JP2019500902A5 - - Google Patents
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- Publication number
- JP2019500902A5 JP2019500902A5 JP2018553039A JP2018553039A JP2019500902A5 JP 2019500902 A5 JP2019500902 A5 JP 2019500902A5 JP 2018553039 A JP2018553039 A JP 2018553039A JP 2018553039 A JP2018553039 A JP 2018553039A JP 2019500902 A5 JP2019500902 A5 JP 2019500902A5
- Authority
- JP
- Japan
- Prior art keywords
- morpholino oligomer
- antisense morpholino
- formula
- cpp
- antisense
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 230000000692 anti-sense effect Effects 0.000 claims description 68
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 67
- 108010051109 Cell-Penetrating Peptides Proteins 0.000 claims description 26
- 102000020313 Cell-Penetrating Peptides Human genes 0.000 claims description 26
- 108020004418 ribosomal RNA Proteins 0.000 claims description 22
- 230000008685 targeting Effects 0.000 claims description 21
- 102000004169 proteins and genes Human genes 0.000 claims description 20
- 108090000623 proteins and genes Proteins 0.000 claims description 20
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 230000008238 biochemical pathway Effects 0.000 claims description 18
- 230000033077 cellular process Effects 0.000 claims description 18
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims description 16
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 16
- 125000003696 stearoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 16
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 claims description 16
- -1 4-methoxytrityl Chemical group 0.000 claims description 14
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 14
- 241000894006 Bacteria Species 0.000 claims description 13
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 230000001580 bacterial effect Effects 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 108020004999 messenger RNA Proteins 0.000 claims description 12
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 10
- 230000000845 anti-microbial effect Effects 0.000 claims description 9
- 125000005647 linker group Chemical group 0.000 claims description 8
- 239000002773 nucleotide Substances 0.000 claims description 8
- 125000003729 nucleotide group Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 229940113082 thymine Drugs 0.000 claims description 8
- 229940035893 uracil Drugs 0.000 claims description 8
- 239000012634 fragment Substances 0.000 claims description 7
- 102000007056 Recombinant Fusion Proteins Human genes 0.000 claims description 6
- 108010008281 Recombinant Fusion Proteins Proteins 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- MHCMWGPPLOSCJY-UHFFFAOYSA-N 4-$l^{1}-azanylmorpholine Chemical compound [N]N1CCOCC1 MHCMWGPPLOSCJY-UHFFFAOYSA-N 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 102000002278 Ribosomal Proteins Human genes 0.000 claims description 4
- 108010000605 Ribosomal Proteins Proteins 0.000 claims description 4
- 108091081024 Start codon Proteins 0.000 claims description 4
- 210000004899 c-terminal region Anatomy 0.000 claims description 4
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 4
- 229930195729 fatty acid Natural products 0.000 claims description 4
- 239000000194 fatty acid Substances 0.000 claims description 4
- 150000004665 fatty acids Chemical class 0.000 claims description 4
- 230000014621 translational initiation Effects 0.000 claims description 4
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims description 3
- 229910052698 phosphorus Inorganic materials 0.000 claims description 3
- 239000011574 phosphorus Substances 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims description 3
- 108020004465 16S ribosomal RNA Proteins 0.000 claims description 2
- 101100000756 Bacillus subtilis (strain 168) acpA gene Proteins 0.000 claims description 2
- 101150023061 acpP gene Proteins 0.000 claims description 2
- 101150051130 acpP1 gene Proteins 0.000 claims description 2
- 239000004599 antimicrobial Substances 0.000 claims description 2
- 230000003115 biocidal effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 101150040440 rpmB gene Proteins 0.000 claims description 2
- 101150081398 rpmB1 gene Proteins 0.000 claims description 2
- 238000011144 upstream manufacturing Methods 0.000 claims description 2
- 230000000844 anti-bacterial effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 10
- 241000589291 Acinetobacter Species 0.000 description 3
- 241000588722 Escherichia Species 0.000 description 3
- 241000588748 Klebsiella Species 0.000 description 3
- 241000589516 Pseudomonas Species 0.000 description 3
- 230000032823 cell division Effects 0.000 description 2
- 108050003931 30S ribosomal proteins Proteins 0.000 description 1
- 101710135912 50S ribosomal protein L28 Proteins 0.000 description 1
- 241000588626 Acinetobacter baumannii Species 0.000 description 1
- 101710146995 Acyl carrier protein Proteins 0.000 description 1
- 101100278439 Archaeoglobus fulgidus (strain ATCC 49558 / DSM 4304 / JCM 9628 / NBRC 100126 / VC-16) pol gene Proteins 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- 241000588747 Klebsiella pneumoniae Species 0.000 description 1
- MSFSPUZXLOGKHJ-UHFFFAOYSA-N Muraminsaeure Natural products OC(=O)C(C)OC1C(N)C(O)OC(CO)C1O MSFSPUZXLOGKHJ-UHFFFAOYSA-N 0.000 description 1
- 206010034133 Pathogen resistance Diseases 0.000 description 1
- 108010013639 Peptidoglycan Proteins 0.000 description 1
- 108010040201 Polymyxins Proteins 0.000 description 1
- 101710150114 Protein rep Proteins 0.000 description 1
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 1
- 101710152114 Replication protein Proteins 0.000 description 1
- 101150102982 RpS10 gene Proteins 0.000 description 1
- 108010085193 UDP-N-acetylglucosamine 1-carboxyvinyltransferase Proteins 0.000 description 1
- 229940126574 aminoglycoside antibiotic Drugs 0.000 description 1
- 239000002647 aminoglycoside antibiotic agent Substances 0.000 description 1
- 239000003782 beta lactam antibiotic agent Substances 0.000 description 1
- 230000002759 chromosomal effect Effects 0.000 description 1
- 101150076598 dnaB gene Proteins 0.000 description 1
- 239000002158 endotoxin Substances 0.000 description 1
- 101150015067 fabB gene Proteins 0.000 description 1
- 101150111615 ftsZ gene Proteins 0.000 description 1
- 101150070420 gyrA gene Proteins 0.000 description 1
- 108010087116 holo-(acyl-carrier-protein) synthase Proteins 0.000 description 1
- 229920006008 lipopolysaccharide Polymers 0.000 description 1
- 101150033242 lpxC gene Proteins 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 101150005648 polB gene Proteins 0.000 description 1
- 101150103887 rpsJ gene Proteins 0.000 description 1
- 239000002132 β-lactam antibiotic Substances 0.000 description 1
- 229940124586 β-lactam antibiotics Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562387178P | 2015-12-23 | 2015-12-23 | |
| US62/387,178 | 2015-12-23 | ||
| PCT/US2016/068376 WO2017112888A1 (en) | 2015-12-23 | 2016-12-22 | Antisense antibacterial compounds and methods |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019500902A JP2019500902A (ja) | 2019-01-17 |
| JP2019500902A5 true JP2019500902A5 (OSRAM) | 2020-02-06 |
| JP7393121B2 JP7393121B2 (ja) | 2023-12-06 |
Family
ID=59091240
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018553039A Active JP7393121B2 (ja) | 2015-12-23 | 2016-12-22 | アンチセンス抗菌化合物および方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US11142764B2 (OSRAM) |
| EP (1) | EP3394262B1 (OSRAM) |
| JP (1) | JP7393121B2 (OSRAM) |
| AU (1) | AU2016379402B2 (OSRAM) |
| CA (1) | CA3009342A1 (OSRAM) |
| WO (1) | WO2017112888A1 (OSRAM) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2948373A1 (en) | 2014-05-16 | 2015-11-19 | Oregon State University | Antisense antibacterial compounds and methods |
| AU2015264449B2 (en) | 2014-05-19 | 2022-05-05 | Board Of Regents, The University Of Texas System | Antisense antibacterial compounds and methods |
| US11293024B2 (en) | 2014-12-31 | 2022-04-05 | Board Of Regents, The University Of Texas System | Antisense antibacterial compounds and methods |
| EP3394261A4 (en) | 2015-12-23 | 2019-11-27 | Oregon State University | ANTIBACTERIAL ANTISENSE COMPOUNDS AND METHOD |
| GB2579253A (en) | 2018-11-28 | 2020-06-17 | Pedanius Therapeutics Ltd | Antibacterial antisense agents |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5034506A (en) | 1985-03-15 | 1991-07-23 | Anti-Gene Development Group | Uncharged morpholino-based polymers having achiral intersubunit linkages |
| US5166315A (en) | 1989-12-20 | 1992-11-24 | Anti-Gene Development Group | Sequence-specific binding polymers for duplex nucleic acids |
| US5185444A (en) | 1985-03-15 | 1993-02-09 | Anti-Gene Deveopment Group | Uncharged morpolino-based polymers having phosphorous containing chiral intersubunit linkages |
| US5217866A (en) | 1985-03-15 | 1993-06-08 | Anti-Gene Development Group | Polynucleotide assay reagent and method |
| JP2528107B2 (ja) | 1985-03-15 | 1996-08-28 | サマ−トン，ジエ−ムス | ポリヌクレオチド測定試薬と方法 |
| US5506337A (en) | 1985-03-15 | 1996-04-09 | Antivirals Inc. | Morpholino-subunit combinatorial library and method |
| US5521063A (en) | 1985-03-15 | 1996-05-28 | Antivirals Inc. | Polynucleotide reagent containing chiral subunits and methods of use |
| WO1993001286A2 (en) | 1991-06-28 | 1993-01-21 | Massachusetts Institute Of Technology | Localized oligonucleotide therapy |
| PT1704878E (pt) | 1995-12-18 | 2013-07-17 | Angiodevice Internat Gmbh | Composições de polímeros reticulados e métodos para a sua utilização |
| US6245747B1 (en) | 1996-03-12 | 2001-06-12 | The Board Of Regents Of The University Of Nebraska | Targeted site specific antisense oligodeoxynucleotide delivery method |
| ATE393221T1 (de) | 1999-11-29 | 2008-05-15 | Avi Biopharma Inc | Gegen bakterielle 16s und 23s rrnas gerichtete ungeladene antisense oligonukleotide und deren verwendungen |
| US6965025B2 (en) | 2001-12-10 | 2005-11-15 | Isis Pharmaceuticals, Inc. | Antisense modulation of connective tissue growth factor expression |
| EP1629105B1 (en) | 2003-04-29 | 2010-09-01 | AVI BioPharma, Inc. | Compositions for enhancing transport and antisense efficacy of nucleic acid analog into cells |
| AU2006267051B2 (en) * | 2005-07-13 | 2013-03-07 | Sarepta Therapeutics, Inc. | Antisense antibacterial method and compound |
| US8067571B2 (en) * | 2005-07-13 | 2011-11-29 | Avi Biopharma, Inc. | Antibacterial antisense oligonucleotide and method |
| US20100016215A1 (en) | 2007-06-29 | 2010-01-21 | Avi Biopharma, Inc. | Compound and method for treating myotonic dystrophy |
| WO2009005793A2 (en) | 2007-06-29 | 2009-01-08 | Avi Biopharma, Inc. | Tissue specific peptide conjugates and methods |
| CA2704261C (en) | 2007-11-15 | 2015-05-26 | Avi Biopharma, Inc. | Method of synthesis of morpholino oligomers |
| US8076476B2 (en) | 2007-11-15 | 2011-12-13 | Avi Biopharma, Inc. | Synthesis of morpholino oligomers using doubly protected guanine morpholino subunits |
| US8299206B2 (en) | 2007-11-15 | 2012-10-30 | Avi Biopharma, Inc. | Method of synthesis of morpholino oligomers |
| US20110269665A1 (en) * | 2009-06-26 | 2011-11-03 | Avi Biopharma, Inc. | Compound and method for treating myotonic dystrophy |
| WO2012031243A2 (en) * | 2010-09-03 | 2012-03-08 | Avi Biopharma, Inc. | dsRNA MOLECULES COMPRISING OLIGONUCLEOTIDE ANALOGS HAVING MODIFIED INTERSUBUNIT LINKAGES AND/OR TERMINAL GROUPS |
| JP5831455B2 (ja) | 2010-09-30 | 2015-12-09 | 日本新薬株式会社 | モルホリノ核酸誘導体 |
| JP6478632B2 (ja) | 2011-05-05 | 2019-03-06 | サレプタ セラピューティクス， インコーポレイテッド | ペプチドオリゴヌクレオチドコンジュゲート |
| CA2948373A1 (en) * | 2014-05-16 | 2015-11-19 | Oregon State University | Antisense antibacterial compounds and methods |
| AU2015264449B2 (en) * | 2014-05-19 | 2022-05-05 | Board Of Regents, The University Of Texas System | Antisense antibacterial compounds and methods |
| US11293024B2 (en) | 2014-12-31 | 2022-04-05 | Board Of Regents, The University Of Texas System | Antisense antibacterial compounds and methods |
| EP3394261A4 (en) | 2015-12-23 | 2019-11-27 | Oregon State University | ANTIBACTERIAL ANTISENSE COMPOUNDS AND METHOD |
| US20200283768A1 (en) | 2017-10-23 | 2020-09-10 | Board Of Regents, The University Of Texas System | Antisense antibacterial compounds and methods |
-
2016
- 2016-12-22 EP EP16880107.4A patent/EP3394262B1/en active Active
- 2016-12-22 CA CA3009342A patent/CA3009342A1/en active Pending
- 2016-12-22 WO PCT/US2016/068376 patent/WO2017112888A1/en not_active Ceased
- 2016-12-22 AU AU2016379402A patent/AU2016379402B2/en active Active
- 2016-12-22 JP JP2018553039A patent/JP7393121B2/ja active Active
- 2016-12-22 US US16/064,306 patent/US11142764B2/en active Active
-
2021
- 2021-10-12 US US17/498,880 patent/US12209240B2/en active Active
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