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11. 发明申请

US20100286377A1 BIOMOLECULES HAVING MULTIPLE ATTACHMENT MOIETIES FOR BINDING TO A SUBSTRATE SURFACE 有权
标题翻译：具有多个附着力的生物分子结合到基底表面
公开(公告)号：US20100286377A1
公开(公告)日：2010-11-11
申请号：US11655009
申请日：2007-01-18
申请人： Markus Schweitzer , Norbert Windhab , John R. Havens , Thomas J. Onofrey , Charles Greef , Daguang Wang
发明人： Markus Schweitzer , Norbert Windhab , John R. Havens , Thomas J. Onofrey , Charles Greef , Daguang Wang
IPC分类号： C07H21/02 , C07H21/00 , C07H21/04
CPC分类号： C07H19/04 , C07H21/00 , C12Q1/68 , G01N33/54353
摘要： Methods of binding biomolecules to a substrate are provided that include contacting the biomolecule with a branched linking moiety to form a branched linking structure. The branched linking structure is then contacted with a binding moiety on the substrate to form a coupled substrate binding structure, thereby binding the biomolecule to the substrate. The biomolecule may contain a Lewis base or a nucleophile to react with a Lewis acid or electrophile in the branched linking moiety. Alternatively, the biomolecule may contain a Lewis acid or electrophile that can react with a Lewis base or nucleophile in the branched linking moiety. Additionally, the biomolecule can be bound to the substrate through a covalent or non-covalent bond.
摘要翻译：提供了将生物分子与底物结合的方法，包括使生物分子与支链连接部分接触以形成支链结构。然后将支链连接结构与基底上的结合部分接触以形成偶联的底物结合结构，从而将生物分子结合到底物上。生物分子可以含有路易斯碱或亲核试剂以与支链连接部分中的路易斯酸或亲电子试剂反应。或者，生物分子可以含有路易斯酸或亲电子试剂，其可以与支链连接部分中的路易斯碱或亲核试剂反应。此外，生物分子可以通过共价或非共价键与底物结合。

12. 发明授权

US07129229B2 Hydrazide building blocks and hydrazide modified biomolecules 有权
标题翻译：酰肼结构单元和酰肼改性生物分子
公开(公告)号：US07129229B2
公开(公告)日：2006-10-31
申请号：US10344092
申请日：2001-08-10
申请人： Stefan Raddatz , Jochen Müller-Ibeler , Markus Schweitzer , Christoph Brücher , Norbert Windhab , John R. Havens , Thomas J. Onofrey , Charles H. Greef , Daguang Wang
发明人： Stefan Raddatz , Jochen Müller-Ibeler , Markus Schweitzer , Christoph Brücher , Norbert Windhab , John R. Havens , Thomas J. Onofrey , Charles H. Greef , Daguang Wang
IPC分类号： A61K31/66 , C07F9/02
CPC分类号： A61K31/66 , C07F9/2408 , C07F9/2429
摘要： This invention relates to attachment chemistries for binding macromolecules to a substrate surface or to other conjugation targets. More particularly, this invention relates to attachment chemistries involving branched or linear structures having one or more hydrazide attachment moieties for binding the macromolecules to a substrate surface, or for other conjugation reactions. Novel modifying reagents are provided for the introduction of protected hydrazide attachment moieties or precursor forms of such hydrazides to the macromolecule, either as a single hydrazide or as multiple hydrazides.
摘要翻译：本发明涉及用于将大分子结合到底物表面或其它共轭靶的附着化学物质。更具体地说，本发明涉及包含具有一个或多个用于将大分子结合到底物表面或其它共轭反应的一个或多个酰肼连接部分的支链或线性结构的附着化学物质。提供了新的改性试剂，用于将受保护的酰肼连接部分或这种酰肼的前体形式引入高分子，作为单酰肼或多个酰肼。

13. 发明申请

US20050053945A1 Process for the preparation of a pentopyranosyl conjugate 审中-公开
标题翻译：制备戊吡喃糖结合物的方法
公开(公告)号：US20050053945A1
公开(公告)日：2005-03-10
申请号：US10654274
申请日：2003-09-02
申请人： Christian Miculka , Norbert Windhab , Tilmann Brandstetter , Gerhard Burdinski
发明人： Christian Miculka , Norbert Windhab , Tilmann Brandstetter , Gerhard Burdinski
IPC分类号： C12Q1/68 , A61K49/00 , C07H1/00 , C07H19/04 , C07H19/067 , C07H21/00 , C07K16/00 , G01N33/532 , G01N33/53 , C07H21/02 , C07H21/04 , C07K16/46
CPC分类号： C07H21/00 , A61K47/549 , A61K49/0013 , C07H19/04 , C07H21/02 , C07H21/04 , G01N33/532 , Y02P20/55 , Y10S977/728 , Y10S977/80 , Y10S977/836 , Y10S977/894 , Y10S977/896 , Y10S977/904 , Y10S977/914 , Y10S977/915 , Y10S977/924 , Y10S977/925
摘要： The invention relates to a pentopyranosylnucleoside of the formula (I) or of the formula (II) their preparation and use for the production of a therapeutic, diagnostic and/or electronic component.
摘要翻译：本发明涉及式（I）或式（II）的戊吡喃糖基核苷及其制备和用于制备治疗，诊断和/或电子成分的方法。

14. 发明授权

US06699978B1 Linker nucleoside, and production and use of the same 有权
标题翻译：连接核苷，生产和使用相同
公开(公告)号：US06699978B1
公开(公告)日：2004-03-02
申请号：US09509011
申请日：2000-07-11
申请人： Christian Miculka , Norbert Windhab , Tilmann Brandstetter , Stefan Scherer
发明人： Christian Miculka , Norbert Windhab , Tilmann Brandstetter , Stefan Scherer
IPC分类号： C07H1900
CPC分类号： G01N33/532 , A61K47/54 , A61K47/549 , B82Y10/00 , C07H19/04 , C07H21/00 , H01L51/0093 , Y02P20/55
摘要： The present invention relates to a linker nucleoside, its preparation and use for the covalent bonding of biomolecules to oligonucleotides, in particular p-RNA oligonucleotides.
摘要翻译：本发明涉及连接体核苷，其制备和用于将生物分子共价键合到寡核苷酸，特别是p-RNA寡核苷酸的用途。

15. 发明授权

US06689884B1 Supramolecular pairing system, its preparation and use 有权
标题翻译：超分子配对体系，其制备和应用
公开(公告)号：US06689884B1
公开(公告)日：2004-02-10
申请号：US09509040
申请日：2000-08-03
申请人： Christian Miculka , Norbert Windhab , Albert Eschenmoser , Stefan Scherer , Gerhard Quinkert
发明人： Christian Miculka , Norbert Windhab , Albert Eschenmoser , Stefan Scherer , Gerhard Quinkert
IPC分类号： C07D23900
CPC分类号： C12Q1/68
摘要： The invention relates to a compound of formula (I), wherein R1 is NR3R4, OR3 or SR3 with R3 and R4 being H or CnH2n+1 independently of each other and being the same or different, n being a whole number from 1 to 12; R2 is equal to CmH2m—C(X)—Y with X being ═O, ═S or ═N, Y being equal to OR3, NR3R4 or SR3, R3 and R4 having the same meaning given above, and m being a whole number from 1 to 4; or R2 is equal to CmH2m—Z—Y′ with Z being a sulfonyl, phosphonyl, ether or amine group, Y′ being equal to H, CnH2n+1, OR3, NR3R4 or SR3 then Z is sulphonyl or phosphonyl group, n, R3 and R4 having the meaning given above, and Y′ being equal to CnH2n+1 when Z is an ether or an amine group; A, B, and D are the same or different and mean CR5R6, O, NR7 ou S independently of each other with R5, R6 and R7 being H or CnH2n+1, independently of each other, n having the meaning given above; and C is equal to CR8 or N with R8 having the meaning of R5 independently, A—B, B—C or C—D not being two identical heteroatoms; and nucleobase means thymine, uracile, adenine, cytosine, guanine, isocytosine, isoguanine, xanthine or hypoxanthine. The invention also relates to a method for producing these derivatives and to their use in pairing and/or testing systems.
摘要翻译：本发明涉及式（I）化合物，其中R 1为NR 3 R 4，OR 3或SR 3，R 3和R 4为H或C n H 2n +1彼此独立且相同或不同，n为1至12的整数; R 2等于CmH2m-C（X）-Y，其中X为= O，= S或= N，Y等于OR 3，NR 3 R 4或SR 3， R 3和R 4具有上述相同的含义，m为1至4的整数; 或R 2等于C m H 2 m-Z Y'，其中Z是磺酰基，膦酰基，醚或胺基，Y'等于H，C n H 2n + 1，OR 3，NR 3 R 4或当Z为醚或胺基时，Z为磺酰基或膦酰基，n，R 3和R 4具有上述含义，Y'等于C n H 2n + 1; A，B和D相同或不同，并且R 5，R 6和R 7独立地为CR 5，R 6和R 7独立地为CR 5 R 6，O，NR 7 H或C n H 2n + 1彼此独立地具有上述含义的n; 并且C等于CR 8或N，其中R 8独立地具有R 5的含义，A-B，B-C或C-D不是两个相同的杂原子; 核碱基是指胸腺嘧啶，尿嘧啶，腺嘌呤，胞嘧啶，鸟嘌呤，异胞嘧啶，异鸟嘌呤，黄嘌呤或次黄嘌呤。本发明还涉及一种制备这些衍生物的方法及其在配对和/或测试系统中的用途。

16. 发明授权

US06506896B1 Use of a pentopyranosyl nucleoside for producing an electronic component, and conjugates of said pentopyranosyl nucleoside 有权
标题翻译：戊吡喃糖基核苷用于制备电子成分的用途，以及所述五倍吡喃糖基核苷的共轭物
公开(公告)号：US06506896B1
公开(公告)日：2003-01-14
申请号：US09509039
申请日：2000-07-11
申请人： Christian Miculka , Norbert Windhab , Tilmann Brandstetter , Gerhard Burdinski
发明人： Christian Miculka , Norbert Windhab , Tilmann Brandstetter , Gerhard Burdinski
IPC分类号： C07H1920
CPC分类号： C07H21/00 , A61K47/549 , A61K49/0013 , C07H19/04 , C07H21/02 , C07H21/04 , G01N33/532 , Y10S977/728 , Y10S977/80 , Y10S977/836 , Y10S977/894 , Y10S977/896 , Y10S977/904 , Y10S977/914 , Y10S977/915 , Y10S977/924 , Y10S977/925
摘要： The invention relates to a pentopyranosylnucleoside of the formula (I) or of the formula (II) their preparation and use for the production of a therapeutic, diagnostic and/or electronic component.
摘要翻译：本发明涉及式（I）或式（II）的戊吡喃糖基核苷及其制备和用于制备治疗，诊断和/或电子成分的方法。

17. 发明申请

US20130108662A1 PEPTIDES USEFUL AS CELL-PENETRATING PEPTIDES 审中-公开
标题翻译：肽可用作细胞穿刺肽
公开(公告)号：US20130108662A1
公开(公告)日：2013-05-02
申请号：US13557706
申请日：2012-07-25
申请人： Roland Brock , Rainer Fischer , Mariola Fotin-Mleczek , Hansjoerg Hufnagel , Norbert Windhab
发明人： Roland Brock , Rainer Fischer , Mariola Fotin-Mleczek , Hansjoerg Hufnagel , Norbert Windhab
IPC分类号： C07K14/47
CPC分类号： C07K14/47 , A61K31/713 , A61K39/385 , A61K47/644 , A61K51/088 , A61K2039/53 , C07K14/79
摘要： A peptide having an amino acid sequence containing at least eight consecutive amino acids of the human lactoferrin protein or of the bovine lactoferrin protein. The peptide is suitable as a cell-penetrating peptide. A complex of the peptide and a cargo molecule non-covalently bound to the peptide. The cargo molecule may be a nucleic acid, an amino acid, a peptide, a protein, a carbohydrate, a lipid, or a small molecule. A method of penetrating or transfecting a cell using the complex.
摘要翻译：具有含有人乳铁蛋白蛋白质或牛乳铁蛋白蛋白质的至少8个连续氨基酸的氨基酸序列的肽。该肽适合作为细胞穿透肽。肽和与肽共价结合的货物分子的复合物。载体分子可以是核酸，氨基酸，肽，蛋白质，碳水化合物，脂质或小分子。使用复合物渗透或转染细胞的方法。

18. 发明授权

US08313778B2 Drug-delivery systems 有权
标题翻译：给药系统
公开(公告)号：US08313778B2
公开(公告)日：2012-11-20
申请号：US12090754
申请日：2006-10-25
申请人： Matthias Seiler , Norbert Windhab , Manfred Stickler , Hans-Ulrich Petereit
发明人： Matthias Seiler , Norbert Windhab , Manfred Stickler , Hans-Ulrich Petereit
IPC分类号： A61K9/14
CPC分类号： A61K9/146 , A61K9/1641 , A61K47/34 , A61K47/59 , A61K47/595 , A61K47/62
摘要： The invention relates to novel particulate drug-delivery systems based on a polymer support containing at least one linear, branched or cross-linked polymer in a fraction of over 50 percent by weight in relation to the total weight of the support. The system is characterized in that at least one signal substance for transport through a biological barrier and at least one active ingredient are stored, the support, signal substance and active ingredient having no covalent links and no active-ingredient specific and signal substance specific coordinative links between one another.
摘要翻译：本发明涉及基于聚合物载体的新型颗粒药物递送系统，其包含至少一种相对于载体总重量超过50重量％的直链，支链或交联聚合物。该系统的特征在于，存储用于传输通过生物屏障和至少一种活性成分的至少一种信号物质，所述载体，信号物质和没有共价连接并且没有活性成分特异性和信号物质特异性协调链接的信号物质和活性成分在彼此之间

19. 发明授权

US08067581B2 Biomolecules having multiple attachment moieties for binding to a substrate surface 有权
标题翻译：具有多个附着部分的生物分子用于结合底物表面
公开(公告)号：US08067581B2
公开(公告)日：2011-11-29
申请号：US12946777
申请日：2010-11-15
申请人： Markus Schweitzer , Norbert Windhab , John R. Havens , Thomas J. Onofrey , Charles Greef , Daguang Wang
发明人： Markus Schweitzer , Norbert Windhab , John R. Havens , Thomas J. Onofrey , Charles Greef , Daguang Wang
IPC分类号： C07H19/04 , C07H21/02 , C07K2/00 , C07K16/00 , C12Q1/68
CPC分类号： C07H19/04 , C07H21/00 , C12Q1/68 , G01N33/54353
摘要： Compounds relating to attachment chemistries for binding biomolecules to a substrate surface are described. These include compounds of the following structure: The biomolecule includes a single nucleic acid, oligonucleotides, polynucleotides, DNAs, RNAs, proteins, peptides, enzymes, antibodies, CNAs (cyclohexyl nucleic acids), p-MeNAs (methyl or methoxy phosphate nucleic acids), peptide nucleic acids (PNAs), and pyranosyl RNAs (p-RNAs).
摘要翻译：描述了与用于将生物分子结合到基底表面的附着化学物质有关的化合物。这些包括以下结构的化合物：生物分子包括单个核酸，寡核苷酸，多核苷酸，DNAs，RNAs，蛋白质，肽，酶，抗体，CNA（环己基核酸），p-MeNA（甲基或甲氧基磷酸核酸），肽核酸（PNA）和吡喃糖基RNA（p-RNA）。

20. 发明授权

US07700761B2 3-deoxypentopyranosyl nucleic acid, its production and its use 失效
标题翻译： 3-脱氧吡喃糖基核酸，其生产及其应用
公开(公告)号：US07700761B2
公开(公告)日：2010-04-20
申请号：US11445037
申请日：2006-05-31
申请人： Christian Miculka , Thomas Wagner , Norbert Windhab
发明人： Christian Miculka , Thomas Wagner , Norbert Windhab
IPC分类号： C07H21/00 , C07H19/04
CPC分类号： C07H21/02 , C07H19/04 , C07H21/00 , F16H15/42 , Y02P20/55
摘要： Provided are processes for preparing a 3′-deoxypentopyranosyl oligomers with linkers for linking biomolecules. The processes can the steps of: bonding a 4′-protected-3′-deoxypentopyranosyl nucleoside to a solid support by coupling the 2′-OH group with a CPG support or other similar support with an amide linkage; deprotecting the 4′-protected-3′-deoxypentopyranosyl nucleoside at the 4′ position; deprotecting the 4′-protected-3′-deoxypentopyranosyl nucleoside at the 4′ position; and conjugating a linker to the free 4′ position. The resulting product can be conjugated via the linker to a biomolecule. The method can include, prior to addition of the linker, reacting the 4′-OH group of the 4′-protected-3′-deoxypentopyranosyl nucleoside that is linked to the solid support with a 4′-protected-3′-deoxypentopyranosyl nucleoside phosphoramidite in the presence of a coupling reagent, and oxidizing the reaction product. This step can be repeated one or more times to produce an oligomer of desired length.
摘要翻译：提供制备具有用于连接生物分子的接头的3'-脱氧吡喃糖基寡聚物的方法。该方法可以通过以下步骤：通过将2'-OH基团与CPG载体或其它类似载体与酰胺键偶联，将4'-保护的-3'-脱氧吡喃糖基核苷键合到固体支持物上; 在4'位保护4'-保护的3'-脱氧吡喃糖基核苷; 在4'位保护4'-保护的3'-脱氧吡喃糖基核苷; 并将接头缀合到游离的4'位置。所得产物可通过接头与生物分子结合。该方法可以包括在加入连接体之前，将与固体支持物连接的4'-保护的3'-脱氧吡喃糖基核苷的4'-OH基团与4'-保护的-3'-脱氧吡喃糖基核苷亚磷酰胺在偶联剂存在下反应，氧化反应产物。该步骤可以重复一次或多次以制备所需长度的低聚物。

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