CA3180372A1 - 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
CA3180372A1
CA3180372A1 CA3180372A CA3180372A CA3180372A1 CA 3180372 A1 CA3180372 A1 CA 3180372A1 CA 3180372 A CA3180372 A CA 3180372A CA 3180372 A CA3180372 A CA 3180372A CA 3180372 A1 CA3180372 A1 CA 3180372A1
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CA
Canada
Prior art keywords
6alkyl
substituted
unsubstituted
aryl
6a1ky1
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
CA3180372A
Other languages
English (en)
French (fr)
Inventor
Ashok Arasappan
Ian M. Bell
Jason M. Cox
Michael J. Kelly Iii
Mark E. Layton
Hong Liu
Jian Liu
Akshay A. 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 CA3180372A1 publication Critical patent/CA3180372A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • 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
    • 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]
    • 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
CA3180372A 2020-06-17 2021-06-14 5-oxopyrrolidine-3-carboxamides as nav1.8 inhibitors Pending CA3180372A1 (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
CA3180372A1 true CA3180372A1 (en) 2021-12-23

Family

ID=79268285

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3180372A Pending CA3180372A1 (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
JP2023530319A (ja) 2020-06-17 2023-07-14 メルク・シャープ・アンド・ドーム・エルエルシー Nav1.8阻害剤としての2-オキソ-オキサゾリジン-5-カルボキサミド
MX2023013147A (es) * 2021-05-07 2023-11-28 Merck Sharp & Dohme Llc Aril 3-oxopiperazin carboxamidas y heteroaril 3-oxopiperazin carboxamidas como inhibidores de nav1.8.
EP4334293A1 (en) * 2021-05-07 2024-03-13 Merck Sharp & Dohme LLC Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors
WO2022256676A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
MA64856B1 (fr) 2021-06-04 2026-02-27 Vertex Pharmaceuticals Incorporated Formes de dosage solides et regimens de dosage comprenant le [[3-(3,4-difluoro-2-méthoxy-phényl)-4,5-diméthyl-5-(trifluorométhyl) tétrahydrofuranne-2-carbonyl]amino]pyridine-2-carboxamide
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
CA3221788A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
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
JP2024520643A (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調節因子としてのヒドロキシ及び(ハロ)アルコキシ置換テトラヒドロフラン
AU2023257313A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
UY40234A (es) 2022-04-22 2023-11-15 Vertex Pharma Compuestos heteroarilo para el tratamiento del dolor
GEAP202516634A (en) 2022-04-22 2025-02-25 Vertex Pharma Heteroaryl compounds for the treatment of pain
JP2025513452A (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
IL316433A (en) 2022-04-25 2024-12-01 Siteone Therapeutics Inc Bicyclic heterocyclic amide inhibitors of NA v1.8 for the treatment of pain
AU2023391870A1 (en) 2022-12-06 2025-06-05 Vertex Pharmaceuticals Incorporated Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
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
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
WO2025122953A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic 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
US8202861B2 (en) * 2003-08-08 2012-06-19 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of voltage-gated sodium channels
GB0514017D0 (en) * 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
US8710043B2 (en) * 2011-06-24 2014-04-29 Amgen Inc. TRPM8 antagonists and their use in treatments
WO2014146111A2 (en) * 2013-03-15 2014-09-18 The Regents Of The University Of California Analgesic compounds and methods of use
CA2979534A1 (en) * 2015-03-13 2016-09-22 Abbvie Inc. (indazol-4-yl)hexahydropyrrolopyrrolones and method of use

Also Published As

Publication number Publication date
EP4167993A1 (en) 2023-04-26
US20230227405A1 (en) 2023-07-20
AU2021292062A1 (en) 2023-01-19
MX2022015580A (es) 2023-01-24
JP2023530320A (ja) 2023-07-14
WO2021257420A1 (en) 2021-12-23
EP4167993A4 (en) 2024-07-24
CN115697327A (zh) 2023-02-03
KR20230026405A (ko) 2023-02-24
BR112022024476A2 (pt) 2022-12-27

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