-
公开(公告)号：US6124271A
公开(公告)日：2000-09-26
申请号：US12198
申请日：1998-01-23
IPC分类号： A61K31/7088 , A61K47/48 , A61P31/04 , A61K31/70 , C07H21/00
CPC分类号： A61K47/48092 , A61K47/48023 , A61K47/48315
摘要： A method and comjugate 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共轭物。 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。
-
公开(公告)号：US5506337A
公开(公告)日：1996-04-09
申请号：US242159
申请日：1994-05-11
IPC分类号： A61K47/48 , C07D417/14 , C07D473/00 , C07H21/00 , C07K14/00 , C08G79/02 , C12Q1/68 , C07D413/12 , C07D413/14 , C08G59/00 , C08G65/00
CPC分类号： C07D417/14 , A61K47/48061 , A61K47/48084 , A61K47/48192 , A61K47/48215 , C07D473/00 , C07H21/00 , C07K14/003 , C08G79/02 , C12Q1/6813 , C12Q1/682 , C12Q1/6839 , B01J2219/0072
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低聚物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，并确定其碱基部分的序列。 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。
-
13.发明授权
公开(公告)号：US4123610A
公开(公告)日：1978-10-31
申请号：US775800
申请日：1977-03-09
CPC分类号： C07C243/00 , C07H21/00
摘要： The crosslinking agent contains an acylhydrazide moiety, through which it is linked to a cytosine residue on the first chain; and an .alpha.-haloketal moiety which, after attachment of the crosslinking agent to the first chain, is hydrolyzed to an .alpha.-haloketone moiety, through which linking is effected to the base-paired guanine residue on the second chain.
摘要翻译： 交联剂含有酰肼部分，其通过其与第一链上的胞嘧啶残基连接; 和α-卤代酮部分，其在将交联剂连接到第一链之后，被水解成α-卤代酮部分，通过该α-卤代酮部分与第二链上的碱基配对的鸟嘌呤残基进行连接。
-
公开(公告)号：US20230357763A1
公开(公告)日：2023-11-09
申请号：US17803316
申请日：2022-05-06
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , C12N2310/11 , C12N2310/3233 , C12N2310/3513 , C12N2310/51 , C12N2320/30
摘要： Morpholino antisense oligos (Morpholinos) are a class of synthetic non-ionic molecules, each designed to very specifically bind to a selected complementary RNA sequence (targeted RNA transcript). Custom-sequence Morpholinos are used in a broad range of biological research areas, as well as for therapeutic applications in vivo (in living animals such as humans).
For most in vivo applications the “bare” Morpholino (FIG. 1a) is linked to a cationic delivery component to give a “delivery-enabled” Morpholino (FIG. 1b) with significantly improved delivery efficiency. However, cytosolic delivery was still markedly less than expected. Then recently we discovered that by adding a special disconnect component between the Morpholino component and the cationic delivery component (FIG. 1c), the cytosolic delivery efficiency for the Morpholino was dramatically increased (about a 1,000% increase in delivery efficiency).
This patent application describes designing, making, and using such delivery-enabled Morpholinos containing a key disconnect component.-
15.发明申请Photocleavable morpholino oligos with integral photolinkers for modulating the activity of any selected gene transcript by exposure to light 审中-公开具有整体光引发剂的可透光吗啉代寡核苷酸，用于通过暴露于光调节任何所选择的基因转录物的活性公开(公告)号：US20130053556A1
公开(公告)日：2013-02-28
申请号：US13199337
申请日：2011-08-26
申请人： Yong-Fu Li , James E. Summerton , Paul A. Morcos
发明人： Yong-Fu Li , James E. Summerton , Paul A. Morcos
IPC分类号： C07F9/6561 , C07D233/61
CPC分类号： C07F9/65583 , C12N15/111 , C12N2310/11 , C12N2310/3233 , C12N2320/50
摘要： Morpholinos are widely used to block the activity of selected single-stranded genetic sequences. This invention comprises Morpholinos containing one or more integral photolinkers (Photo-Morpholinos) wherein the photolinkers are directly incorporated into the sequence of a Morpholino, where the photolinker has a size and structure which emulates the size and structure of a Morpholino subunit. This integrated photolinker design substantially simplifies and reduces cost of production relative to earlier photocleavable compositions.The invention also comprises use of these Photo-Morpholinos for modulating the expression of any selected gene transcript at any selected time and at any selected site simply by exposure to light. These Photo-Morpholinos afford a new use wherein a gene transcript is rendered inactive by contacting with a Photo-Morpholino—and then later exposure to light cleaves the Photo-Morpholino to inactive fragments—thereby reactivating that previously inactivated gene transcript.
摘要翻译： 吗啉代被广泛用于阻断选择的单链遗传序列的活性。 本发明包括含有一种或多种整合的光连接剂（Photo-Morpholinos）的Morpholinos，其中光连接剂直接并入Morpholino的序列中，其中光连接剂具有模拟吗啉亚基的大小和结构的大小和结构。 这种集成的光连接器设计相对于早期的可光致发色组合物大大简化并降低了生产成本。 本发明还包括使用这些Photo-Morpholinos在任何选定的时间和在任何选择的位点上简单地通过暴露于光来调节任何选择的基因转录物的表达。 这些Photo-Morpholinos提供了一种新的用途，其中基因转录物通过与Photo-Morpholino接触而变得无活性，然后随后暴露于光将Photo-Morpholino切割为无活性片段，由此重新激活以前灭活的基因转录物。
-
-
-
-
搜索结果
15 条记录 (耗时 0.029 秒)
