Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-06-15
1998-09-15
Chang, Ceila
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546210, A61K 31445, C07D40106
Patent
active
058078720
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/US 92/10698 filed Dec. 16, 1992.
BACKGROUND
H.sub.3 receptor sites are known and are of current interest to those skilled in the art--for example, see: West, Jr. et al., "Biexponential H.sub.3 Histamine Receptor", Journal of Neurochemistry, Vol. 55, No. 5, pp. 1612-1616, 1990; West, Jr. et al., "Identification of Two H.sub.3 -Histamine Receptor Subtypes", Molecular Pharmacology, 38:610-613; and Korte et al., "Characterization and Tissue Distribution of H.sub.3 Histamine Receptors in Guinea Pigs by N.sup..alpha. -Methylhistamine", Biochemical and Biophysical Research Communications, Vol. 168, No. 3, pp. 979-986.
Arrang et al. in U.S. Pat. No. 4,767,778 (Issued Aug. 30, 1988) disclose a pharmaceutical composition containing a histamine derivative of the formula: ##STR2## wherein each of R.sub.1, R.sub.2, and R.sub.4, represents a hydrogen or a methyl, or R.sub.1 and R.sub.2 taken together represent a methylene, and R.sub.3 is a hydrogen, a methyl or a carboxy, with the proviso that R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are not simultaneously methyl groups. It is disclosed that the derivatives behave as complete agonists of the H.sub.3 receptors in rat brain and produce a maximal inhibition of release identical to that induced by histamine (approximately 60%). It is also disclosed that the histamine derivatives powerfully inhibit the release and synthesis of histamine by very selectively stimulating the H.sub.3 receptors. Consequently, according to Arrang et al., the derivatives are likely to decrease histaminergic transmission in the digestive tract and in the nervous, cardiovascular and immune systems. Arrang et al. disclose that the derivatives can be used in therapy as a drug having sedative effects, as a sleep regulator, anticonvulsant, regulator of hypothalamo-hypophyseal secretion, antidepressant, and modulator of cerebral circulation. According to Arrang et al., inhibition of the release of inflammation messengers in various allergic conditions (e.g., asthma) is expected to result from stimulation of the H.sub.3 receptors of the lung. It is further disclosed that the inhibition of release of gastric histamine is likely to exert antisecretory and antiulcerative effects. According to Arrang et al., modification of release of the messengers of immune responses is likely to modulate the latter responses.
EP 0 338 939 discloses compounds of the formula: ##STR3##
Derwent abstract 86-273706(42 for EP 0 197 840 discloses imidazole derivatives of the formula: ##STR4## wherein R.sub.1 is H, methyl or ethyl; R is H or R.sub.2 ; and R.sub.2 is 1-6C alkyl, piperonyl, 3-(benzimidazolon-1-yl)propyl, --CZ--NHR.sub.5 or a group (i): ##STR5## wherein n is 0-3; X is a bond, O, S, NH, CO, CH.dbd.CH or a group (ii): ##STR6## R.sub.3 is H, methyl, halo, CN, CF.sub.3 or COR.sub.4 ; R.sub.4 is 1-6C alkyl, 3-6C cycloalkyl or phenyl (optionally substituted by methyl or F); Z is O, S, NH, N-methyl or N--CN; and R.sub.5 is 1-8C alkyl, 3-6C cycloalkyl (optionally substituted by phenyl), 3-6C cycloalkyl(1-3C)alkyl, phenyl (optionally substituted by methyl, halo or CF.sub.3), phenyl(1-3C)alkyl, naphthyl, adamantyl or p-toluenesulphonyl. It is disclosed that these compounds are psychotropic agents. It is also disclosed that these compounds antagonise the histamine H3 receptors and increase the speed of cerebral histamine renewal.
Derwent abstract 90184730/24 for U.S. Pat. No. 4,925,851 discloses 2- or 4-(2-(1H-imidazol-1-yl)ethyl) piperidine compounds useful as antitumour agents for inhibiting lymphoma, sarcoma, myeloma and leukaemia. The compounds have the formula: ##STR7## wherein R is --CH.sub.2 (CH.sub.2).sub.m --Me, --CO--(CH.sub.2).sub.m --Me or --CO--CMe.sub.2 --R.sub.2 ; m is 2-18; R.sub.2 is H or Me; R.sub.1 is --(CH.sub.2).sub.n --R.sub.3; n is 0-13; R.sub.3 is H, i-Pr or t-Bu; and the floating group is at the 2- or 4- position; with the proviso that (1) the sum of C atoms in R.sub.1 does not exceed 13; and (2) the sum of C atoms in R and R.sub.1 does not exceed 25.
Derwent abstract 90-
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West Jr. et al., Journal of Neurochemistry, vol. 55, No. 5, pp. 1612-1616 (1990).
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Green Michael J.
Shih Neng-Yang
Chang Ceila
Jeanette Henry C.
Schering Corporation
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