JP2014521652A5 - - Google Patents
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- JP2014521652A5 JP2014521652A5 JP2014522997A JP2014522997A JP2014521652A5 JP 2014521652 A5 JP2014521652 A5 JP 2014521652A5 JP 2014522997 A JP2014522997 A JP 2014522997A JP 2014522997 A JP2014522997 A JP 2014522997A JP 2014521652 A5 JP2014521652 A5 JP 2014521652A5
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- Prior art keywords
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- sulfur
- oxygen
- Prior art date
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 65
- 150000001875 compounds Chemical class 0.000 claims 58
- 229910052757 nitrogen Inorganic materials 0.000 claims 50
- 229910052760 oxygen Inorganic materials 0.000 claims 34
- 229910052717 sulfur Inorganic materials 0.000 claims 33
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 32
- 239000001301 oxygen Substances 0.000 claims 32
- 125000005842 heteroatom Chemical group 0.000 claims 31
- 239000011593 sulfur Substances 0.000 claims 31
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 29
- 229910052736 halogen Inorganic materials 0.000 claims 24
- 150000002367 halogens Chemical class 0.000 claims 24
- 229920006395 saturated elastomer Polymers 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 17
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 238000000034 method Methods 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 230000000269 nucleophilic effect Effects 0.000 claims 9
- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical group C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- -1 4-hydroxypiperidin-1-yl Chemical group 0.000 claims 6
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 claims 6
- 125000001931 aliphatic group Chemical group 0.000 claims 6
- 229910052805 deuterium Inorganic materials 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 6
- 229910052722 tritium Inorganic materials 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- IMNIMPAHZVJRPE-UHFFFAOYSA-N triethylenediamine Chemical compound C1CN2CCN1CC2 IMNIMPAHZVJRPE-UHFFFAOYSA-N 0.000 claims 3
- SGUVLZREKBPKCE-UHFFFAOYSA-N 1,5-diazabicyclo[4.3.0]-non-5-ene Chemical compound C1CCN=C2CCCN21 SGUVLZREKBPKCE-UHFFFAOYSA-N 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 claims 2
- BWHDROKFUHTORW-UHFFFAOYSA-N tritert-butylphosphane Chemical compound CC(C)(C)P(C(C)(C)C)C(C)(C)C BWHDROKFUHTORW-UHFFFAOYSA-N 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- XULIXFLCVXWHRF-UHFFFAOYSA-N 1,2,2,6,6-pentamethylpiperidine Chemical compound CN1C(C)(C)CCCC1(C)C XULIXFLCVXWHRF-UHFFFAOYSA-N 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- HVHZEKKZMFRULH-UHFFFAOYSA-N 2,6-ditert-butyl-4-methylpyridine Chemical compound CC1=CC(C(C)(C)C)=NC(C(C)(C)C)=C1 HVHZEKKZMFRULH-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 101100004408 Arabidopsis thaliana BIG gene Proteins 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 101100485279 Drosophila melanogaster emb gene Proteins 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 102100029095 Exportin-1 Human genes 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- GSCCALZHGUWNJW-UHFFFAOYSA-N N-Cyclohexyl-N-methylcyclohexanamine Chemical compound C1CCCCC1N(C)C1CCCCC1 GSCCALZHGUWNJW-UHFFFAOYSA-N 0.000 claims 1
- 101100485284 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) CRM1 gene Proteins 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 101150094313 XPO1 gene Proteins 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- UURSXESKOOOTOV-UHFFFAOYSA-N dec-5-ene Chemical compound CCCCC=CCCCC UURSXESKOOOTOV-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 108700002148 exportin 1 Proteins 0.000 claims 1
- 230000037406 food intake Effects 0.000 claims 1
- 235000012631 food intake Nutrition 0.000 claims 1
- 208000037824 growth disorder Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 230000003301 hydrolyzing effect Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000004262 quinoxalin-2-yl group Chemical group [H]C1=NC2=C([H])C([H])=C([H])C([H])=C2N=C1* 0.000 claims 1
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical compound C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 230000008467 tissue growth Effects 0.000 claims 1
- WLPUWLXVBWGYMZ-UHFFFAOYSA-N tricyclohexylphosphine Chemical compound C1CCCCC1P(C1CCCCC1)C1CCCCC1 WLPUWLXVBWGYMZ-UHFFFAOYSA-N 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161513428P | 2011-07-29 | 2011-07-29 | |
| US201161513432P | 2011-07-29 | 2011-07-29 | |
| US61/513,428 | 2011-07-29 | ||
| US61/513,432 | 2011-07-29 | ||
| US201261610178P | 2012-03-13 | 2012-03-13 | |
| US61/610,178 | 2012-03-13 | ||
| US201261653588P | 2012-05-31 | 2012-05-31 | |
| US61/653,588 | 2012-05-31 | ||
| US201261654651P | 2012-06-01 | 2012-06-01 | |
| US61/654,651 | 2012-06-01 | ||
| PCT/US2012/048319 WO2013019548A1 (en) | 2011-07-29 | 2012-07-26 | Hydrazide containing nuclear transport modulators and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016174614A Division JP6309057B2 (ja) | 2011-07-29 | 2016-09-07 | ヒドラジド含有核輸送調節因子およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014521652A JP2014521652A (ja) | 2014-08-28 |
| JP2014521652A5 true JP2014521652A5 (enExample) | 2015-08-20 |
| JP6005740B2 JP6005740B2 (ja) | 2016-10-12 |
Family
ID=46634546
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014522997A Active JP6005740B2 (ja) | 2011-07-29 | 2012-07-26 | ヒドラジド含有核輸送調節因子およびその使用 |
| JP2016174614A Active JP6309057B2 (ja) | 2011-07-29 | 2016-09-07 | ヒドラジド含有核輸送調節因子およびその使用 |
| JP2018044974A Active JP6675431B2 (ja) | 2011-07-29 | 2018-03-13 | ヒドラジド含有核輸送調節因子およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016174614A Active JP6309057B2 (ja) | 2011-07-29 | 2016-09-07 | ヒドラジド含有核輸送調節因子およびその使用 |
| JP2018044974A Active JP6675431B2 (ja) | 2011-07-29 | 2018-03-13 | ヒドラジド含有核輸送調節因子およびその使用 |
Country Status (35)
Families Citing this family (51)
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| CN103002742B (zh) | 2010-03-05 | 2016-07-13 | 卡尔约药物治疗公司 | 核转运调节剂及其应用 |
| US9303000B2 (en) | 2011-01-17 | 2016-04-05 | Karyopharm Therapeutics Inc. | Olefin containing nuclear transport modulators and uses thereof |
| UA117902C2 (uk) * | 2011-07-29 | 2018-10-25 | Каріофарм Терапеутікс, Інк. | Модулятори ядерного транспорту та їхнє застосування |
| CN103874690B (zh) | 2011-07-29 | 2016-07-06 | 卡尔约药物治疗公司 | 含酰肼的核运输调节剂及其用途 |
| JP5906327B2 (ja) | 2012-01-18 | 2016-04-20 | バイオニア コーポレーションBioneer Corporation | 磁性ナノ粒子−SAMiRNA複合体およびその製造方法 |
| EA036639B1 (ru) * | 2012-05-09 | 2020-12-02 | Байоджен Ма Инк. | Модуляторы ядерного транспорта и их применение |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
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| WO2014205393A1 (en) * | 2013-06-21 | 2014-12-24 | Karyopharm Therapeutics Inc. | Nuclear transport modulators and uses thereof |
| MX365939B (es) * | 2013-06-21 | 2019-06-19 | Karyopharm Therapeutics Inc | Moduladores del transporte nuclear y usos de los mismos. |
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| EA202092627A1 (ru) | 2013-11-18 | 2021-09-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
| EP3074007B1 (en) * | 2013-11-28 | 2019-07-03 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of beta-thalassemias |
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| WO2017117529A1 (en) | 2015-12-31 | 2017-07-06 | Karyopharm Therapeutics Inc. | Nuclear transport modulators and uses thereof |
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| EP3512515A1 (en) | 2016-09-16 | 2019-07-24 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of systemic mastocytosis |
| WO2018098472A1 (en) | 2016-11-28 | 2018-05-31 | Karyopharm Therapeutics Inc. | Crm1 inhibitors for treating epilepsy |
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| CN106831617A (zh) * | 2017-01-17 | 2017-06-13 | 广州市闻皓生物科技有限公司 | 一种Selinexor中间体的合成工艺 |
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| US20200222410A1 (en) * | 2017-04-13 | 2020-07-16 | Brown University | Nucleocytoplasmic regulator of autophagy-associated transcription factors |
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| CN108947982A (zh) * | 2018-08-16 | 2018-12-07 | 刘璐 | 治疗非酒精性脂肪肝病的吡嗪衍生物、组合物和应用 |
| WO2020092965A1 (en) * | 2018-11-01 | 2020-05-07 | Karyopharm Therapeutics Inc. | E2f1 as a biomarker for treatments using xpo1 inhibitors |
| CN111606890A (zh) | 2019-02-26 | 2020-09-01 | 微境生物医药科技(上海)有限公司 | 含丙烯酰基的核转运调节剂及其用途 |
| EP3941588A1 (en) * | 2019-03-20 | 2022-01-26 | Johnson Matthey Public Limited Company | Co-crystal forms of selinexor |
| GB201905721D0 (en) | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| MA55808A (fr) | 2019-05-01 | 2022-03-09 | Karyopharm Therapeutics Inc | Procédé de préparation d'inhibiteurs de xpo1 et intermédiaires destinés à être utilisés dans la préparation d'inhibiteurs de xpo1 |
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| CN115485272A (zh) | 2020-03-27 | 2022-12-16 | 朗多生物制药股份有限公司 | Plxdc2配体 |
| WO2021202745A1 (en) | 2020-03-31 | 2021-10-07 | Karyopharm Therapeutics Inc. | Treatment of covid-19 with a sine compound |
| US20230218644A1 (en) | 2020-04-16 | 2023-07-13 | Som Innovation Biotech, S.A. | Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus |
| WO2021252905A1 (en) | 2020-06-11 | 2021-12-16 | Karyopharm Therapeutics Inc. | Biomarkers for response to exportin-1 inhibitors in diffuse large b-cell lymphoma patients |
| WO2021252900A1 (en) | 2020-06-11 | 2021-12-16 | Karyopharm Therapeutics Inc. | Biomarkers for response to exportin-1 inhibitors in multiple myeloma patients |
| WO2021252874A1 (en) | 2020-06-11 | 2021-12-16 | Karyopharm Therapeutics Inc. | Xpo1 inhibitors for use in treating cancer |
| US20230391754A1 (en) | 2020-10-21 | 2023-12-07 | Karyopharm Therapeutics Inc. | Crystalline form of selinexor |
| CN112679477B (zh) * | 2020-12-17 | 2021-10-26 | 佛山奕安赛医药科技有限公司 | 塞利尼索及其中间体的制备方法 |
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