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1. 发明申请

WO1997045116A1 USE OF THIOCARBOXANILIDE DERIVATIVES FOR THE PREPARATION OF A MEDICAMENT FOR PREVENTING THE TRANSMISSION OF HIV TO UNINFECTED CELLS AND CONTRACEPTIVE COMPOSITIONS COMPRISING THE SAID DERIVATIVES 审中-公开
标题翻译：用于制备用于预防艾滋病病毒向不明细胞传播的药物和包含该衍生物的合成组合物的硫代碳酰胺衍生物的使用
公开(公告)号：WO1997045116A1
公开(公告)日：1997-12-04
申请号：PCT/US1997008838
申请日：1997-05-23
申请人： UNIROYAL CHEMICAL COMPANY, INC. , BORKOW, Gadi , PARNIAK, Michael, A. , WAINBERG, Mark, A.
发明人： UNIROYAL CHEMICAL COMPANY, INC.
IPC分类号： A61K31/34
CPC分类号： A61K31/381 , A61K31/34
摘要： Method for preventing or inhibiting the transmission of HIV to susceptible uninfected cells by administering to the HIV, to cells infected with HIV, and/or to the uninfected cells, an effective amount of a compound of formula (I), wherein X is O or S, prior to the HIV or the cells infected with HIV, contacting the uninfected cells.
摘要翻译：通过向HIV施用HIV感染的细胞和/或向未感染的细胞施用有效量的式（I）化合物，其中X为O或 S，在HIV或感染HIV的细胞之前，接触未感染的细胞。

2. 发明申请

WO2003064441A2 OLIGONUCLEOTIDES COMPRISING ALTERNATING SEGMENTS AND USES THEREOF 审中-公开
标题翻译：包含替代部分的寡核苷酸及其用途
公开(公告)号：WO2003064441A2
公开(公告)日：2003-08-07
申请号：PCT/CA2003/000129
申请日：2003-01-31
申请人： McGILL UNIVERSITY , DAMHA, Masad, J. , PARNIAK, Michael, A.
发明人： DAMHA, Masad, J. , PARNIAK, Michael, A.
IPC分类号： C07H21/00
CPC分类号： C12N15/113 , A61K38/00 , C07H21/00 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/323 , C12N2310/3231 , C12N2310/346
摘要： The invention relates to oligonucleosides having alternating segments of sugar-modified nucleosides and 2’-deoxynucleosides, and uses thereof. The invention further relates to oligonucleotides having alternating segments of sugar-modified nucleotides and 2’-deoxynucleotides, and uses thereof. Such uses include the preparation of antisense oligonucleotides and their use for the prevention or depletion of function of a target nucleic acid of interest, such as an RNA, in a system. Accordingly, an oligonucleotide of the invention is useful for therapeutic, analytical and diagnostic methods and uses, as well as a component of compositions and commercial packages corresponding to such methods and uses.
摘要翻译：本发明涉及具有糖修饰核苷和2'-脱氧核苷的交替片段的寡核苷酸及其应用。本发明还涉及具有糖修饰的核苷酸和2'-脱氧核苷酸的交替片段的寡核苷酸及其应用。这样的用途包括制备反义寡核苷酸及其在系统中预防或消除目的靶核酸（例如RNA）的功能的用途。因此，本发明的寡核苷酸可用于治疗，分析和诊断方法和用途，以及对应于这些方法和用途的组合物和商业包装的组分。

3. 发明申请

WO2003012127A2 ASSAY FOR IDENTIFYING INHIBITORS OF HIV RT DIMERIZATION 审中-公开
标题翻译：用于鉴定HIV RT DIM的化学抑制剂的测定
公开(公告)号：WO2003012127A2
公开(公告)日：2003-02-13
申请号：PCT/CA2002/001162
申请日：2002-07-26
申请人： BOEHRINGER INGELHEIM (CANADA) LTD , SLUIS-CREMER, Nicolas , PARNIAK, Michael , PELLETIER, Alex
发明人： SLUIS-CREMER, Nicolas , PARNIAK, Michael , PELLETIER, Alex
IPC分类号： C12Q1/00
CPC分类号： C12Q1/48 , G01N2333/9125 , G01N2500/02
摘要： A method for measuring heterodimerization of HIV RT, which comprises the steps of:a) providing a first solution comprising p66 subunit homodimers in the presence of a dissociation agent; b) contacting the first solution with p51 RT subunits and incubating in the presence of a reassociation buffer to allow association of a complex of p66/p51 RT subunits, wherein one of the subunits comprises an affinity tag and the other of the subunits comprises a detectable label; c) contacting the incubate of step b) with an affinity medium under conditions that enable the p66/p51 complex to bind to the affinity medium; and d) determining the amount of complex formed by measuring the level of detectable label bound to the affinity medium (or by measuring the reconstituted RT polymerase activity). Steps a) to d) can be carried out in the presence or absence of a test compound followed by e) comparing the test compound sample to a control sample lacking the compound, whereby modulated p66/p51 complex formation in the test compound sample is indicative of the ability of the compound to modulate, inhibit or enhance heterodimerization.The method can be used to screen for inhibitors of HIV RT dimerization.
摘要翻译：一种用于测量HIV RT的异二聚化的方法，其包括以下步骤：a）在解离剂存在下提供包含p66亚基同源二聚体的第一溶液; b）使第一溶液与p51RT亚基接触，并在再结合缓冲液存在下孵育以允许p66 / p51 RT亚基的复合物缔合，其中一个亚基包含亲和标签，另一个亚基包含可检测的标签; c）使能使p66 / p51复合物与亲和介质结合的条件下使步骤b）的培养物与亲和介质接触; 和d）通过测量与亲和介质结合的可检测标记的水平（或通过测量重组的RT聚合酶活性）来测定形成的复合物的量。步骤a）至d）可以在存在或不存在测试化合物的情况下进行，随后e）将测试化合物样品与缺少化合物的对照样品进行比较，由此在测试化合物样品中调节的p66 / p51复合体形成是指示性的的化合物调节，抑制或增强异二聚化的能力。该方法可用于筛选HIV RT二聚化的抑制剂。

4. 发明申请

WO2005023270A2 COMPOSITIONS AND METHODS FOR USE OF ANTIVIRAL DRUGS IN THE TREATMENT OF RETROVIRAL DISEASES RESISTANT TO NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：组合物和方法用于治疗抗核素逆转录酶抑制剂的抗逆转录病毒药物
公开(公告)号：WO2005023270A2
公开(公告)日：2005-03-17
申请号：PCT/US2004/029375
申请日：2004-09-09
申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION , UNIVERSITY OF ILLINOIS , PARNIAK, Michael , MELLORS, John, W. , OLDFIELD, Eric , TOVIAN, Zev , CHAN, Julian, Mun, Weng
发明人： PARNIAK, Michael , MELLORS, John, W. , OLDFIELD, Eric , TOVIAN, Zev , CHAN, Julian, Mun, Weng
IPC分类号： A61K31/663
CPC分类号： A61K31/663 , A61K31/66 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： The present invention relates to novel compositions comprising an excisioninhibiting bisphosphonate and a nucleoside reverse transcriptase inhibitor. The present invention also relates to methods for preventing or treating retrovirus-related diseases using a composition comprising a bisphosphonate and a nucleoside reverse transcriptase inhibitor. In a specific embodiment, the invention provides methods for preventing or treating AIDS by administering a bisphosphonate-based compound in combination with 3'-azido-3'-deoxythymidine (AZT) to patients infected with AZTresistant HIV to improve the effectiveness of AZT therapy.
摘要翻译：本发明涉及包含切除抑制双膦酸盐和核苷逆转录酶抑制剂的新型组合物。本发明还涉及使用包含双膦酸盐和核苷逆转录酶抑制剂的组合物预防或治疗逆转录病毒相关疾病的方法。在一个具体实施方案中，本发明提供了通过将双膦酸盐类化合物与3'-叠氮基-3'-脱氧胸苷（AZT）组合施用于感染耐AZ抗药性HIV的患者来提高AZT疗法的有效性来预防或治疗AIDS的方法。

5. 发明申请

WO03064441A3 OLIGONUCLEOTIDES COMPRISING ALTERNATING SEGMENTS AND USES THEREOF 审中-公开
标题翻译：包含替代部分的寡核苷酸及其用途
公开(公告)号：WO03064441A3
公开(公告)日：2003-10-02
申请号：PCT/CA0300129
申请日：2003-01-31
申请人： UNIV MCGILL , DAMHA MASAD J , PARNIAK MICHAEL A
发明人： DAMHA MASAD J , PARNIAK MICHAEL A
IPC分类号： C12N15/09 , A61K31/7088 , A61K38/00 , A61K48/00 , A61P1/16 , A61P3/10 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/18 , A61P31/20 , A61P35/00 , C07H21/00 , C07H21/02 , C12N15/113 , C12Q1/68 , C12Q1/70 , A61K31/712 , C12N15/11
CPC分类号： C12N15/113 , A61K38/00 , C07H21/00 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/323 , C12N2310/3231 , C12N2310/346
摘要： The invention relates to oligonucleosides having alternating segments of sugar-modified nucleosides and 2'-deoxynucleosides, and uses thereof. The invention further relates to oligonucleotides having alternating segments of sugar-modified nucleotides and 2'-deoxynucleotides, and uses thereof. Such uses include the preparation of antisense oligonucleotides and their use for the prevention or depletion of function of a target nucleic acid of interest, such as an RNA, in a system. Accordingly, an oligonucleotide of the invention is useful for therapeutic, analytical and diagnostic methods and uses, as well as a component of compositions and commercial packages corresponding to such methods and uses.
摘要翻译：本发明涉及具有糖修饰核苷和2'-脱氧核苷的交替片段的寡核苷酸及其应用。本发明还涉及具有糖修饰的核苷酸和2'-脱氧核苷酸的交替片段的寡核苷酸及其应用。这样的用途包括制备反义寡核苷酸及其在系统中预防或消除目的靶核酸（例如RNA）的功能的用途。因此，本发明的寡核苷酸可用于治疗，分析和诊断方法和用途，以及对应于这些方法和用途的组合物和商业包装的组分。

6. 发明申请

WO2002020773A3 CHIMERIC ANTISENSE OLIGONUCLEOTIDES OF ARABINOFURANOSE ANALOGUES AND DEOXYRIBOSE NUCLEOTIDES 审中-公开
公开(公告)号：WO2002020773A3
公开(公告)日：2002-03-14
申请号：PCT/CA2001/001252
申请日：2001-09-04
申请人： MCGILL UNIVERSITY , DAMHA, Masad, José , PARNIAK, Michael, A. , LOK, Chun-Nam , VIAZOVKINA, Ekaterina
发明人： DAMHA, Masad, José , PARNIAK, Michael, A. , LOK, Chun-Nam , VIAZOVKINA, Ekaterina
IPC分类号： C12N15/11
摘要： The present invention relates to novel oligonucleotide chimera used as therapeutic agents to selectively prevent gene transcription and expression in a sequence-specific manner. In particular, this invention is directed to the selective inhibition of protein biosynthesis via antisense strategy using oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length. Particularly this invention relates to the use of antisense oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length, to hybridize to complementary RNA such as cellular messenger RNA, viral RNA, etc. More particularly this invention relates to the use of antisense oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length, to hybridize to and induce cleavage of (via RNaseH activation) the complementary RNA.

7. 发明申请

WO2005023270A3 COMPOSITIONS AND METHODS FOR USE OF ANTIVIRAL DRUGS IN THE TREATMENT OF RETROVIRAL DISEASES RESISTANT TO NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：组合物和方法的抗病毒药物逆转录病毒抵抗疾病治疗中的应用核苷类逆转录酶抑制剂
公开(公告)号：WO2005023270A3
公开(公告)日：2005-06-02
申请号：PCT/US2004029375
申请日：2004-09-09
申请人： UNIV PITTSBURGH , UNIV ILLINOIS , PARNIAK MICHAEL , MELLORS JOHN W , OLDFIELD ERIC , TOVIAN ZEV , CHAN JULIAN MUN WENG
发明人： PARNIAK MICHAEL , MELLORS JOHN W , OLDFIELD ERIC , TOVIAN ZEV , CHAN JULIAN MUN WENG
IPC分类号： A61K31/66 , A61K31/663 , A61K31/7072 , A61K45/06 , A61P31/18
CPC分类号： A61K31/663 , A61K31/66 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： The present invention relates to novel compositions comprising an excisioninhibiting bisphosphonate and a nucleoside reverse transcriptase inhibitor. The present invention also relates to methods for preventing or treating retrovirus-related diseases using a composition comprising a bisphosphonate and a nucleoside reverse transcriptase inhibitor. In a specific embodiment, the invention provides methods for preventing or treating AIDS by administering a bisphosphonate-based compound in combination with 3'-azido-3'-deoxythymidine (AZT) to patients infected with AZTresistant HIV to improve the effectiveness of AZT therapy.
摘要翻译：本发明涉及包含切除抑制剂二膦酸盐和核苷逆转录酶抑制剂的新型组合物。本发明还涉及使用包含双膦酸盐和核苷逆转录酶抑制剂的组合物预防或治疗逆转录病毒相关疾病的方法。在一个具体的实施方案中，本发明提供用于预防或通过用3'-叠氮基-3'-脱氧胸苷（AZT）与AZTresistant HIV感染来提高AZT治疗的有效性的患者组合施用基于双膦酸酯类化合物治疗AIDS的方法。

8. 发明申请

WO03012127A3 ASSAY FOR IDENTIFYING INHIBITORS OF HIV RT DIMERIZATION 审中-公开
标题翻译：分析鉴定HIV逆转录酶抑制剂的抑制剂
公开(公告)号：WO03012127A3
公开(公告)日：2003-10-16
申请号：PCT/CA0201162
申请日：2002-07-26
申请人： BOEHRINGER INGELHEIM CA LTD , SLUIS-CREMER NICOLAS , PARNIAK MICHAEL , PELLETIER ALEX
发明人： SLUIS-CREMER NICOLAS , PARNIAK MICHAEL , PELLETIER ALEX
IPC分类号： G01N33/53 , A61K38/00 , C07K2/00 , C07K4/00 , C07K5/00 , C07K7/00 , C07K14/00 , C07K16/00 , C07K17/00 , C12N15/09 , C12P19/34 , C12P21/06 , C12Q1/48 , C12Q1/68 , C12Q1/70 , G01N21/78 , G01N33/15 , G01N33/50
CPC分类号： C12Q1/48 , G01N2333/9125 , G01N2500/02
摘要： A method for measuring heterodimerization of HIV RT, which comprises the steps of:a) providing a first solution comprising p66 subunit homodimers in the presence of a dissociation agent; b) contacting the first solution with p51 RT subunits and incubating in the presence of a reassociation buffer to allow association of a complex of p66/p51 RT subunits, wherein one of the subunits comprises an affinity tag and the other of the subunits comprises a detectable label; c) contacting the incubate of step b) with an affinity medium under conditions that enable the p66/p51 complex to bind to the affinity medium; and d) determining the amount of complex formed by measuring the level of detectable label bound to the affinity medium (or by measuring the reconstituted RT polymerase activity). Steps a) to d) can be carried out in the presence or absence of a test compound followed by e) comparing the test compound sample to a control sample lacking the compound, whereby modulated p66/p51 complex formation in the test compound sample is indicative of the ability of the compound to modulate, inhibit or enhance heterodimerization.The method can be used to screen for inhibitors of HIV RT dimerization.
摘要翻译：用于测量HIV RT的异源二聚化的方法，其包括以下步骤：a）在解离剂存在下提供包含p66亚基同源二聚体的第一溶液; b）使第一溶液与p51RT亚基接触，并在重新结合缓冲液存在下温育以允许p66 / p51RT亚基复合物的缔合，其中一个亚基包含亲和标签并且另一个亚基包含可检测的标签; c）在能够使p66 / p51复合物结合亲和介质的条件下，将步骤b）的孵育物与亲和介质接触; 和d）通过测量与亲和介质结合的可检测标记的水平（或通过测量重建的RT聚合酶活性）来确定形成的复合物的量。可以在存在或不存在测试化合物的情况下进行步骤a）至d），然后e）将测试化合物样品与缺乏该化合物的对照样品进行比较，由此在测试化合物样品中调节的p66 / p51复合物形成是指示性的该化合物调节，抑制或增强异二聚化的能力。该方法可用于筛选HIV RT二聚化的抑制剂。

9. 发明申请

WO2003037909A1 ACYCLIC LINKER-CONTAINING OLIGONUCLEOTIDES AND USES THEREOF 审中-公开
标题翻译：含有交联链接的寡核苷酸及其用途
公开(公告)号：WO2003037909A1
公开(公告)日：2003-05-08
申请号：PCT/CA2002/001628
申请日：2002-10-29
申请人： McGILL UNIVERSITY , DAMHA, Masad, J. , VIAZOVKINA, Ekaterina , MANGOS, Maria, M. , PARNIAK, Michael, A. , MIN, Kyung-Lyum
发明人： DAMHA, Masad, J. , VIAZOVKINA, Ekaterina , MANGOS, Maria, M. , PARNIAK, Michael, A. , MIN, Kyung-Lyum
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H21/02
摘要： Oligonucleotides having an internal acyclic linker residue, and the preparation and uses thereof, are described. Such uses include the preparation of acyclic linker-containing antisense oligonucleotides, and their use for the prevention or depletion of function of a target nucleic acid of interest, such as RNA, in a system. Such a prevention or depletion of .function includes, for example, the prevention or inhibition of the expression, reverse transcription and/or replication of the target nucleic acid, as well as the cleavage/degradation of the target nucleic acid. Accordingly, an oligonucleotide of the invention is useful for analytical and therapeutic methods and uses in which the function of a target nucleic acid is implicated, as well as a component of commercial packages corresponding to such methods and uses.
摘要翻译：描述了具有内部无环接头残基的寡核苷酸及其制备和用途。这样的用途包括制备无环连接体的反义寡核苷酸，以及它们在系统中用于预防或消除靶核酸如RNA的功能的用途。功能的这种预防或消除包括例如预防或抑制靶核酸的表达，逆转录和/或复制以及靶核酸的切割/降解。因此，本发明的寡核苷酸可用于涉及靶核酸的功能的分析和治疗方法和用途，以及对应于这些方法和用途的商业包装的组分。

10. 发明申请

WO0220773A2 CHIMERIC ANTISENSE OF ARABINOFURANOSE ANALOGUE AND DEOXYRIBOSE NUCLEOTIDES 审中-公开
标题翻译：阿拉伯呋喃糖苷类似物和脱氧核糖核酸的重要抗体
公开(公告)号：WO0220773A2
公开(公告)日：2002-03-14
申请号：PCT/CA0101252
申请日：2001-09-04
申请人： UNIV MCGILL , DAMHA MASAD JOSE , PARNIAK MICHAEL A , LOK CHUN NAM , VIAZOVKINA EKATERINA
发明人： DAMHA MASAD JOSE , PARNIAK MICHAEL A , LOK CHUN-NAM , VIAZOVKINA EKATERINA
IPC分类号： C12N15/09 , A61K31/712 , A61K48/00 , A61P31/12 , A61P43/00 , C12N15/113 , C12N15/11
CPC分类号： C12N15/113 , C12N2310/315 , C12N2310/32 , C12N2310/322 , C12N2310/341 , C12N2310/346
摘要： The present invention relates to novel oligonucleotide chimera used as therapeutic agents to selectively prevent gene transcription and expression in a sequence-specific manner. In particular, this invention is directed to the selective inhibition of protein biosynthesis via antisense strategy using oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length. Particularly this invention relates to the use of antisense oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length, to hybridize to complementary RNA such as cellular messenger RNA, viral RNA, etc. More particularly this invention relates to the use of antisense oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length, to hybridize to and induce cleavage of (via RNaseH activation) the complementary RNA.
摘要翻译：本发明涉及用作治疗剂的新型寡核苷酸嵌合体，其以序列特异性方式选择性地预防基因转录和表达。特别地，本发明涉及通过使用由阿拉伯核苷酸或修饰的阿拉伯糖核苷酸残基构建的寡核苷酸的反义策略来选择性抑制蛋白质生物合成，其侧翼是一系列可变长度的脱氧核糖核苷酸残基。特别地，本发明涉及由一系列可变长度的脱氧核糖核苷酸残基侧翼的阿拉伯核苷酸或修饰的阿拉伯糖核苷酸残基构建的反义寡核苷酸与互补RNA如细胞信使RNA，病毒RNA等杂交的用途。更具体地说，本发明涉及使用由阿拉伯核苷酸或修饰的阿拉伯糖核苷酸残基构建的反义寡核苷酸，侧翼于一系列可变长度的脱氧核糖核苷酸残基，与互补RNA杂交并诱导（通过RNaseH激活）切割。

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