JP2017514830A5 - - Google Patents
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- Publication number
- JP2017514830A5 JP2017514830A5 JP2016565219A JP2016565219A JP2017514830A5 JP 2017514830 A5 JP2017514830 A5 JP 2017514830A5 JP 2016565219 A JP2016565219 A JP 2016565219A JP 2016565219 A JP2016565219 A JP 2016565219A JP 2017514830 A5 JP2017514830 A5 JP 2017514830A5
- 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
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- 150000001875 compounds Chemical class 0.000 claims 33
- 150000003839 salts Chemical class 0.000 claims 33
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- -1 substituted Chemical class 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
- 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
- 125000005346 substituted cycloalkyl group Chemical group 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
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 150000001345 alkine derivatives Chemical class 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000004449 heterocyclylalkenyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 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
- BCIIMDOZSUCSEN-UHFFFAOYSA-N piperidin-4-amine Chemical group NC1CCNCC1 BCIIMDOZSUCSEN-UHFFFAOYSA-N 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 125000004426 substituted alkynyl 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 |
|---|---|---|---|
| US201461987354P | 2014-05-01 | 2014-05-01 | |
| US61/987,354 | 2014-05-01 | ||
| PCT/US2015/028635 WO2015168466A1 (en) | 2014-05-01 | 2015-04-30 | Inhibitors of lysine specific demethylase-1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514830A JP2017514830A (ja) | 2017-06-08 |
| JP2017514830A5 true JP2017514830A5 (OSRAM) | 2018-05-24 |
| JP6493890B2 JP6493890B2 (ja) | 2019-04-03 |
Family
ID=54354743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016565219A Active JP6493890B2 (ja) | 2014-05-01 | 2015-04-30 | リジン特異的なデメチラーゼ−１の阻害剤 |
Country Status (32)
| Country | Link |
|---|---|
| US (9) | US9255097B2 (OSRAM) |
| EP (1) | EP3137169B1 (OSRAM) |
| JP (1) | JP6493890B2 (OSRAM) |
| KR (1) | KR102400920B1 (OSRAM) |
| CN (1) | CN106659914B (OSRAM) |
| AR (1) | AR100251A1 (OSRAM) |
| AU (1) | AU2015253040B2 (OSRAM) |
| BR (1) | BR112016025248B1 (OSRAM) |
| CA (1) | CA2947283C (OSRAM) |
| CL (1) | CL2016002736A1 (OSRAM) |
| CY (1) | CY1124959T1 (OSRAM) |
| DK (1) | DK3137169T3 (OSRAM) |
| EA (1) | EA036672B8 (OSRAM) |
| ES (1) | ES2903423T3 (OSRAM) |
| HR (1) | HRP20220096T1 (OSRAM) |
| HU (1) | HUE057895T2 (OSRAM) |
| IL (1) | IL248505B (OSRAM) |
| LT (1) | LT3137169T (OSRAM) |
| MX (1) | MX373373B (OSRAM) |
| NI (1) | NI201600165A (OSRAM) |
| PE (1) | PE20161438A1 (OSRAM) |
| PH (1) | PH12016502179A1 (OSRAM) |
| PL (1) | PL3137169T3 (OSRAM) |
| PT (1) | PT3137169T (OSRAM) |
| RS (1) | RS62874B1 (OSRAM) |
| SA (2) | SA519410025B1 (OSRAM) |
| SG (1) | SG11201609033TA (OSRAM) |
| SI (1) | SI3137169T1 (OSRAM) |
| SM (1) | SMT202200066T1 (OSRAM) |
| TW (1) | TWI676620B (OSRAM) |
| WO (1) | WO2015168466A1 (OSRAM) |
| ZA (1) | ZA201607613B (OSRAM) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105899491B (zh) | 2014-01-17 | 2019-04-02 | 诺华股份有限公司 | 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物 |
| CN105899493B (zh) | 2014-01-17 | 2019-03-29 | 诺华股份有限公司 | 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| DK3137169T3 (da) | 2014-05-01 | 2022-02-14 | Celgene Quanticel Res Inc | Hæmmere af lysin-specifik demethylase-1 |
| PL3160956T3 (pl) * | 2014-06-27 | 2020-11-30 | Celgene Quanticel Research, Inc. | Inhibitory demetylazy-1 specyficznej dla lizyny |
| LT3511319T (lt) * | 2014-07-03 | 2023-08-25 | Celgene Quanticel Research, Inc. | Lizinui specifinės demetilazės-1 inhibitoriai |
| EP3307909A1 (en) | 2015-06-12 | 2018-04-18 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| CN112625028B (zh) | 2015-06-19 | 2024-10-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| EP3310771B1 (en) | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| US10059668B2 (en) | 2015-11-05 | 2018-08-28 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| CN108473442B (zh) | 2015-11-05 | 2022-03-25 | 赛尔基因昆蒂赛尔研究公司 | 包含赖氨酸特异性脱甲基酶-1的抑制剂的组合物 |
| CN108602770B (zh) * | 2015-11-27 | 2022-02-08 | 大鹏药品工业株式会社 | 新型联苯化合物或其盐 |
| MX384792B (es) | 2015-12-29 | 2025-03-14 | Mirati Therapeutics Inc | Inhibidores de desmetilasa especifica de lisina 1 (lsd1). |
| SG11201807965YA (en) | 2016-03-15 | 2018-10-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
| ES3042059T3 (en) | 2016-03-16 | 2025-11-18 | Oryzon Genomics Sa | 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 |
| WO2017216706A1 (en) | 2016-06-14 | 2017-12-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| US10328077B2 (en) | 2016-08-10 | 2019-06-25 | Celgene Corporation | Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomas |
| CN110582488A (zh) * | 2016-09-30 | 2019-12-17 | 诺华股份有限公司 | 具有增强功效的免疫效应细胞疗法 |
| WO2018083138A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| EP3535420A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| KR102571130B1 (ko) | 2017-01-10 | 2023-08-28 | 노파르티스 아게 | Alk 저해제 및 shp2 저해제를 포함하는 약제학적 조합 |
| WO2018183370A2 (en) | 2017-03-30 | 2018-10-04 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
| 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 |
| RU2765152C2 (ru) | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| US12435128B2 (en) | 2017-05-31 | 2025-10-07 | Taiho Pharmaceutical Co., Ltd. | Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1 |
| DK3661510T3 (da) | 2017-08-03 | 2025-01-02 | Oryzon Genomics Sa | Fremgangsmåder til behandling af adfærdsændringer |
| KR102724968B1 (ko) * | 2018-03-21 | 2024-10-31 | 수조우 푸허 바이오파마 컴퍼니 리미티드 | Shp2 억제제 및 이의 용도 |
| CN109668987A (zh) * | 2019-02-27 | 2019-04-23 | 浙江华贝药业有限责任公司 | 一种3-氨基哌啶二盐酸盐对映异构体测定分析方法 |
| JP7535797B2 (ja) | 2019-03-20 | 2024-08-19 | オリソン ヘノミクス，ソシエダ アノニマ | 化合物バフィデムスタット（ｖａｆｉｄｅｍｓｔａｔ）などｋｄｍ１ａ阻害剤を使用した注意欠陥多動性障害の処置方法 |
| SG11202109159VA (en) | 2019-03-20 | 2021-10-28 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| KR20220024426A (ko) | 2019-06-13 | 2022-03-03 | 셀진 코포레이션 | 콜드 종양을 표적화함으로써 암을 치료하는 방법 |
| 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 |
| US20220411381A1 (en) * | 2019-10-01 | 2022-12-29 | Bayer Aktiengesellschaft | Pyrimidinedione derivatives |
| WO2021095840A1 (en) | 2019-11-13 | 2021-05-20 | Taiho Pharmaceutical Co., Ltd. | METHODS OF TREATING LSD1-RELATED DISEASES and Disorders WITH LSD1 INHIBITORS |
| CA3170456A1 (en) * | 2020-03-06 | 2021-09-10 | Ellen Filvaroff | Combination of an lsd-1 inhibitor and nivolumab for use in treating sclc or sqnsclc |
| KR20230035569A (ko) | 2020-06-05 | 2023-03-14 | 셀젠 콴티셀 리서치, 인크. | 전립선암의 치료 방법 |
| US20240199571A1 (en) * | 2021-03-11 | 2024-06-20 | Medshine Discovery Inc. | Thiophene compound and application thereof |
| 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 |
| JP2025516647A (ja) | 2022-05-09 | 2025-05-30 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｌｓｄ１阻害薬を用いる悪性末梢神経鞘腫（ｍｐｎｓｔ）の治療法 |
| 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 |
| WO2024110649A1 (en) | 2022-11-24 | 2024-05-30 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| EP4626878A1 (en) | 2022-12-02 | 2025-10-08 | Neumora Therapeutics, Inc. | Methods of treating neurological disorders |
Family Cites Families (21)
| 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 |
| JP4533534B2 (ja) * | 1998-06-19 | 2010-09-01 | ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド | グリコーゲンシンターゼキナーゼ３のインヒビター |
| HUP0402352A2 (hu) * | 2001-06-19 | 2005-02-28 | Bristol-Myers Squibb Co. | Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| PT2316831E (pt) | 2002-11-21 | 2013-06-06 | Novartis Ag | 2-(morfolin-4-il)pirimidinas como inibidores da fosfatidilinositol (pi) quinase e a sua utilização no tratamento do cancro |
| US7183287B2 (en) * | 2003-04-03 | 2007-02-27 | Pharmacia Corporation | Substituted pyrimidinones |
| TW200526641A (en) * | 2003-12-26 | 2005-08-16 | Daiichi Seiyaku Co | Amidopyrazole derivatives |
| AU2007332143B2 (en) | 2006-12-11 | 2012-11-08 | Bionomics Limited | Chemical compounds and processes |
| ES2597903T3 (es) * | 2008-07-29 | 2017-01-24 | Boehringer Ingelheim International Gmbh | 5-Alquinil-pirimidinas |
| TWI435874B (zh) * | 2008-10-31 | 2014-05-01 | Toray Industries | 環己烷衍生物及其醫藥用途 |
| US9365539B2 (en) * | 2010-05-11 | 2016-06-14 | Merck Sharp & Dohme Corp. | Prolylcarboxypeptidase inhibitors |
| WO2012034116A2 (en) | 2010-09-10 | 2012-03-15 | The Johns Hopkins University | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| PE20141322A1 (es) | 2011-03-25 | 2014-10-05 | Glaxosmithkline Intellectual Property (N 2) Limited | Ciclopropilaminas como inhibidores de desmetilasa 1 especifica de lisina |
| WO2013175789A1 (ja) | 2012-05-24 | 2013-11-28 | 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 |
| BR112015022674A2 (pt) | 2013-03-11 | 2017-07-18 | Abbvie Inc | inibidores de bromodomínio |
| WO2015018522A1 (en) | 2013-08-06 | 2015-02-12 | Oncoethix Sa | Bet-bromodomain inhibitor shows synergism with several anti-cancer agents in pre-clinical models of diffuse large b-cell lymphoma (dlbcl) |
| PE20161065A1 (es) | 2013-10-18 | 2016-11-19 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| LT3080100T (lt) * | 2013-12-11 | 2023-02-27 | Celgene Quanticel Research, Inc. | Lizinui specifinės demetilazės-1 inhibitoriai |
| DK3137169T3 (da) * | 2014-05-01 | 2022-02-14 | Celgene Quanticel Res Inc | Hæmmere af lysin-specifik demethylase-1 |
| US20160022684A1 (en) | 2014-07-25 | 2016-01-28 | Pharmacyclics Llc | Bet inhibitor and bruton's tyrosine kinase inhibitor combinations |
| CA2966452A1 (en) | 2014-12-17 | 2016-06-23 | Samuel David Brown | Substituted bicyclic compounds as bromodomain inhibitors |
| CN108473442B (zh) * | 2015-11-05 | 2022-03-25 | 赛尔基因昆蒂赛尔研究公司 | 包含赖氨酸特异性脱甲基酶-1的抑制剂的组合物 |
-
2015
- 2015-04-30 DK DK15785884.6T patent/DK3137169T3/da active
- 2015-04-30 PT PT157858846T patent/PT3137169T/pt unknown
- 2015-04-30 MX MX2016014253A patent/MX373373B/es active IP Right Grant
- 2015-04-30 SG SG11201609033TA patent/SG11201609033TA/en unknown
- 2015-04-30 BR BR112016025248-9A patent/BR112016025248B1/pt not_active IP Right Cessation
- 2015-04-30 WO PCT/US2015/028635 patent/WO2015168466A1/en not_active Ceased
- 2015-04-30 HU HUE15785884A patent/HUE057895T2/hu unknown
- 2015-04-30 AR ARP150101317A patent/AR100251A1/es unknown
- 2015-04-30 JP JP2016565219A patent/JP6493890B2/ja active Active
- 2015-04-30 KR KR1020167033658A patent/KR102400920B1/ko active Active
- 2015-04-30 RS RS20220059A patent/RS62874B1/sr unknown
- 2015-04-30 LT LTEPPCT/US2015/028635T patent/LT3137169T/lt unknown
- 2015-04-30 CN CN201580035484.6A patent/CN106659914B/zh active Active
- 2015-04-30 AU AU2015253040A patent/AU2015253040B2/en not_active Ceased
- 2015-04-30 PL PL15785884T patent/PL3137169T3/pl unknown
- 2015-04-30 EP EP15785884.6A patent/EP3137169B1/en active Active
- 2015-04-30 PE PE2016002162A patent/PE20161438A1/es unknown
- 2015-04-30 CA CA2947283A patent/CA2947283C/en active Active
- 2015-04-30 US US14/701,304 patent/US9255097B2/en active Active
- 2015-04-30 HR HRP20220096TT patent/HRP20220096T1/hr unknown
- 2015-04-30 EA EA201692079A patent/EA036672B8/ru not_active IP Right Cessation
- 2015-04-30 SM SM20220066T patent/SMT202200066T1/it unknown
- 2015-04-30 ES ES15785884T patent/ES2903423T3/es active Active
- 2015-04-30 TW TW104114015A patent/TWI676620B/zh not_active IP Right Cessation
- 2015-04-30 SI SI201531769T patent/SI3137169T1/sl unknown
-
2016
- 2016-01-05 US US14/988,022 patent/US9573930B2/en active Active
- 2016-02-08 US US15/018,814 patent/US9771329B2/en active Active
- 2016-10-26 IL IL248505A patent/IL248505B/en active IP Right Grant
- 2016-10-27 CL CL2016002736A patent/CL2016002736A1/es unknown
- 2016-10-31 SA SA519410025A patent/SA519410025B1/ar unknown
- 2016-10-31 SA SA516380201A patent/SA516380201B1/ar unknown
- 2016-11-01 NI NI201600165A patent/NI201600165A/es unknown
- 2016-11-02 PH PH12016502179A patent/PH12016502179A1/en unknown
- 2016-11-04 ZA ZA2016/07613A patent/ZA201607613B/en unknown
-
2017
- 2017-01-09 US US15/401,894 patent/US9776974B2/en active Active
- 2017-08-23 US US15/684,886 patent/US10207999B2/en active Active
- 2017-08-25 US US15/687,251 patent/US10023543B2/en active Active
-
2018
- 2018-06-13 US US16/007,937 patent/US10654810B2/en active Active
-
2020
- 2020-04-06 US US16/841,595 patent/US11084793B2/en active Active
-
2021
- 2021-06-23 US US17/356,389 patent/US11987560B2/en active Active
-
2022
- 2022-02-01 CY CY20221100083T patent/CY1124959T1/el unknown
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