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    ANTI-HIV TABLET FORMULATIONS COMPRISING DARUNAVIR
    1.
    发明申请
    ANTI-HIV TABLET FORMULATIONS COMPRISING DARUNAVIR 审中-公开
    包含DARUNAVIR的抗HIV片剂制剂

    公开(公告)号：WO2009013356A3

    公开(公告)日：2009-04-02

    申请号：PCT/EP2008059802

    申请日：2008-07-25

    Applicant: TIBOTEC PHARM LTD ,  SMANS GUIDO FRANCISCUS ,  JANS EUGEEN MARIA JOZEF

    Inventor： SMANS GUIDO FRANCISCUS ,  JANS EUGEEN MARIA JOZEF

    IPC: A61K9/20 ,  A61K9/36 ,  A61K31/34 ,  A61P31/18

    CPC classification number: A61K9/2054 ,  A61K9/2866 ,  A61K31/34

    Abstract: An anti-HIV tablet formulation comprising a core containing 0.1 to 1.5% by weight (w/w) of colloidal silicon dioxide and 0.4 to 0.9% by weight (w/w) of a lubricant, the balance of the core comprising darunavir, a disintegrant and a filler comprising a spray-dried mixture of microcrystalline cellulose and colloidal silicon dioxide, the core being optionally coated with a film coating.

    Abstract translation: 一种抗HIV片剂制剂，其包含含有0.1至1.5重量％（w / w）胶态二氧化硅和0.4至0.9重量％（w / w）润滑剂的核心，其余核心包含地瑞那韦， 崩解剂和包含微晶纤维素和胶体二氧化硅的喷雾干燥混合物的填料，所述芯任选地涂覆有薄膜包衣。

    TREATING HIV INFECTION, WHEREIN HIV HAS A K65R MUTATION
    3.
    发明申请
    TREATING HIV INFECTION, WHEREIN HIV HAS A K65R MUTATION 审中-公开
    治疗艾滋病毒感染艾滋病毒有一个K65R突变

    公开(公告)号：WO2007088214A3

    公开(公告)日：2008-10-09

    申请号：PCT/EP2007051087

    申请日：2007-02-05

    Applicant: TIBOTEC PHARM LTD ,  JOCHMANS DIRK EDWARD DESIRE ,  WIGERINCK PIET TOM BERT PAUL

    Inventor： JOCHMANS DIRK EDWARD DESIRE ,  WIGERINCK PIET TOM BERT PAUL

    IPC: A61K31/437 ,  A61P31/18

    CPC classification number: A61K31/437

    Abstract: Nucleotide-competing reverse transcriptase inhibitors (NcRTI) bind to the active site of HIV reverse transcriptase (RT) in competition with the next incoming nucleotide. To further investigate the impact of RT inhibitor resistance mutations on the activity of NcRTIs, the susceptibility of > 6000 recent clinical isolates for a prototype compound, NcRTI-1, was determined. Over 80% of the profiled clinical isolates remained susceptible for NcRTI-1 (FC 1700 of these viruses showed that the combination of active site mutations M184V + Y115F correlated most with resistance to NcRTI-1 (FC = 75). Analysis also indicated that the K65R mutation is associated with hypersusceptibility to NcRTI-1 and that it reverses the reduced susceptibility caused by 20 M184V. These findings were confirmed in SDM strains. This reciprocity between the K65R and M184V mutation is unparalleled among RT inhibitors. When replicating wild-type HIV-1 in the presence of NcRTI-1, M184V + Y115F were selected. In the presence of both NcRTI-1 and tenofovir, NcRTI-1 prevents the selection of K65R.

    Abstract translation: 核苷酸竞争性逆转录酶抑制剂（NcRTI）与HIV逆转录酶（RT）的活性位点结合，与下一个进入的核苷酸竞争。 为了进一步研究RT抑制剂抗性突变对NcRTIs活性的影响，确定了原始化合物NcRTI-1的> 6000个近临床分离株的敏感性。 超过80％的异型临床分离物对NcRTI-1仍然敏感（FC <4）。 NcRTI-1和目前使用的RT抑制剂之间没有观察到交叉电阻，除了3TC / FTC的有限交叉电阻外。 对这些病毒> 1700的基因型的分析显示，活性位点突变M184V + Y115F的组合与NcRTI-1的抗性最相关（FC = 75）。 分析也表明，K65R突变与NcRTI-1的过度敏感性相关，并且反转了由20 M184V引起的降低的易感性。 这些发现在SDM菌株中得到证实。 K65R和M184V突变之间的这种互惠性在RT抑制剂中是无与伦比的。 在NcRTI-1存在下复制野生型HIV-1时，选择M184V + Y115F。 在NcRTI-1和替诺福韦两者的存在下，NcRTI-1阻止了K65R的选择。

    PROTEASE INHIBITOR PRECURSOR SYNTHESIS
    5.
    发明申请
    PROTEASE INHIBITOR PRECURSOR SYNTHESIS 审中-公开
    PROTEASE抑制剂前体合成

    公开(公告)号：WO2006089942A8

    公开(公告)日：2007-12-13

    申请号：PCT/EP2006060246

    申请日：2006-02-24

    Applicant: TIBOTEC PHARM LTD ,  LINCLAU BRUNO

    Inventor： LINCLAU BRUNO

    IPC: C07D493/04 ,  A61K31/34 ,  A61P31/12

    CPC classification number: C07D493/04

    Abstract: The present invention provides a compound having the structure (I) and processes for the production thereof and the intermediates used in such process.

    Abstract translation: 本发明提供具有结构（I）的化合物及其制备方法和在该方法中使用的中间体。

    ANTI-FUSION ASSAY
    6.
    发明申请
    ANTI-FUSION ASSAY 审中-公开
    抗融合测定

    公开(公告)号：WO03027255A2

    公开(公告)日：2003-04-03

    申请号：PCT/US0230611

    申请日：2002-09-27

    Applicant: TIBOTEC PHARM LTD ,  XIE DONG ,  ERICKSON JOHN W ,  GRULICH PAUL

    Inventor： XIE DONG ,  ERICKSON JOHN W ,  GRULICH PAUL

    IPC: A61K45/00 ,  A61P31/18 ,  C07K7/00 ,  C07K14/47 ,  G01N27/447 ,  G01N33/15 ,  G01N33/48 ,  G01N33/50 ,  G01N33/561 ,  G01N33/569 ,  G01N33/68 ,  G06F19/00 ,  C12N

    CPC classification number: G01N33/56988 ,  G01N33/6803 ,  G01N2333/162 ,  G01N2500/02

    Abstract: Methods of identifying a fusion inhibitor and inhibitors of gp41-mediated membrane fusion are disclosed. The methods comprise, for example, providing a first helical polypeptide comprising a sequence of IQN17 (SEQ ID NO: 1); providing a second helical polypeptide of 34 or less than 34 amino acids comprising the amino acid sequence W-X1-X2-W-X3-X4-X5-I, wherein X1, X2, X3, X4, and X5 are each independently chosen from any amino acid except proline; measuring, by capillary zone electrophoresis, the degree of complex formation between these peptides; and comparing the measured degree of complex formation to the degree in the presence of a test composition.

    Abstract translation: 公开了鉴定融合抑制剂和gp41介导的膜融合抑制剂的方法。 所述方法包括例如提供包含IQN17（SEQ ID NO：1）序列的第一螺旋多肽; 提供包含氨基酸序列W-X1-X2-W-X3-X4-X5-I的34个或小于34个氨基酸的第二螺旋多肽，其中X1，X2，X3，X4和X5各自独立地选自 除脯氨酸以外的任何氨基酸; 通过毛细管区带电泳测量这些肽之间的复合物形成程度; 并将测量的复合物形成程度与存在测试组合物的程度进行比较。

    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    7.
    发明申请
    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
    BROADSPECTRUM 2-（取代氨基） - 苯并噻唑磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：WO02081478A2

    公开(公告)日：2002-10-17

    申请号：PCT/EP0204012

    申请日：2002-04-09

    Applicant: TIBOTEC PHARM LTD ,  SURLERAUX DOMINIQUE LOUIS NEST ,  VENDEVILLE SANDRINE MARIE HELE ,  VERSCHUEREN WIM GASTON ,  DE BETHUNE MARIE-PIERRE T M M ,  DE KOCK HERMAN AUGUSTINUS ,  TAHRI ABDELLAH ,  ERRA SOLA MONTSERRAT

    Inventor： SURLERAUX DOMINIQUE LOUIS NEST ,  VENDEVILLE SANDRINE MARIE HELE ,  VERSCHUEREN WIM GASTON ,  DE BETHUNE MARIE-PIERRE T M M ,  DE KOCK HERMAN AUGUSTINUS ,  TAHRI ABDELLAH ,  ERRA SOLA MONTSERRAT

    IPC: A61K31/423 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07D263/58 ,  C07D413/04 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04

    CPC classification number: C07D413/04 ,  C07D263/58 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04

    Abstract: The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8-C1-6alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1-6alkanediyl-C(=O)-, C1-6alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2-; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

    Abstract translation: 本发明涉及具有式（I）的N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3 -7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷二基-C （= O） - ， - S（= O）2 - ， - OS（= O）2 - ， - NR 8 -S（= O）2; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代的C 1 1-6; A是C 1-6烷二基，-C（= O） - ， - C（= S） - ， - S（= O）2 - ，C 1-6烷二基-C（= O） - ，C 1-6烷二基-C ） - 或C 1-6烷二基-S（= O）2 - ; R 5是H，OH，C 1-6烷基，Het 1 C 1-6烷基，Het 2 C 1-6烷基，任选取代的氨基C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 10，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在-A-不是C 1-6烷二基的情况下，则R6还可以是C 1-6烷基，Het 1 C 1-4烷基，Het 1 OC 1-4烷基，Het 2 C 1-4烷基，Het 2 OC 1-4烷基，芳基C 1-4烷基，芳基OC 1-4烷基或氨基C 1-4烷基; 其中R6的定义中的每个氨基可任选被取代; -A-R6是羟基C 1-6烷基; R5和-A-R6与它们所连接的氮原子一起也可以形成Het1或Het2。 它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。 它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

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