Non-steroidal compounds useful as glucocorticoid receptor modulators

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United States of America Patent

PATENT NO 8575152
APP PUB NO 20080188459A1
SERIAL NO

12065241

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or —(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, —(1-4C)alkyl or —OR16; —R4 is —H, —(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; —(1-6C)alkyl, —(2-6C)alkenyl or —(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; —(1-6C)alkyl, —(2-6C)alkenyl, —(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, —(1-4C)alkyl, —(1-4C)alkoxy, —(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or —(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or —(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or —(1-4C)alkyl; —R13 is —H, —(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, —(1-4C)alkyl or -(hetero)aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used for treating inflammatory diseases.

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Patent Owner(s)

Patent OwnerAddress
MERCK SHARP & DOHME B V2031 BN HAARLEM

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Jans, Christiaan Gerardus Johannes Maria Oss, NL 22 124
Plate, Ralf Oss, NL 11 13

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