发明名称 N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides
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,;wherein the variables R1, R2 and R3 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 US9611264(B1) 申请公布日期 2017.04.04
申请号 US201615272820 申请日期 2016.09.22
申请人 Pfizer Inc. 发明人 Brodney Michael Aaron;Butler Christopher Ryan;Zhang Lei;O'Neill Brian Thomas;Verhoest Patrick Robert;Salomon Ferrer Romelia del Carmen
分类号 C07D417/14 主分类号 C07D417/14
代理机构 代理人 Wichtowski John A.
主权项 1. A compound of Formula I wherein R1 is a 5- to 6-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 R5; and wherein said 5- to 6-membered heteroaryl is optionally substituted on carbon with one to three R4; R2 and R3 are each independently hydrogen, C1-6alkyl, C3-6cycloalkyl or 3- to 7-membered heterocycloalkyl; wherein the C1-6alkyl is optionally substituted with a C1-3alkoxy or with one to three fluoro; and the C3-6cycloalkyl and 3- to 7-membered heterocycloalkyl are each optionally and independently substituted with one to three fluoro, C1-3alkyl or C1-3alkoxy; or R2 and R3, taken together with the carbon to which they are attached, form a C3-6cycloalkyl ring or 3- to 7-membered heterocycloalkyl ring, each of which is optionally and independently substituted with one to three fluoro, C1-3alkyl or C1-3alkoxy; R4 at each occurrence is independently selected from the group consisting of halo, hydroxy, cyano, C1-6alkyl, C1-6alkoxy, C3-6alkenyl, C3-6alkenyloxy, C3-6alkynyl, C3-6alkynyloxy, C1-6alkoxy-C1-6alkyl, C3-6cycloalkoxy, C3-6cycloalkyl, C3-6cycloalkyl-C1-6alkyl, C3-6cycloalkyl-C1-6alkoxy, 4- to 6-membered heterocycloalkyl and 4- to 6-membered heterocycloalkyl-C1-6alkyl; wherein said C1-6alkyl, C1-6alkoxy, C3-6alkenyl, C3-6alkenyloxy, C3-6alkynyl, C3-6alkynyloxy, C1-6alkoxy-C1-6alkyl, C3-6cycloalkoxy, C3-6cycloalkyl, C3-6cycloalkyl-C1-6alkyl, C3-6cycloalkyl-C1-6alkoxy, 4- to 6-membered heterocycloalkyl and 4- to 6-membered heterocycloalkyl-C1-6alkyl are each optionally substituted with one to three substituents independently selected from fluoro, chloro, hydroxy, cyano, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, methoxy, fluoromethoxy, difluoromethoxy and trifluoromethoxy; and R5 is hydrogen or C1-6alkyl optionally substituted with one to three fluoro; or a tautomer thereof or a pharmaceutically acceptable salt of said compound or tautomer.
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