CN112839647B - Sarm1抑制剂 - Google Patents
Sarm1抑制剂Info
- Publication number
- CN112839647B CN112839647B CN201980052437.0A CN201980052437A CN112839647B CN 112839647 B CN112839647 B CN 112839647B CN 201980052437 A CN201980052437 A CN 201980052437A CN 112839647 B CN112839647 B CN 112839647B
- Authority
- CN
- China
- Prior art keywords
- compound
- sarm1
- compounds
- disease
- axonal
- 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.)
- Active
Links
Classifications
-
- 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
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/28—Cinnolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862682033P | 2018-06-07 | 2018-06-07 | |
| US62/682,033 | 2018-06-07 | ||
| PCT/US2019/035833 WO2019236879A1 (en) | 2018-06-07 | 2019-06-06 | Inhibitors of sarm1 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN112839647A CN112839647A (zh) | 2021-05-25 |
| CN112839647B true CN112839647B (zh) | 2025-09-23 |
Family
ID=68769462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980052437.0A Active CN112839647B (zh) | 2018-06-07 | 2019-06-06 | Sarm1抑制剂 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US12338238B2 (https=) |
| EP (1) | EP3801500B1 (https=) |
| JP (2) | JP2021527125A (https=) |
| CN (1) | CN112839647B (https=) |
| CA (1) | CA3102645A1 (https=) |
| ES (1) | ES3028093T3 (https=) |
| MA (1) | MA52813A (https=) |
| WO (1) | WO2019236879A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES3028093T3 (en) | 2018-06-07 | 2025-06-18 | Disarm Therapeutics Inc | Inhibitors of sarm1 |
| US12448374B2 (en) | 2018-06-07 | 2025-10-21 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| WO2020132045A1 (en) | 2018-12-19 | 2020-06-25 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| CA3141404A1 (en) | 2019-06-14 | 2020-12-17 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| JP7534390B2 (ja) | 2019-09-12 | 2024-08-14 | 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 |
| EP4065714A1 (en) * | 2019-11-26 | 2022-10-05 | Disarm Therapeutics, Inc. | Methods and compositions for neuroprotection |
| CN115916764B (zh) * | 2020-04-09 | 2024-09-20 | 达萨玛治疗公司 | 作为sarm1抑制剂的吲唑衍生物 |
| US12606558B2 (en) | 2020-04-09 | 2026-04-21 | Disarm Therapeutics, Inc. | Condensed pyrazole derivatives as inhibitors of SARM1 |
| IL298577A (en) * | 2020-05-27 | 2023-01-01 | Emendobio Inc | Biallelic silencing of sarm1 |
| TW202334117A (zh) | 2020-08-24 | 2023-09-01 | 美商達薩瑪治療公司 | Ｓａｒｍ１之抑制劑 |
| EP4536637A2 (en) * | 2022-06-06 | 2025-04-16 | Nico Therapeutics, Inc. | Compounds, compositions, and methods |
| WO2023244788A1 (en) * | 2022-06-17 | 2023-12-21 | Neuron23, Inc. | Kinase modulators and methods of use thereof |
| JP2026503618A (ja) | 2023-01-24 | 2026-01-29 | 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阻害剤としての置換された１ｈ－ピラゾール－４－カルボキサミド |
| 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 |
Citations (7)
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|---|---|---|---|---|
| WO2007000240A1 (en) * | 2005-06-28 | 2007-01-04 | Sanofi-Aventis | Isoquinoline derivatives as inhibitors of rho-kinase |
| WO2007012422A1 (en) * | 2005-07-26 | 2007-02-01 | Sanofi-Aventis | Cyclohexylamin isoquinolone derivatives as rho-kinase inhibitors |
| WO2009155121A2 (en) * | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| WO2010091310A1 (en) * | 2009-02-06 | 2010-08-12 | Elan Pharmaceuticals, Inc. | Inhibitors of jun n-terminal kinase |
| WO2013005157A1 (en) * | 2011-07-05 | 2013-01-10 | Lupin Limited | Sulfone derivatives and their use as pkm2 modulators for the treatment of cancer |
| WO2016036636A1 (en) * | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2018167800A1 (en) * | 2017-03-13 | 2018-09-20 | Impetis Biosciences Limited | Fused bicyclic compounds, compositions and applications thereof |
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| GB1022214A (en) | 1963-01-31 | 1966-03-09 | Sterling Drug Inc | Novel 1,3-disubstituted-1,4-dihydro-4-oxo-1,7-naphthyridines and their preparation |
| US3429887A (en) | 1965-01-26 | 1969-02-25 | Sterling Drug Inc | 1,7-naphthyridine-3-carboxylic acid derivatives and their preparation |
| US3506668A (en) | 1965-01-26 | 1970-04-14 | Sterling Drug Inc | Method of preparing 8-hydroxy-quinolines |
| US3429882A (en) | 1968-03-25 | 1969-02-25 | Geigy Chem Corp | 1,2,8,9-tetraazaphenalenes |
| US3539567A (en) | 1968-04-23 | 1970-11-10 | Geigy Chem Corp | 8-carboxy-1(2h) phthalazinones |
| US3624108A (en) | 1968-04-23 | 1971-11-30 | Geigy Chem Corp | 7-carboxyphthalides |
| US3761493A (en) | 1968-04-23 | 1973-09-25 | Ciba Geigy Corp | 3-dibromomethylphthalic anhydride |
| US3542777A (en) | 1968-08-12 | 1970-11-24 | Geigy Chem Corp | Derivatives of 9-pyridylalkyl-1,2,8,9-tetraazaphenalenes |
| US3517014A (en) | 1969-06-16 | 1970-06-23 | Sterling Drug Inc | Method of preparing 8-hydroxyquinoline-3-carboxylic acids |
| US3711473A (en) | 1970-04-06 | 1973-01-16 | Ciba Geigy Corp | 3-hydrazino-1,2,8,9-tetraazaphenalenes |
| CA1043616A (en) | 1973-10-16 | 1978-12-05 | Fuji Photo Film Co. | Heat developable light-sensitive material |
| US4207112A (en) | 1974-01-29 | 1980-06-10 | Fuji Photo Film Co., Ltd. | Heat developable light-sensitive materials |
| JPS50123331A (https=) | 1974-03-14 | 1975-09-27 | ||
| GB9310700D0 (en) * | 1993-05-24 | 1993-07-07 | Zeneca Ltd | Novel composition |
| HK1053833A1 (zh) | 2000-04-27 | 2003-11-07 | Abbott Laboratories | 取代苯基法呢基转移酶抑制剂 |
| CN100411686C (zh) | 2001-04-11 | 2008-08-20 | 千寿制药株式会社 | 视觉功能障碍改善剂 |
| ES2211344B1 (es) * | 2002-12-26 | 2005-10-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
| WO2005102345A1 (en) * | 2004-03-30 | 2005-11-03 | Alcon, Inc. | Use of rho kinase inhibitors in the treatment of hearing loss, tinnitus and improving body balance |
| US20060078890A1 (en) * | 2004-10-08 | 2006-04-13 | Ole Isacson | Methods for identifying parkinson's disease therapeutics |
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| US12448374B2 (en) | 2018-06-07 | 2025-10-21 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| JP7481329B2 (ja) | 2018-06-07 | 2024-05-10 | 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阻害剤 |
| ES3028093T3 (en) | 2018-06-07 | 2025-06-18 | Disarm Therapeutics Inc | Inhibitors of sarm1 |
| CN109223787A (zh) | 2018-10-04 | 2019-01-18 | 南京先进生物材料与过程装备研究院有限公司 | 一种喜树碱和新型酞嗪酮类化合物联合用药物组合物 |
| CN109180642A (zh) | 2018-10-04 | 2019-01-11 | 南京先进生物材料与过程装备研究院有限公司 | 酞嗪酮类btk抑制剂及其应用 |
| CN109293635A (zh) | 2018-10-04 | 2019-02-01 | 南京先进生物材料与过程装备研究院有限公司 | 一种新型btk激酶抑制剂的p晶型及其制备方法 |
| CN109336863A (zh) | 2018-10-04 | 2019-02-15 | 南京先进生物材料与过程装备研究院有限公司 | 一种新型酞嗪酮类btk抑制剂、制备及其应用 |
| CN109485636A (zh) | 2018-10-04 | 2019-03-19 | 南京先进生物材料与过程装备研究院有限公司 | 一种新型btk激酶抑制剂的盐酸盐及其制备方法与用途 |
| US20220072019A1 (en) | 2018-10-19 | 2022-03-10 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with nad+ or a nad+ precursor |
| CN109172562A (zh) | 2018-10-31 | 2019-01-11 | 南京先进生物材料与过程装备研究院有限公司 | 一种紫杉醇和甲氧基酞嗪酮类btk抑制剂联合用药物组合物及其应用 |
| CN109331018A (zh) | 2018-10-31 | 2019-02-15 | 南京先进生物材料与过程装备研究院有限公司 | 一种紫杉醇和硝基酞嗪酮btk抑制剂联合用药物组合物及其应用 |
| CN109394766A (zh) | 2018-10-31 | 2019-03-01 | 南京先进生物材料与过程装备研究院有限公司 | 一种紫杉醇和对苯硝基酞嗪酮类btk抑制剂联合用药物组合物及其应用 |
| CN109276571A (zh) | 2018-10-31 | 2019-01-29 | 南京先进生物材料与过程装备研究院有限公司 | 一种紫杉醇和新型硝基酞嗪酮btk抑制剂联合用药物组合物及其应用 |
| CN109481441A (zh) | 2018-10-31 | 2019-03-19 | 南京先进生物材料与过程装备研究院有限公司 | 一种紫杉醇和新型甲氧基酞嗪酮类btk抑制剂联合用药物组合物及其应用 |
| WO2021261540A1 (ja) | 2020-06-25 | 2021-12-30 | 富士フイルム株式会社 | 腸管上皮細胞の製造方法、及びその利用 |
-
2019
- 2019-06-06 ES ES19816172T patent/ES3028093T3/es active Active
- 2019-06-06 CA CA3102645A patent/CA3102645A1/en active Pending
- 2019-06-06 CN CN201980052437.0A patent/CN112839647B/zh active Active
- 2019-06-06 MA MA052813A patent/MA52813A/fr unknown
- 2019-06-06 EP EP19816172.1A patent/EP3801500B1/en active Active
- 2019-06-06 US US16/972,684 patent/US12338238B2/en active Active
- 2019-06-06 WO PCT/US2019/035833 patent/WO2019236879A1/en not_active Ceased
- 2019-06-06 JP JP2021518045A patent/JP2021527125A/ja active Pending
-
2023
- 2023-11-30 JP JP2023203259A patent/JP7576145B2/ja active Active
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007000240A1 (en) * | 2005-06-28 | 2007-01-04 | Sanofi-Aventis | Isoquinoline derivatives as inhibitors of rho-kinase |
| WO2007012422A1 (en) * | 2005-07-26 | 2007-02-01 | Sanofi-Aventis | Cyclohexylamin isoquinolone derivatives as rho-kinase inhibitors |
| WO2009155121A2 (en) * | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| WO2010091310A1 (en) * | 2009-02-06 | 2010-08-12 | Elan Pharmaceuticals, Inc. | Inhibitors of jun n-terminal kinase |
| WO2013005157A1 (en) * | 2011-07-05 | 2013-01-10 | Lupin Limited | Sulfone derivatives and their use as pkm2 modulators for the treatment of cancer |
| WO2016036636A1 (en) * | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2018167800A1 (en) * | 2017-03-13 | 2018-09-20 | Impetis Biosciences Limited | Fused bicyclic compounds, compositions and applications thereof |
Non-Patent Citations (6)
| Title |
|---|
| Domino Inverse Electron-Demand Diels-Alder/Cyclopropanation Reaction of Diazines Catalyzed by a Bidentate Lewis Acid;KESSLER SIMON等;JOURNAL OF THE AMERICAN CHEMICAL SOCIETY;第134卷(第43期);17885-17888 * |
| Kitaoka Yasushi等.Axonal protection by ripasudil,a rho kinase inhibitor, via modulating autophagy in TNF-Induced Optic Nerve Degeneration.Investigative Opthalmology & Visual Science.2017,第58卷(第12期),5056. * |
| phthalazine derivatives from aromatic aldazines;Robev Stefan K等;TETRAHEDRON LETTERS;第22卷(第4期);345-348 * |
| PREPARATION AND CYCLIzATION OF 2-HYDRAZINO-1- PENTAFLUOROPHENYLETHANOL;PETROV V P等;CHEMISTRY OF HETEROCYCLIC COMPOUNDS;第6卷(第3期);381-364 * |
| Synthesis and SAR exploration of dinapsoline analogues;S SIT等;BIOORGANIC & MEDICINAL CHEMISTRY;第12卷(第4期);715-734 * |
| The Novel Rho Kinese(ROCK) Inhibitor K-115: A new candidate drug for neuroprotective treatment in glaucoma;Kotaro Yamamoto等;Investigative Opthalmology & Visual Science;第55卷(第11期);7126-7136 * |
Also Published As
| Publication number | Publication date |
|---|---|
| MA52813A (fr) | 2021-04-14 |
| US12338238B2 (en) | 2025-06-24 |
| JP2024037770A (ja) | 2024-03-19 |
| CN112839647A (zh) | 2021-05-25 |
| JP2021527125A (ja) | 2021-10-11 |
| CA3102645A1 (en) | 2019-12-12 |
| WO2019236879A1 (en) | 2019-12-12 |
| EP3801500B1 (en) | 2025-03-05 |
| JP7576145B2 (ja) | 2024-10-30 |
| US20210261540A1 (en) | 2021-08-26 |
| ES3028093T3 (en) | 2025-06-18 |
| EP3801500A4 (en) | 2022-03-02 |
| EP3801500A1 (en) | 2021-04-14 |
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