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 (cg-RX-API-DMAC7.html) | 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 |
|---|---|---|---|---|
| JP6473457B2 (ja) | 2014-01-17 | 2019-02-20 | ノバルティス アーゲー | Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| 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 |
| HRP20220096T1 (hr) | 2014-05-01 | 2022-04-15 | Celgene Quanticel Research, Inc. | Inhibitori lizin specifične demetilaze-1 |
| LT3160956T (lt) * | 2014-06-27 | 2020-09-10 | Celgene Quanticel Research, Inc. | Lizinui specifinės demetilazės-1 inhibitoriai |
| EA201891526A3 (ru) * | 2014-07-03 | 2019-05-31 | Селджен Квонтисел Рисёрч, Инк. | Ингибиторы лизин-специфической деметилазы-1 |
| US20180284095A1 (en) | 2015-06-12 | 2018-10-04 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| ES2741746T3 (es) | 2015-06-19 | 2020-02-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| EP3310771B1 (en) * | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| JP6718889B2 (ja) | 2015-06-19 | 2020-07-08 | ノバルティス アーゲー | Ｓｈｐ２の活性を阻害するための化合物および組成物 |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| SI3371152T1 (sl) | 2015-11-05 | 2021-06-30 | Celgene Quanticel Research, Inc. | Sestavki, ki vsebujejo lisin specifični demetilaze-1 inhibitor s piridinskim obročem in njihova uporaba pri zdravljenju raka |
| US10059668B2 (en) | 2015-11-05 | 2018-08-28 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| CA3006434C (en) | 2015-11-27 | 2021-03-16 | Taiho Pharmaceutical Co., Ltd. | Biphenyl compound or salt thereof |
| SG11201805645QA (en) | 2015-12-29 | 2018-07-30 | Mirati Therapeutics Inc | Lsd1 inhibitors |
| CA3017411C (en) | 2016-03-15 | 2024-06-25 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
| EP3430015B9 (en) | 2016-03-16 | 2025-12-31 | Oryzon Genomics, S.A. | METHODS FOR DETERMINING THE ENGAGEMENT OF A KDM1A TARGET AND CORRESPONDING USEFUL CHEMOPROBE |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| CN114057689A (zh) | 2016-06-14 | 2022-02-18 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| EP4286381A3 (en) * | 2016-08-10 | 2024-02-28 | Celgene Quanticel Research, Inc. | Treatment of merkel celll carcinoma |
| EP3523290A4 (en) * | 2016-09-30 | 2020-07-29 | Novartis AG | IMPROVED EFFICIENCY IMMUNE EFFICIENT CELL THERAPIES |
| WO2018083138A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| EP3568204B1 (en) | 2017-01-10 | 2023-08-30 | Novartis AG | Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor |
| US20200039938A1 (en) | 2017-03-30 | 2020-02-06 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
| 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 |
| RU2765152C2 (ru) | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| TWI749235B (zh) | 2017-05-31 | 2021-12-11 | 日商大鵬藥品工業股份有限公司 | 基於insm1表現之lsd1抑制劑之治療效果的預測方法 |
| AU2018309372B2 (en) | 2017-08-03 | 2024-08-15 | Oryzon Genomics, S.A. | Methods of treating behavior alterations |
| 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 |
| 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 |
| AU2020242302B2 (en) | 2019-03-20 | 2025-10-30 | Oryzon Genomics, S.A. | Methods of treating borderline personality disorder |
| EP3983016A4 (en) | 2019-06-13 | 2023-06-07 | Celgene Corporation | CANCER TREATMENT METHODS BY TARGETING COLD TUMORS |
| WO2020257665A1 (en) | 2019-06-20 | 2020-12-24 | Celgene Corporation | Azacitidine in combination with venetoclax, gilteritinib, midostaurin or other compounds for treating leukemia or myelodysplastic syndrome |
| 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 |
| EP4038054A1 (en) * | 2019-10-01 | 2022-08-10 | Bayer Aktiengesellschaft | Pyrimidinedione derivatives |
| WO2021095835A1 (en) | 2019-11-13 | 2021-05-20 | Taiho Pharmaceutical Co., Ltd. | Novel salt of terphenyl compound |
| US20230089536A1 (en) | 2020-03-06 | 2023-03-23 | Celgene Quanticel Research, Inc. | 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 |
| 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 |
| AU2022254484A1 (en) | 2021-04-08 | 2023-11-09 | 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 |
| WO2023217758A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| KR20250109775A (ko) | 2022-11-24 | 2025-07-17 | 오리존 지노믹스 에스.에이. | 암 치료를 위한 lsd1 억제제 및 메닌 억제제의 조합 |
| JP2025541771A (ja) | 2022-12-02 | 2025-12-23 | ニューモラ セラピューティクス インコーポレイテッド | 神経障害を処置する方法 |
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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 |
| ATE274510T1 (de) * | 1998-06-19 | 2004-09-15 | Chiron Corp | Glycogen synthase kinase 3 inhibitoren |
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| 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 |
| JP5599791B2 (ja) * | 2008-07-29 | 2014-10-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ５−アルキニル−ピリミジン |
| TWI435874B (zh) * | 2008-10-31 | 2014-05-01 | Toray Industries | 環己烷衍生物及其醫藥用途 |
| WO2011143057A1 (en) * | 2010-05-11 | 2011-11-17 | Merck Sharp & Dohme Corp. | Novel 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 |
| KR101884493B1 (ko) | 2011-03-25 | 2018-08-01 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | Lsd1 억제제로서의 시클로프로필아민 |
| 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 |
| WO2014164780A1 (en) | 2013-03-11 | 2014-10-09 | 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) |
| US9034900B2 (en) | 2013-10-18 | 2015-05-19 | Quanticel Pharmaceuticals, Inc. | Bromodomain inhibitors |
| FI3080100T3 (fi) * | 2013-12-11 | 2023-03-15 | Celgene Quanticel Res Inc | Lysiinispesifisen demetylaasi-1:n estäjät |
| HRP20220096T1 (hr) * | 2014-05-01 | 2022-04-15 | Celgene Quanticel Research, Inc. | Inhibitori lizin specifične demetilaze-1 |
| WO2016014859A1 (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 |
| SI3371152T1 (sl) * | 2015-11-05 | 2021-06-30 | Celgene Quanticel Research, Inc. | Sestavki, ki vsebujejo lisin specifični demetilaze-1 inhibitor s piridinskim obročem in njihova uporaba pri zdravljenju raka |
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2015
- 2015-04-30 HR HRP20220096TT patent/HRP20220096T1/hr unknown
- 2015-04-30 AR ARP150101317A patent/AR100251A1/es unknown
- 2015-04-30 SI SI201531769T patent/SI3137169T1/sl unknown
- 2015-04-30 ES ES15785884T patent/ES2903423T3/es active Active
- 2015-04-30 KR KR1020167033658A patent/KR102400920B1/ko active Active
- 2015-04-30 PT PT157858846T patent/PT3137169T/pt unknown
- 2015-04-30 TW TW104114015A patent/TWI676620B/zh not_active IP Right Cessation
- 2015-04-30 JP JP2016565219A patent/JP6493890B2/ja active Active
- 2015-04-30 SG SG11201609033TA patent/SG11201609033TA/en unknown
- 2015-04-30 DK DK15785884.6T patent/DK3137169T3/da active
- 2015-04-30 BR BR112016025248-9A patent/BR112016025248B1/pt not_active IP Right Cessation
- 2015-04-30 SM SM20220066T patent/SMT202200066T1/it unknown
- 2015-04-30 CA CA2947283A patent/CA2947283C/en active Active
- 2015-04-30 RS RS20220059A patent/RS62874B1/sr unknown
- 2015-04-30 WO PCT/US2015/028635 patent/WO2015168466A1/en not_active Ceased
- 2015-04-30 MX MX2016014253A patent/MX373373B/es active IP Right Grant
- 2015-04-30 PE PE2016002162A patent/PE20161438A1/es unknown
- 2015-04-30 EP EP15785884.6A patent/EP3137169B1/en active Active
- 2015-04-30 EA EA201692079A patent/EA036672B8/ru not_active IP Right Cessation
- 2015-04-30 PL PL15785884T patent/PL3137169T3/pl unknown
- 2015-04-30 US US14/701,304 patent/US9255097B2/en active Active
- 2015-04-30 HU HUE15785884A patent/HUE057895T2/hu 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
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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
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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
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2021
- 2021-06-23 US US17/356,389 patent/US11987560B2/en active Active
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2022
- 2022-02-01 CY CY20221100083T patent/CY1124959T1/el unknown