New pyrimidine derivatives (options)

 

The invention relates to new pyrimidine derivative of General formula (I) or their pharmaceutically acceptable salts, with high antisecretory activity with the properties of reversible proton pump inhibitor that can be used to obtain valuable medicines. In the compounds of General formula I is3-7cycloalkyl, C1-3alkoxyethyl, 1-naphthylmethyl, 4-methylthiazole-2-yl or 4-phenylthiazol-2-yl, R1represents hydrogen or methyl, R2, R3, R4and R5are hydrogen; or represents a group of formula II listed in the description, in which R7is hydrogen or halogen, R1represents hydroxymethyl or C1-3alkoxymethyl, R2, R3, R4, R5and R6are hydrogen; or represents a group of formula II, above, and R1represents hydrogen or methyl, and one or two R2, R3, R4, R5and R6are hydroxy, methoxyacetyl or a group of the formula III listed in the description: -O-C(O)-Z, in which Z represents C1-4alkyl, C2-4alkenyl,3-6cycloalkyl, morpholinomethyl, piperidinomethyl, phenyl, naphthyl, thiophene-2-ylmethyl or chr8Other9hdiutil, carbamoylmethyl, carbamoylethyl or 1-benzimidazole-4-ylmethyl, and R9represents hydrogen or tert. -butoxycarbonyl, and other R2, R3, R4, R5and R6are hydrogen or stands. 2 S. and 11 C.p. f-crystals, 2 PL.

Description text in facsimile form (see graphic part). T T

Claims

1. The derivative of a pyrimidine of formula (I)where is (C3-C7) cycloalkyl, (C1-C3) alkoxyethyl, 1-naphthylmethyl, 4-methylthiazole-2-yl or 4-phenylthiazol-2-yl; R1represents hydrogen or methyl; R2, R3, R4and R5are hydrogen; or represents a group of formula (II)in which R7represents hydrogen or halogen; and R1represents hydroxymethyl or (C1-C3)alkoxymethyl, a R2, R3, R4, R5and R6are hydrogen; or represents the group (II) above, and R1represents hydrogen or methyl, and one or two R2, R3, R4, R5and R6are hydroxy, methoxy radical or a group of the formula (III)

2. Connection on p. 1, where In is (C3-C7-cycloalkyl, (C1-C3)alkoxyethyl, 1-naphthylmethyl, 4-methylthiazole-2-yl or 4-phenylthiazol-2-yl.

3. Connection on p. 1, where In is a group of formula (II); R1represents hydrogen or methyl; one or two of R2, R3, R4, R5and R6represent hydroxy or methoxy.

4. Connection on p. 1, where In is a group of formula (II), R1represents hydrogen or methyl; one or two of R2, R3, R4, R5and R6represent a group of formula (III).

5. Connection on p. 1, where In is a group of formula (II) and R1represents hydroxymethyl or (C1-C3)alkoxymethyl.

6. Connection on p. 1, represents citiesi acceptable salt.

7. Connection on p. 1 representing 5,6-dimethyl-2-(4-forgenerating)-4-(1-methyl-6-hydroxy-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine or its pharmaceutically acceptable salt.

8. Connection on p. 1, representing 5-hydroxymethyl-6-methyl-4-(1-methyl-1,2,3,4-tetrahydro-isoquinoline-2-yl)-2-(4-forgenerating)pyrimidine or its pharmaceutically acceptable salt.

9. Connection on p. 1, representing 5-methyl-6-(thiophene-2-yl-acetoxymethyl)-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine or its pharmaceutically acceptable salt.

10. Connection on p. 1, representing 5-methyl-6-valrocemide-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine or its pharmaceutically acceptable salt.

11. Connection on p. 1, representing 5-methyl-6-(phenyleneoxymethylene)-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine or its pharmaceutically acceptable salt.

12. Connection on p. 1 representing 5,6-dimethyl-2-(4-methylthiazole-2-yl)amino-4-(1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine or its pharmaceutically acceptable salt.

13. The derivative of a pyrimidine selected from the group consisting of:
5-methyl-6-{ (2-ethoxycarbonylethyl)carbonylmethyl} -2-(4-forgenerating)-4-(1-methyl-1,2,3,tetrahydroisoquinoline-2-yl)pyrimidine;
5-methyl-6-(4-propylbenzenesulfonyl)-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine;
5-methyl-6-(4-interventionstitel)-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine;
5-methyl-6-(3-forantibiotic)-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine;
5-methyl-6-benzyloxycarbonyl-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine;
5-methyl-6-cinnamoyloxy-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2-ethoxycarbonylethyl)carbonyloxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-methylbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-ethylbenzoic)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-propylbenzoyl)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-tert-butylbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-pentylbenzoyl)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,methyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-chlorobenzoyloxy)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(3-chlorobenzoyloxy)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,4-dichloro-5-perbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,4,6-trichlorobenzoyl)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(3-perbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,3-differentiate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,6-differentiate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,4-differentiate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,3,4-triterpenols)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4{ 1-methyl-6-(2,3,6-triterpenols)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,4,5-triterpenols)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(3-triftormetilfosfinov)-1,2,3,4-tetrahydroisoquinoline-2-yl} Phil} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(2,3,4,5-tetrafluorobenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(3-methoxyphenyl)acetoxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-methoxyphenyl)acetoxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(4-butoxybenzoyl)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(nitrobenzyloxy)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-(3-cyanobenzoyl)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-cinnamoyloxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-6-benzisoxazole-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(2-ethoxycarbonylethyl)carbonyloxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(4-methylbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(propylbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;< /> 5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(2-chlorobenzoyloxy)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(3-perbenzoate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(3-triftormetilfosfinov)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(2,3-differentiate)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(3-methoxyphenyl)acetoxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(4-methoxyphenyl)acetoxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(4-nitrobenzyloxy)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(3-cyanobenzoyl)-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-cinnamoyloxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-benzisoxazole-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5-methyl-6-(4-benzylpiperazine)acetoxymethyl-2-(4-forgenerating)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine;
5,6-d/> 5,6-dimethyl-2-(4-forgenerating)-4-{ 1-methyl-7-(4-benzylpiperazine)acetoxy-1,2,3,4-tetrahydroisoquinoline-2-yl} pyrimidine,
or its pharmaceutically acceptable salt.

 

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