发明名称 3-aryl-2-((arylamino)methyl)quinazolin-4-(3H)-ones
摘要 The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3Kδ, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3Kδ, are disclosed.
申请公布号 US9216985(B2) 申请公布日期 2015.12.22
申请号 US201414228876 申请日期 2014.03.28
申请人 SciFluor Life Sciences, Inc. 发明人 Askew Ben C.;Furuya Takeru
分类号 C07D487/04;C07D473/34;C07D471/04 主分类号 C07D487/04
代理机构 Cooley LLP 代理人 Cooley LLP ;Elrifi Ivor R.;Erlacher Heidi A.
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein X1 is selected from N, CH, CF, CCF3, CCHF2, and CCH2F;X2 is N or CH;R1 is (CX3AX4A)s—(O)v—(CX3BX4B)t—(O)w—(CX3CX4C)u—(O)x—X5; X3A, X3B, X3C, X4A, X4B, and X4C are each independently selected from H and F; X5 is selected from H, F, CF3, CHF2, CH2F, OCF3, OCHF2, OCH2F, OCH2CF3, OCH2CHF2, and OCH2CH2F; s, t, and u are each independently selected from 0, 1, 2, 3, 4, 5, 6, and 7; v, w, and x are each independently selected from 0 and 1; R2 is Cl or F; each X6 is independently (CX7AX8A)e—(O)h—(CX7BX8B)f—(O)i—(CX7CX8C)g—(O)j—X9; X7A, X7B, X7C, X8A, X8B, and X8C are each independently selected from H and F; X9 is selected from H, F, CF3, CHF2, CH2F, OCF3, OCHF2, OCH2F, OCH2CF3, OCH2CHF2, and OCH2CH2F; e, f, and g are each independently selected from 0, 1, 2, 3, 4, 5, 6, and 7; h, i, and j are each independently selected from 0 and 1; and z is selected from 0, 1, and 2, provided that when X1 and X2 are each N and z is 0, then R1 comprises at least one F atom; and that when X1 and X2 are each N and R2 is Cl, then z is 1 or 2 and X9 is selected from CF3, CHF2, CH2F, OCF3, OCHF2, OCH2F, OCH2CF3, OCH2CHF2, and OCH2CH2F, and provided that R1 does not contain a total number of more than 8 atoms of carbon and oxygen and R1 does not contain adjacent oxygen atoms, and that each X6 does not contain a total number of more than 8 atoms of carbon and oxygen and X6 does not contain adjacent oxygen atoms.
地址 Cambridge MA US