发明名称 Inhibitor compounds of semicarbazide-sensitive amine oxidases
摘要 Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
申请公布号 US9227967(B2) 申请公布日期 2016.01.05
申请号 US201113634732 申请日期 2011.03.14
申请人 Proximagen Limited 发明人 Evans David;Carley Allison;Stewart Alison;Higginbottom Michael;Savory Edward;Simpson Iain;Nilsson Marianne;Haraldsson Martin;Nordling Erik;Koolmeister Tobias
分类号 C07D471/04;C07D487/04;C07D498/08;C07D519/00;C07D491/08 主分类号 C07D471/04
代理机构 代理人 Mahoney Sean B.
主权项 1. A compound of formula (I) or a pharmaceutically acceptable salt, or N-oxide thereof: wherein R1 is phenyl or 6-membered heteroaryl, optionally substituted with one or more substituents selected from halogen, cyano, C1-4-alkyl, and halo-C1-4-alkyl; R2 is —B-Q-[R3]n or —B—R3, wherein n=1, 2, 3, or 4; B is a bond or C1-3-alkylene; Q is saturated or partially unsaturated monocyclic 5-7 membered heterocyclic or C5-7-cycloalkyl ring, either of which optionally comprises a bridge formed by an ethylene or propylene radical; when R2 is —B-Q-[R3]n, R3 is individually selected from hydrogen, halogen, hydroxyl, oxo, C1-4-alkyl, C1-4-alkoxy, hydroxy-C1-4-alkyl, cyano-C1-4-alkyl, amino-C1-4-alkyl, —NR4AR4B, —NR6C(O)OR5, —NR6C(O)NR4AR4B, —C(O)NR4AR4B, —C(O)R5, —C(O)OR5, and heteroaryl-C1-4-alkyl, and wherein any heteroaryl residue is optionally substituted with C1-4-alkyl; when R2 is —B—R3, R3 is selected from hydroxy-C1-4-alkyl; and R4A, R4B and R5 are each independently selected from hydrogen, C1-4-alkyl, hydroxy-C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, amino-C1-4-alkyl, C1-4-alkylamino-C1-4-alkyl, di(C1-4-alkyl)-amino-C1-4-alkyl and C1-4alkoxy-C1-4alkyl; or R4A and R4B together with the nitrogen to which they are attached form a cyclic amino group; R6 is hydrogen or C1-4-alkyl; and X is selected from the radicals of formulae (1-6) wherein the bond marked * is attached to R1— and the bond marked ** is attached to —R2: wherein Y is selected from hydrogen, hydroxyl, and —OCH3; Z is selected from hydrogen, fluorine, hydroxyl, and C1-4-alkoxy; and W is selected from hydrogen, and C1-4-alkyl.
地址 London GB