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 US9220710(B2) 申请公布日期 2015.12.29
申请号 US201414151746 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;Link John O.;Liu Qi;Schroeder Scott D.;Tse Winston C.;Zhang Jennifer R.
分类号 C07D403/12;C07D417/12;C07D413/12;A61K31/437;C07D471/04;A61K31/4178;A61K31/4192;A61K31/4196;A61K31/4245;A61K31/427;A61K45/06 主分类号 C07D403/12
代理机构 代理人 Marquart Timothy A.
主权项 1. A compound of formula I: wherein: A is a 5-membered N-heteroaryl, wherein the 5-membered N-heteroaryl is substituted with one Z1 group and optionally substituted with 1, 2, or 3 Z2 groups; R1 is a bicyclic-heteroaryl or tricyclic heteroaryl, wherein the bicyclic-heteroaryl has 4 to 12 carbon atoms and 1-5 heteroatoms, and wherein any bicyclic-heteroaryl of R1 is optionally substituted with 1, 2, 3, 4, or 5 Z3 groups; R2 is a phenyl, 5-membered heteroaryl or 6-membered heteroaryl, wherein any phenyl, 5-membered heteroaryl or 6-membered heteroaryl of R2 is optionally substituted with 1, 2, 3, 4 or 5 Z4 groups; Z1 is selected from (C3-C8)alkyl, (C6-C20)aryl,and aryl(C1-C6)alkyl-, wherein any aryl, and aryl(C1-C6)alkyl- of Z1 is optionally substituted with 1, 2, 3, 4, or 5 Z1a or Z1b groups and wherein any (C3-C8)alkyl of Z1 is optionally substituted with 1, 2, 3, 4, or 5 Z1a groups; each Z1a is independently selected from (C3-C7)carbocycle, halogen, —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; each Z1b is independently selected from (C1-C6)alkyl and (C3-C5)carbocycle wherein any (C1-C6)alkyl and (C3-C5)carbocycle of Z1b is optionally substituted with 1, 2, 3, 4, or 5 halogen; each Z2 is independently selected from (C1-C3)alkyl, (C1-C3)haloalkyl, halogen and —O(C1-C3)alkyl; each Z3 is independently selected from (C1-C6)alkyl, (C3-C7)carbocycle, 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, wherein any (C3-C7)carbocycle and (C1-C6)alkyl of Z3 is optionally substituted with 1, 2, 3, 4, or 5 halogen; each Z4 is independently selected from (C1-C6)alkyl, halogen and —ORn3, wherein any (C1-C6)alkyl of Z4 is optionally substituted with 1, 2, 3, 4, or 5 halogen; each Rn1 is independently selected from H, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl and (C3-C7)carbocycle; each Rp1 is independently selected from (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl and (C3-C7)carbocycle; Rq1 and Rn1 are each independently selected from H, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl and (C3-C7)carbocycle, or Rq1 and Rr1 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle; each Rn2 is independently selected from H, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl and (C3-C7)carbocycle; each Rp2 is independently selected from (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl and (C3-C7)carbocycle; Rq2 and Rr2 are each independently selected from H, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl and (C3-C7)carbocycle, or Rq2 and Rr2 together with the nitrogen to which they are attached form a 5, 6 or 7-membered heterocycle; and each Rn3 is independently selected from H, (C1-C3)alkyl, (C1-C3)haloalkyl, and (C3-C7)carbocycle; or a salt thereof.
地址 Foster City CA US