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 (OSRAM) | 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)
| Country | Link |
|---|---|
| US (4) | US10758530B2 (OSRAM) |
| EP (2) | EP3848373A1 (OSRAM) |
| JP (2) | JP6912486B2 (OSRAM) |
| KR (1) | KR102746242B1 (OSRAM) |
| CN (2) | CN113620950A (OSRAM) |
| AU (1) | AU2017220738B2 (OSRAM) |
| CA (1) | CA3014395A1 (OSRAM) |
| CO (1) | CO2018008846A2 (OSRAM) |
| DK (1) | DK3416964T3 (OSRAM) |
| ES (1) | ES2858753T3 (OSRAM) |
| IL (1) | IL261170B (OSRAM) |
| MX (1) | MX376974B (OSRAM) |
| PL (1) | PL3416964T3 (OSRAM) |
| PT (1) | PT3416964T (OSRAM) |
| WO (1) | WO2017141116A1 (OSRAM) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201202319D0 (en) | 2012-02-10 | 2012-03-28 | Orbsen Therapeutics Ltd | Stromal stem cells |
| JP6920207B2 (ja) | 2015-03-20 | 2021-08-18 | オルブセン セラピューティクス リミテッド | シンデカン−２のモジュレーターとその使用 |
| US10513524B2 (en) | 2015-07-07 | 2019-12-24 | H. Lundbeck A/S | PDE9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases |
| US11918687B2 (en) | 2016-01-15 | 2024-03-05 | Orbsen Therapeutics Limited | SDC-2 exosome compositions and methods of isolation and use |
| MX376974B (es) | 2016-02-19 | 2025-03-07 | Phoenix Molecular Designs | Derivados de carboxamida útiles como inhibidores de rsk. |
| EP3652305A2 (en) | 2017-07-14 | 2020-05-20 | Orbsen Therapeutics Limited | Cd39 stromal stem cells methods of isolation and use |
| JP2021526134A (ja) | 2018-05-25 | 2021-09-30 | イマラ インク． | ６−［（３Ｓ，４Ｓ）−４−メチル−ｌ−（ピリミジン−２−イルメチル）ピロリジン−３−イル］−３−テトラヒドロピラン−４−イル−７Ｈ−イミダゾ［ｌ，５−Ａ］ピラジン−８−オンの一水和物および結晶形態 |
| 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) |
| AU2022380979A1 (en) | 2021-11-02 | 2024-06-06 | 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 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| 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 |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| 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 |
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 |
| AU4652697A (en) | 1996-10-08 | 1998-05-05 | Eli Lilly And Company | New serotonin 5-ht1f agonists |
| ZA979961B (en) * | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
| ATE227120T1 (de) | 1997-05-07 | 2002-11-15 | Galen Chemicals Ltd | Vorrichtungen zur intravaginalen verabreichung von testosteron und testosteron- vorläuferverbindungen |
| US6093742A (en) | 1997-06-27 | 2000-07-25 | Vertex Pharmaceuticals, Inc. | Inhibitors of p38 |
| EP1495016A2 (en) | 2002-04-09 | 2005-01-12 | 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 |
| NZ587549A (en) * | 2004-06-24 | 2012-10-26 | Vertex Pharma | 6-Amino-indole derivatives and processes for their preparation |
| 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 |
| WO2009036175A2 (en) | 2007-09-14 | 2009-03-19 | 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 |
| US9150577B2 (en) | 2009-12-07 | 2015-10-06 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing an indole core |
| US9073926B2 (en) | 2009-12-07 | 2015-07-07 | 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 |
| JP6437452B2 (ja) * | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| 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 |
| RU2692479C2 (ru) * | 2014-04-07 | 2019-06-25 | Недерлэндс Транслэшинал Рисерч Сентер Б.В. | (5,6-дигидро)пиримидо[4,5-е]индолизины |
| MX376974B (es) | 2016-02-19 | 2025-03-07 | Phoenix Molecular Designs | Derivados de carboxamida útiles como inhibidores de rsk. |
-
2017
- 2017-02-17 MX MX2018010028A patent/MX376974B/es active IP Right Grant
- 2017-02-17 EP EP20211105.0A patent/EP3848373A1/en not_active Withdrawn
- 2017-02-17 DK DK17752742.1T patent/DK3416964T3/da active
- 2017-02-17 US US16/077,029 patent/US10758530B2/en active Active
- 2017-02-17 EP EP17752742.1A patent/EP3416964B1/en active Active
- 2017-02-17 US US15/436,587 patent/US9771366B2/en active Active
- 2017-02-17 JP JP2018543101A patent/JP6912486B2/ja active Active
- 2017-02-17 ES ES17752742T patent/ES2858753T3/es active Active
- 2017-02-17 PL PL17752742T patent/PL3416964T3/pl unknown
- 2017-02-17 CA CA3014395A patent/CA3014395A1/en active Pending
- 2017-02-17 WO PCT/IB2017/000237 patent/WO2017141116A1/en not_active Ceased
- 2017-02-17 PT PT177527421T patent/PT3416964T/pt unknown
- 2017-02-17 AU AU2017220738A patent/AU2017220738B2/en active Active
- 2017-02-17 CN CN202110838177.9A patent/CN113620950A/zh active Pending
- 2017-02-17 CN CN201780024735.XA patent/CN109071542B/zh active Active
- 2017-02-17 KR KR1020187027085A patent/KR102746242B1/ko active Active
- 2017-07-31 US US15/665,181 patent/US10081632B2/en active Active
-
2018
- 2018-08-15 IL IL261170A patent/IL261170B/en unknown
- 2018-08-24 CO CONC2018/0008846A patent/CO2018008846A2/es unknown
-
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