Derivatives of 2-(iminomethyl)aminophenyl, methods for their preparation, compound, pharmaceutical composition

 

The invention relates to 2-(iminomethyl)aminoaniline derivative of General formula I, And where the aromatic residue of the formula Ia, R1and R2independently H, halogen, HE, linear or branched C1-C6alkyl, linear or branched C1-C6alkoxyl, R3-H, linear or branched C1-C6alkyl, or-COR4where R4-C1-C6alkyl or the residue IC, linear or branched C1-C6the five-membered alkyl or a heterocycle containing 1-4 heteroatoms selected from O, S, N, and in particular: thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched C1-C6of alkyl, C1-C6alkoxyl or halogen; X is-CO-N(R3)-X'-, -NH-CO-X'-, -CH=,-CO -, or a bond, and X' represents -(CH2)n- where n = 0-6; Y means Y'-, -Y'-NH-CO-, -CO-Y', Y'-CO-, -N(R3)-Y'-, -Y,-N(R3)-, Y'-CH2-N(R3)-CO-, -Y'-O-, -Y'-O-Y' - or a bond, and Y' is -(CH2)n- where n = 0-6; t-pyrrole, pyrrolidine, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazole and inhibition of perechisleniya lipids. 5 C. and 10 C. p. F.-ly.

Description text in facsimile form (see drawings) T T T

Claims

1. Derivatives of 2-(iminomethyl)AMINOPHENYL formula (I)in which a represents an aromatic residue, corresponding to structureswhere R1and R2independently mean a hydrogen atom, halogen atom, hydroxyl, linear or branched alkyl with 1-6 carbon atoms, linear or branched alkoxy with 1-6 atoms of the hydrocarbon; R3means a hydrogen atom, a linear or branched alkyl with 1-6 carbon atoms or the radical-R4where R4means alkyl with 1-6 carbon atoms; or

In the mean linear or branched alkyl with 1-6 carbon atoms or the five-membered heterocycle containing 1-4 heteroatoms selected from O, S, N, and in particular, thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched alkyl with 1-6 carbon atoms, alkoxyl with 1-6 and the sub>)n- where n = 0-6;
Y means Y'-, -Y'-NH-CO-, -CO-Y', Y'-CO -,- N(R3)-Y'-, -Y,-N(R3)-, Y'-CH2-N(R3)-CO-, -Y'-O-, -Y'-O-Y'-, or a bond, and Y' is - (CH2)n- where n = 0-6;
t means pyrrole, pyrrolidine, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazolidine, imidazolidinone.

2. Derivatives of formula (I) under item 1, in which a represents an aromatic residue, corresponding to the structure

where R1and R2independently denote a linear or branched alkyl with 1-6 carbon atoms or a linear or branched alkoxy with 1-6 carbon atoms;
R3means a hydrogen atom or a linear or branched alkyl with 1-6 carbon atoms;
In the means of the five-membered heterocycle containing 1-4 heteroatoms selected from O, S, N, and more specifically, thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched alkyl with 1-6 carbon atoms, alkoxyl with 1-6 carbon atoms or halogen; X is-NH-CO-X'-, -CH=, -CO -, or a bond, and X' represents -(CH2)n-, where n is irreligion, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazolidine, imidazolidinone.

3. Connection on p. 2, characterized In that means titanovyi cycle, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched alkyl with 1-6 carbon atoms, alkoxyl with 1-6 carbon atoms or halogen.

4. Derivatives of formula (I) according to one of paragraphs.1-3, representing the following connections:
N-(3,5-di-tert. -butyl-4-hydroxyphenyl)-5-[4-{imino(2-thienyl)methylamino} phenyl]-2-furancarboxaldehyde;
3-(3,5-di-tert. -butyl-4-hydroxyphenyl)-1-[4-{imino(2-thienyl)methylamino} phenyl]-2.5-imidazolidinethione;
2-(3,5-di-tert. -butyl-4-hydroxyphenyl)-3-[4-{imino(2-thienyl)methylamino} phenyl]-4-thiazolidinedione;
5-[(3,5-di-tert. -butyl-4-hydroxyphenyl)methylene]-1-methyl-3-[4-{imino(2-thienyl)methylamino}phenyl]-2,4-imidazolidinedione;
2-(S)-4-(S)-N-[4-hydroxy-3,5-bis(1,1-dimethylethyl)phenyl] -4-{ 4-[(imino(2-thienyl)methyl)amino]phenoxy}polyamideacid
N-[4-hydroxy-3,5-bis(1,1-dimethylethyl)phenyl] -2-(R, S)-{4-[(imino(2-thienyl)methyl)amino]phenyl}-4-(R)-thiazolecarboxamide dihydroiodide;
N-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] -4-(S)-{ 4-[(imino(2-thienyl)methyl)amino]phenoxy}pyrrolidin-2-(R)-carboxymethylated;
hydrochloride methyl ester 1-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-[1]-benzopyran-2-yl)carbonyl]-4-(S)-{4-[(imino(2-thienyl)methyl)amino]phenoxy}-pyrrolidin-2-(S)-carboxylic acid;
1-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-[1] -benzopyran-2-yl)carbonyl] -3-(S)-{ 4-[(imino(2-thienyl)methyl)amino]-phenoxy}pyrrolidinedione;
3-{ [(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-[1] -benzopyran-2-yl)carbonyl]amino}-1-{4-[(imino(2-thienyl)methyl)amino]phenyl}pyrrolidin;
4-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] -N-{ 4-[(imino(2-thienyl)methyl)amino]benzoyl}-N-methyl-1H-imidazol-2-methanimidamide;
N-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] -1-{ 4-[(imino(2-thienyl)methyl)amino]phenyl}-1H-pyrrol-2-carboxaldehyde;
1-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] -3-{ [4-[[imino(2-thienyl)methyl]amino]phenyl]carbonyl}-2-imidazolidinethione;
3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] -4,5-dihydro-N-{ 4-[(imino(2-thienyl)methyl)amino]phenyl]-5-isoxazolidinone;
4-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] -N-{ 4-[(imino(2-thienyl)methyl)amino]phenyl}-N-methyl-2-thiazolidinethione;
4-[3,5-bis(1,1-dimethylethyl)-4-vertility)-4-hydroxyphenyl] -4,5-dihydro-5-{ 2-{ 4-[(imino(2-thienyl)methyl)amino]phenoxy}ethyl}isoxazol;
1-{ [3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl] amino} carbonyl} -3-{ 4-[(imino(2-thienyl)methyl)amino]phenoxy}azetidinone;
1-(2-hydroxy-5-methoxybenzoyl)-3-{4-[(imino(2-thienyl)methyl)amino]phenoxy}azetidinone;
1-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-[1] -benzopyran-2-yl)carbonyl]-4-{4-[(imino(2-thienyl)methyl)amino]phenoxy}piperidinedione;
1-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-[1] -benzopyran-2-yl)carbonyl]-3-{4-[(imino(2-thienyl)methyl)amino]phenoxy}azetidinone;
or one of its salts or one of their enantiomers.

5. Derivatives of formula (I) according to one of paragraphs.1-4, representing the following connections:
3-(3,5-di-tert. -butyl-4-hydroxyphenyl)-1-[4-{imino(2-thienyl)methylamino} phenyl]-2.5-imidazolidinethione;
2-(3,5-di-tert. -butyl-4-hydroxyphenyl)-3-[4-{imino(2-thienyl)methylamino} phenyl]-4-thiazolidinedione;
5-[(3,5-di-tert. -butyl-4-hydroxyphenyl)methylene]-1-methyl-3-[4-{imino(2-thienyl)methylamino}phenyl]-2,4-imidazolidinedione;
2-(S)-4-(S)-N-[4-hydroxy-3,5-bis(1,1-dimethylethyl)phenyl] -4-{ 4-[(imino(2-thienyl)methyl)amino]phenoxy}polyamideacid
5,6-dihydro-N-{ 4-[(imino(2-thienyl)methyl)amino] phenyl} -1-(2H)-pyridinecarboxamide;
N-[4-hydroxy-3,5-bis(1,1-dimethyl)ethylphenyl] -2-{ 4-[-(Omarov.

6. Compounds of General formula (II), (III), (V), (VI) and (VII)





in which a represents an aromatic residue, corresponding to structures

where R1and R2independently mean a hydrogen atom, halogen atom, hydroxy, linear or branched alkyl with 1-6 carbon atoms, linear or branched alkoxy with 1-6 carbon atoms;
R3means a hydrogen atom, a linear or branched alkyl with 1-6 carbon atoms or a radical fulfills I TS cor4where R4means alkyl with 1-6 carbon atoms;
or

In the mean linear or branched alkyl with 1-6 carbon atoms or the five-membered heterocycle containing 1-4 heteroatoms selected from O, S, N, and in particular, thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched alkyl with 1-6 carbon atoms, alkoxyl with 1-6 carbon atoms or halogen;
X represents-CO-N(R3)-X'-, -NH-CO-X'-, -CH=, -CO -, or a bond, and X' means - (, -Y'-O-, -Y'-O-Y' - or a bond, and Y' is -(CH2)n- where n = 0-6;
t means pyrrole, pyrrolidine, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazolidine, imidazolidinone.

Gp protective means for the amine function group, preferably tsepliaeva in anhydrous acidic medium, such as, for example, tert.-butyl carbamate, trichlorethylene or trimethylsilyltriflate, or triphenylmethyl representing industrial products.

7. The method of obtaining derivatives of 2-(iminomethyl)AMINOPHENYL) of General formula (I) under item 1, characterized in that conduct the condensation is preferably in a mixture of isopropanol with dimethylformamide, at room temperature, aniline derivatives of General formula (III)

with S-alkylthiomethyl derivatives of General formula (IV)

to obtain the desired compounds of General formula (I) with compounds of General formula (I), (III) and (IV) are such that
A represents an aromatic residue, corresponding to the structures:

where R1and R2independently denote a branched alkoxy with 1-6 carbon atoms;
R3means a hydrogen atom, a linear or branched alkyl with 1-6 carbon atoms or the radical-R4where R4means alkyl with 1-6 carbon atoms;
or

In the mean linear or branched alkyl with 1-6 carbon atoms, or the five-membered heterocycle containing 1-4 heteroatoms selected from O, S, N, in particular, thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched alkyl with 1-6 carbon atoms, alkoxyl with 1-6 carbon atoms or halogen;
X represents-CO-N(R3)-X'-, -NH-CO-X'-, -CH=, -CO -, or a bond, and X' represents - (CH2)n- where n = 0-6;
Y means Y'-, -Y'-NH-CO-, -CO-Y'-, -Y'-CO-, -N(R3)-Y'-, -Y,-N(R3)-, -Y'-CH2-N(R3)-CO-, -Y'-O-, -Y'-O-Y'-, or a bond, and Y' is -(CH2)n- where n = 0-6;
t means pyrrole, pyrrolidine, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazolidine, imidazolidinone.

8. The method of obtaining derivatives of 2-(iminomethyl)AMINOPHENYL General formula (I) under item 1, a heterocycle which Het includes at least one of propanol with dimethylformamide and at room temperature, compounds of General formula (VI)

with a compound of General formula (IV)

obtaining compounds of General formula (VII)

cleavage of the protective group Gp from compounds of the above General formula (VII) to give compounds of General formula (I); and compounds of General formula (I), (IV), (VI) and (VII) are such that
A represents an aromatic residue, corresponding to structures

where R1and R2independently mean a hydrogen atom, halogen atom, hydroxyl, linear or branched alkyl with 1-6 carbon atoms, linear or branched alkoxy with 1-6 carbon atoms;
R3means a hydrogen atom, a linear or branched alkyl with 1-6 carbon atoms or the radical-R4where R4means alkyl with 1-6 carbon atoms;
or

In the mean linear or branched alkyl with 1-6 carbon atoms, or the five-membered heterocycle containing 1-4 heteroatoms selected from O, S, N, in particular, thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from lynchet-CO-N(R3)-X'-, -NH-CO-X'-, -CH=, -CO -, or a bond, and X' represents -(CH2)n- where n = 0-6;
Y means Y'-, -Y'-NH-CO-, -CO-Y', Y'-CO -,- N(R3)-Y'-, -Y,-N(R3)-, -Y'-CH2-N(R3)-CO-, -Y'-O-, -Y'-O-Y' - or a bond, and Y' is -(CH2)n- where n = 0-6;
t means pyrrole, pyrrolidine, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazolidine, imidazolidinone;
Gp protective means for the amine function group, preferably tsepliaeva in an anhydrous acid medium, such as, for example, tert.-butyl carbamate, trichlorethylene or trimethylsilyltriflate, or triphenylmethyl representing industrial products.

9. Compounds selected from the group including
N-[4-(1H-imidazol-1-yl)phenyl]-2-thiophenecarboxaldehyde;
N-[4-(3-thiazolidinone)phenyl]-2-thiophenecarboxylate;
N-[4-(1,2,3,6-tetrahydropyridine-1-yl)phenyl] -2-thiophenecarboxaldehyde;
N-[4-(1H-imidazol-1-ylmethyl)phenyl]-2-thiophenecarboxaldehyde;
N-[4-{2-(3-thiazolidin)ethyl}phenyl]-2-thiophenecarboxylate;
N-{4-[2-(1H-imidazol-1-yl)ethyl]phenyl}-2-thiophenecarboxaldehyde;
N-{ 4-[2-(1,2,3,6-the tetrahydropyridine-1 is damid;
N-(4-{ [2-thiazolidine] carbonylmethyl} phenyl)-2-thiophenecarboxaldehyde;
5,6-dihydro-N-{ 4-[(imino-(2-thienyl)-methyl)amino] phenyl}-1-(2H)-pyridinecarboxamide.

10. Connection on p. 9, representing the following connections:
N-[4-(1H-imidazol-1-yl)phenyl]-2-thiophenecarboxaldehyde;
N-[4-(1,2,3,6-tetrahydropyridine-1-yl)phenyl] -2-thiophenecarboxaldehyde;
N-{4-[2-(1H-imidazol-1-yl)ethyl]phenyl}-2-thiophenecarboxaldehyde;
N-{ 4-[2-(1,2,3,6-the tetrahydropyridine-1-yl)ethyl] phenyl} -2-thiophenecarboxaldehyde;
N-[4-(3-thiazolidinedione)phenyl]-2-thiophenecarboxylate.

11. Connection at one PM. 9 and 10, representing the N-[4-(1,2,3,6-tetrahydropyridine-1-yl)phenyl] -2-thiophenecarboxaldehyde or one of its salts.

12. Pharmaceutical composition having inhibitory activity against NO-synthase and/or lipid perechisleniya containing as active principle at least one compound of formula (I) according to one of paragraphs.1-5 or its pharmaceutically acceptable salt.

13. The compound of General formula (I) according to any one of paragraphs.1-5 or its pharmaceutically acceptable salt for a medicinal product intended for the inhibition of paracillin is Holocene medicines simultaneously possessing activity against inhibition of NO-synthase and inhibition of perechisleniya lipids.

15. The compound of General formula (I) according to any one of paragraphs.1-5 or its pharmaceutically acceptable salt to obtain a medicinal product intended for the inhibition of NO-synthase.

 

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< / BR>
where R1- H, C1-C6alkyl; phenyl, possibly substituted; biphenyl, possibly substituted; 1H, 5H - pyrido [3,2,1-ij] chinolin; phenyl WITH1-C6alkyl, optionally substituted; biphenyl WITH1-C6alkyl, optionally substituted; biphenylcarboxylic; terphenyl; naphthyl, optionally substituted; Z denotes-S-, -O-, -och2-, -N(R16), where R16- H, C1-C6alkyl, C3-C8cycloalkyl1-C6alkyl, panels1-C6alkyl, a chemical bond; X1means-CO-, -(CH2)r-CO-N(R17), where R17means H, C1-C6alkyl (where r = 0 or 1), -CH2NHSO2-, -(CH2)s-N (R18)-CO- (where R18- N, s=1-3), - CH2NHCОСН2O-, -CH2N (R19Of PINES = CH- (where R19- H, -CH2OCH2-, -CH2-N (R20)-CH2- (where R20- H, C1-C6alkyl, C1-C6alkylsulphonyl, phenylcarbinol)1-C5alkylen,2-C4albaniles, a chemical bond; X2- phenylene, optionally substituted hydroxy, theoffender, purandar, piperidinyl,< / BR>
< / BR>
< / BR>
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The invention relates to compounds of the formula I

< / BR>
in which R1denotes-C(=NH)-NH2which may be substituted once by a group-COA, -CO-[C(R6)2]n-Ar, -COOA, -HE or normal aminosidine group

< / BR>
R2denotes H, A, OR6N(R6)2, NO2CN, Hal, NHCOA, NHCOAr, NHSO2A, NHSО2Ar, COOR6, SOPS(R6)2, CONHAr, COR6, COAr, S(O)nA or S(O)nAr,

R3means And, cycloalkyl, - [C(R6)2]nAr, - [C(R6)2]n-O-Ar, -[C(R6)2]nHet or-C(R6)2=C(R6)2-Ar,

R6denotes H, a or benzyl,

X is absent or represents-CO-, -C(R6)2-, -C(R6)2-C(R6)2-, -C(R6)2-CO-, -C(R6)2-C(R6)2-CO-, -C(R6)= C(R6)-CO-, NR6CO-, -N{[CR6)2]n-COOR6} -CO - or-C(COOR6R6-C(R6)2-CO-,

Y represents-C(R6)2-, -SO2-, -CO-, -COO - or-CONR6-,

And denotes alkyl with 1-20 C-atoms, where one or two CH2-groups can be replaced by O - or S-atom or single, two - or three-fold substituted by the group And, Ah', OR6N(R6)2, NO2CN, Hal, NHCOA, NHCOAr', NHSO2A, NHSО2Ar', COOR6, CON(R6)2, CONHAr', COR6, COAr', S(O)nA or S(O)nAr is phenyl or naphthyl,

AG' refers to unsubstituted or one-, two - or three-fold substituted by a group A, OR6N(R6)2, NO2CN, Hal, NHCOA, COOR6, SOPS(R6)2, COR6or S(0)nA phenyl or naphthyl,

Het denotes a single or dual core unsubstituted or one - or multi-substituted by a group of Hal, A, Ar', COOR6, CN, N(R6)2, NO2, Ar-CONH-CH2and/or carbonyl oxygen saturated or unsaturated heterocyclic ring system containing one, two, three or four identical or different heteroatoms, such as nitrogen, oxygen or sulphur,

Hal denotes F, C1, Br or J,

n denotes 0, 1 or 2,

and their salts

The invention relates to new derivatives of kalaidjieva, fungicides, method of combating fungal diseases of crops and intermediate compounds for obtaining

The invention relates to organic chemistry, namely to new derivatives of benzoperylene
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