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US 8,772,286 B2Granted
MK2 inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsTjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
Claims16
A compound of Formula I,
- or a pharmaceutically acceptable salt thereof, wherein
- A is CH or N;
- Y is a bond, or —C(O)NH—;
- X is a bond, —CH2—, —CH2CH2—;
- V is —CH2—, O, C(O), —CHF—, or —CF2—, with the proviso that if V is O, X is —CH2CH2— and that if V is C(O), X is —CH2;
- W is a bond or —CH2—;
- R1 is hydrogen or F;
- R2 is a (1-12C)heteroaryl or (6-10C)aryl both optionally substituted with one or more groups independently selected from R4;
- R3 is a hydrogen;
- (3-6C)cycloalkyl;
- (1-6C)alkyl, —(CH2)mOR5;
- —(CH2)mNR5R6;
- or —C(O)CH2NR5R6;
- R4 is taken from halogen;
- OH;
- SH;
- nitrile, nitro, NH2;
- (3-6C)cycloalkyl, (3-6C)cycloalkoxy, (1-6C)alkoxy or (1-6C)alkyl, all optionally substituted with one or more halogen;
- phenoxy;
- —O(CH2)mOR5, —O(CH2)mNR7R8, —OC(O)R7 with the proviso that R7 is not hydrogen, —O(1-12C)heteroaryl), —S(1-6C)alkyl);
- —S(3-6C)cycloalkyl)-;
- NR7R8;
- —NR9(CH2)mOR7, —NR9(CH2)mNR7R8;
- (1-6C)alkylcarbonyl;
- (3-6C)cycloalkylcarbonyl;
- —C(O)NR7R8;
- —C(O)NR9(CH2)mNR7R8, —C(O)NR9(CH2)mOR7, —C(O)OR7, —SO2(1-6C)alkyl), —SO2(3-6C)cycloalkyl);
- —O(1-6C)alkyl)O— where the oxygens are attached to the (1-12C)heteroaryl or (6-10C)aryl ring on two neighboring carbons;
- phenyl or (1-12C)heteroaryl;
- R5 is hydrogen (3-6C)cycloalkyl;
- or (1-6C)alkyl;
- R6 is hydrogen;
- (3-6C)cycloalkyl;
- (1-6C)alkyl;
- or (1-6C)alkylcarbonyl;
- R7 is hydrogen, (1-6C)alkyl or (3-6C)cycloalkyl;
- R8 is hydrogen;
- (3-6C)cycloalkyl;
- (1-6C)alkyl;
- or (1-6C)alkylcarbonyl;
- or
- R7 and R8 together with the nitrogen to which they are bonded in NR7R8 can form a 5-7-membered at least one nitrogen containing (4-6C)heterocyclyl ring which optionally contains one additional heteroatom selected from N, O or S;
- R9 is hydrogen;
- (1-6C)alkyl or (3-6)cycloalkyl;
- and
- m is 2 or 3.
43 more elements
Dependencies are inferred from the claim text.