发明名称 AMMONIUM DERIVATIVES FOR THE TREATMENT OF HEPATITIS C
摘要 Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these 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 US2015322085(A1) 申请公布日期 2015.11.12
申请号 US201414762537 申请日期 2014.01.23
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 Wang Tao;Yin Zhiwei;Zhang Zhongxing;Scola Paul Michael
分类号 C07D498/08;A61K31/53;A61K45/06;C07D251/52 主分类号 C07D498/08
代理机构 代理人
主权项 1. A compound of Formula I, including pharmaceutically acceptable salts thereof: wherein a, b and c are nitrogen; or a and b are nitrogen, while c is —CH; or b and c are nitrogen, while a is —CH; or a and c are nitrogen, while b is —CH; R1 is selected from alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, halocycloalkyl, cycloalkenyl, indanyl, alkylcarbonyl, and benzyl, wherein the benzyl moiety is substituted with 0-3 substituents selected from halo, alkyl, cycloalkyl, alkenyl, alkynyl, hydroxyl, cyano, haloalkyl, alkoxy, and haloalkoxy; R2 is selected from alkyl, cycloalkyl, ((Ar1)alkyl, (Ar1)cycloalkyl, ((Ar1)cycloalkyl)alkyl, ((Ar1)alkyl)cycloalkyl, and (((Ar1)alkyl)cycloalkyl)alkyl; Ar1 is phenyl substituted with 0-3 substituents selected from halo, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, alkoxy, and haloalkoxy; R3 is hydrogen, alkyl or cycloalkyl; R4 is selected from the group of hydrogen, halogen, alkyl, alkoxyl, alkylamino and alkylthio; or R2 and R4 can be connected by a carbon, oxygen, nitrogen or sulfur atom to form a ring; X is selected from the group of O, NR11, CONR11, NR11NR12 and CONR11NR12; R11 is selected from the group of hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, halocycloalkyl, cycloalkenyl, indanyl, alkylcarbonyl, and benzyl, wherein the benzyl moiety is substituted with 0-3 substituents selected from halo, alkyl, haloalkyl, alkoxy, and haloalkoxy; R12 is selected from the group of hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, halocycloalkyl, cycloalkenyl, indanyl, alkylcarbonyl, and benzyl, wherein the benzyl moiety is substituted with 0-3 substituents selected from halo, alkyl, haloalkyl, alkoxy, and haloalkoxy; R5 is selected from the group of alkyl, cycloalkyl, (cycloalkyl)alkyl, (alkyl)cycloalkyl, ((alkyl))cycloalkyl)alkyl, bridged bicycloalkyl, fused bicycloalkyl, and spiro bicycloalkyl, and is substituted with 0-4 substituents selected from the group of halo, alkyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, hydroxy, alkoxy, benzyloxy, CO2R13, CON(R14)(R15), N(R14)(R15), tetrahydrofuranyl, tetrahydropyranyl, and Ar2; or R5 is hydrogen, N-alkoxycarbonylpiperidinyl, piperidinonyl, or Ar3; R13 is selected from the group of hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, ((hydroxyalkyl)alkoxy)alkoxy, and ((alkoxy)alkoxy)alkoxy; R14 is selected from the group of hydrogen, alkyl, cycloalkyl, alkylcarbonyl, and alkoxycarbonyl; R15 is hydrogen or alkyl; or R14 and R15 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, alkylcarbonyl, and alkoxycarbonyl; Ar2 is selected from the group of phenyl, indanyl, tetrahydronaphthyl, isochromanyl, benzodioxolyl, pyridinyl, pyrazolyl, imidazolyl, and triazolyl, and is substituted with 0-3 substituents selected from cyano, halo, alkyl, alkyenyl, haloalkyl, alkoxy, haloalkoxy, N(R16)(R17), and alkylCO; R16 is selected from the group of hydrogen, alkyl, cycloalkyl, alkylcarbonyl, and alkoxycarbonyl; R17 is hydrogen or alkyl; or R16 and R17 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, alkylcarbonyl, and alkoxycarbonyl; Ar3 is selected from the group of phenyl, indanyl, fluorenyl, biphenyl, terphenyl, pyridinyl, pyrazolyl, isoxazolyl, imidazolyl, thiazolyl, triazolyl, benzoxazolyl, indolinyl, and dibenzofuranyl, and is substituted with 0-3 substituents selected from the group of cyano, halo, alkyl, alkenyl, haloalkyl, cycloalkyl, (CO2R13)alkyl, (CO2R13)alkenyl, (CON(R16)(R17))alkyl, phenyl, hydroxyl, alkoxy, haloalkoxy, alkylcarbonyl, CO2R13, CON(R16)(R17), and PhCONHSO2; or Ar3 is phenyl substituted with 1 substituent selected from benzyl, tetrazolyloxy, thiazolyl, phenylpyrazolyl, methyloxadiazolyl, thiadiazolyl, triazolyl, methyltriazolyl, tetrazolyl, pyridinyl, and dimethoxypyrimdinyl; and R6 is alkyl or cycloalkyl; R7 is alkyl or cycloalkyl; R8 is alkyl or cycloalkyl; or R7 and R8 can be connected by a carbon, oxygen, nitrogen or sulfur atom to form a ring; or R6, R7 and R8 can be connected by a carbon, oxygen, nitrogen or sulfur atom to form a bicyclic ring; or R5 and R6 can be connected by a carbon, oxygen, nitrogen or sulfur atom to form a ring; or R5, R6 and R7 can be connected by a carbon, oxygen, nitrogen or sulfur atom to form a bicyclic or tricyclic ring; or R5, R6, R7 and R8 can be connected by a carbon, oxygen, nitrogen or sulfur atom to form a tricyclic or tetracyclic ring.
地址 Princeton NJ US