AU2021292062A1 - 5-oxopyrrolidine-3-carboxamides as Nav1.8 inhibitors - Google Patents

5-oxopyrrolidine-3-carboxamides as Nav1.8 inhibitors Download PDF

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Publication number
AU2021292062A1
AU2021292062A1 AU2021292062A AU2021292062A AU2021292062A1 AU 2021292062 A1 AU2021292062 A1 AU 2021292062A1 AU 2021292062 A AU2021292062 A AU 2021292062A AU 2021292062 A AU2021292062 A AU 2021292062A AU 2021292062 A1 AU2021292062 A1 AU 2021292062A1
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AU
Australia
Prior art keywords
alkyl
cycloalkyl
aryl
substituted
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
AU2021292062A
Other languages
English (en)
Inventor
Ashok Arasappan
Ian M. Bell
Jason M. Cox
Michael J. Kelly Iii
Mark E. Layton
Hong Liu
Jian Liu
Akshay Shah
Michael D. Vanheyst
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of AU2021292062A1 publication Critical patent/AU2021292062A1/en
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/4015Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/18Heterocyclic 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
    • C07D207/22Heterocyclic 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-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
    • C07D207/277Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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)
AU2021292062A 2020-06-17 2021-06-14 5-oxopyrrolidine-3-carboxamides as Nav1.8 inhibitors Pending AU2021292062A1 (en)

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 (1)

Publication Number Publication Date
AU2021292062A1 true AU2021292062A1 (en) 2023-01-19

Family

ID=79268285

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021292062A Pending AU2021292062A1 (en) 2020-06-17 2021-06-14 5-oxopyrrolidine-3-carboxamides as Nav1.8 inhibitors

Country Status (10)

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

Families Citing this family (24)

* 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
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
AU2022270061B2 (en) * 2021-05-07 2026-02-19 Merck Sharp & Dohme Llc Aryl 3-oxopiperazine carboxamides and heteroaryl 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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20001420A1 (es) * 1998-12-23 2000-12-18 Pfizer Moduladores de ccr5
EP1673357A2 (en) * 2003-08-08 2006-06-28 Vertex Pharmaceuticals Incorporated Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
GB0514017D0 (en) * 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
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
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

Also Published As

Publication number Publication date
BR112022024476A2 (pt) 2022-12-27
JP2023530320A (ja) 2023-07-14
US20230227405A1 (en) 2023-07-20
WO2021257420A1 (en) 2021-12-23
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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