PE20220016A1 - Inhibidores y metodos de uso de kcnt1 - Google Patents
Inhibidores y metodos de uso de kcnt1Info
- Publication number
- PE20220016A1 PE20220016A1 PE2021001828A PE2021001828A PE20220016A1 PE 20220016 A1 PE20220016 A1 PE 20220016A1 PE 2021001828 A PE2021001828 A PE 2021001828A PE 2021001828 A PE2021001828 A PE 2021001828A PE 20220016 A1 PE20220016 A1 PE 20220016A1
- Authority
- PE
- Peru
- Prior art keywords
- oxadiazol
- carboxamide
- pyrazole
- methyl
- kcnt1
- Prior art date
Links
- 101000944018 Homo sapiens Potassium channel subfamily T member 1 Proteins 0.000 title abstract 2
- 102100033508 Potassium channel subfamily T member 1 Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010015037 epilepsy Diseases 0.000 abstract 3
- CLINQEGUIZAEPS-GFCCVEGCSA-N 5-cyclopropyl-2-methyl-N-[(1R)-1-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]ethyl]pyrazole-3-carboxamide Chemical compound N([C@H](C)C=1ON=C(N=1)C=1C=C(C)C=CC=1)C(=O)C(N(N=1)C)=CC=1C1CC1 CLINQEGUIZAEPS-GFCCVEGCSA-N 0.000 abstract 1
- 208000014644 Brain disease Diseases 0.000 abstract 1
- 206010010904 Convulsion Diseases 0.000 abstract 1
- 208000032274 Encephalopathy Diseases 0.000 abstract 1
- 206010061334 Partial seizures Diseases 0.000 abstract 1
- 230000001617 migratory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE UN COMPUESTO DE FORMULA (I) DONDE X, Y, Z, Y', Z', R1, R2, R3, R4, R5, R12, n Y x SON TAL COMO SE DEFINEN EN LA DESCRIPCION. SON COMPUESTOS PREFERIDOS: (R)-3-CICLOPROPIL-1-METIL-N-(1-(3-(M-TOLIL)-1,2,4-OXADIAZOL-5-IL)ETIL)-1H-PIRAZOL-5-CARBOXAMIDA; N-(1-(3-(3-HIDROXIFENIL)-1,2,4-OXADIAZOL-5-IL)ETIL)-1-METIL-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDA; (S)-1-METIL-N-(1-(3-(2-METILPIRIDIN-4-IL)-1,2,4-OXADIAZOL-5-IL)PROPIL)-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDA; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE KCNT1 SIENDO UTILES EN EL TRATAMIENTO DE EPILEPSIA Y OTRAS ENCEFALOPATIAS TAL COMO EPILEPSIA DE LA INFANCIA CON CONVULSIONES FOCALES MIGRATORIAS, EPILEPSIA DEL LOBULO FRONTAL NOCTURNA AUTOSOMICA DOMINANTE.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962842849P | 2019-05-03 | 2019-05-03 | |
| US202062982864P | 2020-02-28 | 2020-02-28 | |
| PCT/US2020/031046 WO2020227101A1 (en) | 2019-05-03 | 2020-05-01 | Kcnt1 inhibitors and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220016A1 true PE20220016A1 (es) | 2022-01-11 |
Family
ID=73051241
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001828A PE20220016A1 (es) | 2019-05-03 | 2020-05-01 | Inhibidores y metodos de uso de kcnt1 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20220259193A1 (es) |
| EP (1) | EP3962481A4 (es) |
| JP (2) | JP7667573B2 (es) |
| KR (1) | KR20220016086A (es) |
| CN (2) | CN114269340A (es) |
| AU (1) | AU2020267356B2 (es) |
| BR (1) | BR112021022067A2 (es) |
| CA (1) | CA3139063A1 (es) |
| CL (2) | CL2021002877A1 (es) |
| CO (1) | CO2021016471A2 (es) |
| EC (1) | ECSP21087884A (es) |
| IL (1) | IL287768A (es) |
| MX (1) | MX2021013421A (es) |
| PE (1) | PE20220016A1 (es) |
| SA (1) | SA521430751B1 (es) |
| SG (1) | SG11202112158YA (es) |
| WO (1) | WO2020227101A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114206335B (zh) * | 2019-05-03 | 2025-03-11 | 普拉克西斯精密药物股份有限公司 | Kcnt1抑制剂和使用方法 |
| CN115443129A (zh) * | 2020-02-28 | 2022-12-06 | 普拉西斯精密医药公司 | Kcnt1抑制剂和使用方法 |
| EP4210824A1 (en) * | 2020-09-09 | 2023-07-19 | University of Virginia Patent Foundation | Inhibitors of spinster homolog 2 (spns2) for use in therapy |
| US11773088B2 (en) | 2020-11-02 | 2023-10-03 | Praxis Precision Medicines, Inc. | KCNT1 inhibitors and methods of use |
| WO2022111605A1 (zh) * | 2020-11-27 | 2022-06-02 | 瑞石生物医药有限公司 | 芳基或杂芳基取代五元芳杂环化合物及其用途 |
| EP4267133A4 (en) * | 2020-12-22 | 2025-01-22 | Praxis Precision Medicines, Inc. | KCNT1 INHIBITORS AND METHODS OF USE |
| WO2022231872A1 (en) * | 2021-04-29 | 2022-11-03 | Praxis Precision Medicines, Inc. | Kcnt1 inhibitors and methods of use |
| EP4329735A4 (en) * | 2021-04-29 | 2025-03-05 | Praxis Precision Medicines, Inc. | KCNT1 INHIBITORS AND METHODS OF USE |
| WO2023211850A1 (en) * | 2022-04-25 | 2023-11-02 | Praxis Precision Medicines, Inc. | Kcnt1 inhibitors comprising an isoxazole or oxadiazole core and methods of use |
| EP4536644A1 (en) * | 2022-06-08 | 2025-04-16 | Praxis Precision Medicines, Inc. | Kcnt1 inhibitors comprising an isoxazole or oxadiazole core and methods of use |
| CN116813505B (zh) * | 2023-06-29 | 2025-09-02 | 爱斯特（成都）生物制药股份有限公司 | 一种制备o-甲基-n-苄氧羰基-l-高丝氨酸的方法 |
| WO2025117662A1 (en) * | 2023-11-29 | 2025-06-05 | Actio Biosciences, Inc. | Heterocyclic compounds useful as kcnt1 inhibitors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| TW200301698A (en) * | 2001-12-21 | 2003-07-16 | Bristol Myers Squibb Co | Acridone inhibitors of IMPDH enzyme |
| JP2005060255A (ja) * | 2003-08-20 | 2005-03-10 | Nippon Nohyaku Co Ltd | カルボキサミド類及びこれを有効成分とする有害生物防除剤 |
| US7585881B2 (en) * | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| US20080021217A1 (en) * | 2006-07-20 | 2008-01-24 | Allen Borchardt | Heterocyclic inhibitors of rho kinase |
| GEP201706699B (en) * | 2013-03-14 | 2017-07-10 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| SG11201702483QA (en) | 2014-09-29 | 2017-04-27 | Scripps Research Inst | Sphingosine-1-phospate receptor modulators for treatment of cardiopulmonary disorders |
| US10538516B2 (en) * | 2015-03-25 | 2020-01-21 | National Center For Geriatrics And Gerontology | Oxadiazole derivative and pharmaceutical containing same |
| WO2017170826A1 (ja) * | 2016-03-30 | 2017-10-05 | 味の素株式会社 | グルカゴン様ペプチド－１受容体作用増強活性を有する化合物 |
| WO2018187480A1 (en) * | 2017-04-04 | 2018-10-11 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| CN115443129A (zh) * | 2020-02-28 | 2022-12-06 | 普拉西斯精密医药公司 | Kcnt1抑制剂和使用方法 |
| BR112022019041A2 (pt) * | 2020-03-23 | 2022-12-27 | Praxis Prec Medicines Inc | Inibidores de kcnt1 e métodos de uso |
| EP4175624A4 (en) * | 2020-07-06 | 2024-08-07 | Praxis Precision Medicines, Inc. | Kcnt1 inhibitors and methods of use |
| US11773088B2 (en) * | 2020-11-02 | 2023-10-03 | Praxis Precision Medicines, Inc. | KCNT1 inhibitors and methods of use |
| EP4267133A4 (en) * | 2020-12-22 | 2025-01-22 | Praxis Precision Medicines, Inc. | KCNT1 INHIBITORS AND METHODS OF USE |
| EP4329735A4 (en) * | 2021-04-29 | 2025-03-05 | Praxis Precision Medicines, Inc. | KCNT1 INHIBITORS AND METHODS OF USE |
-
2020
- 2020-05-01 US US17/607,802 patent/US20220259193A1/en active Pending
- 2020-05-01 CA CA3139063A patent/CA3139063A1/en active Pending
- 2020-05-01 PE PE2021001828A patent/PE20220016A1/es unknown
- 2020-05-01 EP EP20801870.5A patent/EP3962481A4/en active Pending
- 2020-05-01 WO PCT/US2020/031046 patent/WO2020227101A1/en not_active Ceased
- 2020-05-01 KR KR1020217039174A patent/KR20220016086A/ko active Pending
- 2020-05-01 BR BR112021022067A patent/BR112021022067A2/pt unknown
- 2020-05-01 CN CN202080047961.1A patent/CN114269340A/zh active Pending
- 2020-05-01 JP JP2021564995A patent/JP7667573B2/ja active Active
- 2020-05-01 CN CN202510784123.7A patent/CN120817941A/zh active Pending
- 2020-05-01 MX MX2021013421A patent/MX2021013421A/es unknown
- 2020-05-01 AU AU2020267356A patent/AU2020267356B2/en active Active
- 2020-05-01 SG SG11202112158YA patent/SG11202112158YA/en unknown
-
2021
- 2021-11-01 IL IL287768A patent/IL287768A/en unknown
- 2021-11-02 CL CL2021002877A patent/CL2021002877A1/es unknown
- 2021-11-03 SA SA521430751A patent/SA521430751B1/ar unknown
- 2021-12-02 CO CONC2021/0016471A patent/CO2021016471A2/es unknown
- 2021-12-03 EC ECSENADI202187884A patent/ECSP21087884A/es unknown
-
2024
- 2024-07-08 CL CL2024002067A patent/CL2024002067A1/es unknown
-
2025
- 2025-04-04 JP JP2025062493A patent/JP2025102975A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022531388A (ja) | 2022-07-06 |
| CA3139063A1 (en) | 2020-11-12 |
| EP3962481A4 (en) | 2023-03-22 |
| JP7667573B2 (ja) | 2025-04-23 |
| IL287768A (en) | 2022-01-01 |
| SG11202112158YA (en) | 2021-12-30 |
| WO2020227101A1 (en) | 2020-11-12 |
| CL2024002067A1 (es) | 2024-12-13 |
| ECSP21087884A (es) | 2022-01-31 |
| US20220259193A1 (en) | 2022-08-18 |
| SA521430751B1 (ar) | 2024-02-01 |
| KR20220016086A (ko) | 2022-02-08 |
| MX2021013421A (es) | 2022-02-11 |
| BR112021022067A2 (pt) | 2022-05-17 |
| CN120817941A (zh) | 2025-10-21 |
| CN114269340A (zh) | 2022-04-01 |
| AU2020267356A1 (en) | 2022-01-06 |
| EP3962481A1 (en) | 2022-03-09 |
| CO2021016471A2 (es) | 2022-04-08 |
| JP2025102975A (ja) | 2025-07-08 |
| CL2021002877A1 (es) | 2022-08-12 |
| AU2020267356B2 (en) | 2025-04-24 |
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