FIELD: organic chemistry, pharmacology, pharmacy.
SUBSTANCE: invention relates to β-carboline compounds of the general formula (I) or their racemic and diastereomeric mixture and optical isomers, pharmaceutically acceptable salts wherein: ----- represents optional bond; X represents nitrogen atom (N) or N-R4 wherein X means nitrogen atom (N) when both optional bonds are present, and X means NR4 when indicated bonds are absent; R1 represents hydrogen atom (H); R2 represents (C1-C12)-alkyl, (C0-C)-alkyl-C(O)-NH-(CH2)mZ3 or phenyl optionally substituted with (C1-C6)-alkyl, (C1-C6)-alkoxy-group or nitro-group; Z3 represents (C6H6)-CH-(diphenylmethylene), N,N-di-(C1-C12)-alkylamino-group, imidazolyl, pyridinyl, morpholinyl, pyrrolidinyl, piperidinyl substituted with benzyl group, pyrazolidinyl substituted with (C1-C6)-alkyl, piperazinyl substituted with (C1-C6)-alkyl; R3 represents hydrogen atom (H); R4 represents hydrogen atom (H) or -C(=Y)-N(X1X2) wherein Y represents oxygen atom (O); X2 represents -(CH2)m-Y1-X3 wherein X3 represents unsubstituted phenyl; R5 represents (C1-C12)-alkyl, -(CH2)m-Y1-(CH2)m-phenyl-(X1)n, (C3-C12)-cycloalkyl, -(CH2)m-S-(C1-C12)-alkyl, (C1-C12)-alkyl-S-S-(C1-C12)-alkyl, -(CH2)m-(C2-C12)-alkenyl, unsubstituted phenyl or phenyl substituted with (C1-C6)-alkyl, (C1-C6)-alkoxy-group, hydroxy-group, halogen atom, nitro-group, phenyl, (C1-C6)-alkylthio-group, amino-group, cyano-group, -O-CF3, di-(C1-C6)-alkylamino-(C1-C6)-alkoxy-group, (C1-C6)-alkylcarbonylamino-group or the group: the group that is unsubstituted or substituted with nitro-group; Y1 means -O or a bond; R6 and R7 represent hydrogen atom (H); X1 means hydrogen atom; m represents a whole number from 0 to 2; n represents a whole number from 0 to 5; R8 means (C1-C12)-alkyl; or R5 andR8 taken in common with carbon atom © to which they are joined from spiro-(C4-C12)-cycloalkyl or fragment wherein A means a bond, -CO-, -C(O)O-, -C(O)NH- or -C(S)NH; B means a bond or -(CH2)q wherein q means a whole number 1-6; J1 means N-R6 or sulfur atom (S); J2 means NR1, oxygen atom (O) or sulfur atom (S); J3 means H1(C1-C)-alkyl, phenyl possibly substituted with (C1-C6)-alkyl or CF3. Invention relates also to a pharmaceutical composition containing these compounds and methods for binding, attainment of agonistic/antagonistic effect with one or some receptors of somatostatin subtype.
EFFECT: valuable pharmacological properties of compounds.
12 cl, 4 tbl, 1504 ex
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Authors
Dates
2004-08-10—Published
1999-06-08—Filed