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)
- Epidemiology (AREA)
- Immunology (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)
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 |
| CA3226869A1 (en) | 2021-07-28 | 2023-02-02 | Rao Kolluri | Substituted pyridine derivatives as sarm1 inhibitors |
| KR20250040698A (ko) * | 2022-07-21 | 2025-03-24 | 아밀릭스 파마슈티컬스, 인코포레이티드 | 올리고뉴클레오티드 조성물 및 이의 방법 |
| 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 |
| 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 |
| WO2025076017A1 (en) * | 2023-10-05 | 2025-04-10 | Genentech, Inc. | Carbamates for use as sarm1 inhibitors |
| WO2025076088A1 (en) * | 2023-10-05 | 2025-04-10 | Genentech, Inc. | Lactams 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 |
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| 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 |
| CA2504320A1 (en) | 2002-10-30 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of rock and other protein kinases |
| AU2003300099A1 (en) | 2003-01-02 | 2004-07-29 | Millennium Pharmaceuticals, Inc. | COMPOSITIONS AND METHODS FOR INHIBITING TGF-Beta |
| TW200519106A (en) | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
| 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 |
| KR20070095952A (ko) | 2004-12-16 | 2007-10-01 | 버텍스 파마슈티칼스 인코포레이티드 | 염증성 질환, 증식성 질환 및 면역학적으로 매개된 질환치료용 Ｔｅｃ 계열 단백질 키나제의 억제제로서 유용한피리드-2-온 |
| AU2007265965B2 (en) | 2006-06-28 | 2012-03-08 | Aska Pharmaceutical Co., Ltd. | Pyridylisoxazole derivative |
| EP2069333A1 (en) | 2006-09-21 | 2009-06-17 | Novartis Ag | Pyrrole derivatives useful for the treatment of cytokine-mediated diseases |
| WO2009080705A2 (en) | 2007-12-20 | 2009-07-02 | Novartis Ag | Bis-thiazole derivatives, process for their preparation and their use as medicaments |
| KR20100093129A (ko) | 2007-12-20 | 2010-08-24 | 노파르티스 아게 | Ｐｉ ３ 키나제 억제제로서 사용되는 티아졸 유도체 |
| 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 |
| US20120328629A1 (en) | 2011-06-24 | 2012-12-27 | University Of Miami | Therapeutic Applications Targeting SARM1 |
| JP6482466B2 (ja) | 2012-11-03 | 2019-03-13 | 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 | サイトメガロウイルスの阻害剤 |
| WO2014099694A1 (en) | 2012-12-19 | 2014-06-26 | 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. |
| EP3076789A4 (en) | 2013-12-04 | 2017-11-22 | The Scripps Research Institute | Novel compounds as jnk kinase inhibitors |
| EP3500285B1 (en) | 2016-08-16 | 2022-04-20 | Henry Ford Health System | Compositions for the treatment of chemotherapy-induced neuropathic pain |
| WO2018057989A1 (en) | 2016-09-24 | 2018-03-29 | Washington University | INHIBITORS OF SARM1 NADase ACTIVITY AND USES THEREOF |
| US20180251431A1 (en) | 2016-12-09 | 2018-09-06 | Vertex Pharmaceuticals Incorporated | 1,3-substituted pyrazole compounds useful for reduction of very long chain fatty acid levels |
| 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 |
| EP3801500B1 (en) | 2018-06-07 | 2025-03-05 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| EP3801499B1 (en) | 2018-06-07 | 2024-02-28 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| WO2020158762A1 (ja) * | 2019-01-30 | 2020-08-06 | 武田薬品工業株式会社 | 複素環化合物 |
| 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 |
| WO2020252229A2 (en) | 2019-06-14 | 2020-12-17 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| BR112022000354A2 (pt) | 2019-07-22 | 2022-05-10 | Bayer Ag | Pirazóis e trizóis substituídos com amino na posição 5 como pesticidas |
| US12441719B2 (en) | 2019-09-12 | 2025-10-14 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| CN114845709B (zh) | 2019-11-05 | 2024-10-01 | 德米拉公司 | 用于治疗炎性病症的mrgprx2拮抗剂 |
| CR20220375A (es) | 2020-01-07 | 2022-09-22 | Disarm Therapeutics Inc | Inhibidores de sarm1 |
| JP7478252B2 (ja) | 2020-04-09 | 2024-05-02 | 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 |
| JP7477642B2 (ja) | 2020-04-09 | 2024-05-01 | 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 |
| 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 IL IL300586A patent/IL300586A/en unknown
- 2021-08-23 PE PE2023000530A patent/PE20230737A1/es unknown
- 2021-08-23 EP EP21770372.7A patent/EP4200293A1/en active Pending
- 2021-08-23 MX MX2023002256A patent/MX2023002256A/es unknown
- 2021-08-23 CA CA3189181A patent/CA3189181A1/en active Pending
- 2021-08-23 JP JP2023513172A patent/JP7349046B2/ja active Active
- 2021-08-23 US US17/408,956 patent/US12043613B2/en active Active
- 2021-08-23 WO PCT/US2021/047093 patent/WO2022046606A1/en not_active Ceased
- 2021-08-23 CR CR20230113A patent/CR20230113A/es unknown
- 2021-08-23 AU AU2021333558A patent/AU2021333558C1/en active Active
- 2021-08-23 KR KR1020237009643A patent/KR20230057396A/ko active Pending
- 2021-08-23 BR BR112023002575A patent/BR112023002575A2/pt unknown
-
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 DO DO2023000038A patent/DOP2023000038A/es unknown
- 2023-02-23 EC ECSENADI202312981A patent/ECSP23012981A/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 |
|---|---|
| TW202334117A (zh) | 2023-09-01 |
| MX2023002256A (es) | 2023-03-17 |
| KR20230057396A (ko) | 2023-04-28 |
| PE20230737A1 (es) | 2023-05-03 |
| JP2023535236A (ja) | 2023-08-16 |
| TW202214597A (zh) | 2022-04-16 |
| JP2024016014A (ja) | 2024-02-06 |
| TW202530197A (zh) | 2025-08-01 |
| AU2024203373A1 (en) | 2024-06-13 |
| DOP2023000038A (es) | 2023-03-15 |
| AU2021333558C1 (en) | 2024-06-20 |
| BR112023002575A2 (pt) | 2023-03-07 |
| ECSP23012981A (es) | 2023-03-31 |
| CO2023001975A2 (es) | 2023-03-07 |
| JP7756130B2 (ja) | 2025-10-17 |
| US20220056013A1 (en) | 2022-02-24 |
| CA3189181A1 (en) | 2022-03-03 |
| CR20230113A (es) | 2023-04-14 |
| CL2023000525A1 (es) | 2023-09-15 |
| JP7349046B2 (ja) | 2023-09-21 |
| IL300586A (en) | 2023-04-01 |
| EP4200293A1 (en) | 2023-06-28 |
| AU2021333558B2 (en) | 2024-02-22 |
| WO2022046606A1 (en) | 2022-03-03 |
| ZA202301801B (en) | 2024-09-25 |
| US12043613B2 (en) | 2024-07-23 |
| US20240376083A1 (en) | 2024-11-14 |
| AU2021333558A1 (en) | 2023-03-02 |
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