TWI786777B - Sarm1之抑制劑 - Google Patents
Sarm1之抑制劑 Download PDFInfo
- Publication number
- TWI786777B TWI786777B TW110130799A TW110130799A TWI786777B TW I786777 B TWI786777 B TW I786777B TW 110130799 A TW110130799 A TW 110130799A TW 110130799 A TW110130799 A TW 110130799A TW I786777 B TWI786777 B TW I786777B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- chiral
- mmol
- Prior art date
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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
- A61P25/28—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
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- 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)
- Immunology (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)
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 |
|---|---|
| TW202214597A TW202214597A (zh) | 2022-04-16 |
| TWI786777B true TWI786777B (zh) | 2022-12-11 |
Family
ID=77775005
Family Applications (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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW111144632A TW202334117A (zh) | 2020-08-24 | 2021-08-20 | Sarm1之抑制劑 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US12043613B2 (enExample) |
| EP (1) | EP4200293A1 (enExample) |
| JP (2) | JP7349046B2 (enExample) |
| KR (1) | KR20230057396A (enExample) |
| AU (2) | AU2021333558C1 (enExample) |
| BR (1) | BR112023002575A2 (enExample) |
| CA (1) | CA3189181A1 (enExample) |
| CL (1) | CL2023000525A1 (enExample) |
| CO (1) | CO2023001975A2 (enExample) |
| CR (1) | CR20230113A (enExample) |
| DO (1) | DOP2023000038A (enExample) |
| EC (1) | ECSP23012981A (enExample) |
| IL (1) | IL300586A (enExample) |
| MX (1) | MX2023002256A (enExample) |
| PE (1) | PE20230737A1 (enExample) |
| TW (2) | TWI786777B (enExample) |
| WO (1) | WO2022046606A1 (enExample) |
| ZA (1) | ZA202301801B (enExample) |
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 |
| WO2022060812A1 (en) | 2020-09-16 | 2022-03-24 | Nura Bio, Inc. | Substituted pyridine derivatives as sarm1 inhibitors |
| CA3226869A1 (en) | 2021-07-28 | 2023-02-02 | Rao Kolluri | Substituted pyridine derivatives as sarm1 inhibitors |
| AU2023311008A1 (en) * | 2022-07-21 | 2025-01-23 | Amylyx Pharmaceuticals, Inc. | Oligonucleotide compositions and methods thereof |
| WO2024125624A1 (en) * | 2022-12-15 | 2024-06-20 | Sironax Ltd. | Sarm1 modulators, preparations, and uses thereof |
| EP4655069A1 (en) | 2023-01-24 | 2025-12-03 | Disarm Therapeutics, Inc. | Pyridazines as sarm1 inhibitors |
| WO2024222835A1 (en) * | 2023-04-27 | 2024-10-31 | Sironax Ltd. | Sarm1 modulators, preparations, and uses thereof |
| 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 |
| WO2025049184A1 (en) | 2023-08-25 | 2025-03-06 | Eli Lilly And Company | (s)-3-((6-fluoropyridin-3-yl)methyl)-1-(5-(pyridin-4-yl)-4h-1,2,4-triazol-3-yl)piperidin-2-one benzenesulfonate |
| WO2025045746A1 (en) * | 2023-08-25 | 2025-03-06 | F. Hoffmann-La Roche Ag | Pyrazole derivatives as sarm1 inhibitors useful for the treatment of neurodegenerative disorders |
| 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 |
| WO2025157895A1 (en) | 2024-01-25 | 2025-07-31 | UCB Biopharma SRL | Pyrrolidinone derivatives |
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 |
|---|---|---|---|---|
| EP1027050B1 (en) | 1997-10-27 | 2004-01-14 | Takeda Chemical Industries, Ltd. | 1,3-thiazoles as adenosine a3 receptor antagonists for the treatment of allergy, asthma and diabetes |
| 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 |
| DE602005020611D1 (de) | 2004-04-28 | 2010-05-27 | Vertex Pharma | Als inhibitoren von rock und anderen proteinkinasen geeignete zusammensetzungen |
| RU2423351C2 (ru) | 2004-12-16 | 2011-07-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний |
| JP5244591B2 (ja) | 2006-06-28 | 2013-07-24 | あすか製薬株式会社 | ピリジルイソオキサゾール誘導体 |
| WO2008034600A1 (en) | 2006-09-21 | 2008-03-27 | Novartis Ag | Pyrrole derivatives useful for the treatment of cytokine-mediated diseases |
| 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 |
| EA201000947A1 (ru) | 2007-12-20 | 2011-02-28 | Новартис Аг | Производные тиазола, применимые в качестве ингибиторов киназы pi3 |
| TW201004941A (en) | 2008-07-16 | 2010-02-01 | Wyeth Corp | Alpha7 nicotinic acetylcholine receptor inhibitors |
| WO2010093849A2 (en) | 2009-02-13 | 2010-08-19 | 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 |
| US9284310B2 (en) | 2012-11-03 | 2016-03-15 | Boehringer Ingelheim International Gmbh | Inhibitors of cytomegalovirus |
| EP2934536B1 (en) | 2012-12-19 | 2017-09-27 | 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. |
| US20160304466A1 (en) | 2013-12-04 | 2016-10-20 | The Scripps Research Institute | Novel compounds as jnk kinase inhibitors |
| US11357800B2 (en) | 2016-08-16 | 2022-06-14 | 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 |
| UY37512A (es) | 2016-12-09 | 2019-04-30 | Vertex Pharma | Compuestos pirazol 1,3-sustituido útiles para la reducción de los niveles de ácidos grasos de cadena muy larga |
| JP2020504115A (ja) | 2016-12-22 | 2020-02-06 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 置換アゾリルピロロンおよびアゾリルヒダントインならびにその塩ならびに除草活性物質としてのその使用 |
| CA3085460A1 (en) | 2017-12-22 | 2019-06-27 | Petra Pharma Corporation | Aryl-bipyridine amine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| WO2019236879A1 (en) | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| 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 |
| US20220242859A1 (en) | 2019-06-06 | 2022-08-04 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| CN113966217B (zh) | 2019-06-14 | 2025-07-04 | 达萨玛治疗公司 | Sarm1抑制剂 |
| KR20220035939A (ko) | 2019-07-22 | 2022-03-22 | 바이엘 악티엔게젤샤프트 | 살충제로서의 5-아미노-치환된 피라졸 및 트리아졸 |
| CN114728007B (zh) | 2019-09-12 | 2025-04-29 | 达萨玛治疗公司 | Sarm1的抑制剂 |
| WO2021092240A1 (en) | 2019-11-05 | 2021-05-14 | Dermira, Inc. | Mrgprx2 antagonists for the treatment of inflammatory disorders |
| UA128949C2 (uk) | 2020-01-07 | 2024-12-04 | Дісарм Серап'Ютікс, Інк. | Інгібітори sarm1 |
| EP4132928A1 (en) | 2020-04-09 | 2023-02-15 | Disarm Therapeutics, Inc. | Condensed pyrazole derivatives as inhibitors of sarm1 |
| US12435084B2 (en) | 2020-04-09 | 2025-10-07 | Eli Lilly And Company | Indazole 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 TW110130799A patent/TWI786777B/zh active
- 2021-08-20 TW TW111144632A patent/TW202334117A/zh unknown
- 2021-08-23 CR CR20230113A patent/CR20230113A/es unknown
- 2021-08-23 KR KR1020237009643A patent/KR20230057396A/ko active Pending
- 2021-08-23 EP EP21770372.7A patent/EP4200293A1/en active Pending
- 2021-08-23 US US17/408,956 patent/US12043613B2/en active Active
- 2021-08-23 BR BR112023002575A patent/BR112023002575A2/pt unknown
- 2021-08-23 CA CA3189181A patent/CA3189181A1/en active Pending
- 2021-08-23 IL IL300586A patent/IL300586A/en unknown
- 2021-08-23 PE PE2023000530A patent/PE20230737A1/es unknown
- 2021-08-23 JP JP2023513172A patent/JP7349046B2/ja active Active
- 2021-08-23 MX MX2023002256A patent/MX2023002256A/es unknown
- 2021-08-23 WO PCT/US2021/047093 patent/WO2022046606A1/en not_active Ceased
- 2021-08-23 AU AU2021333558A patent/AU2021333558C1/en active Active
-
2023
- 2023-02-14 ZA ZA2023/01801A patent/ZA202301801B/en unknown
- 2023-02-22 CO CONC2023/0001975A patent/CO2023001975A2/es unknown
- 2023-02-22 CL CL2023000525A patent/CL2023000525A1/es unknown
- 2023-02-23 EC ECSENADI202312981A patent/ECSP23012981A/es unknown
- 2023-02-23 DO DO2023000038A patent/DOP2023000038A/es unknown
- 2023-09-08 JP JP2023145779A patent/JP7756130B2/ja active Active
-
2024
- 2024-05-21 AU AU2024203373A patent/AU2024203373A1/en active Pending
- 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023535236A (ja) | 2023-08-16 |
| AU2021333558C1 (en) | 2024-06-20 |
| TW202214597A (zh) | 2022-04-16 |
| MX2023002256A (es) | 2023-03-17 |
| US20220056013A1 (en) | 2022-02-24 |
| JP7756130B2 (ja) | 2025-10-17 |
| WO2022046606A1 (en) | 2022-03-03 |
| CO2023001975A2 (es) | 2023-03-07 |
| US12043613B2 (en) | 2024-07-23 |
| DOP2023000038A (es) | 2023-03-15 |
| AU2024203373A1 (en) | 2024-06-13 |
| BR112023002575A2 (pt) | 2023-03-07 |
| TW202530197A (zh) | 2025-08-01 |
| PE20230737A1 (es) | 2023-05-03 |
| CR20230113A (es) | 2023-04-14 |
| AU2021333558B2 (en) | 2024-02-22 |
| CA3189181A1 (en) | 2022-03-03 |
| AU2021333558A1 (en) | 2023-03-02 |
| ZA202301801B (en) | 2024-09-25 |
| JP7349046B2 (ja) | 2023-09-21 |
| ECSP23012981A (es) | 2023-03-31 |
| KR20230057396A (ko) | 2023-04-28 |
| IL300586A (en) | 2023-04-01 |
| EP4200293A1 (en) | 2023-06-28 |
| JP2024016014A (ja) | 2024-02-06 |
| TW202334117A (zh) | 2023-09-01 |
| US20240376083A1 (en) | 2024-11-14 |
| CL2023000525A1 (es) | 2023-09-15 |
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