Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-09-20
2010-06-29
Hui, San-ming (Department: 1628)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S138000
Reexamination Certificate
active
07745459
ABSTRACT:
A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided.The present invention relates to a quinolizinone compound represented by the following formula [I]wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing same as an active ingredient.The compound of the present invention has an HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compounds can become a more effective anti-HIV agent. Since the compound has a high inhibitory activity specific for integrases, the compound can provide a safe pharmaceutical agent for human with a fewer side effects.
REFERENCES:
patent: 4650804 (1987-03-01), Kitaura et al.
patent: 6624159 (2003-09-01), Anderson et al.
patent: 2002/0025960 (2002-02-01), Bundy et al.
patent: 2004/0229903 (2004-11-01), Fukumoto et al.
patent: 2005/0054645 (2005-03-01), Miyazaki et al.
patent: 2005/0239819 (2005-10-01), Satoh et al.
patent: 2006/0052361 (2006-03-01), Miyazaki et al.
patent: 0 157 346 (1990-01-01), None
patent: 1 437 354 (2004-07-01), None
patent: 1 564 210 (2005-08-01), None
patent: B-6-49701 (1985-03-01), None
patent: 5-503709 (1991-05-01), None
patent: A-2004-502770 (2001-06-01), None
patent: A-2004-502771 (2001-06-01), None
patent: WO 91/16894 (1991-11-01), None
patent: WO 00/17197 (1999-09-01), None
patent: WO 99/62513 (1999-12-01), None
patent: WO 01/00578 (2001-01-01), None
patent: WO 02/04444 (2002-01-01), None
patent: WO 02/04445 (2002-01-01), None
patent: WO 03/029253 (2003-04-01), None
patent: WO 2004/019933 (2004-03-01), None
patent: WO 2004/024078 (2004-03-01), None
patent: WO 2004/035576 (2004-04-01), None
patent: WO 2004/035577 (2004-04-01), None
patent: WO 2004/039803 (2004-05-01), None
patent: WO 2004/046115 (2004-06-01), None
Carey FA and Sundberg RJ, “Advanced Organic Chemistry, 3rd Ed., Part A: Structure and Mechanisms,” Plenum Press, New York, 1990.
Kawasuji T, Yoshinaga T, Sato A, Yodo M, Fujiwara T, and Kiyama R, “A platform for designing HIV integrase inhibitors. Part 1: 2-Hydroxy-3-heteroaryl acrylic acid derivatives as novel HIV integrase inhibitor and modeling of hydrophilic and hydrophobic pharmacophores,” Bioorganic & Medicinal Chemistry, Dec. 2006, 14(24), 8430-8445.
Maurin C, Bailly F, and Cotelle P, “Structure-activity relationships of HIV-1 integrase inhibitors—enzyme-ligand interactions,” Current Medicinal Chemistry, Sep. 2003, 10(18), 1795-1810.
Zouhiri F, Mouscadet JF, Mekouar K, Desmaële D, Savouré D, Leh H, Subra F, Le Bret M, Auclair C, and d'Angelo J, “Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture,” Journal of Medicinal Chemistry, Apr. 2000, 43(8), 1533-1540.
Guidelines for the Use of Antiretroviral Agents in HIV-Infected Adults and Adolescent, pp. i-iii and 1-111, (Aug. 13, 2001).
Göschke, Richard et al., the Nonchiral Bislactin Diethoxy Ether as a Highly Stereo-Inducing Synthon for Sterically Hindered, γ-Branched α-Amino Acids: A Practical, Large-Scale Route to an Intermediate of the Novel Renin Inhibitor Aliskiren, Helvetica Chemica Acta, vol. 86, pp. 2848-2870 (2003).
Vincent, K.A., et al. Characterization of Human Immunodeficiency Virus Type I Integrase Expressed inEschericia coliand Analysis of Variants and Amino-Terminal Mutations, J. Virol. 67:425-437 (1993).
Evans, David A., Total Synthesis of the Polyether Antibiotic Ionomycin, Journal of the American Chemical Society, 1990, 112, 5290-5313.
Evans, D.A., et al., Asymmetric Alkylation Reactions of Chiral Imide Emolates. A Practical Approach to the Enantioselective Synthesis of α-Substituted Carboxylic Acid Derivatives, Journal of the American Chemical Society, 1982, 104, 1737-1739.
PCT International Search Report (PCT/JP2005/017556) dated Oct. 25, 2005.
Aramaki Hisateru
Inoue Masafumi
Kawakami Hiroshi
Matsuzaki Yuji
Nakamura Hiroshi
Finnegan Henderson Farabow Garrett & Dunner LLP
Hui San-ming
Japan Tobacco Inc.
Zarek Paul
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