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AssigneeN.V. Organon
InventorsRalf Plate, Christiaan Gerardus Johannes Maria Jans
Estimating the term…
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.
A compound according to general formula I:
A compound selected from the group of
6-7. (canceled)
A method for treating a disease, condition or disorder responsive to glucocorticoid receptor activity, wherein the disease, condition or disorder is selected from the group consisting of rheumatic disease, dermatological disease, allergic disorder, pulmonary condition and immune and inflammatory disease, the method comprising administering to an individual a therapeutically effective amount of the compound of formula I or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.