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US 8,133,885 B2Granted
Non steroidal glucocorticoid receptor modulators
AssigneeMerck Sharp & Dohme Corp.
InventorsRalf Plate, Guido Jenny Rudolf Zaman, Pedro Harold Han Hermkens, Christiaan Gerardus Johannes Maria Jans, Rogier Christian Buijsman, Adrianus Petrus Antonius De Man, Paolo Giovanni Martino Conti, Scott James Lusher, Willem Hendrik Abraham Dokter
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Abstract
The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
Claims11
A compound according to formula I:
- or a pharmaceutically acceptable salt thereof, wherein
- 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, —C(H)NOR16;
- R7 is H, halogen or cyano;
- or R7 is (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl, all three optionally substituted with OH, halogen or NH2;
- or R7 is —C(H)NOR16, —OR16, —C(O)OR16 or —C(O)R16;
- R8 is cyano;
- or R8 is (1-6C) alkyl, (2-6C)alkenyl, (2-6C)alkynyl or —O(1-6C)alkyl, all substituted with amino, hydroxyl or halogen;
- or R8 is (hetero)aryl, optionally substituted with cyano, halogen, (1-4C)alkyl, (1-4C)alkoxy or (1-4C)alkoxy(1-4C)alkyl;
- or R8 is —C(H)NOR16, —C(O)NHR17, —C(O)R18, —C(O)OR19, or —C(1-4C)alkylNOR21;
- 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, (2-6C)alkenyl, C(O)R21 or (hetero)aryl;
- R15 is H;
- or R15 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, —O(2-6C)alkyl, —O(2-6C)alkenyl or —O(2-6C)alkynyl, all optionally substituted with one or more OH, halogen, cyano or (hetero)aryl;
- or R15 is (hetero)aryl, optionally substituted with (1-4C)alkyl, halogen, cyano, nitro or amino;
- or R15 is NH2, (di)(1-4C)alkylamino, (1-4C)alkyl(1-4C)alkoxyamine, (1-4C)alkylthio(1-4C)alkyl or (1-4C)alkoxy(1-4C)alkyl;
- each R16 independently is H, (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl;
- R17 is H, (1-4C)alkoxy or (3-6C)cycloalkyl;
- or R17 is (1-6C)alkyl, optionally substituted with halogen;
- or R17 is (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1-4C)alkoxy;
- R18 is H, NH2, —C(O)R21 or —S(1-4C)alkyl;
- or R18 is (1-4C)alkyl, optionally substituted with OH, halogen or cyano;
- R19 is H or (1-6C)alkyl, optionally substituted with OH or halogen, and
- each R21 independently is H or (1-6C)alkyl.
28 more elements
Dependencies are inferred from the claim text.