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1. 发明申请

WO2005062049A3 THE USE OF MICROELECTRONIC STRUCTURES FOR PATTERNED DEPOSITION OF MOLECULES ONTO SURFACES 审中-公开
标题翻译：微电子结构在分子表面沉积上的应用
公开(公告)号：WO2005062049A3
公开(公告)日：2005-12-15
申请号：PCT/BE2004000182
申请日：2004-12-22
申请人： IMEC INTER UNI MICRO ELECTR , DE KEERSMAECKER KOEN , BORGHS GUSTAAF , LEUVEN K U RES & DEV
发明人： DE KEERSMAECKER KOEN , BORGHS GUSTAAF , HERDEWIJN PIET
IPC分类号： G01N33/543
CPC分类号： B82Y15/00 , B82Y30/00 , G01N33/54366 , H01L2924/0002 , H01L2924/00
摘要： The present invention is related to the localised/patterned deposition and/or desorption of (bio)molecules using microelectronic structures. Often pre-existing structures needed for proper functioning of the device (e.g. sensors, ...) can be used as individually addressable control structures to achieve localised deposition through thermal and/or electrochemical spotting, thereby reducing the need for and simplifying additional processing steps to achieve localised/patterned deposition. If these multi-purpose structures are not available, additional control structures can be implemented, using microelectronic VLSI production technology.
摘要翻译：本发明涉及使用微电子结构的（生物）分子的局部/图案化沉积和/或解吸附。通常，设备（例如传感器，...）正常运行所需的预先存在的结构可以被用作单独寻址的控制结构，以通过热和/或电化学点样实现局部沉积，从而减少对附加处理步骤的需要和简化以实现局部/图案化沉积。如果这些多用途结构不可用，则可以使用微电子VLSI生产技术实现附加的控制结构。

2. 发明申请

WO2005113571A3 METHODS FOR THE DELIVERY OF OLIGOMERIC COMPOUNDS 审中-公开
标题翻译：递送低分子化合物的方法
公开(公告)号：WO2005113571A3
公开(公告)日：2006-12-14
申请号：PCT/US2005016746
申请日：2005-05-13
申请人： UNIV NORTH CAROLINA , LEUVEN K U RES & DEV , JULIANO RUDY , KANG HYUNMIN , ASTRIAB-FISHER ANNA , HERDEWIJN PIET , CHALTIN PATRICK , VAN AERSCHOT ARTHUR
发明人： JULIANO RUDY , KANG HYUNMIN , ASTRIAB-FISHER ANNA , HERDEWIJN PIET , CHALTIN PATRICK , VAN AERSCHOT ARTHUR
IPC分类号： C07H21/04 , A61K31/70 , C12N15/11 , C12N15/113 , C12Q1/68
CPC分类号： C12N15/1138 , C07H21/04 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/341 , C12N2310/3513 , C12N2310/3515 , C12N2310/53 , C12N2320/32 , C12N2320/51 , C12N2310/3521 , C12N2310/3525 , C12N2310/3527
摘要： The presently disclosed subject matter relates to the delivery of oligonucleotides to cells through the delivery of a composition or reagent comprising a hybridization complex comprising a first antisense oligonucleotide which is modified to have a higher stability against degradation, and a second sense oligonucleotide which is prone to degradation. The presently disclosed subject matter furthermore relates to dendrimeric bioconjugates and compositions or reagents comprising them, wherein the bioconjugate comprises a conjugate moiety coupled to a dendrimeric structure and to their use to deliver oligomeric compounds including oligonucleotides or duplexes, as described above, to cells for modulation of gene expression (i.e. antisense or antigene therapy/research, RNA interference).
摘要翻译：目前公开的主题涉及通过递送包含杂交复合物的组合物或试剂递送寡核苷酸，所述杂交复合物包含经修饰以具有较高抗降解稳定性的第一反义寡核苷酸，以及易于降解。目前公开的主题还涉及含有它们的树枝状聚合生物共轭物和组合物或试剂，其中生物缀合物包含与树枝状大分子结构偶联的缀合物部分，以及它们用于将如上所述的寡核苷酸或双链体的寡聚化合物递送至用于调制的细胞的基因表达（即反义或反向治疗/研究，RNA干扰）。

3. 发明申请

WO2006047842A2 MODIFIED NUCLEOSIDES FOR RNA INTERFERENCE 审中-公开
标题翻译：用于RNA干扰的修饰核苷酸
公开(公告)号：WO2006047842A2
公开(公告)日：2006-05-11
申请号：PCT/BE2005000159
申请日：2005-11-08
申请人： LEUVEN K U RES & DEV , UNIV NORTH CAROLINA , HERDEWIJN PIET , VAN AERSCHOT ARTHUR , WANG JING , JULIANO RUDY
发明人： HERDEWIJN PIET , VAN AERSCHOT ARTHUR , WANG JING , JULIANO RUDY
IPC分类号： C12N15/11 , C12N15/113
CPC分类号： C12N15/111 , A61K31/712 , C07D487/04 , C12N15/1138 , C12N2310/14 , C12N2310/323 , C12N2320/51 , C12N2330/30
摘要： The present invention relates to the use of modified nucleotides and single or double stranded oligonucleotides comprising at least one of said modified nucleotides for performing RNA interference. The modified nucleotides are selected from 6-membered ring containing nucleotides such as hexitol, altritol, O-subsituted or O-alkylated altritol, cyclohexenyl, ribo-cyclohexenyl and O-subsituted or O-alkylated ribo-cyclohexenyl nucleotides. The present invention also relates to novel modified nucleosides or nucleotides and to the use of said novel modified nucleosides and nucleotides in single or double stranded oligonucleotides for RNA interference, antisense therapy or other applications.
摘要翻译：本发明涉及修饰的核苷酸和包含至少一个所述修饰的核苷酸的单链或双链寡核苷酸用于进行RNA干扰的用途。修饰的核苷酸选自含有6员环的核苷酸，例如己糖醇，阿卓糖醇，O-取代的或O-烷基化的阿卓糖醇，环己烯基，核 - 环己烯基和O-取代的或O-烷基化的核 - 环己烯基核苷酸。本发明还涉及新的修饰的核苷或核苷酸以及所述新的修饰的核苷和核苷酸在单链或双链寡核苷酸中用于RNA干扰，反义治疗或其他应用的用途。

4. 发明申请

WO2008104408A3 PHOSPHATE MODIFIED NUCLEOSIDES USEFUL AS SUBSTRATES FOR POLYMERASES AND AS ANTIVIRAL AGENTS 审中-公开
标题翻译：有用的磷酸改性核苷作为聚合物和抗病毒剂的基质
公开(公告)号：WO2008104408A3
公开(公告)日：2008-12-04
申请号：PCT/EP2008001764
申请日：2008-02-27
申请人： LEUVEN K U RES & DEV , ADELFINSKAYA OLGA , HERDEWIJN PIET
发明人： ADELFINSKAYA OLGA , HERDEWIJN PIET
IPC分类号： C07H19/00 , A61K31/7052 , A61K31/7076 , C07H19/02 , C07H19/10 , C07H19/20
CPC分类号： C07H19/02 , C07H19/10 , C07H19/20
摘要： This invention provides phosphate-modified nucleosides represented by the structural formula: wherein - B is a pyrimidine or purine base, or an analogue thereof, optionally substituted with one or two substituents independently selected from the group consisting of halogen, hydroxyl, sulfhydryl, methyl, ethyl, amino and methylamino; - R1 is H or OH; - R3 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl, aryl-C1-6alkyl and 2-cyanoethyl, wherein said C1-6 alkyl, C3-6 cycloalkyl or aryl-C1-6 alkyl is optionally substituted with one or more, preferably 1, 2 or 3, substituents independently selected from the group consisting of halogen, OH, C1-6 alkoxy, trifluoromethyl, trifluoromethoxy, nitro, cyano and amino; - W is O or S; and - R2 is a group derived from an amino-acid. These compounds are useful as substrates for DNA/RNA polymerases, and as anti-viral agents.
摘要翻译：本发明提供了由结构式表示的磷酸酯修饰的核苷：其中-B是嘧啶或嘌呤碱或其类似物，任选地被一个或两个独立地选自卤素，羟基，巯基，甲基，乙基，氨基和甲基氨基; -R 1是H或OH; -R 3选自H，C 1-6烷基，C 3-6环烷基，芳基-C 1-6烷基和2-氰基乙基，其中所述C 1-6烷基，C 3-6环烷基或芳基-C 1-6烷基是任选地被一个或多个，优选1,2或3个独立地选自卤素，OH，C 1-6烷氧基，三氟甲基，三氟甲氧基，硝基，氰基和氨基的取代基取代; - W是O或S; 和 - R2是衍生自氨基酸的基团。这些化合物可用作DNA / RNA聚合酶和作为抗病毒剂的底物。

5. 发明申请

WO0149687A2 CYCLOHEXENE NUCLEIC ACIDS 审中-公开
标题翻译：环己烯核酸
公开(公告)号：WO0149687A2
公开(公告)日：2001-07-12
申请号：PCT/IB0002041
申请日：2000-12-27
申请人： LEUVEN K U RES & DEV , WANG JING , HERDEWIJN PIET
发明人： WANG JING , HERDEWIJN PIET
IPC分类号： G01N33/68 , A61K9/08 , A61K9/14 , A61K31/712 , A61P25/00 , A61P43/00 , C07D473/34 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/09 , C07D473/00
CPC分类号： C07H21/00 , C07D473/34
摘要： Replacement of the furanose moiety of, for example, DNA by a cyclohexene ring gives a new nucleic acid structure: cyclohexene nucleic acids or CeNA. Cyclohexene nucleic acids can be obtained by the classical phosphoramidite chemistry starting from protected cyclohexenyl nucleoside building blocks. Incorporation of cyclohexenyl nucleosides in a DNA chain increases the stability of a DNA/RNA hybrid, the complex formed between cyclohexenyl oligoadenylate and its DNA or RNA complement is of similar stability. CD and NMR studies indicate easy conformational adaptation of a cyclohexenyl nucleoside when incorporated in a natural nucleic acid structure. CeNA is stable against degradation in serum and a CeNA/RNA hybrid is able to activate E. Coli Rnase H, resulting in cleavage of the RNA strand.
摘要翻译：通过环己烯环代替例如DNA的呋喃糖部分得到新的核酸结构：环己烯核酸或CeNA。环己烯核酸可以通过经保护的环己烯基核苷结构从经典的亚磷酰胺化学中获得。环己烯基核苷在DNA链中的引入提高了DNA / RNA杂交体的稳定性，环己烯基寡腺苷酸与其DNA或RNA补体之间形成的复合物具有相似的稳定性。 CD和NMR研究表明当掺入天然核酸结构时，环己烯基核苷的容易构象适应。 CeNA对血清中的降解是稳定的，并且CeNA / RNA杂交体能够激活大肠杆菌Rnase H，导致RNA链的切割。

6. 发明申请

WO0149687A9 CYCLOHEXENE NUCLEIC ACIDS 审中-公开
标题翻译：环己烯核酸
公开(公告)号：WO0149687A9
公开(公告)日：2002-09-06
申请号：PCT/IB0002041
申请日：2000-12-27
申请人： LEUVEN K U RES & DEV , WANG JING , HERDEWIJN PIET
发明人： WANG JING , HERDEWIJN PIET
IPC分类号： G01N33/68 , A61K9/08 , A61K9/14 , A61K31/712 , A61P25/00 , A61P43/00 , C07D473/34 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/09 , A61K31/70
CPC分类号： C07H21/00 , C07D473/34
摘要： Replacement of the furanose moiety of, for example, DNA by a cyclohexene ring gives a new nucleic acid structure: cyclohexene nucleic acids or CeNA. Cyclohexene nucleic acids can be obtained by the classical phosphoramidite chemistry starting from protected cyclohexenyl nucleoside building blocks. Incorporation of cyclohexenyl nucleosides in a DNA chain increases the stability of a DNA/RNA hybrid, the complex formed between cyclohexenyl oligoadenylate and its DNA or RNA complement is of similar stability. CD and NMR studies indicate easy conformational adaptation of a cyclohexenyl nucleoside when incorporated in a natural nucleic acid structure. CeNA is stable against degradation in serum and a CeNA/RNA hybrid is able to activate E. Coli Rnase H, resulting in cleavage of the RNA strand.
摘要翻译：例如用环己烯环替代DNA的呋喃糖部分产生新的核酸结构：环己烯核酸或CeNA。环己烯核酸可以由经保护的环己烯基核苷结构单元开始的经典亚磷酰胺化学获得。将环己烯基核苷掺入DNA链增加了DNA / RNA杂合体的稳定性，环己烯基低聚腺苷酸与其DNA或RNA补体之间形成的复合物具有相似的稳定性。 CD和NMR研究表明，当掺入天然核酸结构时，环己烯基核苷容易构象适应。 CeNA对血清中的降解稳定并且CeNA / RNA杂合体能够激活大肠杆菌RNA酶H，导致RNA链的切割。

7. 发明申请

WO2005085268A2 PHOSPONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION 审中-公开
标题翻译：用作治疗病毒感染的药物组合物中的活性成分和用于其生产的中间体的膦酸核苷
公开(公告)号：WO2005085268A2
公开(公告)日：2005-09-15
申请号：PCT/BE2005000032
申请日：2005-03-04
申请人： LEUVEN K U RES & DEV , HERDEWIJN PIET , PANNECOUQUE CHRISTOPHE , WU TONGFEI , DE CLERCQ ERIK
发明人： HERDEWIJN PIET , PANNECOUQUE CHRISTOPHE , WU TONGFEI , DE CLERCQ ERIK
IPC分类号： A61K31/706 , C07H19/00 , C07H19/06 , C07H19/16
CPC分类号： C07H19/20 , C07F7/0812 , C07H1/00 , C07H15/04 , C07H17/02 , C07H19/00 , C07H19/06 , C07H19/10 , C07H19/16
摘要： The present invention relates to novel phosponate nucleosides, more specifically to novel phosponalkoxy substituted nucleosides. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.
摘要翻译：本发明涉及新的磷酸核苷，更具体地涉及新的磷酸烷氧基取代的核苷。本发明进一步涉及具有HIV（人免疫缺陷病毒）复制抑制特性的化合物和涉及相对于其他病毒具有抗病毒活性的化合物。本发明还涉及制备所有这些化合物的方法和包含它们的药物组合物。本发明进一步涉及所述化合物作为药物的用途以及用于制造用于治疗患有HIV感染的受试者以及用于治疗其他病毒，逆转录病毒或慢病毒感染以及治疗动物的药物的用途患有FIV，病毒，逆转录病毒或慢病毒感染。

8. 发明专利

ES2376998T3 Derivados de N-aminoimidazol inhibidores de HIV 未知
公开(公告)号：ES2376998T3
公开(公告)日：2012-03-21
申请号：ES01919343
申请日：2001-02-23
申请人： LEUVEN K U RES & DEV
发明人： DE CLERCQ ERIK , VAN AERSCHOT ARTHUR , HERDEWIJN PIET , LAGOJA IRENE , PANNECOUCQUE CHRISTOPHE
IPC分类号： C07D233/84 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K45/00 , A61P31/12 , A61P31/18 , A61P35/00 , C07D233/54 , C07D233/64 , C07D233/90
摘要： Un derivado de N-aminoimidazol o N-aminoimidazoltiona, una sal farmacéuticamente aceptable, un tautómero o una forma estereoquímicamente isómera del mismo, siendo dicho derivado un compuesto representado por la fórmula general (I): en la cual: m es cero o 1; n es cero o 1; R1 se selecciona entre hidrógeno, metilo, etilo, propilo o isopropilo; R2 se selecciona entre hidrógeno y -SH; Q se selecciona entre 1-naftilo, 2-naftilo, bifenilo, 2-piridilo, 3-piridilo, 4-piridilo, 2-pirimidilo, 4-pirimidilo, 5-pirimidilo, tienilo, carboxilo, aminocarbonilo, alquilamino-carbonilo, dialquilaminocarbonilo, fenilaminocarbonilo, alquiloxicarbonilo o fenilo; en que el alquilo es un metilo, etilo, propilo o isopropilo y fenilo es un anillo fenilo sustituido o sin sustituir representado por la fórmula general (II) en la que o es 1 ó 2, y R3 se selecciona entre H, F, Cl, Br, I, hidroxi, alquiloxi, amino, alquilamino, dialquilamino, ciano, nitro, carboxilo, aminocarbonilo, alquilaminocarbonilo, aquiloxicarbonilo, metilo, etilo, propilo, isopropilo o haloalquilo C1-3 en el que haloalquilo contiene 1 a 4 haloátomos y alquilo se selecciona entre metilo, etilo, propilo o isopropilo; L se selecciona entre 1-naftilo, 2-naftilo, bifenilo, 2-piridilo, 3-piridilo, 4-piridilo, 2-pirimidilo, 4-pirimidilo, 5-pirimidilo, tienilo o un anillo fenilo sustituido o sin sustituir representado por la fórmula general (III) en la que p es 1 ó 2 y R4 se selecciona entre H, F, Cl, Br, I, hidroxi, alquiloxi, amino, alquilamino, dialquilamino, ciano, nitro, carboxilo, aminocarbonilo, alquilaminocarbonilo, alquiloxicarbonilo, metilo, etilo, propilo, isopropilo o haloalquilo C1-3 en que haloalquilo contiene 1 a 4 haloátomos y alquilo se selecciona entre metilo, etilo, propilo o isopropilo, con la condición de que el compuesto (I) no se selecciona entre 1-(3-Clorofenilamino)-2,3-dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 1-(2-Clorofenilamino)-2,3-dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 1-(4-Clorofenilamino)-2,3-dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 1-(fenilamino)-2,3-Dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 1-(4-nitrofenilamino)-2,3-dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 1-(4-metilfenilamino)-2,3-dihidro-4-metil-5-5 fenil-1H-imidazol-2-tiona; 1-(4-metiloxifenilamino)-2,3-dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 1-(bencilamino)-2,3-dihidro-4-metil-5-fenil-1H-imidazol-2-tiona; 4-Metil-5-fenil-1-fenilamino-1H-imidazol; 4-Metil-5-fenil-1-(4-nitrofenil)amino-1H-imidazol; 10 4-Metil-5-fenil-1-(4-clorofenil)amino-1H-imidazol; 4-Metil-5-fenil-1-(4-metilfenil)amino-1H-imidazol; o 4-Metil-5-fenil-1-(4-metiloxifenil)amino-1H-imidazol.

9. 发明专利

AT532771T 未知
公开(公告)号：AT532771T
公开(公告)日：2011-11-15
申请号：AT01919343
申请日：2001-02-23
申请人： LEUVEN K U RES & DEV
发明人： DE CLERCQ ERIK , VAN AERSCHOT ARTHUR , HERDEWIJN PIET , LAGOJA IRENE , PANNECOUCQUE CHRISTOPHE
IPC分类号： C07D233/84 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K45/00 , A61P31/12 , A61P31/18 , A61P35/00 , C07D233/54 , C07D233/64 , C07D233/90
摘要： An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R 1 is selected from hydrogen, methyl or ethyl, R 2 is selected from hydrogen, SH or -SR 0 wherein R 0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl. This invention further relates to the use of compounds of formula (I) as agents having biological activity, especially against viral infections.

10. 发明专利

SG170825A1 PHOSPONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION 未知
公开(公告)号：SG170825A1
公开(公告)日：2011-05-30
申请号：SG2011023728
申请日：2005-03-04
申请人： LEUVEN K U RES & DEV
发明人： HERDEWIJN PIET , PANNECOUQUE CHRISTOPHE , WU TONGFEI , DE CLERCQ ERIK
IPC分类号： A61K31/706 , C07H19/00 , C07H19/06 , C07H19/16
摘要： The present invention relates to novel phosponate nucleosides, more specifically to novel phosponalkoxy substituted nucleosides. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections. No Suitable Figure

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