PE20230860A1 - Compuestos de dihidroquinolinsulfonamida de ciclobutilo - Google Patents
Compuestos de dihidroquinolinsulfonamida de ciclobutiloInfo
- Publication number
- PE20230860A1 PE20230860A1 PE2022002892A PE2022002892A PE20230860A1 PE 20230860 A1 PE20230860 A1 PE 20230860A1 PE 2022002892 A PE2022002892 A PE 2022002892A PE 2022002892 A PE2022002892 A PE 2022002892A PE 20230860 A1 PE20230860 A1 PE 20230860A1
- Authority
- PE
- Peru
- Prior art keywords
- cyclobutyl
- haloalk
- alk
- halo
- compounds
- Prior art date
Links
- PAPIDPZGJVSNRS-UHFFFAOYSA-N N-cyclobutyl-1,2-dihydroquinoline-2-sulfonamide Chemical class O=S(C1NC2=CC=CC=C2C=C1)(NC1CCC1)=O PAPIDPZGJVSNRS-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 206010011224 Cough Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000003251 Pruritus Diseases 0.000 abstract 1
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 abstract 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 230000007803 itching Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/36—Sulfur atoms
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K31/505—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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Abstract
Referido a un compuesto de formula I, un enantiomero, diastereoisomero, atropisomero del mismo, una mezcla de los mismos o una sal farmaceuticamente aceptable del mismo; donde: R1 es un anillo monociclico de 4 miembros saturado o parcialmente saturado; o un anillo biciclico de 4 a 2 miembros; R2 es H, halo, alq C1-6 o haloalq C1-6; R3 es alq C1-6, haloalq C1-6, -O-alq C1-6 o -CN; R4 es un heteroarilo de 5 a 6 miembros; cada uno de R6 y R7 es H; y cada uno de R5a; R5b;R5c; R5d; y R5e es independientemente H o halo. Un compuesto seleccionado es cis-(P)-1-(5-fluoro-2-metoxi-4-(3-(trifluorometil)ciclobutil)fenil)-N-(isoxazol-3-il)-2-oxo-1,2-dihidroquinolin-6-sulfonamida. Estos compuestos de dihidroquinolinsulfonamida de ciclobutilo inhiben los canales de sodio activados por voltaje. Tambien se refiere a composiciones farmaceuticas que contienen los mismos y su uso en el tratamiento para tratar el dolor, la tos o la picazon.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063037001P | 2020-06-10 | 2020-06-10 | |
| PCT/US2021/036896 WO2021252820A1 (en) | 2020-06-10 | 2021-06-10 | Cyclobutyl dihydroquinoline sulfonamide compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230860A1 true PE20230860A1 (es) | 2023-05-30 |
Family
ID=76797115
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022002892A PE20230860A1 (es) | 2020-06-10 | 2021-06-10 | Compuestos de dihidroquinolinsulfonamida de ciclobutilo |
Country Status (28)
| Country | Link |
|---|---|
| US (3) | US12240839B2 (es) |
| EP (2) | EP4653050A2 (es) |
| JP (2) | JP7739051B2 (es) |
| KR (1) | KR20230022996A (es) |
| CN (2) | CN119735588A (es) |
| AR (1) | AR122592A1 (es) |
| AU (1) | AU2021288696A1 (es) |
| BR (1) | BR112022025201A2 (es) |
| CA (1) | CA3183889A1 (es) |
| CL (1) | CL2022003499A1 (es) |
| CO (1) | CO2022017903A2 (es) |
| CR (1) | CR20220631A (es) |
| DK (1) | DK4165024T3 (es) |
| ES (1) | ES3037072T3 (es) |
| FI (1) | FI4165024T3 (es) |
| HR (1) | HRP20251229T1 (es) |
| IL (1) | IL298325A (es) |
| JO (1) | JOP20220334A1 (es) |
| LT (1) | LT4165024T (es) |
| MA (1) | MA59968B1 (es) |
| MX (2) | MX2022015856A (es) |
| PE (1) | PE20230860A1 (es) |
| PL (1) | PL4165024T3 (es) |
| PT (1) | PT4165024T (es) |
| RS (1) | RS67268B1 (es) |
| SM (1) | SMT202500328T1 (es) |
| UY (1) | UY39263A (es) |
| WO (1) | WO2021252820A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7739051B2 (ja) | 2020-06-10 | 2025-09-16 | アムジエン・インコーポレーテツド | シクロブチルジヒドロキノリンスルホンアミド化合物 |
| CN117794919A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | N-(羟烷基(杂)芳基)四氢呋喃甲酰胺类似物作为钠通道调节剂 |
| DK4347031T3 (da) | 2021-06-04 | 2025-12-01 | Vertex Pharma | N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler |
| CA3221938A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| EP4346818B1 (en) | 2021-06-04 | 2025-12-03 | Vertex Pharmaceuticals Incorporated | Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide |
| CN117858875A (zh) | 2021-06-04 | 2024-04-09 | 沃泰克斯药物股份有限公司 | 羟基和(卤代)烷氧基取代的四氢呋喃作为钠通道调节剂 |
| EP4347032A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| US20250154105A1 (en) * | 2021-08-12 | 2025-05-15 | Tyk Medicines, Inc. | Polycyclic compound and use thereof |
| CR20240513A (es) | 2022-04-22 | 2025-04-30 | Vertex Pharma | Compuestos de heteroarilo para el tratamiento del dolor |
| WO2023205778A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | 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 |
| CN119487003A (zh) | 2022-04-22 | 2025-02-18 | 沃泰克斯药物股份有限公司 | 用于治疗疼痛的杂芳基化合物 |
| CN120603815A (zh) | 2022-12-06 | 2025-09-05 | 沃泰克斯药物股份有限公司 | 钠通道的取代四氢呋喃调节剂的合成方法 |
| TW202523313A (zh) | 2023-10-23 | 2025-06-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| TW202535867A (zh) | 2023-10-23 | 2025-09-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法 |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating pain |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US4412994A (en) | 1980-04-24 | 1983-11-01 | Interx Research Corporation | Mannich-base hydroxamic acid prodrugs, compositions and use |
| 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 |
| US5707985A (en) | 1995-06-07 | 1998-01-13 | Tanabe Seiyaku Co. Ltd. | Naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives as cell adhesion modulators |
| IT1298159B1 (it) | 1997-01-28 | 1999-12-20 | Hoffmann La Roche | Derivati di un 5-aroilnaftalene |
| CN1315836C (zh) | 2002-04-26 | 2007-05-16 | 奥索-麦克尼尔药品公司 | 用作雄激素受体调节剂的2－(喹诺酮基)－稠合杂环 |
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| US8101647B2 (en) | 2008-10-17 | 2012-01-24 | Xenon Pharmaceuticals Inc. | Spiro-oxindole compounds and their use as therapeutic agents |
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| CN102030780B (zh) * | 2010-10-26 | 2014-01-29 | 浙江大学 | 一种手性螺环磷酸和制备方法及其应用 |
| CA2844799A1 (en) | 2011-08-17 | 2013-02-21 | Amgen Inc. | Heteroaryl sodium channel inhibitors |
| WO2013086229A1 (en) | 2011-12-07 | 2013-06-13 | Amgen Inc. | Bicyclic aryl and heteroaryl sodium channel inhibitors |
| WO2013122897A1 (en) | 2012-02-13 | 2013-08-22 | Amgen Inc. | Dihydrobenzoxazine and tetrahydroquinoxaline sodium channel inhibitors |
| 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 |
| CN107428683B (zh) * | 2015-02-04 | 2020-06-02 | 上海海雁医药科技有限公司 | 杂环取代的n-磺酰基苯甲酰胺衍生物、其制法与医药上的用途 |
| EP3265465B1 (en) | 2015-03-02 | 2019-04-24 | Amgen Inc. | Bicyclic ketone sulfonamide compounds |
| JP6985271B2 (ja) * | 2015-12-18 | 2021-12-22 | アムジエン・インコーポレーテツド | アルキニルジヒドロキノリンスルホンアミド化合物 |
| WO2017106871A1 (en) * | 2015-12-18 | 2017-06-22 | Amgen Inc. | Alkyl dihydroquinoline sulfonamide compounds |
| CN109563045B (zh) * | 2016-03-21 | 2022-08-23 | 斯克里普斯研究学院 | Pd(II)-催化的对映选择性β-亚甲基C(sp3)-H键活化 |
| JP7739051B2 (ja) | 2020-06-10 | 2025-09-16 | アムジエン・インコーポレーテツド | シクロブチルジヒドロキノリンスルホンアミド化合物 |
| JP2021195367A (ja) * | 2020-06-10 | 2021-12-27 | アムジエン・インコーポレーテツド | シクロプロピルジヒドロキノリンスルホンアミド化合物 |
| US20250154105A1 (en) | 2021-08-12 | 2025-05-15 | Tyk Medicines, Inc. | Polycyclic compound and use thereof |
| KR20240049804A (ko) | 2021-08-19 | 2024-04-17 | 암젠 인크 | 트랜스 할로 시클로부탄의 입체선택적 제조 |
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2021
- 2021-05-31 JP JP2021090960A patent/JP7739051B2/ja active Active
- 2021-06-10 CA CA3183889A patent/CA3183889A1/en active Pending
- 2021-06-10 CN CN202510007130.6A patent/CN119735588A/zh active Pending
- 2021-06-10 CN CN202180040963.2A patent/CN115697971B/zh active Active
- 2021-06-10 FI FIEP21737878.5T patent/FI4165024T3/fi active
- 2021-06-10 RS RS20250992A patent/RS67268B1/sr unknown
- 2021-06-10 LT LTEPPCT/US2021/036896T patent/LT4165024T/lt unknown
- 2021-06-10 CR CR20220631A patent/CR20220631A/es unknown
- 2021-06-10 BR BR112022025201A patent/BR112022025201A2/pt unknown
- 2021-06-10 MA MA59968A patent/MA59968B1/fr unknown
- 2021-06-10 HR HRP20251229TT patent/HRP20251229T1/hr unknown
- 2021-06-10 MX MX2022015856A patent/MX2022015856A/es unknown
- 2021-06-10 WO PCT/US2021/036896 patent/WO2021252820A1/en not_active Ceased
- 2021-06-10 PL PL21737878.5T patent/PL4165024T3/pl unknown
- 2021-06-10 EP EP25188659.4A patent/EP4653050A2/en active Pending
- 2021-06-10 DK DK21737878.5T patent/DK4165024T3/da active
- 2021-06-10 EP EP21737878.5A patent/EP4165024B1/en active Active
- 2021-06-10 PE PE2022002892A patent/PE20230860A1/es unknown
- 2021-06-10 JO JOP/2022/0334A patent/JOP20220334A1/ar unknown
- 2021-06-10 PT PT217378785T patent/PT4165024T/pt unknown
- 2021-06-10 ES ES21737878T patent/ES3037072T3/es active Active
- 2021-06-10 IL IL298325A patent/IL298325A/en unknown
- 2021-06-10 AU AU2021288696A patent/AU2021288696A1/en active Pending
- 2021-06-10 AR ARP210101586A patent/AR122592A1/es unknown
- 2021-06-10 KR KR1020237000972A patent/KR20230022996A/ko active Pending
- 2021-06-10 US US17/633,151 patent/US12240839B2/en active Active
- 2021-06-10 UY UY0001039263A patent/UY39263A/es unknown
- 2021-06-10 SM SM20250328T patent/SMT202500328T1/it unknown
- 2021-06-11 US US17/344,947 patent/US20210387978A1/en not_active Abandoned
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2022
- 2022-12-09 CL CL2022003499A patent/CL2022003499A1/es unknown
- 2022-12-09 CO CONC2022/0017903A patent/CO2022017903A2/es unknown
- 2022-12-09 MX MX2025010506A patent/MX2025010506A/es unknown
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2025
- 2025-01-28 US US19/039,379 patent/US20250171425A1/en active Pending
- 2025-09-02 JP JP2025145171A patent/JP2025179137A/ja active Pending
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