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
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- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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)
Abstract
En la presente se describen compuestos bifuncionales, que tienen utilidad como moduladores de la cinasa 2 repetida rica en leucina (LRRK2). En particular, los compuestos heterobifuncionales de la presente descripción contienen en un extremo un resto que se une a la ligasa de ubiquitina E3 Cereblon y en el otro extremo un resto que se une a LRRK2, de modo que la proteína seleccionada como diana se coloque cerca de la ligasa de ubiquitina para efectuar la degradación (e inhibición) de la proteína seleccionada como diana. Los compuestos heterobifuncionales de la presente descripción presentan una amplia gama de actividades farmacológicas asociadas con degradación/inhibición de una proteína seleccionada como diana. Las enfermedades o trastornos que resultan de la regulación anómala de la proteína seleccionada como diana se tratan o previenen con compuestos y composiciones de la presente descripción.
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 (1) | US20210315896A1 (es) |
| EP (1) | EP4121422A1 (es) |
| JP (1) | JP2023518830A (es) |
| KR (1) | KR20230004511A (es) |
| CN (1) | CN115697990A (es) |
| AU (1) | AU2021244180A1 (es) |
| BR (1) | BR112022018909A2 (es) |
| CA (1) | CA3172387A1 (es) |
| CO (1) | CO2022014718A2 (es) |
| IL (1) | IL296648A (es) |
| MX (1) | MX2022011674A (es) |
| WO (1) | WO2021194879A1 (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20230449A (es) | 2021-03-19 | 2023-11-23 | Arvinas Operations Inc | Compuestos a base de indazol y métodos de uso asociados |
| CN116003418A (zh) * | 2021-10-22 | 2023-04-25 | 标新生物医药科技(上海)有限公司 | Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 |
| 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 |
Family Cites Families (12)
| 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 |
| SI2576541T1 (sl) * | 2010-06-04 | 2016-07-29 | F. Hoffmann-La Roche Ag | Aminopirimidinski derivati kot modulatorji lrrk2 |
| RU2666530C2 (ru) | 2012-01-12 | 2018-09-11 | Йейл Юниверсити | Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы |
| 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 |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| WO2015160845A2 (en) | 2014-04-14 | 2015-10-22 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US20190374657A1 (en) * | 2017-02-08 | 2019-12-12 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation with heterobifunctional compounds |
| EP3866801A4 (en) * | 2018-10-16 | 2022-11-09 | Dana-Farber Cancer Institute, Inc. | DEGRADING AGENTS OF WILD-TYPE AND MUTANT FORMS OF LRRK2 KINASE |
-
2021
- 2021-03-19 IL IL296648A patent/IL296648A/en unknown
- 2021-03-19 EP EP21719336.6A patent/EP4121422A1/en active Pending
- 2021-03-19 US US17/207,325 patent/US20210315896A1/en active Pending
- 2021-03-19 CA CA3172387A patent/CA3172387A1/en active Pending
- 2021-03-19 KR KR1020227036283A patent/KR20230004511A/ko unknown
- 2021-03-19 CN CN202180035521.9A patent/CN115697990A/zh active Pending
- 2021-03-19 BR BR112022018909A patent/BR112022018909A2/pt not_active Application Discontinuation
- 2021-03-19 JP JP2022557169A patent/JP2023518830A/ja active Pending
- 2021-03-19 AU AU2021244180A patent/AU2021244180A1/en active Pending
- 2021-03-19 MX MX2022011674A patent/MX2022011674A/es unknown
- 2021-03-19 WO PCT/US2021/023183 patent/WO2021194879A1/en active Application Filing
-
2022
- 2022-10-18 CO CONC2022/0014718A patent/CO2022014718A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023518830A (ja) | 2023-05-08 |
| US20210315896A1 (en) | 2021-10-14 |
| MX2022011674A (es) | 2022-12-15 |
| CA3172387A1 (en) | 2021-09-30 |
| CN115697990A (zh) | 2023-02-03 |
| AU2021244180A1 (en) | 2022-11-03 |
| IL296648A (en) | 2022-11-01 |
| KR20230004511A (ko) | 2023-01-06 |
| BR112022018909A2 (pt) | 2022-12-13 |
| EP4121422A1 (en) | 2023-01-25 |
| WO2021194879A1 (en) | 2021-09-30 |
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