Naphthyridine derivatives having inhibitory activity against...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

active

07919623

ABSTRACT:
A compound having HIV Integrase Inhibitory activity of the formula:(wherein:R1is optionally substituted aralkyl;R2and R3are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for “optionally substituted” is a noncyclic group);R4is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in “optionally substituted formylamino”, “optionally substituted carbamoyl” and “optionally substituted amino” may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.

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Andrea Savarino, A Historical Sketch of the Discovery and Development of HIV-1 Integrase Inhibitors, 15 Expert Opin. Investig. Drugs 1507 (2006).
Fatima Zouhiri, et al, Structure-Activity Relationships and Binding Mode of Styrylquinolines as Potent Inhibitors of HIV-1 Integrase and Replication of HIV-1 in Cell Culture, 43 J Med. Chem. 1533 (2000).
Ya-Qiu Long, et al, Rational Design and Synthesis of Novel Dimeric Diketoacid-Containing Inhibitors of HIV-1 Integrase: Implication for Binding to Two Metal Ions on the Active Site of Integrase, 47 J Med. Chem. 2561 (2004).

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