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 |
|---|---|---|---|---|
| JP6525422B2 (ja) * | 2014-07-03 | 2019-06-05 | セルジーン クオンティセル リサーチ，インク． | リジン特異的なデメチラーゼ−１の阻害剤 |
| FI3511319T3 (fi) * | 2014-07-03 | 2023-07-20 | Celgene Quanticel Res Inc | Lysiinispesifisen demetylaasi-1:n inhibiittoreita |
| AU2016275702A1 (en) | 2015-06-12 | 2017-12-21 | 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 |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| WO2017158136A1 (en) | 2016-03-16 | 2017-09-21 | 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 |
| FI3661510T3 (fi) | 2017-08-03 | 2024-12-18 | Oryzon Genomics Sa | Menetelmiä käyttäytymismuutosten hoitamiseksi |
| AR112900A1 (es) * | 2017-09-13 | 2019-12-26 | Hanmi Pharm Ind Co Ltd | Compuesto derivado de pirazol y uso de este |
| US20220151999A1 (en) | 2019-03-20 | 2022-05-19 | Oryzon Genomics, S.A. | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| LT3941466T (lt) | 2019-03-20 | 2026-02-25 | Oryzon Genomics, S.A. | Vafidemstatas ribinio asmenybės sutrikimo simptomų, nesusijusių su agresija, gydymui |
| 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 |
| US20250073232A1 (en) | 2021-04-08 | 2025-03-06 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
| WO2023069884A1 (en) * | 2021-10-18 | 2023-04-27 | Imago Biosciences, Inc. | Kdm1a inhibitors for the treatment of disease |
| US20250295660A1 (en) | 2022-05-09 | 2025-09-25 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
| EP4522136A1 (en) | 2022-05-09 | 2025-03-19 | 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 |
| AU2002367424A1 (en) * | 2001-12-28 | 2003-07-24 | Takeda Chemical Industries, Ltd. | Androgen receptor antagonists |
| 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 |
| US7026311B2 (en) * | 2002-01-10 | 2006-04-11 | Abbott Gmbh & Co., Kg | Dibenzodiazepine derivatives, their preparation and use |
| TW200424183A (en) * | 2002-08-09 | 2004-11-16 | Nps Pharma Inc | New compounds |
| EA013811B1 (ru) | 2002-11-21 | 2010-08-30 | Новартис Вэксинес Энд Дайэгностикс, Инк. | 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака |
| US7320644B2 (en) * | 2005-02-22 | 2008-01-22 | American Axle & Manufacturing, Inc. | Universal joint with bearing retention device and method |
| MX2010014066A (es) * | 2008-06-16 | 2011-06-01 | Univ Tennessee Res Foundation | Compuestos para el tratamiento del cancer. |
| JP2012102018A (ja) * | 2009-03-03 | 2012-05-31 | Astellas Pharma Inc | アミド化合物 |
| BR112012027062B8 (pt) * | 2010-04-20 | 2021-05-25 | Fond Ieo | composto, processo para a preparação de um composto e usos do mesmo |
| WO2014085613A1 (en) * | 2012-11-30 | 2014-06-05 | Mccord Darlene E | Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition |
| EP2969007B1 (en) | 2013-03-14 | 2019-05-08 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| JP6525422B2 (ja) * | 2014-07-03 | 2019-06-05 | セルジーン クオンティセル リサーチ，インク． | リジン特異的なデメチラーゼ−１の阻害剤 |
-
2015
- 2015-06-30 JP JP2016575769A patent/JP6525422B2/ja not_active Expired - Fee Related
- 2015-06-30 US US15/323,384 patent/US10414750B2/en active Active
- 2015-06-30 SG SG11201700007YA patent/SG11201700007YA/en unknown
- 2015-06-30 WO PCT/US2015/038661 patent/WO2016004105A1/en not_active Ceased
- 2015-06-30 EP EP15815609.1A patent/EP3164509B1/en not_active Not-in-force
- 2015-06-30 ES ES15815609T patent/ES2905280T3/es active Active
- 2015-06-30 KR KR1020177002953A patent/KR102450671B1/ko active Active
- 2015-06-30 AU AU2015284197A patent/AU2015284197B2/en not_active Ceased
- 2015-06-30 CN CN201580047272.XA patent/CN106604997B/zh not_active Expired - Fee Related
- 2015-06-30 BR BR112017000042-3A patent/BR112017000042B1/pt not_active IP Right Cessation
- 2015-06-30 CA CA2954060A patent/CA2954060A1/en not_active Abandoned
- 2015-06-30 EA EA201790082A patent/EA201790082A1/ru unknown
- 2015-06-30 MX MX2017000170A patent/MX391865B/es unknown
-
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