(1,10b-dihydro-2-(aminoalkyl-phenyl)-5H-pyrazolo[1,5 C][1,3]benzoxazin-5-yl)phenyl methanone derivatives as HIV viral replication inhibitors
    1.
    发明授权
    (1,10b-dihydro-2-(aminoalkyl-phenyl)-5H-pyrazolo[1,5 C][1,3]benzoxazin-5-yl)phenyl methanone derivatives as HIV viral replication inhibitors 有权
    (1,10b-二氢-2-(氨基烷基 - 苯基)-5H-吡唑并[1,5-C] [1,3]苯并恶嗪-5-基)苯基甲酮衍生物作为HIV病毒复制抑制剂

    公开(公告)号:US07745432B2

    公开(公告)日:2010-06-29

    申请号:US12241317

    申请日:2008-09-30

    IPC分类号: A61K31/5386

    CPC分类号: C07D498/04

    摘要: The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

    摘要翻译: 本发明涉及作为HIV病毒的病毒复制的抑制剂的5H-吡唑并[1,5-c] [1,3]苯并恶嗪-5-基)苯基甲酮衍生物,其制备方法以及药物组合物, 它们用作药物,以及包括它们的诊断试剂盒。 本发明还涉及本发明的HIV抑制剂与其它抗逆转录病毒剂的组合。 它还涉及它们在测定中作为参考化合物或作为试剂的用途。 本发明的化合物可用于预防或治疗HIV感染和治疗AIDS。

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    10.
    发明申请
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒大肠杆菌抑制剂

    公开(公告)号:US20100240698A1

    公开(公告)日:2010-09-23

    申请号:US11995573

    申请日:2006-07-28

    CPC分类号: C07D487/04 C07K5/06165

    摘要: Inhibitors of HCV of formula al and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 8 to 12 membered bicyclic heterocyclic ring system containing one nitrogen, and optionally one to three oxygen, sulfur or nitrogen, wherein said ring system may be optionally substituted; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(═O)—NR5a— or —O—C(═O)—NR5a—C1-4alkanediyl-; R2 is hydrogen, —OR6, —C(═O)OR6, —C(═O)R7, —C(═O)NR5aR5b, —C(═O)NHR5c, —NR5aR5b, —NHR5c, —NHSOpNR5aR5b, —NR5aSOpR8, or —B(OR6)2; R3 and R4 are hydrogen or C1-6alkyl; or R3 and R4 taken together may form a C3-7cycloalkyl ring; n is 3, 4, 5, or 6; p is 1 or 2; aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be optionally substituted Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be optionally substituted; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

    摘要翻译: 式A1的HCV的抑制剂及其N-氧化物,盐和立体化学异构形式,其中R 1是芳基或饱和的部分不饱和或完全不饱和的5或6元单环或8至12元双环杂环体系,其含有一个 氮和任选的一至三个氧,硫或氮,其中所述环系可以任选被取代; L是直接键,-O - , - O-C 1-4烷二基 - , - O-CO - , - O-C(= O)-NR 5a - 或-O-C(= O)-NR 5a -C 1-4烷二基 - ; R2是氢,-OR6,-C(= O)OR6,-C(= O)R7,-C(= O)NR5aR5b,-C(= O)NHR5c,-NR5aR5b,-NHR5c,-NHSOpNR5aR5b,-NR5aSOpR8 ,或-B(OR 6)2; R3和R4是氢或C1-6烷基; 或者R 3和R 4一起形成C 3-7环烷基环; n为3,4,5或6; p为1或2; 芳基是苯基,萘基,茚满基或1,2,3,4-四氢萘基,其各自可以被任选地取代。Het是含有1至4个杂原子的5或6元饱和,部分不饱和或完全不饱和的杂环,各自独立地选择 来自氮,氧和硫,任选地与苯环稠合,并且其中基团Het作为整体可以任选被取代; 含有化合物(I)的药物组合物和制备化合物(I)的方法。 还提供了式(I)的HCV抑制剂与利托那韦的生物可利用组合。