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 |
|---|---|---|---|---|
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| WO2015107493A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| ES2699354T3 (es) | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2 |
| AU2015253040B2 (en) | 2014-05-01 | 2020-04-09 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| HUE050564T2 (hu) * | 2014-06-27 | 2020-12-28 | Celgene Quanticel Res Inc | Lizinspecifikus demetiláz-1 inhibitorai |
| SI3511319T1 (sl) * | 2014-07-03 | 2023-10-30 | Celgene Quanticel Research, Inc. | Inhibitorji lizin specifične demetilaze-1 |
| SG10201911989SA (en) | 2015-06-12 | 2020-02-27 | Oryzon Genomics Sa | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2016203405A1 (en) * | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| CN107922388B (zh) | 2015-06-19 | 2020-12-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | 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 |
| HRP20210144T8 (hr) * | 2015-11-05 | 2021-04-16 | Celgene Quanticel Research, Inc. | Kompozicije koje sadrže inhibitor lizin specifične demetilaze-1 koje imaju pirimidinski prsten i njihova primjena u liječenju raka |
| US10059668B2 (en) | 2015-11-05 | 2018-08-28 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| SG11201804121RA (en) * | 2015-11-27 | 2018-06-28 | Taiho Pharmaceutical Co Ltd | Novel biphenyl compound or salt thereof |
| CN108884029B (zh) | 2015-12-29 | 2021-10-26 | 米拉蒂医疗股份有限公司 | Lsd1抑制剂 |
| 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 |
| 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 |
| RU2021106500A (ru) | 2016-06-14 | 2021-04-16 | Новартис Аг | Соединения и композиции для подавления активности shp2 |
| IL264718B2 (en) | 2016-08-10 | 2023-11-01 | Celgene Corp | Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomas |
| EP3523290A4 (en) * | 2016-09-30 | 2020-07-29 | Novartis AG | IMPROVED EFFICIENCY IMMUNE EFFICIENT CELL THERAPIES |
| US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| WO2018083138A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| ES2964956T3 (es) | 2017-01-10 | 2024-04-10 | Novartis Ag | Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2 |
| US20200039938A1 (en) | 2017-03-30 | 2020-02-06 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
| DK3632443T3 (da) | 2017-05-26 | 2023-09-11 | Taiho Pharmaceutical Co Ltd | Potentiator af antitumorvirkning ved hjælp af en biphenylforbindelse |
| RU2765152C2 (ru) | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| MA50518A (fr) | 2017-05-31 | 2020-09-09 | Taiho Pharmaceutical Co Ltd | Méthode de prédiction de l'effet thérapeutique d'un inhibiteur de lsd1 en fonction de l'expression d'insm1 |
| DK3661510T3 (da) | 2017-08-03 | 2025-01-02 | Oryzon Genomics Sa | Fremgangsmåder til behandling af adfærdsændringer |
| AU2019239658A1 (en) * | 2018-03-21 | 2020-11-12 | Suzhou Puhe BioPharma Co., Ltd. | SHP2 inhibitors and uses thereof |
| 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 |
| EP3941465B1 (en) | 2019-03-20 | 2025-09-17 | Oryzon Genomics, S.A. | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| CN121370879A (zh) | 2019-03-20 | 2026-01-23 | 奥莱松基因组股份有限公司 | 治疗边缘型人格障碍的方法 |
| US12357633B2 (en) | 2019-06-13 | 2025-07-15 | Celgene Corporation | Methods of treating cancer by targeting cold tumors |
| MX2021015993A (es) * | 2019-06-20 | 2022-04-06 | Celgene Corp | Azacitidina en combinación con venetoclax, gilteritinib, midostaurina u otros compuestos para el tratamiento de leucemia o síndrome mielodisplásico. |
| WO2021004610A1 (en) | 2019-07-05 | 2021-01-14 | 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 |
| BR112022008020A2 (pt) | 2019-11-13 | 2022-07-12 | Taiho Pharmaceutical Co Ltd | Métodos de tratamento de doenças e distúrbios relacionados a lsd1 com inibidores de lsd1 |
| AU2021230575A1 (en) * | 2020-03-06 | 2022-10-20 | Celgene Quanticel Research, Inc. | Combination of an LSD-1 inhibitor and nivolumab for use in treating SCLC or sqNSCLC |
| CN116056707A (zh) * | 2020-06-05 | 2023-05-02 | 赛尔基因昆蒂赛尔研究公司 | 治疗前列腺癌的方法 |
| TWI834127B (zh) * | 2021-03-11 | 2024-03-01 | 大陸商南京明德新藥研發有限公司 | 噻吩類化合物及其應用 |
| US20240216357A1 (en) * | 2021-03-24 | 2024-07-04 | Sichuan Huiyu Pharmaceutical Co., Ltd. | Polycyclic compound and application thereof |
| BR112023020554A2 (pt) | 2021-04-08 | 2023-12-05 | Oryzon Genomics Sa | Combinações de inibidores de lsd1 para o tratamento de cânceres mieloides |
| 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 |
| 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 |
| CN120379982A (zh) | 2022-12-02 | 2025-07-25 | 纽摩拉治疗公司 | 治疗神经障碍的方法 |
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| US5550147A (en) * | 1992-02-05 | 1996-08-27 | Fujisawa Pharmaceutical Co., Ltd. | Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same |
| KR100581199B1 (ko) | 1998-06-19 | 2006-05-17 | 카이론 코포레이션 | 글리코겐 신타제 키나제 3의 억제제 |
| EP1397142A4 (en) * | 2001-06-19 | 2004-11-03 | Bristol Myers Squibb Co | PYRIMIDINE PHOSPHODIESTERASE (PDE) INHIBITORS 7 |
| MXPA05005477A (es) | 2002-11-21 | 2005-07-25 | Chiron Corp | Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer. |
| 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 |
| 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 |
| EP2970285B1 (en) | 2013-03-11 | 2019-04-17 | AbbVie Inc. | Fused tetracyclic bromodomain inhibitors |
| 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) |
| SG11201602996RA (en) | 2013-10-18 | 2016-05-30 | Celgene Quanticel Res Inc | Bromodomain inhibitors |
| SMT202300014T1 (it) * | 2013-12-11 | 2023-05-12 | Celgene Quanticel Research Inc | Inibitori della demetilasi lisina-specifica-1 |
| AU2015253040B2 (en) * | 2014-05-01 | 2020-04-09 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific 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 |
| HRP20210144T8 (hr) * | 2015-11-05 | 2021-04-16 | Celgene Quanticel Research, Inc. | Kompozicije koje sadrže inhibitor lizin specifične demetilaze-1 koje imaju pirimidinski prsten i njihova primjena u liječenju raka |
-
2015
- 2015-04-30 AU AU2015253040A patent/AU2015253040B2/en not_active Ceased
- 2015-04-30 AR ARP150101317A patent/AR100251A1/es unknown
- 2015-04-30 SM SM20220066T patent/SMT202200066T1/it unknown
- 2015-04-30 CA CA2947283A patent/CA2947283C/en active Active
- 2015-04-30 KR KR1020167033658A patent/KR102400920B1/ko active Active
- 2015-04-30 HU HUE15785884A patent/HUE057895T2/hu unknown
- 2015-04-30 PL PL15785884T patent/PL3137169T3/pl unknown
- 2015-04-30 BR BR112016025248-9A patent/BR112016025248B1/pt not_active IP Right Cessation
- 2015-04-30 SG SG11201609033TA patent/SG11201609033TA/en unknown
- 2015-04-30 US US14/701,304 patent/US9255097B2/en active Active
- 2015-04-30 MX MX2016014253A patent/MX373373B/es active IP Right Grant
- 2015-04-30 PT PT157858846T patent/PT3137169T/pt unknown
- 2015-04-30 LT LTEPPCT/US2015/028635T patent/LT3137169T/lt unknown
- 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 DK DK15785884.6T patent/DK3137169T3/da active
- 2015-04-30 EA EA201692079A patent/EA036672B8/ru not_active IP Right Cessation
- 2015-04-30 EP EP15785884.6A patent/EP3137169B1/en active Active
- 2015-04-30 ES ES15785884T patent/ES2903423T3/es active Active
- 2015-04-30 RS RS20220059A patent/RS62874B1/sr unknown
- 2015-04-30 JP JP2016565219A patent/JP6493890B2/ja active Active
- 2015-04-30 CN CN201580035484.6A patent/CN106659914B/zh active Active
- 2015-04-30 WO PCT/US2015/028635 patent/WO2015168466A1/en not_active Ceased
- 2015-04-30 PE PE2016002162A patent/PE20161438A1/es unknown
- 2015-04-30 HR HRP20220096TT patent/HRP20220096T1/hr 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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