发明名称 5-oxo-ETE receptor antagonist compounds
摘要 The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.
申请公布号 US9464048(B2) 申请公布日期 2016.10.11
申请号 US201414324579 申请日期 2014.07.07
申请人 Florida Institute of Technology;The Royal Institution for the Advancement of Learning/McGill University 发明人 Powell William S.;Rokach Joshua
分类号 C07D209/12;C07D403/06;C07D209/18;C07C59/84;C07D209/08;C07D209/10;C07D209/24;C07D215/12;C07D235/08;C07D307/79 主分类号 C07D209/12
代理机构 Buchanan Ingersoll & Rooney P.C. 代理人 Buchanan Ingersoll & Rooney P.C.
主权项 1. A method for treating inflammation or a disease selected from asthma, allergic rhinitis, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), atopic dermatitis and acne, in a patient in need thereof said method comprising administering an effective amount of a compound of Formula II wherein X1, X2, X3 and X4 are independently selected from the group consisting of H, halogen, alkyl group, aralkyl group and OR5 wherein R5 is selected from the group consisting of H, acyl, alkyl, aralkyl, alkenyl, alkoxy, aryl, haloalkyl, cycloalkyl, haloalkoxy, heterocycloalkyl, cycloalkenyl and heterocycloalkenyl, any of which may be optionally substituted; and i) R1 is (CO)alkyl-COOH, said alkyl is straight or branched and optionally substituted with C3-7 cycloalkyl; R2 is alkyl, said alkyl is straight or branched and optionally substituted with OH, SH, COOR6, NR6R7, a C6-16 aryl, a C6-16 heterocycle, a C3-7 cycloalkyl, or a heterocyclic ring, wherein R6 and R7 are a C6-16 aryl, C6-16 heterocycle, C3-7 cycloalkyl, a heterocyclic ring or a hydrophobic group; R3 is alkyl; or ii) R1 is H R2 is alkyl, said alkyl is straight or branched and optionally substituted with OH, SH, COOR6, NR6R7, C6-16 aryl, C6-16 heterocycle, C3-7 cycloalkyl, or a heterocyclic ring, wherein R6 and R7are a C6-16 aryl, C6-16 heterocycle, C3-7 cycloalkyl, or a heterocyclic R3 is (CO)alkyl-COOH, said alkyl is straight or branched and optionally substituted with C3-7 cycloalkyl; or a pharmaceutically acceptable salt thereof.
地址 Melbourne FL US