA, CONA ₂ or 2-or 3-thienyl;
Het is a saturated, partially or fully unsaturated mono- or bicyclic heterocyclic residue with 5-10 cycle members, where 1 or 2 N-atoms and / or 1 or 2 O-atoms can be represented, and the heterocyclic residue can be single or F is substituted by F, Cl, Br, I, OA, CF ₃ , A or NO ₂ , and
And denotes alkyl with 1-6 C-atoms,
and their physiologically acceptable salts. 2. The compound according to claim 1, selected from the group including (a) 1- (2-pyrimidinyl) -4- (3- (3-thienylbenzyl) piperazine, (b) 1- [5- (4-fluorophenyl) pyrid -3-ylmethyl] -4- (2-pyrimidyl) piperazine, (c) 4- [4- (3-biphenylylmethyl) -1-piperazinyl] benzonitrile, (g) 1- (4-chlorophenyl) -4- [5 - (4-fluorophenyl) -3-pyridylmethyl) piperazine, (e) 1- (3'-fluoro-3-biphenylylmethyl) -4- (2-pyrimidinyl) piperazine, (e) 2- [4- (5- ( 3-thienyl) -3-pyridylmethyl) -1-piperazinyl] pyrimidine,
and their salts. 3. The method of obtaining piperazine derivatives of formula 1 according to claim 1 and their salts, characterized in that the compound of formula II

in which R ² has the indicated value,
subjected to interaction with the compound of the formula III

in which L represents Cl, Br, I, OH, O-CO-A, O-CO-Ph, O-SO ₂ -Ar, where Ar denotes phenyl or tolyl, and A denotes alkyl, or another reactive esterified with OH- a group or an easily nucleophilically substitutable leaving group, and in which R ¹ has the indicated value,
or that compound of formula IV

in which R ² has the indicated value,
subjected to interaction with the compound of the formula V

in which X ¹ and X ² can have the same or different meaning or denote by Cl, Br, I, OH or a reactive functionally modified OH group, and R ¹ has the indicated value,
or that compound of formula VI

in which R ² , X ¹ and X ² have the indicated meanings,
subjected to interaction with the compound of the formula VII

in which R ¹ has the indicated value,
or that any compound corresponding to formula I, but containing instead of one or more hydrogen atoms one or more reducible groups and / or one or more additional C-C-bonds and / or C-N-bonds, is treated with a reducing agent, or that any compound corresponding to formula I, but containing instead of one or several hydrogen atoms one or more solvilizable groups is treated with a solvolizer, and / or, if necessary, the residue R ¹ and / or R ^{2 is} converted into another residue R ¹ and / or R ² due to the fact that, for example, the OA group is cleaved to form the OH group and / or CN-, COOH-, COOA-group is derived and / or that, for example, primary or secondary N-atom is alkylated and / or that the resulting base or acid is of formula I by treatment with acid or base is converted into one of their salts.  4. A method for preparing pharmaceutical compositions, characterized in that an appropriate dosage form is prepared from a compound of formula I and / or from one of its physiologically acceptable salts, together with at least one solid, liquid or semi-liquid carrier or auxiliary substance.  5. Pharmaceutical composition, characterized in that it contains at least one compound of general formula I and / or one of its physiologically acceptable salts.  6. The use of compounds of the formula I according to claim 1 or their physiologically acceptable salts for the manufacture of a medicament.  7. The use of compounds of the formula I according to claim 1 or their physiologically acceptable salts for the control of diseases.