JP2019505541A5 - - Google Patents
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- Publication number
- JP2019505541A5 JP2019505541A5 JP2018543101A JP2018543101A JP2019505541A5 JP 2019505541 A5 JP2019505541 A5 JP 2019505541A5 JP 2018543101 A JP2018543101 A JP 2018543101A JP 2018543101 A JP2018543101 A JP 2018543101A JP 2019505541 A5 JP2019505541 A5 JP 2019505541A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- alkyl
- pharmaceutically acceptable
- solvate
- compound
- 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 14
- 239000012453 solvate Substances 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 3
- -1 1- (4-aminobenzyl) -1H-pyrazol-4-yl Chemical group 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- FXZXQVHCNBZISN-CQSZACIVSA-N (13R)-N-[1-[[4-(aminomethyl)phenyl]methyl]pyrazol-4-yl]-13-methyl-10-oxo-1,3,11-triazatricyclo[7.4.0.02,7]trideca-2(7),3,5,8-tetraene-4-carboxamide Chemical compound NCC1=CC=C(CN2N=CC(=C2)NC(=O)C=2C=CC=3C=C4N([C@@H](CNC4=O)C)C=3N=2)C=C1 FXZXQVHCNBZISN-CQSZACIVSA-N 0.000 claims 1
- KEDIARBEFYPUKX-PFEQFJNWSA-N (13R)-N-[1-[[4-(aminomethyl)phenyl]methyl]pyrazol-4-yl]-13-methyl-10-oxo-1,3,11-triazatricyclo[7.4.0.02,7]trideca-2(7),3,5,8-tetraene-4-carboxamide hydrochloride Chemical compound Cl.C[C@@H]1CNC(=O)c2cc3ccc(nc3n12)C(=O)Nc1cnn(Cc2ccc(CN)cc2)c1 KEDIARBEFYPUKX-PFEQFJNWSA-N 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- DZTKXKYLNSLJPQ-UHFFFAOYSA-N 1H-pyrrolo[1,2-a]pyrazine-2-carboxamide Chemical compound C1C=2N(C=CN1C(=O)N)C=CC=2 DZTKXKYLNSLJPQ-UHFFFAOYSA-N 0.000 claims 1
- XZZQXWUGYNFMJB-UHFFFAOYSA-N 1H-pyrrolo[1,2-a]pyrazine-2-carboxamide hydrochloride Chemical compound Cl.C1C=2N(C=CN1C(=O)N)C=CC2 XZZQXWUGYNFMJB-UHFFFAOYSA-N 0.000 claims 1
- 102000019050 90-kDa Ribosomal Protein S6 Kinases Human genes 0.000 claims 1
- 108010012196 90-kDa Ribosomal Protein S6 Kinases Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021112227A JP7289876B2 (ja) | 2016-02-19 | 2021-07-06 | Ｒｓｋ阻害剤として有用なカルボキサミド誘導体 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662297522P | 2016-02-19 | 2016-02-19 | |
| US62/297,522 | 2016-02-19 | ||
| PCT/IB2017/000237 WO2017141116A1 (en) | 2016-02-19 | 2017-02-17 | Carboxamide derivatives useful as rsk inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021112227A Division JP7289876B2 (ja) | 2016-02-19 | 2021-07-06 | Ｒｓｋ阻害剤として有用なカルボキサミド誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019505541A JP2019505541A (ja) | 2019-02-28 |
| JP2019505541A5 true JP2019505541A5 (cg-RX-API-DMAC10.html) | 2020-03-26 |
| JP6912486B2 JP6912486B2 (ja) | 2021-08-04 |
Family
ID=59625645
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018543101A Active JP6912486B2 (ja) | 2016-02-19 | 2017-02-17 | Ｒｓｋ阻害剤として有用なカルボキサミド誘導体 |
| JP2021112227A Active JP7289876B2 (ja) | 2016-02-19 | 2021-07-06 | Ｒｓｋ阻害剤として有用なカルボキサミド誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021112227A Active JP7289876B2 (ja) | 2016-02-19 | 2021-07-06 | Ｒｓｋ阻害剤として有用なカルボキサミド誘導体 |
Country Status (15)
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201202319D0 (en) | 2012-02-10 | 2012-03-28 | Orbsen Therapeutics Ltd | Stromal stem cells |
| US10124038B2 (en) | 2015-03-20 | 2018-11-13 | Orbsen Therapeutics Limited | Modulators of syndecan-2 and uses thereof |
| ES2971969T3 (es) | 2015-07-07 | 2024-06-10 | H Lundbeck As | Inhibidores de PDE9 con cadena principal de imidazopirazinona para el tratamiento de enfermedades periféricas |
| WO2017122095A1 (en) | 2016-01-15 | 2017-07-20 | Orbsen Therapeutics Limited | Sdc-2 exosome compositions and methods of isolation and use |
| ES2858753T3 (es) * | 2016-02-19 | 2021-09-30 | Phoenix Molecular Designs | Derivados de 6-oxo-N-(1-(bencil)-1H-pirazol-4-il)-6,7,8,9-tetrahidropirido[3',2':4,5]pirrolo[1,2-a]pirazin-2-carboxamida como inhibidores de cinasa S6 ribosómica (RSK) p90 para el tratamiento del cáncer |
| EP3652305A2 (en) | 2017-07-14 | 2020-05-20 | Orbsen Therapeutics Limited | Cd39 stromal stem cells methods of isolation and use |
| MA52792A (fr) | 2018-05-25 | 2021-04-14 | Imara Inc | Formes cristallines et monohydrate de 6- [(3s,4s)-4-méthyl-1-(pyrimidin-2-ylméthyl) pyrrolidin-3-yl]-3-tétrahydropyran-4-yl-7h-imidazo [1,5-a] pyrazin-8-one |
| KR20250108770A (ko) | 2018-08-31 | 2025-07-15 | 카듀리온 파마슈티칼스, 인크. | 겸상 세포 질환의 치료를 위한 pde9 억제제 |
| CN109847063B (zh) * | 2018-12-26 | 2023-02-28 | 南方医科大学皮肤病医院（广东省皮肤病医院、广东省皮肤性病防治中心、中国麻风防治研究中心） | Rsk信号通路抑制剂在抑制沙眼衣原体感染中的应用 |
| CN109438403A (zh) * | 2018-12-28 | 2019-03-08 | 凯瑞斯德生化(苏州)有限公司 | 一种5-氨基苯并呋喃-2-甲酸乙酯的制备方法 |
| US12378245B2 (en) | 2019-02-11 | 2025-08-05 | Phoenix Molecular Designs | Crystalline forms of an RSK inhibitor |
| WO2022251597A1 (en) * | 2021-05-28 | 2022-12-01 | Verge Analytics, Inc. | Methods of treating neurological disorders with modulators of ribosomal protein s6 kinase alpha-1 (rsk1) and ribosomal protein s6 kinase alpha-3 (rsk2) |
| CA3237199A1 (en) | 2021-11-02 | 2023-05-11 | Flare Therapeutics Inc. | Pparg inverse agonists and uses thereof |
| WO2023236960A1 (zh) * | 2022-06-07 | 2023-12-14 | 上海科恩泰生物医药科技有限公司 | 一种具有rsk抑制作用的羧酰胺衍生物、包含其的药物组合物及其用途 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
| WO2025255438A1 (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 |
| WO2026015790A1 (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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5792763A (en) | 1996-10-08 | 1998-08-11 | Eli Lilly And Company | Serotonin 5-HT1F agonists |
| ZA979961B (en) * | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
| JP2001524124A (ja) | 1997-05-07 | 2001-11-27 | ガレン（ケミカルズ）リミティド | テストステロンおよびテストステロン前駆体の投与のための膣内薬物送達用具 |
| US6093742A (en) | 1997-06-27 | 2000-07-25 | Vertex Pharmaceuticals, Inc. | Inhibitors of p38 |
| AU2003224257A1 (en) * | 2002-04-09 | 2003-10-27 | Astex Technology Limited | Heterocyclic compounds and their use as modulators of p38 map kinase |
| US20050032869A1 (en) * | 2003-07-08 | 2005-02-10 | Pharmacia Italia S.P.A. | Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| CN104788328B (zh) * | 2004-06-24 | 2017-09-12 | 沃泰克斯药物股份有限公司 | Atp‑结合弹夹转运蛋白的调控剂 |
| US7790712B2 (en) | 2005-03-17 | 2010-09-07 | Boehringer Ingelheim Pharmaceutical, Inc. | Substituted [1,4]diazepino[1,2-A]indoles and azepino[1,2-A]indoles as anti-cytokine inhibitors |
| FR2884516B1 (fr) | 2005-04-15 | 2007-06-22 | Cerep Sa | Antagonistes npy, preparation et utilisations |
| US8765802B2 (en) * | 2007-06-12 | 2014-07-01 | Provid Pharmaceuticals, Inc. | Kinase inhibitors, compositions thereof, and methods of use therewith |
| AU2008298870C1 (en) | 2007-09-14 | 2014-10-09 | The Regents Of The University Of Michigan | F1F0-ATPase inhibitors and related methods |
| GB0718870D0 (en) | 2007-09-27 | 2007-11-07 | Univ Dundee | Modulation of RSK |
| JP2013512952A (ja) | 2009-12-07 | 2013-04-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | インドールコアを含有する複素環化合物 |
| WO2011071725A1 (en) * | 2009-12-07 | 2011-06-16 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core |
| WO2013181742A1 (en) | 2012-06-04 | 2013-12-12 | Phoenix Molecular Diagnostics Ltd. | Methods of inhibiting rsk for treatment of breast cancer |
| ES2649156T3 (es) * | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| CN103724251B (zh) * | 2014-01-18 | 2015-07-22 | 福州大学 | 一种靶向stat3的小分子化合物及其制备方法和应用 |
| MX368767B (es) | 2014-04-07 | 2019-10-15 | Netherlands Translational Res Center B V | (5,6-dihidro)pirimido[4,5-e]indolizinas. |
| ES2858753T3 (es) | 2016-02-19 | 2021-09-30 | Phoenix Molecular Designs | Derivados de 6-oxo-N-(1-(bencil)-1H-pirazol-4-il)-6,7,8,9-tetrahidropirido[3',2':4,5]pirrolo[1,2-a]pirazin-2-carboxamida como inhibidores de cinasa S6 ribosómica (RSK) p90 para el tratamiento del cáncer |
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2017
- 2017-02-17 ES ES17752742T patent/ES2858753T3/es active Active
- 2017-02-17 EP EP17752742.1A patent/EP3416964B1/en active Active
- 2017-02-17 DK DK17752742.1T patent/DK3416964T3/da active
- 2017-02-17 MX MX2018010028A patent/MX376974B/es active IP Right Grant
- 2017-02-17 PL PL17752742T patent/PL3416964T3/pl unknown
- 2017-02-17 US US15/436,587 patent/US9771366B2/en active Active
- 2017-02-17 EP EP20211105.0A patent/EP3848373A1/en not_active Withdrawn
- 2017-02-17 AU AU2017220738A patent/AU2017220738B2/en active Active
- 2017-02-17 CN CN201780024735.XA patent/CN109071542B/zh active Active
- 2017-02-17 PT PT177527421T patent/PT3416964T/pt unknown
- 2017-02-17 JP JP2018543101A patent/JP6912486B2/ja active Active
- 2017-02-17 WO PCT/IB2017/000237 patent/WO2017141116A1/en not_active Ceased
- 2017-02-17 CA CA3014395A patent/CA3014395A1/en active Pending
- 2017-02-17 US US16/077,029 patent/US10758530B2/en active Active
- 2017-02-17 CN CN202110838177.9A patent/CN113620950A/zh active Pending
- 2017-02-17 KR KR1020187027085A patent/KR102746242B1/ko active Active
- 2017-07-31 US US15/665,181 patent/US10081632B2/en active Active
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2018
- 2018-08-15 IL IL261170A patent/IL261170B/en unknown
- 2018-08-24 CO CONC2018/0008846A patent/CO2018008846A2/es unknown
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2020
- 2020-06-30 US US16/917,595 patent/US20210186961A1/en not_active Abandoned
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2021
- 2021-07-06 JP JP2021112227A patent/JP7289876B2/ja active Active