RU2658920C2 - Амиды в качестве модуляторов натриевых каналов - Google Patents

Амиды в качестве модуляторов натриевых каналов Download PDF

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Publication number
RU2658920C2
RU2658920C2 RU2015136779A RU2015136779A RU2658920C2 RU 2658920 C2 RU2658920 C2 RU 2658920C2 RU 2015136779 A RU2015136779 A RU 2015136779A RU 2015136779 A RU2015136779 A RU 2015136779A RU 2658920 C2 RU2658920 C2 RU 2658920C2
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Russia
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another embodiment
alkyl
benzamido
pain
compound
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RU2015136779A
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Russian (ru)
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RU2015136779A (ru
Inventor
Сара Сабина АДИДА-РУА
Кори АНДЕРСОН
Виджаялаксми АРУМУГАМ
Иулиана Люси АСГИАН
Брайан Ричард БЕАР
Андреас П. ТЕРМИН
Джеймс Филип ДЖОНСОН
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Вертекс Фармасьютикалз Инкорпорейтед
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/64Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
RU2015136779A 2013-01-31 2014-01-29 Амиды в качестве модуляторов натриевых каналов RU2658920C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361759062P 2013-01-31 2013-01-31
US61/759,062 2013-01-31
PCT/US2014/013667 WO2014120820A1 (en) 2013-01-31 2014-01-29 Amides as modulators of sodium channels

Publications (2)

Publication Number Publication Date
RU2015136779A RU2015136779A (ru) 2017-03-07
RU2658920C2 true RU2658920C2 (ru) 2018-06-26

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RU2015136779A RU2658920C2 (ru) 2013-01-31 2014-01-29 Амиды в качестве модуляторов натриевых каналов

Country Status (15)

Country Link
US (2) US9108903B2 (en:Method)
EP (1) EP2951155B1 (en:Method)
JP (1) JP6346622B2 (en:Method)
KR (1) KR102226588B1 (en:Method)
CN (1) CN104968647B (en:Method)
AR (1) AR094668A1 (en:Method)
AU (1) AU2014212431B2 (en:Method)
BR (1) BR112015018284B1 (en:Method)
CA (1) CA2898653C (en:Method)
IL (1) IL240196B (en:Method)
MX (1) MX359882B (en:Method)
RU (1) RU2658920C2 (en:Method)
SG (1) SG11201505954RA (en:Method)
TW (1) TWI659945B (en:Method)
WO (1) WO2014120820A1 (en:Method)

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BR112015017997B1 (pt) 2013-01-31 2023-03-07 Vertex Pharmaceuticals Incorporated Amidas de quinolina e quinoxalina como moduladores de canais de sódio, seus usos, e composição farmacêutica
ES2857687T3 (es) 2013-01-31 2021-09-29 Vertex Pharma Piridona amidas como moduladores de los canales de sodio
EP3022175B1 (en) 2013-07-19 2017-11-08 Vertex Pharmaceuticals Incorporated Sulfonamides as modulators of sodium channels
JP6463580B2 (ja) 2013-12-13 2019-02-06 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ
KR102714561B1 (ko) 2017-05-16 2024-10-10 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 조절제로서의 중수소화 피리돈 아미드 및 이의 프로드럭
ES3008911T3 (en) 2017-07-11 2025-03-25 Vertex Pharma Carboxamides as modulators of sodium channels
JP2021512935A (ja) 2018-02-12 2021-05-20 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated 疼痛を処置する方法
US11377438B2 (en) 2018-11-02 2022-07-05 Merck Sharp & Dohme Llc 2-amino-n-heteroaryl-nicotinamides as Nav1.8 inhibitors
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WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
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JP2022548104A (ja) * 2019-09-12 2022-11-16 オリオン コーポレーション ピリジン窒素酸化物及びその製造方法と使用
BR112022010924A2 (pt) * 2019-12-06 2022-09-06 Vertex Pharma Tetra-hidrofuranos substituídos como moduladores de canais de sódio
CN114437062B (zh) * 2020-04-30 2024-05-17 成都海博为药业有限公司 一种可作为钠通道调节剂的化合物及其用途
US12516046B2 (en) 2020-06-17 2026-01-06 Merck Sharp & Dohme Llc 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors
PE20231383A1 (es) 2020-06-17 2023-09-12 Merck Sharp And Dohme Llc 2-oxoimidazolidin-4-carboxamidas como inhibidores de nav1.8
CN113880771B (zh) * 2020-07-03 2023-09-19 福建盛迪医药有限公司 一种选择性Nav抑制剂的结晶形式及其制备方法
CN114031518B (zh) * 2020-12-08 2023-08-18 成都海博为药业有限公司 一种苄胺或苄醇衍生物及其用途
CN112225695B (zh) * 2020-12-15 2021-03-02 上海济煜医药科技有限公司 一种氮氧化合物及其制备方法和用途
WO2022188872A1 (zh) * 2021-03-11 2022-09-15 上海济煜医药科技有限公司 吡啶氮氧化合物晶型及其应用
US20220380338A1 (en) 2021-05-07 2022-12-01 Merck Sharp & Dohme Llc Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors
KR20240031300A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널 조절제로서의 n-(하이드록시알킬 (헤테로)아릴) 테트라하이드로푸란 카르복스아미드
AU2022285758A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
CA3221939A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
US20240368135A1 (en) 2021-06-04 2024-11-07 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides 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
US20250388541A1 (en) 2022-04-22 2025-12-25 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
AU2023257313A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
TW202404969A (zh) 2022-04-22 2024-02-01 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
CN119522214A (zh) 2022-04-22 2025-02-25 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
GEAP202516637A (en) 2022-04-25 2025-03-25 Siteone Therapeutics Inc Bicyclic heterocyclic amide inhibitors of na v1.8 for the treatment of pain
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
TW202434235A (zh) * 2023-01-18 2024-09-01 芬蘭商奧利安公司 3-(4,5-二氯-2-(4-(三氟甲氧基)苯氧基)苯甲醯胺基)吡啶1-氧化物的製備方法
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
WO2025090511A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing modulators of sodium channels and solid forms of the same for treating pain
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
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WO2009049181A1 (en) * 2007-10-11 2009-04-16 Vertex Pharmaceuticals Incorporated Amides useful as inhibitors of voltage-gated sodium channels
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WO2010137351A1 (en) * 2009-05-29 2010-12-02 Raqualia Pharma Inc. Aryl substituted carboxamide derivatives as calcium or sodium channel blockers

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Publication number Publication date
CN104968647A (zh) 2015-10-07
RU2015136779A (ru) 2017-03-07
IL240196B (en) 2019-08-29
SG11201505954RA (en) 2015-08-28
KR20150118964A (ko) 2015-10-23
BR112015018284B1 (pt) 2023-03-07
JP6346622B2 (ja) 2018-06-20
AU2014212431B2 (en) 2018-04-05
MX359882B (es) 2018-10-15
JP2016508500A (ja) 2016-03-22
CN104968647B (zh) 2018-01-26
WO2014120820A9 (en) 2015-07-02
HK1217692A1 (en) 2017-01-20
US9421196B2 (en) 2016-08-23
NZ710293A (en) 2020-09-25
AU2014212431A1 (en) 2015-08-06
CA2898653A1 (en) 2014-08-07
MX2015009591A (es) 2016-04-15
US20150328196A1 (en) 2015-11-19
WO2014120820A1 (en) 2014-08-07
KR102226588B1 (ko) 2021-03-11
TW201443005A (zh) 2014-11-16
US20140221435A1 (en) 2014-08-07
IL240196A0 (en) 2015-09-24
BR112015018284A2 (pt) 2017-07-18
CA2898653C (en) 2021-09-28
US9108903B2 (en) 2015-08-18
AR094668A1 (es) 2015-08-19
EP2951155A1 (en) 2015-12-09
TWI659945B (zh) 2019-05-21
EP2951155B1 (en) 2019-06-19

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