发明名称 MATRIX METALLOPROTEINASE INHIBITORS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES
摘要 The present invention relates generally to bis-amide containing MMP inhibiting compounds, and more particularly to selectively deuterated bis-amide MMP-13 inhibiting compounds that exhibit increased stability or potency in relation to currently known MMP-13 inhibitors. Additionally, the present invention relates to methods for treating pain and inflammation in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
申请公布号 US2015274702(A1) 申请公布日期 2015.10.01
申请号 US201214433692 申请日期 2012.11.27
申请人 SUCHOLEIKI Irving;AQUILUS PHARMACEUTICALS, INC. 发明人 Sucholeiki Irving
分类号 C07D403/12;A61K45/06;C07D413/12;A61K31/505;C07D413/14;A61K31/538;A61K31/506;C07D239/28 主分类号 C07D403/12
代理机构 代理人
主权项 1. A compound according to Formula (I):wherein: R5 and R6 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl, wherein alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl are optionally substituted one or more times and wherein two substituents in the cycloalkyl-, aryl-, or heteroarylring when taken together with the nitrogen or carbon to which they are attached optionally complete an additional 3- to 8-membered ring containing carbon atoms and optionally containing one or more heteroatoms selected from O, SOx, or NR50 and which is optionally substituted or partially saturated; R1, R2, R3, R4 are independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, CD3, haloalkyl, fluoroalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl-alkyl, arylalkyl, heteroarylalkyl, COOR10, CONR10R11, SO2R10 and SO2NR10R11 wherein alkyl, haloalkyl, fluoroalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl-alkyl, arylalkyl, and heteroarylalkyl are optionally substituted one or more times; R10 and R11 are independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, CD3, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, fluoroalkyl, heterocycloalkylalkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and aminoalkyl, wherein alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, fluoroalkyl, heterocycloalkylalkyl, alkenyl, alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and aminoalkyl are optionally substituted, or R10 and R11 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NR50 and which is optionally substituted; R22 and R23 are independently selected from the group consisting of hydrogen, deuterium, halo, alkyl, deuteroalkyl, CD3, cycloalkyl, hydroxy, alkoxy, aryl, heteroaryl, arylalkyl, heteroarylalkyl, alkenyl, alkynyl, NO2, NR10R11, NR10NR10R11, NR10N═CR10RU, NR10SO2R11, CN, COOR10, and fluoroalkyl, wherein alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, and fluoroalkyl are optionally substituted; R50 is selected from the group consisting of hydrogen, deuterium, deuteroalkyl, CD3, alkyl, aryl, heteroaryl, C(O)R10, C(O)NR10R11, SO2R10 and SO2NR10R11, wherein alkyl, aryl, and heteroaryl are optionally substituted; x is selected from 0 to 2; or N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, tautomers, racemic mixtures, optically active enantiomers, diasterioisomers, or stereoisomers thereof.
地址 Winchester MA US