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1. 发明申请

WO2009013356A3 ANTI-HIV TABLET FORMULATIONS COMPRISING DARUNAVIR 审中-公开
标题翻译：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
申请人： TIBOTEC PHARM LTD , SMANS GUIDO FRANCISCUS , JANS EUGEEN MARIA JOZEF
发明人： SMANS GUIDO FRANCISCUS , JANS EUGEEN MARIA JOZEF
IPC分类号： A61K9/20 , A61K9/36 , A61K31/34 , A61P31/18
CPC分类号： A61K9/2054 , A61K9/2866 , A61K31/34
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2008040778A3 CARBOXAMIDE 4-[(4-PYRIDYL)AMINO] PYRIMIDINES FOR THE TREATMENT OF HEPATITIS C 审中-公开
标题翻译：碳酰胺4 - [（4-吡啶基）氨基]嘧啶治疗乙型肝炎
公开(公告)号：WO2008040778A3
公开(公告)日：2009-01-29
申请号：PCT/EP2007060539
申请日：2007-10-04
申请人： TIBOTEC PHARM LTD , RABOISSON PIERRE JEAN-MARIE BE , LENZ OLIVER , LIN TSE-I , SIMMEN KENNETH
发明人： RABOISSON PIERRE JEAN-MARIE BERNARD , LENZ OLIVER , LIN TSE-I , SIMMEN KENNETH
IPC分类号： A61K31/506 , A61P31/14
CPC分类号： A61K31/506 , A61K31/535 , A61K2300/00
摘要： The present invention relates to the use of carboxamide 4-[(4-pyridyl)amino]- pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections.
摘要翻译：本发明涉及甲酰胺4 - [（4-吡啶基）氨基]嘧啶作为HCV复制的抑制剂的用途，以及它们在旨在治疗或对抗HCV感染的药物组合物中的用途。

3. 发明申请

WO2007088214A3 TREATING HIV INFECTION, WHEREIN HIV HAS A K65R MUTATION 审中-公开
标题翻译：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
申请人： TIBOTEC PHARM LTD , JOCHMANS DIRK EDWARD DESIRE , WIGERINCK PIET TOM BERT PAUL
发明人： JOCHMANS DIRK EDWARD DESIRE , WIGERINCK PIET TOM BERT PAUL
IPC分类号： A61K31/437 , A61P31/18
CPC分类号： A61K31/437
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2006108879A3 USE OF A SULFONAMIDE COMPOUND FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开
标题翻译：使用磺酰胺化合物改善药物的药代动力学
公开(公告)号：WO2006108879A3
公开(公告)日：2008-01-10
申请号：PCT/EP2006061614
申请日：2006-04-14
申请人： TIBOTEC PHARM LTD , VAN T KLOOSTER GERBEN ALBERT E , WIGERINCK PIET TOM BERT PAUL , DE MEYER SANDRA , BAERT LIEVEN ELVIRE COLETTE , DE KOCK HERMAN AUGUSTINUS
发明人： VAN T KLOOSTER GERBEN ALBERT E , WIGERINCK PIET TOM BERT PAUL , DE MEYER SANDRA , BAERT LIEVEN ELVIRE COLETTE , DE KOCK HERMAN AUGUSTINUS
IPC分类号： A61K31/426 , A61P31/18
CPC分类号： C07D417/12
摘要： A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.
摘要翻译：公开了一种改善由细胞色素P450单加氧酶代谢的药物的药代动力学的方法。更具体地说，本发明涉及一种用于改善逆转录病毒蛋白酶抑制剂的药代动力学的方法，特别涉及改善人类免疫缺陷病毒（HIV）蛋白酶抑制剂的药代动力学。药物组合物及其在制备用于抑制或治疗人体中的HIV感染或AIDS的药物中的用途也是本发明的一部分。

5. 发明申请

WO2006089942A8 PROTEASE INHIBITOR PRECURSOR SYNTHESIS 审中-公开
标题翻译： 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
申请人： TIBOTEC PHARM LTD , LINCLAU BRUNO
发明人： LINCLAU BRUNO
IPC分类号： C07D493/04 , A61K31/34 , A61P31/12
CPC分类号： C07D493/04
摘要： The present invention provides a compound having the structure (I) and processes for the production thereof and the intermediates used in such process.
摘要翻译：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。

6. 发明申请

WO03027255A2 ANTI-FUSION ASSAY 审中-公开
标题翻译：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
申请人： TIBOTEC PHARM LTD , XIE DONG , ERICKSON JOHN W , GRULICH PAUL
发明人： XIE DONG , ERICKSON JOHN W , GRULICH PAUL
IPC分类号： 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分类号： G01N33/56988 , G01N33/6803 , G01N2333/162 , G01N2500/02
摘要： 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.
摘要翻译：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。

7. 发明申请

WO02081478A2 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： 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
申请人： 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
发明人： 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分类号： 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分类号： C07D413/04 , C07D263/58 , C07D417/12 , C07D417/14 , C07D493/04
摘要： 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.
摘要翻译：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。

8. 发明申请

WO2011080141A2 DEGRADABLE REMOVABLE IMPLANT FOR THE SUSTAINED RELEASE OF AN ACTIVE COMPOUND 审中-公开
标题翻译：可拆卸的可拆卸植入物用于活性化合物的持续释放
公开(公告)号：WO2011080141A2
公开(公告)日：2011-07-07
申请号：PCT/EP2010070246
申请日：2010-12-20
申请人： TIBOTEC PHARM LTD , SCHACHTER DEBORAH M , BAERT LIEVEN ELVIRE COLETTE , KRAUS GUENTER , ZHANG QIANG , CHUN IKSOO
发明人： SCHACHTER DEBORAH M , BAERT LIEVEN ELVIRE COLETTE , KRAUS GUENTER , ZHANG QIANG , CHUN IKSOO
IPC分类号： A61K9/16
CPC分类号： A61L31/148 , A61K9/0024 , A61K9/0092 , A61K9/06 , A61K9/14 , A61K9/5031 , A61K9/5084 , A61K31/34 , A61K31/343 , A61K31/505 , A61K45/06 , A61L31/146 , A61K2300/00
摘要： A degradable, removable, pharmaceutical implant for the sustained release of one or more drugs in a subject, wherein the pharmaceutical implant is composed of a tube comprising an outer wall made of a degradable polymer completely surrounding a cavity, wherein the outer wall has a plurality of openings and wherein the cavity contains one or more sets of micro-particles, which micro-particles contain an active agent or a combination of two or more active agents, and wherein the size of the microparticles is selected such that the majority of the microparticles cannot pass through the openings.
摘要翻译：一种可降解的，可移除的药物植入物，用于在受试者中持续释放一种或多种药物，其中所述药物植入物由包含由完全环绕空腔的可降解聚合物制成的外壁的管组成，其中所述外壁具有多个的开口，并且其中所述空腔包含一组或多组微粒，所述微粒含有活性剂或两种或更多种活性剂的组合，并且其中所述微粒的尺寸选择为使得大部分微粒不能通过开口。

9. 发明申请

WO2009071650A3 AMIDE COMPOUNDS AS BOOSTERS OF ANTIVIRALS 审中-公开
标题翻译：酰胺化合物作为抗病毒剂
公开(公告)号：WO2009071650A3
公开(公告)日：2009-09-11
申请号：PCT/EP2008066847
申请日：2008-12-05
申请人： TIBOTEC PHARM LTD , JONCKERS TIM HUGO MARIA , SCHEPENS WIM BERT GRIET , HACHE GEERWIN YVONNE PAUL , HALLENBERGER BEATE SABINE , SASAKI JENNIFER CHIYOMI , BAUMEISTER JUDITH EVA , VAN T KLOOSTER GERBEN ALBERT ELEUTHERUS
发明人： JONCKERS TIM HUGO MARIA , SCHEPENS WIM BERT GRIET , HACHE GEERWIN YVONNE PAUL , HALLENBERGER BEATE SABINE , SASAKI JENNIFER CHIYOMI , BAUMEISTER JUDITH EVA , VAN T KLOOSTER GERBEN ALBERT ELEUTHERIUS
IPC分类号： C07D417/12 , A61K31/427 , A61P31/18 , C07D277/82 , C07D417/14
CPC分类号： C07D417/14 , C07D277/82 , C07D417/12
摘要： The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.
摘要翻译：本发明涉及具有CYP450抑制性质的化合物，因此可用作某些药物的助推剂，即当共同给药时能够增加某些药物的药代动力学变量中的至少一种。本发明还提供了所述化合物作为某些药物的生物利用度的改进剂的用途。还提供了制备本发明化合物和药物组合物的方法。

10. 发明申请

WO2008068299A3 HYDROBROMIDE SALT OF AN ANTI-HIV COMPOUND 审中-公开
标题翻译：抗HIV复合物的盐酸氢盐
公开(公告)号：WO2008068299A3
公开(公告)日：2009-04-23
申请号：PCT/EP2007063386
申请日：2007-12-06
申请人： TIBOTEC PHARM LTD , THONE DANIEL JOSEPH CHRISTIAAN
发明人： THONE DANIEL JOSEPH CHRISTIAAN
IPC分类号： A61K9/16 , A61K9/10 , A61K9/14 , A61K31/505
CPC分类号： A61K9/1635 , A61K9/145 , A61K9/1641 , A61K9/1652
摘要： Solid dispersions and dosage forms comprising the hydrobromide salt of a diarylpyrimidine derivative, useful as an anti-HIV agent.
摘要翻译：包含可用作抗HIV剂的二芳基嘧啶衍生物的氢溴酸盐的固体分散体和剂型。

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