JP2016516067A5 - - Google Patents
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- JP2016516067A5 JP2016516067A5 JP2016503202A JP2016503202A JP2016516067A5 JP 2016516067 A5 JP2016516067 A5 JP 2016516067A5 JP 2016503202 A JP2016503202 A JP 2016503202A JP 2016503202 A JP2016503202 A JP 2016503202A JP 2016516067 A5 JP2016516067 A5 JP 2016516067A5
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- JP
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- Prior art keywords
- compound
- optionally substituted
- pharmaceutically acceptable
- acceptable salt
- compound according
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 116
- 150000003839 salts Chemical class 0.000 claims 30
- 201000010099 disease Diseases 0.000 claims 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 230000001404 mediated effect Effects 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004452 carbocyclyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 239000000546 pharmaceutical excipient Substances 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 101000757232 Homo sapiens Protein arginine N-methyltransferase 2 Proteins 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 102000046485 human PRMT2 Human genes 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 102100025210 Histone-arginine methyltransferase CARM1 Human genes 0.000 claims 2
- 101000757216 Homo sapiens Protein arginine N-methyltransferase 1 Proteins 0.000 claims 2
- 101000924541 Homo sapiens Protein arginine N-methyltransferase 3 Proteins 0.000 claims 2
- 101000775582 Homo sapiens Protein arginine N-methyltransferase 6 Proteins 0.000 claims 2
- 101000796142 Homo sapiens Protein arginine N-methyltransferase 8 Proteins 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 102100022985 Protein arginine N-methyltransferase 1 Human genes 0.000 claims 2
- 102100034603 Protein arginine N-methyltransferase 3 Human genes 0.000 claims 2
- 102100032140 Protein arginine N-methyltransferase 6 Human genes 0.000 claims 2
- 102100031365 Protein arginine N-methyltransferase 8 Human genes 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 108010030886 coactivator-associated arginine methyltransferase 1 Proteins 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000003367 polycyclic group Chemical group 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 230000014509 gene expression Effects 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- -1 methoxyethyl Chemical group 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 201000006938 muscular dystrophy Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- YHQXJYOLULPBBH-GLRZTSSQSA-N CC(C)(C1)CO[C@]1(CC1)CC[C@H]1c1n[nH]cc1CN(C)CCNC Chemical compound CC(C)(C1)CO[C@]1(CC1)CC[C@H]1c1n[nH]cc1CN(C)CCNC YHQXJYOLULPBBH-GLRZTSSQSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361781051P | 2013-03-14 | 2013-03-14 | |
| US61/781,051 | 2013-03-14 | ||
| US201361876034P | 2013-09-10 | 2013-09-10 | |
| US61/876,034 | 2013-09-10 | ||
| PCT/US2014/029710 WO2014153226A1 (en) | 2013-03-14 | 2014-03-14 | Arginine methyltransferase inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016516067A JP2016516067A (ja) | 2016-06-02 |
| JP2016516067A5 true JP2016516067A5 (cg-RX-API-DMAC7.html) | 2017-01-26 |
| JP6581076B2 JP6581076B2 (ja) | 2019-09-25 |
Family
ID=50483598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503202A Active JP6581076B2 (ja) | 2013-03-14 | 2014-03-14 | アルギニンメチルトランスフェラーゼ阻害剤およびその使用 |
Country Status (24)
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2894228C (en) | 2012-12-21 | 2021-08-17 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| US9908887B2 (en) | 2012-12-21 | 2018-03-06 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| WO2014100716A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| CA2894157A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| US8940726B2 (en) | 2012-12-21 | 2015-01-27 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| AU2014260433A1 (en) | 2013-03-14 | 2015-09-10 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| WO2014153235A2 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153090A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives asprmt1 inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EA030481B1 (ru) | 2013-03-14 | 2018-08-31 | Эпизим, Инк. | Ингибиторы аргининметилтрансферазы и их применения |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9045455B2 (en) | 2013-03-14 | 2015-06-02 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US20160031839A1 (en) | 2013-03-14 | 2016-02-04 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153214A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyl transferase inhibtors and uses thereof |
| EP2970133B1 (en) | 2013-03-14 | 2018-10-24 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
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| CN110950841A (zh) * | 2019-11-22 | 2020-04-03 | 济南大学 | 一类新型三唑类化合物的合成及应用 |
| KR102219251B1 (ko) | 2020-03-03 | 2021-02-22 | 김명수 | 전문가 추천 플랫폼을 제공하는 서버 및 그 운용방법 |
| CN111481532B (zh) * | 2020-06-28 | 2020-09-22 | 南京中澳转化医学研究院有限公司 | 化合物28d在制备提高γ-珠蛋白表达量的药物中的应用 |
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2014
- 2014-03-14 EA EA201591531A patent/EA030481B1/ru unknown
- 2014-03-14 PT PT147173710T patent/PT2970132T/pt unknown
- 2014-03-14 DK DK14717371.0T patent/DK2970132T3/da active
- 2014-03-14 EP EP14717371.0A patent/EP2970132B1/en active Active
- 2014-03-14 CN CN201480020631.8A patent/CN105339351B/zh active Active
- 2014-03-14 US US14/775,794 patent/US9598374B2/en active Active
- 2014-03-14 MX MX2015012850A patent/MX382991B/es unknown
- 2014-03-14 SI SI201431734T patent/SI2970132T1/sl unknown
- 2014-03-14 CN CN201811160725.1A patent/CN109265400B/zh active Active
- 2014-03-14 KR KR1020197028270A patent/KR102158756B1/ko active Active
- 2014-03-14 HU HUE14717371A patent/HUE052926T2/hu unknown
- 2014-03-14 JP JP2016503202A patent/JP6581076B2/ja active Active
- 2014-03-14 LT LTEP14717371.0T patent/LT2970132T/lt unknown
- 2014-03-14 RS RS20201553A patent/RS61231B1/sr unknown
- 2014-03-14 PL PL14717371T patent/PL2970132T3/pl unknown
- 2014-03-14 CA CA2903394A patent/CA2903394C/en active Active
- 2014-03-14 AU AU2014236146A patent/AU2014236146B2/en active Active
- 2014-03-14 BR BR112015022785A patent/BR112015022785A2/pt not_active Application Discontinuation
- 2014-03-14 ES ES14717371T patent/ES2837034T3/es active Active
- 2014-03-14 HR HRP20202008TT patent/HRP20202008T1/hr unknown
- 2014-03-14 WO PCT/US2014/029710 patent/WO2014153226A1/en not_active Ceased
- 2014-03-14 KR KR1020157029130A patent/KR102028793B1/ko active Active
- 2014-03-14 SG SG11201506972PA patent/SG11201506972PA/en unknown
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2015
- 2015-09-09 IL IL241368A patent/IL241368B/en active IP Right Grant
- 2015-10-07 ZA ZA2015/07441A patent/ZA201507441B/en unknown
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2017
- 2017-02-01 US US15/421,699 patent/US10081603B2/en active Active
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2018
- 2018-05-02 AU AU2018203056A patent/AU2018203056B2/en active Active
- 2018-09-07 US US16/124,936 patent/US10800743B2/en active Active
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2020
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- 2023-10-06 US US18/482,475 patent/US20240182426A1/en not_active Abandoned
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