Indolizineacetic Acids and Their Therapeutic Use as Ligands of the CRTH2 Receptor

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United States of America Patent

APP PUB NO 20100093751A1
SERIAL NO

12520004

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, inter alia, respiratory diseases: wherein R.sup.1 is fluoro, chloro, cyano or trifluoromethyl; R.sup.2 is hydrogen, fluoro or chloro; R.sup.3 is hydrogen, fluoro, chloro or trifluoromethyl; X is --CH.sub.2--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2--; one of Y and Y.sup.1 is hydrogen and the other is --C(.dbd.O)R.sup.4, or --S(.dbd.O).sub.2R.sup.4, or --CR.sup.5R.sup.6OR.sup.7 or a heterocyclic group selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, furazanyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,2,4-triazinyl and 1,3,5-triazinyl any of which may be optionally substituted; R.sup.4 is an optionally substituted cyclic amino group having 5, 6 or 7 ring atoms which is linked to the carbonyl or sulfonyl through a ring nitrogen; R.sup.5 and R.sup.6 are independently hydrogen, (C.sub.1C.sub.3)alkyl, cyclopropyl, or R.sup.5 and R.sup.6 taken together with the carbon atom to which they are attached form a 3-6 membered cycloalkyl ring; and R.sup.7 is optionally substituted (C.sub.1-C.sub.6)alkyl or (C.sub.3-C.sub.6)cycloalkyl, ##STR00001##

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Patent Owner(s)

Patent OwnerAddress
ARGENTA DISCOVERY LIMITEDHARLOW ESSEX CM19 5TR

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Finch, Harry Essex, GB 95 958
Harrison, Trevor Essex, GB 2 17
Hynd, George Essex, GB 64 241
Kulagowski, Janusz Essex, GB 10 179
Montana, John Gary Essex, GB 69 638

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