Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing
Patent
1995-04-29
1996-08-27
Raymond, Richard L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Amino nitrogen containing
564385, 564386, 564390, C07C21758
Patent
active
055502920
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/01332, filed Aug. 11, 1994.
FIELD OF THE INDUSTRIAL UTILIZATION
The present invention relates to novel benzylamine derivatives and their salts.
BACKGROUND ART
As to the current human society is becoming increasingly complex in structure and mechanism, so that people undergo increasing stresses of various kinds. In such an ever-changing society, the number of people suffering from mental disorder, particularly depression and anxiety neurosis are increasing, posing a big social problem.
Unlike the typical depression seen in the past, depression appearing currently is relatively slight and tends to become chronic, in many cases. Depression is often difficult to distinguish from neurosis and tends to become chronic. It is reported that most of the patients of chronic depression have neurosis as well and that the number of depression patients is increasing more and more in recent years (cf. Japanese Journal of Clinical Psychiatry, Vol. 21, No. 4, pp. 691-695, 1992).
Thus, the features of mental disorder are becoming more complex as the structure and mechanism of society become complex. The following two facts are pointed out as the recent major changes in the features of metal disorder.
(1) In neurosis, those neuroses are increasing which show depressive syndrome and which are difficult to distinguish from depression.
(2) Among the patients which have been judged to have neurosis, patients of slight depression are included. Among, in particular, the patients which have been judged to have neurosis because of their anxiety attack and expectation fear, patients of slight depression are included at a fairly high ratio (cf. Japanese Journal of Clinical Psychiatry, Vol. 21, No. 4, pp. 691-695, 1992).
According to a clinical research (cf. "Anxious Depression" edited by Racagni G. Smeraldi, Raven Press, N.Y., 1987), analysis of the symptoms of the patients who had been judged to have serious depression, indicated that the symptoms comprised worry of intermediate level (72%), psychological anxiety (62%), physical anxiety (of autonomic nervous system and muscle system) (42%), fear attack (29%), fear symptom (19%) and obsessive-compulsive symptom (1.2%). Patients of depression include patients of anxiety symptom at a high ratio.
Mental disorder which show complex and diversified symptoms as mentioned above, are currently treated, in many cases, with an antidepressant, an antianxiety agent or a combination thereof, depending upon the symptoms. Such treatment is effective in some cases but is said to be insufficient in most cases. Conventional antidepressants are effective for endogeneous depression, but are not sufficiently effective for character-originated depression or highly neurotic depression (cf. Journal of Neuropsychopharmacology, Vol. 9, No. 4, pp. 279-285, 1987). Use of antianxiety agent by patients who show anxiety symptom on the surface while actually having a depressive phase, prolongs the depression in some cases (cf. Japanese Journal of Clinical Psychiatry, Vol. 21, No. 4, pp. 691-695, 1992). Use of antidepressant based on the indiscreet judgement by clinical department other than psychiatry department, may overlook suicidal ideation and induce the prolongation of depression (cf. Journal of Neuropsychopharmacology, Vol. 9, No. 4, pp. 279-285, 1987).
Conventional antidepressants have problems; that is, (1) they show no immediate effect and need to be administered continuously for at least 2 weeks, (2) they have undesirable side effects such as anti-cholinergic effect and the like and (3) they are ineffective in some cases (effective ratio: 65%) (cf. Journal of Neuropsychopharmacology, Vol. 11, No. 10, pp. 753-761, 1989). Conventional antianxiety agents have problems; that is, (1) they have side effects such as excessive sedation, somnolence, muscle relaxation and the like and (2) there often appear serious adverse symptoms such as dependency, abstinence symptom, memory impairment and the like (cf. Journal of Neuropsychopharmacology, Vol. 11. No. 9, pp. 709-719, 198
REFERENCES:
patent: 4687865 (1987-08-01), Thottathil
"The Place of the SSRIs and Fluvoxamine in the Treatment of Patients with Depression", Y. Lecrubier, Drugs 43 (2): 1-2 (1992).
"Pharmacological Differences of Serotonin Reuptake Inhibitors and Possible Clinical Relevance", B. E. Leonard, Drugs 43 (2): 3-10 (1992).
"Comparative Efficacy of Antidepressants", S. Kasper et al., Drugs 43 (2) pp. 11-23 (1992).
"The Synthesis of a Conformationally Rigid Calcium Channel Blocker", J. C. Barrish et al., Chemical Abstracts 119:203257n (1993).
Hirose Tsuyoshi
Kurahashi Nobuyuki
Miwa Takashi
Mori Atsushi
Nishi Takao
Otsuka Pharmaceutical Co. Ltd.
Raymond Richard L.
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