Cyclopropyl compounds as ccr5 antagonists

Details Cyclopropyl compounds as ccr5 antagonists Cyclopropyl compounds as ccr5 antagonists

2003-12-12

2009-08-04

Dentz, Bernard (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S304000, C514S329000, C546S020000, C546S126000, C546S224000, C546S234000

Reexamination Certificate

active

07569579

ABSTRACT:
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

REFERENCES:
patent: 6331541 (2001-12-01), Ko et al.
patent: WO00/39125 (2000-07-01), None
patent: WO0038680 (2000-07-01), None
Finke et al., Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-aryl-1-'N-(methyl)-N-(phenylsulfonyl)amino)-4-(piperidin-1-y1) butanes, Bioorganic and Medicinal Chemistry Letters 11(2):265-270 (2001).
Finke et al., Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-(N-(methyl)-N-(phenylsulfonyl)amino)-2-(phenyl)-4-(4-(substituted)piperidin-1-yl)butanes, Bioorganic and Medicinal Chemistry Letters 11(18):2469-2473(2001).
Finke et al., Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-benzyloxycarbonyl)amino)piperidin-1-yl)butanes, Bioorganic and Medicinal Chemistry Letters 11:2475-2479 (2001).
Dorn et al., Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes, Bioorganic and Medicinal Chemistry Letter 11(2):259-264 (2001).
Maeda et al., The current status of the challenges in, the development of CCR5 inhibitors as therapeutics for HI infection, Current Opinion in Pharmacology 4(5):447-452 (2004).
Kumar et al., Pharmacokinetics and Interactions of a Novel Antagonist of Chemokine Receptor 5 (CCR5) with Ritonavir in Rats and Monkeys: Role of CYP3A and P-glycoprotein, J. of Pharmacology and Experimental therapeutics 304(3):1161-1171(2003).
Bonnaud et al., 1-Aryl-2-(aminomethyl))cyclopropanecarboxylic Acid Derivatives. A New Series of Potential Antidepressants, J. Med. Chem 30:318-325 (1987).

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