Morpholine derivative and pharmaceutical composition based on it

 

Describes the new morpholine derivative of the formula or its pharmaceutically acceptable salt, where R1selected from the group consisting of: (1) hydrogen; (2) C1-6-alkyl, unsubstituted or substituted phenyl or heterocycle, where the heterocycle selected from a group comprising imidazolyl or triazolyl, and where the heterocycle is unsubstituted or substituted by oxopropoxy; R2and R3denote each hydrogen; R6, R7and R8independently selected from the group consisting of: (1) hydrogen, (2)1-6is alkyl, substituted with halogen, and (3) halogen; R11, R12and R13independently selected from hydrogen and halogen; X represents-O-; Y represents-O-; Z represents C1-6-alkyl. New compounds are antagonists of the receptor tachykinin. Also describes a pharmaceutical composition comprising an effective amount of the compounds on p. 1. 2 C. and 12 C.p. f-crystals.

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

Claims

1. Morpholino derived structural formulaor its pharmaceutically acceptable salt, where R1wyble a heterocycle selected from the group including imidazolyl or triazolyl, and where the heterocycle is unsubstituted or substituted by oxopropoxy; R2and R3denote each hydrogen; R6, R7and R8independently selected from the group consisting of (1) hydrogen, (2) C1-6is alkyl, substituted with halogen, and (3) halogen; R11, R12and R13independently selected from hydrogen and halogen; X represents-O-; Y represents-O-;
Z represents a C1-6-alkyl.

2. Connection on p. 1, where R1represents a C1-6-alkyl, substituted heterocycle, where the heterocycle selected from a group including imidazolyl or triazolyl, and where the heterocycle is unsubstituted or substituted by exography.

3. Connection on p. 1, where R6, R7and R8independently selected from the group consisting of (1) hydrogen, (2) C1-6-alkyl, (3) fluoro, (4) chlorine, (5) bromine, and (6) iodine; R11, R12and R13independently selected from the group consisting of: (1) hydrogen, (3) fluoro, (4) chlorine, (5) bromine, and (6) iodine.

4. Connection on p. 1, where Z represents a C1-4-alkyl.

5. Connection on p. 1, where Z represents-CH3.

6. Connection on p. 1, where R1selected from the group consisting of


7. the

8. Connection on p. 1, where R1selected from the group consisting of: (1,3-imidazole)methyl and (2-oxo-1,3-imidazole)methyl.

9. Connection on p. 1 of structural formula

or its pharmaceutically acceptable salt,
where R1, R2, R3, R6, R7, R8, R11, R12, R13, Y and Z indicated in paragraph 1.

10. Connection on p. 1 of structural formula II

or its pharmaceutically acceptable salt,
where R1, R2, R3, R6, R7, R8, R11, R12, R13and Z are specified in paragraph 1
11. Connection on p. 1 of structural formula III

or its pharmaceutically acceptable salt,
where R1, R2, R3, R6, R7, R8, R11, R12, R13and Z are specified in paragraph 1.

12. Connection on p. 1, selected from the group consisting of:
2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-phenylmorpholine;
2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-phenylmorpholine;
2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)morpholine;
2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)morpholine;
2-(R)-(1-(S)-(3,5-fenil)morpholine;
2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-morpholine;
2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-morpholine;
2-(R)-(1-(R)-(3-(trifluoromethyl)phenyl)ethoxy)-3-(S)-phenyl-4-(3-(5-oxo-1H, 4H-1,2,4-triazolo)methyl)morpholine;
2-(R)-(1-(R)-(3-fluoro-5-(trifluoromethyl)phenyl)ethoxy)-3-(S)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)morpholine;
2(S)-(1-(S)-(3-fluoro-5-(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)morpholine;
2-(S)-(1-(R)-(3-fluoro-5-(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)morpholine;
2-(S)-(1-(R)-(3-fluoro-5-(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal))-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-morpholine;
2(S)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(4-(2-oxo-1,3-imidazole)methyl)morpholine;
2(S)-(1(R)-(3-fluoro-5-(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(4-(2-oxo-1,3-imidazole)methyl)morpholine;
2-(S)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(R)-(4-forfinal)-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-morpholine;
2(R)-(1(R)-(2,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)morpholine;
2(R)-(1-(R)-(2,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-morpholine;
2-(R)-(1-(R)-(2,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(3-(1,2,4-triazolo)methyl)morpholine;
eticeskaja composition for counteracting the effect of substance P at its receptor site or for the blockade of receptors neirokinina-1 in a mammal, containing an effective amount of the compounds on p. 1 and a pharmaceutically acceptable carrier.

14. Connection on p. 1 representing 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-forfinal)-4-(3-(5-oxo-1H, 4H-1,2,4-triazolo)methyl)morpholine, or its pharmaceutically acceptable salt.

 

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