Displaced heterocyclic derivatives and their application

FIELD: chemistry.

SUBSTANCE: invention relates to new displaced heterocyclic derivatives that can be used in treatment of diabetes and to reduce the content of cholesterol. In formula m is 1; n is 1; Q is C; A is -(CH2)x2-0-(CH2)x3-, where x2 varies from 1 to 3 and x3 is 0; B is a bond or it is (CH2)x4, where x4 varies from 1 to 2; X represents CH or N; X2, X3, X4, X5, X6 represent C, N, O; provided that one from X2 X3 X4 X5 and X6 represents N; and at least one of X2, X3, X4, X5, and X6 represents C; R1 represents H or C1-C6alkyl; R2 is H; R2a, R2b and R2c can be equal or different and selected from H, C1-C6alkyl, C1-C6alkoxy, halogen or thyano; R3 is selected from phenyloxycarbonile, C1-C6alkyloxycarbonile, phenylcarbinol, phenyl, alkoxy; Y represents CO2R4 (where R4 represents H or C1-C6alkyl); (CH2)m can be not necessarily displaced by 1 substitute.

EFFECT: produced are pharmaceutical composition for treatment of diabetes and to reduce the content of cholesterol.

13 cl, 2 tbl, 22 dwg, 88 ex

 

The text descriptions are given in facsimile form.

1. Substituted heterocyclic derivative of the formula:

where m is 1; n is 1;

Q represents C;

And represents - (CH2)x2-O-(CH2)x3-where x2has a value from 1 to 3 and x3has a value of 0;

Represents a bond or represents (CH2)x4where x4has a value from 1 to 2;

X represents CH or N;

X2represents C, N, O;

X3represents C, N, O;

X4represents C, N, O;

X5represents C, N, O;

X6represents C, N, O;

provided that at least one of X2, X3, X4X5and X6represents N; and at least one of X2, X3X4, X5and X6is,

R1represents N or C1-C6alkyl;

R2represents N;

R2a, R2band R2cmay be the same or different and selected from H, C1-C6of alkyl, C1-C6alkoxy, halogen or cyano;

R3select the from vinyloxycarbonyl, C1-C6allyloxycarbonyl, phenylcarbamoyl, phenyl, alkoxystyrene;

Y represents CO2R4,where R4represents N or C1-C6alkyl;

(CH2)mmay be optionally substituted by 1 Deputy;

including all stereoisomers, esters and pharmaceutically acceptable salt,

except for the structure:

where X2=N, X3=, X4=O or S, Z=O or communication.

2. The compound according to claim 1, in which X represents CH.

3. The compound according to claim 1, in which a represents a - (CH2)x2-O-.

4. The compound according to claim 1, which is a link.

5. The compound according to claim 1, in which

represents,,or

6. The compound according to claim 1, which has the formula:

7. The compound according to claim 1, which has the formula:

8. The connection according to claim 7, in which R2a, R2band R2ceach represents H; R1represents a C1-C6alkyl, x2has a value from 1 to 3; R2is the Wallpaper N; (CH2)mrepresents CH2, X2, X3, X4, X5and X6represent in the amount of 1, 2 or 3 nitrogen atom, (CH2)nrepresents CH2and R3is alcoxyphenylsubstituted.

9. The connection of claim 8, in which R1represents CH3and R3is methoxyphenylacetylene.

10. The compound according to claim 1, in which

represents,,or

11. Compounds according to claim 1, having the formula:

12. Pharmaceutical composition for treatment of diabetes and reduce cholesterol containing compound according to claim 1 and pharmaceutically acceptable carrier.

13. The use of compounds according to claim 1 to obtain pharmaceutical compositions for the treatment of diabetes and reduce cholesterol.



 

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SUBSTANCE: invention relates to compounds represented by the formula: wherein values of substitutes are given in the invention description. Also, invention relates to pharmaceutically acceptable salts of the compound that can be used in treatment and/or prophylaxis of cathepsin-dependent states or diseases of mammals. Proposed compound are useful in treatment of diseases wherein bone resorption inhibition is desired, such as osteoporosis, increased mineral density of bone and reducing risk of fractures. Proposed claimed compounds are designated for preparing a drug possessing the inhibitory activity with respect to cathepsin.

EFFECT: valuable medicinal and biochemical properties of compounds.

24 cl, 13 sch, 4 tbl, 15 ex

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EFFECT: improved and valuable medicinal properties of agent.

7 cl, 232 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new compounds of the following formulae:

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

10 cl, 1 tbl, 104 ex

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EFFECT: improved preparing method, valuable medicinal properties of compounds and compositions.

9 cl, 1 tbl, 41 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

28 cl, 6 tbl, 6 sch, 251 ex

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EFFECT: valuable medicinal and biochemical properties of compounds.

24 cl, 13 sch, 4 tbl, 15 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

20 cl, 1 tbl, 13 sch, 71 ex

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EFFECT: valuable medicinal properties of compounds.

19 cl, 1 tbl, 7 sch, 56 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

28 cl, 3 tbl, 131 ex

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EFFECT: valuable medicinal properties of compounds.

15 cl, 5 tbl, 48 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

16 cl, 5 sch, 26 ex

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EFFECT: valuable medicinal properties of compounds.

29 cl, 12 tbl, 587 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

10 cl, 1 tbl, 104 ex

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EFFECT: valuable medicinal properties of compounds and agent.

21 cl, 15 tbl, 14 ex

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EFFECT: improved method of synthesis.

18 cl, 19 ex

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