JP2016505596A5 - - Google Patents
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- JP2016505596A5 JP2016505596A5 JP2015549821A JP2015549821A JP2016505596A5 JP 2016505596 A5 JP2016505596 A5 JP 2016505596A5 JP 2015549821 A JP2015549821 A JP 2015549821A JP 2015549821 A JP2015549821 A JP 2015549821A JP 2016505596 A5 JP2016505596 A5 JP 2016505596A5
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- Prior art keywords
- compound
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- 150000001875 compounds Chemical class 0.000 claims 236
- 150000003839 salts Chemical class 0.000 claims 65
- 239000008194 pharmaceutical composition Substances 0.000 claims 19
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000005842 heteroatom Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 9
- 125000001931 aliphatic group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 239000001301 oxygen Chemical group 0.000 claims 9
- 229910052717 sulfur Chemical group 0.000 claims 9
- 239000011593 sulfur Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 3
- 201000002528 pancreatic cancer Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102100034607 Protein arginine N-methyltransferase 5 Human genes 0.000 claims 2
- 101710084427 Protein arginine N-methyltransferase 5 Proteins 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 2
- 125000003367 polycyclic group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 1
- NOIXNOMHHWGUTG-UHFFFAOYSA-N 2-[[4-[4-pyridin-4-yl-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline Chemical compound C=1C=C(OCC=2N=C3C=CC=CC3=CC=2)C=CC=1C1=NN(CC(F)(F)F)C=C1C1=CC=NC=C1 NOIXNOMHHWGUTG-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 208000018565 Hemochromatosis Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 208000005980 beta thalassemia Diseases 0.000 claims 1
- 201000009036 biliary tract cancer Diseases 0.000 claims 1
- 208000020790 biliary tract neoplasm Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 1
- 230000014509 gene expression Effects 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000007426 ovarian cystadenocarcinoma Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 150000004885 piperazines Chemical class 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 150000003235 pyrrolidines Chemical class 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261745485P | 2012-12-21 | 2012-12-21 | |
| US61/745,485 | 2012-12-21 | ||
| US201361790525P | 2013-03-15 | 2013-03-15 | |
| US61/790,525 | 2013-03-15 | ||
| PCT/US2013/077235 WO2014100719A2 (en) | 2012-12-21 | 2013-12-20 | Prmt5 inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016505596A JP2016505596A (ja) | 2016-02-25 |
| JP2016505596A5 true JP2016505596A5 (enExample) | 2017-02-02 |
| JP6678455B2 JP6678455B2 (ja) | 2020-04-08 |
Family
ID=49958717
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015549821A Active JP6678455B2 (ja) | 2012-12-21 | 2013-12-20 | Ｐｒｍｔ５阻害剤およびその使用 |
Country Status (31)
| Country | Link |
|---|---|
| US (10) | US8993555B2 (enExample) |
| EP (3) | EP2935222B1 (enExample) |
| JP (1) | JP6678455B2 (enExample) |
| KR (2) | KR102024417B1 (enExample) |
| CN (1) | CN105452226B (enExample) |
| AU (1) | AU2018202150B2 (enExample) |
| BR (1) | BR112015014590B1 (enExample) |
| CA (1) | CA2894228C (enExample) |
| CL (1) | CL2015001790A1 (enExample) |
| CR (1) | CR20150371A (enExample) |
| CY (1) | CY1121625T1 (enExample) |
| DK (1) | DK2935222T3 (enExample) |
| DO (1) | DOP2015000158A (enExample) |
| EA (1) | EA027908B1 (enExample) |
| ES (1) | ES2701069T3 (enExample) |
| HR (1) | HRP20182037T1 (enExample) |
| HU (1) | HUE040323T2 (enExample) |
| IL (3) | IL239296B (enExample) |
| LT (1) | LT2935222T (enExample) |
| MX (1) | MX375184B (enExample) |
| MY (1) | MY199894A (enExample) |
| PE (1) | PE20151501A1 (enExample) |
| PH (2) | PH12015501351A1 (enExample) |
| PL (1) | PL2935222T3 (enExample) |
| PT (1) | PT2935222T (enExample) |
| RS (1) | RS58040B1 (enExample) |
| SI (1) | SI2935222T1 (enExample) |
| SM (1) | SMT201800669T1 (enExample) |
| UA (1) | UA118548C2 (enExample) |
| WO (1) | WO2014100719A2 (enExample) |
| ZA (1) | ZA201505212B (enExample) |
Families Citing this family (127)
| Publication number | Priority date | Publication date | Assignee | Title |
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| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| CA2894157A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| WO2014100716A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| ES2865402T3 (es) | 2012-12-21 | 2021-10-15 | Janssen Biopharma Inc | 4'-fluoronucleósidos, 4'-fluoronucleótidos y análogos de los mismos para el tratamiento del VHC |
| JP2016505000A (ja) | 2012-12-21 | 2016-02-18 | エピザイム，インコーポレイティド | Ｐｒｍｔ５阻害剤およびその使用 |
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| HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| AU2014260433A1 (en) | 2013-03-14 | 2015-09-10 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| SG11201506972PA (en) | 2013-03-14 | 2015-10-29 | Epizyme Inc | Arginine methyltransferase inhibitors and uses thereof |
| EP2970133B1 (en) | 2013-03-14 | 2018-10-24 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9394258B2 (en) | 2013-03-14 | 2016-07-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
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| JP6559719B2 (ja) | 2014-06-25 | 2019-08-14 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | （ｓ）−６−（（１−アセチルピペリジン−４−イル）アミノ）−ｎ−（３−（３、４−ジヒドロイソキノリン−２（１ｈ）−イル）−２−ヒドロキシプロピル）ピリミジン−４−カルボキサミドの結晶塩 |
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| US10494376B2 (en) | 2014-09-03 | 2019-12-03 | Ctxt Pty. Ltd. | Tetrahydroisoquinoline derived PRMT5-inhibitors |
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| US10479997B2 (en) | 2014-12-01 | 2019-11-19 | Novartis Ag | Compositions and methods for diagnosis and treatment of prostate cancer |
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| CN105497034B (zh) * | 2015-12-08 | 2018-08-07 | 暨南大学 | 一种通过靶向prmt5抑制骨肉瘤生长的组合物及其制备方法 |
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| GB201604022D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
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