JP2017527561A5 - - Google Patents
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- Publication number
- JP2017527561A5 JP2017527561A5 JP2017512320A JP2017512320A JP2017527561A5 JP 2017527561 A5 JP2017527561 A5 JP 2017527561A5 JP 2017512320 A JP2017512320 A JP 2017512320A JP 2017512320 A JP2017512320 A JP 2017512320A JP 2017527561 A5 JP2017527561 A5 JP 2017527561A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- formula
- heterocyclyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 54
- 150000003839 salts Chemical class 0.000 claims 54
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- -1 4- (methylsulfonyl) phenyl Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 101000615488 Homo sapiens Methyl-CpG-binding domain protein 2 Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 2
- 239000004472 Lysine Substances 0.000 claims 2
- 102100021299 Methyl-CpG-binding domain protein 2 Human genes 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020072573A JP6983273B2 (ja) | 2014-09-05 | 2020-04-14 | リジン特異的なデメチラーゼ−１の阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462046842P | 2014-09-05 | 2014-09-05 | |
| US62/046,842 | 2014-09-05 | ||
| PCT/US2015/048429 WO2016037005A1 (en) | 2014-09-05 | 2015-09-03 | Inhibitors of lysine specific demethylase-1 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020072573A Division JP6983273B2 (ja) | 2014-09-05 | 2020-04-14 | リジン特異的なデメチラーゼ−１の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017527561A JP2017527561A (ja) | 2017-09-21 |
| JP2017527561A5 true JP2017527561A5 (enExample) | 2018-10-18 |
| JP6692350B2 JP6692350B2 (ja) | 2020-05-13 |
Family
ID=55440376
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017512320A Expired - Fee Related JP6692350B2 (ja) | 2014-09-05 | 2015-09-03 | リジン特異的なデメチラーゼ−１の阻害剤 |
| JP2020072573A Expired - Fee Related JP6983273B2 (ja) | 2014-09-05 | 2020-04-14 | リジン特異的なデメチラーゼ−１の阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020072573A Expired - Fee Related JP6983273B2 (ja) | 2014-09-05 | 2020-04-14 | リジン特異的なデメチラーゼ−１の阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US9822119B2 (enExample) |
| EP (1) | EP3189038B1 (enExample) |
| JP (2) | JP6692350B2 (enExample) |
| KR (1) | KR102476459B1 (enExample) |
| CN (2) | CN107074787B (enExample) |
| AU (2) | AU2015311805B2 (enExample) |
| BR (1) | BR112017004334A2 (enExample) |
| CA (1) | CA2960188A1 (enExample) |
| CL (1) | CL2017000521A1 (enExample) |
| CO (1) | CO2017002191A2 (enExample) |
| EA (1) | EA201790376A1 (enExample) |
| EC (1) | ECSP17013466A (enExample) |
| ES (1) | ES2935114T3 (enExample) |
| IL (1) | IL250876B (enExample) |
| MX (1) | MX381597B (enExample) |
| SG (2) | SG10202008486SA (enExample) |
| WO (1) | WO2016037005A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3189038B1 (en) * | 2014-09-05 | 2022-11-23 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| US20180284095A1 (en) | 2015-06-12 | 2018-10-04 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017079476A1 (en) | 2015-11-05 | 2017-05-11 | Mirati Therapeutics, Inc. | Lsd1 inhibitors |
| JP6510068B2 (ja) | 2015-11-27 | 2019-05-08 | 大鵬薬品工業株式会社 | 新規なビフェニル化合物又はその塩 |
| US9809541B2 (en) | 2015-12-29 | 2017-11-07 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| CN120661674A (zh) | 2016-03-15 | 2025-09-19 | 奥莱松基因组股份有限公司 | 用于治疗实体瘤的lsd1抑制剂的组合 |
| US11034991B2 (en) | 2016-03-16 | 2021-06-15 | Oryzon Genomics S.A. | Methods to determine KDM1A target engagement and chemoprobes useful therefor |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| CN105924397B (zh) * | 2016-04-29 | 2017-11-24 | 河南省农业科学院植物保护研究所 | 一种1,5‑二芳基‑3‑甲酸酯吡唑类化合物、制备方法及用途 |
| EA202092442A3 (ru) * | 2016-06-07 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| KR102598895B1 (ko) | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| TWI770925B (zh) * | 2017-05-26 | 2022-07-11 | 日商大鵬藥品工業股份有限公司 | 使用有新穎聯苯化合物之抗腫瘤效果增強劑 |
| RU2765152C2 (ru) * | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| JP6915056B2 (ja) | 2017-05-31 | 2021-08-04 | 大鵬薬品工業株式会社 | Ｉｎｓｍ１の発現に基づくｌｓｄ１阻害剤の治療効果の予測方法 |
| CA3071804A1 (en) | 2017-08-03 | 2019-02-07 | Oryzon Genomics, S.A. | Use of a kdm1a inhibitor in the treatment of behavior alterations |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| HRP20260110T1 (hr) | 2019-03-20 | 2026-03-13 | Oryzon Genomics, S.A. | Vafidemstat za liječenje neagresivnih simptoma graničnog poremećaja osobnosti |
| CN113631164A (zh) | 2019-03-20 | 2021-11-09 | 奥莱松基因组股份有限公司 | 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法 |
| JP2022537384A (ja) * | 2019-06-20 | 2022-08-25 | セルジーン コーポレーション | ベネトクラクス、ギルテリチニブ、ミドスタウリン、または白血病もしくは骨髄異形成症候群を治療するための他の化合物との組み合わせにおけるアザシチジン |
| JP2022546908A (ja) | 2019-07-05 | 2022-11-10 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法 |
| EP4058018A4 (en) | 2019-11-13 | 2023-06-21 | Taiho Pharmaceutical Co., Ltd. | METHODS OF TREATING LSD1-ASSOCIATED DISEASES AND DISORDERS WITH LSD1 INHIBITORS |
| CN117015540A (zh) * | 2021-03-11 | 2023-11-07 | 南京明德新药研发有限公司 | 噻吩类化合物及其应用 |
| CN117062813A (zh) * | 2021-03-24 | 2023-11-14 | 四川汇宇制药股份有限公司 | 一种多环化合物及其应用 |
| MX2023011779A (es) | 2021-04-08 | 2023-11-22 | Oryzon Genomics Sa | Combinaciones de inhibidores de lsd1 para el tratamiento de canceres mieloides. |
| WO2023069884A1 (en) * | 2021-10-18 | 2023-04-27 | Imago Biosciences, Inc. | Kdm1a inhibitors for the treatment of disease |
| CN118206499A (zh) * | 2021-11-29 | 2024-06-18 | 郑州大学 | 一种2,3,5-三取代吡嗪类化合物及其制备方法和应用 |
| WO2023142641A1 (zh) * | 2022-01-25 | 2023-08-03 | 成都苑东生物制药股份有限公司 | 一种吡啶类衍生物、其制备方法及用途 |
| CN116836167B (zh) * | 2022-03-25 | 2025-09-09 | 腾讯科技（深圳）有限公司 | 咪唑并[1,2-a]吡嗪或吡唑并[1,5-a]嘧啶衍生物及其用途 |
| CN119497613A (zh) | 2022-05-09 | 2025-02-21 | 奥莱松基因组股份有限公司 | 使用lsd1抑制剂治疗nf1-突变肿瘤的方法 |
| US20250275969A1 (en) | 2022-05-09 | 2025-09-04 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| CN120529900A (zh) | 2022-11-24 | 2025-08-22 | 奥莱松基因组股份有限公司 | 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合 |
| WO2024208187A1 (zh) * | 2023-04-03 | 2024-10-10 | 上海复星医药（集团）股份有限公司 | 氮杂芳基化合物及其作为lsd1抑制剂的用途 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6432975B1 (en) * | 1998-12-11 | 2002-08-13 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
| HUP0402352A2 (hu) * | 2001-06-19 | 2005-02-28 | Bristol-Myers Squibb Co. | Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| ES2412273T3 (es) | 2002-11-21 | 2013-07-10 | Novartis Ag | Inhibidores de 2-morfolín-4-pirimidinas como inhibidores de fosfotidilinositol (PI) 3-quinasa y su uso en el tratamiento del cáncer. |
| CA2506568A1 (en) * | 2002-11-22 | 2004-06-10 | Merck & Co., Inc. | 2-[(4-benzyl)-1-piperidinyl)methyl]benzimidazole-5-ol derivatives as nr2b receptor antagonists |
| WO2005058876A1 (en) * | 2003-12-16 | 2005-06-30 | Gpc Biotech Ag | Pyrazine derivatives as effective compounds against infectious diseases |
| WO2005100349A2 (en) * | 2004-04-13 | 2005-10-27 | Icagen, Inc. | Polycyclic pyridines as potassium ion channel modulators |
| EP1871762A2 (en) | 2005-04-18 | 2008-01-02 | Neurogen Corporation | Subtituted heteroaryl cb1 antagonists |
| FR2896800B1 (fr) * | 2006-01-30 | 2008-04-11 | Servier Lab | Nouveaux composes pyridinylaminoalkylene-et pyridinyloxyalkylene-cyclopropanamines polysubstitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| KR20110041536A (ko) * | 2008-07-29 | 2011-04-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 5-알키닐-피리미딘 |
| EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
| RU2012132682A (ru) * | 2009-12-31 | 2014-02-10 | Пирамал Энтерпрайзис Лимитед | Ингибиторы диацилглицерин ацилтрансферазы |
| ES2564352T3 (es) | 2010-04-20 | 2016-03-22 | Università Degli Studi Di Roma "La Sapienza" | Derivados de tranilcipromina como inhibidores de la histona-desmetilasa LSD1 y/o LSD2 |
| US9006449B2 (en) * | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| KR101351919B1 (ko) | 2012-05-23 | 2014-01-24 | 현대모비스 주식회사 | 차선 유지 보조 시스템 및 방법 |
| EP2925307B1 (en) | 2012-11-30 | 2020-10-28 | McCord, Darlene E. | Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition |
| AR098203A1 (es) | 2013-11-13 | 2016-05-18 | Dow Global Technologies Llc | Reactivo de ensayo de formaldehído |
| CA3161836A1 (en) * | 2013-12-11 | 2015-06-18 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| EP3189038B1 (en) * | 2014-09-05 | 2022-11-23 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
-
2015
- 2015-09-03 EP EP15838524.5A patent/EP3189038B1/en active Active
- 2015-09-03 SG SG10202008486SA patent/SG10202008486SA/en unknown
- 2015-09-03 AU AU2015311805A patent/AU2015311805B2/en not_active Ceased
- 2015-09-03 EA EA201790376A patent/EA201790376A1/ru unknown
- 2015-09-03 CN CN201580059765.5A patent/CN107074787B/zh not_active Expired - Fee Related
- 2015-09-03 SG SG11201701683XA patent/SG11201701683XA/en unknown
- 2015-09-03 US US14/845,120 patent/US9822119B2/en active Active
- 2015-09-03 BR BR112017004334A patent/BR112017004334A2/pt active Search and Examination
- 2015-09-03 WO PCT/US2015/048429 patent/WO2016037005A1/en not_active Ceased
- 2015-09-03 CN CN202011074135.4A patent/CN112125901A/zh active Pending
- 2015-09-03 KR KR1020177009066A patent/KR102476459B1/ko active Active
- 2015-09-03 ES ES15838524T patent/ES2935114T3/es active Active
- 2015-09-03 MX MX2017002824A patent/MX381597B/es unknown
- 2015-09-03 CA CA2960188A patent/CA2960188A1/en active Pending
- 2015-09-03 JP JP2017512320A patent/JP6692350B2/ja not_active Expired - Fee Related
-
2017
- 2017-03-01 IL IL250876A patent/IL250876B/en unknown
- 2017-03-03 EC ECIEPI201713466A patent/ECSP17013466A/es unknown
- 2017-03-03 CL CL2017000521A patent/CL2017000521A1/es unknown
- 2017-03-06 CO CONC2017/0002191A patent/CO2017002191A2/es unknown
- 2017-10-02 US US15/723,050 patent/US10543198B2/en not_active Expired - Fee Related
-
2019
- 2019-12-05 US US16/705,135 patent/US10864202B2/en active Active
-
2020
- 2020-04-14 JP JP2020072573A patent/JP6983273B2/ja not_active Expired - Fee Related
- 2020-06-26 AU AU2020204287A patent/AU2020204287A1/en not_active Abandoned
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