Piperidine derivatives useful as CCR5 antagonists

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United States of America Patent

PATENT NO 6602885
APP PUB NO 20030004185A1
SERIAL NO

10010481

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The use of CCR5 antagonists of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein ##STR2## R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is H, alkyl or alkenyl; R.sup.2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R.sup.3 is optionally substituted phenyl, heteroaryl or naphthyl; R.sup.4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 --O-alkyl, --CH.sub.2 C(O)--O-alkyl, --CH.sub.2 C(O)NH.sub.2, --CH.sub.2 C(O)--NHalkyl or --CH.sub.2 C(O)--N(alkyl).sub.2 ; R.sup.19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R.sup.5, R.sup.13, R.sup.14, R.sup.15 and R.sup.16 are hydrogen or alkyl 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.

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Patent Owner(s)

Patent OwnerAddress
MERCK SHARP & DOHME CORPONE MERCK DRIVE P O BOX 100 WHITEHOUSE STATION NJ 08889

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Baroudy, Bahige M Westfield, NJ 9 162
Clader, John W Cranford, NJ 70 1194
Josien, Hubert B Jersey City, NJ 38 421
Laughlin, Mark A Edison, NJ 11 202
McCombie, Stuart W Caldwell, NJ 45 660
McKittrick, Brian A Bloomfield, NJ 46 1051
Miller, Michael W Westfield, NJ 86 1116
Neustadt, Bernard R West Orange, NJ 80 1209
Palani, Anandan Kenilworth, NJ 108 651
Steensma, Ruo Weehawken, NJ 12 395
Tagat, Jayaram R Westfield, NJ 21 410
Vice, Susan F Mountainside, NJ 16 427

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