发明名称 Heteroaryl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds
摘要 The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I,;;and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
申请公布号 US2014228356(A1) 申请公布日期 2014.08.14
申请号 US201414178470 申请日期 2014.02.12
申请人 Pfizer Inc. 发明人 Brodney Michael Aaron;Butler Christopher Ryan;Beck Elizabeth Mary;Davoren Jennifer Elizabeth;LaChapelle Erik Alphie;O'Neill Brian Thomas
分类号 C07D513/04 主分类号 C07D513/04
代理机构 代理人
主权项 1. A compound of Formula Iwherein R1 is hydrogen or methyl, wherein said methyl is optionally substituted with one to three fluoro; R2 is a 5- to 10-membered heteroaryl, having one to four heteroatoms independently selected from N, O or S, wherein at least one of the heteroatoms is N and wherein said N is optionally substituted with R4; and wherein said 5- to 10-membered heteroaryl is optionally substituted on carbon with one to three R3; R3 at each occurrence is independently selected from the group consisting of halogen, hydroxy, cyano, C1-6alkyl, C1-6alkoxy, C1-6alkoxy-C1-6alkyl, C3-6Cycloalkoxy, C3-6cycloalkoxy-(CR5aR5b)m—, C3-6cycloalkyl-(CR5aR5b)n—O—, —(CR5aR5b)m—C3-6cycloalkyl or —(CR5aR5b)m-(4- to 6-membered heterocycloalkyl); wherein said C1-6alkyl, C1-6alkoxy or C1-6alkoxy-C1-6alkyl are each optionally substituted with one to three fluoro and wherein said C3-6cycloalkyl, C3-6cycloalkoxy and (4- to 6-membered heterocycloalkyl) moieties are optionally substituted with one to three substituents independently selected from the group consisting of fluoro, methyl, fluoromethyl, difluoromethyl or trifluoromethyl; R4 is hydrogen, C1-6alkyl, —(CR5aR5b)m—C3-6cycloalkyl or —(CR5aR5b)m-(4- to 6-membered heterocycloalkyl); wherein said C1-6alkyl, C3-6cycloalkyl and -(4- to 6-membered heterocycloalkyl) moieties are each optionally substituted with one to three substituents independently selected from fluoro, methyl, trifluoromethyl, methoxy or trifluoromethoxy; R5a and R5b are independently hydrogen, methyl, fluoromethyl, difluoromethyl, trifluoromethyl or methoxy; m at each occurrence is independently 0, 1 or 2; and n is 1, 2 or 3;or a tautomer thereof or a pharmaceutically acceptable salt of said compound or tautomer.
地址 Groton CT US