Indolizine Derivatives as Ligands of the Crth2 Receptor

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United States of America Patent

APP PUB NO 20080306109A1
SERIAL NO

12065963

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R.sub.1, R.sub.2. R.sub.3 and R.sub.4 each independently are hydrogen, C.sub.1-C.sub.6alkyl, fully or partially fluorinated C.sub.1-C.sub.6alkyl, halo, --S(O).sub.nR.sub.10, --SO.sub.2N(R.sub.10).sub.2, --N(R.sub.10).sub.2, --C(O)N(R.sub.10).sub.2, --NR.sub.10C(O)R.sub.9, --CO.sub.2R.sub.10, --C(O)R.sub.9, --NO.sub.2, --CN or --OR.sub.11; wherein each R.sub.9 is independently C.sub.1-C.sub.6alkyl, aryl, heteroaryl; R.sub.10 is independently hydrogen, C.sub.1-C.sub.6alkyl, aryl, or heteroaryl; R.sub.11 is hydrogen, C.sub.1-C.sub.6alkyl, fully or partially fluorinated C.sub.1-C.sub.6alkyl or a group --SO.sub.2R.sub.10; n is 0, 1 or 2; R.sub.5 is C.sub.1-C.sub.6alkyl, fully or partially fluorinated C.sub.1-C.sub.6alkyl, C.sub.1-C.sub.6alkenyl, C.sub.1-C.sub.6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R.sub.6 is hydrogen, C.sub.1-C.sub.6alkyl or fully or partially fluorinated C.sub.1-C.sub.6alkyl; R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-C.sub.6alkyl, or R.sub.7 and R.sub.8 together with the atom to which they are attached form a cycloalkyl group; and X is --CHR.sub.6--, --S(O).sub.n--, --C(O)--, --NR.sub.6SO.sub.2-- or --SO.sub.2NR.sub.6- wherein n is 0, 1 or 2.

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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
Arienzo, Rosa Essex, GB 8 43
Blaney, Paul Essex, GB 6 83
Cramp, Michael Colin Essex, GB 12 40
Finch, Harry Essex, GB 95 958
Griffon, Yann Essex, GB 5 29
Harrison, Trevor Keith Essex, GB 6 29
Hynd, George Essex, GB 64 241
Middlemiss, David Essex, GB 43 328
Montana, John Gary Hertfordshire, GB 69 638
Ray, Nicholas Charles Essex, GB 60 328

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