Derivatives cyanophenylacetic

 

The present invention relates to a derivative cyanophenylacetic formula I:

in which R represents aryl, cycloalkyl or POLYHALOGENATED group, r1represents alkyl, alkoxy, polyporales-, hydroxy - or triftormetilfullerenov, each of R2and R3represents, independently, a hydrogen atom or halogen, or alkoxy - or polytherapy, and n is 0, 1 or 2, or N-oxide or pharmaceutically acceptable salt of such compounds. Also described two variants of the method of production thereof and pharmaceutical composition based on compounds of the formula I. the Compounds possess high selectivity for1-adrenergic receptor and low activity in lowering blood pressure. 4 C. and 11 C.p. f-crystals, 3 tables.

Description text in facsimile form (see graphic part)

Claims

1. Derivatives cyanophenylacetic General formula I

in which R represents aryl, cycloalkyl or POLYHALOGENATED group;

R1PR is of R2and R3represents, independently, a hydrogen atom or halogen or alkoxy - or polyvoreshop; and

n is 0, 1 or 2,

or N-oxide or pharmaceutically acceptable salt of such compounds.

2. Connection on p. 1, in which R represents phenyl, tsiklogeksilnogo or triptorelin group.

3. Connection under item 1 or 2, in which R1represents methyl, methoxy - or 2,2,2-triptracker.

4. The compound according to any one of the preceding paragraphs, in which R2represents a hydrogen atom or fluorine.

5. The compound according to any one of the preceding paragraphs, in which R3represents a hydrogen atom or a chlorine or 2,2,2-triptracker.

6. The compound according to any one of the preceding paragraphs, in which n is equal to 1.

7. Any of the following compounds:

N-{3-[4-(5-chloro-2-methoxyphenyl)-1-piperazinil]propyl}-7-oxo-5-phenyl-7H-thieno[3,2-b]Piran-3-carboxamide,

N-{3-[4-(2-methoxyphenyl)-1-piperazinil]propyl}-7-oxo-5-phenyl-7H-thieno[3,2-b]Piran-3-carboxamide,

5-cyclohexyl-N-{3-[4-(2-methoxyphenyl)-1-piperazinil]propyl}-7-oxo-7H-thieno[3,2-b]Piran-3-carboxamide,

N-{3-[4-(2-methoxyphenyl)-1-piperazinil]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]Piran-3-carboxamide,

7-oxo-5-phenyl-N-{3-[4-[2-(2,2,2-cryptgetuserkey]propyl}-7-oxo-5-phenyl-7H-thieno[3,2-b]Piran-3-carboxamide and

N-{3-[4-[4-fluoro-2-(2,2,2-triptoreline)phenyl]-1-piperazinil]propyl}-7-oxo-5-phenyl-7H-thieno[3,2-b]Piran-3-carboxamide.

8. The pharmaceutical composition exhibiting L1-adrenergic activity, comprising a compound according to any one of the preceding paragraphs or N-oxide or pharmaceutically acceptable salt of such a compound in a mixture with a pharmaceutically acceptable diluent or carrier.

9. The pharmaceutical composition according to p. 8, further comprising an anticholinergic agent.

10. The pharmaceutical composition under item 9, which is an anticholinergic agent is one or more agent selected from the group consisting of tolterodine, oxybutynin, darifenacin, Alamein and temiverine.

11. The method of obtaining compounds of General formula I

in which R represents aryl, cycloalkyl or POLYHALOGENATED group;

R1represents alkyl, alkoxy, polyporales-, hydroxy - or triftormetilfullerenov;

each of R2and R3represents, independently, a hydrogen atom or halogen, or alkoxy - or polyvoreshop; and

n is 0, 1 or 2,

including condensation derivative of 7-oxo-7H-thieno[3,2-b]Piran-3-Kurbanova,

or of ester, halide or anhydride of such compounds with N-(w-aminoalkyl)-N’-phenylpiperazine derivative of General formula 2

in which n, R1, R2and R3have the meanings given above.

12. The method according to p. 11, in which the condensation is carried out in the presence of a condensing agent such as dicyclohexylcarbodiimide or diethylthiophosphate, optionally, in the presence of a promoting agent, such as N-hydroxysuccinimide or 4-dimethylaminopyridine or N,N’-carbonyldiimidazole, in an aprotic or chlorinated solvent at a temperature of from 10 to 140aboutC.

13. The method of obtaining compounds of General formula I

in which R represents aryl, cycloalkyl or POLYHALOGENATED group;

R1represents alkyl, alkoxy, polyporales-, hydroxy - or triftormetilfullerenov;

each of R2and R3represents, independently, a hydrogen atom or halogen or alkoxy - or polyvoreshop;

n is 0, 1 or 2,

including condensation derivative of 7-oxo-7H-thieno[3,2-b]Piran-3-carboxylic acid of General formula 1

b>nCH2X,

in which X represents a group to delete or group which is easily transformed into a group to delete;

n has the values defined above,

transformation, if necessary, the group X of the Oh-group in the deleted group in the resulting compound of General formula 3

and the interaction of the compounds of General formula 3 with phenylpiperazine derivative 8

in which R1, R2and R3have the meanings given above.

14. The method according to p. 13, in which the condensation derivative of 7-oxo-7H-thieno[3,2-b]Piran-3-carboxylic acid 1 with the amine2NCH2(CH2)nCH2X is carried out in the presence of a condensing agent such as dicyclohexylcarbodiimide or diethylthiophosphate, optionally, in the presence of promoterwise agent, such as N-hydroxysuccinimide, or 4-dimethylaminopyridine, or N,N’-carbonyldiimidazole, in an aprotic or chlorinated solvent at a temperature of from 10 to 140aboutC.

15. The method according to p. 13 or 14, in which the reaction of compound 3 with phenylpiperazine 8 is carried out in the absence of solvent, or, alternatively, in a polar solvent such as dimethylformamide, or acetonuria potassium.

 

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