Piperazine derivatives useful as CCR5 antagonists

Details Piperazine derivatives useful as CCR5 antagonists Piperazine derivatives useful as CCR5 antagonists

2005-10-21

2010-11-02

Wang, Shengjun (Department: 1627)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S242000, C544S333000, C544S295000, C514S256000, C514S252120

Reexamination Certificate

active

07825121

ABSTRACT:
The use of CCR5 antagonists of the formulaor a pharmaceutically acceptable salt thereof, whereinR is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;R1is hydrogen or alkyl;R2is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl;R3is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl;R4, R5and R7are hydrogen or alkyl;R6is hydrogen, alkyl or alkenyl;for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

REFERENCES:
patent: 6391865 (2002-05-01), Baroudy et al.
patent: WO00/66558 (2000-11-01), None
patent: WO02/079157 (2002-10-01), None
West et al., Solid Solutions, Solid State Chemistry and its applications, John Wiley & Sons, 1986, pp. 364-365.
Vippagunta et al. Advanced Drug Defivery Reviews, 2001, vol. 48, 3-26.
Ulrich, Chapter 4 in Crystallization, Kirk-Othmer Encyclopedia of Chemical Technology, 2002.
International Search Report for International Application No. PCT/US2006/040636 dated Apr. 4, 2007.

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