JP2016531952A5 - - Google Patents
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- Publication number
- JP2016531952A5 JP2016531952A5 JP2016546894A JP2016546894A JP2016531952A5 JP 2016531952 A5 JP2016531952 A5 JP 2016531952A5 JP 2016546894 A JP2016546894 A JP 2016546894A JP 2016546894 A JP2016546894 A JP 2016546894A JP 2016531952 A5 JP2016531952 A5 JP 2016531952A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- heterocyclyl
- cycloalkyl
- hetaryl
- alkyl
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 98
- 125000001072 heteroaryl group Chemical group 0.000 claims description 95
- 125000000623 heterocyclic group Chemical group 0.000 claims description 90
- 125000003118 aryl group Chemical group 0.000 claims description 89
- 239000000651 prodrug Substances 0.000 claims description 58
- 229940002612 prodrug Drugs 0.000 claims description 58
- 150000003839 salts Chemical class 0.000 claims description 58
- 125000000217 alkyl group Chemical group 0.000 claims description 52
- 125000000304 alkynyl group Chemical group 0.000 claims description 47
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 239000001257 hydrogen Substances 0.000 claims description 17
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 125000003342 alkenyl group Chemical group 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 102000001253 Protein Kinase Human genes 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 108060006633 protein kinase Proteins 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 125000005842 heteroatom Chemical group 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 201000010208 Seminoma Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 description 21
- 238000000034 method Methods 0.000 description 13
- 229910052757 nitrogen Inorganic materials 0.000 description 11
- 229910052760 oxygen Inorganic materials 0.000 description 8
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 description 6
- 108010007457 Extracellular Signal-Regulated MAP Kinases Proteins 0.000 description 5
- 229910052799 carbon Inorganic materials 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 208000035475 disorder Diseases 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 3
- 208000020084 Bone disease Diseases 0.000 description 1
- 101000876610 Dictyostelium discoideum Extracellular signal-regulated kinase 2 Proteins 0.000 description 1
- 101001052493 Homo sapiens Mitogen-activated protein kinase 1 Proteins 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 238000010162 Tukey test Methods 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 208000026278 immune system disease Diseases 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361886552P | 2013-10-03 | 2013-10-03 | |
| US61/886,552 | 2013-10-03 | ||
| US201462032446P | 2014-08-01 | 2014-08-01 | |
| US62/032,446 | 2014-08-01 | ||
| PCT/US2014/059197 WO2015051341A1 (en) | 2013-10-03 | 2014-10-03 | Inhibitors of erk and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018201905A Division JP2019031549A (ja) | 2013-10-03 | 2018-10-26 | Ｅｒｋの阻害剤および使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016531952A JP2016531952A (ja) | 2016-10-13 |
| JP2016531952A5 true JP2016531952A5 (https=) | 2017-11-09 |
| JP6427197B2 JP6427197B2 (ja) | 2018-11-21 |
Family
ID=52779215
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546894A Expired - Fee Related JP6427197B2 (ja) | 2013-10-03 | 2014-10-03 | Ｅｒｋの阻害剤および使用方法 |
| JP2018201905A Pending JP2019031549A (ja) | 2013-10-03 | 2018-10-26 | Ｅｒｋの阻害剤および使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018201905A Pending JP2019031549A (ja) | 2013-10-03 | 2018-10-26 | Ｅｒｋの阻害剤および使用方法 |
Country Status (28)
| Country | Link |
|---|---|
| US (4) | US9624228B2 (https=) |
| EP (2) | EP3363800A1 (https=) |
| JP (2) | JP6427197B2 (https=) |
| KR (1) | KR20160081908A (https=) |
| CN (2) | CN105636586B (https=) |
| AU (2) | AU2014331628B2 (https=) |
| BR (1) | BR112016006994A8 (https=) |
| CA (1) | CA2924584A1 (https=) |
| CY (1) | CY1120095T1 (https=) |
| DK (1) | DK3052096T3 (https=) |
| EA (1) | EA032196B1 (https=) |
| ES (1) | ES2664794T3 (https=) |
| HK (1) | HK1255851A1 (https=) |
| HR (1) | HRP20180538T1 (https=) |
| HU (1) | HUE036600T2 (https=) |
| IL (1) | IL244488A0 (https=) |
| LT (1) | LT3052096T (https=) |
| ME (1) | ME02991B (https=) |
| MX (1) | MX2016004163A (https=) |
| PH (1) | PH12016500432A1 (https=) |
| PL (1) | PL3052096T3 (https=) |
| PT (1) | PT3052096T (https=) |
| RS (1) | RS57058B1 (https=) |
| SG (1) | SG11201602572YA (https=) |
| SI (1) | SI3052096T1 (https=) |
| SM (1) | SMT201800205T1 (https=) |
| WO (1) | WO2015051341A1 (https=) |
| ZA (1) | ZA201601701B (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3363800A1 (en) | 2013-10-03 | 2018-08-22 | Kura Oncology, Inc. | Heterocyclic inhibitors of erk and methods of use |
| TW201805000A (zh) * | 2016-06-20 | 2018-02-16 | 庫拉腫瘤技術股份有限公司 | 利用erk抑制劑之鱗狀細胞癌之治療 |
| CN110506038B (zh) | 2017-03-28 | 2023-11-24 | 巴斯夫欧洲公司 | 杀害虫化合物 |
| WO2018183762A1 (en) | 2017-03-29 | 2018-10-04 | United States Government As Represented By The Department Of Veterans Affairs | Methods and compositions for treating cancer |
| US20200247815A1 (en) * | 2017-10-19 | 2020-08-06 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Pyrazolyl-containing tricyclic derivative, preparation method therefor and use thereof |
| CN109761986B (zh) * | 2017-11-10 | 2021-10-08 | 上海翰森生物医药科技有限公司 | 三并环类衍生物抑制剂、其制备方法和应用 |
| CN107879989B (zh) * | 2017-11-29 | 2020-01-03 | 重庆市中药研究院 | 具有生物活性的3,4,5-取代苯并二氮卓2-酮类药物分子及其制备方法 |
| EP3643705A1 (en) | 2018-10-24 | 2020-04-29 | Basf Se | Pesticidal compounds |
| MX2021005171A (es) | 2018-11-16 | 2021-10-01 | California Inst Of Techn | Inhibidores de cinasas reguladas por señal extracelular (erk) y usos de los mismos. |
| CN112020357B (zh) * | 2019-04-02 | 2023-08-29 | 上海翰森生物医药科技有限公司 | 含吲唑基的三并环类衍生物的盐及其晶型 |
| EP3766879A1 (en) | 2019-07-19 | 2021-01-20 | Basf Se | Pesticidal pyrazole derivatives |
| WO2022075445A1 (ja) * | 2020-10-08 | 2022-04-14 | 株式会社Adeka | ポリオレフィン系樹脂組成物、それを用いた成形品、及びポリオレフィン系樹脂組成物の製造方法 |
| EP4198023A1 (en) | 2021-12-16 | 2023-06-21 | Basf Se | Pesticidally active thiosemicarbazone compounds |
| US20250197358A1 (en) | 2022-02-17 | 2025-06-19 | Basf Se | Pesticidally active thiosemicarbazone compounds |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024240859A1 (en) | 2023-05-25 | 2024-11-28 | Basf Se | Lactam pesticidal compounds |
| EP4467535A1 (en) | 2023-05-25 | 2024-11-27 | Basf Se | Lactam pesticidal compounds |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| TW202529768A (zh) | 2023-09-29 | 2025-08-01 | 大陸商德昇濟醫藥（無錫）有限公司 | 癌症治療的療法 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | 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 |
| 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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| 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 |
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| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
-
2014
- 2014-10-03 EP EP17204999.1A patent/EP3363800A1/en not_active Withdrawn
- 2014-10-03 KR KR1020167011270A patent/KR20160081908A/ko not_active Ceased
- 2014-10-03 MX MX2016004163A patent/MX2016004163A/es unknown
- 2014-10-03 SG SG11201602572YA patent/SG11201602572YA/en unknown
- 2014-10-03 EP EP14850964.9A patent/EP3052096B8/en active Active
- 2014-10-03 WO PCT/US2014/059197 patent/WO2015051341A1/en not_active Ceased
- 2014-10-03 CA CA2924584A patent/CA2924584A1/en not_active Abandoned
- 2014-10-03 RS RS20180373A patent/RS57058B1/sr unknown
- 2014-10-03 US US15/026,581 patent/US9624228B2/en not_active Expired - Fee Related
- 2014-10-03 ES ES14850964.9T patent/ES2664794T3/es active Active
- 2014-10-03 CN CN201480054909.3A patent/CN105636586B/zh not_active Expired - Fee Related
- 2014-10-03 HU HUE14850964A patent/HUE036600T2/hu unknown
- 2014-10-03 CN CN201810401122.XA patent/CN108864102A/zh active Pending
- 2014-10-03 EA EA201690708A patent/EA032196B1/ru not_active IP Right Cessation
- 2014-10-03 ME MEP-2018-90A patent/ME02991B/me unknown
- 2014-10-03 HR HRP20180538TT patent/HRP20180538T1/hr unknown
- 2014-10-03 PT PT148509649T patent/PT3052096T/pt unknown
- 2014-10-03 SM SM20180205T patent/SMT201800205T1/it unknown
- 2014-10-03 JP JP2016546894A patent/JP6427197B2/ja not_active Expired - Fee Related
- 2014-10-03 AU AU2014331628A patent/AU2014331628B2/en not_active Ceased
- 2014-10-03 BR BR112016006994A patent/BR112016006994A8/pt not_active Application Discontinuation
- 2014-10-03 SI SI201430659T patent/SI3052096T1/en unknown
- 2014-10-03 DK DK14850964.9T patent/DK3052096T3/en active
- 2014-10-03 PL PL14850964T patent/PL3052096T3/pl unknown
- 2014-10-03 LT LTEP14850964.9T patent/LT3052096T/lt unknown
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2016
- 2016-03-07 PH PH12016500432A patent/PH12016500432A1/en unknown
- 2016-03-08 IL IL244488A patent/IL244488A0/en unknown
- 2016-03-11 ZA ZA2016/01701A patent/ZA201601701B/en unknown
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2017
- 2017-02-22 US US15/439,719 patent/US9951078B2/en not_active Expired - Fee Related
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2018
- 2018-02-14 US US15/896,929 patent/US10301317B2/en not_active Expired - Fee Related
- 2018-03-27 CY CY20181100340T patent/CY1120095T1/el unknown
- 2018-10-18 AU AU2018250439A patent/AU2018250439A1/en not_active Abandoned
- 2018-10-26 JP JP2018201905A patent/JP2019031549A/ja active Pending
- 2018-11-22 HK HK18114927.9A patent/HK1255851A1/en unknown
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2019
- 2019-03-29 US US16/370,718 patent/US20190292194A1/en not_active Abandoned
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