Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-05-21
2000-02-01
Huang, Evelyn Mei
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546194, 546226, A61K 31445, C07D40112, C07D40114, C07D40514, C07D40914
Patent
active
060203455
DESCRIPTION:
BRIEF SUMMARY
The present application is a U.S. National Application filed under 35 USC 371 of PCT/FR97/02097, filed Nov. 20, 1997 based upon French application Ser. No. 96/14217 filed Nov. 21, 1996.
Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter and a neuromodulator of the central nervous system which exerts its multiple physiological functions by interaction with the specific 5-HT receptors. These 5-HT receptors have been grouped into several main classes. Among these main classes, the 5-HT.sub.1 class comprises receptors characterized by a high affinity for serotonin. The 5-HT.sub.1 class is itself divided into a subclass of receptors whose pharmacological characteristics and regional distributions in the central nervous system are distinct.
Clinical studies of compounds having an agonist activity for the 5-HT.sub.1A subtype have demonstrated that the 5-HT.sub.1A agonists were effective in the treatment of anxiety (J. Clin. Psychiatry 1987, 48 (12 suppl.), 3-6; Int. Clin. Psychopharmacol. 1993, 8, 173-6), of depression (J. Clin. Psychopharmacol. 1990, 10 (3 suppl.), 67-76; J. Clin. Psychiatry 1991, 52, 217-20), of compulsive-obsessive disorders (Am. J. Psychiatry 1991, 148, 127-9), of panic attacks (J. Clin. Psychopharmacol. 1993, 13, 145-9), of sleeping disorders (Psychopharmacol. 1995, 117, 186-92) and of alcohol abuse (J. Clin. Psychopharmacol. 1989, 9, 379-80).
Studies in animals have demonstrated that the 5-HT.sub.1A agonists possess analgesic (Eur. J. Pharmacol. 1996, 295, 181-8), antiagressive (Neurosci. Biobehav. Rev. 1994, 18, 325-38) and antiemetic (Pharmacol. Biochem. Behav. 1989, 33, 627-31; Pharmacol. Biochem. Behav. 1995, 52, 571-5) properties. The compounds having a 5-HT.sub.1A agonist activity have also been reported as being capable of being useful in the treatment of sexual behavior disorders (Behavioural. pharmacol. 1995, 6, 276-82), for regulating food intake (Int. Clin. Psychopharmacol. 1994, 9, 7-17) and for regulating gastric secretion (J. Pharmacol. Exp. Ther. 1995, 272, 832-7). The antihypertensive action of the 5-HT.sub.1A agonists, via a central mechanism, is recognized (Trends Pharm. Sci. 1990, 11, 95-6; Fundam. Clin. Pharmacol. 1993, 7, 499-511); furthermore, the 5-HT.sub.1A agonists have shown neuroprotective properties in models of local and global ischemia in rodents (Brain Research 1993, 630, 10-20; Arch. Int. Pharmacodyn. Ther. 1995, 329, 347-59).
Studies in vitro also tend to implicate the 5-HT.sub.1A receptors in the stimulation of the proliferation of lymphocytes (INPHARMA.RTM., Aug. 26, 1995, 10; Life Sciences, 57, 2197-203).
Given the substantial therapeutic potential of compounds endowed with an agonist activity for the receptors of the 5-HT.sub.1A subtype, the discovery of new structures possessing 5-HT.sub.1A agonist properties is highly desirable. The applicant has discovered that several compounds derived from pyridin-2-yl-methylamine have an agonist activity towards the central 5-HT.sub.1A receptor.
The present invention therefore relates to new compounds corresponding to the general formula (I) ##STR2## in which: u represents a hydrogen atom or a methyl radical with the proviso that when u is a methyl radical then v and w represent a hydrogen atom; the proviso that when v represents a chlorine atom or a methyl radical then u and w represent a hydrogen atom; the proviso that when w represents a fluorine atom or a methyl radical then u and v represent a hydrogen atom; methyl radical; saturated aliphatic hydrocarbon radical containing 1 to 5 carbon atoms such as methyl, ethyl, propyl, butyl, pentyl, isopropyl, 1-methyl-ethyl, 1-methyl-propyl, 1-methyl-butyl, 2-methyl-propyl, 2-methyl-butyl or 3-methyl-butyl, 1-ethyl-propyl, 2-ethyl-propyl; difluoromethyl (--CHF.sub.2) or trifluoromethyl (--CF.sub.3) or 1-fluoro-1-ethyl (--CHFCH.sub.3) or 1,1-difluoro-1-ethyl (--CF.sub.2 CH.sub.3); containing 1, 2, 3 or 4 heteroatoms selected from nitrogen, oxygen and sulfur without, however, more than one oxygen and/or sulfur atom being present in the heterocycle A. The aromatic
REFERENCES:
patent: 5286735 (1994-02-01), Bonnaud
Favre H et al. Canadian Journal of Chemistry, 49(19) , 3075-3085, Oct. 1971 .
Bonnaud Bernard
Koek Wouter
Vacher Bernard
Huang Evelyn Mei
Pierre Fabre Medicament
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