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1. 发明申请

WO9740854A3 Polypeptide conjugates for transporting substancesacross cell membranes 审中-公开
标题翻译：用于在细胞膜上运输物质的多肽缀合物
公开(公告)号：WO9740854A3
公开(公告)日：1998-03-12
申请号：PCT/US9707335
申请日：1997-04-30
申请人： ANTIVIRALS INC
发明人： SUMMERTON JAMES E , WELLER DWIGHT D
IPC分类号： A61K31/00 , A61K31/335 , A61K31/337 , A61K31/74 , A61K38/00 , A61K47/48 , A61P1/00 , A61P1/04 , A61P31/00 , A61P31/04 , A61P35/00 , A61P43/00
CPC分类号： A61K47/645
摘要： Polymeric compositions effective for delivering compounds in living organisms are described. The compositions include polypeptides which exhibit solubility in both hydrophilic and lipophilic environments by undergoing a reversible pH-dependent transition from a low-pH, lipophilic form to a high-pH, hydrophilic form.
摘要翻译：描述了有效递送生物体中化合物的聚合物组合物。组合物包括通过经历从低pH，亲脂性形式到高pH亲水形式的可逆pH依赖性转变而在亲水和亲油环境中表现出溶解性的多肽。

2. 发明申请

WO1994012517A1 SEQUENCE-SPECIFIC BINDING POLYMERS FOR DUPLEX NUCLEIC ACIDS 审中-公开
标题翻译：用于双相核酸的序列特异性结合聚合物
公开(公告)号：WO1994012517A1
公开(公告)日：1994-06-09
申请号：PCT/US1993011377
申请日：1993-11-23
申请人： ANTIVIRALS INC.
发明人： ANTIVIRALS INC. , SUMMERTON, James, E. , WELLER, Dwight, D.
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , A61K47/54 , A61K47/545 , A61K47/548 , A61K47/59 , B01J2219/0072 , C12Q1/6813 , C12Q1/6839
摘要： The present invention describes a polymer composition effective to bind, in a sequence-specific manner to a target sequence of a duplex polynucleotide, at least two different-oriented Watson/Crick base-pairs at selected positions in the target sequence. The composition includes an uncharged backbone with 5- or 6-membered cyclic backbone structures and selected bases attached to the backbone structures effective to hydrogen bond specifically with different oriented base-pairs in the target sequence. Also disclosed are subunits useful for the construction of the polymer composition. The present invention further includes methods for (i) coupling a first free or polymer-terminal subunit, and (ii) isolating, from a liquid sample, a target duplex nucleic acid fragment having a selected sequence of base-pairs.
摘要翻译：本发明描述了一种聚合物组合物，其有效地以双链多核苷酸的靶序列以序列特异性方式结合靶序列中选定位置处的至少两个不同取向的沃森/克里克碱基对。该组合物包括具有5-或6-元环状主链结构的不带电荷的主链，并且连接于有效与靶序列中不同取向碱基对氢键特异性结合的主链结构的选定碱基。还公开了可用于构建聚合物组合物的亚基。本发明还包括以下方法：（i）将第一游离或聚合物末端亚基偶联，和（ii）从液体样品中分离具有选定的碱基对序列的靶双链体核酸片段。

3. 发明申请

WO9832467A2 METHOD AND CONJUGATE FOR TREATING H. PYLORI INFECTION 审中-公开
标题翻译：用于治疗H.PYLORI感染的方法和结合
公开(公告)号：WO9832467A2
公开(公告)日：1998-07-30
申请号：PCT/US9801393
申请日：1998-01-23
申请人： ANTIVIRALS INC , UNIV NEBRASKA
发明人： IVERSON PATRICK L , BRAGG RANDALL , WELLER DWIGHT D , SUMMERTON JAMES E
IPC分类号： A61K31/7088 , A61K47/48 , A61P31/04
CPC分类号： A61K47/645 , A61K47/54 , A61K47/549
摘要： A method and conjugate for treating H. pylori infection in a subject are disclosed. The conjugate is composed of (a) a nuclease-resistant antisense oligomer effective to inhibit H. pylori infection in the subject by base-specific Watson-Crick binding to an H. pylori mRNA transcript, and (b) a transport moiety conjugated to the oligomer. The transport moiety is effective to facilitate uptake of the conjugate from the environment of the stomach into the cytoplasm of H. pylori cells by active transport or by pH-gradient transport across of the cell membrane of H. pylori. The conjugate is administered by oral route, preferably in a swellable polymer bolus designed to release the conjugate in sustained release.
摘要翻译：公开了用于治疗受试者中幽门螺杆菌感染的方法和缀合物。缀合物由（a）通过碱基特异性Watson-Crick结合幽门螺杆菌mRNA转录物有效抑制幽门螺杆菌感染的核酸酶抗性反义寡聚体，和（b）与低聚物。运输部分有利于通过主动转运或通过幽门螺旋杆菌的细胞膜上的pH梯度转运来促进缀合物从胃的环境吸收到幽门螺杆菌细胞的细胞质中。缀合物通过口服途径施用，优选在可膨胀聚合物推注中，其设计用于释放持续释放的缀合物。

4. 发明申请

WO1997040854A2 POLYPEPTIDE CONJUGATES FOR TRANSPORTING SUBSTANCES ACROSS CELL MEMBRANES 审中-公开
标题翻译：用于在细胞膜上运输物质的聚合物
公开(公告)号：WO1997040854A2
公开(公告)日：1997-11-06
申请号：PCT/US1997007335
申请日：1997-04-30
申请人： ANTIVIRALS INC.
发明人： ANTIVIRALS INC. , SUMMERTON, James, E. , WELLER, Dwight, D.
IPC分类号： A61K47/48
CPC分类号： A61K47/645
摘要： Polymeric compositions effective for delivering compounds in living organisms are described. The compositions include polypeptides which exhibit solubility in both hydrophilic and lipophilic environments by undergoing a reversible pH-dependent transition from a low-pH, lipophilic form to a high-pH, hydrophilic form.
摘要翻译：描述了有效递送生物体中化合物的聚合物组合物。组合物包括通过经历从低pH，亲脂性形式到高pH亲水形式的可逆pH依赖性转变而在亲水和亲油环境中表现出溶解性的多肽。

5. 发明申请

WO1995031459A1 MORPHOLINO-SUBUNIT COMBINATORIAL LIBRARY AND METHOD 审中-公开
标题翻译： MORPHOLINO-SUBUNIT组合图书馆和方法
公开(公告)号：WO1995031459A1
公开(公告)日：1995-11-23
申请号：PCT/US1995006041
申请日：1995-05-11
申请人： ANTIVIRALS INC.
发明人： ANTIVIRALS INC. , SUMMERTON, James, E. , WELLER, Dwight, D.
IPC分类号： C07D473/00
CPC分类号： C07D417/14 , A61K47/545 , A61K47/548 , A61K47/59 , A61K47/60 , B01J2219/0072 , C07D473/00 , C07H21/00 , C07K14/003 , C08G79/02 , C12Q1/6813 , C12Q1/682 , C12Q1/6839
摘要： A method of generating a compound capable of interacting specifically with a selected macromolecular ligand is disclosed. The method involves contacting the ligand with a combinatorial library of oligomers composed of morpholino subunits with a variety of nucleobase and non-nucleobase side chains. Oligomer molecules that bind specifically to the receptor are isolated and their sequence of base moieties is determined. Also disclosed is a combinatorial library of oligomers useful in the method and novel morpholino-subunit polymer compositions.
摘要翻译：公开了一种产生能够与选定的大分子配体特异性相互作用的化合物的方法。该方法包括使配体与由吗啉代亚基组成的寡核苷酸与多种核碱基和非核碱基侧链的组合文库接触。分离与特异性结合受体的低聚物分子，并确定其碱基部分序列。还公开了可用于该方法和新颖的吗啉代亚基聚合物组合物的低聚物的组合文库。

6. 发明申请

WO1991009073A1 UNCHARGED MORPHOLINO-BASED POLYMERS HAVING ACHIRAL INTERSUBUNIT LINKAGES 审中-公开
标题翻译：具有基因型的基于多环芳烃的聚合物具有ACHIRAL INTERSUBUNIT链接
公开(公告)号：WO1991009073A1
公开(公告)日：1991-06-27
申请号：PCT/US1990007565
申请日：1990-12-20
申请人： ANTIVIRALS, INC.
发明人： ANTIVIRALS, INC. , SUMMERTON, James, E. , WELLER, DWIGHT, D.
IPC分类号： C08G75/18
CPC分类号： C07H21/00 , A61K47/545 , A61K47/548 , A61K47/59 , B01J2219/0072 , C07K14/003 , C12Q1/6813 , C12Q1/682 , C12Q1/6839
摘要： A polymer composition is disclosed composed of morpholino subunit structures which are linked together by uncharged, achiral linkages. These linkages are one to three atoms in length, joining the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-paring moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide.
摘要翻译：公开了由不饱和的非手性连接物连接在一起的吗啉亚基结构构成的聚合物组合物。这些键长度为1-3个原子，将一个亚基的吗啉代氮连接到相邻亚基的5'环外碳上。每个亚基含有通过氢键与靶多核苷酸中的特定碱基或碱基对有效结合的嘌呤或嘧啶碱基部分。

7. 发明申请

WO1991009033A1 UNCHARGED MORPHOLINO-BASED POLYMERS HAVING PHOSPHOROUS-CONTAINING CHIRAL INTERSUBUNIT LINKAGES 审中-公开
标题翻译：含有基于多晶硅的基于聚合物的聚合物，含有含磷的CHIRAL INTERSUBUNIT链接
公开(公告)号：WO1991009033A1
公开(公告)日：1991-06-27
申请号：PCT/US1990007563
申请日：1990-12-20
申请人： ANTIVIRALS, INC.
发明人： ANTIVIRALS, INC. , SUMMERTON, James, E. , WELLER, Dwight, D.
IPC分类号： C07D413/12
CPC分类号： C08G79/02 , B01J2219/0072 , C07H21/00
摘要： A polymer composition is disclosed composed of morpholino subunit structures linked together by uncharged, phosphorous-containing chiral linkages, one to three atoms in length. These chiral linkages join the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide.
摘要翻译：公开的聚合物组合物由通过不带电荷的含磷手性键连接在一起的吗啉亚基结构构成，长度为1-3个原子。这些手性连接将一个亚基的吗啉代氮连接到相邻亚基的5'环外碳上。每个亚基含有通过氢键与靶多核苷酸中的特定碱基或碱基对有效结合的嘌呤或嘧啶碱基配对部分。

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