发明名称 NEW DIAZASPIROCYCLOALKANE AND AZASPIROCYCLOALKANE
摘要 Compounds having the general formula (I);;wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
申请公布号 US2017029425(A1) 申请公布日期 2017.02.02
申请号 US201615293080 申请日期 2016.10.13
申请人 Hoffmann-La Roche Inc. 发明人 Hunziker Daniel;Mattei Patrizio;Mauser Harald;Prunotto Marco;Ullmer Christoph
分类号 C07D471/10;C07D403/10;C07D205/12;C07D401/10;C07D487/10;C07D249/18;C07D401/12;C07D403/12;C07D413/12 主分类号 C07D471/10
代理机构 代理人
主权项 1. A compound of formula (I) wherein R1 is alkyl, haloalkyl, cycloalkyl, substituted phenyl, substituted phenylalkyl, substituted phenoxyalkyl, substituted phenylcycloalkyl, substituted phenylalkenyl, substituted phenylalkynyl, substituted pyridinyl, substituted pyridinylalkyl, substituted pyridinylalkenyl, substituted pyridinylalkynyl, substituted thiophenyl, substituted thiophenylalkyl, substituted thiophenylalkenyl, substituted thiophenylalkynyl, substituted 2,3-dihydro-1H-isoindol-2-yl, substituted 1H-indol-2-yl or substituted benzofuran-2-yl, wherein substituted phenyl, substituted phenylalkyl, substituted phenoxyalkyl, substituted phenylcycloalkyl, substituted phenylalkenyl, substituted phenylalkynyl, substituted pyridinyl, substituted pyridinylalkyl, substituted pyridinylalkenyl, substituted pyridinylalkynyl, substituted thiophenyl, substituted thiophenylalkyl, substituted thiophenylalkenyl, substituted thiophenylalkynyl, substituted 2,3-dihydro-1H-isoindol-2-yl, substituted 1H-indol-2-yl and substituted benzofuran-2-yl are substituted with R8, R9 and R10, wherein in case R1 is alkyl and Y is —C(O)—, then R3 is selected from the groups S, T, U, V, X, Z, AA, AB, AC, AD, AE, AF, AG, AH, AI, AJ, AK and AL; R2 is —(CR4R5)n—R3, —C(O)—R3, —S(O)2—R3 or —C(O)—NR6R3; Y is —OC(O)—, —NR14C(O)—, —C(O)—, —S(O)2—,wherein in case R1 is substituted phenylalkenyl, substituted pyridinylalkenyl or substituted thiophenylalkenyl, then Y is not —OC(O)—; W is selected from one of the following ring systems:wherein in case W is one of the ring systems M or N, then R3 is selected from the groups S, T, U, V, X, Z, AA, AB, AC, AD, AE, AF, AG, AH, AI, AJ, AK and AL and wherein in case W is the ring system O, then R2 is —C(O)—NR6R3; R3 is selected from S, T, V, W, X, Y, Z, AA, AB, AC, AD, AE, AG, AH, AI, AJ, AK and AL from the following groups or R3 is substituted phenyl, substituted pyridinyl or substituted thiophenyl, wherein substituted phenyl, substituted pyridinyl and substituted thiophenyl are substituted with R11, R12 and R13; R4 and R5 are independently selected from H, halogen, alkyl and cycloalkyl; R6, R7 and R14 are independently selected from H, alkyl and cycloalkyl; R8, R9, R10, R11, R12, and R13 are independently selected from H, alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, cycloalkoxy, cycloalkoxyalkyl, cycloalkylalkoxyalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, alkoxyalkoxy, alkoxyalkoxyalkyl, halogen, hydroxy, cyano, alkylsulfonyl, cycloalkylsulfonyl, substituted aminosulfonyl, substituted amino and substituted aminoalkyl, wherein substituted aminosulfonyl, substituted amino and substituted aminoalkyl are substituted on the nitrogen atom with one to two substituents independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl and cycloalkylcarbonyl; n is zero, 1, 2 or 3; or pharmaceutically acceptable salts.
地址 Little Falls NJ US