Tricyclic condensed heterocyclic compounds, the retrieval method (variants) and a pharmaceutical composition

 

The invention relates to tricyclic condensed heterocyclic compounds of the formula I, X is, for example, CH, CH2, R (where R means a lower alkyl group or a substituted lower alkyl group) or CRR' (where R and R' have the values specified above for R); Y means, for example, CH, CH2or C=O; z means, for example, S, S=O=; U denotes C; R1-R4independent means, for example, a hydrogen atom, SR (where R has the above values), phenyl group, substituted phenyl group, follow group, thienyl group, benzofuran or benzothiazyl at least one element of R5and R8means, for example, HE and the rest of the elements of R5and R8independent means, for example, a hydrogen atom; and their optical isomers, conjugates, and pharmaceutically acceptable salts. These compounds are characterized by a wide spectrum of pharmacological activity, in particular they have a relaxing effect on smooth muscles of the trachea, perfectly suppress the allergic reaction of the respiratory tract, inhibit infiltration of inflammatory cells in the Airways and in addition, are harmless. Also described is a method of obtaining compounds, �://img.russianpatents.com/img_data/63/639973.gif">

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

Claims

1. The compound of formula (1)where is the link X-Y is a simple or a double bond and when link X-Y is a simple bond, then x is the CHW0or CW0W0where W0means a lower alkyl group or a lower alkyl group, a substituted phenyl group, and Y represents CH2or C= O; and when link X-Y is a double bond, then X is CW0where W0means a lower alkyl group or a lower alkyl group, a substituted phenyl group, and Y represents CW4where W4means a hydrogen atom or a lower alkoxygroup; Z is S or S= O; U denotes C; R1-R4that may be the same or different values, independently selected from the group including a hydrogen atom, halogen, a group SW5where W5is a lower alkyl group, phenyl group, substituted phenyl group where the Deputy is any group selected from hydroxyl group, amino group, nitro group, trihalomethanes group, halogen, a lower alkyl group and trihalogen the spruce of R5-R8means a hydroxyl group (provided that when link X-Y is CH(C2H5)And R6means a hydroxyl group, at least one substituent R5, R7and R8means a hydroxyl group), and other deputies from among R5-R8that may be the same or different values are selected, each independently, from the group comprising a hydrogen atom, a hydroxyl group and a lower alkoxygroup;
its optical isomer, conjugate or pharmaceutically acceptable salt.

2. Connection on p. 1, in which R6means a hydroxyl group.

3. Connection on p. 1, in which R6and R7mean hydroxyl group.

4. Connection on p. 1, in which R6and R8mean hydroxyl group.

5. Connection on p. 1, in which R5and R6mean hydroxyl group.

6. The compound according to any one of paragraphs. 1-5, in which Y means WITH.

7. The compound according to any one of paragraphs. 1-6, in which the lower alkyl group is methyl group, ethyl group, n-sawn group, isopropyl group, n-butilkoi group, sec-butilkoi group, isobutylene group or tert-butilkoi group.

ing group, where the Deputy determined as specified in paragraph 1, follow group, thienyl group, benzofuran or sensational.

9. The compound according to any one of paragraphs. 1-8, in which R2or R3means SW5where W5means a lower alkyl group.

10. The compound according to any one of paragraphs. 1-9, in which Z signifies S.

11. Connection on p. 1 which is 7,8-dihydroxy-11-ethyl-10,11-dihydrobenzo[b, f] thiepin-10-one.

12. Connection on p. 1, which is 11-diethyl-7,8-dihydroxy-10,11-dihydrobenzo[b, f] thiepin-10-one.

13. The method of obtaining the compounds of formula (1)

where is the link X-Y is a simple or a double bond and when link X-Y is a simple bond, then x is the CHW0or CW0W0where W0means a lower alkyl group or a lower alkyl group, a substituted phenyl group, and Y represents CH2or C= O; and when link X-Y is a double bond, then X is CW0where W0means a lower alkyl group or a lower alkyl group, a substituted phenyl group, and Y represents CW4where W4means a hydrogen atom or a lower alkoxygroup;
Z is S or S= O;
U mean With;
R1-R4that may have W5where W5is a lower alkyl group, phenyl group, substituted phenyl group where the Deputy is any group selected from hydroxyl group, amino group, nitro group, trihalomethanes group, halogen, a lower alkyl group and trigalogenmetany, follow group, thienyl group, benzofuran and sensational;
at least one Deputy from R5-R8means a hydroxyl group (provided that when link X-Y is CH(C2H5)And R6means a hydroxyl group, at least one substituent R5, R7and R8means a hydroxyl group), and other deputies from among R5-R8that may be the same or different values are selected, each independently, from the group comprising a hydrogen atom, a hydroxyl group and a lower alkoxygroup,
its optical isomer, conjugate or pharmaceutically acceptable salt, which comprises performing the reaction stages of the linking rings And ring by reaction Ullman (stage 1) and the binding ring And ring by reaction Friedel-(stage 2), as shown in the formula 2

15. A pharmaceutical composition of a wide range of pharmacological effects, including a relaxing effect on smooth muscles of the trachea, the suppression of allergic reactions and inhibition of infiltration of inflammatory cells in the Airways, which contains an effective amount of a compound according to any one of paragraphs. 1-12 and a pharmaceutically acceptable carrier or diluent.

16. The pharmaceutical composition according to p. 15, which contains the connection, providing a relaxing effect on smooth muscles of the trachea.

17. The pharmaceutical composition according to p. 15, which contains a compound overwhelming allergic reaction of the respiratory tract.

18. The pharmaceutical composition according to p. 16, which contains a compound inhibiting the infiltration of inflammatory cells.

19. The pharmaceutical composition according to p. 15, which is designed for use as anti-asthma drugs.

20. The compound of the formula

where Q denotes a lower alkyl group,
its optical isomer, or salt.sub>1-Q5that may be the same or different values, independently mean a hydrogen atom, a lower CNS group or hydroxyl group, provided that at least one element of Q1-Q5is not a hydrogen atom,
its optical isomer, or salt.

 

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