AR122593A1 - Compuestos de dihidroquinolinsulfonamida de ciclopropilo - Google Patents
Compuestos de dihidroquinolinsulfonamida de ciclopropiloInfo
- Publication number
- AR122593A1 AR122593A1 ARP210101587A ARP210101587A AR122593A1 AR 122593 A1 AR122593 A1 AR 122593A1 AR P210101587 A ARP210101587 A AR P210101587A AR P210101587 A ARP210101587 A AR P210101587A AR 122593 A1 AR122593 A1 AR 122593A1
- Authority
- AR
- Argentina
- Prior art keywords
- alk
- compounds
- haloalk
- formula
- cyclopropyl
- Prior art date
Links
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
- C07D401/02—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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención proporciona un compuesto de fórmula I, (I); un enantiómero, diastereoisómero, atropisómero del mismo, una mezcla de los mismos, o una sal farmacéuticamente aceptable del mismo, que inhibe los canales de sodio activados por voltaje, en particular NaV1.7. Los compuestos son útiles para el tratamiento de enfermedades asociadas con la actividad de los canales de sodio tales como trastornos del dolor, tos y picazón. También se proporcionan composiciones farmacéuticas que contienen los compuestos de la presente invención. También se proporciona además una preparación atropi-selectiva de dichos compuestos de fórmula (1), y un producto intermedio de los mismos. Reivindicación 1: Un compuesto de fórmula (1); un enantiómero, diastereoisómero, atropisómero del mismo, una mezcla de los mismos, o una sal farmacéuticamente aceptable del mismo, donde: R¹ es un anillo ciclopropilo; o un anillo bicíclico de 4, 5, 6, 7, ó 8 miembros que contiene 0, 1, 2 ó 3 átomos de N y 0, 1, ó 2 átomos seleccionados de O y S; y donde dicho anillo ciclopropilo o anillo bicíclico está sustituido por 0, 1, 2 ó 3 grupos R¹ᵃ seleccionados de hidroxilo, halo, alq C₁₋₈, haloalq C₁₋₈, -O-alq C₁₋₄, -O-haloalq C₁₋₈, -C(=O)-alq C₁₋₄, -O-C(=O)alq C₁₋₄, -NH₂, -NH-alq C₁₋₄, -N(alq C₁₋₄)alq C₁₋₄, cicloalquilo de 3, 4, ó 5 miembros, o arilo de 6 miembros; R² es H, halo, CN, alq C₁₋₆ o haloalq C₁₋₆; R³ es alq C₁₋₆, haloalq C₁₋₆, -O-alq C₁₋₆, -O-ciclopropilo, o -O-ciclobutilo; R⁴ es un heteroarilo de 5 a 6 miembros; cada uno de R⁶ y R⁷ es hidrógeno; y cada uno de R⁵ᵃ; R⁵ᵇ; R⁵ᶜ; R⁵ᵈ; y R⁵ᵉ es independientemente hidrógeno o halo; donde el compuesto no es de fórmula (2) o una sal o tautómero del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063036999P | 2020-06-10 | 2020-06-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR122593A1 true AR122593A1 (es) | 2022-09-21 |
Family
ID=76845312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210101587A AR122593A1 (es) | 2020-06-10 | 2021-06-10 | Compuestos de dihidroquinolinsulfonamida de ciclopropilo |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20230234948A1 (es) |
| EP (1) | EP4164748A1 (es) |
| JP (1) | JP2021195367A (es) |
| AR (1) | AR122593A1 (es) |
| AU (1) | AU2021289741A1 (es) |
| CA (1) | CA3183814A1 (es) |
| MX (1) | MX2022015622A (es) |
| TW (1) | TW202214587A (es) |
| UY (1) | UY39264A (es) |
| WO (1) | WO2021252818A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112023025264A2 (pt) | 2021-06-04 | 2024-02-20 | Vertex Pharma | Formas farmacêuticas sólidas e regimes posológicos compreendendo (2r,3s,4s,5r)-4-[[3- (3,4-difluoro-2-metóxi-fenil)-4,5-dimetil-5-(trifluorometil) tetra-hidrofuran-2-carbonil]amino ]piridina-2-carboxamida |
| WO2022256679A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| AR126073A1 (es) | 2021-06-04 | 2023-09-06 | Vertex Pharma | N-(hidroxialquil(hetero)aril)tetrahidrofuran carboxamidas como moduladores de canales de sodio |
| WO2022256676A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| AU2022283934A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| WO2022256842A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| US20230373925A1 (en) | 2022-04-22 | 2023-11-23 | Vertex Pharma | Heteroaryl compounds for the treatment of pain |
| WO2023205468A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2023205465A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| AR129116A1 (es) | 2022-04-22 | 2024-07-17 | Vertex Pharma | Compuestos de heteroarilo para el tratamiento del dolor |
| WO2024123815A1 (en) | 2022-12-06 | 2024-06-13 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| US4412994A (en) | 1980-04-24 | 1983-11-01 | Interx Research Corporation | Mannich-base hydroxamic acid prodrugs, compositions and use |
| GT200600381A (es) | 2005-08-25 | 2007-03-28 | Compuestos organicos | |
| CA2741024A1 (en) | 2008-10-17 | 2010-04-22 | Xenon Pharmaceuticals Inc. | Spiro-oxindole compounds and their use as therapeutic agents |
| WO2013134518A1 (en) | 2012-03-09 | 2013-09-12 | Amgen Inc. | Sulfamide sodium channel inhibitors |
| WO2014201173A1 (en) | 2013-06-12 | 2014-12-18 | Amgen Inc. | Bicyclic sulfonamide compounds as sodium channel inhibitors |
| AR103833A1 (es) * | 2015-03-02 | 2017-06-07 | Amgen Inc | Compuestos bicíclicos de sulfonamida cetona |
| WO2017106871A1 (en) * | 2015-12-18 | 2017-06-22 | Amgen Inc. | Alkyl dihydroquinoline sulfonamide compounds |
| MA44066A (fr) * | 2015-12-18 | 2018-10-24 | Amgen Inc | Composés sulfonamides de dihydroquinoline d'alcynyle |
-
2021
- 2021-05-31 JP JP2021090941A patent/JP2021195367A/ja active Pending
- 2021-06-10 WO PCT/US2021/036894 patent/WO2021252818A1/en unknown
- 2021-06-10 EP EP21739831.2A patent/EP4164748A1/en active Pending
- 2021-06-10 AR ARP210101587A patent/AR122593A1/es unknown
- 2021-06-10 AU AU2021289741A patent/AU2021289741A1/en active Pending
- 2021-06-10 US US18/009,682 patent/US20230234948A1/en active Pending
- 2021-06-10 UY UY0001039264A patent/UY39264A/es unknown
- 2021-06-10 MX MX2022015622A patent/MX2022015622A/es unknown
- 2021-06-10 US US17/344,939 patent/US11807634B2/en active Active
- 2021-06-10 CA CA3183814A patent/CA3183814A1/en active Pending
- 2021-06-10 TW TW110121156A patent/TW202214587A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UY39264A (es) | 2021-12-31 |
| MX2022015622A (es) | 2023-01-11 |
| TW202214587A (zh) | 2022-04-16 |
| EP4164748A1 (en) | 2023-04-19 |
| CA3183814A1 (en) | 2021-12-16 |
| JP2021195367A (ja) | 2021-12-27 |
| US20210387977A1 (en) | 2021-12-16 |
| US11807634B2 (en) | 2023-11-07 |
| AU2021289741A1 (en) | 2022-12-22 |
| WO2021252818A1 (en) | 2021-12-16 |
| US20230234948A1 (en) | 2023-07-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |