Patent Number: 8,575,152

Title: Non-steroidal compounds useful as glucocorticoid receptor modulators

Abstract: This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: --R.sub.1 is --H or --(1-4C)alkyl; --R.sub.2 is --C(O)R.sub.15 or --S(O).sub.2R.sub.15; --R.sub.3 is --H, --(1-4C)alkyl or --OR.sub.16; --R.sub.4 is --H, --(1-4C)alkyl or --OR.sub.16; --R.sub.6 is --H or --C(R.sub.16)NOR.sub.16; --R.sub.7 is --H, -halogen, -cyano; --(1-6C)alkyl, --(2-6C)alkenyl or --(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; --R.sub.8 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(R.sub.16)NOR.sub.16; --C(O)N(R.sub.17).sub.2; --C(O)R18, --C(O)OR.sub.19, --NHC(O)R.sub.20, or --NHS(O).sub.2R.sub.21; --R.sub.9 is --H, -halogen, -cyano, or --(1-4C)alkyl, optionally substituted with -halogen; --R.sub.10 is --H or --(1-4C)alkyl; --R.sub.11 is --H; --R.sub.12 is --H, -cyano or --(1-4C)alkyl; --R.sub.13 is --H, --(1-4C)alkyl, -halogen or -formyl; --R.sub.14 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. ##STR00001##

Inventors: Plate; Ralf (Oss, NL), Jans; Christiaan Gerardus Johannes Maria (Oss, NL)

Assignee: Merck Sharp & Dohme B.V.

International Classification: A61P 5/44 (20060101); C07D 471/04 (20060101); A61K 31/55 (20060101); A61P 29/00 (20060101)

Expiration Date: 1/05/12017