发明名称 5, 6-D2 URIDINE NUCLEOSIDE/TIDE DERIVATIVES
摘要 In one aspect, the invention provides compounds represented by Formula I,;;and pharmaceutically acceptable salts, esters, stereoisomers, tautomers, solvates, and combinations thereof, pharmaceutical compositions comprising these compounds and the use of these compounds for treating a viral infection in a subject.
申请公布号 US2014219958(A1) 申请公布日期 2014.08.07
申请号 US201414169387 申请日期 2014.01.31
申请人 ENANTA PHARMACEUTICALS, INC. 发明人 Luly Jay R.;Ma Jun;Wang Guoqiang;Or Yat Sun
分类号 A61K31/7072;A61K45/06;C07H17/02 主分类号 A61K31/7072
代理机构 代理人
主权项 1. A compound represented by Formula I or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, or combination thereof: wherein: R1 is selected from the group consisting of: 1) Hydrogen;2) R6; where R6 is selected from the group consisting of: hydrogen, hydroxy protecting group, —C(O)R7, —C(O)OR7, and —C(O)NR8aR8b; wherein R7 is selected from the group consisting of: substituted or unsubstituted —C1-C8 alkyl, substituted or unsubstituted —C2-C8 alkenyl, substituted or unsubstituted —C2-C8 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heterocyclic; R8a and R8b are each independently selected from the group consisting of: hydrogen and R7; or alternatively R8a and R8b taken together with the nitrogen atom to which they are attached form a heterocyclic ring;3) —P(O)(OR7a)(OR7b); wherein R7a and R7b are each independently selected from the group consisting of a) hydrogen; b) unsubstituted or substituted —C1-C8 alkyl;4) —P(O)(OR7a)—O—P(O)(OR7b)(OR7c); wherein R7a and R7b are previously defined; R7c is selected from the group consisting of a) hydrogen; b) unsubstituted or substituted —C1-C8 alkyl;5) —P(O)(OR7a)—O—P(O)(OR7b)—O—P(O)(OR7c)(OR7d); wherein R7a, R7b and R7c are previously defined; R7d is selected from the group consisting of a) hydrogen; b) unsubstituted or substituted —C1-C8 alkyl;6)  where X is O or S; R9 is R7 wherein R7 is previously defined; R10, R11 and R12 are each independently selected from the group consisting of: a) hydrogen; b) unsubstituted or substituted —C1-C8 alkyl; c) R11 is hydrogen, R12 and R10 taken together with the nitrogen which R10 is attached to form a heterocyclic ring; d) R11 and R12 taken together with the carbon which they are attached form a ring; R13 is hydrogen or R7, wherein R7 is previously defined; and7)  where X is O or S; n is 1-4; R8a and R8b are as previously defined; R14 is hydrogen or —(CO)—R7, wherein R7 is as previously defined;8) Or, R1 and R3 are taken together to form  where X is O or S; and R15 is is selected from the group consisting of a) hydrogen; b) unsubstituted or substituted —C1-C8 alkyl; c) substituted or unsubstituted —C2-C8 alkenyl; d) substituted or unsubstituted —C2-C8 alkynyl; e) substituted or unsubstituted aryl; f) substituted or unsubstituted heteroaryl; R2a at each occurrence is selected from the group consisting of: 1) hydrogen;2) halogen;3) Substituted or unsubstituted —C1-C8 alkyl;4) Substituted or unsubstituted —C2-C8 alkenyl; and5) Substituted or unsubstituted —C2-C8 alkynyl; R2b and R4 are independently selected from the group consisting of: 1) hydrogen;2) halogen;3) —CN;4) —N3; and5) OR9;R9 at each occurrence is selected from the group consisting of: hydrogen, hydroxy protecting group, R10, —C(O)R10, —C(O)OR10, and —C(O)NR11aR11b; wherein R10 at each occurrence is independently selected from the group consisting of: substituted or unsubstituted —C1-C8 alkyl, substituted or unsubstituted —C2-C8 alkenyl, substituted or unsubstituted —C2-C8 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heterocyclic; R11a and R11b at each occurrence are each independently selected from the group consisting of: hydrogen and R10; or alternatively R11a and R11b taken together with the nitrogen atom to which they are attached form a heterocyclic ring; R3 is R6; wherein R6 is as previously defined; R5a and R5b are independently selected from the group consisting of: 1) hydrogen;2) substituted or unsubstituted —C1-C8 alkyl;3) substituted or unsubstituted —C2-C8 alkenyl; and4) substituted or unsubstituted —C2-C8 alkynyl;or R5a and R5b are taken together with the carbon atom to which they are attached to form a group selected from —C3-C8 cycloalkyl, —C3-C8 cycloalkenyl, or —C3-C8 cycloalkynyl.
地址 WATERTOWN MA US