JP2017514830A5 - - Google Patents
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- 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
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- 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.)
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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 (esLanguage) | 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)
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| 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 |
| AU2015253040B2 (en) | 2014-05-01 | 2020-04-09 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| EA030946B1 (ru) * | 2014-06-27 | 2018-10-31 | Селджен Квонтисел Рисёрч, Инк. | Ингибиторы лизин-специфической деметилазы-1 |
| HUE058852T2 (hu) * | 2014-07-03 | 2022-09-28 | Celgene Quanticel Res Inc | Lizinspecifikus demetiláz-1 inhibitorai |
| CN107849611A (zh) | 2015-06-12 | 2018-03-27 | 奥瑞泽恩基因组学股份有限公司 | 与lsd1抑制剂相关的生物标志物及其用途 |
| WO2016203405A1 (en) * | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| US10287266B2 (en) | 2015-06-19 | 2019-05-14 | 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 |
| WO2017079476A1 (en) | 2015-11-05 | 2017-05-11 | Mirati Therapeutics, Inc. | Lsd1 inhibitors |
| LT3371152T (lt) | 2015-11-05 | 2021-04-12 | Celgene Quanticel Research, Inc. | Kompozicijos, apimančios lizinui specifinės demetilazės-1 inhibitorių, turinčios pirimidino žiedą, ir jų panaudojimas vėžio gydymui |
| PL3381896T3 (pl) | 2015-11-27 | 2023-05-08 | Taiho Pharmaceutical Co., Ltd. | Związek bifenylowy lub jego sól |
| US9809541B2 (en) | 2015-12-29 | 2017-11-07 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| CN109195593A (zh) | 2016-03-15 | 2019-01-11 | 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 |
| KR102457146B1 (ko) | 2016-06-14 | 2022-10-19 | 노파르티스 아게 | Shp2의 활성을 억제하기 위한 화합물 및 조성물 |
| WO2018031658A1 (en) * | 2016-08-10 | 2018-02-15 | 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 |
| EP3535420A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| EP3535414A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| CA3048340A1 (en) | 2017-01-10 | 2018-07-19 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| US20180290977A1 (en) | 2017-03-30 | 2018-10-11 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
| JP6738962B2 (ja) * | 2017-05-26 | 2020-08-12 | 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 |
| MX391414B (es) | 2017-05-26 | 2025-03-21 | Taiho Pharmaceutical Co Ltd | Compuesto novedoso de bifenilo o sal del mismo. |
| 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 |
| BR112020000827A2 (pt) | 2017-08-03 | 2020-07-21 | Oryzon Genomics, S.A. | métodos de tratamento de alterações de comportamento |
| JP7265275B2 (ja) * | 2018-03-21 | 2023-04-26 | スージョウ プーヘー バイオファーマ カンパニー リミテッド | Ｓｈｐ２阻害剤およびその使用 |
| 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 |
| ES3053813T3 (en) | 2019-03-20 | 2026-01-26 | Oryzon Genomics Sa | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| SG11202109159VA (en) | 2019-03-20 | 2021-10-28 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| MX2021015447A (es) | 2019-06-13 | 2022-04-06 | Celgene Corp | Métodos de tratamiento del cáncer dirigidos a tumores fríos. |
| AU2020297596A1 (en) | 2019-06-20 | 2022-02-03 | Celgene Corporation | Azacitidine in combination with venetoclax, gilteritinib, midostaurin or other compounds for treating leukemia or myelodysplastic syndrome |
| EP3994280A1 (en) | 2019-07-05 | 2022-05-11 | Oryzon Genomics, S.A. | Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors |
| WO2021063821A1 (en) * | 2019-10-01 | 2021-04-08 | Bayer Aktiengesellschaft | Pyrimidinedione derivatives |
| ES3034158T3 (en) | 2019-11-13 | 2025-08-13 | Taiho Pharmaceutical Co Ltd | Novel salt of terphenyl compound |
| IL296564A (en) | 2020-03-06 | 2022-11-01 | Celgene Quanticel Res Inc | Combination of an lsd-1 inhibitor and nivolumab for use in treating sclc or sqnsclc |
| US20230241063A1 (en) * | 2020-06-05 | 2023-08-03 | Celgene Quanticel Research, Inc. | Methods of treating prostate cancer |
| EP4306520A4 (en) * | 2021-03-11 | 2025-05-07 | Medshine Discovery Inc. | THIOPHENE COMPOUND AND ITS USE |
| WO2022199662A1 (zh) * | 2021-03-24 | 2022-09-29 | 四川汇宇制药股份有限公司 | 一种多环化合物及其应用 |
| EP4319732A1 (en) | 2021-04-08 | 2024-02-14 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
| JP2025516648A (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ｎｆ１変異腫瘍の治療法 |
| CN119546292A (zh) | 2022-05-09 | 2025-02-28 | 奥莱松基因组股份有限公司 | 使用lsd1抑制剂治疗恶性周围神经鞘瘤(mpnst)的方法 |
| EP4622635A1 (en) | 2022-11-24 | 2025-10-01 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| WO2024119067A1 (en) | 2022-12-02 | 2024-06-06 | 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 |
| ATE274510T1 (de) * | 1998-06-19 | 2004-09-15 | Chiron Corp | Glycogen synthase kinase 3 inhibitoren |
| WO2002102313A2 (en) * | 2001-06-19 | 2002-12-27 | Bristol-Myers Squibb Company | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
| US7423148B2 (en) | 2002-11-21 | 2008-09-09 | Chiron Corporation | Small molecule PI 3-kinase inhibitors and methods of their use |
| 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 |
| US8466163B2 (en) | 2006-12-11 | 2013-06-18 | Bionomics Limited | Furo[2,3-d]pyrimidines and related compounds and methods for treating disease states by inhibiting tubulin polymerization |
| PL2323992T3 (pl) | 2008-07-29 | 2017-01-31 | Boehringer Ingelheim International Gmbh | 5-alkinylo-pirymidyny |
| 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 |
| US9527805B2 (en) | 2010-09-10 | 2016-12-27 | Robert A. Casero | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| CA2831143C (en) | 2011-03-25 | 2019-05-21 | Glaxosmithkline Intellectual Property Development Limited | Cyclopropylamines as lsd1 inhibitors |
| 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 |
| JP2016516701A (ja) | 2013-03-11 | 2016-06-09 | アッヴィ・インコーポレイテッド | 縮合四環系ブロモドメイン阻害剤 |
| 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) |
| EP3640241B1 (en) | 2013-10-18 | 2022-09-28 | Celgene Quanticel Research, Inc. | Bromodomain inhibitors |
| SI3080100T1 (sl) * | 2013-12-11 | 2023-04-28 | Celgene Quanticel Research, Inc. | Inhibitorji lizin specifične demetilaze-1 |
| AU2015253040B2 (en) * | 2014-05-01 | 2020-04-09 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| WO2016014859A1 (en) | 2014-07-25 | 2016-01-28 | Pharmacyclics Llc | Bet inhibitor and bruton's tyrosine kinase inhibitor combinations |
| US20190055235A1 (en) | 2014-12-17 | 2019-02-21 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| LT3371152T (lt) * | 2015-11-05 | 2021-04-12 | Celgene Quanticel Research, Inc. | Kompozicijos, apimančios lizinui specifinės demetilazės-1 inhibitorių, turinčios pirimidino žiedą, ir jų panaudojimas vėžio gydymui |
-
2015
- 2015-04-30 AU AU2015253040A patent/AU2015253040B2/en not_active Ceased
- 2015-04-30 SG SG11201609033TA patent/SG11201609033TA/en unknown
- 2015-04-30 LT LTEPPCT/US2015/028635T patent/LT3137169T/lt 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
- 2015-04-30 PE PE2016002162A patent/PE20161438A1/es unknown
- 2015-04-30 PT PT157858846T patent/PT3137169T/pt unknown
- 2015-04-30 MX MX2016014253A patent/MX373373B/es active IP Right Grant
- 2015-04-30 BR BR112016025248-9A patent/BR112016025248B1/pt not_active IP Right Cessation
- 2015-04-30 HU HUE15785884A patent/HUE057895T2/hu unknown
- 2015-04-30 HR HRP20220096TT patent/HRP20220096T1/hr unknown
- 2015-04-30 KR KR1020167033658A patent/KR102400920B1/ko active Active
- 2015-04-30 US US14/701,304 patent/US9255097B2/en active Active
- 2015-04-30 WO PCT/US2015/028635 patent/WO2015168466A1/en not_active Ceased
- 2015-04-30 CN CN201580035484.6A patent/CN106659914B/zh active Active
- 2015-04-30 EA EA201692079A patent/EA036672B8/ru not_active IP Right Cessation
- 2015-04-30 DK DK15785884.6T patent/DK3137169T3/da active
- 2015-04-30 PL PL15785884T patent/PL3137169T3/pl unknown
- 2015-04-30 SM SM20220066T patent/SMT202200066T1/it unknown
- 2015-04-30 CA CA2947283A patent/CA2947283C/en active Active
- 2015-04-30 EP EP15785884.6A patent/EP3137169B1/en active Active
- 2015-04-30 RS RS20220059A patent/RS62874B1/sr unknown
- 2015-04-30 JP JP2016565219A patent/JP6493890B2/ja active Active
- 2015-04-30 AR ARP150101317A patent/AR100251A1/es 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 SA516380201A patent/SA516380201B1/ar unknown
- 2016-10-31 SA SA519410025A patent/SA519410025B1/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
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2018
- 2018-06-13 US US16/007,937 patent/US10654810B2/en active Active
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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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