发明名称 1,2,4-TRIAZOL-5-ONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
摘要 Described are compounds of Formula I;;which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
申请公布号 US2014296252(A1) 申请公布日期 2014.10.02
申请号 US201414214160 申请日期 2014.03.14
申请人 Deciphera Pharmaceuticals, LLC 发明人 Flynn Daniel L.;Brandt Gary E. L.;Kaufman Michael D.;Telikepalli Hanumaiah;Caldwell Timothy Malcolm;Samarakoon Thiwanka
分类号 C07D417/14;C07D405/14;C07D413/14;C07D401/14 主分类号 C07D417/14
代理机构 代理人
主权项 1. A compound of Formula I, or a pharmaceutically acceptable salt, enantiomer, stereoisomer, or tautomer thereof, wherein A is selected from the group consisting of C1-C6 alkyl, branched C3-C8alkyl, fluoroC1-C6alkyl wherein the alkyl is fully or partially fluorinated, C3-C8carbocyclyl, phenyl, 4-8 membered heterocyclic ring and heteroaryl, wherein each A moiety may be further substituted with one, two, or three R3 moieties; W is C5-C6heteroaryl, phenyl, —NHC(O)R6, —NHC(O)R7, —NHC(O)N(R8)R9 or —C(O)N(R8)R9, and wherein each C5-C6heteroaryl or phenyl is optionally substituted by one, two, or three R5 moieties; Q1 is CH or N; X1 and X2 are individually and independently hydrogen, or C1-C6 alkyl; Y is NR4 or O; Z is N or CR11; each R1 and R2 is individually and independently hydrogen, C1-C6 alkyl, deutero-C1-C6 alkyl wherein the alkyl chain is partially or completely deuterated, fluoroC1-C6alkyl wherein the alkyl is fully or partially fluorinated, hydroxyl, C1-C6 alkoxy, fluoroC1-C6alkoxy wherein the alkyl group is fully or partially fluorinated, or halogen; each R3 is individually and independently hydrogen, halogen, C1-C6 alkyl, fluoro-C1-C6 alkyl wherein the alkyl chain is partially or completely fluorinated, branched C3-C8 alkyl, C3-C8 cycloalkyl, C1-C6 alkoxy, fluoro-C1-C6 alkoxy wherein the alkyl chain is partially or completely fluorinated, branched C3-C6 alkoxy, hydroxyl, or cyano; R4 is hydrogen, C1-C6 alkyl, deutero-C1-C6 alkyl wherein the alkyl chain is partially or completely deuterated, or branched C3-C8 alkyl; each R5 is individually and independently hydrogen, C1-C6 alkyl, deutero-C1-C6 alkyl wherein the alkyl chain is partially or completely deuterated, branched C3-C8 alkyl, halogen, cyano, fluoro-C1-C6 alkyl wherein the alkyl chain is partially or completely fluorinated, —(CH2)m—C(O)NR8(R9), —(CH2)m—C(O)R7, —(CH2)m—OR8, —(CH2)m—NR8(R9), or —(CH2)m—R7, wherein each alkylene is optionally substituted with C1-C4 alkyl; Each R6 is individually and independently hydrogen, C1-C6 alkyl, branched C3-C8 alkyl, C3-C8 cycloalkyl, —(CH2)m—CN, —(CH2)m—OR8, —(CH2)m—NR8(R9), or —(CH2)m—R7, wherein each alkylene is optionally substituted with C1-C4 alkyl; each R7 is independently and individually selected from the group consisting ofand wherein the symbol (##) is the point of attachment to respective W, R5 or R6 moieties containing a R7 moiety; each R7 is optionally substituted with —(R10)p; each R8 and R9 is individually and independently hydrogen, C1-C6 alkyl, fluoro-C1-C6 alkyl wherein the alkyl chain is partially or completely fluorinated, or branched C3-C8 alkyl; each R10 is individually and independently C1-C6 alkyl, —(CH2)m—CN, —(CH2)m—OR3, —(CH2)m—NR8(R9), or —(CH2)m—C(O)—R6, wherein each alkyl or alkylene is optionally substituted with one or two C1-C6 alkyl; wherein each alkylene is optionally substituted with C1-C4 alkyl; R11 is hydrogen, C1-C6 alkyl, deutero-C1-C6 alkyl wherein the alkyl chain is partially or completely deuterated, or branched C3-C8 alkyl; each m is individually and independently 0, 1, 2, or 3; each n is individually and independently 0, 1, 2, or 3; each p is 0, 1, 2, or 3; and each q is 0, 1, or 2.
地址 Lawrence KS US
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