Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-05-31
1998-06-09
Chang, Ceila
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514320, 546196, 546235, A61K 31445, C07D21132
Patent
active
057634580
ABSTRACT:
The present invention relates to novel 5-HT.sub.4 receptor ligands which are 1-(5-halo-4-aminophenyl) (C.sub.2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C.sub.1-4)alkyloxy or phenyl(C.sub.1-4)alkyloxy and optionally substituted at its 3-position with (C.sub.1-4)alkyloxy or substituted at its 2- and 3-positions together with methylenedioxy or ethylenedioxy and the highest numbered carbon of the (C.sub.2-6)alkan-1-one is substituted with di(C.sub.1-4)alkylamino, morpholin-1-yl or pyrrolidin-1-yl or optionally substituted piperidin-1-yl, piperidin-4-yl, azacyclohept-1-yl, individual isomers and mixtures of isomers and methods of using and making such derivatives.
REFERENCES:
patent: 3957823 (1976-05-01), Seebach et al.
patent: 4294841 (1981-10-01), Champseix et al.
patent: 5116846 (1992-05-01), Cain
Reynolds, "Prokinetic Agents: A Key in the Future of Gastroenterology", Gastroenterology Clinics of North America, 18: 437-457 (1989).
Corsi et al., "Pharmacological analysis of 5-hydroxtryptamine . . .", Br. J. Pharmacol., 104: 719-725 (1991).
Kaumann et al., "A 5-HT.sub.4 -like receptor in human right atrium ", Naunyn-Schmiedeberg's Arch. Pharmacol., 344: 150-159 (1991).
Frye et al., "Synthesis of 2-Aminobenzophenones . . . ", J. Org. Chem., 56: 3750-3752 (1991).
Fieser et al., Reagents for Organic Synthesis, John Wiley & Sons, 8: 294-295 (1980).
Fieser et al., Reagents for Organic Synthesis, John Wiley & Sons, 1: 280 (1967).
Oster et al., "Acetylations of Strongly Basic . . . ", Tetrahedron Lett., 24(18): 1851-1854 (1983).
Clark et al., Principles of Psychopharmacology, Academic Press, 166-167 (1970).
Tyers, "5-HT.sub.3 Receptors", in Whitaker-Azmita et al., ed., Ann. N. Y. Acad. Sci., 600: 195-196 (1990).
Turner et al., "Acylation of Ester Enolates . . . ", J. Org. Chem., 54: 4229-4231 (1989).
Morrison and Boyd, Organic Chemistry, 3rd ed., Allyn and Bacon, 853-854 (1973).
Blum et al., "Design and Synthesis of Novel Ligands . . . ", Bioorganic & Medicinal Chemistry Letters, 2(5): 461-466 (1992).
"Silver halide color photographic material . . . ", abstract of Japanese Patent Kokai No. 241,306/1993 (Kokai published Sep. 21, 1993), Chemical Abstracts, 120(18): 993 (left column), Abstract 231861u (2 May 1994).
Clark et al. "Synthesis and preliminary pharmacological evaluation of 2-benzyloxy substituted aryl ketones as 5HT4 receptor antagonists" Bioorg. Med. Chem. Lett. v. 4 pp. 2481-2484, 1994.
Whitaker-Azmita et al. "The neuropharmacology of serotonin" N.Y. Aca. Sci. v. 600, pp. 194-196, 1990.
Clark Robin Douglas
Eglen Richard Malcolm
Gardner John Otis
Jahangir Alam
Miller Aaron Bayne
Chang Ceila
Syntex (U.S.A.) Inc.
LandOfFree
1-phenylalkanone 5-HT.sub.4 receptor ligands does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 1-phenylalkanone 5-HT.sub.4 receptor ligands, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1-phenylalkanone 5-HT.sub.4 receptor ligands will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2199495