JP2017502940A5 - - Google Patents
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- Publication number
- JP2017502940A5 JP2017502940A5 JP2016538535A JP2016538535A JP2017502940A5 JP 2017502940 A5 JP2017502940 A5 JP 2017502940A5 JP 2016538535 A JP2016538535 A JP 2016538535A JP 2016538535 A JP2016538535 A JP 2016538535A JP 2017502940 A5 JP2017502940 A5 JP 2017502940A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- heterocyclyl
- hydrogen
- 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 61
- 150000001875 compounds Chemical class 0.000 claims 54
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims 2
- -1 carbocyclylalkyloxy Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000005312 heteroarylalkynyl group Chemical group 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000719 pyrrolidinyl 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
- 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
- 201000011510 cancer Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 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
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl 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
- 125000000168 pyrrolyl group Chemical group 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 |
|---|---|---|---|
| US201361914927P | 2013-12-11 | 2013-12-11 | |
| US61/914,927 | 2013-12-11 | ||
| PCT/US2014/069562 WO2015089192A1 (en) | 2013-12-11 | 2014-12-10 | Inhibitors of lysine specific demethylase-1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017502940A JP2017502940A (ja) | 2017-01-26 |
| JP2017502940A5 true JP2017502940A5 (enExample) | 2017-12-28 |
| JP6430512B2 JP6430512B2 (ja) | 2018-11-28 |
Family
ID=53371806
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016538535A Expired - Fee Related JP6430512B2 (ja) | 2013-12-11 | 2014-12-10 | リジン特異的デメチラーゼ−１の阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US9944636B2 (enExample) |
| EP (2) | EP4257591A3 (enExample) |
| JP (1) | JP6430512B2 (enExample) |
| CA (2) | CA3161836A1 (enExample) |
| DK (1) | DK3080100T3 (enExample) |
| ES (1) | ES2935746T3 (enExample) |
| FI (1) | FI3080100T3 (enExample) |
| HR (1) | HRP20230086T1 (enExample) |
| HU (1) | HUE061252T2 (enExample) |
| LT (1) | LT3080100T (enExample) |
| MX (2) | MX376047B (enExample) |
| PL (1) | PL3080100T3 (enExample) |
| PT (1) | PT3080100T (enExample) |
| RS (1) | RS63939B1 (enExample) |
| SI (1) | SI3080100T1 (enExample) |
| SM (1) | SMT202300014T1 (enExample) |
| WO (1) | WO2015089192A1 (enExample) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9493450B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| PE20161438A1 (es) | 2014-05-01 | 2017-01-18 | Celgene Quanticel Res Inc | Inhibidores de desmetilasa 1 especifica a lisina |
| PL3160956T3 (pl) | 2014-06-27 | 2020-11-30 | Celgene Quanticel Research, Inc. | Inhibitory demetylazy-1 specyficznej dla lizyny |
| SMT202300205T1 (it) * | 2014-07-03 | 2023-09-06 | Celgene Quanticel Research Inc | Inibitori della demetilasi lisina-specifica-1 |
| 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 |
| EP3189038B1 (en) * | 2014-09-05 | 2022-11-23 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| PE20180455A1 (es) | 2015-04-03 | 2018-03-05 | Incyte Corp | Compuestos heterociclicos como inhibidores de lsd1 |
| 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 |
| SG10202001219UA (en) | 2015-08-12 | 2020-03-30 | Incyte Corp | Salts of an lsd1 inhibitor |
| 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 |
| CN109414410B (zh) | 2016-04-22 | 2022-08-12 | 因赛特公司 | Lsd1抑制剂的制剂 |
| 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 |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| US20190256929A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| US11168082B2 (en) * | 2017-05-15 | 2021-11-09 | The Regents Of The University Of Michigan | Pyrrolo[2,3-C]pyridines and related analogs as LSD-1 inhibitors |
| RU2765152C2 (ru) | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| 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 |
| 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 |
| AR112900A1 (es) | 2017-09-13 | 2019-12-26 | Hanmi Pharm Ind Co Ltd | Compuesto derivado de pirazol y uso de este |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| 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 |
| 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 |
| CN114105950B (zh) * | 2020-08-31 | 2022-09-06 | 南京明德新药研发有限公司 | 吡唑类化合物及其应用 |
| 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 |
| 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 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5550147A (en) * | 1992-02-05 | 1996-08-27 | Fujisawa Pharmaceutical Co., Ltd. | Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same |
| HUP0402352A2 (hu) * | 2001-06-19 | 2005-02-28 | Bristol-Myers Squibb Co. | Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| US7291630B2 (en) * | 2002-03-28 | 2007-11-06 | Eisai Co., Ltd. | Azaindoles as inhibitors of c-Jun N-terminal kinases |
| 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. |
| TW200526641A (en) * | 2003-12-26 | 2005-08-16 | Daiichi Seiyaku Co | Amidopyrazole derivatives |
| US7858395B2 (en) | 2005-07-13 | 2010-12-28 | Universitaetsklinikum Freiburg | Antibodies for use in identifying and/or scoring prostate cancer and androgen receptor-dependent gene expression control |
| EA200870217A1 (ru) * | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| KR101737753B1 (ko) * | 2007-03-12 | 2017-05-18 | 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 | 페닐 아미노 피리미딘 화합물 및 이의 용도 |
| KR20110041536A (ko) * | 2008-07-29 | 2011-04-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 5-알키닐-피리미딘 |
| WO2010046780A2 (en) * | 2008-10-22 | 2010-04-29 | Institut Pasteur Korea | Anti viral compounds |
| TWI435874B (zh) * | 2008-10-31 | 2014-05-01 | Toray Industries | 環己烷衍生物及其醫藥用途 |
| EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
| EP2258858A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Transgenic LSD1 animal model for cancer |
| US9708255B2 (en) | 2009-08-18 | 2017-07-18 | Robert A. Casero | (bis)urea and (bis)thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| TW201111378A (en) * | 2009-09-11 | 2011-04-01 | Bayer Schering Pharma Ag | Substituted (heteroarylmethyl) thiohydantoins |
| EP2568812B1 (en) * | 2010-05-11 | 2016-10-26 | Merck Sharp & Dohme Corp. | Novel prolylcarboxypeptidase inhibitors |
| US9006449B2 (en) * | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| GB201106829D0 (en) * | 2011-04-21 | 2011-06-01 | Proximagen Ltd | Heterocyclic compounds |
| US9289415B2 (en) | 2011-09-01 | 2016-03-22 | The Brigham And Women's Hospital, Inc. | Treatment of cancer |
| AR088351A1 (es) * | 2011-10-31 | 2014-05-28 | Lilly Co Eli | Analogos de pirazol sustituidos |
| CN107417707A (zh) * | 2012-05-04 | 2017-12-01 | 萨穆梅德有限公司 | 1H‑吡唑并[3,4‑b]吡啶及其治疗应用 |
| JP6195828B2 (ja) | 2012-05-24 | 2017-09-13 | 出光興産株式会社 | 有機エレクトロルミネッセンス素子用材料、及びそれを用いた有機エレクトロルミネッセンス素子 |
-
2014
- 2014-12-10 CA CA3161836A patent/CA3161836A1/en active Pending
- 2014-12-10 PL PL14868829.4T patent/PL3080100T3/pl unknown
- 2014-12-10 EP EP22201620.6A patent/EP4257591A3/en not_active Withdrawn
- 2014-12-10 HU HUE14868829A patent/HUE061252T2/hu unknown
- 2014-12-10 SM SM20230014T patent/SMT202300014T1/it unknown
- 2014-12-10 JP JP2016538535A patent/JP6430512B2/ja not_active Expired - Fee Related
- 2014-12-10 MX MX2016007585A patent/MX376047B/es active IP Right Grant
- 2014-12-10 ES ES14868829T patent/ES2935746T3/es active Active
- 2014-12-10 RS RS20230070A patent/RS63939B1/sr unknown
- 2014-12-10 DK DK14868829.4T patent/DK3080100T3/da active
- 2014-12-10 PT PT148688294T patent/PT3080100T/pt unknown
- 2014-12-10 HR HRP20230086TT patent/HRP20230086T1/hr unknown
- 2014-12-10 FI FIEP14868829.4T patent/FI3080100T3/fi active
- 2014-12-10 EP EP14868829.4A patent/EP3080100B1/en active Active
- 2014-12-10 WO PCT/US2014/069562 patent/WO2015089192A1/en not_active Ceased
- 2014-12-10 CA CA2933480A patent/CA2933480C/en active Active
- 2014-12-10 US US15/103,024 patent/US9944636B2/en active Active
- 2014-12-10 LT LTEPPCT/US2014/069562T patent/LT3080100T/lt unknown
- 2014-12-10 SI SI201432008T patent/SI3080100T1/sl unknown
-
2016
- 2016-06-09 MX MX2020010496A patent/MX2020010496A/es unknown
-
2018
- 2018-02-20 US US15/900,737 patent/US10131664B2/en active Active
- 2018-10-22 US US16/166,832 patent/US10385051B2/en active Active
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