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
Prior art keywords
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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (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 (enExample)
EP (1) EP2951155B1 (enExample)
JP (1) JP6346622B2 (enExample)
KR (1) KR102226588B1 (enExample)
CN (1) CN104968647B (enExample)
AR (1) AR094668A1 (enExample)
AU (1) AU2014212431B2 (enExample)
BR (1) BR112015018284B1 (enExample)
CA (1) CA2898653C (enExample)
IL (1) IL240196B (enExample)
MX (1) MX359882B (enExample)
RU (1) RU2658920C2 (enExample)
SG (1) SG11201505954RA (enExample)
TW (1) TWI659945B (enExample)
WO (1) WO2014120820A1 (enExample)

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US11203571B2 (en) 2013-07-19 2021-12-21 Vertex Pharmaceuticals Incorporated Sulfonamides as modulators of sodium channels
EP3459958B1 (en) 2013-12-13 2024-08-07 Vertex Pharmaceuticals Incorporated Process and intermediates for preparing prodrugs of pyridone amides useful as modulators of sodium channels
CA3063901A1 (en) 2017-05-16 2018-11-22 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
EP3651752B1 (en) 2017-07-11 2024-11-20 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
TW202002971A (zh) 2018-02-12 2020-01-16 美商維泰克斯製藥公司 治療疼痛的方法
US12344595B2 (en) 2018-11-02 2025-07-01 Merck Sharp & Dohme Llc 2-amino-n-phenyl-nicotinamides as NAV1.8 inhibitors
CN113272293B (zh) 2018-11-02 2024-06-14 默沙东有限责任公司 作为nav1.8抑制剂的2-胺基-n-杂芳基-烟酰胺
MX2021007970A (es) * 2019-01-04 2021-08-16 Jiangsu Hengrui Medicine Co Derivado de 6-oxo-1,6-dihidropiridazina, metodo de preparacion del mismo y uso medico del mismo.
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
CN112996776B (zh) * 2019-02-20 2024-03-15 福建盛迪医药有限公司 6-氧代-1,6-二氢哒嗪类前药衍生物、其制备方法及其在医药上的应用
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
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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
GEP20257750B (en) 2020-06-17 2025-03-25 Merck Sharp & Dohme Llc 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors
AU2021292061A1 (en) 2020-06-17 2023-01-19 Merck Sharp & Dohme Llc 2-oxo-oxazolidine-5-carboxamides as Nav1.8 inhibitors
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
JP2024509939A (ja) * 2021-03-11 2024-03-05 シャンハイ ジェミンケア ファーマシューティカル カンパニー,リミティド ピリジン窒素酸化物の結晶形態およびその使用
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
MX2023014376A (es) 2021-06-04 2024-03-04 Vertex Pharma Formas de dosificación sólidas y regímenes de dosificación que comprenden (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-metoxi-fenil)-4,5-d imetil-5-(trifluorometil) tetrahidrofuran-2- carbonil]amino]piridi na-2-carboxamida.
JP2024520646A (ja) 2021-06-04 2024-05-24 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 ナトリウムチャネルのモジュレーターとしてのn-(ヒドロキシアルキル(ヘテロ)アリール)テトラヒドロフランカルボキサミド類似体
CR20230586A (es) 2021-06-04 2024-05-07 Vertex Pharma N-(hydroxyalquil (hetero)aril) tetrahidrofurano carboxamidas como moduladores de canales de sodio
CN117794918A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 经取代的四氢呋喃类似物作为钠通道调节剂
CN117813302A (zh) 2021-06-04 2024-04-02 沃泰克斯药物股份有限公司 经取代的四氢呋喃-2-甲酰胺作为钠通道调节剂
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
CA3257285A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
CA3256604A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
CA3256248A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
JP2025513455A (ja) 2022-04-22 2025-04-24 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 疼痛の治療のためのヘテロアリール化合物
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KR20250120351A (ko) 2022-12-06 2025-08-08 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법
WO2024153856A1 (en) * 2023-01-18 2024-07-25 Orion Corporation Process for the preparation of 3-(4,5-dichloro-2-(4-(trifluoromethoxy)phenoxy)benzamido)pyridine 1-oxide
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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
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WO2009049181A1 (en) * 2007-10-11 2009-04-16 Vertex Pharmaceuticals Incorporated Amides useful as inhibitors of voltage-gated sodium channels
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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RU2010118467A (ru) * 2007-10-11 2011-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ариламиды, пригодные в качестве ингибиторов потенциалзависимых натриевых каналов
WO2010137351A1 (en) * 2009-05-29 2010-12-02 Raqualia Pharma Inc. Aryl substituted carboxamide derivatives as calcium or sodium channel blockers

Also Published As

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

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