JP2020512315A5 - - Google Patents
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- JP2020512315A5 JP2020512315A5 JP2019550579A JP2019550579A JP2020512315A5 JP 2020512315 A5 JP2020512315 A5 JP 2020512315A5 JP 2019550579 A JP2019550579 A JP 2019550579A JP 2019550579 A JP2019550579 A JP 2019550579A JP 2020512315 A5 JP2020512315 A5 JP 2020512315A5
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- Prior art keywords
- hydrogen
- deuterium
- disease
- fibrosis
- 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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- 229910052739 hydrogen Inorganic materials 0.000 claims 57
- 239000001257 hydrogen Substances 0.000 claims 57
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 33
- 229910052805 deuterium Inorganic materials 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 26
- 150000002431 hydrogen Chemical class 0.000 claims 23
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 22
- 208000035475 disorder Diseases 0.000 claims 12
- 206010016654 Fibrosis Diseases 0.000 claims 11
- 230000004761 fibrosis Effects 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 10
- 208000011580 syndromic disease Diseases 0.000 claims 10
- 230000001363 autoimmune Effects 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 208000023275 Autoimmune disease Diseases 0.000 claims 7
- 230000001404 mediated effect Effects 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 208000019425 cirrhosis of liver Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 206010052779 Transplant rejections Diseases 0.000 claims 5
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- 206010040070 Septic Shock Diseases 0.000 claims 4
- 206010047115 Vasculitis Diseases 0.000 claims 4
- 230000000735 allogeneic effect Effects 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
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- 239000000203 mixture Substances 0.000 claims 4
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- QNRATNLHPGXHMA-XZHTYLCXSA-N (r)-(6-ethoxyquinolin-4-yl)-[(2s,4s,5r)-5-ethyl-1-azabicyclo[2.2.2]octan-2-yl]methanol;hydrochloride Chemical compound Cl.C([C@H]([C@H](C1)CC)C2)CN1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OCC)C=C21 QNRATNLHPGXHMA-XZHTYLCXSA-N 0.000 claims 1
- OTLLEIBWKHEHGU-UHFFFAOYSA-N 2-[5-[[5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy]-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,5-dihydroxy-4-phosphonooxyhexanedioic acid Chemical compound C1=NC=2C(N)=NC=NC=2N1C(C(C1O)O)OC1COC1C(CO)OC(OC(C(O)C(OP(O)(O)=O)C(O)C(O)=O)C(O)=O)C(O)C1O OTLLEIBWKHEHGU-UHFFFAOYSA-N 0.000 claims 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762472019P | 2017-03-16 | 2017-03-16 | |
| US62/472,019 | 2017-03-16 | ||
| PCT/US2018/022544 WO2018170200A1 (en) | 2017-03-16 | 2018-03-15 | Heteroaryl compounds useful as mk2 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020512315A JP2020512315A (ja) | 2020-04-23 |
| JP2020512315A5 true JP2020512315A5 (enExample) | 2021-04-30 |
| JP7200120B2 JP7200120B2 (ja) | 2023-01-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019550579A Active JP7200120B2 (ja) | 2017-03-16 | 2018-03-15 | Ｍｋ２阻害剤として有用なヘテロアリール化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US11124525B2 (enExample) |
| EP (1) | EP3596083A4 (enExample) |
| JP (1) | JP7200120B2 (enExample) |
| WO (1) | WO2018170200A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG10201902326XA (en) | 2014-09-17 | 2019-04-29 | Celgene Car Llc | Mk2 inhibitors and uses thereof |
| US11124525B2 (en) | 2017-03-16 | 2021-09-21 | Celgene Car Llc | Heteroaryl compounds useful as MK2 inhibitors |
| CA3054826A1 (en) | 2017-03-16 | 2018-09-20 | Celgene Car Llc | Mk2 inhibitors, synthesis thereof, and intermediates thereto |
| CN110678178B (zh) | 2017-03-16 | 2023-10-03 | 百时美施贵宝公司 | Mk2抑制剂的形式和组合物 |
| JP2020514361A (ja) * | 2017-03-16 | 2020-05-21 | セルジーン シーエーアール エルエルシー | ９，１０，１１，１２−テトラヒドロ−８ｈ−［１，４］ジアゼピノ［５’，６’：４，５］チエノ［３，２−ｆ］キノリン−８−オン化合物およびその使用 |
| JP2020511468A (ja) * | 2017-03-16 | 2020-04-16 | セルジーン シーエーアール エルエルシー | Ｍｋ２阻害剤の重水素化アナログおよびその使用 |
| WO2020236636A1 (en) * | 2019-05-17 | 2020-11-26 | Celgene Car Llc | Methods of treating a mk2-mediated disorder |
| EP4284805A1 (en) | 2021-02-01 | 2023-12-06 | Celgene Corporation | Mk2 inhibitors, the synthesis thereof, and intermediates thereto |
| CN117940433A (zh) * | 2021-08-27 | 2024-04-26 | 瑞石生物医药有限公司 | 喹啉并呋喃衍生物及其用途 |
| AU2023207395A1 (en) | 2022-01-14 | 2024-07-11 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Pyridine-containing polycyclic derivative, and preparation method therefor and use thereof |
| CN115925718A (zh) * | 2022-12-27 | 2023-04-07 | 瑞石生物医药有限公司 | 一种四环内酰胺衍生物及其用途 |
| WO2024229401A2 (en) * | 2023-05-04 | 2024-11-07 | Matchpoint Therapeutics Inc. | Diazepino-thieno-quinoxaline compounds and their use in therapy |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5015778A (en) | 1989-12-18 | 1991-05-14 | The Dow Chemical Company | Catalytic method to produce hydroxy substituted arylophenones |
| JP3696884B2 (ja) | 1994-03-25 | 2005-09-21 | アイソテクニカ、インコーポレーテッド | ジュウテリウム化による薬物の効能の増強 |
| US5441946A (en) | 1994-04-14 | 1995-08-15 | Rhone-Poulenc-Rorer Pharmaceuticals, Inc. | Phosphonate derivatives of lipophilic amines |
| TW200413273A (en) | 2002-11-15 | 2004-08-01 | Wako Pure Chem Ind Ltd | Heavy hydrogenation method of heterocyclic rings |
| AU2003301226A1 (en) | 2002-12-20 | 2004-07-22 | Pharmacia Corp | Acyclic pyrazole compounds for the inhibition of mitogen activated protein kinase-activated protein kinase-2 |
| WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| CN101687869A (zh) | 2007-07-16 | 2010-03-31 | 诺瓦提斯公司 | 作为mk2抑制剂的四环内酰胺衍生物 |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
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2018
- 2018-03-15 US US16/494,690 patent/US11124525B2/en active Active
- 2018-03-15 EP EP18767335.5A patent/EP3596083A4/en not_active Withdrawn
- 2018-03-15 JP JP2019550579A patent/JP7200120B2/ja active Active
- 2018-03-15 WO PCT/US2018/022544 patent/WO2018170200A1/en not_active Ceased
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2021
- 2021-09-17 US US17/477,649 patent/US11760763B2/en active Active