AU2014212431B2 - Amides as modulators of sodium channels - Google Patents

Amides as modulators of sodium channels Download PDF

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Publication number
AU2014212431B2
AU2014212431B2 AU2014212431A AU2014212431A AU2014212431B2 AU 2014212431 B2 AU2014212431 B2 AU 2014212431B2 AU 2014212431 A AU2014212431 A AU 2014212431A AU 2014212431 A AU2014212431 A AU 2014212431A AU 2014212431 B2 AU2014212431 B2 AU 2014212431B2
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Australia
Prior art keywords
alkyl
another embodiment
halogen
benzamido
pain
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AU2014212431A
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AU2014212431A1 (en
Inventor
Corey Anderson
Vijayalaksmi Arumugam
Iuliana Luci Asgian
Brian Richard Bear
Sara Sabina Hadida-Ruah
James Philip Johnson
Andreas P. Termin
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary 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
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic 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
    • C07C235/44—Carboxylic 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
    • C07C235/58—Carboxylic 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
    • C07C235/64—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
AU2014212431A 2013-01-31 2014-01-29 Amides as modulators of sodium channels Active AU2014212431B2 (en)

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
AU2014212431A1 AU2014212431A1 (en) 2015-08-06
AU2014212431B2 true AU2014212431B2 (en) 2018-04-05

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AU2014212431A Active AU2014212431B2 (en) 2013-01-31 2014-01-29 Amides as modulators of sodium channels

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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US9139529B2 (en) 2013-01-31 2015-09-22 Vertex Pharmaceuticals Incorporated Substituted quinoxalines as sodium channel modulators
SG11201600383SA (en) 2013-07-19 2016-02-26 Vertex Pharma Sulfonamides as modulators of sodium channels
GEP20207082B (en) 2013-12-13 2020-04-10 Vertex Pharma Prodrugs of pyridone amides useful as modulators of sodium channels
CN110740993B (zh) 2017-05-16 2023-09-01 沃泰克斯药物股份有限公司 用作钠通道调节剂的氘代吡啶酮酰胺及其前药
AU2018300150A1 (en) * 2017-07-11 2020-01-30 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
CA3091012A1 (en) 2018-02-12 2019-08-15 Vertex Pharmaceuticals Incorporated A method of treating pain
EP3873893A1 (en) 2018-11-02 2021-09-08 Merck Sharp & Dohme Corp. 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors
EP3873468A4 (en) 2018-11-02 2022-10-26 Merck Sharp & Dohme LLC 2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
WO2020140959A1 (zh) * 2019-01-04 2020-07-09 江苏恒瑞医药股份有限公司 6-氧代-1,6-二氢哒嗪类衍生物、其制备方法及其在医药上的应用
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020169042A1 (zh) * 2019-02-20 2020-08-27 江苏恒瑞医药股份有限公司 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
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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
HRP20241695T1 (hr) * 2019-12-06 2025-02-14 Vertex Pharmaceuticals Incorporated Supstituirani tetrahidrofurani kao modulatori natrijevih kanala
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
TWI806073B (zh) 2020-06-17 2023-06-21 美商默沙東有限責任公司 作為nav1.8抑制劑之2-氧基咪唑啶-4-甲醯胺
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
KR20240005878A (ko) 2021-05-07 2024-01-12 머크 샤프 앤드 돔 엘엘씨 Nav1.8 억제제로서의 시클로알킬 3-옥소피페라진 카르복스아미드 및 시클로헤테로알킬 3-옥소피페라진 카르복스아미드
JP2024520649A (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 （２ｒ，３ｓ，４ｓ，５ｒ）－４－［［３－（３，４－ジフルオロ－２－メトキシ－フェニル）－４，５－ジメチル－５－（トリフルオロメチル）テトラヒドロフラン－２－カルボニル］アミノ］ピリジン－２－カルボキサミドを含む固体剤形及び投与レジメン
KR20240031300A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널 조절제로서의 n-(하이드록시알킬 (헤테로)아릴) 테트라하이드로푸란 카르복스아미드
EP4347033A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans 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
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
CA3256248A1 (en) 2022-04-22 2023-10-26 Vertex Pharma HETEROARYL COMPOUNDS FOR PAIN RELIEF
AU2023255558A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
AR129104A1 (es) 2022-04-22 2024-07-17 Vertex Pharma Compuestos heteroarilo para el tratamiento del dolor
AU2023255771A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
PE20251183A1 (es) 2022-04-25 2025-04-23 Siteone Therapeutics Inc Inhibidores de amida heterociclica biciclica de sodio activado por voltaje 1.8 (nav 1.8) para el tratamiento del dolor
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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
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WO2025090465A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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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Also Published As

Publication number Publication date
AR094668A1 (es) 2015-08-19
HK1217692A1 (en) 2017-01-20
JP2016508500A (ja) 2016-03-22
WO2014120820A9 (en) 2015-07-02
IL240196A0 (en) 2015-09-24
AU2014212431A1 (en) 2015-08-06
MX2015009591A (es) 2016-04-15
US9108903B2 (en) 2015-08-18
CN104968647A (zh) 2015-10-07
MX359882B (es) 2018-10-15
KR102226588B1 (ko) 2021-03-11
RU2015136779A (ru) 2017-03-07
EP2951155B1 (en) 2019-06-19
CA2898653C (en) 2021-09-28
NZ710293A (en) 2020-09-25
KR20150118964A (ko) 2015-10-23
BR112015018284B1 (pt) 2023-03-07
WO2014120820A1 (en) 2014-08-07
TWI659945B (zh) 2019-05-21
SG11201505954RA (en) 2015-08-28
CN104968647B (zh) 2018-01-26
CA2898653A1 (en) 2014-08-07
TW201443005A (zh) 2014-11-16
EP2951155A1 (en) 2015-12-09
BR112015018284A2 (pt) 2017-07-18
US20150328196A1 (en) 2015-11-19
RU2658920C2 (ru) 2018-06-26
US20140221435A1 (en) 2014-08-07
US9421196B2 (en) 2016-08-23
JP6346622B2 (ja) 2018-06-20
IL240196B (en) 2019-08-29

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