JP2023530320A - Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド - Google Patents

Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド Download PDF

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Publication number
JP2023530320A
JP2023530320A JP2022577341A JP2022577341A JP2023530320A JP 2023530320 A JP2023530320 A JP 2023530320A JP 2022577341 A JP2022577341 A JP 2022577341A JP 2022577341 A JP2022577341 A JP 2022577341A JP 2023530320 A JP2023530320 A JP 2023530320A
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JP
Japan
Prior art keywords
alkyl
cycloalkyl
aryl
substituted
methyl
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Pending
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JP2022577341A
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English (en)
Japanese (ja)
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JP2023530320A5 (enExample
Inventor
アラサパン，アショーカ
ベル，イアン・エム
コックス，ジェイソン・エム
ケリー・サード，マイケル・ジェー
レイトン，マーク・イー
リウ，ホン
リウ，ジャン
シャー，アクシャイ・エー
ヴァンヘイスト，マイケル・ディー
Original Assignee
メルク・シャープ・アンド・ドーム・エルエルシー
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Publication of JP2023530320A publication Critical patent/JP2023530320A/ja
Publication of JP2023530320A5 publication Critical patent/JP2023530320A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
JP2022577341A 2020-06-17 2021-06-14 Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド Pending JP2023530320A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063040465P 2020-06-17 2020-06-17
US63/040,465 2020-06-17
PCT/US2021/037160 WO2021257420A1 (en) 2020-06-17 2021-06-14 5-oxopyrrolidine-3-carboxamides as nav1.8 inhibitors

Publications (2)

Publication Number Publication Date
JP2023530320A true JP2023530320A (ja) 2023-07-14
JP2023530320A5 JP2023530320A5 (enExample) 2024-06-20

Family

ID=79268285

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022577341A Pending JP2023530320A (ja) 2020-06-17 2021-06-14 Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド

Country Status (10)

Country Link
US (1) US20230227405A1 (enExample)
EP (1) EP4167993A4 (enExample)
JP (1) JP2023530320A (enExample)
KR (1) KR20230026405A (enExample)
CN (1) CN115697327A (enExample)
AU (1) AU2021292062A1 (enExample)
BR (1) BR112022024476A2 (enExample)
CA (1) CA3180372A1 (enExample)
MX (1) MX2022015580A (enExample)
WO (1) WO2021257420A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024519487A (ja) * 2021-05-07 2024-05-14 メルク・シャープ・アンド・ドーム・エルエルシー Ｎａｖ１．８阻害薬としてのアリール ３－オキソピペラジンカルボキサミド類及びヘテロアリール ３－オキソピペラジンカルボキサミド類
US12516046B2 (en) 2020-06-17 2026-01-06 Merck Sharp & Dohme Llc 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20257795B (en) * 2021-05-07 2025-09-25 Merck Sharp & Dohme Llc Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors
CA3221938A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
SMT202500481T1 (it) 2021-06-04 2026-01-12 Vertex Pharma N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio
US20240400544A1 (en) 2021-06-04 2024-12-05 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide 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
HRP20260068T1 (hr) 2021-06-04 2026-02-27 Vertex Pharmaceuticals Incorporated Čvrsti farmaceutski oblici i režimi doziranja koji obuhvaćaju (2r,3s,4s,5r)-4-[[3-(3,4-difluor-2-metoksifenil)-4,5-dimetil-5-(trifluormetil)tetrahidrofuran-2-karbonil]amino]piridin-2-karboksamid
CA3256248A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
US20230382910A1 (en) 2022-04-22 2023-11-30 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205463A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CA3257285A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
JP2025516005A (ja) 2022-04-25 2025-05-23 サイトワン セラピューティクス インコーポレイテッド 疼痛の処置のためのｎａｖ１．８の二環式複素環アミド阻害剤
WO2024123815A1 (en) 2022-12-06 2024-06-13 Vertex Pharmaceuticals Incorporated Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
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
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2025090465A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
WO2025160286A1 (en) 2024-01-24 2025-07-31 Siteone Therapeutics, Inc. 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain
US20260001877A1 (en) 2024-06-28 2026-01-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2026013449A2 (en) 2024-07-11 2026-01-15 Sea4Us - Biotecnologia E Recursos Marinhos, Sa Oxazolidone-derived compounds and their use in the treatment of chronic and acute pain
WO2026030525A1 (en) 2024-07-31 2026-02-05 Vertex Pharmaceuticals Incorporated Zilvetrigine dosage forms and dosing regimens for treating pain

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007007057A1 (en) * 2005-07-07 2007-01-18 Vernalis (R & D) Limited Antagonists of sns sodium channels
JP2011032294A (ja) * 2003-08-08 2011-02-17 Vertex Pharmaceuticals Inc 電位開口型のナトリウムチャネルのインヒビターとして有用な組成物
JP2014527511A (ja) * 2011-06-24 2014-10-16 アムジエン・インコーポレーテツド Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用

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PE20001420A1 (es) * 1998-12-23 2000-12-18 Pfizer Moduladores de ccr5
WO2014146111A2 (en) * 2013-03-15 2014-09-18 The Regents Of The University Of California Analgesic compounds and methods of use
JP2018507900A (ja) * 2015-03-13 2018-03-22 アッヴィ・インコーポレイテッド （インダゾール−４−イル）ヘキサヒドロピロロピロロン及び使用方法

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
JP2011032294A (ja) * 2003-08-08 2011-02-17 Vertex Pharmaceuticals Inc 電位開口型のナトリウムチャネルのインヒビターとして有用な組成物
WO2007007057A1 (en) * 2005-07-07 2007-01-18 Vernalis (R & D) Limited Antagonists of sns sodium channels
JP2014527511A (ja) * 2011-06-24 2014-10-16 アムジエン・インコーポレーテツド Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用

Non-Patent Citations (4)

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Title
REGISTRY (STN) [ONLINE], JPN7025002043, ISSN: 0005592125 *
REGISTRY (STN) [ONLINE], JPN7025002044, ISSN: 0005592126 *
REGISTRY (STN) [ONLINE], JPN7025002045, ISSN: 0005592127 *
REGISTRY (STN) [ONLINE], JPN7025002046, ISSN: 0005592128 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12516046B2 (en) 2020-06-17 2026-01-06 Merck Sharp & Dohme Llc 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors
JP2024519487A (ja) * 2021-05-07 2024-05-14 メルク・シャープ・アンド・ドーム・エルエルシー Ｎａｖ１．８阻害薬としてのアリール ３－オキソピペラジンカルボキサミド類及びヘテロアリール ３－オキソピペラジンカルボキサミド類
JP7846132B2 (ja) 2021-05-07 2026-04-14 メルク・シャープ・アンド・ドーム・エルエルシー Ｎａｖ１．８阻害薬としてのアリール ３－オキソピペラジンカルボキサミド類及びヘテロアリール ３－オキソピペラジンカルボキサミド類

Also Published As

Publication number Publication date
BR112022024476A2 (pt) 2022-12-27
US20230227405A1 (en) 2023-07-20
WO2021257420A1 (en) 2021-12-23
AU2021292062A1 (en) 2023-01-19
CN115697327A (zh) 2023-02-03
EP4167993A4 (en) 2024-07-24
CA3180372A1 (en) 2021-12-23
EP4167993A1 (en) 2023-04-26
KR20230026405A (ko) 2023-02-24
MX2022015580A (es) 2023-01-24

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