JP2018528946A5 - - Google Patents
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- JP2018528946A5 JP2018528946A5 JP2018510334A JP2018510334A JP2018528946A5 JP 2018528946 A5 JP2018528946 A5 JP 2018528946A5 JP 2018510334 A JP2018510334 A JP 2018510334A JP 2018510334 A JP2018510334 A JP 2018510334A JP 2018528946 A5 JP2018528946 A5 JP 2018528946A5
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- 125000000217 alkyl group Chemical group 0.000 claims 78
- 229910052739 hydrogen Inorganic materials 0.000 claims 53
- 239000001257 hydrogen Substances 0.000 claims 53
- 150000001875 compounds Chemical class 0.000 claims 38
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 35
- 125000005843 halogen group Chemical group 0.000 claims 27
- 229910052757 nitrogen Inorganic materials 0.000 claims 23
- 125000001424 substituent group Chemical group 0.000 claims 21
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 12
- 201000011510 cancer Diseases 0.000 claims 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000002619 bicyclic group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 206010052779 Transplant rejections Diseases 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000004770 neurodegeneration Effects 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 208000034486 Multi-organ failure Diseases 0.000 claims 2
- 208000010718 Multiple Organ Failure Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000014951 hematologic disease Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000019100 sperm motility Effects 0.000 claims 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 2
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021120042A JP7720732B2 (ja) | 2015-08-26 | 2021-07-20 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
| JP2023184701A JP2024012405A (ja) | 2015-08-26 | 2023-10-27 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562209941P | 2015-08-26 | 2015-08-26 | |
| US62/209,941 | 2015-08-26 | ||
| EP15184011.3 | 2015-09-07 | ||
| EP15184011 | 2015-09-07 | ||
| US201662306233P | 2016-03-10 | 2016-03-10 | |
| US62/306,233 | 2016-03-10 | ||
| PCT/EP2016/070097 WO2017032840A1 (en) | 2015-08-26 | 2016-08-25 | Novel 6-6 bicyclic aromatic ring substituted nucleoside analogues for use as prmt5 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021120042A Division JP7720732B2 (ja) | 2015-08-26 | 2021-07-20 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018528946A JP2018528946A (ja) | 2018-10-04 |
| JP2018528946A5 true JP2018528946A5 (enExample) | 2019-10-24 |
| JP6917978B2 JP6917978B2 (ja) | 2021-08-11 |
Family
ID=54065259
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018510334A Active JP6917978B2 (ja) | 2015-08-26 | 2016-08-25 | Prmt5阻害剤として使用するための新規な6−6二環式芳香環置換ヌクレオシド類似体 |
| JP2021120042A Active JP7720732B2 (ja) | 2015-08-26 | 2021-07-20 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
| JP2023184701A Withdrawn JP2024012405A (ja) | 2015-08-26 | 2023-10-27 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021120042A Active JP7720732B2 (ja) | 2015-08-26 | 2021-07-20 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
| JP2023184701A Withdrawn JP2024012405A (ja) | 2015-08-26 | 2023-10-27 | Prmt5阻害剤として使用するための新規な6-6二環式芳香環置換ヌクレオシド類似体 |
Country Status (35)
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MX374813B (es) * | 2016-03-10 | 2025-03-06 | Janssen Pharmaceutica Nv | Análogos de nucleósidos sustituidos para su uso como inhibidores de prmt5. |
| CA2969295A1 (en) * | 2016-06-06 | 2017-12-06 | Pfizer Inc. | Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| AU2017326487B2 (en) | 2016-09-14 | 2021-08-05 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| US10611778B2 (en) | 2016-09-14 | 2020-04-07 | Janssen Pharmaceutica Nv | Fused bicyclic inhibitors of menin-MLL interaction |
| JP7101171B2 (ja) | 2016-10-03 | 2022-07-14 | ヤンセン ファーマシューティカ エヌ.ベー. | Prmt5阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
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| GB201700526D0 (en) * | 2017-01-12 | 2017-03-01 | Univ Of Hull | Therapeutic use |
| EA201990851A1 (ru) | 2017-02-24 | 2019-09-30 | Янссен Фармацевтика Нв | Новые аналоги карбануклеозида, замещенные моноциклической и бициклической кольцевой системой, для применения в качестве ингибиторов prmt5 |
| JP7225106B2 (ja) | 2017-02-27 | 2023-02-20 | ヤンセン ファーマシューティカ エヌ.ベー. | Prmt5阻害剤による治療に応答する癌患者の同定におけるバイオマーカーの使用 |
| BR112020002736A2 (pt) | 2017-08-09 | 2020-07-28 | Prelude Therapeutics, Incorporated | inibidores seletivos da proteína arginina metiltransferase 5 (prmt5) |
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| JP2016505002A (ja) | 2012-12-21 | 2016-02-18 | エピザイム,インコーポレイティド | ジヒドロイソキノリンまたはテトラヒドロイソキノリンを含有するprmt5阻害剤およびその使用 |
| WO2014145214A2 (en) | 2013-03-15 | 2014-09-18 | Ohio State Innovation Foundation | Inhibitors of prmt5 and methods of their use |
| US10087151B2 (en) | 2014-01-09 | 2018-10-02 | The J. David Gladstone Institutes, A Testimentary Trust Established Under The Will Of J. David Gladstone | Substituted benzoxazine and related compounds |
| US20170198006A1 (en) | 2014-06-25 | 2017-07-13 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| RS59474B1 (sr) | 2014-07-01 | 2019-12-31 | Millennium Pharm Inc | Heteroarilna jedinjenja koja su korisna kao inhibitori sumo-aktivirajućeg enzima |
| TN2017000357A1 (en) | 2015-02-24 | 2019-01-16 | Pfizer | Substituted nucleoside derivatives useful as anticancer agents |
| TWI870767B (zh) * | 2015-08-26 | 2025-01-21 | 比利時商健生藥品公司 | 使用作為prmt5抑制劑之新穎經6-6雙環芳香環取代之核苷類似物 |
| AU2017230658B2 (en) | 2016-03-10 | 2021-03-04 | Janssen Pharmaceutica Nv | Substituted nucleoside analogues for use as PRMT5 inhibitors |
| JP7101171B2 (ja) * | 2016-10-03 | 2022-07-14 | ヤンセン ファーマシューティカ エヌ.ベー. | Prmt5阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
| EA201990851A1 (ru) | 2017-02-24 | 2019-09-30 | Янссен Фармацевтика Нв | Новые аналоги карбануклеозида, замещенные моноциклической и бициклической кольцевой системой, для применения в качестве ингибиторов prmt5 |
| JP7225106B2 (ja) | 2017-02-27 | 2023-02-20 | ヤンセン ファーマシューティカ エヌ.ベー. | Prmt5阻害剤による治療に応答する癌患者の同定におけるバイオマーカーの使用 |
| MA51004A (fr) | 2017-12-08 | 2020-10-14 | Janssen Pharmaceutica Nv | Nouveaux analogues spirobicycliques |
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