PE20211975A1 - DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3 - Google Patents
DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3Info
- Publication number
- PE20211975A1 PE20211975A1 PE2021000636A PE2021000636A PE20211975A1 PE 20211975 A1 PE20211975 A1 PE 20211975A1 PE 2021000636 A PE2021000636 A PE 2021000636A PE 2021000636 A PE2021000636 A PE 2021000636A PE 20211975 A1 PE20211975 A1 PE 20211975A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- alkoxy
- potassium channels
- arylsulfonylpirrolcarboxamide
- activators
- Prior art date
Links
- 102000004536 Shaw Potassium Channels Human genes 0.000 title abstract 2
- 108010017604 Shaw Potassium Channels Proteins 0.000 title abstract 2
- 239000012190 activator Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- SYXXDQBJFICKFJ-UHFFFAOYSA-N 1-(2-fluorophenyl)sulfonyl-N-[(5-methylpyrazin-2-yl)methyl]pyrrole-3-carboxamide Chemical compound FC1=C(C=CC=C1)S(=O)(=O)N1C=C(C=C1)C(=O)NCC1=NC=C(N=C1)C SYXXDQBJFICKFJ-UHFFFAOYSA-N 0.000 abstract 1
- -1 5-methylpyrimidin-2-yl Chemical group 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000029560 autism spectrum disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- A61K31/33—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/505—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
-
- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
- C07D413/02—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Esta referido a compuestos de Formula I, en donde: R1 es H, alquilo, fluoroalquilo, alcoxi, entre otros; R2, R6 son H, alquilo, alcoxi, halogeno; R3 es H, F, alquilo; R4, R5 son H, F; R7 es H, alquilo, halogeno, alcoxi, fluoroalquilo, fluoroalcoxi, alquil-amino; Y es O, S; HetAr es heteroarilo de 5 o 6 miembros, sistema anular heteroaromatico biciclico. Entre los compuestos preferidos tenemos los siguientes: N-[(5-metilpirimidin-2-il)metil]-1-(p-tolilsulfonil)pirrol-3-carboxamida; 1-(2-fluorofenil)sulfonil-N-[(5-metilpirazin-2- il)metil]pirrol-3-carboxamida; entre otros. Estos compuestos activan los canales de potasio Kv3 y se emplean en el tratamiento de la epilepsia, esquizofrenia, trastorno del espectro autista, trastorno bipolar, trastornos relacionados con la ansiedad, depresion, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201800787 | 2018-10-30 | ||
| PCT/EP2019/079587 WO2020089262A1 (en) | 2018-10-30 | 2019-10-30 | Arylsulfonylpyrolecarboxamide derivatives as kv3 potassium channel activators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211975A1 true PE20211975A1 (es) | 2021-10-05 |
Family
ID=70327875
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000636A PE20211975A1 (es) | 2018-10-30 | 2019-10-30 | DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20200131156A1 (es) |
| EP (1) | EP3873891A1 (es) |
| JP (1) | JP2022509416A (es) |
| KR (1) | KR20210086661A (es) |
| CN (1) | CN113056461A (es) |
| AR (1) | AR116898A1 (es) |
| AU (1) | AU2019373367A1 (es) |
| BR (1) | BR112020013011A2 (es) |
| CA (1) | CA3116273A1 (es) |
| CL (1) | CL2021001123A1 (es) |
| CO (1) | CO2021005579A2 (es) |
| CR (1) | CR20210285A (es) |
| DO (1) | DOP2021000081A (es) |
| EA (1) | EA202190899A1 (es) |
| EC (1) | ECSP21038534A (es) |
| IL (1) | IL282639A (es) |
| JO (1) | JOP20210091A1 (es) |
| MA (1) | MA54061A (es) |
| MX (1) | MX2021004935A (es) |
| PE (1) | PE20211975A1 (es) |
| PH (1) | PH12021550957A1 (es) |
| SG (1) | SG11202104348XA (es) |
| TW (1) | TW202031645A (es) |
| WO (1) | WO2020089262A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12358901B2 (en) | 2018-10-16 | 2025-07-15 | Autifony Therapeutics Limited | KV3 modulators |
| US20220220095A1 (en) * | 2019-04-26 | 2022-07-14 | H. Lundbeck A/S | N-((HETEROARYL)METHYL)-1-TOSYL-1H-PYRAZOLE-3-CARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS FOR TREATING NEUROLOGICAL AND PSYCHIATRIC DISORDERS |
| EP4384504A1 (en) | 2021-08-10 | 2024-06-19 | Autifony Therapeutics Limited | Potassium channel modulators |
| EP4630117A1 (en) | 2022-12-06 | 2025-10-15 | Autifony Therapeutics Limited | Compounds for the treatment of centra nervous system disorders |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009003921A1 (en) * | 2007-07-04 | 2009-01-08 | Neurosearch A/S | Novel pyrazole derivatives useful as potassium channel modulators |
| TW201028421A (en) * | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
| WO2011073269A1 (en) * | 2009-12-16 | 2011-06-23 | Evotec Ag | Piperidine aryl sulfonamide derivatives as kv1.3 modulators |
| WO2011073276A1 (en) * | 2009-12-16 | 2011-06-23 | Evotec Ag | Benzoxazine aryl sulfonamide derivatives as kv1.3 modulators |
| US9290485B2 (en) * | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| FR2967674B1 (fr) * | 2010-11-23 | 2012-12-14 | Pf Medicament | Derives d'heteroarylsulfonamides, leur preparation et leur application en therapeutique humaine |
| CA2862289C (en) * | 2012-02-10 | 2019-11-26 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9422252B2 (en) * | 2012-05-22 | 2016-08-23 | Autifony Therapeutics Limited | Triazoles as Kv3 inhibitors |
| GB201521751D0 (en) * | 2015-12-10 | 2016-01-27 | Autifony Therapeutics Ltd | Novel uses |
| GB201522179D0 (en) | 2015-12-16 | 2016-01-27 | Autifony Therapeutics Ltd | Novel compounds |
| GB201613163D0 (en) * | 2016-07-29 | 2016-09-14 | Autifony Therapeutics Ltd | Novel compounds |
-
2019
- 2019-10-29 TW TW108139051A patent/TW202031645A/zh unknown
- 2019-10-29 US US16/667,563 patent/US20200131156A1/en not_active Abandoned
- 2019-10-29 AR ARP190103138A patent/AR116898A1/es not_active Application Discontinuation
- 2019-10-30 CN CN201980071046.3A patent/CN113056461A/zh active Pending
- 2019-10-30 JP JP2021547926A patent/JP2022509416A/ja active Pending
- 2019-10-30 EA EA202190899A patent/EA202190899A1/ru unknown
- 2019-10-30 KR KR1020217015490A patent/KR20210086661A/ko not_active Withdrawn
- 2019-10-30 MA MA054061A patent/MA54061A/fr unknown
- 2019-10-30 SG SG11202104348XA patent/SG11202104348XA/en unknown
- 2019-10-30 BR BR112020013011-7A patent/BR112020013011A2/pt not_active Application Discontinuation
- 2019-10-30 CA CA3116273A patent/CA3116273A1/en not_active Abandoned
- 2019-10-30 PE PE2021000636A patent/PE20211975A1/es unknown
- 2019-10-30 CR CR20210285A patent/CR20210285A/es unknown
- 2019-10-30 PH PH1/2021/550957A patent/PH12021550957A1/en unknown
- 2019-10-30 EP EP19798210.1A patent/EP3873891A1/en not_active Withdrawn
- 2019-10-30 MX MX2021004935A patent/MX2021004935A/es unknown
- 2019-10-30 AU AU2019373367A patent/AU2019373367A1/en not_active Abandoned
- 2019-10-30 WO PCT/EP2019/079587 patent/WO2020089262A1/en not_active Ceased
- 2019-10-30 JO JOP/2021/0091A patent/JOP20210091A1/ar unknown
-
2021
- 2021-04-26 IL IL282639A patent/IL282639A/en unknown
- 2021-04-28 CO CONC2021/0005579A patent/CO2021005579A2/es unknown
- 2021-04-29 DO DO2021000081A patent/DOP2021000081A/es unknown
- 2021-04-29 CL CL2021001123A patent/CL2021001123A1/es unknown
- 2021-05-28 EC ECSENADI202138534A patent/ECSP21038534A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3116273A1 (en) | 2020-05-07 |
| CR20210285A (es) | 2021-09-16 |
| IL282639A (en) | 2021-06-30 |
| JP2022509416A (ja) | 2022-01-20 |
| AR116898A1 (es) | 2021-06-23 |
| BR112020013011A2 (pt) | 2021-05-04 |
| EA202190899A1 (ru) | 2021-08-19 |
| PH12021550957A1 (en) | 2022-05-02 |
| CN113056461A (zh) | 2021-06-29 |
| WO2020089262A1 (en) | 2020-05-07 |
| JOP20210091A1 (ar) | 2023-01-30 |
| MA54061A (fr) | 2021-12-15 |
| AU2019373367A1 (en) | 2021-05-27 |
| DOP2021000081A (es) | 2021-07-30 |
| KR20210086661A (ko) | 2021-07-08 |
| CL2021001123A1 (es) | 2021-10-22 |
| MX2021004935A (es) | 2021-06-08 |
| ECSP21038534A (es) | 2021-06-30 |
| SG11202104348XA (en) | 2021-05-28 |
| US20200131156A1 (en) | 2020-04-30 |
| CO2021005579A2 (es) | 2021-05-10 |
| EP3873891A1 (en) | 2021-09-08 |
| TW202031645A (zh) | 2020-09-01 |
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