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1. WO1995006630 - DERIVES DE BENZYLAMINE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

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CLAIMS
1. A benzylamine derivative represented by the general formula (1):


wherein Ri is a lower alkyl group;
R2 is a cycloalkyl group; and
R3 is a halogen atom;
or a salt thereof.
2. The benzylamine derivative or salt thereof according to Claim 1, wherein Ri is a methyl group or ethyl group.
3. The benzylamine derivative or salt thereof according to Claim 2, wherein Ri is a methyl group.
4. The benzylamine derivative or salt thereof according to Claim 1, wherein R2 is a cyclopropyl group or cyclobutyl group.
5. The benzylamino derivative or salt thereof according to Claim 1, wherein R2 is a cyclopropyl group.

6. The benzylamine derivative or salt thereof according to Claim 1, wherein R3 is a chlorine atom. 7. The benzylamine derivative or salt thereof according to Claim 1, wherein Ri is a methyl group or ethyl group; R is a cyclopropyl group or cyclobutyl group; and R3 is a chlorine atom.
8. The benzylamine derivative or salt thereof according to Claim 6 or 7, wherein R3 is substituted at 4-position in the benzene ring.
9. 3-( 4-Chlorobenzyloxy)-N-cyclopropyl-N-methylbenzylamine .
10. 4-(4-Chlorobenzyloxy)-N-cyclopropyl-N-methylbenzylamine .
11. 2-(4-Chlorobenzyloxy)-N-cyclopropyl-N-methylbenzylamine .
12. An antidepressant --antianxiety agent
containing, as the active ingredient, the benzylamine derivative or salt thereof being claimed in Claim 1. 13. An agent for activating the central nervous system containing, as the active ingredient, the benzylamine derivative or salt thereof being claimed in Claim 1.
14. An agent for ameliorating disorder of
consciousness containing, as the active ingredient, the benzylamine derivative or salt thereof being claimed in Claim 1.
15. A sigma receptor-agonistic agent containing, as the active ingredient, the benzylamine derivative or salt thereof being claimed in Claim 1.
16. The antidepressant-antianxiety agent according to Claim 12, wherein the active ingredient is the benzylamine derivative being claimed in Claim 9, 10 or 11.
17. The agent for activating the central nervous system according to Claim 13, wherein the active ingredient is the benzylamine derivative being claimed in Claim 9, 10 or 11.
18. The agent for ameliorating disorder of consciousness according to Claim 14, wherein the active ingredient is the benzylamine derivative being claimed in Claim 9, 10 or 11.
19. The sigma receptor-agonistic agent according to Claim 15, wherein the active ingredient is the benzylamine derivative being claimed in Claim 9, 10 or 11.
20. Process for preparing a benzylamine derivative (1):


wherein Ri is a lower alkyl group; R is a cycloalkyl group; and R3 is a halogen atom;
by reacting a benzyloxybenzaldehyde (2):



OCH2 (2)

wherein R3 is the same as defined above; .
with an amine compound (3):

.Rl
HN (3)
~CH2-R2

wherein Ri and R2 are the same as defined above;
thus obtained Schiff's base compound (A):


wherein Ri, R2 and R3 are the same as defined above; is subjected to a reducution, without being isolated from the reaction system, to prepare the desired benzylamine derivative (1) .
21. Process for preparing a benzylamine derivative (1):


wherein Ri, R2 and R3 are the same as defined above; by reacting a benzyloxybenzylamine compound (4):

wherein R2 and R3 are the same as defined above; with an alkyl halide (5):

Ri-X (5)

wherein Ri is the same as defined above; and X is a halogen atom; or with an aldehyde or ketone (6):

O

wherein R4 and R5 are each a hydrogen atom or a lower alkyl group; to prepare the desired benzylamine
derivative (1).
22. Process for preparing a benzylamine derivative (1):


wherein Ri, R2 and R3 are the same as defined above; by reducing a benzyloxybenzylamine compound (9):

wherein Ri, R2 and R3 are the same as defined above; to prepare the desired benzylamine derivative (1).
23. Process for preparing a benzylamine derivative

(1):


wherein Ri, R2 and R3 are the same as defined above; by reacting a benzyloxybenzylamine compound (7):


wherein Ri and R3 are the same as defined above; with a cycloalkylmethyl halide (10):

R2-CH2-X (10) wherein R2 and X are the same as defined above; to prepare the desired benzylamine derivative (1).
24. Process for preparing a benzylamine derivative

(1):


wherein Ri, R and R3 are the same as defined above: by reducing a benzyloxybenzoylamine compound (12):



wherein Ri, R2 and R3 are the same as defined above; to prepare the desired benzylamine dereivative (1).