CO2022014718A2 - Compuestos a base de indazol y métodos de uso asociados - Google Patents
Compuestos a base de indazol y métodos de uso asociadosInfo
- Publication number
- CO2022014718A2 CO2022014718A2 CONC2022/0014718A CO2022014718A CO2022014718A2 CO 2022014718 A2 CO2022014718 A2 CO 2022014718A2 CO 2022014718 A CO2022014718 A CO 2022014718A CO 2022014718 A2 CO2022014718 A2 CO 2022014718A2
- Authority
- CO
- Colombia
- Prior art keywords
- targeted protein
- compounds
- present disclosure
- lrrk2
- binds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 abstract 4
- 108090000623 proteins and genes Proteins 0.000 abstract 4
- 101000941879 Homo sapiens Leucine-rich repeat serine/threonine-protein kinase 2 Proteins 0.000 abstract 3
- 102100032693 Leucine-rich repeat serine/threonine-protein kinase 2 Human genes 0.000 abstract 3
- 230000015556 catabolic process Effects 0.000 abstract 2
- 238000006731 degradation reaction Methods 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 102100032783 Protein cereblon Human genes 0.000 abstract 1
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000001588 bifunctional effect Effects 0.000 abstract 1
- 230000033228 biological regulation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062992952P | 2020-03-21 | 2020-03-21 | |
| PCT/US2021/023183 WO2021194879A1 (en) | 2020-03-21 | 2021-03-19 | Indazole based compounds and associated methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2022014718A2 true CO2022014718A2 (es) | 2022-10-31 |
Family
ID=75539924
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2022/0014718A CO2022014718A2 (es) | 2020-03-21 | 2022-10-18 | Compuestos a base de indazol y métodos de uso asociados |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US12053469B2 (https=) |
| EP (1) | EP4121422A1 (https=) |
| JP (2) | JP7644139B2 (https=) |
| KR (1) | KR20230004511A (https=) |
| CN (1) | CN115697990B (https=) |
| AU (1) | AU2021244180A1 (https=) |
| BR (1) | BR112022018909A2 (https=) |
| CA (1) | CA3172387A1 (https=) |
| CO (1) | CO2022014718A2 (https=) |
| IL (1) | IL296648A (https=) |
| MX (1) | MX2022011674A (https=) |
| WO (1) | WO2021194879A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10654809B2 (en) | 2016-06-10 | 2020-05-19 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| JP7644139B2 (ja) | 2020-03-21 | 2025-03-11 | アルヴィナス・オペレーションズ・インコーポレイテッド | インダゾール系化合物及び関連使用方法 |
| WO2021194878A1 (en) * | 2020-03-21 | 2021-09-30 | Arvinas Operations, Inc. | Selective modulators of mutant lrrk2 proteolysis and associated methods of use |
| CN117321046A (zh) * | 2021-03-19 | 2023-12-29 | 阿维纳斯企业公司 | 基于吲唑的化合物和相关使用方法 |
| JP2024512501A (ja) * | 2021-03-19 | 2024-03-19 | アルヴィナス・オペレーションズ・インコーポレイテッド | インダゾール系化合物及び関連使用方法 |
| CA3235512A1 (en) * | 2021-10-22 | 2023-04-27 | Xiaobao Yang | Crbn e3 ligase ligand compound, protein degrader developed based thereon and their applications |
| EP4276097A1 (en) | 2022-05-10 | 2023-11-15 | University Of Dundee | Aminopyrimidinyl derivatives for the treament of parkinson's disease |
| WO2024010818A2 (en) * | 2022-07-07 | 2024-01-11 | University Of Tennessee Research Foundation | Proteolysis targeting chimera (protac) of selective androgen receptor degrader (sard) compounds and methods of use thereof |
| WO2024054876A1 (en) * | 2022-09-07 | 2024-03-14 | Arvinas Operations, Inc. | Leucine rich repeat kinase 2 (lrrk2) degrading compounds and associated methods of use |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
| WO2024173646A1 (en) * | 2023-02-16 | 2024-08-22 | Innovo Therapeutics, Inc. | Cyclin-dependent kinase degrading compounds |
| WO2025056074A1 (zh) * | 2023-09-14 | 2025-03-20 | 中国科学院上海药物研究所 | 杂环基取代的吲唑酮类化合物、其制备方法、药物组合物及其应用 |
| TW202515874A (zh) | 2023-09-28 | 2025-04-16 | 美商亞文納營運公司 | 用於靶向降解富含白胺酸之重複激酶２（ｌｒｒｋ２）的基於苯并咪唑及苯并咪唑酮之ｐｒｏｔａｃ化合物 |
| WO2025123046A1 (en) | 2023-12-07 | 2025-06-12 | Arvinas Operations, Inc. | Synthesis of leucine-rich repeat kinase 2 modulators |
| CN120787222A (zh) * | 2024-02-04 | 2025-10-14 | 标新生物医药科技(上海)有限公司 | 基于取代的异吲哚啉酮新颖骨架化合物、含有其的双功能蛋白降解剂及它们的应用 |
| CN118344284A (zh) * | 2024-03-06 | 2024-07-16 | 杭州医学院 | 一种具有苯甲酰胺结构的化合物及其制备方法和应用 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| ES2577829T3 (es) | 2010-06-04 | 2016-07-19 | F. Hoffmann-La Roche Ag | Derivados de aminopirimidina como moduladores de la LRRK2 |
| KR102668696B1 (ko) | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| WO2014134774A1 (en) | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| WO2014134776A1 (en) | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| US9718818B2 (en) | 2013-08-22 | 2017-08-01 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| RU2738833C9 (ru) | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| MX2019005007A (es) * | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| AU2018219292B2 (en) * | 2017-02-08 | 2024-09-26 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation with heterobifunctional compounds |
| WO2019060742A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc | AGENTS FOR DEGRADING PROTEINS AND USES THEREOF |
| IL302595A (en) | 2018-04-13 | 2023-07-01 | Arvinas Operations Inc | Servalon ligands and bifunctional compounds containing them |
| US20210261553A1 (en) | 2018-05-15 | 2021-08-26 | E-Scape Bio, Inc. | Fused tetrazoles as lrrk2 inhibitors |
| JP7297053B2 (ja) * | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| US20210361774A1 (en) | 2018-10-16 | 2021-11-25 | Dana-Farber Cancer Institute, Inc. | Degraders of wild-type and mutant forms of lrrk2 |
| US20230219945A1 (en) | 2019-12-17 | 2023-07-13 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| JP7644139B2 (ja) | 2020-03-21 | 2025-03-11 | アルヴィナス・オペレーションズ・インコーポレイテッド | インダゾール系化合物及び関連使用方法 |
| WO2021194878A1 (en) * | 2020-03-21 | 2021-09-30 | Arvinas Operations, Inc. | Selective modulators of mutant lrrk2 proteolysis and associated methods of use |
| JP2024512501A (ja) * | 2021-03-19 | 2024-03-19 | アルヴィナス・オペレーションズ・インコーポレイテッド | インダゾール系化合物及び関連使用方法 |
-
2021
- 2021-03-19 JP JP2022557169A patent/JP7644139B2/ja active Active
- 2021-03-19 WO PCT/US2021/023183 patent/WO2021194879A1/en not_active Ceased
- 2021-03-19 CN CN202180035521.9A patent/CN115697990B/zh active Active
- 2021-03-19 KR KR1020227036283A patent/KR20230004511A/ko not_active Withdrawn
- 2021-03-19 US US17/207,325 patent/US12053469B2/en active Active
- 2021-03-19 BR BR112022018909A patent/BR112022018909A2/pt not_active Application Discontinuation
- 2021-03-19 AU AU2021244180A patent/AU2021244180A1/en not_active Abandoned
- 2021-03-19 EP EP21719336.6A patent/EP4121422A1/en active Pending
- 2021-03-19 IL IL296648A patent/IL296648A/en unknown
- 2021-03-19 CA CA3172387A patent/CA3172387A1/en active Pending
- 2021-03-19 MX MX2022011674A patent/MX2022011674A/es unknown
-
2022
- 2022-10-18 CO CONC2022/0014718A patent/CO2022014718A2/es unknown
-
2024
- 2024-08-05 US US18/794,292 patent/US20250114356A1/en active Pending
-
2025
- 2025-02-27 JP JP2025030446A patent/JP2025078673A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021194879A1 (en) | 2021-09-30 |
| US12053469B2 (en) | 2024-08-06 |
| KR20230004511A (ko) | 2023-01-06 |
| US20250114356A1 (en) | 2025-04-10 |
| CN115697990A (zh) | 2023-02-03 |
| EP4121422A1 (en) | 2023-01-25 |
| MX2022011674A (es) | 2022-12-15 |
| CN115697990B (zh) | 2025-06-13 |
| JP7644139B2 (ja) | 2025-03-11 |
| JP2023518830A (ja) | 2023-05-08 |
| JP2025078673A (ja) | 2025-05-20 |
| IL296648A (en) | 2022-11-01 |
| AU2021244180A1 (en) | 2022-11-03 |
| BR112022018909A2 (pt) | 2022-12-13 |
| US20210315896A1 (en) | 2021-10-14 |
| CA3172387A1 (en) | 2021-09-30 |
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