发明名称 Compounds for the treatment of hepatitis C
摘要 The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.;
申请公布号 US8741884(B2) 申请公布日期 2014.06.03
申请号 US201113086704 申请日期 2011.04.14
申请人 Bristol-Myers Squibb Company 发明人 Wang Tao;Yin Zhiwei;Zhang Zhongxing;Pendri Annapurna;Li Guo;Gerritz Samuel;Zhai Weixu;Scola Paul Michael;Sun Li-Qiang;Mull Eric
分类号 A61K31/33;C07D487/00 主分类号 A61K31/33
代理机构 代理人
主权项 1. A compound of formula Iwhere R1 is alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, halocycloalkyl, cycloalkenyl, benzyl, indanyl, or alkylcarbonyl; R2 is hydrogen, halo, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, CO2R6, or CON(R7)(R8); R3 is hydrogen, alkyl, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, or dialkyaminocarbonyl; R4 is hydrogen or alkyl; R5 is hydrogen, alkyl, (amino)alkyl, (alkylamino)alkyl, or (dialkylamino)alkyl; R6 is hydrogen, alkyl, or benzyl; R7 is hydrogen, alkyl, pyrrolidinonyl, piperidinonyl, homopiperazinonyl, (R9)alkyl, (Q)alkyl, ((R9)alkyl)-Q-alkyl, (R9)(R9)alkyl, or (R9)(Q)alkyl; or R7 is pyrrolidinonyl, piperidinonyl, homopiperazinonyl, or R8 is hydrogen or alkyl; or R7 and R8 taken together with the nitrogen to which they are attached is azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl, and is substituted with 0-2 substituents selected from alkyl, (CO2R6)alkyl, CO2R6,CON(R10)(R10), and N(R10)CO2R6; or R7 and R8 taken together with the nitrogen to which they are attached is a spiro [3-7.3-7] bicyclic ring system where the bicylic ring system contains 0-1 additional nitrogens, and is substituted with 0-2 substituents selected from alkyl, (CO2R6)alkyl, CO2R6, CON(R10)(R11), and N(R10)CO2R6; R9 is CO2R6, C(O)(N(R10)(R11)), C(═NR12)(N(R10)(R11)),CON(R10)SO2R13,N(R10)(R11), N(R10)COR6,N(R10)COPh, N(R10)CO2R6,N(R10)C(O)(N(R10)(R11)),N(R10)C(═NR12)(N(R10)(R11)), or (R13)SO2; R10is hydrogen or alkyl; R11 is hydrogen or alkyl; or N(R10)(R11) taken together with the nitrogen to which they are attached is azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl R12 is hydrogen, alkyl, or phenyl; R13 is alkyl, cycloalkyl, or phenyl; Q is cycloalkyl, phenyl, tetrahydrofuranyl, tetrahydropyranyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl, and is substituted with 0-2 R9 substituents; X is an alkylene or alkenylene chain containing 0-6 groups selected from the group consisting of O, NR3, S, S(O), S(O2), C(O)O, C(O)NR4, OC(O)NR4, NR4C(O)NR4, NR4C(NR12)NR4,, and Z, provided that O, NR3, S, S(O), S(O2), C(O)O, C(O)NR4, OC(O)NR4, NR4C(O)NR4, and NR4C(NR12)NR4 do not directly bond to each other or to NH, such that ring A is 13-24 membered; and where the alkylene or alkenylene chain is substituted with 0-6 substituents selected from the group consisting of alkyl, alkylidinyl, hydroxy, alkoxy, and phenyl where the phenyl substituent is further substituted with 0-4 cyano, halo, alkyl, haloalkyl, alkoxy, or haloalkoxy substituents; Y is CH2, O, CO2, or C(O)NR5; and Z is C3-7 cycloalkylene or phenylene; or a pharmaceutically acceptable salt therof.
地址 Princeton NJ US