摘要 |
An acyclic or cyclic amine derivative or pharmaceutically acceptable salts thereof has the formula (I) wherein: X is -CH2CH2-, -CH=CH-, -C(OH)CH2-, -CH2C(OH)-, =C(F)CH2-, - C(F)=CH2-, -NHC(O)-, -P(O)(OH)CH2-, -CH2SO2-, -C(S)NR1-, - C(O)CH2CH(OH)-, -C(OH)CF2-, -C(O)CF2-, -CH(F)CH2-, - C(F)2CH2-, tetrazolyl or an epoxy group; A, B and R1 are independently E, optionally substituted alkyl, alkenyl or alkynyl, cycloalkyl or cycloalkenyl wherein 1 to 2 of the-CH2- groups in the alkyl, alkenyl, or alkynyl is optionally and independently replaced by -O-, - S(O)0-2-, =N-, -N= or -N(R3)- or B and R1 are independently hydrogen; E is an optionally substituted optionally saturated or aromatic monocyclic or bicyclic ring system, wherein each ring comprises 5 to 7 ring atoms independently selected from C, N, N(R3), O or S(O)0-2 and wherein no more than 4 ring atoms are selected from N, N(R3), O or S(O)0-2; J is H, methyl, ethyl or benzyl and K and K1 are independently optionally substituted alkyl, alkenyl or alkynyl, or cyclohexylmethyl, or J and K, taken together with the nitrogen and carbon atom to which they are respectively bound, form optionally substituted 5-7 membered heterocyclic ring, optionally containing up to 3 additional heteroatoms selected from N, N(R3), O, or S(O)0- 2; G, when present, is -S(O)-2-, -C(O)-, S(O)2-Y-, C(O)-Y-, - C(O)-C(O)-, or -C(O)-C(O)-Y-; Y is oxygen or N(R6); D is hydrogen or optionally substituted alkyl, alkenyl or alkynyl, cycloalkyl or cycloalkenyl optionally substituted with alkyl or alkenyl or alkynyl, alkyl-E, -alkenyl-E or alkynyl-E, or E; x is 0 or 1 and R3 and R6 are as defined in the specification; provided that when J is hydrogen or G is S(O)2, C(O)C(O), SO2-Y, C(O)-Y, or C(O)C(O)-Y and Y is O; then D is not hydrogen. The compounds are useful for stimulating neuronal regeneration or preventing neurodegeneration in a patient or in an ex vivo nerve cell.
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