Indole, azaindole and related heterocyclic N-substituted...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S159000

Reexamination Certificate

active

08039486

ABSTRACT:
This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formulawherein:Z isQ is selected from the group consisting ofm is 2;A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and—W— is

REFERENCES:
patent: 3135794 (1964-06-01), Archer
patent: 3188313 (1965-06-01), Archer
patent: 5023265 (1991-06-01), Scherlock et al.
patent: 5124327 (1992-06-01), Greenlee et al.
patent: 5424329 (1995-06-01), Boschelli et al.
patent: 6008231 (1999-12-01), Lebaut et al.
patent: 6232327 (2001-05-01), Nickel et al.
patent: 6344467 (2002-02-01), Lebaut et al.
patent: 6469006 (2002-10-01), Blair et al.
patent: 6476034 (2002-11-01), Wang et al.
patent: 6573262 (2003-06-01), Wallace et al.
patent: 6632819 (2003-10-01), Wang et al.
patent: 6919344 (2005-07-01), Lebaut et al.
patent: 7807671 (2010-10-01), Wang et al.
patent: 2003/0207910 (2003-11-01), Wang et al.
patent: 2004/0063744 (2004-04-01), Wang et al.
patent: 2005/0075364 (2005-04-01), Yeung et al.
patent: 0530907 (1993-03-01), None
patent: WO 91/09849 (1991-07-01), None
patent: WO 93/01181 (1993-01-01), None
patent: WO 95/04742 (1995-02-01), None
patent: WO 96/11929 (1996-04-01), None
patent: WO 96/18628 (1996-06-01), None
patent: WO 99/51224 (1999-10-01), None
patent: WO 02/085301 (2002-10-01), None
patent: WO 03/092695 (2003-11-01), None
patent: WO 04/000210 (2003-12-01), None
patent: WO 2004/011425 (2004-02-01), None
patent: WO 2005/090367 (2005-09-01), None
Chemical Abstracts Service—Proceedings of the National Academy of Sciences of the USA, 1963, v50(4), pp. 679-686 Okubo, S. et al, “Separation of the transforming and viral deoxyribonucleic acids of a transducing bacteriophage ofBacillus subtilis”.
M. Font, et al., “Indoles and Pyridazino[4,5-b]indoles as Nonnucleoside Analog Inhibitors of HIV-1 Reverse Transcriptase,” Eur. J. Med. Chem., 30, pp. 963-971, 1995.
D.L. Romero, et al., Bis(heteroaryl)pipera;zine (BHAP) Reverse Transcriptase Inhibitors: Structure-Activity Relationships of Novel Substituted Indole Analogues and the Identification of 1-[(5-Methanesulfonamido-1H-indole-2-yl)-carbonyl]-4-[3-[(1-methylethyl)amino]-pyridinyl]piperazine Monomethanesulfonate (U-90152S), a Second-Generation Clinical Candidate, J. Med. Chem., 36, pp. 1505-1508, 1993.
S.D. Young, et al., “2-Heterocyclic Indole-3-Sulfones as Inhibitors of HIV-1 Reverse Transcriptase,” Bioorganic & Medicinal Chemistry Letters, 5(5), pp. 491-496, 1995.
M.J. Genin, et al., “Synthesis and Bioactivity of Novel Bis(Heteroaryl)Piperazine (BHAP) Reverse Transcriptase Inhibitors: Structure-Activity Relationships and Increased Metabolic Stability of Novel Substituted Pyridine Analogs,” J. Med. Chem., 39, pp. 5267-5275, 1996.
R. Silvestri, et al., “Synthesis and biological evaluation of 5H-indole[3,2-b][1,5]benzothiazepine derivatives, designed as conformationally constrained analogues of the human immunodeficiency virus type 1 reverse transcriptase inhibitor L737,126,” Antiviral Chemistry & Chemotherapy, 9, pp. 139-148,1998.
A. Fredenhagen, et al., “Semicochliodinol A and B: Inhibitors of HIV-1 Protease and EGF-R Protein Tyrosine Kinase Related to Asterriquinones Produced by the FungusChrysosporium merdarium,” Journal of Antibiotics, 50(5), pp. 395-401, 1997.
M. Kato, et al., “New 5-HT3(Serotonin-3) Receptor Antagonists. IV. Synthesis and Structure-Activity Relationships of Azabicycloalkaneacetamide Derivatives,” Chem. Pharm. Bull., 43(8), pp. 1351-1357, 1995.
V. Levacher, et al., “Broadening in the Scope of NADH Models by Using Chiral and Non-Chiral Pyrrolo[2,3-b]Pyridine Derivatives, ”Tetrahedron, 47(3), pp. 429-440, 1991.
Romero, D.L., “Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors,” J. Med. Chem., 1994, vol. 37, No. 7, pp. 999-1014.

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