首页> 外国专利> NON-NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR THE PROPHYLAXIS OR TREATMENT OF HIV-1 INFECTIONS

NON-NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR THE PROPHYLAXIS OR TREATMENT OF HIV-1 INFECTIONS

机译:非核苷酸逆转录酶抑制剂,包含它们的药物组合物及其在制备预防或治疗HIV-1感染药物中的用途

摘要

Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from S(O)pRa, where Ra is C1-C4 alkyl, ORx, NRxRx, NHNRxRx, NHNHC(O)ORx, NRxOH; C(O)Rb, where Rb is CT-C4-alkyl, ORx, NRxRx, NHNRxRx, NHC1-C3-alkyl-C(O)Orx NRxRc, where Rc is H, C1-C4 alkyl, NRxRx; C(=0)Rd, CN, S(O)pRx, where Rd is Rd is C1-C4-alkyl, ORx, NRxRx C1-C3-alkyl-OC1-C3-alkylC(O)ORx, C1-C3-alkyl-COORx; C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (OC1-C3alkyl)q-ORx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, S(O), or CH2, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is (CR8R8)n-D-(CR8R8)m-; D is a bond, NR9, -0-, S, S(=0)- or S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
机译:式Z的化合物:其中; A是CH或N; R1是在包含选自S(O)pRa的A的环中碳原子的取代基,其中Ra是C1-C4烷基,ORx,NRxRx,NHNRxRx,NHNHC(O)ORx,NRxOH; C(O)Rb,其中Rb为CT-C4-烷基,ORx,NRxRx,NHNRxRx,NHC1-C3-烷基-C(O)Orx NRxRc,其中Rc为H,C1-C4烷基,NRxRx; C(= 0)Rd,CN,S(O)pRx,其中Rd是Rd是C1-C4-烷基,ORx,NRxRx C1-C3-烷基-OC1-C3-烷基C(O)ORx,C1-C3-烷基-COORx; C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯(OC 1 -C 3烷基)q -OR x a具有1-3个杂原子的5或6元芳香环,p为1或2; Rx独立地选自H,C1-C4烷基或乙酰基;或一对Rx可与相邻的N原子一起形成环; L为-0-,S(O)或CH2,其中r为0、1或2; R3-R7是说明书中定义的取代基; X为(CR8R8)n-D-(CR8R8)m-; D是键,NR9,-0-,S,S(= 0)-或S(= 0)2-;及其药学上可接受的盐和前药可用作HIV抗病毒药。

著录项

  • 公开/公告号IL176740A

    专利类型

  • 公开/公告日2011-09-27

    原文格式PDF

  • 申请/专利权人 MEDIVIR AB;

    申请/专利号IL20060176740

  • 发明设计人

    申请日2006-07-06

  • 分类号C07D405/12;C07D405/14;C07D409/12;C07D409/14;

  • 国家 IL

  • 入库时间 2022-08-21 18:06:23

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