JP2017521407A5 - - Google Patents
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- Publication number
- JP2017521407A5 JP2017521407A5 JP2016575769A JP2016575769A JP2017521407A5 JP 2017521407 A5 JP2017521407 A5 JP 2017521407A5 JP 2016575769 A JP2016575769 A JP 2016575769A JP 2016575769 A JP2016575769 A JP 2016575769A JP 2017521407 A5 JP2017521407 A5 JP 2017521407A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- pharmaceutically acceptable
- acceptable salt
- compound
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 30
- 125000000547 substituted alkyl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 3
- 101000615488 Homo sapiens Methyl-CpG-binding domain protein 2 Proteins 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
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 150000003053 piperidines Chemical class 0.000 claims 2
- 150000003235 pyrrolidines Chemical class 0.000 claims 2
- -1 substituted Chemical class 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000009134 cell regulation Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000005438 isoindazolyl group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- PEUGKEHLRUVPAN-UHFFFAOYSA-N piperidin-3-amine Chemical class NC1CCCNC1 PEUGKEHLRUVPAN-UHFFFAOYSA-N 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- NGXSWUFDCSEIOO-UHFFFAOYSA-N pyrrolidin-3-amine Chemical class NC1CCNC1 NGXSWUFDCSEIOO-UHFFFAOYSA-N 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462020758P | 2014-07-03 | 2014-07-03 | |
| US62/020,758 | 2014-07-03 | ||
| PCT/US2015/038661 WO2016004105A1 (en) | 2014-07-03 | 2015-06-30 | Inhibitors of lysine specific demethylase-1 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019086398A Division JP6833896B2 (ja) | 2014-07-03 | 2019-04-26 | リジン特異的なデメチラーゼ−１の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017521407A JP2017521407A (ja) | 2017-08-03 |
| JP2017521407A5 true JP2017521407A5 (enExample) | 2018-05-31 |
| JP6525422B2 JP6525422B2 (ja) | 2019-06-05 |
Family
ID=55019933
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016575769A Expired - Fee Related JP6525422B2 (ja) | 2014-07-03 | 2015-06-30 | リジン特異的なデメチラーゼ−１の阻害剤 |
| JP2019086398A Active JP6833896B2 (ja) | 2014-07-03 | 2019-04-26 | 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 |
|---|---|---|---|
| JP2019086398A Active JP6833896B2 (ja) | 2014-07-03 | 2019-04-26 | リジン特異的なデメチラーゼ−１の阻害剤 |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US10414750B2 (enExample) |
| EP (1) | EP3164509B1 (enExample) |
| JP (2) | JP6525422B2 (enExample) |
| KR (1) | KR102450671B1 (enExample) |
| CN (1) | CN106604997B (enExample) |
| AU (1) | AU2015284197B2 (enExample) |
| BR (1) | BR112017000042B1 (enExample) |
| CA (1) | CA2954060A1 (enExample) |
| CL (1) | CL2016003423A1 (enExample) |
| CO (1) | CO2017000363A2 (enExample) |
| EA (1) | EA201790082A1 (enExample) |
| EC (1) | ECSP17006776A (enExample) |
| ES (1) | ES2905280T3 (enExample) |
| IL (1) | IL249876B (enExample) |
| MX (1) | MX391865B (enExample) |
| SG (1) | SG11201700007YA (enExample) |
| WO (1) | WO2016004105A1 (enExample) |
| ZA (1) | ZA201700072B (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SMT202300205T1 (it) * | 2014-07-03 | 2023-09-06 | Celgene Quanticel Research Inc | Inibitori della demetilasi lisina-specifica-1 |
| CA2954060A1 (en) * | 2014-07-03 | 2016-01-07 | 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 |
| 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 |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| CA3071804A1 (en) | 2017-08-03 | 2019-02-07 | Oryzon Genomics, S.A. | Use of a kdm1a inhibitor in the treatment of behavior alterations |
| AR112900A1 (es) | 2017-09-13 | 2019-12-26 | Hanmi Pharm Ind Co Ltd | Compuesto derivado de pirazol y uso de este |
| 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 |
| HRP20260110T1 (hr) | 2019-03-20 | 2026-03-13 | Oryzon Genomics, S.A. | Vafidemstat za liječenje neagresivnih simptoma graničnog poremećaja osobnosti |
| 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 |
| 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 |
| 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 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5776954A (en) * | 1996-10-30 | 1998-07-07 | Merck & Co., Inc. | Substituted pyridyl pyrroles, compositions containing such compounds and methods of use |
| JP4316232B2 (ja) * | 2001-12-28 | 2009-08-19 | 武田薬品工業株式会社 | アンドロゲン受容体拮抗剤 |
| US20050101657A1 (en) * | 2001-12-28 | 2005-05-12 | Takeda Chemical Industries Ltd. | Androgen receptor antagonists |
| US7026311B2 (en) * | 2002-01-10 | 2006-04-11 | Abbott Gmbh & Co., Kg | Dibenzodiazepine derivatives, their preparation and use |
| AU2003268064A1 (en) | 2002-08-09 | 2004-02-25 | Astrazeneca Ab | Oxadiazoles as modulators of metabotropic glutamate receptor-5 |
| 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. |
| US7320644B2 (en) * | 2005-02-22 | 2008-01-22 | American Axle & Manufacturing, Inc. | Universal joint with bearing retention device and method |
| UA105005C2 (uk) | 2008-06-16 | 2014-04-10 | Юніверсіті Оф Теннессі Рісерч Фаундейшн | Сполуки для лікування раку |
| JP2012102018A (ja) * | 2009-03-03 | 2012-05-31 | Astellas Pharma Inc | アミド化合物 |
| 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 |
| 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 |
| US9133166B2 (en) | 2013-03-14 | 2015-09-15 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| CA2954060A1 (en) * | 2014-07-03 | 2016-01-07 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
-
2015
- 2015-06-30 CA CA2954060A patent/CA2954060A1/en not_active Abandoned
- 2015-06-30 CN CN201580047272.XA patent/CN106604997B/zh not_active Expired - Fee Related
- 2015-06-30 MX MX2017000170A patent/MX391865B/es unknown
- 2015-06-30 WO PCT/US2015/038661 patent/WO2016004105A1/en not_active Ceased
- 2015-06-30 BR BR112017000042-3A patent/BR112017000042B1/pt not_active IP Right Cessation
- 2015-06-30 AU AU2015284197A patent/AU2015284197B2/en not_active Ceased
- 2015-06-30 JP JP2016575769A patent/JP6525422B2/ja not_active Expired - Fee Related
- 2015-06-30 SG SG11201700007YA patent/SG11201700007YA/en unknown
- 2015-06-30 US US15/323,384 patent/US10414750B2/en active Active
- 2015-06-30 KR KR1020177002953A patent/KR102450671B1/ko active Active
- 2015-06-30 EA EA201790082A patent/EA201790082A1/ru unknown
- 2015-06-30 EP EP15815609.1A patent/EP3164509B1/en not_active Not-in-force
- 2015-06-30 ES ES15815609T patent/ES2905280T3/es active Active
-
2016
- 2016-12-30 CL CL2016003423A patent/CL2016003423A1/es unknown
-
2017
- 2017-01-01 IL IL249876A patent/IL249876B/en active IP Right Grant
- 2017-01-04 ZA ZA2017/00072A patent/ZA201700072B/en unknown
- 2017-01-16 CO CONC2017/0000363A patent/CO2017000363A2/es unknown
- 2017-02-01 EC ECIEPI20176776A patent/ECSP17006776A/es unknown
-
2019
- 2019-02-27 US US16/288,085 patent/US10626103B2/en not_active Expired - Fee Related
- 2019-02-28 US US16/289,278 patent/US10626104B2/en not_active Expired - Fee Related
- 2019-04-26 JP JP2019086398A patent/JP6833896B2/ja active Active
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