Imidazolidinedione, the pharmaceutical composition based on them, the method of stimulation of cytokine biosynthesis and intermediate substances

 

The invention relates to new imidazolidine formulas (I) and (II) in which a is a =N-CR=CR-CR=, =CR-N=CR-CR=, =CR-CR=N=CR or = CR-CR= CR-N= ; B represents-NR-C(R)2-C(R)2-C(R)2C(R)2-NR-C(R)2-C(R)2, -C(R)2-C(R)2-NR-C(R)2or C(R)2-C(R)2-C(R)2-NR, where R is hydrogen, R1is hydrogen, unsubstituted or substituted C1-20-alkyl, C1-20-alkylene-NR3-Q-X-R4where Q represents-CO-or-SO2-, X is a simple bond, -O - or-NR3and R4- aryl, heteroaryl, heterocyclyl or1-20-alkyl or C2-20alkenyl. Other values radicals are presented in the claims. Compounds of formula (I) and (II) stimulate the biosynthesis of cytokines, such as interferon and tumor necrosis factor, and can be used in medicine. The invention also relates to pharmaceutical compositions and intermediate compounds. 10 C. 10 C.p. f-crystals, 5 PL.

Description text in facsimile form (see graphic part)and

Claims

1. The compound of the formula I

where a represents =N-the seal or substituted by one or more substituents, selected from the group consisting of aryl; -O-C1-20of alkyl; -O-(C1-20alkyl)0-1-aryl; -N(R3)2; -IT; -C1-20alkylene-NR3-Q-X-R4where Q represents-CO - or-SO2-; X is a simple bond, -O - or-NR3; R4- aryl, heteroaryl, heterocyclyl or-C1-20-alkyl or C2-20alkenyl, unsubstituted or substituted by one or more substituents selected from the group consisting of aryl; heteroaryl; heterocyclyl; -O-C1-20of alkyl; -O-(C1-20alkyl)0-1-aryl; -C1-20alkoxycarbonyl; -S(O)0-2-(C1-20alkyl)0-1-heteroaryl; -N(R3)2; -NR3-CO-O-C1-20of alkyl; the carbonyl group; halogen; -NO2; -HE;

or R4representing

where Y is-N - or-CR-;

R2selected from the group consisting of hydrogen; -C1-10of alkyl; -C1-10alkyl-O-C1-10-alkyl; -C1-10of alkyl, substituted aryl,

each R3independently selected from the group consisting of hydrogen and C1-10of alkyl;

each R represents hydrogen;

or its pharmaceutically acceptable salt.

2. Connection on p. 1, wherein R1selected from the group consisting of C1-6

4. Connection on p. 1, wherein R2selected from the group consisting of C1-6the alkyl and alkoxyalkyl with unbranched chain, in which CNS component and the alkyl component, each independently one from the other, contains 1 to 4 carbon atoms.

5. Connection on p. 1, wherein R2selected from the group consisting of methyl, n-butyl, benzyl, ethoxymethyl.

6. Connection on p. 1, wherein R1represents-C1-20alkyl-NR3-Q-X-R4.

7. Connection on p. 6, wherein R4represents a

8. Connection on p. 1, characterized in that a represents =CH-CH=CH-N=.

9. The compound of formula II

where In represents-NR-C(R)2-C(R)2(C)R2-; -C(R)2-NR-C(R)2-C(R)2-; -C(R)2-C(R)2-NR-C(R)2- or-C(R)2-C(R)2-C(R)2-NR-;

R1selected from the group consisting of hydrogen; -C1-20the alkyl unsubstituted or substituted by one or more substituents selected from the group consisting of aryl; -O-C1-20of alkyl; -O-(C1-20alkyl)0-1-aryl; -N(R33-; R4- aryl, heterocyclyl or-C1-20alkyl or C2-20alkenyl, unsubstituted or substituted by one or more substituents selected from the group consisting of aryl; heterocyclyl; -O-C1-20of alkyl; -O-(C1-20alkyl)0-1-aryl; -C1-20alkoxycarbonyl; -N(R3)2; -NR3-CO-O-C1-20of alkyl; the carbonyl group; halogen; -NO2; -HE;

or R4representing

where Y is-N - or-CR-;

R2selected from the group consisting of hydrogen; -C1-10of alkyl; -C1-10alkyl-O-C1-10-alkyl; -C1-10of alkyl, substituted aryl;

each R3independently selected from the group consisting of hydrogen and C1-10of alkyl;

each R represents hydrogen;

or its pharmaceutically acceptable salt.

10. Connection on p. 9, wherein R1selected from the group consisting of C1-6the alkyl and C1-6hydroxyalkyl.

11. Connection on p. 10, wherein R1selected from the group consisting of n-butyl, 2-hydroxy-2-methylpropyl and 2-methylpropyl.

12. Connection on p. 9, wherein R2selected from the group consisting of methyl, n-butyl, benzyl, toxemia pharmaceutically effective amount of the compounds under item 1 or 9 and a pharmaceutically acceptable carrier.

14. The method of stimulation of cytokine biosynthesis in an animal's body, which consists in introducing into the animal an effective amount of the compounds under item 1 or 9.

15. The connection formulas

where a represents =N-CR=CR-CR=; =CR-N=CR-CR=; =CR-CR=N CR= or =CR-CR=CR-N=;

R1selected from the group consisting of hydrogen and-C1-20of alkyl;

R2selected from the group consisting of hydrogen and-C1-10of alkyl;

and each R represents hydrogen;

or its pharmaceutically acceptable salt.

16. The compound of the formula:

R1selected from the group consisting of hydrogen; -C1-20the alkyl, unsubstituted or substituted by one or more substituents selected from the group consisting of aryl; -O-C1-20of alkyl; -O-(C1-20alkyl)0-1-aryl; -HE; and-NR3-CO-O-C1-20of alkyl;

R2selected from the group consisting of hydrogen; -C1-10of alkyl; -C1-10alkyl-O-C1-10-alkyl and-C1-10of alkyl, substituted aryl, and each R and R3represents hydrogen;

or a pharmaceutically acceptable salt.

17. The connection formulas

where R1selected from the group consisting of videostamil from aryl; -O-C1-20of alkyl; -O-(C1-20alkyl)0-1-aryl; -HE; and-NR3-CO-O-C1-20of alkyl;

R2selected from the group consisting of hydrogen; -C1-10of alkyl; -C1-10alkyl-O-C1-10-alkyl and-C1-10of alkyl, substituted - aryl;

each R and R3represent hydrogen;

or a pharmaceutically acceptable salt.

18. The connection formulas

where a represents =N-CR=CR-CR=; =CR-N=CR-CR=; =CR-CR=N CR= or =CR-CR=CR-N=;

R7is a HE, halogen or other1, R1selected from the group consisting of hydrogen and-C1-20of alkyl;

R8represents H, NO2or NH2;

and each R represents hydrogen;

or its pharmaceutically acceptable salt.

19. The connection formulas

where a represents =N-CR=CR-CR=; =CR-N=CR-CR=; =CR-CR=N CR or =CR-CR=CR-N=, where R represents hydrogen;

R9represents hydrogen or C1-10alkyl.

20. The connection formulas

where R1selected from the group consisting of-C1-20the alkyl, unsubstituted or substituted by one or more substituents selected from the group consisting of aryl; -O-C1-20of alkyl; -O-(battle hydrogen, Q represents-CO-; X is a simple bond or-O-; R4represents a C1-20alkyl, each R and R3represent hydrogen;

R10represents-NO2or-NH2;

or its pharmaceutically acceptable salt.

 

Same patents:
The invention relates to a method by which you can lower cost and with greater purity to obtain alkaloids from plants

The invention relates to tetracyclic analogues of camptothecins formula (I), where R1, R2, R3, R4, R5and R10such as defined in the claims

The invention relates to novel analogues of camptothecin, in particular to the compounds corresponding to the following formulas (I) and (II), as well as their racemic or enantiomeric forms or combinations of these forms, where the substituents have the values

The invention relates to the field of medicine

The invention relates to new alkaloids of the formula I

< / BR>
present in various parts of Mappia foetida, and their pharmaceutical use and use them as the new synthons for preparing compounds with antitumor and antiviral activity, the same products are new synthons for new analogues of camptothecin and palidino

--carboline" target="_blank">

The invention relates to bellrowan-carbolines, formula I, where R3denotes-CO-R1or group (a); R1- C1-C6alkoxy; R2- N2C1-C4alkyl, C1-C4alkoxy - C1-C2alkyl; And -- 5-6-membered unsaturated cycle, in which 1-2 carbon atoms may be replaced by N, O and/or S, which may be substituted with one R5or R6; R5and R6identical or different, denote H, C1-C6alkyl, NR7R8C1-C6alkyl which may be substituted by hydroxyl or C1-C4alkoxyl, phenyl, 5-6-membered heteroaryl residue, which contains one or two atoms of N, O or S, and phenyl and heteroaryl residue may be substituted C1-C4the alkyl, C1-C4alkoxyl, halogen, or R5and R6together,- CH2)nwhere n = 4; R7and R8- H, C1-C4alkyl, acyl, as well as their isomers, tautomers and salts

The invention relates to tetracyclic analogues of camptothecins formula (I), where R1, R2, R3, R4, R5and R10such as defined in the claims

The invention relates to the field of organic chemistry, namely to new bicyclic derivative

The invention relates to new derivatives oksiminoalkil acid of the formula (I), where R1is oxazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl, teinila, furil; thiazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl; unsubstituted chinoline and so on; X represents a bond or the group-NR6- where R6represents hydrogen or C1-4alkyl; n represents an integer from 1 to 3; Y represents an oxygen atom or the group-NR7- where R7is hydrogen; ring a represents a benzene ring, optionally substituted by one or two1-4alkoxy; p is an integer from 1 to 3; R2represents phenyl, optionally substituted lower alkyl, halogen, and so on; unsubstituted furyl; unsubstituted pyridyl; pyridinyl-1-oxide; q is an integer from 0 to 6; m represents 0 or 1; R3represents a hydroxy-group, lower alkoxy or-NR9R10where R9and R10represent identical or different groups selected from hydrogen, lower alkyl and lower alkylsulfonyl; R4and R5represent identical or different groups selected from hydrogen or

The invention relates to tetrahydro-gamma carbolines formula (I), where R1, R2D, Alk and n are such as defined in the claims

The invention relates to a derivative of tetrahydroimidazo[2,1-a]isoquinoline of the formula (I), where X represents a group (A) or (B), R1, R2and R3are hydrogen, C1-6by alkyl or halogen, a R4, R5, R6and R7are hydrogen
Up!