AU2019381808A1 - ERK inhibitors and uses thereof - Google Patents
ERK inhibitors and uses thereof Download PDFInfo
- Publication number
- AU2019381808A1 AU2019381808A1 AU2019381808A AU2019381808A AU2019381808A1 AU 2019381808 A1 AU2019381808 A1 AU 2019381808A1 AU 2019381808 A AU2019381808 A AU 2019381808A AU 2019381808 A AU2019381808 A AU 2019381808A AU 2019381808 A1 AU2019381808 A1 AU 2019381808A1
- Authority
- AU
- Australia
- Prior art keywords
- optionally substituted
- compound
- instance
- heterocyclyl
- 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.)
- Abandoned
Links
- MZRNKOAHWWOPRM-OAQYLSRUSA-N C1N=C(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)N[C@H]1c1ccccc1 Chemical compound C1N=C(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)N[C@H]1c1ccccc1 MZRNKOAHWWOPRM-OAQYLSRUSA-N 0.000 description 1
- NZLLVEXXRVWXKJ-NRFANRHFSA-N C1N=C(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)O[C@@H]1c1ccccc1 Chemical compound C1N=C(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)O[C@@H]1c1ccccc1 NZLLVEXXRVWXKJ-NRFANRHFSA-N 0.000 description 1
- SEBPVFUPPNKZSS-NRFANRHFSA-N C1OC(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)=N[C@@H]1c1ccccc1 Chemical compound C1OC(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)=N[C@@H]1c1ccccc1 SEBPVFUPPNKZSS-NRFANRHFSA-N 0.000 description 1
- SEBPVFUPPNKZSS-OAQYLSRUSA-N C1OC(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)=N[C@H]1c1ccccc1 Chemical compound C1OC(c(nc2)ncc2-c(c2c3)c[nH]c2ncc3N2CCOCC2)=N[C@H]1c1ccccc1 SEBPVFUPPNKZSS-OAQYLSRUSA-N 0.000 description 1
- YDADJLUGZXOHCU-UHFFFAOYSA-N O=C(c(nc1)ncc1-c(c1c2)c[nH]c1ncc2N1CCOCC1)N(CCC1)C1c1ncccc1 Chemical compound O=C(c(nc1)ncc1-c(c1c2)c[nH]c1ncc2N1CCOCC1)N(CCC1)C1c1ncccc1 YDADJLUGZXOHCU-UHFFFAOYSA-N 0.000 description 1
- DRYXPEBRHVACRS-HSZRJFAPSA-N O=C(c(nc1)ncc1-c(c1c2)c[nH]c1ncc2N1CCOCC1)N(CCC1)[C@H]1c1ccccc1 Chemical compound O=C(c(nc1)ncc1-c(c1c2)c[nH]c1ncc2N1CCOCC1)N(CCC1)[C@H]1c1ccccc1 DRYXPEBRHVACRS-HSZRJFAPSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862768565P | 2018-11-16 | 2018-11-16 | |
| US62/768,565 | 2018-11-16 | ||
| US201962908965P | 2019-10-01 | 2019-10-01 | |
| US62/908,965 | 2019-10-01 | ||
| PCT/US2019/061750 WO2020102686A1 (en) | 2018-11-16 | 2019-11-15 | Erk inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2019381808A1 true AU2019381808A1 (en) | 2021-05-27 |
Family
ID=70730924
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2019381808A Abandoned AU2019381808A1 (en) | 2018-11-16 | 2019-11-15 | ERK inhibitors and uses thereof |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US12428416B2 (https=) |
| EP (1) | EP3880677A4 (https=) |
| JP (1) | JP2022507514A (https=) |
| KR (1) | KR20210130701A (https=) |
| CN (1) | CN113423707A (https=) |
| AU (1) | AU2019381808A1 (https=) |
| BR (1) | BR112021009430A2 (https=) |
| CA (1) | CA3119988A1 (https=) |
| IL (1) | IL283106A (https=) |
| MX (1) | MX2021005171A (https=) |
| SG (1) | SG11202104404XA (https=) |
| WO (1) | WO2020102686A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4212531A1 (en) * | 2022-01-14 | 2023-07-19 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ras相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ras抑制劑 |
| 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 |
| WO2026015801A1 (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 |
| WO2026015796A1 (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 |
| 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 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR049333A1 (es) * | 2004-04-02 | 2006-07-19 | Vertex Pharma | Azaindoles inhibidores de proteinquinasas rock y otras proteinas quinasas. composiciones farmaceuticas. |
| ZA200700751B (en) | 2004-06-30 | 2008-08-27 | Vertex Pharma | Azalndoles useful as inhibitors of protein kinases |
| UA95244C2 (ru) * | 2005-06-22 | 2011-07-25 | Плексикон, Инк. | Соединения и способ модулирования активности киназ, и показания для их применения |
| DE102008031517A1 (de) * | 2008-07-03 | 2010-01-07 | Merck Patent Gmbh | Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate |
| ES2402087T3 (es) * | 2008-07-23 | 2013-04-26 | Vertex Pharmaceuticals Incorporated | Inhibidores de la pirazolopiridina quinasa |
| DE102009043260A1 (de) | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
| DE102009060174A1 (de) * | 2009-12-23 | 2011-06-30 | Merck Patent GmbH, 64293 | Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate |
| WO2012094313A1 (en) | 2011-01-04 | 2012-07-12 | Kinentia Biosciences Llc | Pyrazole derivatives as erk inhibitors |
| US9096598B2 (en) | 2011-10-03 | 2015-08-04 | Merck Sharp & Dohme Corp. | Azaindoles as Janus kinase inhibitors |
| MX2015004615A (es) * | 2012-10-16 | 2015-07-17 | Hoffmann La Roche | Inhibidores de serina/treonina cinasa. |
| WO2014109414A1 (ja) | 2013-01-11 | 2014-07-17 | 富士フイルム株式会社 | 含窒素複素環化合物またはその塩 |
| SG11201602572YA (en) * | 2013-10-03 | 2016-04-28 | Kura Oncology Inc | Inhibitors of erk and methods of use |
| WO2016026078A1 (en) * | 2014-08-19 | 2016-02-25 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as erk inhibitors |
| EP3247353A4 (en) * | 2015-01-23 | 2018-07-04 | Confluence Life Sciences, Inc. | Heterocyclic itk inhibitors for treating inflammation and cancer |
| EP3170822A1 (en) | 2015-11-18 | 2017-05-24 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
| CN107973783B (zh) * | 2016-10-21 | 2024-09-06 | 正大天晴药业集团股份有限公司 | 作为erk抑制剂的苯胺嘧啶衍生物 |
| CN108948002A (zh) | 2017-05-19 | 2018-12-07 | 厦门大学 | 五元并六元氮杂芳环类化合物、其制备方法、药用组合物及其应用 |
-
2019
- 2019-11-15 BR BR112021009430-0A patent/BR112021009430A2/pt not_active Application Discontinuation
- 2019-11-15 US US17/294,225 patent/US12428416B2/en active Active
- 2019-11-15 KR KR1020217018334A patent/KR20210130701A/ko not_active Withdrawn
- 2019-11-15 MX MX2021005171A patent/MX2021005171A/es unknown
- 2019-11-15 WO PCT/US2019/061750 patent/WO2020102686A1/en not_active Ceased
- 2019-11-15 CA CA3119988A patent/CA3119988A1/en active Pending
- 2019-11-15 CN CN201980085273.1A patent/CN113423707A/zh active Pending
- 2019-11-15 JP JP2021526509A patent/JP2022507514A/ja active Pending
- 2019-11-15 EP EP19884483.9A patent/EP3880677A4/en not_active Withdrawn
- 2019-11-15 AU AU2019381808A patent/AU2019381808A1/en not_active Abandoned
- 2019-11-15 SG SG11202104404XA patent/SG11202104404XA/en unknown
-
2021
- 2021-05-11 IL IL283106A patent/IL283106A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG11202104404XA (en) | 2021-05-28 |
| BR112021009430A2 (pt) | 2021-08-17 |
| KR20210130701A (ko) | 2021-11-01 |
| WO2020102686A1 (en) | 2020-05-22 |
| US20220002294A1 (en) | 2022-01-06 |
| MX2021005171A (es) | 2021-10-01 |
| EP3880677A1 (en) | 2021-09-22 |
| EP3880677A4 (en) | 2022-06-22 |
| CA3119988A1 (en) | 2020-05-22 |
| IL283106A (en) | 2021-06-30 |
| JP2022507514A (ja) | 2022-01-18 |
| CN113423707A (zh) | 2021-09-21 |
| US12428416B2 (en) | 2025-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK5 | Application lapsed section 142(2)(e) - patent request and compl. specification not accepted |