发明名称 5,5-fused arylene or heteroarylene hepatitis C virus inhibitors
摘要 Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.;
申请公布号 US9187496(B2) 申请公布日期 2015.11.17
申请号 US201213675787 申请日期 2012.11.13
申请人 Idenix Pharmaceuticals LLC 发明人 Dousson Cyril B.;Dukhan David;Parsy Christophe Claude;Pierra Claire;Alexandre Francois-Rene;Brandt Guillaume;Da Costa Daniel;Rahali Houcine;Paparin Jean-Laurent;Derock Michel;Convard Thierry;Surleraux Dominique
分类号 A61K31/4178;A61K31/381;C07D513/04;C07D487/04;C07D491/048;C07D495/04;C07D498/04;A61K31/4184;A61K31/429;A61K31/5377;A61K31/7056;A61K38/05;A61K38/20;A61K38/21;C07K5/078 主分类号 A61K31/4178
代理机构 Jones Day 代理人 Jones Day
主权项 1. A method for treating or preventing an HCV infection in a human patient, which comprises administering to the patient a compound of Formula IC:or a single enantiomer, a racemic mixture, a mixture of diastereomers, or a pharmaceutically acceptable salt, or solvate thereof;wherein: each R1 and R2 is independently (a) hydrogen; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (c) —C(O)R1a, —C(O)CH(NR1bR1c)R1a, —C(O)CH(N(R1c)C(O)R1b)R1a, —C(O)CH(N(R1c)C(O)OR1b)R1a, —C(O)CH(N(R1c)C(O)NR1bR1d)R1a, —C(O)OR1a, —C(O)NR1bR1c, —C(NR1a)NR1bR1c, —P(O)(OR1a)R1d, —CH2P(O)(OR1a)R1d, —S(O)R1a, —S(O)2R1a, —S(O)NR1bR1c, or —S(O)2NR1bR1c; each R3a is independently hydrogen or R3; each R3, R5, and R6 is independently (a) cyano, halo, or nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (c) —C(O)R1a, —C(O)OR1a, —C(O)NR1bR1c, —C(NR1a)NR1bR1c, —OR1a, —OC(O)R1a, —OC(O)OR1a, —OC(O)NR1bR1c, —OC(═NR1a)NR1bR1c, —OS(O)R1a, —OS(O)2R1a, —OS(O)NR1bR1c, —OS(O)2NR1bR1c, —NR1bR1c, —NR1aC(O)R1d, —NR1aC(O)OR1d, —NR1aC(O)NR1bR1c, —NR1aC(═NR1d)NR1bR1c, —NR1aS(O)R1d, —NR1aS(O)2R1d, —NR1aS(O)NR1bR1c, —NR1aS(O)2NR1bR1c, —SR1a, —S(O)R1a, —S(O)2R1a, —S(O)NR1bR1c, or —S(O)2NR1bR1c; or two R5 or two R6 that are attached to the same ring are linked together to form a bond, —O—, —NR7—, —S—, C1-6 alkylene, C1-6 heteroalkylene, C2-6 alkenylene, or C2-6 heteroalkenylene; L1 and L2 are each independently selected from: a bond,wherein each moiety is optionally substituted with one, two, three, or four R3; the star (*) on each moiety represents the point of attachment thought which the moiety is connected toand the zigzag line () on each moiety represents the point of attachment through which the moiety is connected toand wherein T3 is a bond, C, N, O, S, CR3a, or NR3a; U3, V3, W3, and X3 are each independently C, N, O, S, CR3a, or NR3a; and Y3 is C or N; each Z1 and Z2 is independently a bond; each R7 is independently (a) hydrogen; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (c) —C(O)R1a, —C(O)OR1a, —C(O)NR1bR1c, —C(NR1a)NR1bR1c, —OR1a, —OC(O)R1a, —OC(O)OR1a, —OC(O)NR1bR1c, —OC(═NR1a)NR1bR1c, —OS(O)R1a, —OS(O)2R1a, —OS(O)NR1bR1c,—OS(O)2NR1bR1c,—NR1bR1c, —NR1aC(O)R1d, —NR1aC(O)OR1d, —NR1aC(O)NR1bR1c,—NR1aC(═NR1d)NR1bR1c, —NR1aS(O)R1d, —NR1aS(O)2R1d, —NR1aS(O)NR1bR1c,—NR1aS(O)2NR1bR1c, —P(O)(OR1a)R1d, —CH2P(O)(OR1a)R1d, —S(O)R1a, —S(O)2R1a, —S(O)NR1bR1c, or —S(O)2NR1bR1c; each R1a, R1b, R1c, and R1d is independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or R1a and R1c together with the C and N atoms to which they are attached form heterocyclyl; or R1b and R1c together with the N atom to which they are attached form heterocyclyl; each n and p is independently an integer of 0, 1, 2, 3, 4, 5, 6, or 7; each q and r is independently an integer of 1, 2, 3, or 4; wherein each alkyl, alkylene, heteroalkylene, alkenyl, alkenylene, heteroalkenylene, alkynyl, cycloalkyl, aryl, aralkyl, heteroaryl, and heterocyclyl is optionally substituted with one or more substituents Q, where each Q is independently selected from (a) cyano, halo, or nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl, each of which is further optionally substituted with one or more substituents Qa; or (c) —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —C(NRa)NRbRc, —ORa, —OC(O)Ra, —OC(O)ORa, —OC(O)NRbRc, —OC(═NRa)NRbRc, —OS(O)Ra, —OS(O)2Ra, —OS(O)NRbRc, —OS(O)2NRbRc, —NRbRc, —NRaC(O)Rd, —NRaC(O)ORd, —NRaC(O)NRbRc, —NRaC(═NRd)NRbRc, —NRaS(O)Rd, —NRaS(O)2Rd, —NRaS(O)NRbRc, —NRaS(O)2NRbRc, —SRa, —S(O)Ra, —S(O)2Ra, —S(O)NRbRc, or —S(O)2NRbRc, wherein each Ra, Rb, Rc, and Rd is independently (i) hydrogen; (ii) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl, each optionally substituted with one or more substituents Qa; or (iii) Rb and Rc together with the N atom to which they are attached form heterocyclyl, optionally substituted with one or more substituents Qa; wherein each Qa is independently (a) cyano, halo, and nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (c) —C(O)Re, —C(O)ORe, —C(O)NRfRg, —C(NRe)NRfRg, —ORe, —OC(O)Re, —OC(O)ORe, —OC(O)NRfRg, —OC(═NRe)NRfRg, —OS(O)Re, —OS(O)2Re, —OS(O)NRfRg, —OS(O)2NRfRg, —NRfRg, —NReC(O)Rh, —NReC(O)ORf, —NReC(O)NRfRg, —NReC(═NRh)NRfRg, —NReS(O)Rh, —NReS(O)2Rh, —NReS(O)NRfRg, —NReS(O)2NRfRg, —SRe, —S(O)Re, —S(O)2Re, —S(O)NRfRg, or —S(O)2NRfRg; wherein each Re, Rf, Rg, and Rh is independently (i) hydrogen; (ii) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (iii) Rf and Rg together with the N atom to which they are attached form heterocyclyl.
地址 Cambridge MA US