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Pyrimidine derivatives, characterised by antiproliferative activity, and pharmaceutical composition
Pyrimidine derivatives, characterised by antiproliferative activity, and pharmaceutical composition
IPC classes for russian patent Pyrimidine derivatives, characterised by antiproliferative activity, and pharmaceutical composition (RU 2336275):
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FIELD: chemistry.

SUBSTANCE: invention relates to new pyrimidine derivatives of formula I and their pharmaceutically acceptable salts, which are selective inhibitors of kinases KDR, FGFR and PDGFR and can be used for treatment of oncological diseases. Compound of formula I corresponds to structural formula , where R1 is selected from group, including H, COR4 and COOCHR5OCOR4; R2 and R3 are independently selected from group, including C1-6alkyl, C1-6alkyl, substituted with not more than 4 groups, which are independently selected from group, including -NR5R6,-R5, -OR5-phenyl,-phenyl, substituted with not more than 2 groups, which are independently selected from group, including OR5 and -C1-4alkyl and heteroaryl, representing aromatic heterocyclic ring system, which contains not more than two rings and includes from 1 to 3 nitrogen atoms, and heterocyclyl, representing saturated cyclic radical, which includes from 1 to 3 nitrogen atoms; R5 and R6 are independently selected from group H and C1-5alkyl. Invention also relates to pharmaceutical compositions, containing said compounds of formula I and intermediate products.

EFFECT: obtaining new pyrimidine derivatives, which can be used for treating oncological diseases.

17 cl, 2 tbl, 27 ex

 

The text descriptions are given in facsimile form.

1. The compound of the formula

or its pharmaceutically acceptable salt,

where R1selected from the group including

-N,

-COR4and

-COOCHR5OCOR4;

R2and R3independently selected from the group including

Mr. and

-OR5;

R4selected from the group including

-C1-6alkyl,

-C1-6alkyl, substituted not more than 4 groups that are independently selected from the group including

-NR5R6,

-SR5,

-OR5,

-phenyl,

is phenyl, substituted by no more than 2 groups that are independently selected from the group including

p num="27"> -OR, and-C1-4alkyl and

-heteroaryl represents an aromatic heterocyclic ring system, containing not more than two rings and containing from 1 to 3 nitrogen atoms, and

-heterocyclyl representing a saturated cyclic radical comprising from 1 to 3 nitrogen atoms;

R5and R6independently selected from the group

Mr. and

-C1-5alkyl.

2. The compound of formula I according to claim 1,

where R1selected from the group including

-N,

-COR4and

-COOCHR5OCOR4;

R2and R3independently selected from the group including

Mr. and

-OR5;

R4selected from the group including

-C1-6alkyl,

-C1-6alkyl containing from 1 to 4 substituents that are independently selected from the group including

-NR5R6,

-SR5,

-OR5,

-phenyl,

-phenyl containing from 1 to 2 substituents that are independently selected from the group including

-OR5and-C1-4alkyl and

-indolyl, -pyrrolyl, -pyridinyl, -pyrazinyl-chinoline-pyrimidinyl-imidazolyl

and-piperidinyl, -piperazinil-pyrrolidinyl;

R5and R6independently selected from the group

Mr. and

-C1-5alkyl.

3. The connection is of the formula I according to claim 1 or 2, where R1means-COR4.

4. The compound of formula I according to claim 3, where R4means C1-6alkyl.

5. The compound of formula I according to claim 4, which is chosen from the group including

N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylacetamide,

N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylpropanamide,

N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylpentane, and

N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylbutyramide.

6. The compound of formula I according to claim 3, where R4means

-C1-6alkyl, substituted by a group-NR5R6or

-C1-6alkyl, substituted by a group-NR5R6and the additional group selected from the set:

-NR5R6,

-SR5,

-OR5,

-phenyl,

-phenyl containing from 1 to 2 substituents that are independently selected from the group including

-OR5and-C1-4alkyl, and

-indolyl, -pyrrolyl, -pyridinyl, -pyrazinyl-chinoline-pyrimidinyl-imidazole,

a R5and R6independently selected from the groups-N and-C1-5alkyl.

7. The compound of formula I according to claim 6, which is selected from the group including

(2S)-2-amino-N-[3-(4-netoxygen the l)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-4-methylthio-N-phenylbutyramide,

(2S)-2-amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-3-phenyl-N-phenylpropanamide,

acetate (2S)-2-amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-4-methyl-N-phenylphthalimide and

hydrochloride, (2S)-2-amino-3-indol-3-yl-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylpropanamide.

8. The compound of formula I according to claim 3, where R3means-OR5, a R5means-N or-C1-5alkyl.

9. The compound of formula I of claim 8, which is chosen from the group comprising N-(4-hydroxyphenyl)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]ndimethylacetamide, and

N-(4-methoxyphenyl)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-4]pyrimidine-7-yl)]ndimethylacetamide.

10. The compound of formula I according to claim 1 or 2, where R1means COOCHR5OCOR4.

11. The compound of formula I of claim 10, which is selected from the group including

{N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylcarbamoyloxy}methyl ether acetic acid,

{N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylcarbamoyloxy}methyl ether 2-(dimethylamino)acetic acid,

hydrochloride {N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-is l)]-N-phenylcarbamoyloxy}methyl ether, 2-(dimethylamino)acetic acid and

triptorelin {N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-phenylcarbamoyloxy}methyl ether piperidine-4-carboxylic acid.

12. The compound of formula I according to claim 1 or 2, where R is N.

13. The compound of formula I according to item 12, which is selected from the group including

3-(4-methoxyphenyl)-1-phenyl-7-(phenylamino)-1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-2-it,

methanesulfonate 3-(4-methoxyphenyl)-1-phenyl-7-(phenylamino)-1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-2-it,

7-[(4-hydroxyphenyl)amino]-3-(4-methoxyphenyl)-1-phenyl-1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-2-it 3-(4-methoxyphenyl)-7-[(4-methoxyphenyl)amino]-1-phenyl-1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-2-it.

14. Compounds according to any one of claims 1 to 13, having antiproliferative activity.

15. Pharmaceutical composition having anti-proliferative activity comprising a therapeutically effective amount of a compound according to any one of claims 1 to 13 and a suitable pharmaceutical carrier or exipient.

16. The pharmaceutical composition according to item 15, which is intended for administration to a patient with cancer.

17. Compound which is selected from the group including

(chloromethoxy)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-benzamide (example 4A),

3-(4-methoxyphenyl)-1-phenyl-7-{[4-(1,1,2,2-t is trimethyl-1 salepropecia)phenyl]amino}-1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-2-he (example 19c) and

N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydroxypyrimidine[4,5-d]pyrimidine-7-yl)]-N-[4-(1,1,2,2-tetramethyl-1-salepropecia)phenyl]ndimethylacetamide (example 19 g).

 
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