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Enhanced biodistribution of oligomers

An oligomer and oligomerization technology, applied in the field of oligomers, can solve problems that are not yet ready for mainstream applications

Inactive Publication Date: 2013-12-25
GROOVE BIOPHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Thus, these molecules are not yet ready for mainstream use in the clinic

Method used

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  • Enhanced biodistribution of oligomers
  • Enhanced biodistribution of oligomers
  • Enhanced biodistribution of oligomers

Examples

Experimental program
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Effect test

Embodiment 1

[0318] anti- MI Quantitative Whole Body Autoradiography (QWBA) Analysis of RNA

[0319] Intravenously administered a single dose of 14 After C-labeled anti-miRNA, quantitative whole body autoradiography (QWBA) analysis was performed to compare conjugated anti-miRNA (for example, MI-01453 (SEQ ID NO: 2) and MI-01454 (SEQ ID NO: 2) 3)) Tissue distribution and concentration parameters with unconjugated anti-miRNA (eg, MI-01452 (SEQ ID NO: 1)). MI-01452, MI-01453 and MI-01454 are anti-miRNAs against miR-21, see Table 2.

[0320] Table 2: Anti-miRNA

[0321]

[0322] To clarify the sequence composition of these anti-miRNAs, the lower case "m" indicates the incorporation of 2'-OMe on the sugar. "*" indicates the incorporation of a phosphorothioate linkage (PS) instead of a phosphodiester linkage. L1 is a linker and has the following composition: "-P(=O)(OH)O(CH2) 6 NH-".

[0323] method

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Abstract

This invention relates generally to oligomers useful for modulating expression and / or activity of RNAs or genes. More particularly, the invention relates to single stranded, double stranded, partially double stranded and hairpin structured chemically modified oligomers that have a broad biodistribution profile for inhibiting RNA expression in a plurality of cells, tissues, or organs, and to methods of making and using the modified oligomers.

Description

[0001] Statement Regarding Sequence Listing [0002] The Sequence Listing pertaining to this application is provided in text format in lieu of a paper copy and is hereby incorporated by reference into this specification. The name of the text file containing the sequence listing is GROO_001_01WO_ST25.txt. The text file is 4KB, created on March 2, 2012, and submitted electronically via EFS-Web. [0003] Cross References to Related Applications [0004] This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61 / 448,618, filed March 2, 2011, which is incorporated by reference in its entirety. [0005] background technical field [0006] The present invention generally relates to oligomers useful for modulating gene expression in a variety of tissues. More specifically, the present invention relates to the discovery that oligomers conjugated to one or more minor groove binders have favorable biodistribution properties compared to existing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/68C12N15/113A61K48/00A61K31/7105C12N15/63
CPCA61K31/7105A61K31/713C12N15/111C12N2310/113C12N2310/14C12N2310/3511C12N2310/531C12N2320/32A61P1/04A61P1/16A61P17/00A61P17/06A61P19/02A61P21/04A61P25/00A61P29/00A61P31/12A61P35/00A61P35/02A61P37/06A61P7/04A61P9/00A61P9/10Y02A50/30C12N15/113
Inventor 大卫·L·麦瑟里哥特
Owner GROOVE BIOPHARMA CORP
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