RU2001101433A - β-CARBOLINE COMPOUNDS - Google Patents

Claims (1)

1. The compound of formula (I)

racemic-diastereomeric mixtures and optical isomers of said compound of formula (I), pharmaceutically acceptable salts or prodrugs thereof, or a pharmaceutically acceptable salt of said prodrug,
where ---- represents an optional bond;
X represents N or NR ⁴ , where X is N when both optional bonds are present, and X is NR ⁴ when these optional bonds are absent;
R ¹ represents H, - (CH ₂ ) _m —C (O) - (CH ₂ ) _m —Z ¹ , - (CH ₂ ) _m —Z ¹ , - (CH ₂ ) _m —OZ ^1, or (C ₀ - C ₆ } alkyl-C (O) -NH- (CH ₂ ) _m -Z ³ ;
Z ¹ represents an optionally substituted moiety selected from the group consisting of (C ₁ -C ₁₂ ) alkyl, benzo [b] thiophene, phenyl, naphthyl, benzo [b] furanyl, thiophene, isoxazolyl, indolyl,

R ² represents (C ₁ -C ₁₂ ) alkyl, (C ₀ -C ₆ ) alkyl-C (O) -OZ ⁵ ; (C ₀ -C ₆ ) alkyl-C (O) -NH- (CH ₂ ) _m -Z ³ or optionally substituted phenyl;
Z ⁵ represents H, (C ₁ -C ₁₂ ) alkyl or (CH ₂ ) _m -aryl;
Z ³ represents an amino group, (C ₁ -C ₁₂ ) alkylamino, N, N-di- (C ₁ -C ₁₂ ) -alkylamino, -NH-C (O) -O- (CH ₂ ) _m- phenyl, -NH -C (O) -O- (CH ₂ ) _m - (C ₁ -C ₆ ) alkyl or an optionally substituted moiety selected from the group consisting of imidazolyl, pyridinyl and morpholinyl, piperidinyl, piperazinyl, pyrazolidinyl, furanyl and thiophene;
R ³ represents H;
R ⁴ represents H, —C (═Y) —N (X ¹ X ² ); C (= O) X ² or X ² ;
Y represents O or S;
X ² represents - (CH ₂ ) _m —Y ¹ —X ³ ;
X ³ represents H or an optionally substituted moiety selected from (C ₁ -C ₁₂ ) alkyl, (C ₃ -C ₈ ) cycloalkyl, (C ₁ -C ₁₂ ) alkoxy, aryloxy, (C ₁ -C ₁₂ ) alkylamino, N , N-di- (C ₁ -C ₁₂ ) alkylamino, -CH-di- (C ₁ -C ₁₂ ) alkoxy or phenyl;
R ⁵ represents (C ₁ -C ₁₂ ) alkyl, - (CH ₂ ) _m -Y ¹ - (CH ₂ ) _m- phenyl- (X ¹ ) _n , (C ₃ -C ₁₂ ) cycloalkyl, - (CH ₂ ) _m -S- (C ₁ -C ₁₂ ) alkyl, (C ₁ -C ₁₂ ) -alkyl-SS- (C ₁ -C ₁₂ ) alkyl, - (CH ₂ ) _m - (C ₁ -C ₁₂ ) alkenyl or an optionally substituted moiety selected from phenyl, furanyl, thiophene, pyrrolyl, pyridinyl and

Y ¹ means O, S, NH or a bond;
R ⁶ represents H or SO ₂ phenyl;
R ⁷ represents H, alkyl optionally substituted with alkoxy or dialkylamino;
where an optionally substituted fragment or optionally substituted phenyl is optionally substituted with one or more substituents, each of which is independently selected from the group consisting of Cl, F, Br, I, CF ₃ , NO ₂ , OH, SO ₂ NH ₂ , CN, N ₃ , -OCF ₃ , (C ₁ -C ₁₂ ) alkoxy, - (CH ₂ ) _m -phenyl- (X ¹ ) _n , -NH-CO- (C ₁ -C ₆ ) alkyl, -S-phenyl- (X ¹ ) _n , -O- (CH ₂ ) _m- phenyl- (X ¹ ) _n , - (CH ₂ ) _m -C (O) -O- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -C (O) - (C ₁ -C ₆ ) alkyl, -O- (CH ₂ ) _m -NH ₂ , -O- (CH ₂ ) _m -NH- (C ₁ -C ₆ ) alkyl, -O- (CH ₂ ) _m -N-di- (C ₁ -C ₆ ) alkyl; and - (C ₀ -C ₁₂ ) alkyl- (X ¹ ) _n ; X ¹ in each case is independently selected from the group consisting of hydrogen, Cl, F, Br, I, NO ₂ , OH, -CF ₃ , -OCF ₃ , (C ₁ -C ₁₂ ) alkyl, (C ₁ -C ₁₂ ) alkoxy, -S- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -amino, - (CH ₂ ) _m -NH- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -N -di- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -phenyl and - (CH ₂ ) _m -NH- (C ₃ -C ₆ ) cycloalkyl;
m in each case independently represents 0 or an integer from 1 to 6, and
n in each case independently represents an integer from 1 to 5. 2. The compound of claim 1, wherein X is NH, R ¹ is H; R ² represents —CH (CH ₃ ) ₂ —CO — NH— (CH ₂ ) _m —Z ³ , where m in the definition of R ² is 1, 2 or 3;
Z ³ represents imidazolyl, pyridinyl, morpholino or N, N-diethylamino;
R ⁵ represents propyl, n-butyl, n-pentyl, - (CH ₂ ) -O- (CH ₂ ) phenyl, 2-nitro-3-OME-phenyl, p-tert-Bu-phenyl, m-OME-phenyl , O-OMe-phenyl, p-nitrophenyl, - (CH ₂ ) ₂ -S-Me, cyclohexyl, m-Br-phenyl, p-S-Me-phenyl, p-N, N-dimethylaminophenyl, m-methyl- phenyl or

R ⁶ represents H; and R ⁷ represents N. 3. The compound of claim 1, wherein X is NH; R ¹ represents H;
R ² represents phenyl;
R ⁵ represents propyl, n-butyl, n-pentyl, n-heptyl, isobutyl, neopentyl, cyclopropyl, cyclohexyl, - (CH ₂ ) ₂ -S-Me, phenyl, - (CH ₂ ) -O- (CH ₂ ) -phenyl, 2-nitro-3-OMe-phenyl, p-tert-Bu-phenyl, o-ОМе-phenyl, m-ОМе-phenyl, p-ОМе-phenyl, 3,4,5-tri-ОМе-phenyl , p-butoxyphenyl, 3-ethoxy-4-methoxyphenyl, o-nitrophenyl, p-nitrophenyl, p-OCF ₃ -phenyl, o-CF ₃ -phenyl, 3-F-4-OMe-phenyl, oF-phenyl, o -Br-phenyl, m-Br-phenyl, p-Br-phenyl, 2,4-di-Cl-phenyl, 3,4-di-Cl-phenyl, p- (3- (N, N-dimethylamino) - propoxy) phenyl, - (CH ₂ ) ₂ -S-Me, cyclohexyl, p- (Me-CO-NH) - phenyl, p-tert-Bu-phenyl, p-OH-phenyl, p - (- S-Me ) -phenyl, p (-S-t-Bu) phenyl, p-N, N-dimethylaminophenyl, m methylphenyl, 3-OH-4-OMe phenyl, p-phenyl phenyl,

R ⁶ represents H; and R ⁷ represents H,
4. The compound according to claim 1, in which X represents NH, R ¹ represents H; R ² is p-OMe-phenyl or p-nitro-phenyl;
R ⁵ represents n-butyl, n-pentyl, n-hexyl, isobutyl, cyclohexyl, - (CH ₂ ) ₂ -S-Me, phenyl, m-OMe-phenyl, 2-nitro-3-OMe-phenyl, p- nitrophenyl, p-tert-Bu-phenyl, p-thiomethyl-phenyl, m-Br-phenyl, 2-Ome-4-dimethylaminophenyl, p- (3- (N, N-dimethylamino) propoxy) phenyl, p-dimethylaminophenyl, 3-nitro-4-Cl-phenyl, - (CH ₂ ) -O- (CH ₂ ) phenyl or

R ⁶ represents H; and R ⁷ represents N. 5. The compound of formula (II)

its racemic-diastereomeric mixtures and optical isomers of the indicated compound of formula (II), pharmaceutically acceptable salts or prodrugs thereof or pharmaceutically acceptable salts of the indicated prodrug, where ---- is an optional bond; J ¹ represents NR ⁶ or S; J ² represents NR ¹ , O or S; X represents N or NR ⁴ , where X represents N when both optional bonds are present, and X represents NR ⁴ when optional bonds are absent; R ¹ represents H, - (CH ₂ ) _m —C (O) - (CH ₂ ) _m —Z ¹ , - (CH ₂ ) _m —Z ¹ , - (CH ₂ ) _m —OZ ^1, or (C ₀ - C ₆ ) alkyl-C (O) -NH- (CH ₂ ) _m -Z ³ ; Z ¹ represents an optionally substituted moiety selected from (C ₁ -C ₁₂ ) alkyl, benzo [b] thiophene, phenyl, naphthyl, benzo [b] furanyl, thiophene, isoxazolyl, indolyl,

R ² represents (C ₁ -C ₁₂ ) alkyl, (C ₀ -C ₆ ) alkyl-C (O) -OZ ⁵ ; (C ₀ -C ₆ ) alkyl-C (O) -NH- (CH ₂ ) _m -Z ³ or optionally substituted phenyl;
Z ⁵ represents H, (C ₁ -C ₁₂ ) alkyl or (CH ₂ ) _m -aryl;
Z ³ represents amino, (C ₁ -C ₁₂ ) alkylamino, N, N-di- (C ₁ -C ₁₂ ) -alkylamino, -NH-C (O) -O- (CH ₂ ) _m- phenyl, -NH -C (O) -O- (CH ₂ ) _m - (C ₁ -C ₆ ) alkyl or an optionally substituted moiety selected from the group consisting of phenyl, imidazolyl, pyridinyl and morpholinyl, piperidinyl, piperazinyl, pyrazolidinyl, furanyl and thiophene ;
R ³ represents H, (C ₁ -C ₁ ) alkyl or optionally substituted phenyl;
R ⁴ represents H, —C (═Y) —N (X ¹ X ² ); C (= O) X ² or X ² ;
Y represents O or S;
X ² represents H or - (CH ₂ ) _m —Y ¹ —X ³ ;
X ³ represents H or an optionally substituted moiety selected from the group consisting of (C ₁ -C ₁₂ ) alkyl, (C ₃ -C ₈ ) cycloalkyl, (C ₁ -C ₁₂ ) alkoxy, aryloxy, (C ₁ -C ₁₂ ) alkylamino, N, N-di- (C ₁ -C ₁₂ ) alkylamino, -CH-di- (C ₁ -C ₁₂ ) alkoxy or phenyl;
R ⁵ and R ^{8 are} each independently selected from the group consisting of H, (C ₁ -C ₁₂ ) alkyl, - (CH ₂ ) _m -Y ¹ - (CH ₂ ) _m- phenyl- (X ¹ ) _n , (C ₃ -C ₁₂ ) -cycloalkyl, (C ₃ -C ₁₂ ) cycloalkenyl, - (CH ₂ ) _m -S- (C ₁ -C ₁₂ ) -alkyl, (C ₁ -C ₁₂ ) alkyl-SS- (C ₁ -C ₁₂ ) alkyl, - (CH ₂ ) _m - (C ₁ -C ₁₂ ) alkenyl, and an optionally substituted moiety selected from the group consisting of phenyl, furanyl, thiophene, pyrrolyl, pyridinyl and

provided that R ⁵ and R ^{8 are} both not simultaneously H;
or R ⁵ and R ⁸ taken together with the carbon atom to which they are attached form

Spiro (C ₄ -C ₁₂ ) cycloalkyl,

or

;
Y ¹ represents O, S, NH or a bond;
A represents a bond, —CO—, —C (O) O—, —C (O) NH—, —C (S) NH—; or -SO ₂ -;
B represents a bond or - (CH ₂ ) _q -, where q represents an integer from 1 to 6;
J ³ represents H, (C ₁ -C ₆ ) alkyl, optionally substituted phenyl, optionally substituted heteroaryl or N (R ⁹ R ¹⁰ ), where R ⁹ and R ^{10 are} each independently selected from the group consisting of (C ₁ -C ₆ ) alkyl and optionally substituted phenyl, or R ⁹ and R ¹⁰ are taken together with the nitrogen atom to which they are bonded to form a ring having 5-8 members, including the nitrogen atom to which R ⁹ and R ¹⁰ are bonded, where one of the members the ring may optionally be an oxygen atom or NR ¹¹ where R ¹¹ is (C ₁ -C ₆ ) alkyl, —C (O) - (C ₁ -C ₆ ) alkyl, —C (O) -N (V ¹ V ² ), -C (S) -N (V ¹ V ² ) or an optionally substituted pheny l- (C ₀ -C ₆ ) -alkyl-, where V ¹ and V ² each independently represents H, (C ₁ -C ₆ ) alkyl or optionally substituted phenyl- (C ₀ -C ₆ ) alkyl;
R ⁶ represents H or SO ₂ phenyl;
R ⁷ represents H, Cl, F, Br, I, CF ₃ , NO ₂ , OH, SO ₂ NH ₂ , CN, N ₃ , —OCF ₃ , (C ₁ -C ₁₂ ) alkoxy, - (CH ₂ ) _m -phenyl- (X ¹ ) _n , -NH-CO- (C ₁ -C ₆ ) alkyl, -S- (C ₁ -C ₁₂ ) alkyl, -S-phenyl- (X ¹ ) _n , -O- ( CH ₂ ) _m - phenyl (X ¹ ) _n , - (CH ₂ ) _m -C (O) -O- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -C (O) - (C ₁ -C ₆ ) -alkyl, -O- (CH ₂ ) _m -NH ₂ , -O- (CH ₂ ) _m -NH- (C ₁ -C ₆ ) alkyl, -O- (CH ₂ ) _m -N- di - ((C ₁ -C ₆ ) alkyl) and - (C ₀ -C ₁₂ ) alkyl- (X ¹ ) _n ; where an optionally substituted moiety or optionally substituted phenyl is optionally substituted with one or more substituents, each independently selected from the group consisting of Cl, F, Br, I, CF ₃ , NO ₂ , OH, SO ₂ NH ₂ , CN, N ₃ , -OCF ₃ , (C ₁ -C ₁₂ ) alkoxy, - (CH ₂ ) _m -phenyl- (X ¹ ) _n , -NH-CO- (C ₁ -C ₆ ) alkyl, -S- (C ₁ -C ₁₂ ) alkyl, -S-phenyl- (X ¹ ) _n , -O- (CH ₂ ) _m- phenyl- (X ¹ ) n,
- (CH ₂ ) _m -C (O) -O- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -C (O) - (C ₁ -C ₆ ) alkyl, -O- (CH ₂ ) _m -NH ₂ ,
-O- (CH ₂ ) _m -NH- (C ₁ -C ₆ ) alkyl, -O- (CH ₂ ) _m -N-di - ((C ₁ -C ₆ ) alkyl) and - (C ₀ -C ₁₂ ) alkyl- (X ¹ ) _n ;
X ¹ in each case is independently selected from the group consisting of hydrogen, Cl, F, Br, I, NO ₂ , OH, -CF ₃ , -OCF ₃ , (C ₁ -C ₁₂ ) alkyl, (C ₁ -C ₁₂ ) alkoxy, -S- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -amino, - (CH ₂ ) _m -NH- (C ₁ -C ₆ ) alkyl, - (CH ₂ ) _m -N -di - ((C ₁ -C ₆ ) alkyl), - (CH ₂ ) _m -phenyl and - (CH ₂ ) _m -NH- (C ₃ -C ₆ ) cycloalkyl;
m in each case independently represents 0 or an integer from 1 to 6; and
n in each case independently represents an integer from 1 to 5. 6. The compound according to claim 5, having the formula (IIa):

in which R ³ represents H or methyl;
R ⁴ represents H or methyl;
R ⁵ represents H, methyl, ethyl, butyl, pentyl or hexyl;
R ⁸ represents ethyl, butyl, pentyl, hexyl or cyclohexyl;
or, R ⁵ and R ⁸ are taken together with the carbon atom to which they are bonded to form spirocyclohexyl, spirocycloheptyl, spiroadamantyl,

where A represents a bond or —C (O) O—; B represents a bond, - (CH ₂ ) - or - (CH ₂ ) ₂ -;
J ³ represents H or phenyl; and
R ⁷ represents H, Me, F, Cl, OH, —O-methyl or —O — CH ₂ phenyl. 7. The compound according to claim 6, in which:
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R-configuration, or its hydrochloride salt;
R ³ represents methyl, R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is in the R-configuration;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R-configuration or its hydrochloride salt;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-O-CH ₂ phenyl, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R-configuration, or its hydrochloride salt;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R configuration;
R ³ and R ⁷ each represents hydrogen, R ⁴ represents methyl, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is in the R configuration;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 7-fluoro, R ⁵ and R ⁸ each represents n-pentyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-hexyl, and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ represents hydrogen, R ⁸ represents hexyl in the S-configuration, and imidazolyl is in the R-configuration, or its fumarate salt;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is in the R-configuration, or its fumarate salt;
R ³ , R ⁴ , R ⁷ each represents hydrogen, R ⁵ , and R ⁸ together represent

and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is in the S-configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents ethyl, and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-pentyl, and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ^{7 are} each hydrogen, R ⁵ is methyl, and R ⁸ is cyclohexyl, and imidazolyl is present in the R configuration;
R ³ and R ⁴ each represents hydrogen, R ³ represents 6-methyl, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture in S- and R-configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 7-fluoro, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-methoxy, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-hydroxy, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-fluoro, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S- and R-configurations, or its hydrochloride mixture;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 8-methyl, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-methyl, R ⁵ and R ⁸ each represents n-pentyl, and imidazolyl represents a racemic mixture of S and R configurations, or
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-chloro, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is a racemic mixture of S and R configurations. 8. The compound of claim 7, wherein said compounds are selected from the group consisting of compounds in which
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ represents hydrogen, and R ⁸ represents hexyl in the S-configuration, and imidazolyl is in the R-configuration, or its fumarate salt;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is in the R-configuration, or its fumarate salt;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ and R ⁸ together represent

and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl is in the S-configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents ethyl, and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represents hydrogen, R ⁵ and R ⁸ each represents n-pentyl, and imidazolyl is in the R configuration;
R ³ , R ⁴ and R ⁷ each represent hydrogen, R ⁵ represents methyl, and R ⁸ represents cyclohexyl, and imidazolyl is in the R configuration;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-methyl, and R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 7-fluoro, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-methoxy, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-hydroxy, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-fluoro, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S- and R-configurations, or its hydrochloride salt;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents, 8-methyl, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations;
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-methyl, R ⁵ and R ⁸ each represents n-pentyl, and imidazolyl represents a racemic mixture of S and R configurations and
R ³ and R ⁴ each represents hydrogen, R ⁷ represents 6-chloro, R ⁵ and R ⁸ each represents n-butyl, and imidazolyl represents a racemic mixture of S and R configurations.  9. A pharmaceutical composition comprising a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.  10. A pharmaceutical composition for use as a local anesthetic, comprising the compound of claim 1 or 5, or a pharmaceutically acceptable salt thereof and, optionally, a pharmaceutically acceptable carrier.  11. A method for achieving an agonistic effect in one or more somatostatin subtype receptors in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  12. A method of achieving an antagonistic effect in one or more somatostatin subtype receptors in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  13. A method of binding one or more somatostatin subtype receptors in an individual in need thereof, which comprises administering to this individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  14. A method of treating acromegaly, restenosis, Crohn’s disease, systemic sclerosis, external and internal pseudocystosis and pancreatic ascites, apudoma, nezidoblastosis, hyperinsulinism, gastrinoma, Zollinger-Ellison syndrome, diarrhea, diarrhea associated with AIDS, diarrhea associated with x scleroderma, intestinal irritation syndrome, pancreatitis, blockage or withdrawal of the small intestine, gastroesophageal reflux, gastro-duodenal reflux, Cushing's syndrome, gonadotropinomas, hyperparathyroidism, pain Graves’s illness, diabetic neuropathy, Paget’s disease, polycystic ovary, cancer, cancer cachexia, hypotension, hypotension that occurs after eating, panic attacks, GH-secreting adenomas and TSH-secreting adenomas in an individual in need, which involves the introduction of the specified individual compounds according to claim 1 or 5, or a pharmaceutically acceptable salt thereof.  15. A method for the treatment of diabetes mellitus, hyperlipidemia, insulin resistance, syndrome X, angiopathy, proliferative retinopathy, the phenomenon of "morning dawn", nephropathy; peptic ulcers, skin-intestinal and skin-pancreatic fistulas, dumping syndrome, watery stool syndrome, acute or chronic pancreatitis and tumors that secrete gastrointestinal hormones, angiogenesis, inflammatory diseases, chronic rejection of allografts, disorders caused by angioplasty, bleeding with vessels and gastrointestinal bleeding in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutical thereof Ki acceptable salt.  16. A method of inhibiting helicobacter pylori proliferation in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  17. A method of blocking sodium channels in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  18. A method of alleviating neuropathic pain in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  19. A method of treating any pathologies, disorders or clinical conditions, the etiological factor of which is the release of glutamate, in an individual in need thereof, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  20. The method according to p. 19, in which the pathology, disorder or clinical condition relates to the group consisting of mental disorders, hormonal disorders, brain damage caused by metabolic factors, sulfite oxidase deficiency, hepatic encephalopathy associated with liver failure, vomiting, muscle cramping, tinnitus, pain and illness caused by drug abuse, and withdrawal.  21. A method for treating any pathology associated with damage to neurons in an individual in need of treatment, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  22. The method according to p. 21, in which the pathology relates to a group consisting of Alzheimer's disease, Huntington's disease, Parkinson's disease, virus-induced neurodegeneration (including HIV), amyotrophic lateral sclerosis (ALS), supranuclear palsy, oligopontomolecular atrophy (ORSA) and environmental diseases, exogenous neurotoxins.  23. A method of treating arrhythmia in an individual in need of treatment, which comprises administering to said individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.  24. A method of treating epilepsy in an individual in need of treatment, which comprises administering to the individual a compound according to claim 1 or 5 or a pharmaceutically acceptable salt thereof.