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) | CN112125901A (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 |
|---|---|---|---|---|
| ES2935114T3 (es) * | 2014-09-05 | 2023-03-01 | Celgene Quanticel Res Inc | Inhibidores de la desmetilasa 1 específica de lisina |
| KR20180011331A (ko) | 2015-06-12 | 2018-01-31 | 오리존 지노믹스 에스.에이. | Lsd1 억제제와 관련된 바이오마커 및 그의 용도 |
| 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 |
| FI3381896T3 (fi) | 2015-11-27 | 2023-04-21 | Taiho Pharmaceutical Co Ltd | Bifenyyliyhdiste tai sen suola |
| KR102720551B1 (ko) | 2015-12-29 | 2024-10-21 | 미라티 테라퓨틱스, 인크. | Lsd1 억제제 |
| 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 |
| JP2019512546A (ja) | 2016-03-16 | 2019-05-16 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ標的会合を決定するための方法、およびそれに有用な化学プローブ |
| 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 |
| KR102218333B1 (ko) * | 2016-06-07 | 2021-02-22 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| IL311645B2 (en) * | 2016-07-12 | 2025-11-01 | Revolution Medicines Inc | 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors |
| US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| RU2765152C2 (ru) * | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| WO2018216795A1 (ja) * | 2017-05-26 | 2018-11-29 | 大鵬薬品工業株式会社 | 新規なビフェニル化合物を用いた抗腫瘍効果増強剤 |
| AU2018276611B2 (en) | 2017-05-31 | 2022-01-06 | Taiho Pharmaceutical Co., Ltd. | Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1 |
| AU2018309372B2 (en) | 2017-08-03 | 2024-08-15 | Oryzon Genomics, S.A. | Methods of treating behavior alterations |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| HRP20251471T1 (hr) | 2019-03-20 | 2026-01-02 | Oryzon Genomics, S.A. | Postupci liječenja poremećaja hiperaktivnosti s deficitom pažnje korištenjem inhibitora kdm1a kao što je spoj vafidemstat |
| SI3941466T1 (sl) | 2019-03-20 | 2026-04-30 | Oryzon Genomics, S.A. | Vafidemstat za zdravljenje neagresivnih simptomov mejne osebnostne motnje |
| WO2020257671A1 (en) * | 2019-06-20 | 2020-12-24 | Celgene Corporation | Azacitidine in combination with venetoclax, gilteritinib, midostaurin or other compounds for treating leukemia or myelodysplastic syndrome |
| CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
| MX2022005811A (es) | 2019-11-13 | 2022-06-08 | Taiho Pharmaceutical Co Ltd | Sal novedosa de compuesto de terfenilo. |
| EP4306520A4 (en) * | 2021-03-11 | 2025-05-07 | Medshine Discovery Inc. | THIOPHENE COMPOUND AND ITS USE |
| US20240216357A1 (en) * | 2021-03-24 | 2024-07-04 | Sichuan Huiyu Pharmaceutical Co., Ltd. | Polycyclic compound and application thereof |
| CA3231846A1 (en) | 2021-04-08 | 2022-10-13 | Tamara Maes | Combinations of lsd1 inhibitors for treating myeloid cancers |
| US20250032454A1 (en) * | 2021-10-18 | 2025-01-30 | Imago Biosciences, Inc. | Kdm1a inhibitors for the treatment of disease |
| CN113968824B (zh) * | 2021-11-29 | 2024-01-19 | 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 |
| JP2025503099A (ja) * | 2022-01-25 | 2025-01-30 | 成都苑▲東▼生物制▲薬▼股▲ふん▼有限公司 | ピリジン系誘導体、その製造方法及び使用 |
| 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 |
| US20250275969A1 (en) | 2022-05-09 | 2025-09-04 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| US20250295660A1 (en) | 2022-05-09 | 2025-09-25 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
| US20260151399A1 (en) | 2022-11-24 | 2026-06-04 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| 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 |
| CA2450934A1 (en) * | 2001-06-19 | 2002-12-27 | Marco Dodier | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
| DK2316831T3 (da) | 2002-11-21 | 2013-06-10 | Novartis Ag | 2-(Morpholin-4-yl)pyrimidiner som phosphotidylinositol (PI)-3-kinaseinhibitorer samt deres anvendelse ved behandling af cancer |
| US20060160853A1 (en) * | 2002-11-22 | 2006-07-20 | Mccauley John A | 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 |
| EP1737852A2 (en) * | 2004-04-13 | 2007-01-03 | 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. |
| WO2010012740A1 (en) * | 2008-07-29 | 2010-02-04 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
| CN102781915A (zh) * | 2009-12-31 | 2012-11-14 | 皮拉马尔有限公司 | 二酰甘油酰基转移酶抑制剂 |
| US8765820B2 (en) | 2010-04-20 | 2014-07-01 | Universita Degli Studi Di Roma “La Sapienza” | Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2 |
| EP2598480B1 (en) * | 2010-07-29 | 2019-04-24 | 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 |
| US9144555B2 (en) | 2012-11-30 | 2015-09-29 | Darlene E. McCord | 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 |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| ES2935114T3 (es) * | 2014-09-05 | 2023-03-01 | Celgene Quanticel Res Inc | Inhibidores de la desmetilasa 1 específica de lisina |
-
2015
- 2015-09-03 ES ES15838524T patent/ES2935114T3/es active Active
- 2015-09-03 EA EA201790376A patent/EA201790376A1/ru unknown
- 2015-09-03 SG SG10202008486SA patent/SG10202008486SA/en unknown
- 2015-09-03 KR KR1020177009066A patent/KR102476459B1/ko active Active
- 2015-09-03 MX MX2017002824A patent/MX381597B/es unknown
- 2015-09-03 JP JP2017512320A patent/JP6692350B2/ja not_active Expired - Fee Related
- 2015-09-03 AU AU2015311805A patent/AU2015311805B2/en not_active Ceased
- 2015-09-03 SG SG11201701683XA patent/SG11201701683XA/en unknown
- 2015-09-03 CN CN202011074135.4A patent/CN112125901A/zh active Pending
- 2015-09-03 CA CA2960188A patent/CA2960188A1/en active Pending
- 2015-09-03 CN CN201580059765.5A patent/CN107074787B/zh not_active Expired - Fee Related
- 2015-09-03 EP EP15838524.5A patent/EP3189038B1/en active Active
- 2015-09-03 WO PCT/US2015/048429 patent/WO2016037005A1/en not_active Ceased
- 2015-09-03 BR BR112017004334A patent/BR112017004334A2/pt active Search and Examination
- 2015-09-03 US US14/845,120 patent/US9822119B2/en active Active
-
2017
- 2017-03-01 IL IL250876A patent/IL250876B/en unknown
- 2017-03-03 CL CL2017000521A patent/CL2017000521A1/es unknown
- 2017-03-03 EC ECIEPI201713466A patent/ECSP17013466A/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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