JP2017514479A5 - - Google Patents
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- Publication number
- JP2017514479A5 JP2017514479A5 JP2016564990A JP2016564990A JP2017514479A5 JP 2017514479 A5 JP2017514479 A5 JP 2017514479A5 JP 2016564990 A JP2016564990 A JP 2016564990A JP 2016564990 A JP2016564990 A JP 2016564990A JP 2017514479 A5 JP2017514479 A5 JP 2017514479A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- protected
- polynucleotide
- thiophosphoramidate
- composition
- 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
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- 238000000034 method Methods 0.000 claims description 28
- 239000002777 nucleoside Substances 0.000 claims description 22
- -1 oxo phosphoramidate Chemical compound 0.000 claims description 21
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims description 18
- 239000000539 dimer Substances 0.000 claims description 17
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- 239000001257 hydrogen Substances 0.000 claims description 11
- 239000000178 monomer Substances 0.000 claims description 11
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 125000006239 protecting group Chemical group 0.000 claims description 5
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 55
- 108091033319 polynucleotide Proteins 0.000 claims 24
- 239000002157 polynucleotide Substances 0.000 claims 24
- 102000040430 polynucleotide Human genes 0.000 claims 24
- 239000000203 mixture Substances 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 17
- 230000000694 effects Effects 0.000 claims 10
- 239000004615 ingredient Substances 0.000 claims 10
- 108010017842 Telomerase Proteins 0.000 claims 8
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 8
- 230000000295 complement effect Effects 0.000 claims 8
- 239000000306 component Substances 0.000 claims 8
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims 8
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical compound O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 claims 8
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 claims 8
- 125000003277 amino group Chemical group 0.000 claims 7
- 125000003835 nucleoside group Chemical group 0.000 claims 7
- 230000001590 oxidative effect Effects 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 239000008186 active pharmaceutical agent Substances 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 229930024421 Adenine Natural products 0.000 claims 4
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 claims 4
- 229960000643 adenine Drugs 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229940104302 cytosine Drugs 0.000 claims 4
- 125000006245 phosphate protecting group Chemical group 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 229940113082 thymine Drugs 0.000 claims 4
- 229940035893 uracil Drugs 0.000 claims 4
- 238000010511 deprotection reaction Methods 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000012011 nucleophilic catalyst Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 229910052796 boron Inorganic materials 0.000 claims 2
- 150000002500 ions Chemical class 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 150000008300 phosphoramidites Chemical class 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 238000005987 sulfurization reaction Methods 0.000 claims 2
- 101000585553 Homo sapiens Glycodelin Proteins 0.000 claims 1
- 108091034117 Oligonucleotide Proteins 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 125000003729 nucleotide group Chemical group 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000005426 pharmaceutical component Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- SXADIBFZNXBEGI-UHFFFAOYSA-N phosphoramidous acid Chemical group NP(O)O SXADIBFZNXBEGI-UHFFFAOYSA-N 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 238000001308 synthesis method Methods 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
- 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 description 3
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461987396P | 2014-05-01 | 2014-05-01 | |
| US61/987,396 | 2014-05-01 | ||
| US201562151909P | 2015-04-23 | 2015-04-23 | |
| US62/151,909 | 2015-04-23 | ||
| PCT/US2015/028327 WO2015168310A1 (en) | 2014-05-01 | 2015-04-29 | Oligonucleotide compositions and methods of making the same |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018088277A Division JP2018131453A (ja) | 2014-05-01 | 2018-05-01 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2019234301A Division JP2020050670A (ja) | 2014-05-01 | 2019-12-25 | オリゴヌクレオチド組成物及びその作製方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514479A JP2017514479A (ja) | 2017-06-08 |
| JP2017514479A5 true JP2017514479A5 (enExample) | 2018-07-12 |
| JP7040892B2 JP7040892B2 (ja) | 2022-03-23 |
Family
ID=54359301
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016564990A Active JP7040892B2 (ja) | 2014-05-01 | 2015-04-29 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2018088277A Pending JP2018131453A (ja) | 2014-05-01 | 2018-05-01 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2019234301A Withdrawn JP2020050670A (ja) | 2014-05-01 | 2019-12-25 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2021144677A Active JP7736489B2 (ja) | 2014-05-01 | 2021-09-06 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2022005584A Active JP7308309B2 (ja) | 2014-05-01 | 2022-01-18 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2023060170A Withdrawn JP2023073510A (ja) | 2014-05-01 | 2023-04-03 | オリゴヌクレオチド組成物及びその作製方法 |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018088277A Pending JP2018131453A (ja) | 2014-05-01 | 2018-05-01 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2019234301A Withdrawn JP2020050670A (ja) | 2014-05-01 | 2019-12-25 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2021144677A Active JP7736489B2 (ja) | 2014-05-01 | 2021-09-06 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2022005584A Active JP7308309B2 (ja) | 2014-05-01 | 2022-01-18 | オリゴヌクレオチド組成物及びその作製方法 |
| JP2023060170A Withdrawn JP2023073510A (ja) | 2014-05-01 | 2023-04-03 | オリゴヌクレオチド組成物及びその作製方法 |
Country Status (34)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE037166T2 (hu) | 2004-07-02 | 2018-08-28 | Geron Corp | Védett 3'-amino-nukleozid monomerek szintézise |
| JOP20200257A1 (ar) | 2014-05-01 | 2017-06-16 | Geron Corp | تركيبات أوليجو نوكليوتيد وطرق لتحضيرها |
| TWI736532B (zh) | 2015-04-23 | 2021-08-21 | 美商傑龍公司 | 使用多價陽離子鹽組合物之聚核苷酸製備方法 |
| SMT202100701T1 (it) | 2017-07-10 | 2022-01-10 | Geron Corp | Processo migliorato per preparare imetelstat |
| MX2022005007A (es) | 2019-10-28 | 2022-08-08 | Geron Corp | Sólidos cristalinos de 3-palmitoil-amido-1, 2-propanodiol y 3-palmitoil-amido-2-hidroxi-1-dimetoxitrifenilmetileter-propano y métodos para elaborarlos y usarlos. |
| AU2020372865A1 (en) | 2019-10-28 | 2022-05-26 | Geron Corporation | Amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane salts and methods of making the same |
| CN115315430A (zh) * | 2020-01-08 | 2022-11-08 | 日东电工株式会社 | 使用了链段型亚磷酰胺化合物的核酸合成法 |
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2014
- 2014-05-01 JO JOP/2020/0257A patent/JOP20200257A1/ar unknown
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2015
- 2015-04-29 ES ES15785822T patent/ES2963740T3/es active Active
- 2015-04-29 AU AU2015253158A patent/AU2015253158B2/en active Active
- 2015-04-29 CN CN201580022353.4A patent/CN106459134B/zh active Active
- 2015-04-29 PE PE2016002150A patent/PE20170147A1/es unknown
- 2015-04-29 SI SI201531963T patent/SI3137479T1/sl unknown
- 2015-04-29 SG SG10201911086XA patent/SG10201911086XA/en unknown
- 2015-04-29 FI FIEP15785822.6T patent/FI3137479T3/fi active
- 2015-04-29 BR BR112016025196-2A patent/BR112016025196B1/pt active IP Right Grant
- 2015-04-29 LT LTEPPCT/US2015/028327T patent/LT3137479T/lt unknown
- 2015-04-29 HU HUE15785822A patent/HUE064289T2/hu unknown
- 2015-04-29 JO JOP/2015/0089A patent/JO3767B1/ar active
- 2015-04-29 MA MA63525A patent/MA63525B1/fr unknown
- 2015-04-29 HR HRP20231505TT patent/HRP20231505T1/hr unknown
- 2015-04-29 PL PL15785822.6T patent/PL3137479T3/pl unknown
- 2015-04-29 MY MYPI2016703971A patent/MY178617A/en unknown
- 2015-04-29 SG SG11201608226YA patent/SG11201608226YA/en unknown
- 2015-04-29 TW TW108147051A patent/TWI712413B/zh active
- 2015-04-29 MY MYPI2020002421A patent/MY196927A/en unknown
- 2015-04-29 US US14/699,902 patent/US9796747B2/en active Active
- 2015-04-29 TW TW104113709A patent/TWI709406B/zh active
- 2015-04-29 DK DK15785822.6T patent/DK3137479T5/da active
- 2015-04-29 CN CN202311295220.7A patent/CN117357548A/zh active Pending
- 2015-04-29 KR KR1020237018801A patent/KR20230088509A/ko not_active Ceased
- 2015-04-29 MX MX2016014178A patent/MX382233B/es unknown
- 2015-04-29 EA EA201691786A patent/EA034882B9/ru unknown
- 2015-04-29 SM SM20230405T patent/SMT202300405T1/it unknown
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