发明名称 MK2 INHIBITORS
摘要 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.
申请公布号 US2016159800(A1) 申请公布日期 2016.06.09
申请号 US201514795085 申请日期 2015.07.09
申请人 Merck Sharp & Dohme B.V. 发明人 Barf Tjeerd Andries;Oubrie Arthur;Schultz-Fademrecht Carsten;Zwart Eduard Willem;Hoogenboom Niels;De Wilde Sander Martijn;Kaptein Allard
分类号 C07D471/20;C07D498/20 主分类号 C07D471/20
代理机构 代理人
主权项 1. 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.
地址 Haarlem NL