JP2019512474A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
Links
- 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 |
|---|---|---|---|
| CN2016075195 | 2016-03-01 | ||
| CNPCT/CN2016/075195 | 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 (38)
| 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 |
| WO2018059549A1 (en) * | 2016-09-30 | 2018-04-05 | Novartis Ag | Immune effector cell therapies with enhanced efficacy |
| US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| WO2018106984A1 (en) | 2016-12-09 | 2018-06-14 | 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 |
| AU2018309372B2 (en) | 2017-08-03 | 2024-08-15 | Oryzon Genomics, S.A. | Methods of treating behavior alterations |
| 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 |
| 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 |
| SI3941466T1 (sl) | 2019-03-20 | 2026-04-30 | Oryzon Genomics, S.A. | Vafidemstat za zdravljenje neagresivnih simptomov mejne osebnostne motnje |
| 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 |
| CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
| CA3231846A1 (en) | 2021-04-08 | 2022-10-13 | Tamara Maes | Combinations of lsd1 inhibitors for treating myeloid cancers |
| US20250275969A1 (en) | 2022-05-09 | 2025-09-04 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| US20250295660A1 (en) | 2022-05-09 | 2025-09-25 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
| US20260151399A1 (en) | 2022-11-24 | 2026-06-04 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| 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 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic 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 |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | 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 |
| WO2004078163A2 (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 |
| AU2012324803B9 (en) * | 2011-10-20 | 2017-08-24 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as LSD1 inhibitors |
| WO2015031564A2 (en) * | 2013-08-30 | 2015-03-05 | University Of Utah | Substituted-1h-benzo[d]imidazole series compounds as lysine-specfic demethylase 1 (lsd1) inhibitors |
| JP2017508798A (ja) * | 2014-03-07 | 2017-03-30 | ザ ジョンズ ホプキンス ユニバーシティ | ヒストンリジン特異的デメチラーゼ（ｌｓｄ１）およびヒストンデアセチラーゼ（ｈｄａｃ）の阻害剤 |
| 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 CN CN201780027005.5A patent/CN110267945A/zh not_active Withdrawn
- 2017-02-28 JP JP2018546035A patent/JP2019512474A/ja not_active Ceased
- 2017-02-28 EP EP17710061.7A patent/EP3423443B1/en not_active Not-in-force
- 2017-02-28 ES ES17710061T patent/ES2831832T3/es active Active
- 2017-02-28 US US16/081,543 patent/US10590079B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018500342A5 (enExample) | ||
| AU2019220632B2 (en) | IRAK degraders and uses thereof | |
| JP2019522051A5 (enExample) | ||
| TWI773730B (zh) | 治療性樹枝狀聚合物 | |
| CN101370497B (zh) | 包含parp抑制剂和细胞毒性剂的联合产品及用途 | |
| US20260027217A1 (en) | Degraders that target alk and therapeutic uses thereof | |
| ES2393900T3 (es) | Compuestos de aril-urea en combinación con otros agentes citostáticos o citotóxicos para tratamiento de cánceres humanos | |
| CN114174303B (zh) | 作为sting激动剂的大环化合物及其方法和用途 | |
| JP2018504379A5 (enExample) | ||
| JP2016505586A5 (enExample) | ||
| JP2009541223A5 (enExample) | ||
| AR045387A1 (es) | Compuestos bencimidazolil n-sustituidos inhibidores de c-kit; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de un trastorno proliferativo | |
| JP2019506403A5 (enExample) | ||
| JP2013534922A5 (enExample) | ||
| JP2018507877A5 (enExample) | ||
| JP2021500055A5 (enExample) | ||
| JP2008001718A5 (enExample) | ||
| JP2013544846A5 (enExample) | ||
| JP2017536344A5 (enExample) | ||
| JP2017526677A5 (enExample) | ||
| JP2009514870A5 (enExample) | ||
| CN101784543A (zh) | 作为细胞坏死抑制剂的吲哚和吲唑化合物 | |
| AR056186A1 (es) | Compuesto de imidazo[1,2-a]piridinilo, su uso para la fabricacion de un medicamento y formulacion farmaceutica que lo comprende | |
| JP2008515959A5 (enExample) | ||
| JP2010530885A5 (enExample) |