JP2015511638A5 - - Google Patents
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- JP2015511638A5 JP2015511638A5 JP2015503165A JP2015503165A JP2015511638A5 JP 2015511638 A5 JP2015511638 A5 JP 2015511638A5 JP 2015503165 A JP2015503165 A JP 2015503165A JP 2015503165 A JP2015503165 A JP 2015503165A JP 2015511638 A5 JP2015511638 A5 JP 2015511638A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- pharmaceutical composition
- composition according
- kinase inhibitor
- 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 25
- 238000000034 method Methods 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 229940043355 kinase inhibitor Drugs 0.000 claims 9
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 102100026299 MAP kinase-interacting serine/threonine-protein kinase 1 Human genes 0.000 claims 4
- 101710139011 MAP kinase-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 4
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 claims 4
- 101710138999 MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 239000012828 PI3K inhibitor Substances 0.000 claims 3
- 229940124302 mTOR inhibitor Drugs 0.000 claims 3
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 3
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 230000004968 inflammatory condition Effects 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 230000002503 metabolic effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1205669.3 | 2012-03-30 | ||
| GBGB1205669.3A GB201205669D0 (en) | 2012-03-30 | 2012-03-30 | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| PCT/SG2013/000126 WO2013147711A1 (en) | 2012-03-30 | 2013-04-01 | Bicyclic heterocyclic derivatives as mnk1 and mnk2 modulators and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018206109A Division JP6662984B2 (ja) | 2012-03-30 | 2018-10-31 | Mnk1およびmnk2調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015511638A JP2015511638A (ja) | 2015-04-20 |
| JP2015511638A5 true JP2015511638A5 (enExample) | 2016-06-09 |
| JP6475158B2 JP6475158B2 (ja) | 2019-02-27 |
Family
ID=46160013
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Active JP6475158B2 (ja) | 2012-03-30 | 2013-04-01 | Mnk1およびmnk2調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
| JP2018206109A Active JP6662984B2 (ja) | 2012-03-30 | 2018-10-31 | Mnk1およびmnk2調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018206109A Active JP6662984B2 (ja) | 2012-03-30 | 2018-10-31 | Mnk1およびmnk2調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US9908886B2 (enExample) |
| EP (2) | EP2831079B1 (enExample) |
| JP (2) | JP6475158B2 (enExample) |
| KR (1) | KR102153320B1 (enExample) |
| CN (1) | CN104350055B (enExample) |
| AU (2) | AU2013240612B2 (enExample) |
| BR (1) | BR112014024255B1 (enExample) |
| DK (1) | DK2831079T3 (enExample) |
| ES (2) | ES2647959T3 (enExample) |
| GB (1) | GB201205669D0 (enExample) |
| NO (1) | NO2831079T3 (enExample) |
| PL (2) | PL3321268T3 (enExample) |
| SG (2) | SG10201706594PA (enExample) |
| WO (1) | WO2013147711A1 (enExample) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2013142817A2 (en) | 2012-03-23 | 2013-09-26 | Dennis Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| TWI574962B (zh) | 2012-11-14 | 2017-03-21 | 加拓科學公司 | 作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途 |
| BR112015018318A2 (pt) | 2013-02-21 | 2017-08-22 | Sunshine Lake Pharma Co Ltd | Composto, composição farmacêutica, uso de um composto ou de uma composição farmacêutica, e, métodos para prevenir, gerenciar, tratar ou diminuir a severidade de um distúrbio proliferativo em um paciente e para inibir ou modular a atividade de uma proteína quinase em uma amostra biológica |
| US9233961B2 (en) | 2013-03-15 | 2016-01-12 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| US9296754B2 (en) | 2013-03-15 | 2016-03-29 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| WO2014151729A1 (en) | 2013-03-15 | 2014-09-25 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| US9227969B2 (en) | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| AR097543A1 (es) * | 2013-09-06 | 2016-03-23 | Lexicon Pharmaceuticals Inc | COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO |
| TW201542550A (zh) * | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并[1,5-a]嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
| GB2518873A (en) | 2013-10-03 | 2015-04-08 | Agency Science Tech & Res | Bicyclic alkyne derivatives and uses thereof |
| US9920052B2 (en) * | 2013-12-09 | 2018-03-20 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of TNF activity |
| RS58053B1 (sr) | 2013-12-19 | 2019-02-28 | Novartis Ag | [1,2,4] triazolo [1,5-a] pirimidin derivati kao proteazomski inhibitori protozoa za tretman parazitskih bolesti kao što je lišmanijaza |
| CN106029075A (zh) * | 2014-01-09 | 2016-10-12 | 细胞内治疗公司 | 有机化合物 |
| HRP20191283T1 (hr) | 2014-01-24 | 2019-10-18 | Turning Point Therapeutics, Inc. | Diaril makrocikli kao modulatori protein kinaze |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| PE20161573A1 (es) | 2014-02-13 | 2017-01-19 | Incyte Corp | Ciclopropilamina como inhibidor de la lsd1 |
| US9493450B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| TWI713455B (zh) | 2014-06-25 | 2020-12-21 | 美商伊凡克特治療公司 | MnK抑制劑及其相關方法 |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| PE20180455A1 (es) | 2015-04-03 | 2018-03-05 | Incyte Corp | Compuestos heterociclicos como inhibidores de lsd1 |
| CA2982984C (en) | 2015-04-20 | 2023-10-17 | Effector Therapeutics, Inc. | Inhibitors of immune checkpoint modulators for use in treating cancer and infections |
| KR20170140382A (ko) * | 2015-04-29 | 2017-12-20 | 얀센 파마슈티카 엔.브이. | 아자벤즈이미다졸 및 ampa 수용체 조절제로서의 이의 용도 |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| BR112017027339A2 (pt) | 2015-06-18 | 2018-09-04 | Cephalon, Inc. | derivados de piperidina 1,4-substituída |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| EP4397665A3 (en) | 2015-07-06 | 2024-08-21 | Turning Point Therapeutics, Inc. | Diaryl macrocycle polymorph |
| DK3325488T3 (da) | 2015-07-21 | 2020-09-14 | Turning Point Therapeutics Inc | Chiral diaryl-makrocyklus og anvendelse deraf til behandling af cancer |
| SG10202001219UA (en) | 2015-08-12 | 2020-03-30 | Incyte Corp | Salts of an lsd1 inhibitor |
| AU2016315881B2 (en) * | 2015-09-03 | 2019-09-19 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK1A and uses thereof |
| MX2018004879A (es) * | 2015-10-22 | 2019-02-28 | Selvita S A | Nuevos derivados de piridona y su uso como inhibidores de quinasas. |
| US10851082B2 (en) | 2015-10-28 | 2020-12-01 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2) |
| KR20180070696A (ko) * | 2015-10-29 | 2018-06-26 | 이펙터 테라퓨틱스, 인크. | Mnk1 및 mnk2를 억제하는 피롤로-, 피라졸로-, 이미다조-피리미딘 및 피리딘 화합물 |
| SG11201803242TA (en) | 2015-10-29 | 2018-05-30 | Effector Therapeutics Inc | Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2 |
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| GB201700692D0 (en) * | 2017-01-16 | 2017-03-01 | Salvensis | Novel compounds and their use in the treatment of schistosomiasis |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| WO2018152117A1 (en) | 2017-02-14 | 2018-08-23 | Effector Therapeutics, Inc. | Piperidine-substituted mnk inhibitors and methods related thereto |
| BR112020001695A2 (pt) | 2017-07-28 | 2020-07-21 | Turning Point Therapeutics, Inc. | compostos macrocíclicos e usos dos mesmos |
| CN111511746B (zh) | 2017-12-19 | 2024-01-09 | 特普医药公司 | 用于治疗疾病的巨环化合物 |
| CN110156786B (zh) * | 2018-02-13 | 2022-06-03 | 青煜医药研发(上海)有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| SG11202007740TA (en) | 2018-02-13 | 2020-09-29 | Shanghai Blueray Biopharma Co Ltd | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| US12528810B2 (en) | 2018-03-01 | 2026-01-20 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK/CLK and uses thereof |
| EP3564235A1 (en) * | 2018-05-03 | 2019-11-06 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2) |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| CN113164476A (zh) | 2018-09-28 | 2021-07-23 | 代表亚利桑那大学的亚利桑那校董会 | Dyrk1/clk的小分子抑制剂及其用途 |
| US11130757B2 (en) | 2018-10-24 | 2021-09-28 | Effector Therapeutics Inc. | Crystalline forms of MNK inhibitors |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| CN111978325B (zh) * | 2019-05-22 | 2023-11-17 | 中国药科大学 | 咪唑并哒嗪类mnk1/mnk2激酶抑制剂及其制备方法和应用 |
| CN111978317A (zh) * | 2019-05-22 | 2020-11-24 | 上海道熵生物科技有限公司 | 咪唑并吡啶类mnk1/mnk2激酶抑制剂及其制备方法和应用 |
| TWI759829B (zh) * | 2019-08-23 | 2022-04-01 | 財團法人生物技術開發中心 | 作為第iii型受體酪胺酸激酶抑制劑之雜環吡唑衍生物 |
| EP4023647B1 (en) * | 2019-08-30 | 2025-04-09 | TSD Life Sciences Co., Ltd. | Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient |
| WO2021136765A1 (en) * | 2019-12-30 | 2021-07-08 | Devicare, S.L. | Compositions for clinical complications associated to devices implanted in the urinary tract |
| WO2022006331A2 (en) * | 2020-06-30 | 2022-01-06 | 4E Therapeutics, Inc. | Pyridine-1,5-diones exhibitng mnk inhibition and their method of use |
| US20230355617A1 (en) * | 2020-09-14 | 2023-11-09 | The University Of Sussex | Small molecule inhibitors of lemur tyrosine kinase 3 |
| CN112047950B (zh) * | 2020-09-14 | 2023-07-25 | 华东师范大学 | 咪唑并吡嗪类衍生物及其合成方法和应用 |
| US20230000986A1 (en) * | 2021-07-01 | 2023-01-05 | Board Of Regents, The University Of Texas System | Mnk inhibitors and eif4e phosphorylation modulation to treat inflammatory pain in the aged |
| WO2023093700A1 (zh) * | 2021-11-29 | 2023-06-01 | 中国海洋大学 | 咪唑并噻唑衍生物及其制备方法与应用 |
| CN114113639B (zh) * | 2022-01-29 | 2022-04-19 | 北京大有天弘科技有限公司 | 一种血型抗体检测方法及其应用 |
| CN118908959B (zh) * | 2023-05-08 | 2025-11-14 | 广西大学 | 咪唑并[1,2-b]哒嗪类化合物及其制备方法和PI3K抑制剂应用 |
| ES2993583B2 (es) * | 2023-06-27 | 2025-09-22 | Univ Valencia | Derivados de imidazo[1,2-a]piridina con actividad antiinflamatoria |
| WO2025165301A1 (en) * | 2024-01-31 | 2025-08-07 | National University Of Singapore | Targeting metabolic pathways with mnk inhibitors |
| CN121646587A (zh) * | 2024-05-30 | 2026-03-10 | 深圳微芯生物科技股份有限公司 | 一种苯并咪唑类化合物、其制备方法及应用 |
| CN119614691B (zh) * | 2024-12-09 | 2026-03-13 | 武汉大学 | 干扰nlk基因靶点在制备改善巨噬细胞炎性激活的药物中的应用 |
| CN121085942A (zh) * | 2025-08-28 | 2025-12-09 | 中国海洋大学 | 3,5-位取代的咪唑并噻二唑杂环衍生物及其制备方法与应用 |
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| EP1746099A1 (en) | 2004-12-23 | 2007-01-24 | DeveloGen Aktiengesellschaft | Mnk1 or Mnk2 inhibitors |
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| EP2044051B1 (en) | 2006-06-22 | 2010-01-27 | BIOVITRUM AB (publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
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| CA2806655A1 (en) | 2010-07-28 | 2012-02-02 | Bayer Intellectual Property Gmbh | Substituted imidazo[1,2-b]pyridazines |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| JP2016510764A (ja) * | 2013-03-07 | 2016-04-11 | カリフィア バイオ, インク.Califia Bio, Inc. | 混合系キナーゼ阻害剤および治療法 |
-
2012
- 2012-03-30 GB GBGB1205669.3A patent/GB201205669D0/en not_active Ceased
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2013
- 2013-04-01 ES ES13768800.8T patent/ES2647959T3/es active Active
- 2013-04-01 WO PCT/SG2013/000126 patent/WO2013147711A1/en not_active Ceased
- 2013-04-01 ES ES17179630T patent/ES3034431T3/es active Active
- 2013-04-01 NO NO13768800A patent/NO2831079T3/no unknown
- 2013-04-01 CN CN201380027654.7A patent/CN104350055B/zh active Active
- 2013-04-01 SG SG10201706594PA patent/SG10201706594PA/en unknown
- 2013-04-01 PL PL17179630.3T patent/PL3321268T3/pl unknown
- 2013-04-01 PL PL13768800T patent/PL2831079T3/pl unknown
- 2013-04-01 US US14/363,718 patent/US9908886B2/en active Active
- 2013-04-01 BR BR112014024255-0A patent/BR112014024255B1/pt active IP Right Grant
- 2013-04-01 EP EP13768800.8A patent/EP2831079B1/en active Active
- 2013-04-01 EP EP17179630.3A patent/EP3321268B1/en active Active
- 2013-04-01 KR KR1020147027686A patent/KR102153320B1/ko active Active
- 2013-04-01 AU AU2013240612A patent/AU2013240612B2/en active Active
- 2013-04-01 SG SG11201406207PA patent/SG11201406207PA/en unknown
- 2013-04-01 DK DK13768800.8T patent/DK2831079T3/da active
- 2013-04-01 JP JP2015503165A patent/JP6475158B2/ja active Active
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2017
- 2017-08-24 AU AU2017219039A patent/AU2017219039A1/en not_active Abandoned
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2018
- 2018-01-16 US US15/872,571 patent/US20180208600A1/en not_active Abandoned
- 2018-10-31 JP JP2018206109A patent/JP6662984B2/ja active Active
-
2019
- 2019-06-05 US US16/432,469 patent/US11040978B2/en active Active
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