PE20230737A1 - Inhibidores de sarm1 - Google Patents
Inhibidores de sarm1Info
- Publication number
- PE20230737A1 PE20230737A1 PE2023000530A PE2023000530A PE20230737A1 PE 20230737 A1 PE20230737 A1 PE 20230737A1 PE 2023000530 A PE2023000530 A PE 2023000530A PE 2023000530 A PE2023000530 A PE 2023000530A PE 20230737 A1 PE20230737 A1 PE 20230737A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halogen
- heteroaryl ring
- cyano
- sulfur
- Prior art date
Links
- 101000685982 Homo sapiens NAD(+) hydrolase SARM1 Proteins 0.000 title abstract 2
- 102100023356 NAD(+) hydrolase SARM1 Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229910052717 sulfur Chemical group 0.000 abstract 2
- 239000011593 sulfur Chemical group 0.000 abstract 2
- 229910003204 NH2 Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 230000003376 axonal effect Effects 0.000 abstract 1
- 230000007850 degeneration Effects 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (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)
- 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)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto de formula (I), en donde: R1 es un anillo heteroarilo de 5 a 6 miembros que tiene 1-3 heteroatomos seleccionados de oxigeno, nitrogeno y azufre; G es CH, CRx o N; Rx es alquilo C1-C3, halogeno o ciano; X es CH2, NH, N(alquilo C1-C3) u O; Y es C(Rp)2 o NH; Z es enlace, CH2 o -CH2CH2-; R2a es -(alquilo C1-C3)R3; R2b es hidrogeno, halogeno, alquilo C1-C3 o -(alquilo C1-C3)R3; Rp es independientemente hidrogeno, halogeno o NH2; R3 es un anillo de fenilo o un anillo heteroarilo de 5 a 6 miembros que tiene 1-3 heteroatomos seleccionados de oxigeno, nitrogeno y azufre, en donde el anillo fenilo o anillo heteroarilo de 5 a 6 miembros estan opcionalmente sustituidos con 1 a 2 Rq; Rq es halogeno, ciano o -CF3. Dichos compuestos inhiben SARM1 y son utiles en el tratamiento de la neurodegeneracion como por ejemplo la inhibicion de la degeneracion axonal.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063069408P | 2020-08-24 | 2020-08-24 | |
| US202163142398P | 2021-01-27 | 2021-01-27 | |
| PCT/US2021/047093 WO2022046606A1 (en) | 2020-08-24 | 2021-08-23 | Inhibitors of sarm1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230737A1 true PE20230737A1 (es) | 2023-05-03 |
Family
ID=77775005
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023000530A PE20230737A1 (es) | 2020-08-24 | 2021-08-23 | Inhibidores de sarm1 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US12043613B2 (es) |
| EP (1) | EP4200293A1 (es) |
| JP (2) | JP7349046B2 (es) |
| KR (1) | KR20230057396A (es) |
| AU (2) | AU2021333558C1 (es) |
| BR (1) | BR112023002575A2 (es) |
| CA (1) | CA3189181A1 (es) |
| CL (1) | CL2023000525A1 (es) |
| CO (1) | CO2023001975A2 (es) |
| CR (1) | CR20230113A (es) |
| DO (1) | DOP2023000038A (es) |
| EC (1) | ECSP23012981A (es) |
| IL (1) | IL300586A (es) |
| MX (1) | MX2023002256A (es) |
| PE (1) | PE20230737A1 (es) |
| TW (2) | TW202334117A (es) |
| WO (1) | WO2022046606A1 (es) |
| ZA (1) | ZA202301801B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7212781B2 (ja) | 2018-12-19 | 2023-01-25 | 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 | 神経保護剤と組み合わせたｓａｒｍ１の阻害剤 |
| WO2022031736A1 (en) | 2020-08-04 | 2022-02-10 | Nura Bio, Inc. | Substituted pyridine derivatives as sarm1 inhibitors |
| EP4214197A1 (en) | 2020-09-16 | 2023-07-26 | Nura Bio, Inc. | Substituted pyridine derivatives as sarm1 inhibitors |
| TW202313009A (zh) | 2021-07-28 | 2023-04-01 | 美商努拉生物科技公司 | 作為sarm1抑制劑之經取代的吡啶衍生物 |
| US20240102018A1 (en) * | 2022-07-21 | 2024-03-28 | Amylyx Pharmaceuticals, Inc. | Oligonucleotide compositions and methods thereof |
| WO2024125624A1 (en) * | 2022-12-15 | 2024-06-20 | Sironax Ltd. | Sarm1 modulators, preparations, and uses thereof |
| WO2024158775A1 (en) | 2023-01-24 | 2024-08-02 | Disarm Therapeutics, Inc. | Pyridazines as sarm1 inhibitors |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2302417A1 (en) | 1997-10-27 | 1999-05-06 | Takeda Chemical Industries, 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 |
| ATE466855T1 (de) | 2002-10-30 | 2010-05-15 | Vertex Pharma | Zusammensetzungen verwendbar für die hemmung von rock und anderen kinasen |
| 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 |
| US7531556B2 (en) | 2004-04-28 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of rock and other protein kinases |
| 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 |
| WO2008001930A1 (fr) | 2006-06-28 | 2008-01-03 | Aska Pharmaceutical Co., Ltd. | Dérivé de pyridylisoxazole |
| US20100105664A1 (en) | 2006-09-21 | 2010-04-29 | Richard Heng | Organic compounds |
| AU2008340053A1 (en) | 2007-12-20 | 2009-07-02 | 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 |
| US20120328629A1 (en) | 2011-06-24 | 2012-12-27 | University Of Miami | Therapeutic Applications Targeting SARM1 |
| WO2014070978A1 (en) | 2012-11-03 | 2014-05-08 | 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. |
| WO2015084936A1 (en) | 2013-12-04 | 2015-06-11 | The Scripps Research Institute | Novel compounds as jnk kinase inhibitors |
| EP4091622A1 (en) | 2016-08-16 | 2022-11-23 | Henry Ford Health System | Compositions for the treatment of chemotherapy-induced neuropathic pain |
| 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 |
| JP2020503312A (ja) * | 2016-12-22 | 2020-01-30 | 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１，２，４−チアジアゾリルピロロンおよび１，２，４−チアジアゾリルヒダントイン、ならびにその塩、ならびにその除草剤としての使用 |
| MX2020006613A (es) * | 2017-12-22 | 2020-11-13 | Ravenna Pharmaceuticals Inc | Derivados de aril-bipiridina amina como inhibidores de fosfatidilinositol fosfato cinasa. |
| 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 |
| CA3102598A1 (en) | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| CA3102645A1 (en) | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| EP3919055A4 (en) * | 2019-01-30 | 2022-11-09 | Takeda Pharmaceutical Company Limited | HETEROCYCLIC COMPOUND |
| WO2020247701A2 (en) | 2019-06-06 | 2020-12-10 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| EP3982949A4 (en) | 2019-06-14 | 2023-10-11 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS |
| CN114341116A (zh) | 2019-07-22 | 2022-04-12 | 拜耳公司 | 5-氨基取代的吡唑和三唑作为杀虫剂 |
| CA3150878A1 (en) | 2019-09-12 | 2021-03-18 | Jonathan Bentley | Inhibitors of sarm1 |
| CA3159766A1 (en) | 2019-11-05 | 2021-05-14 | Dermira, Inc. | Mrgprx2 antagonists for the treatment of inflammatory disorders |
| KR20220164471A (ko) | 2020-01-07 | 2022-12-13 | 디스암 테라퓨틱스, 인크. | Sarm1의 억제제 |
| EP4132920A1 (en) | 2020-04-09 | 2023-02-15 | Disarm Therapeutics, Inc. | Indazole derivatives as inhibitors of sarm1 |
| CA3174320A1 (en) | 2020-04-09 | 2021-10-14 | Jonathan Bentley | Condensed pyrazole derivatives as inhibitors of sarm1 |
| WO2022031736A1 (en) * | 2020-08-04 | 2022-02-10 | Nura Bio, Inc. | Substituted pyridine derivatives as sarm1 inhibitors |
-
2021
- 2021-08-20 TW TW111144632A patent/TW202334117A/zh unknown
- 2021-08-20 TW TW110130799A patent/TWI786777B/zh active
- 2021-08-23 EP EP21770372.7A patent/EP4200293A1/en active Pending
- 2021-08-23 MX MX2023002256A patent/MX2023002256A/es unknown
- 2021-08-23 AU AU2021333558A patent/AU2021333558C1/en active Active
- 2021-08-23 US US17/408,956 patent/US12043613B2/en active Active
- 2021-08-23 CR CR20230113A patent/CR20230113A/es unknown
- 2021-08-23 BR BR112023002575A patent/BR112023002575A2/pt unknown
- 2021-08-23 PE PE2023000530A patent/PE20230737A1/es unknown
- 2021-08-23 WO PCT/US2021/047093 patent/WO2022046606A1/en active Application Filing
- 2021-08-23 KR KR1020237009643A patent/KR20230057396A/ko active Search and Examination
- 2021-08-23 IL IL300586A patent/IL300586A/en unknown
- 2021-08-23 CA CA3189181A patent/CA3189181A1/en active Pending
- 2021-08-23 JP JP2023513172A patent/JP7349046B2/ja 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 DO DO2023000038A patent/DOP2023000038A/es unknown
- 2023-02-23 EC ECSENADI202312981A patent/ECSP23012981A/es unknown
- 2023-09-08 JP JP2023145779A patent/JP2024016014A/ja active Pending
-
2024
- 2024-05-21 AU AU2024203373A patent/AU2024203373A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| ZA202301801B (en) | 2024-09-25 |
| AU2024203373A1 (en) | 2024-06-13 |
| AU2021333558C1 (en) | 2024-06-20 |
| JP2023535236A (ja) | 2023-08-16 |
| CR20230113A (es) | 2023-04-14 |
| WO2022046606A1 (en) | 2022-03-03 |
| BR112023002575A2 (pt) | 2023-03-07 |
| DOP2023000038A (es) | 2023-03-15 |
| JP2024016014A (ja) | 2024-02-06 |
| EP4200293A1 (en) | 2023-06-28 |
| TW202334117A (zh) | 2023-09-01 |
| KR20230057396A (ko) | 2023-04-28 |
| CO2023001975A2 (es) | 2023-03-07 |
| MX2023002256A (es) | 2023-03-17 |
| TWI786777B (zh) | 2022-12-11 |
| IL300586A (en) | 2023-04-01 |
| AU2021333558A1 (en) | 2023-03-02 |
| CA3189181A1 (en) | 2022-03-03 |
| CL2023000525A1 (es) | 2023-09-15 |
| ECSP23012981A (es) | 2023-03-31 |
| US20220056013A1 (en) | 2022-02-24 |
| US12043613B2 (en) | 2024-07-23 |
| JP7349046B2 (ja) | 2023-09-21 |
| TW202214597A (zh) | 2022-04-16 |
| AU2021333558B2 (en) | 2024-02-22 |
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