ANTI-CONVULSION AMINO ACIDS FOR THE TREATMENT OF OBSESSIVE-COMPULSIVE NEUROSIS.

摘要

Use of a compound of the following formula (I) for the preparation of a medicament for the treatment of obsessive-compulsive neurosis in a mammal: or a pharmaceutically acceptable salt thereof, in which Ar is aryl that is unsubstituted or substituted with at least one electron donor group or an electron extractor group; R1 is alkyl; R3 is alkyl, alkenyl, alkynyl, aryl-alkyl, aryl, halo, heterocyclic, heterocyclic-alkyl, alkyl-heterocyclic, cycloalkyl, cycloalkyl-alkyl, each of which is not substituted or substituted with at least one extracting group of electrons or an electron donor group, or is ZY; Z is O, S, S (O) a, NR4 or PR4; Y is hydrogen, alkyl, aryl, aryl-alkyl, alkenyl, alkynyl, halo, heterocyclic, heterocyclic-alkyl, alkyl-heterocyclic-cycloalkyl, cycloalkyl-alkyl, and Y is unsubstituted or substituted with an electron donor group or a electron extractor group, or 30 ZY, taken together, is NNR4NR5R7, NR4OR5, ONR4R7, OPR4R5, PR4OR5, SNR4R7, NR4SR7, SPR4R5, PR4SR7, NR4PR5R6, PR4NR5R7, NR4C (= O) OR5, SC5 OR5, SC5 OR5, SC5 OR5, SC5 OR5, SC5 OR5, SC5 OR5, SC5 OR5, SC5 (= O) R5 or NR4C (= O) R5, R4, R5 and R6 are, independently, hydrogen, alkyl, aryl, aryl-alkyl, alkenyl, or alkynyl, each being unsubstituted or substituted with an extractor group of electrons or an electron donor group; R7 is hydrogen, alkyl, aryl, aryl-alkyl, alkenyl or alkynyl, each of which may be unsubstituted or substituted with an electron donor group or an electron extractor group, or R7 is COOR8 or COR8, R8 is hydrogen, alkyl or aryl-alkyl, the aryl or alkyl group being optionally substituted with an electron extraction group or an electron donor group; and 45 a is 1-3 in which alkyl contains 1-6 carbon atoms, alkenyl contains 2-6 carbon atoms, alkynyl contains 2-6 carbon atoms, cycloalkyl contains from 3 to 18 5 annular carbon atoms and up to a total of 25 carbon atoms, halo is fluoro, chloro, bromo or iodo, heterocyclic is selected from the group consisting of furyl, thienyl, pyrazolyl, pyrrolyl, imidazolyl, indolyl, thiazolyl, oxazolyl, isothiazolyl, isoxazolyl, piperidyl, pyrrolinyl , piperazinyl, quinolyl, triazolyl, tetrazolyl, isoquinolyl, benzofuryl, benzothienyl, morpholinyl, benzoxazolyl, tetrahydrofuryl, pyranyl, indazolyl, purinyl, 10 indolinyl, pyrazolindinyl, imidazolinyl, imadazolindinyl, pyrrolidinyl, furazanyl, N-methylindolyl, methylfuryl, pyridazinyl, pyrimidinyl, methylpyrrolyl, pyrazinyl, pyridyl, epoxy, aziridino, oxetanyl, azetidinyl and the N-oxides of the nitrogen-containing heterocyclics listed hereinabove having a Annular nitrogen atom, 15 and electron donor and electron extractor groups are halo, nitro, alkanoyl, formyl, arylalkanoyl, aryloyl, carboxyl, carbalkoxy, carboxamido, cyano, aryl, trifluoromethyl, aryloxy, sulfonyl, sulfoxide, heterocyclic, guanidine , quaternary ammonium, alkenyl, alkynyl, sulphonium, hydroxy, alkoxy, alkyl, amino, alkylamino, dialkylamino, amino-alkyl, mercapto, alkylthio, or alkyldithium salts. twenty