Substituted bicyclic compounds, the source and intermediate products for their preparation and pharmaceutical composition based on them

 

The invention relates to new substituted bicyclic compounds of General formula I: R1-A-D-E-G-L-R2(I) where R1means naphthyl or a residue of the formula:where a = 1 or 2, R3means H, C2-C6alkenyl, C1-C6alkyl or C1-C6acyl and all of the above ring systems and the remains unsubstituted or substituted optionally gemenele, one or more, same or different substituents selected from the group: halogen, carboxyl, hydroxy, phenyl, C1-C6alkoxy, a group of the formula -(CO)b-NR4R5where b = 0 or 1, R4and R5the same or different and independently of one another denote hydrogen, phenyl, C1-C6acyl, C4-C7cyclacel, benzene C1-C6alkyl and the other dialkylamino, where alkyl with 1-6 carbon atoms, a and E are the same and different and mean a connection or C1-C4alkylene, D is-O - or a residue of formula-S(O)c- or-N(R9)-, where c = 1, 2; R9means H, C1-C6alkyl, L is-O-, -NH-,and other G on the, aderrasi up to 3 heteroatoms from the series of sulfur, nitrogen and/or oxygen, which may be substituted by one or more identical or different substituents, R2means6-C10aryl or a 5-7 membered saturated or aromatic heterocycle containing up to 3 heteroatoms from the series of sulfur, nitrogen and/or oxygen, unsubstituted or substituted by one or more identical or different substituents with the exception of compounds of the formula I, where R1means of naphthas-1-yl, unsubstituted or substituted in position 3 C1, C1-C4the alkyl and in position 4 chlorine or phenyl; a and E indicate the relationship, D is-O-; G means 1,4-phenyl, unsubstituted or substituted C1-C4by alkyl; L is-O-; R2means of CH3and except for the connection m-bis-(1-naphthyloxy)benzene. Described intermediate compounds of formula II: R1-A-D-E-G-M-H, where M stands for-O-, -N(R32)-, where R32means H, C1-C4alkyl; and the intermediate compounds of formula XVI: R48-SO2-(CH2)h-U-(CH2); -CR49R50-CF2-R51where R48- Cl; R49R50identical and denote H, F; R51means F; U represents a simple bond, h = 1, 2; ; i = 1; provided that when h = 1, then R is political composition, which has the properties of a receptor antagonist cannabinoid. 4 C. and 6 C. p. F.-ly, 37 PL.

Description text in facsimile form (see graphic part).

Claims

1. Substituted bicyclic compounds of General formula (I) R1- A - D - E - G - L - R2(I)
in which R1represents a naphthyl or a residue of the formula




where a = 1 or 2;
R3means hydrogen, alkenyl with 2-6 carbon atoms, alkyl with 1-6 carbon atoms or acyl with 1 to 6 carbon atoms,
while all of the above ring systems and residues, unsubstituted or substituted optionally gemenele one or more identical or different substituents, which are selected from the group comprising halogen, carboxyl, hydroxy, phenyl, alkoxy with 1-6 carbon atoms, alkoxycarbonyl, where alkoxy with 1-6 carbon atoms, alkyl with 1-8 carbon atoms, which in turn may be substituted with halogen, alkylsulfonate with 1-6 carbon atoms, azide, amine, monoalkylamines with 1-6 carbon atoms, dialkylamino, where Ali R5the same or different and independently of one another denote hydrogen, phenyl, acyl with 1 to 6 carbon atoms, cyclacel, in which the cyclic part with 4-7 carbon atoms, benzoyl or alkyl with 1-6 carbon atoms, unsubstituted or substituted amino group, monoalkylamines with 1-6 carbon atoms, dialkylamino, where alkyl with 1-6 carbon atoms, or R4and R5together with the nitrogen atom form a 5 - or 6-membered saturated a heterocycle, which optionally may contain one or more additional(s) heteroatom(s) from the series S, O and/or one or more residue(s) of the formula-NR8where R8denotes hydrogen, alkyl with 1-6 carbon atoms or acyl with 1 to 6 carbon atoms, and a group of the formula-NR6-SO2-R7where R6means hydrogen, phenyl, alkyl with 1-6 carbon atoms or acyl with 1 to 6 carbon atoms, R7means phenyl or alkyl with 1-6 carbon atoms,
A and E are identical or different and represent a link or alkylene with 1-4 carbon atoms;
D represents an oxygen atom or a residue of formula-S(O)c- or-N(R9)-, where = 0, 1, or 2, R9denotes hydrogen, alkyl with 1-6 carbon atoms or acyl with 1 to 6 carbon atoms;
G is a twice 3 heteroatoms from the series of sulfur (S), nitrogen (N) and/or oxygen (O), unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising hydroxy, trifluoromethyl, carboxyl, halogen, alkyl with 1-6 carbon atoms, hydroxyalkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, alkoxycarbonyl, where alkoxy with 1-6 carbon atoms, and groups of the formula
-CO-O-(CH2)d-NR10R11, -NR12-SO2-R13, -(CH2)e-(CO)f-NR14R15or16where d = 1, 2, 3, or 4, e and f are identical or different and denote the number 0 or 1, R10and R11have the above values of R4and R5and the same with or different, R12has the above value of R6and the same with or different, R13has the above value of R7and the same with or different, R14and R15have the above values of R4and R5and the same with or different, or, independently of one another, represent a residue of the formula -(CH2)g-NR17R18where
g = 1, 2, 3 or 4, R17and R18have the above values of R4and R5and the same with or different, R16means aryl with 6-10 atoms "https://img.russianpatents.com/img_data/58/587727.gif">






when this binding residue with G is to the left (from the left),
where R19, R20, R21, R22, R23, R24, R25, R26and R27the same or different and denote hydrogen or alkyl with 1-4 carbon atoms, or R19means the residue of the formula-SO2R2,
R2represents aryl with 6-10 carbon atoms, or a 5-7 membered saturated or aromatic heterocycle containing up to 3 heteroatoms from the series S, N and/or O, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising halogen, trifluoromethyl, nitro, amino and alkyl with 1-6 carbon atoms, or represents a residue of the formula

or morpholine, or cycloalkyl with 3-8 carbon atoms, or alkyl with 1-12 carbon atoms, alkenyl with 2-12 carbon atoms or quinil with 2-12 carbon atoms, unsubstituted or substituted by one or more, same or different and 1 to 6 carbon atoms, perforamce with 1-6 carbon atoms, partially fluorinated alkoxy with 1-6 carbon atoms, a residue of the formula

NR28R29,
where R28and R29have the above values of R4and R5and the same with or different,
phenyl, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising halogen, nitro, hydroxy, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms and a group of formula-NR30R31,
where R30and R31the same or different and denote hydrogen or alkyl with 1-6 carbon atoms, or acyl with 1 to 6 carbon atoms, and 5-6 membered aromatic heterocycle containing up to 3 heteroatoms from the series S, N and/or O, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising halogen, nitro, hydroxy, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms and a group of formula-NR30R31where R30and R31(as)defined above,
or L and R2together represent a residue of the formula

and their salts, excluding the compounds of the formula (the mi of carbon in position 4 chlorine or phenyl, A and E indicate the relationship, D is oxygen, G denotes 1,4-phenyl, unsubstituted or substituted by alkyl with 1 to 4 carbon atoms, L is oxygen, and R2means methyl, and except for the connection m-bis-(1-naphthyloxy)benzene.

2. Substituted bicyclic compounds of the formula (I) under item 1, where R1represents a naphthyl or a residue of the formula




where a = 1 or 2
R3means hydrogen, alkenyl with 2-4 carbon atoms, alkyl with 1-4 carbon atoms or acyl with 1 to 4 carbon atoms,
while all of the above ring systems and the remains unsubstituted or substituted, optionally gemenele, one or more, same or different substituents which are selected from the group comprising halogen, carboxyl, hydroxyl, phenyl, alkoxy with 1-4 carbon atoms, alkoxycarbonyl, where alkoxy with 1-5 carbon atoms, alkyl with 1-6 carbon atoms, which, in turn, can be substituted with halogen, alkylsulfonate with 1-4 carbon atoms, azide, amino, monoalkylamines with 1-4 carbon atoms, dialkylamino, where alkyl with 1-4 carbon atoms, or hydroxy, gropep from each other, denote hydrogen, phenyl, acyl with 1 to 4 carbon atoms, cyclacel, in which the cyclic part with 4-7 carbon atoms, benzoyl or alkyl with 1-4 carbon atoms, unsubstituted or substituted amine, monoalkylamines with 1-4 carbon atoms, dialkylamino, where alkyl with 1-4 carbon atoms, or R4and R5together with the nitrogen atom form morpholino, piperidino or N-methylpiperazine ring, and a group of formula-NR6-SO2-R7where R6means hydrogen, phenyl, alkyl with 1-4 carbon atoms or acyl with 1 to 4 carbon atoms and R7means phenyl or alkyl with 1-5 carbon atoms,
A and E are identical or different and represent a link or alkylene with 1-4 carbon atoms, D represents an oxygen atom or a residue of formula-S(O)c- or-NR9- where = 0, 1, or 2, R9means hydrogen or alkyl with 1-4 carbon atoms or acyl with 1 to 4 carbon atoms, G is a double-linked phenyl, naphthyl, pyrimidyl, pyridazinyl or pyridyl, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising hydroxy, trifluoromethyl, carboxyl, halogen, alkyl with 1-4 carbon atoms, hydroxyalkyl with 1-4 carbon atoms, ALSN2)d-NR10R11, -NR12-SO2R13, -(CH2)e-(CO)f-NR14R15and-OR16where d = 1, 2, 3, or 4, e and f are identical or different and denote the number 0 or 1, R10and R11have the above values of R4and R5and the same with or different, R12has the above value of R6and the same with or different, R13has the above value of R7and the same with or different, R14and R15have the above value of R4and R5and the same with or different or, independently from each other are a residue of the formula -(CH2)g-NR17R18where g = 1, 2, or 3, R17and R18have the above value of R10and R11and the same with or different, R16means phenyl or naphthyl,
L is a residue of formula-O-, -NH-,

-N(R20) SO-







when this binding residue on G is left (by the>the same or different and denote hydrogen or alkyl with 1-3 carbon atoms, or R19means the residue of the formula-SO2R2, R2represents phenyl, naphthyl, pyridyl, furyl, thienyl, or pyrimidyl, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising halogen, amino, trifluoromethyl, nitro and alkyl with 1-4 carbon atoms, or represents a residue of the formula

or morpholine, or cyclopropyl, cyclohexyl or cyclopentyl, or represents alkyl with 1-10 carbon atoms, alkenyl with 2-10 carbon atoms or quinil with 2-10 carbon atoms, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising halogen, trifluoromethyl, hydroxy, azido, alkoxy with 1-4 carbon atoms, perforamce with 1-5 carbon atoms, partially fluorinated alkoxy with 1-4 carbon atoms, a residue of the formula

and-NR28R29where R28and R29have the above values of R4and R5and the same with or different,
phenyl, unsubstituted or samisen is halogen, nitro, hydroxy, alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms and a group of the formula-NR30R31where R30and R31the same or different and denote hydrogen or alkyl with 1-4 carbon atoms or acyl with 1 to 4 carbon atoms, pyridyl and pyrimidyl, optionally substituted by one or more, same or different substituents which are selected from the group comprising halogen, nitro, hydroxy, alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms and a group of the formula-NR30R31where R30and R31have the above values,
or L and R2together represent a residue of the formula

and their salts, excluding the compounds of formula (I) in which R1means of naphthas-1-yl, unsubstituted or substituted in position 3 by chlorine or alkyl with 1-4 carbon atoms in position 4 chlorine or phenyl, and E indicate the relationship, D is oxygen, G denotes 1,4-phenyl, unsubstituted or substituted by alkyl with 1 to 4 carbon atoms, L is oxygen, and R2means methyl, and except for the connection n-bis-(1-naphthyloxy)benzene.

3. Substituted bicyclic compounds of the formula (I) under item 1, where R1represents naphthyl, or f">




where
a = 1 or 2;
R3means hydrogen, alkenyl with 2-3 carbon atoms, alkyl with 1-3 carbon atoms or acyl with 1 to 3 carbon atoms,
while all of the above ring systems and the remains unsubstituted or substituted, if necessary, gemenele, one or more, same or different substituents which are selected from the group comprising chlorine, fluorine, carboxyl, hydroxyl, phenyl, alkoxy with 1-3 carbon atoms, alkoxycarbonyl, where alkoxy with 1-4 carbon atoms, alkyl with 1-4 carbon atoms, which, in turn, can be substituted by chlorine or hydroxy, a group of the formula -(CO)b-NR4R5where b = 0 or 1, R4and R5the same or different and, independently of one another, mean hydrogen, acyl with 1 to 3 carbon atoms, cyclacel, in which the cyclic part with 4-6 carbon atoms, benzoyl or alkyl with 1-3 carbon atoms, unsubstituted or substituted amine, monoalkylamines with 1-3 carbon atoms, dialkylamino, where alkyl with 1-3 carbon atoms, or R4and R5together with the nitrogen atom form morpholino, piperidino sludge with 1-3 carbon atoms or acyl with 1 to 3 carbon atoms, R7means phenyl or alkyl with 1-4 carbon atoms,
A and E are identical or different and represent a bond or alkyl with 1-3 carbon atoms, D represents an oxygen atom or a residue of formula-S(O)c- or-NR9- where = 0, 1, or 2, R9means hydrogen or alkyl with 1-3 carbon atoms or acyl with 1 to 3 carbon atoms, G is a double-linked phenyl, naphthyl, pyrimidyl, pyridazinyl or pyridyl, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising hydroxy, trifluoromethyl, carboxyl, fluorine, chlorine, bromine, alkyl with 1-3 carbon atoms, hydroxyalkyl with 1-3 carbon atoms, alkoxy with 1-3 carbon atoms, alkoxycarbonyl, where alkoxy with 1-3 carbon atoms, and groups of the formulae-CO-O-(CH2)d-NR10R11, -NR12-SO2R13, (CH2)e-(CO)f-NR14R15, -CH2HE-OR16where d = 1, 2, or 3, e and f are identical or different and denote the number 0 or 1, R10and R11mean hydrogen or methyl,
R12means hydrogen, R13means alkyl with 1-4 carbon atoms,
R14and R15have the above values of R4and R6and the same with sup> mean hydrogen or methyl, or R14and R15together with the nitrogen atom form a residue of the formula

R16means phenyl or naphthyl,
L is a residue of formula-O-, -NH-,

-N(R20)-SO







when this binding residue on G is to the left (from the left),
where R19, R20, R21, R22, R23, R24, R25, R26and R27the same or different and mean hydrogen, methyl or ethyl, or R19means the residue of the formula-SO2R2,
R2represents a phenyl, furyl or pyridyl, unsubstituted or substituted by one or more, same or different substituents which are selected from the group comprising fluorine, chlorine, bromine or trifluoromethyl, or represents a residue of the formula

or morpholine, or cyclopentyl or cyclohexyl, or represents Alky the military one or more, identical or different substituents chosen from the group containing: fluorine, chlorine, bromine, trifluoromethyl, hydroxy, azido, alkoxy with 1-3 carbon atoms, perforamce with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, substituted triptorelin group, a residue of the formula

and NR28R29,
where R28and R29mean hydrogen or methyl, phenyl, pyridyl and pyrimidyl optionally substituted by one or more, same or different substituents which are selected from the group comprising fluorine, chlorine, bromine, nitro, hydroxy, alkyl with 1-3 carbon atoms, alkoxy with 1-3 carbon atoms and a group of the formula-NR30-R31where R30and R31the same or different and denote methyl or methylcarbamyl,
or L and R together represent a residue of the formula

and their salts, excluding the compounds of formula (I) in which R1means of naphthas-1-yl, unsubstituted or substituted in position 3 by chlorine or alkyl with 1-4 carbon atoms in position 4 chlorine or phenyl, and E indicate the relationship, D is oxygen, G denotes 1,4-phenyl, unsubstituted or substituted by alkyl with 1 to 4 carbon atoms, L denotes illecebra the compounds of formula (I) under item 1, where R1represents a naphthyl or a residue of the formula



where a = 1 or 2
while all of the above ring systems and the remains unsubstituted or substituted optionally gemenele, from one to three times, equal or different substituents which are selected from the group comprising halogen, carboxyl, hydroxy, alkoxy with 1-6 carbon atoms, alkoxycarbonyl, where alkoxy with 1-6 carbon atoms, alkyl with 1-8 carbon atoms, which, in turn, can be substituted with halogen or hydroxy, a group of formula -(CO)b-NR4R5where b = 0 or 1, R4and R5the same or different and denote hydrogen, phenyl or alkyl with 1-6 carbon atoms, and a group of formula-NR6-SO2-R7where R6means hydrogen, phenyl or alkyl with 1-6 carbon atoms, R7means phenyl or alkyl with 1-6 carbon atoms,
A and E are identical or different and represent a link or alkylene with 1-4 carbon atoms, D represents an oxygen atom or a residue of formula-S(O)c- or-NH-, where = 0, 1, or 2, G is a double-linked aryl with 6-10 carbon atoms or twice include ewenny from one to three times, equal or different substituents, which are selected from the group comprising hydroxy, carboxyl, halogen, alkyl with 1-6 carbon atoms, hydroxyalkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, alkoxycarbonyl, where alkoxy with 1-6 carbon atoms, and groups of the formula
-CO-O-(CH2)d-NR10R11, -NR12-SO2R13and-CO-NR14R15,
where d = 1,2,3 or 4, R10and R11have the above values of R4and R5and the same with or different, R12has the above value of R6and the same with or different, R13has the above value of R7and the same with or different, R14and R15have the above values of R4and R5and the same with or different, or together with the nitrogen atom form a 5-6-membered saturated, a heterocycle, which in some cases may contain an additional heteroatom from the series S and O or a group of the formula-NH-,
L represents a residue of the formula

N(R20) SO-




when this binding residue on G is left,
where R19, R20, RR2represents phenyl, unsubstituted or substituted with halogen, triptorelin group, nitro, amino or alkyl with 1-6 carbon atoms, R2represents a residue of the formula

or morpholine, or represents a perfluoroalkyl containing up to 12 fluorine atoms, or represents alkyl with 1-12 carbon atoms or quinil with 2-12 carbon atoms, unsubstituted or substituted with halogen, triptorelin group, hydroxy, azido or a residue of the formula

or NR28R29,
where R28and R29have the above values of R4and R5and the same with or different,
and/or optionally substituted by phenyl or 5-6-membered aromatic heterocycle containing up to 3 heteroatoms from the series S, N and/or O, which, in turn, can be substituted up to 2 times in an identical or different manner by the following substituents: halogen, nitro, hydroxy, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms or a group of the formula-NR30R31where R30and R31the same or different and mean hydrogen, alkyl with 1-6 carbon atoms or acyl with 1 to 6 carbon atoms,
L and R2together predse the compounds of formula (I) under item 1, where R1is a naphthas-1-yl, unsubstituted or substituted by alkyl with 1-6 carbon atoms, which contains substituents: hydroxy, acylamino with 1-6 carbon atoms, amino or alkoxy with 1-6 atoms operatingin-4-yl, substituted by hydroxyalkyl with 1-6 carbon atoms, a residue of the formula



where R3alkyl with 1-6 carbon atoms,
A and E represents a bond, D represents an oxygen atom, G represents a 1,3-phenylene, 1,4-phenylene or 2,5-peridinin, unsubstituted or substituted with halogen, L is a residue of formula-NH-SO2- or-O-SO2-, and R2represents alkyl with 1-6 carbon atoms, unsubstituted or substituted by chlorine, triptorelin group, a residue of the formula-O-CH2-CF3or phenyl, or pyridium, which, in turn, can be substituted by bromine or chlorine, and salt.

6. Substituted bicyclic compounds on p. 1, selected from the group including (see graphic part).

7. Compounds of General formula (II)
R1-A-D-E-G-M-H (II)
in which R1means the rest of the formula

8. Compounds of General formula (II) under item 7, in which R1means indan-4-yl, substituted hydroxyalkyl group with 1 to 6 carbon atoms or a residue of the formula



where R3means alkyl with 1 to 6 carbon atoms,
A, D, E and G have the values listed in paragraph 5, and M has the meaning specified in paragraph 7.

9. Fluorinated alkylsulfonate General formula (XVI)
R48-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51(XVI)
where R48means chlorine;
R49, R50identical and denote hydrogen or fluorine;
R51means fluorine;
U represents a simple bond;
h = 1 or 2;
i = 1,
provided that if h = 1, R49and R50mean hydrogen, and if h = 2, R49and R50mean fluoride.

10. Farmaceuti, at least one pharmaceutical acceptable carrier or excipient, characterized in that it as the active substance contains at least one compound of General formula (I) according to one of paragraphs.1-6 in the amount of from 0.5 to 90 wt.%.

Priority items 1-3 and 5-10 from 17.09.1997.

21.02.1997 under item 4.

 

Same patents:

The invention relates to the derivatives of aminophenylamino formula I

< / BR>
where R is phenyl, substituted C1-C6by alkyl; R1represents hydrogen; X represents -(CH2)3-Y, cyclopropyl or tetrahydro-2-oxo-3-furoyl; Y represents chlorine, bromine or hydroxy,

or their acid additive salts

The invention relates to alkyl substituted cyclic amines of the formula I, where X and Y are in position 5, 6 or 7, where (i) n = 1, X represents (CH2)mCONR4R5, (CH2)mNR4CONR5, (CH2)mNHSO2R3(where m = 0 or 1, except that when m = 0, then Y cannot be hydrogen and Y is hydrogen or or6; (ii) n = 0 or 1, then X and Y are in the 0-position relative to each other and together form a: a) -C(O)NR10C(O)-, b) -C(O)NR4(CH2)xNR10C(O)- (where x = 0 or 1); (C) -CH2NR10C(O)-; d) -(CH2)NR10C(O) -, (e) -CH2C(O)NR10, g) -N(R3)-C(O)-O-, j) -CH2N(R8)CH2-; (iii) n = 0, and Y represents OR9then X is (CH2)mCONR4R5, (CH2)mNHCOR3(where m = 0 or 1); R1and R2represent, independently, WITH1-C8-alkyl, R3is1-C8-alkyl, aryl; R4and R5represent, independently, H, C1-C8-alkyl, C1-C6-alkylaryl or aryl; R6is1-C8-alkyl, R8is1-C8-alkyl, SO2R4(provided that R4is not hydrogen); R10is H, C is phenyl, possibly replaced by stands, nitro, chlorine, fluorine, bromine, amino, CN, carboxamido, acetyl; or represents thiophenyl, isoxazolyl, imidazolyl

The invention relates to analogs of 2-aminoindane General formula I, where R1and R2independently represent hydrogen, C1-C8alkyl; X is CH2R3or NHSO2R4; Y represents hydrogen, NHSO2R4, SO2(Ph); R3is NHSO2R4,

SO2R4, CONR1R2; R4represents C1-C8alkyl, phenyl or phenyl, substituted by-CN or-CF3; and their pharmaceutically acceptable salts, active receptor Dopamine D3

The invention relates to a new method of obtaining sulfur-containing imidazole derivatives of the formula I

R4-C6H4-C6H4-CH2NC4R, R2R3,

characterized in that the compound of formula (A)

Hal-C6H4-C6H4R'4< / BR>
enter into reaction with the oxidizing agent to obtain a compound of the formula (B)

CHO-C6H4-C6H4-R41,

which is then injected into the reaction with the compound of the formula (II)

H2N-CH(CN)-R31,

where possible functional groups can be protected to obtain a compound of formula (C)

R31-CH(CN)-NH-CH2-C6H4-C6H4-R41,

which enter into reaction with the compound of the formula (III)

R11-CO-Hal

to obtain the compounds of formula (D)

R31-CH(CN)-N(COR1CH2-C6H4C6H4-R41,

which undergoes the reactions proceed on the CN radical with a reagent able to enter the substituent R21where possible functional groups can be protected to obtain a compound of formula (E)


,

after which the compound of formula (E) and the compound of formula (L) is subjected to cyclization reaction to obtain compounds of formula (I)

The invention relates to compounds belonging to the group consisting of compounds of the General formula [I] or their optical isomers, or suitable for pharmacological use of salts

The invention relates to an improved process for the preparation of foramerican sulfonic acids, which find wide application as biologically active compounds and as intermediate products for organic synthesis, in particular to obtain foramerican perfluorinated sulfonic acids by electrochemical fluorination

The invention relates to an improved process for the preparation of triftoratsetofenona, the original product for the synthesis of derivatives triftoratsetata used in fine organic synthesis, pharmaceuticals, fungicides, extractants, catalysts

The invention relates to a new reagent for obtaining oxasulfuron fluorine-containing organic compounds, consisting of percarbonates acid of the formula EA - CF2- COOH, where EA represents an electron-withdrawing atom or group, at least partially converted into a salt with an organic or mineral cation and an aprotic polar solvent, and the amount of released protons of these components, including their impurities is at most half of the original molar concentration percarbonates acid

The invention relates to the field of technology for organofluorine compounds, specifically to obtain salts of triftoratsetata that are used in the synthesis of triftoratsetata and its derivatives

The invention relates to the field of the Navy, namely, diamines, specifically to a new connection - bis-(3-amino-5-phenoxy)phenyl ether of hydroquinone of the formula:

< / BR>
and polyimides (PI) on the basis of the General formula:

< / BR>
where

< / BR>
These PI can most effectively be used as a molding of thermoplastics

The invention relates to the field of medicine and related antidepressant based on amitriptyline

The invention relates to new biologically active compounds, namely spiroheterocyclic heterocyclic compounds of the formula I

< / BR>
where n is 0 or 1;

m is 0 or 1;

p is 0;

X represents oxygen or sulfur;

Y represents CH, N or NO;

W represents oxygen or H2;

And represents N or C(R2);

G represents N or C(R3);

D represents N or C(R4)

provided that not more than one of A, G and D represents nitrogen, but at least one of Y, a, G, and D represents nitrogen or NO;

R1represents hydrogen or C1-C4-alkyl;

R2, R3and R4are independently hydrogen, halogen, C1-C4-alkyl, C2-C4alkenyl,2-C4-quinil, aryl, heteroaryl, including five - or six-membered aromatic ring with 1 or 2 nitrogen atoms, as well as furyl or morpholyl, HE OS1-C4-alkyl, CO2R1, -CN, -NO2, -NR5R6or R2and R3or R3and R4accordingly, together with part a and G or G and D southwest a hydrogen, WITH1-C4-alkyl, C(O)R7C(O)OTHER8WITH(O)OR9, SO2R10, -NR5R6, (CH3)3Si and phenyl, or may together represent (CH2)jQ(CH2)kwhere Q represents a bond; j is 2 and k is 0 to 2;

R7, R8, R9, R10and R11are independently C1-C4-alkyl, NH2, aryl or its enantiomer,

and their pharmaceutically acceptable salts, and methods for their preparation, intermediate compounds and pharmaceutical compositions, which has an activating effect against nicotine7-acetylcholine receptors and can be used for the treatment and prevention of psychotic disorders and disorders of the type of lower intellectual

-converting enzyme)" target="_blank">

The invention relates to novel ortho-sulfonamidophenylhydrazine heteroaryl hydroxamic acids of the formula

< / BR>
where W and X are both carbon, T is nitrogen, U represents CR1where R1represents hydrogen, or alkyl containing 1-8 carbon atoms, R represents-N(CH2R5)-SO2Z, Q represents -(C=O)-NHOH, with

< / BR>
is a benzene ring, or is a heteroaryl ring of 5 to 6 atoms in the cycle, which may contain 0-2 heteroatoms selected from nitrogen, oxygen and sulfur, in addition to the heteroatom of nitrogen, denoted as W, where benzene or heteroaryl ring may optionally contain one or two substituent R1where permissible; Z is phenyl, which is optionally substituted by phenyl, alkyl with 1-8 carbon atoms, or a group OR2; R1represents halogen, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, perfluoroalkyl from 1 to 4 carbon atoms, phenyl, optionally substituted by 1-2 groups OR2group-NO2group -(CH2)nZ, where Z is a phenyl which allows an alkyl with 1-8 carbon atoms, phenyl, optionally substituted with halogen, or heteroaryl radical containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; R5represents hydrogen, alkyl with 1-8 carbon atoms, phenyl, or heteroaryl containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; or their pharmaceutically acceptable salts
The invention relates to medicine and can be used to obtain drugs is got with drugs
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