JP2020519667A5 - - Google Patents
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- Publication number
- JP2020519667A5 JP2020519667A5 JP2019563164A JP2019563164A JP2020519667A5 JP 2020519667 A5 JP2020519667 A5 JP 2020519667A5 JP 2019563164 A JP2019563164 A JP 2019563164A JP 2019563164 A JP2019563164 A JP 2019563164A JP 2020519667 A5 JP2020519667 A5 JP 2020519667A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- solvate
- acceptable salt
- pharmaceutically acceptable
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 23
- 239000012453 solvate Substances 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000001475 halogen functional group Chemical group 0.000 claims 15
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- -1 cyano, aminohydroxy Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000003857 carboxamides Chemical class 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 206010000871 Acute monocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000003757 neuroblast Anatomy 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 0 CC(*1*)=C(C)c2c1s*c(*)c2C Chemical compound CC(*1*)=C(C)c2c1s*c(*)c2C 0.000 description 1
- OYZJWOSONHKRLC-UHFFFAOYSA-N CC1C=C(C(F)(F)F)C(C#N)=CC1 Chemical compound CC1C=C(C(F)(F)F)C(C#N)=CC1 OYZJWOSONHKRLC-UHFFFAOYSA-N 0.000 description 1
- KFINRIKJBULSTD-UHFFFAOYSA-N CCCCc(cc1)ccc1C(N)=O Chemical compound CCCCc(cc1)ccc1C(N)=O KFINRIKJBULSTD-UHFFFAOYSA-N 0.000 description 1
- OWISXYQFTOYGRO-UHFFFAOYSA-N Cc(c(C)c1)ccc1C#N Chemical compound Cc(c(C)c1)ccc1C#N OWISXYQFTOYGRO-UHFFFAOYSA-N 0.000 description 1
- KUQQONVKIURIQU-UHFFFAOYSA-N Cc(c(F)c1)ccc1C#N Chemical compound Cc(c(F)c1)ccc1C#N KUQQONVKIURIQU-UHFFFAOYSA-N 0.000 description 1
- DCUNRLLJHAWKRZ-UHFFFAOYSA-N Cc(cc1)cc2c1[nH]nc2 Chemical compound Cc(cc1)cc2c1[nH]nc2 DCUNRLLJHAWKRZ-UHFFFAOYSA-N 0.000 description 1
- QLZDTHTXOUOSCV-UHFFFAOYSA-N Cc(cc1C)ccc1C#N Chemical compound Cc(cc1C)ccc1C#N QLZDTHTXOUOSCV-UHFFFAOYSA-N 0.000 description 1
- HXQDSHSATAEREW-UHFFFAOYSA-N Cc(cc1C2)ccc1NC2=O Chemical compound Cc(cc1C2)ccc1NC2=O HXQDSHSATAEREW-UHFFFAOYSA-N 0.000 description 1
- WCGNLBCJPBKXCN-UHFFFAOYSA-N Cc(cc1F)ccc1C#N Chemical compound Cc(cc1F)ccc1C#N WCGNLBCJPBKXCN-UHFFFAOYSA-N 0.000 description 1
- ONABUDWHSYOJDU-UHFFFAOYSA-N Cc1ccc(-c2ccc3N(C)CCOc3c2)c(F)c1 Chemical compound Cc1ccc(-c2ccc3N(C)CCOc3c2)c(F)c1 ONABUDWHSYOJDU-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762506349P | 2017-05-15 | 2017-05-15 | |
| US62/506,349 | 2017-05-15 | ||
| PCT/US2018/032619 WO2018213211A1 (en) | 2017-05-15 | 2018-05-15 | Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020519667A JP2020519667A (ja) | 2020-07-02 |
| JP2020519667A5 true JP2020519667A5 (cg-RX-API-DMAC7.html) | 2021-07-26 |
| JP7352284B2 JP7352284B2 (ja) | 2023-09-28 |
Family
ID=62685119
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019563164A Active JP7352284B2 (ja) | 2017-05-15 | 2018-05-15 | ＬＳＤ－１インヒビターとしてのピロロ〔２，３－ｃ〕ピリジン及び関連類似体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11168082B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3628044B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP7352284B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN110914265B (cg-RX-API-DMAC7.html) |
| AU (2) | AU2018269947B2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2018213211A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112119080B (zh) * | 2018-05-15 | 2023-07-11 | 密歇根大学董事会 | 作为lsd-1抑制剂的咪唑并[4,5-c]吡啶化合物 |
| SI3941466T1 (sl) | 2019-03-20 | 2026-04-30 | Oryzon Genomics, S.A. | Vafidemstat za zdravljenje neagresivnih simptomov mejne osebnostne motnje |
| HRP20251471T1 (hr) | 2019-03-20 | 2026-01-02 | Oryzon Genomics, S.A. | Postupci liječenja poremećaja hiperaktivnosti s deficitom pažnje korištenjem inhibitora kdm1a kao što je spoj vafidemstat |
| US20220227763A1 (en) | 2019-05-29 | 2022-07-21 | Syngenta Crop Protection Ag | Microbiocidal derivatives |
| CN112451671B (zh) * | 2020-12-02 | 2021-11-02 | 武汉大学 | KDM1A在抑制RNA病毒刺激下干扰素IFNβ表达中的应用 |
| CA3231846A1 (en) | 2021-04-08 | 2022-10-13 | Tamara Maes | Combinations of lsd1 inhibitors for treating myeloid cancers |
| CN116102533A (zh) * | 2021-11-11 | 2023-05-12 | 中国科学院上海药物研究所 | 一种芳杂环类化合物及其应用 |
| JP2025503099A (ja) * | 2022-01-25 | 2025-01-30 | 成都苑▲東▼生物制▲薬▼股▲ふん▼有限公司 | ピリジン系誘導体、その製造方法及び使用 |
| US20250295660A1 (en) | 2022-05-09 | 2025-09-25 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
| US20250275969A1 (en) | 2022-05-09 | 2025-09-04 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| AU2023327925A1 (en) * | 2022-08-22 | 2025-02-20 | Redx Pharma Limited | Pyrido-pyrazoles as inhibitors of ddr's for the treatment of fibrotic disorders and cancer |
| US20260151399A1 (en) | 2022-11-24 | 2026-06-04 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| WO2024208187A1 (zh) * | 2023-04-03 | 2024-10-10 | 上海复星医药（集团）股份有限公司 | 氮杂芳基化合物及其作为lsd1抑制剂的用途 |
| EP4784570A1 (en) * | 2023-09-28 | 2026-08-05 | The Regents of The University of Michigan | Oxygenated heterocyclic lsd-1 inhibitors and related methods of use |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| JP2002507996A (ja) | 1997-07-03 | 2002-03-12 | デュポン ファーマシューティカルズ カンパニー | 神経学的障害を治療するためのイミダゾピリミジン類およびイミダゾピリジン類 |
| US6365589B1 (en) | 1998-07-02 | 2002-04-02 | Bristol-Myers Squibb Pharma Company | Imidazo-pyridines, -pyridazines, and -triazines as corticotropin releasing factor antagonists |
| EP2295550A3 (en) * | 2001-04-30 | 2011-12-14 | Vertex Pharmaceuticals Incorporated | Crystal structures of GSK-3beta protein and protein complexes and their use |
| AU2006247322A1 (en) | 2005-05-16 | 2006-11-23 | Irm Llc | Pyrrolopyridine derivatives as protein kinase inhibitors |
| WO2007084667A2 (en) | 2006-01-19 | 2007-07-26 | Osi Pharmaceutical, Inc. | Fused heterobicyclic kinase inhibitors |
| KR20090082453A (ko) * | 2006-11-01 | 2009-07-30 | 버텍스 파마슈티칼스 인코포레이티드 | 야누스 키나제의 억제제로서 유용한 트리사이클릭 헤테로아릴 화합물 |
| US20100130496A1 (en) * | 2007-04-12 | 2010-05-27 | F. Hoffmann-La Roche Ag | Pyrimidine derivatives as inhibitors of phosphatidylinositol-3-kinase |
| WO2008138184A1 (fr) * | 2007-05-14 | 2008-11-20 | Shanghai Hengrui Pharmaceutical Co.Ltd. | Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| WO2009029609A1 (en) | 2007-08-27 | 2009-03-05 | Wyeth | Imidazopyridine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system |
| GB201008134D0 (en) | 2010-05-14 | 2010-06-30 | Medical Res Council Technology | Compounds |
| JP5744021B2 (ja) * | 2010-06-30 | 2015-07-01 | 富士フイルム株式会社 | 新規なニコチンアミド誘導体またはその塩 |
| KR20150024669A (ko) * | 2013-08-27 | 2015-03-09 | 제일모직주식회사 | 화합물, 이를 포함하는 유기발광소자 및 상기 유기발광소자를 포함하는 표시장치 |
| CA3161836A1 (en) | 2013-12-11 | 2015-06-18 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| LT3105218T (lt) | 2014-02-13 | 2019-12-10 | Incyte Corp | Ciklopropilaminai kaip lsd1 inhibitoriai |
| WO2015123424A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| RU2692485C2 (ru) * | 2014-04-02 | 2019-06-25 | Интермьюн, Инк. | Противофиброзные пиридиноны |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| EA201792205A1 (ru) * | 2015-04-03 | 2018-02-28 | Инсайт Корпорейшн | Гетероциклические соединения как ингибиторы lsd1 |
| AU2016274956A1 (en) | 2015-06-11 | 2017-12-14 | Usher Iii Initiative, Inc. | Methods of treating or preventing a proteopathy |
| AR110963A1 (es) | 2017-02-07 | 2019-05-22 | Dae Woong Pharma | Compuestos heterocíclicos, su método de preparación y composición farmacéutica que los comprende |
-
2018
- 2018-05-15 JP JP2019563164A patent/JP7352284B2/ja active Active
- 2018-05-15 CN CN201880046207.9A patent/CN110914265B/zh active Active
- 2018-05-15 US US16/611,238 patent/US11168082B2/en active Active
- 2018-05-15 EP EP18733006.3A patent/EP3628044B1/en active Active
- 2018-05-15 AU AU2018269947A patent/AU2018269947B2/en active Active
- 2018-05-15 WO PCT/US2018/032619 patent/WO2018213211A1/en not_active Ceased
-
2022
- 2022-01-13 AU AU2022200197A patent/AU2022200197A1/en not_active Abandoned