发明名称 THERAPEUTIC COMPOUNDS
摘要 Compounds of formula I:;or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
申请公布号 US2014221417(A1) 申请公布日期 2014.08.07
申请号 US201414151762 申请日期 2014.01.09
申请人 GILEAD SCIENCES, INC. 发明人 BONDY Steven S.;CANNIZZARO Carina E.;CHOU Chien-Hung;HU Yunfeng Eric;LINK John O.;LIU Qi;SCHROEDER Scott D.;TSE Winston C.;ZHANG Jennifer R.
分类号 C07D513/04;C07D487/04;C07D471/14 主分类号 C07D513/04
代理机构 代理人
主权项 1. A compound of formula I: wherein: A is (C6-C12)aryl or aryl(C1-C4)alkyl- wherein any aryl or aryl(C1-C4)alkyl- of A is optionally substituted with 1, 2, 3, 4 or 5 Z1 groups; B is heteroaryl, wherein the heteroaryl of B has 2-10 carbon atoms and 1-5 heteratoms and is optionally substituted with 1, 2, 3, 4 or 5 Z2 groups, and wherein Q and W are connected to adjacent ring atoms of B; C is phenyl, 5-membered heteroaryl or 6-membered heteroaryl, wherein any phenyl, 5-membered heteroaryl or 6-membered heteroaryl of C is optionally substituted with 1, 2, 3, or 4 Z3 groups, and wherein Q and Y are connected to adjacent ring atoms of C, or Q and Y are connected to the first and third atom of three consecutive ring atoms of C; each Q is independently selected from —C(R2a)2—, —O—, —NR1a—, —S—, —C(═O)—, —S(═O)— and —S(═O)2—, or two adjacent Q groups taken together can be —CR2b═CR2b—; W is —CH2—; X is CH or N; Y is —CH2—; n is 1, 2, 3, 4 or 5; R1 is selected from (C1-C6)alkyl, (C3-C7)carbocycle, and (C3-C7)carbocycle(C1-C6)alkyl; R1a is H or (C1-C4)alkyl, each R2a is independently H, halogen or (C1-C4)alkyl, and each R2b is independently H or (C1-C4)alkyl, or one R2a together with an adjacent Q group forms a three membered carbocycle; each Z1 is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, —CN, —ORn1, —OC(O)Rp1, —OC(O)NRq1Rr1, —SRn1, —S(O)Rp1, —S(O)2OH, —S(O)2Rp1, —S(O)2NRq1Rr1, —NRq1Rr1, —NRn1CORp1, —NRn1CO2Rp1, —NRn1CONRq1Rr1, —NRn1S(O)2Rp1, —NRn1S(O)2ORp1, —NRn1S(O)2NRq1Rr1, NO2, —C(O)Rn1, —C(O)ORn1 and —C(O)NRq1Rr1, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Z1 is optionally substituted with 1, 2, 3, 4 or 5 Z1a groups; each Z1a is independently selected from halogen, —CN, —ORn2, —OC(O)Rp2, —OC(O)NRq2Rr2, —SRn2, —S(O)Rp2, —S(O)2OH, —S(O)2Rp2, —S(O)2NRq2Rr2, —NRq2Rr2, —NRn2CORp2, —NRn2CO2Rp2, —NRn2CONRq2Rr2, —NRn2S(O)2Rp2, —NRn2S(O)2ORp2, —NRn2S(O)2NRq2Rr2, NO2, —C(O)Rn2, —C(O)ORn2 and —C(O)NRq2Rr2; each Z1b is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl and (C2-C4)alkynyl; each Rn1 is independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Rn1 is optionally substituted with 1, 2, 3, 4 or 5 Z1a groups; each Rpt is independently selected from (C1-C4)alkyl, (C1-C4)haloalkyl, (C2-C4)alkenyl, (C2-C4)alkynyl wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Rpt is optionally substituted with 1, 2, 3, 4 or 5 Z1a groups; Rq1 and Rr1 are each independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Rq1 or Rr1 is optionally substituted with 1, 2, 3, 4 or 5 Z1a groups, or Rq1 and Rr1 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle, wherein the 5, 6 or 7-membered heterocycle is optionally substituted with 1, 2, 3, 4 or 5 Z1a or Z1b groups; each Rn2 is independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)haloalkyl and (C1-C4)heteroalkyl; each Rp2 is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)haloalkyl and (C1-C4)heteroalkyl; Rq2 and Rr2 are each independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)haloalkyl and (C1-C4)heteroalkyl, or Rq2 and Rr2 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle; each Z2 is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, halogen, —CN, —ORn3, —OC(O)Rp3, —OC(O)NRq3Rr3, —SRn3, —S(O)Rp3, —S(O)2OH, —S(O)2Rp3, —S(O)2NRq3Rr3, —NRq3Rr3, —NRn3CORp3, —NRn3CO2Rp3, —NRn3CONRq3Rr3, —NRn3S(O)2Rp3, —NRn3S(O)2ORp3, —NRn3S(O)2NRq3Rr3, NO2, —C(O)Rn3, —C(O)ORn3 and —C(O)NRq3Rr3, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Z2 is optionally substituted with 1, 2, 3, 4 or 5 Z2a groups; each Z2a is independently selected from halogen, —CN, —ORn4, —OC(O)Rp4, —OC(O)NRq4Rr4, —SRn4, —S(O)Rp4, —S(O)2OH, —S(O)2Rp4, —S(O)2NRq4Rr4, —NRq4Rr4, —NRn4CORp4, —NRn4CO2Rp4, —NRn4CONRq4Rr4, —NRn4S(O)2Rp4, —NRn4S(O)2ORp4, —NRn4S(O)2NRq4Rr4, NO2, —C(O)Rn4, —C(O)ORn4 and —C(O)NRq4Rr4; each Z2b is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl and (C2-C4)alkynyl; each Rn3 is independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Rn3 is optionally substituted with 1, 2, 3, 4 or 5 Z2a groups; each Rp3 is independently selected from (C1-C4)alkyl, (C1-C4)haloalkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Rp3 is optionally substituted with 1, 2, 3, 4 or 5 Z2a groups; Rq3 and Rr3 are each independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, wherein any (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl of Rq3 or Rr3 is optionally substituted with 1, 2, 3, 4 or 5 Z2a groups, or Rq3 and Rr3 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle, wherein the 5, 6 or 7-membered heterocycle is optionally substituted with 1, 2, 3, 4 or 5 Z2a or Z2b groups; each Rn4 is independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C3-C7)carbocycle, (C1-C4)haloalkyl and (C1-C4)heteroalkyl; each Rp4 is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C3-C7)carbocycle, (C1-C4)haloalkyl and (C1-C4)heteroalkyl; Rq4 and Rr4 are each independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, (C1-C4)haloalkyl and (C1-C4)heteroalkyl, or Rq4 and Rr4 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle; each Z3 is independently selected from (C1-C4)alkyl, halogen, —CN, —ORn5, —NRn5CORp5, —C(O)Rn5, and —C(O)NRq5Rr5; each Rn5 is independently selected from H, (C1-C4)alkyl, (C1-C4)haloalkyl and (C1-C4)heteroalkyl; each Rp5 is independently selected from (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)haloalkyl and (C1-C4)heteroalkyl; and Rq5 and Rr5 are each independently selected from H, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)haloalkyl and (C1-C4)heteroalkyl, or Rq5 and Rr5 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle; or a salt thereof.
地址 Foster City CA US