| abstract |
REFERS TO 1-HETEROARYL-PYRROLIDINE, 1-HETEROARYL-PIPERIDINE, 1-HETEROARYL-HOMOPIPERIDINE DERIVATIVES OF FORMULA I WHERE: X IS O, S, NH, N (C1-C6 ALKYL); R1, R2, R3, R4 ARE H, OH, OCO-C1-C6 ALKYL, AMONG OTHERS; A IS C3-C5 ALKYLENE; D IS O, S; E IS O, S, NH, N-C1-C6 ALKYL, CR11R12; G IS C1-C14 ALKYL, C2-C14 ALKYL OPTIONALLY SUBSTITUTED WITH HALOGEN, NR5R6; R5 AND R6 ARE H, C1-C6 ALKYL, TOGETHER WITH N FORM A HETEROCYCLE OF 4-7 MEMBERS, WHICH OPTIONALLY CONTAINS NR7, O, SOp; R7 IS H, C1-C6 ALKYL, COR8, SO2NR9R10, AMONG OTHERS; R8 IS C2-C6 ALKENYL, ARYL, C1-C6 ALKYL; R9 AND R10 ARE H, C2-C6 ALKENYL, C3-C7 CYCLOALKYL, C1-C6 ALKYL; R11 AND R12 ARE H, ARYL, C2-C8 ALKYL, C1-C8 ALKYL; p IS 0-2. THE COMPOUND IS NOT METHYL-1- (5-CHLORO-2-BENZOXAZOLIL) PROLIN. A PREFERRED COMPOUND IS (2S) -1- (1,3-BENZOXAZOLE-2-IL) -N2-2 - [(CIS) -2,6-DIMETHYL-1-PIPERIDINYLETHYL) -2-PIPERIDINECARBOXAMIDE; AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR THE PREPARATION AND TO INTERMEDIATE COMPOUNDS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION THAT ALSO INCLUDES ANOTHER NEUROTROPHIC AGENT. COMPOUND I IS AN INHIBITOR OF THE CIS-TRANS PROLIL ISOMERASE (ROTAMASE) ACTIVITY OF THE IMMUNOPHYLLIN FKBP OF PREFERENCE FKBP-12 AND FKBP-52 SO IT MAY BE USEFUL FOR THE TREATMENT OF NEURONAL DEGENERATION, STIMULATION |