TWI904906B - Sarm1之抑制劑 - Google Patents
Sarm1之抑制劑Info
- Publication number
- TWI904906B TWI904906B TW113140249A TW113140249A TWI904906B TW I904906 B TWI904906 B TW I904906B TW 113140249 A TW113140249 A TW 113140249A TW 113140249 A TW113140249 A TW 113140249A TW I904906 B TWI904906 B TW I904906B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- dissolved
- substituted
- mmol
- methanol
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Immunology (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063069408P | 2020-08-24 | 2020-08-24 | |
| US63/069,408 | 2020-08-24 | ||
| US202163142398P | 2021-01-27 | 2021-01-27 | |
| US63/142,398 | 2021-01-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202530197A TW202530197A (zh) | 2025-08-01 |
| TWI904906B true TWI904906B (zh) | 2025-11-11 |
Family
ID=77775005
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW113140249A TWI904906B (zh) | 2020-08-24 | 2021-08-20 | Sarm1之抑制劑 |
| TW110130799A TWI786777B (zh) | 2020-08-24 | 2021-08-20 | Sarm1之抑制劑 |
| TW111144632A TW202334117A (zh) | 2020-08-24 | 2021-08-20 | Sarm1之抑制劑 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110130799A TWI786777B (zh) | 2020-08-24 | 2021-08-20 | Sarm1之抑制劑 |
| TW111144632A TW202334117A (zh) | 2020-08-24 | 2021-08-20 | Sarm1之抑制劑 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US12043613B2 (https=) |
| EP (1) | EP4200293A1 (https=) |
| JP (2) | JP7349046B2 (https=) |
| KR (2) | KR20260016617A (https=) |
| AU (2) | AU2021333558C1 (https=) |
| BR (1) | BR112023002575A2 (https=) |
| CA (1) | CA3189181A1 (https=) |
| CL (1) | CL2023000525A1 (https=) |
| CO (1) | CO2023001975A2 (https=) |
| CR (1) | CR20230113A (https=) |
| DO (1) | DOP2023000038A (https=) |
| EC (1) | ECSP23012981A (https=) |
| IL (1) | IL300586A (https=) |
| JO (1) | JOP20230037A1 (https=) |
| MX (1) | MX2023002256A (https=) |
| NZ (1) | NZ797733A (https=) |
| PE (1) | PE20230737A1 (https=) |
| TW (3) | TWI904906B (https=) |
| UA (1) | UA130657C2 (https=) |
| WO (1) | WO2022046606A1 (https=) |
| ZA (1) | ZA202301801B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3897670A4 (en) | 2018-12-19 | 2022-09-07 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS |
| US12404265B2 (en) * | 2020-08-04 | 2025-09-02 | Nura Bio, Inc. | Substituted pyridine derivatives as SARM1 inhibitors |
| CN116438171A (zh) | 2020-09-16 | 2023-07-14 | 努拉生物公司 | 作为sarm1抑制剂的取代的吡啶衍生物 |
| EP4376840A4 (en) | 2021-07-28 | 2025-05-21 | Nura Bio, Inc. | SUBSTITUTED PYRIDINE DERIVATIVES AS SARM1 INHIBITORS |
| US20240102018A1 (en) * | 2022-07-21 | 2024-03-28 | Amylyx Pharmaceuticals, Inc. | Oligonucleotide compositions and methods thereof |
| IL321043A (en) * | 2022-12-15 | 2025-07-01 | Sironax Ltd | SARM1 modulators, their preparations and uses |
| EP4655069A1 (en) | 2023-01-24 | 2025-12-03 | Disarm Therapeutics, Inc. | Pyridazines as sarm1 inhibitors |
| TW202509019A (zh) * | 2023-04-27 | 2025-03-01 | 香港商維泰瑞隆(香港)生物科技有限公司 | Sarm1調節子、其製劑及用途 |
| CN119219603A (zh) * | 2023-06-28 | 2024-12-31 | 科辉智药(深圳)新药研究中心有限公司 | Sarm1酶活性抑制剂及其用途 |
| CN121712761A (zh) * | 2023-08-25 | 2026-03-20 | 豪夫迈·罗氏有限公司 | 用于治疗神经退行性病症的作为sarm1抑制剂的吡唑衍生物 |
| IL326761A (en) | 2023-08-25 | 2026-04-01 | Lilly Co Eli | (S)-3-((6-fluoropyridin-3-yl)methyl)-1-(5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)piperidin-2-one benzenesulfonate |
| WO2025076088A1 (en) * | 2023-10-05 | 2025-04-10 | Genentech, Inc. | Lactams for use as sarm1 inhibitors |
| WO2025076017A1 (en) * | 2023-10-05 | 2025-04-10 | Genentech, Inc. | Carbamates for use as sarm1 inhibitors |
| TW202545928A (zh) | 2024-01-25 | 2025-12-01 | 比利時商優稀美生物醫藥股份有限公司 | 吡咯啶酮衍生物 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018114662A1 (de) * | 2016-12-22 | 2018-06-28 | Bayer Cropscience Aktiengesellschaft | Substituierte 1,2,4-thiadiazolylpyrrolone und 1,2,4-thiadiazolylhydantoine sowie deren salze und ihre verwendung als herbizide wirkstoffe |
| WO2019236890A1 (en) * | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6436966B1 (en) | 1997-10-27 | 2002-08-20 | Takeda Chemical Ind., Ltd. | Adenosine A3 receptor antagonists |
| US6787555B2 (en) | 2001-04-30 | 2004-09-07 | The Procter & Gamble Company | Triazole compounds useful in treating diseases associated with unwanted cytokine activity |
| AR043057A1 (es) | 2002-10-30 | 2005-07-13 | Vertex Pharma | Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa |
| AU2003300099A1 (en) | 2003-01-02 | 2004-07-29 | Millennium Pharmaceuticals, Inc. | COMPOSITIONS AND METHODS FOR INHIBITING TGF-Beta |
| AR044519A1 (es) | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| US7585881B2 (en) | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| WO2005105780A2 (en) | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of rock and other protein kinases |
| US8101770B2 (en) | 2004-12-16 | 2012-01-24 | Vertex Pharmaceuticals Incorporated | Pyridones useful as inhibitors of kinases |
| EP2036905B1 (en) | 2006-06-28 | 2012-12-12 | ASKA Pharmaceutical Co., Ltd. | Pyridylisoxazole derivative |
| CA2662359A1 (en) | 2006-09-21 | 2008-03-27 | Novartis Ag | Pyrrole derivatives useful for the treatment of cytokine-mediated diseases |
| EP2240475B1 (en) | 2007-12-20 | 2013-09-25 | Novartis AG | Thiazole derivatives used as pi 3 kinase inhibitors |
| JP2011506563A (ja) | 2007-12-20 | 2011-03-03 | ノバルティス アーゲー | ビスチアゾール誘導体、その製造方法および医薬品としてのその使用 |
| TW201004941A (en) | 2008-07-16 | 2010-02-01 | Wyeth Corp | Alpha7 nicotinic acetylcholine receptor inhibitors |
| US8785468B2 (en) | 2009-02-13 | 2014-07-22 | Amgen Inc. | Phenylalanine amide derivatives useful for treating insulin-related diseases and conditions |
| WO2012178022A2 (en) | 2011-06-24 | 2012-12-27 | University Of Massachusetts | Therapeutic applications targeting sarm1 |
| WO2014070978A1 (en) | 2012-11-03 | 2014-05-08 | Boehringer Ingelheim International Gmbh | Inhibitors of cytomegalovirus |
| US9695198B2 (en) | 2012-12-19 | 2017-07-04 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
| RU2570907C2 (ru) | 2013-10-21 | 2015-12-20 | Автономная Некоммерческая Организация "Научно-Исследовательский Центр Биотехнологии Антибиотиков И Других Биологически Активных Веществ "Биоан" | Производные 3-ациламинопиридин-2(1h)-она, применимые как ингибиторы серин-треониновой протеинкиназы gsk3b в качестве лекарственных препаратов для лечения диабета ii типа. |
| WO2015084936A1 (en) | 2013-12-04 | 2015-06-11 | The Scripps Research Institute | Novel compounds as jnk kinase inhibitors |
| WO2018035204A1 (en) | 2016-08-16 | 2018-02-22 | Henry Ford Health System | Compositions for the treatment of neuropathic pain and sensitization of tumors to chemotherapies |
| JP7044789B2 (ja) | 2016-09-24 | 2022-03-30 | ワシントン・ユニバーシティ | Sarm1 nadアーゼ活性の阻害剤およびその使用 |
| WO2018107056A1 (en) | 2016-12-09 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | 1,3-substitued pyrazole compounds useful for reduction of very long chain fatty acic levels |
| EP3558976A1 (de) | 2016-12-22 | 2019-10-30 | Bayer CropScience Aktiengesellschaft | Substituierte azolylpyrrolone und azolylhydantoine sowie deren salze und ihre verwendung als herbizide wirkstoffe |
| US11919902B2 (en) * | 2017-12-22 | 2024-03-05 | Hibercell, Inc. | Aryl-bipyridine amine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| CN112839647B (zh) | 2018-06-07 | 2025-09-23 | 达萨玛治疗公司 | Sarm1抑制剂 |
| CN112839648B (zh) * | 2018-06-07 | 2025-04-04 | 达萨玛治疗公司 | Sarm1抑制剂 |
| US12084436B2 (en) * | 2019-01-30 | 2024-09-10 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| JP7289375B2 (ja) | 2019-06-06 | 2023-06-09 | ディスアーム セラピューティクス, インコーポレイテッド | Sarm1の阻害剤 |
| US12595252B2 (en) | 2019-06-14 | 2026-04-07 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| MX2022000950A (es) | 2019-07-22 | 2022-02-14 | Bayer Ag | 5-amino pirazoles y triazoles como plaguicidas. |
| CA3150878A1 (en) | 2019-09-12 | 2021-03-18 | Jonathan Bentley | Inhibitors of sarm1 |
| WO2021092240A1 (en) | 2019-11-05 | 2021-05-14 | Dermira, Inc. | Mrgprx2 antagonists for the treatment of inflammatory disorders |
| WO2021142006A1 (en) | 2020-01-07 | 2021-07-15 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| US12435084B2 (en) | 2020-04-09 | 2025-10-07 | Eli Lilly And Company | Indazole derivatives as inhibitors of SARM1 |
| US12606558B2 (en) | 2020-04-09 | 2026-04-21 | Disarm Therapeutics, Inc. | Condensed pyrazole derivatives as inhibitors of SARM1 |
| US12404265B2 (en) * | 2020-08-04 | 2025-09-02 | Nura Bio, Inc. | Substituted pyridine derivatives as SARM1 inhibitors |
-
2021
- 2021-08-20 TW TW113140249A patent/TWI904906B/zh active
- 2021-08-20 TW TW110130799A patent/TWI786777B/zh active
- 2021-08-20 TW TW111144632A patent/TW202334117A/zh unknown
- 2021-08-23 PE PE2023000530A patent/PE20230737A1/es unknown
- 2021-08-23 US US17/408,956 patent/US12043613B2/en active Active
- 2021-08-23 CA CA3189181A patent/CA3189181A1/en active Pending
- 2021-08-23 KR KR1020267002225A patent/KR20260016617A/ko active Pending
- 2021-08-23 CR CR20230113A patent/CR20230113A/es unknown
- 2021-08-23 WO PCT/US2021/047093 patent/WO2022046606A1/en not_active Ceased
- 2021-08-23 KR KR1020237009643A patent/KR102918550B1/ko active Active
- 2021-08-23 IL IL300586A patent/IL300586A/en unknown
- 2021-08-23 UA UAA202300576A patent/UA130657C2/uk unknown
- 2021-08-23 NZ NZ797733A patent/NZ797733A/en unknown
- 2021-08-23 BR BR112023002575A patent/BR112023002575A2/pt unknown
- 2021-08-23 MX MX2023002256A patent/MX2023002256A/es unknown
- 2021-08-23 EP EP21770372.7A patent/EP4200293A1/en active Pending
- 2021-08-23 JP JP2023513172A patent/JP7349046B2/ja active Active
- 2021-08-23 AU AU2021333558A patent/AU2021333558C1/en active Active
-
2023
- 2023-02-14 ZA ZA2023/01801A patent/ZA202301801B/en unknown
- 2023-02-22 CL CL2023000525A patent/CL2023000525A1/es unknown
- 2023-02-22 CO CONC2023/0001975A patent/CO2023001975A2/es unknown
- 2023-02-23 EC ECSENADI202312981A patent/ECSP23012981A/es unknown
- 2023-02-23 DO DO2023000038A patent/DOP2023000038A/es unknown
- 2023-02-23 JO JOJO/P/2023/0037A patent/JOP20230037A1/ar unknown
- 2023-09-08 JP JP2023145779A patent/JP7756130B2/ja active Active
-
2024
- 2024-05-21 AU AU2024203373A patent/AU2024203373B2/en active Active
- 2024-06-19 US US18/747,889 patent/US20240376083A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018114662A1 (de) * | 2016-12-22 | 2018-06-28 | Bayer Cropscience Aktiengesellschaft | Substituierte 1,2,4-thiadiazolylpyrrolone und 1,2,4-thiadiazolylhydantoine sowie deren salze und ihre verwendung als herbizide wirkstoffe |
| WO2019236890A1 (en) * | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
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