发明名称 NOVEL 2-PIPERIDIN-1-YL-ACETAMIDE COMPOUNDS FOR USE AS TANKYRASE INHIBITORS
摘要 The present invention provides for compounds of formula (I):;;wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
申请公布号 US2015025070(A1) 申请公布日期 2015.01.22
申请号 US201214154161 申请日期 2012.07.13
申请人 Cheung Atwood Kim;Chin Donovan Noel;Fan Jianmei;Miller-Moslin Karen Marie;Shultz Michael David;Smith Troy D.;Tomlinson Ronald Charles;Toure Bakary-Barry;Visser Michael Scott 发明人 Cheung Atwood Kim;Chin Donovan Noel;Fan Jianmei;Miller-Moslin Karen Marie;Shultz Michael David;Smith Troy D.;Tomlinson Ronald Charles;Toure Bakary-Barry;Visser Michael Scott
分类号 C07D491/052;C07D493/04;C07D401/12 主分类号 C07D491/052
代理机构 代理人
主权项 1. A compound according to formula (I) wherein: X is NH or O; Y is N or CH; R1a and R1b are each independently C1-3 alkyl; or R1a and R1b are joined together with the atoms to which they are attached forming an optionally substituted C5-7 cycloalkenyl ring, an optionally substituted 3,6-dihydro-2H-pyranyl ring, or an optionally substituted 1,2,3,6-tetrahydropyridinyl ring, wherein said C5-7 cycloalkenyl, 3,6-dihydro-2H-pyranyl, and 1,2,3,6-tetrahydropyridinyl are each optionally substituted with one to three substituents each independently selected from the group consisting of: halo, hydroxy, C1-3 alkyl, and benzyl; R2 is H or C1-3 alkyl; R3 is hydrogen, C1-3 haloalkyl, C3-6 alkynyl, or C1-6 alkyl optionally substituted with one substituent selected from the group consisting of: methoxy, cyano, C3-5 cycloalkyl, optionally substituted phenyl, optionally substituted 5-10 membered heteroaryl, and 5-6 membered heterocyclyl, wherein said phenyl, 5-10 membered heteroaryl and 5-6 membered heterocycloalkyl are each optionally substituted with one or two substituents each independently selected from the group consisting of: halo, C1-3 alkoxy, cyano, and morpholinyl-S(O)2—; and R4 is hydrogen, L is C(O),and R5 is optionally substituted phenyl, optionally substituted 5-6 membered heteroaryl, optionally substituted 2,3-dihydrobenzofuran-6-yl, optionally substituted benzyl[1,3]dioxol-5-yl; optionally substituted 1,2,3,4-tetrahydro-quinolin-1-yl, or optionally substituted 1,2,3,4-tetrahydro-isoquinolin-2-yl, wherein each R5 is optionally substituted with one or two substituents each independently selected from the group consisting of: (a) halo,(b) hydroxy,(c) C1-6 alkyl,(d) C1-3 haloalkyl,(e) C1-3 alkoxy optionally substituted with one methoxy, C3-5 cycloalkyl, or phenyl,(f) C1-3 haloalkoxy,(g) C3-6 alkynyloxy,(h) tetrahydropyranyl-O—, and(i) C1-3 alkyl-C(O)NH—; or R4 is hydrogen, L is absent, and R5 is optionally substituted benzo[d]isoxazol-3-yl, optionally substituted 1H-indazol-3-yl, or optionally substituted 1,3-dihydro-benzimidazol-2-one-1-yl, wherein each R5 is optionally substituted with one or two substituents each independently selected from the group consisting of: halo, hydroxy, C1-6 alkyl, C1-3 haloalkyl, and C1-3 alkoxy; or R4 and L-R5, wherein L is C(O), are joined together with the atoms to which they are attached forming an optionally substituted indan-1-one-2-yl group or an optionally substituted 3,4-dihydro-2H-naphthalen-1-one-2-yl each of which are attached to the piperidine ring of formula (I) through spiro carbon 4 and are optionally substituted with one to three substituents each independently selected from the group consisting of: halo and C1-6 alkoxy; or a pharmaceutically acceptable salt thereof.
地址 Cambridge MA US