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1. 发明授权

US07323567B2 RSV polymerase inhibitors 有权
标题翻译： RSV聚合酶抑制剂
公开(公告)号：US07323567B2
公开(公告)日：2008-01-29
申请号：US10975562
申请日：2004-10-28
申请人： Bruno Simoneau , Josee Bordeleau , Gulrez Fazal , Serge Landry , Steve Mason , Jean Rancourt
发明人： Bruno Simoneau , Josee Bordeleau , Gulrez Fazal , Serge Landry , Steve Mason , Jean Rancourt
IPC分类号： C07D471/04 , A61K31/4745
CPC分类号： C07D471/04 , A61K31/4353 , A61K31/437
摘要： Compounds or enantiomers of formula (I) or a salt thereof: wherein R1, R2, R3, R4 and R5 are as defined herein, are useful for the manufacture of a medicament for the treatment or prevention of respiratory syncytial virus infection in a mammal.
摘要翻译：式（I）的化合物或对映异构体或其盐：其中R 1，R 2，R 3，R 4， / SUP>和R 5如本文所定义，可用于制备用于治疗或预防哺乳动物呼吸道合胞病毒感染的药物。

2. 发明申请

US20070172936A1 Purified active HCV NS2/3 protease 审中-公开
公开(公告)号：US20070172936A1
公开(公告)日：2007-07-26
申请号：US11223638
申请日：2005-09-09
申请人： Diane Thibeault , Daniel Lamarre , Roger Maurice , Louise Pilote , Armin Pause
发明人： Diane Thibeault , Daniel Lamarre , Roger Maurice , Louise Pilote , Armin Pause
IPC分类号： C12N9/99 , C12N9/48 , C07K7/08
CPC分类号： C07K14/005 , C12N9/506 , C12N2770/24222 , C12Q1/37 , G01N33/6893 , G01N2333/18 , G01N2500/00 , G01N2500/04
摘要： A method for producing a refolded, inactive form of recombinantly produced NS2/3 protease which comprises the steps of: a) purifying the protease from inclusion bodies in the presence of a chaotropic agent; and b) refolding the purified protease by contacting it with a reducing agent and lauryldiethylamine oxide (LDAO) in the presence of reduced concentration of chaotropic agent or polar additive. The invention further comprises a method for activating this refolded inactive NS2/3 protease by adding an activation detergent. This method produces large amounts of the active NS2/3 protease to allow small molecules and ligands to be screened as potential inhibitors of NS2/3 protease, which may be useful as therapeutic agents against HCV.

3. 发明授权

US07141574B2 Viral polymerase inhibitors 有权
公开(公告)号：US07141574B2
公开(公告)日：2006-11-28
申请号：US10198384
申请日：2002-07-18
申请人： Pierre Louis Beaulieu , Sylvie Goulet , George Kukolj , Martin Poirier , Youla S. Tsantrizos , Eric Jolicoeur , James Gillard , Marc-André Poupart , Jean Rancourt
发明人： Pierre Louis Beaulieu , Sylvie Goulet , George Kukolj , Martin Poirier , Youla S. Tsantrizos , Eric Jolicoeur , James Gillard , Marc-André Poupart , Jean Rancourt
IPC分类号： A61K31/535 , C07D417/00
CPC分类号： C07D333/62 , C07D209/08 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; - - - - - represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7and R8 and Q are as defined herein; Y2is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of which optionally substituted with R90; or R9 is covalently bonded to either of R7 or R8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

4. 发明申请

US20060235010A1 Inhibitors of Papilloma Virus 有权
标题翻译：乳头状瘤病毒抑制剂
公开(公告)号：US20060235010A1
公开(公告)日：2006-10-19
申请号：US11382969
申请日：2006-05-12
申请人： Christiane Yoakim , William Ogilvie , Jeffrey O'Meara , Peter White , Nathalie Goudreau
发明人： Christiane Yoakim , William Ogilvie , Jeffrey O'Meara , Peter White , Nathalie Goudreau
IPC分类号： A61K31/5377 , A61K31/4747 , A61K31/4245 , A61K31/41
CPC分类号： C07D405/12 , C07D307/94 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/048 , C07D493/04 , C07D493/10 , C07D495/12 , C07D495/20
摘要： A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A, X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
摘要翻译：式（I）化合物或其对映异构体或非对映异构体：其中：A，X，W，R 1，Y; 3＆lt; 3＆gt; R 4和R 4如本文所定义。本发明的化合物可用作乳头瘤病毒E1-E2-DNA复合物的抑制剂。本发明还提供了治疗或预防人乳头状瘤病毒感染的方法。

5. 发明授权

US07105510B2 Non-nucleoside reverse transcriptase inhibitors 有权
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US07105510B2
公开(公告)日：2006-09-12
申请号：US10662856
申请日：2003-09-15
申请人： Christiane Yoakim , Eric Malenfant , Bounkham Thavonekham , William Ogilvie , Robert Déziel
发明人： Christiane Yoakim , Eric Malenfant , Bounkham Thavonekham , William Ogilvie , Robert Déziel
IPC分类号： C07D471/14 , A61K31/55 , A61P31/18
CPC分类号： C07D471/14
摘要： Compounds represented by formula I: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4)alkyl; R4 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
摘要翻译：由式I表示的化合物：其中R 1是H，卤素，（C 1-4烷基）烷基，O（C 1-4 - ） - 烷基和卤代烷基; R 2是H或（C 1-4 - ）烷基; R 3是H或（C 1-4 - ）烷基; R 4是（C 1-4烷基）烷基，（C 1-4 - ）烷基（C 1-3 - >）环烷基，或（C 3-7）环烷基; 并且Q是具有一个到两个选自O和N的杂原子的稠合苯基-5或6元饱和杂环，所述Q任选被羟基或（C 1-4烷基）烷基取代，可以任选地被吡啶基-N-氧化物或C（O）OR取代，其中R是H或（C 1-4）烷基; 或其盐。该化合物对野生型具有抑制活性，并具有HIV和HIV的单和双突变株。

6. 发明授权

US06852501B2 Methods for determining ATPase activity and uses thereof 有权
标题翻译：测定ATP酶活性的方法及其应用
公开(公告)号：US06852501B2
公开(公告)日：2005-02-08
申请号：US10041522
申请日：2001-10-24
申请人： Peter White
发明人： Peter White
IPC分类号： G01N33/534 , C12Q1/34 , C12Q1/42 , C12Q1/48
CPC分类号： C12Q1/42 , G01N2500/00 , Y10S436/80 , Y10S436/804 , Y10T436/16
摘要： The present invention uses the principle that phosphomolybdate binds to hydrophobic surfaces to isolate the phosphomolybdate complex from other phosphate-containing molecules and further uses the SPA concept to bring a radiolabeled phosphomolybdate complex in close contact with a scintillant for measurement by scintillation counting. Generally, the present invention provides an assay for detecting and measuring the amount of orthophosphate (Pi) in an aqueous reaction mixture, wherein the amount of Pi released is separated from the reaction mixture by: adding a solution of molybdate to the reaction mixture to form a phosphomolybdate complex; and contacting the phosphomolybdate complex with a hydrophobic surface, wherein the surface is capable of being separated from the aqueous reaction mixture to allow measurement of the Pi. Particularly, this invention provides an assay for measuring the ATPase activity of enzymes, more particularly, the HPV E1 helicase.
摘要翻译：本发明使用磷钼酸盐结合疏水性表面以将磷钼酸盐络合物与其它含磷酸盐分子隔离的原理，并且进一步使用SPA概念以使放射性标记的磷钼酸盐络合物与闪烁剂紧密接触，以通过闪烁计数进行测量。通常，本发明提供了用于检测和测量水性反应混合物中正磷酸盐（Pi）的量的测定法，其中通过以下方式将释放的Pi的量与反应混合物分离：向反应混合物中加入钼酸盐溶液以形成磷钼酸盐络合物; 并使磷钼酸盐络合物与疏水表面接触，其中表面能够与水性反应混合物分离，以允许测量Pi。特别地，本发明提供了用于测量酶的ATPase活性的测定法，更具体地说，涉及HPV E1解旋酶。

7. 发明申请

US20050009855A1 Inhibitors of papilloma virus 有权
标题翻译：乳头状瘤病毒抑制剂
公开(公告)号：US20050009855A1
公开(公告)日：2005-01-13
申请号：US10772721
申请日：2004-02-04
申请人： Christiane Yoakim , Bruno Hache , William Ogilvie , Jeffrey O'Meara , Peter White , Nathalie Goudreau
发明人： Christiane Yoakim , Bruno Hache , William Ogilvie , Jeffrey O'Meara , Peter White , Nathalie Goudreau
IPC分类号： C07D307/94 , C07D405/12 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D491/04 , C07D493/04 , C07D493/10 , C07D495/12 , A61K31/4747 , A61K31/4025 , C07
CPC分类号： C07D405/12 , C07D307/94 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/048 , C07D493/04 , C07D493/10 , C07D495/12 , C07D495/20
摘要： A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
摘要翻译：式（I）化合物或其对映体或非对映异构体：其中：A， X，W，R 1，Y; R 3; 和R 4如本文所定义。本发明的化合物可用作乳头瘤病毒E1-E2-DNA复合物的抑制剂。本发明还提供了治疗或预防人乳头状瘤病毒感染的方法。

8. 发明申请

US20040002059A1 Regions of papilloma virus E1 helicase involved in E1 oligomerization 有权
标题翻译：乳头瘤病毒E1解旋酶区域参与E1寡聚化
公开(公告)号：US20040002059A1
公开(公告)日：2004-01-01
申请号：US10339268
申请日：2003-01-09
申请人： Boehringer Ingelheim (Canada) Ltd.
发明人： Jacques Archambault
IPC分类号： C12Q001/70 , C12Q001/68
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , C12N2710/20022 , C12Q1/708 , G01N33/56983 , G01N33/573 , G01N2333/025 , G01N2500/00
摘要： There is provided an amino acid sequence comprised within the PV E1 protein region A delineated by amino acids 352 and 439, and any derivative variant or fragment thereof, necessary for the oligomerization of the E1 protein. This amino acid sequence is capable of self-association and of associating with the full length E1 protein and any derivative, variant or fragment thereof comprising the sequence of this invention. A specific aspect of this first embodiment, the amino acid domain of this invention delimited by amino acids 353 to 438 of the PV E1 protein. More particularly, the amino acid domain of this invention is as defined by SEQ ID NO. 2. There is also provided a cross-linking assay to directly measure the level of oligomerization (or inhibition thereof) of the E1 protein. In accordance with a fourth embodiment of this invention, there is provided a N-terminally truncated E1 protein. More particularly, one aspect of this fourth embodiment encompasses the E1 protein delimited by amino acid 72 to 649 (SEQ ID NO. 78).
摘要翻译：提供了由E1蛋白的寡聚化所必需的PV E1蛋白质区域A所描绘的氨基酸序列，以及由氨基酸352和439所描绘的任何衍生变体或片段。该氨基酸序列能够自身结合并与全长E1蛋白及其包含本发明序列的任何衍生物，变体或片段缔合。本第一实施方案的具体方面，本发明的氨基酸结构域由PV E1蛋白质的氨基酸353至438界定。更具体地，本发明的氨基酸结构域如SEQ ID NO：还提供了直接测量E1蛋白的低聚（或抑制）水平的交联测定法。根据本发明的第四个实施方案，提供了N-末端截短的E1蛋白。更具体地，该第四实施方案的一个方面包括由氨基酸72至649（SEQ ID NO：78）限定的E1蛋白。

9. 发明申请

US20030194698A1 E2 displacement assay for identifying inhibitors of HPV 有权
标题翻译：用于鉴定HPV抑制剂的E2位移测定
公开(公告)号：US20030194698A1
公开(公告)日：2003-10-16
申请号：US10358790
申请日：2003-02-05
申请人： Boehringer Ingelheim (Canada) Ltd.
发明人： Peter White , Christiane Yoakim
IPC分类号： C12Q001/70 , C07D451/12 , C07D491/12
CPC分类号： C07D407/12 , C07D491/10 , G01N33/532 , G01N33/533 , G01N33/534 , G01N33/535 , G01N33/542 , G01N33/56983 , G01N33/581 , G01N33/582 , G01N33/583 , G01N33/60 , G01N2333/025 , G01N2500/10
摘要： The present invention generally relates to an assay for identifying inhibitors of Human Papillomavirus (HPV), comprising: a) contacting a HPV E2 transactivation domain with a probe to form a E2:probe complex and measuring a signal from said probe to establish a base line level; b) incubating the E2:probe complex with a test compound and measuring the signal from said probe; c) comparing the signal from step b) with the signal from step a); nullwherein said probe is a compound of formula (I) or its enantiomers or diastereoisomers thereof: 1 wherein R1, A, X, W, Y, R3 and R4 are as defined herein; or a derivative thereof, wherein said derivative is a probe of formula (I) labeled with a detectable label or an affinity tag, wherein wavy lines represent bonds of unspecified stereochemistry; and wherein said signal is selected from: fluorescence, resonance energy transfer, time resolved fluorescence, radioactivity, fluorescence polarization, change in the intrinsic spectral properties, luminescence and plasma-resonance; whereby a modulation in said signal is an indication that said test compound binds to said transactivation domain.
摘要翻译：本发明一般涉及用于鉴定人乳头瘤病毒（HPV）抑制剂的测定法，其包括：a）使HPV E2反式激活结构域与探针接触以形成E2：探针复合物并测量来自所述探针的信号以建立基线水平; b）将E2：探针复合物与测试化合物孵育并测量所述探针的信号; c）将来自步骤b）的信号与来自步骤a）的信号进行比较; 其中所述探针是式（I）化合物或其对映体或非对映异构体：其中R 1>，A，X，W，Y，R 3>和R 4> 在这里或其衍生物，其中所述衍生物是用可检测标记或亲和标签标记的式（I）的探针，其中波浪线表示未指定的立体化学键; 并且其中所述信号选自：荧光，共振能量转移，时间分辨荧光，放射性，荧光偏振，固有光谱性质的变化，发光和等离子体共振; 由此所述信号中的调节是所述测试化合物结合所述反式激活结构域的指示。

10. 发明授权

US5948935A Process and intermediates for (s)-.alpha.-amino-1-carboxycyclopentaneacetic acid 失效
标题翻译：（s）-α-氨基-1-羧基环戊烷乙酸的方法和中间体
公开(公告)号：US5948935A
公开(公告)日：1999-09-07
申请号：US12237
申请日：1998-01-23
申请人： Jean-Marie Ferland , Ingrid Guse , Eric Malenfant
发明人： Jean-Marie Ferland , Ingrid Guse , Eric Malenfant
IPC分类号： C07C227/18 , C07C229/46 , C07C237/14 , C07C255/31 , C07C69/74 , C07C61/06
CPC分类号： C07C237/14 , C07C227/18 , C07C255/31 , C07B2200/07 , C07C2101/08
摘要： Disclosed herein is a process for preparing (S)-.alpha.-amino-1-carboxycyclopentaneacetic acid which is a useful intermediate for preparing peptidomimetic inhibitors of herpes viral ribonucleotide reductase. The process comprises the preparation of the key intermediate ##STR1## and its subsequent conversion to the desired product.
摘要翻译：本文公开了一种制备（S）-α-氨基-1-羧基环戊烷乙酸的方法，其是制备疱疹病毒核糖核苷酸还原酶的拟肽抑制剂的有用中间体。该方法包括制备关键中间体及其随后转化成所需产物。

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