JP2019512474A5 - - Google Patents
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- JP2019512474A5 JP2019512474A5 JP2018546035A JP2018546035A JP2019512474A5 JP 2019512474 A5 JP2019512474 A5 JP 2019512474A5 JP 2018546035 A JP2018546035 A JP 2018546035A JP 2018546035 A JP2018546035 A JP 2018546035A JP 2019512474 A5 JP2019512474 A5 JP 2019512474A5
- Authority
- JP
- Japan
- Prior art keywords
- independently selected
- alkyl
- substituted
- independently
- cancer
- 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.)
- Ceased
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- 125000000217 alkyl group Chemical group 0.000 claims description 40
- 150000001875 compounds Chemical class 0.000 claims description 26
- 229910052736 halogen Inorganic materials 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 26
- 150000002367 halogens Chemical class 0.000 claims description 24
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 239000003814 drug Substances 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 7
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 4
- 208000003950 B-cell lymphoma Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 4
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 4
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 4
- 101000615488 Homo sapiens Methyl-CpG-binding domain protein 2 Proteins 0.000 claims description 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 4
- 239000004472 Lysine Substances 0.000 claims description 4
- 102100021299 Methyl-CpG-binding domain protein 2 Human genes 0.000 claims description 4
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 4
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims description 4
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims description 4
- 206010029260 Neuroblastoma Diseases 0.000 claims description 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 206010039491 Sarcoma Diseases 0.000 claims description 4
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 201000004101 esophageal cancer Diseases 0.000 claims description 4
- 201000010175 gallbladder cancer Diseases 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 208000005017 glioblastoma Diseases 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 208000007056 sickle cell anemia Diseases 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 3
- 206010014733 Endometrial cancer Diseases 0.000 claims description 3
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 229940035676 analgesics Drugs 0.000 claims description 2
- 239000000730 antalgic agent Substances 0.000 claims description 2
- 230000003474 anti-emetic effect Effects 0.000 claims description 2
- 239000000043 antiallergic agent Substances 0.000 claims description 2
- 229940125683 antiemetic agent Drugs 0.000 claims description 2
- 239000002111 antiemetic agent Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 230000001120 cytoprotective effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 229940127084 other anti-cancer agent Drugs 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 206010057649 Endometrial sarcoma Diseases 0.000 claims 1
- 206010019668 Hepatic fibrosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010055006 Pancreatic sarcoma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000003866 lung sarcoma Diseases 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 208000011932 ovarian sarcoma Diseases 0.000 claims 1
- 201000002526 pancreas sarcoma Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 description 12
- 125000000753 cycloalkyl group Chemical group 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 125000003342 alkenyl group Chemical group 0.000 description 2
- -1 CF 3 Chemical group 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/075195 | 2016-03-01 | ||
| CN2016075195 | 2016-03-01 | ||
| PCT/IB2017/051181 WO2017149463A1 (en) | 2016-03-01 | 2017-02-28 | Cyano-substituted indole compounds and uses thereof as lsd1 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019512474A JP2019512474A (ja) | 2019-05-16 |
| JP2019512474A5 true JP2019512474A5 (enExample) | 2020-04-02 |
Family
ID=58266015
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018546035A Ceased JP2019512474A (ja) | 2016-03-01 | 2017-02-28 | シアノ置換インドール化合物およびｌｓｄ１阻害剤としてのその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10590079B2 (enExample) |
| EP (1) | EP3423443B1 (enExample) |
| JP (1) | JP2019512474A (enExample) |
| CN (1) | CN110267945A (enExample) |
| ES (1) | ES2831832T3 (enExample) |
| WO (1) | WO2017149463A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017149463A1 (en) | 2016-03-01 | 2017-09-08 | Novartis Ag | Cyano-substituted indole compounds and uses thereof as lsd1 inhibitors |
| 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 |
| US20200069677A1 (en) | 2016-12-09 | 2020-03-05 | Constellation Pharmaceuticals, Inc. | Markers for personalized cancer treatment with lsd1 inhibitors |
| UY37774A (es) * | 2017-06-19 | 2019-01-31 | Novartis Ag | Compuestos 5-cianoindol sustituidos y usos de los mismos |
| DK3661510T3 (da) | 2017-08-03 | 2025-01-02 | Oryzon Genomics Sa | Fremgangsmåder til behandling af adfærdsændringer |
| CN108047258B (zh) * | 2017-12-17 | 2020-06-30 | 沧州普瑞东方科技有限公司 | 一种合成氨基吡啶硼酸酯的方法 |
| 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 |
| CN111909134B (zh) * | 2019-05-07 | 2024-04-26 | 北京鼎材科技有限公司 | 一种化合物及其应用、包含其的有机电致发光器件 |
| 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 |
| 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 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| CN116593621B (zh) * | 2023-06-26 | 2025-07-22 | 中国医学科学院北京协和医院 | 一种利用高效液相色谱-串联质谱联用装置定量分析血浆样本中药物的方法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0647450A1 (en) | 1993-09-09 | 1995-04-12 | BEHRINGWERKE Aktiengesellschaft | Improved prodrugs for enzyme mediated activation |
| CA2514733A1 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| EP2177502A1 (en) * | 2008-10-17 | 2010-04-21 | Oryzon Genomics, S.A. | Compounds and their use |
| DE102008052943A1 (de) * | 2008-10-23 | 2010-04-29 | Merck Patent Gmbh | Azaindolderivate |
| CN104203914B (zh) * | 2011-10-20 | 2017-07-11 | 奥瑞泽恩基因组学股份有限公司 | 作为lsd1抑制剂的(杂)芳基环丙胺化合物 |
| US9556170B2 (en) * | 2013-08-30 | 2017-01-31 | University Of Utah Research Foundation | Substituted-1H-benzo[d]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors |
| AU2015226881A1 (en) * | 2014-03-07 | 2016-09-29 | Intonation Research Laboratories | Inhibitors of histone lysine specific demethylase (LSD1) and histone deacetylases (HDACs) |
| CN104119280B (zh) * | 2014-06-27 | 2016-03-16 | 郑州大学 | 含氨基类脲与端炔结构单元的嘧啶衍生物、制备方法及应用 |
| WO2017149463A1 (en) | 2016-03-01 | 2017-09-08 | Novartis Ag | Cyano-substituted indole compounds and uses thereof as lsd1 inhibitors |
-
2017
- 2017-02-28 WO PCT/IB2017/051181 patent/WO2017149463A1/en not_active Ceased
- 2017-02-28 JP JP2018546035A patent/JP2019512474A/ja not_active Ceased
- 2017-02-28 CN CN201780027005.5A patent/CN110267945A/zh not_active Withdrawn
- 2017-02-28 US US16/081,543 patent/US10590079B2/en active Active
- 2017-02-28 ES ES17710061T patent/ES2831832T3/es active Active
- 2017-02-28 EP EP17710061.7A patent/EP3423443B1/en not_active Not-in-force
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