Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1987-03-12
1989-04-25
Hollrah, Glennon H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544363, 546157, 546158, A61K 31495, C07D40302
Patent
active
048248401
ABSTRACT:
Carbostyril derivatives having antihistaminic action and central nervous controlling action are useful as antihistaminic agents or central nervous controlling agents. The derivatives are represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a phenylalkyl group, an alkylene group containing 1 to 4 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a phenyl group; R.sup.3 is a hydrogen atom, a hydroxy group, an alkyl group having 1 to 4 carbon atoms, an alkanoyloxy group having 1 to 4 carbon atoms or a 3,4,5-trimethoxybenzoyloxy group; R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.5 is a cycloalkyl group having 3 to 8 carbon atoms, a phenyl group (which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, alkyl groups having 1 to 4 carbon atoms and alkoxy groups having 1 to 4 carbon atoms), an alkyl group having 1 to 4 carbon atoms (having one substituted group such as a hydroxy group, a phenyl group or an alkanoyloxy group having 1 to 4 carbon atoms), an alkanoyl group having 1 to 4 carbon atoms or benzoyl group; X is a halogen atom; n is 0, or an integer of 1 or 2; Q is an integer of 2 or 3, l and m are respectively an integer of 0 to 1-6, but the sum of l and m should not exceed 6; the carbon-carbon bond at the 3- and 4-positions in the carbostyril skeleton is a single or double bond and; the substituted position of the side chain of ##STR2## is any one of the 4-, 5-, 6-, 7- or 8-positions.
REFERENCES:
patent: 3362956 (1968-01-01), Archer
patent: 3511841 (1970-05-01), Archer
patent: 3654277 (1972-04-01), Winter et al.
patent: 3703522 (1972-11-01), Plostnicks
patent: 3706749 (1972-12-01), Plostnicks
patent: 3810896 (1974-05-01), Witte et al.
patent: 3810898 (1974-05-01), Witte et al.
patent: 3919226 (1975-11-01), Thiel et al.
patent: 3932411 (1976-01-01), Braun et al.
patent: 3936459 (1976-02-01), Kato et al.
patent: 3940397 (1976-02-01), Wade et al.
patent: 3981864 (1976-09-01), Tanaka et al.
patent: 3983121 (1976-09-01), Murthi et al.
patent: 3994900 (1976-11-01), Krapcho et al.
patent: 4026895 (1977-05-01), Tanaka et al.
patent: 4032528 (1977-06-01), Hardtmann
patent: 4060526 (1977-11-01), Shetty
patent: 4110449 (1978-08-01), Wade et al.
patent: 4117228 (1978-09-01), Tanaka et al.
patent: 4147869 (1979-04-01), Nakagawa et al.
patent: 4166116 (1979-08-01), Coutts et al.
patent: 4210753 (1980-07-01), Tominaga et al.
patent: 4234584 (1980-11-01), Lattrell et al.
patent: 4234585 (1980-11-01), Winter et al.
patent: 4256890 (1981-03-01), Nakagawa et al.
"Chemical Abstracts", vol. 95, 1981, cols. 95:25121q and 95:25127w.
Principles of Medicinal Chemistry, (Foye Ed. 1974), pp. 454-456.
Cutting's Handbook of Pharmacology, (1972), pp. 312-325.
Petigara et al., J. Med. Chem., 11 (2), 332-336.
Zejc et al., Pol. J. Pharmacol. Pharm., 1976, 28, 369-374.
Chem. Abstract, 112035q.
Fielden et al., Journal of Medicinal Chemistry, 1973, vol. 16, No. 10, 1124-1128.
Pp. 47-53, 153-197 and 590-623 of The Pharmacological Basis of Therapeutics, (Goodman and Gilman Ed., 1975).
Kazuyuki Nakagawa et al.; Derivatives of 3,4-Dihydrocarbostyril As .beta.-Adrenergic Blocking Agents; Journal of Medicinal Chemistry, 1974, vol. 17, No. 5, pp. 529-533.
Banno Kazuo
Fujioka Takafumi
Nakagawa Kazuyuki
Oshiro Yasuo
Hollrah Glennon H.
Otsuka Pharmaceutical Co. Ltd.
Turnipseed James H.
LandOfFree
Carbostyril derivatives and pharmaceutical preparations containi does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Carbostyril derivatives and pharmaceutical preparations containi, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Carbostyril derivatives and pharmaceutical preparations containi will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1195956