JP2023010738A5 - - Google Patents
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- JP2023010738A5 JP2023010738A5 JP2022173722A JP2022173722A JP2023010738A5 JP 2023010738 A5 JP2023010738 A5 JP 2023010738A5 JP 2022173722 A JP2022173722 A JP 2022173722A JP 2022173722 A JP2022173722 A JP 2022173722A JP 2023010738 A5 JP2023010738 A5 JP 2023010738A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- formula
- nhc
- optionally substituted
- 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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- 150000001875 compounds Chemical class 0.000 claims 55
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 27
- 238000000034 method Methods 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000002947 alkylene group Chemical group 0.000 claims 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
- 239000003054 catalyst Substances 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 229910052763 palladium Inorganic materials 0.000 claims 6
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 claims 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- CYPYTURSJDMMMP-WVCUSYJESA-N (1e,4e)-1,5-diphenylpenta-1,4-dien-3-one;palladium Chemical compound [Pd].[Pd].C=1C=CC=CC=1\C=C\C(=O)\C=C\C1=CC=CC=C1.C=1C=CC=CC=1\C=C\C(=O)\C=C\C1=CC=CC=C1.C=1C=CC=CC=1\C=C\C(=O)\C=C\C1=CC=CC=C1 CYPYTURSJDMMMP-WVCUSYJESA-N 0.000 claims 3
- 101100030361 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) pph-3 gene Proteins 0.000 claims 3
- 125000005620 boronic acid group Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 claims 3
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 2
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims 2
- 235000019270 ammonium chloride Nutrition 0.000 claims 2
- -1 branched C3-C8 alkyl Chemical group 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 229910052740 iodine Inorganic materials 0.000 claims 2
- 239000011630 iodine Substances 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 239000003586 protic polar solvent Substances 0.000 claims 2
- 229910052725 zinc Inorganic materials 0.000 claims 2
- 239000011592 zinc chloride Substances 0.000 claims 2
- 235000005074 zinc chloride Nutrition 0.000 claims 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical class OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- FJBFPHVGVWTDIP-UHFFFAOYSA-N dibromomethane Chemical compound BrCBr FJBFPHVGVWTDIP-UHFFFAOYSA-N 0.000 claims 1
- NZZFYRREKKOMAT-UHFFFAOYSA-N diiodomethane Chemical compound ICI NZZFYRREKKOMAT-UHFFFAOYSA-N 0.000 claims 1
- IOGXOCVLYRDXLW-UHFFFAOYSA-N tert-butyl nitrite Chemical compound CC(C)(C)ON=O IOGXOCVLYRDXLW-UHFFFAOYSA-N 0.000 claims 1
- 239000012414 tert-butyl nitrite Substances 0.000 claims 1
- JRMUNVKIHCOMHV-UHFFFAOYSA-M tetrabutylammonium bromide Chemical compound [Br-].CCCC[N+](CCCC)(CCCC)CCCC JRMUNVKIHCOMHV-UHFFFAOYSA-M 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024071962A JP2024105360A (ja) | 2013-03-15 | 2024-04-25 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361792812P | 2013-03-15 | 2013-03-15 | |
| US61/792,812 | 2013-03-15 | ||
| JP2019032014A JP6936823B2 (ja) | 2013-03-15 | 2019-02-25 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2021138625A JP7169412B2 (ja) | 2013-03-15 | 2021-08-27 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021138625A Division JP7169412B2 (ja) | 2013-03-15 | 2021-08-27 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024071962A Division JP2024105360A (ja) | 2013-03-15 | 2024-04-25 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023010738A JP2023010738A (ja) | 2023-01-20 |
| JP2023010738A5 true JP2023010738A5 (https=) | 2023-08-07 |
| JP7536064B2 JP7536064B2 (ja) | 2024-08-19 |
Family
ID=51529950
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503185A Active JP6165314B2 (ja) | 2013-03-15 | 2014-03-14 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2017120849A Pending JP2017193567A (ja) | 2013-03-15 | 2017-06-20 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2019032014A Active JP6936823B2 (ja) | 2013-03-15 | 2019-02-25 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2021138625A Active JP7169412B2 (ja) | 2013-03-15 | 2021-08-27 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
| JP2022173722A Active JP7536064B2 (ja) | 2013-03-15 | 2022-10-28 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
| JP2024071962A Pending JP2024105360A (ja) | 2013-03-15 | 2024-04-25 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Family Applications Before (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503185A Active JP6165314B2 (ja) | 2013-03-15 | 2014-03-14 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2017120849A Pending JP2017193567A (ja) | 2013-03-15 | 2017-06-20 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2019032014A Active JP6936823B2 (ja) | 2013-03-15 | 2019-02-25 | 抗癌活性及び抗増殖活性を呈する２−アミノピリミジン−６−オン及び類似体 |
| JP2021138625A Active JP7169412B2 (ja) | 2013-03-15 | 2021-08-27 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024071962A Pending JP2024105360A (ja) | 2013-03-15 | 2024-04-25 | 抗癌活性及び抗増殖活性を呈する２－アミノピリミジン－６－オン及び類似体 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US9181223B2 (https=) |
| EP (1) | EP2968286B1 (https=) |
| JP (6) | JP6165314B2 (https=) |
| KR (5) | KR20260042557A (https=) |
| CN (2) | CN105120864B (https=) |
| AU (5) | AU2014233411B2 (https=) |
| BR (1) | BR112015022288B1 (https=) |
| CA (1) | CA2903285C (https=) |
| DK (1) | DK2968286T3 (https=) |
| ES (1) | ES2651165T3 (https=) |
| FR (1) | FR26C1012I1 (https=) |
| IL (4) | IL241000B (https=) |
| MX (1) | MX365574B (https=) |
| NL (1) | NL301373I2 (https=) |
| PH (1) | PH12015502114B1 (https=) |
| PT (1) | PT2968286T (https=) |
| RU (1) | RU2015143717A (https=) |
| SG (1) | SG11201507660TA (https=) |
| WO (1) | WO2014145025A2 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| DK2968286T3 (en) * | 2013-03-15 | 2018-01-02 | Deciphera Pharmaceuticals Llc | 2-AMINOPYRIMIDIN-6-ONES AND ANALOGS THAT HAVE ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES |
| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| EP3632906B1 (en) * | 2017-05-24 | 2023-12-13 | Abbisko Therapeutics Co., Ltd. | Azaaryl derivative, preparation method therefor, and application thereof for use in pharmacy |
| JP7131837B2 (ja) * | 2017-06-19 | 2022-09-06 | アビスコ セラピューティクス カンパニー リミテッド | Ｃｓｆ－１ｒ阻害活性を有するアザアリール誘導体、その製造方法および応用 |
| CN118416236A (zh) | 2018-01-31 | 2024-08-02 | 德西费拉制药有限责任公司 | 治疗胃肠道间质瘤的组合疗法 |
| IL276398B2 (en) | 2018-01-31 | 2026-03-01 | Deciphera Pharmaceuticals Llc | Combination therapy for mastocytosis |
| CN110845476B (zh) * | 2018-08-21 | 2022-11-18 | 上海和誉生物医药科技有限公司 | 一种高选择性csf1r抑制剂、其制备方法和在药学上的应用 |
| BR112021012812A2 (pt) | 2018-12-28 | 2021-12-07 | Deciphera Pharmaceuticals Llc | Csf1r inhibitors para uso e tratamento de câncer |
| WO2020185812A1 (en) | 2019-03-11 | 2020-09-17 | Teva Pharmaceuticals International Gmbh | Solid state forms of ripretinib |
| US11518758B2 (en) | 2019-05-10 | 2022-12-06 | Deciphera Pharmaceuticals, Llc | Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| PE20220597A1 (es) | 2019-05-10 | 2022-04-22 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos |
| PE20221083A1 (es) | 2019-06-17 | 2022-07-05 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| EP4013412B1 (en) | 2019-08-12 | 2026-01-28 | Deciphera Pharmaceuticals, LLC | Ripretinib for treating gastrointestinal stromal tumors |
| MX2022008103A (es) | 2019-12-30 | 2022-09-19 | Deciphera Pharmaceuticals Llc | Formulaciones de inhibidores de la cinasa amorfa y metodos de estas. |
| EP4084779B1 (en) | 2019-12-30 | 2024-10-09 | Deciphera Pharmaceuticals, LLC | Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea |
| IL302807A (en) | 2020-11-18 | 2023-07-01 | Deciphera Pharmaceuticals Llc | Gcn2 and perk kinase inhibitors and methods of use thereof |
| CN115385896B (zh) * | 2021-05-24 | 2024-11-15 | 上海和誉生物医药科技有限公司 | 一种csf-1r抑制剂中间体或其酸式盐的制备方法 |
| CN113880812A (zh) * | 2021-11-17 | 2022-01-04 | 上海皓元生物医药科技有限公司 | 一种csf-ir抑制剂的制备方法 |
| PE20250609A1 (es) | 2021-12-03 | 2025-02-26 | Deciphera Pharmaceuticals Llc | Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos |
| CA3240263A1 (en) | 2021-12-09 | 2023-06-15 | Daniel L. Flynn | Raf kinase inhibitors and methods of use thereof |
| WO2023125812A1 (zh) * | 2021-12-31 | 2023-07-06 | 上海海雁医药科技有限公司 | 取代的嘧啶酮衍生物、其药物组合物及医药上的用途 |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
| CN117624132B (zh) * | 2023-11-28 | 2026-04-21 | 上海相辉医药科技有限公司 | 一种CSF-1R激酶抑制剂Vimseltinib(DCC-3014)的制备方法 |
| WO2025122952A1 (en) * | 2023-12-08 | 2025-06-12 | Deciphera Pharmaceuticals, Llc | Formulations of vimseltinib |
| US20250206720A1 (en) * | 2023-12-08 | 2025-06-26 | Deciphera Pharmaceuticals, Llc | Solid forms of an ulk inhibitor |
| WO2025231106A1 (en) * | 2024-05-01 | 2025-11-06 | Deciphera Pharmaceuticals, Llc | Csf-1r inhibitors and methods of use thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008046216A1 (en) * | 2006-10-18 | 2008-04-24 | Methylgene, Inc. | Kinase inhibitors and uses thereof |
| AU2007338792B2 (en) * | 2006-12-20 | 2012-05-31 | Amgen Inc. | Substituted heterocycles and methods of use |
| JP5444365B2 (ja) * | 2008-10-29 | 2014-03-19 | デシフェラ ファーマシューティカルズ，エルエルシー | 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質 |
| WO2014145023A1 (en) * | 2013-03-15 | 2014-09-18 | Deciphera Pharmaceuticals, Llc | 1,2,4-triazol-5-ones and analogs exhibiting anti-cancer and anti-proliferative activities |
| DK2968286T3 (en) * | 2013-03-15 | 2018-01-02 | Deciphera Pharmaceuticals Llc | 2-AMINOPYRIMIDIN-6-ONES AND ANALOGS THAT HAVE ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES |
| WO2014145015A2 (en) * | 2013-03-15 | 2014-09-18 | Deciphera Pharmaceuticals, Llc | Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities |
-
2014
- 2014-03-14 DK DK14764032.0T patent/DK2968286T3/en active
- 2014-03-14 KR KR1020267005630A patent/KR20260042557A/ko active Pending
- 2014-03-14 WO PCT/US2014/029661 patent/WO2014145025A2/en not_active Ceased
- 2014-03-14 KR KR1020217026183A patent/KR102399891B1/ko active Active
- 2014-03-14 KR KR1020247001621A patent/KR20240013846A/ko not_active Ceased
- 2014-03-14 PT PT147640320T patent/PT2968286T/pt unknown
- 2014-03-14 CN CN201480021743.5A patent/CN105120864B/zh active Active
- 2014-03-14 CN CN201710265111.9A patent/CN107311981B/zh active Active
- 2014-03-14 RU RU2015143717A patent/RU2015143717A/ru not_active Application Discontinuation
- 2014-03-14 KR KR1020157029134A patent/KR102293086B1/ko active Active
- 2014-03-14 SG SG11201507660TA patent/SG11201507660TA/en unknown
- 2014-03-14 BR BR112015022288-9A patent/BR112015022288B1/pt active IP Right Grant
- 2014-03-14 EP EP14764032.0A patent/EP2968286B1/en active Active
- 2014-03-14 KR KR1020227016381A patent/KR102628583B1/ko active Active
- 2014-03-14 MX MX2015012736A patent/MX365574B/es active IP Right Grant
- 2014-03-14 AU AU2014233411A patent/AU2014233411B2/en active Active
- 2014-03-14 JP JP2016503185A patent/JP6165314B2/ja active Active
- 2014-03-14 ES ES14764032.0T patent/ES2651165T3/es active Active
- 2014-03-14 CA CA2903285A patent/CA2903285C/en active Active
- 2014-03-14 US US14/214,171 patent/US9181223B2/en active Active
-
2015
- 2015-09-01 IL IL241000A patent/IL241000B/en active IP Right Grant
- 2015-09-14 PH PH12015502114A patent/PH12015502114B1/en unknown
-
2017
- 2017-06-20 JP JP2017120849A patent/JP2017193567A/ja active Pending
-
2018
- 2018-07-09 IL IL260502A patent/IL260502B/en active IP Right Grant
- 2018-11-28 AU AU2018271293A patent/AU2018271293B2/en active Active
-
2019
- 2019-02-25 JP JP2019032014A patent/JP6936823B2/ja active Active
-
2020
- 2020-06-16 IL IL275422A patent/IL275422B/en unknown
- 2020-07-15 AU AU2020205294A patent/AU2020205294B2/en active Active
-
2021
- 2021-08-27 JP JP2021138625A patent/JP7169412B2/ja active Active
-
2022
- 2022-01-04 IL IL289629A patent/IL289629B2/en unknown
- 2022-06-15 AU AU2022204166A patent/AU2022204166C1/en active Active
- 2022-10-28 JP JP2022173722A patent/JP7536064B2/ja active Active
-
2024
- 2024-04-02 AU AU2024202088A patent/AU2024202088A1/en active Pending
- 2024-04-25 JP JP2024071962A patent/JP2024105360A/ja active Pending
-
2026
- 2026-03-15 FR FR26C1012C patent/FR26C1012I1/fr active Active
- 2026-03-16 NL NL301373C patent/NL301373I2/nl unknown
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