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
Authority
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

    • 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
    • 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
    • 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]
    • 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

Landscapes

  • 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)
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 (OSRAM)
EP (1) EP4167993A4 (OSRAM)
JP (1) JP2023530320A (OSRAM)
KR (1) KR20230026405A (OSRAM)
CN (1) CN115697327A (OSRAM)
AU (1) AU2021292062A1 (OSRAM)
BR (1) BR112022024476A2 (OSRAM)
CA (1) CA3180372A1 (OSRAM)
MX (1) MX2022015580A (OSRAM)
WO (1) WO2021257420A1 (OSRAM)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4167994A4 (en) 2020-06-17 2024-07-24 Merck Sharp & Dohme LLC 2-OXO-OXAZOLIDINE-5-CARBOXAMIDE AS NAV1.8 INHIBITORS
MX2023013146A (es) * 2021-05-07 2023-11-28 Merck Sharp & Dohme Llc Cicloalquil 3-oxopiperazin carboxamidas y cicloheteroalquil 3-oxopiperazin carboxamidas como inhibidores de nav1.8.
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.
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
AU2022286511A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
CN117794920A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 N-(羟烷基(杂)芳基)四氢呋喃甲酰胺作为钠通道调节剂
KR20240031299A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 (2r,3s,4s,5r)-4-[[3-(3,4-디플루오로-2-메톡시-페닐)-4,5-디메틸-5-(트리플루오로메틸)테트라하이드로푸란-2-카르보닐]아미노]피리딘-2-카르복사미드를 포함하는 고체 투여 형태 및 투여 요법
CA3221938A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran 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
AU2023255771A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
JP2025513454A (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
CN119487003A (zh) 2022-04-22 2025-02-18 沃泰克斯药物股份有限公司 用于治疗疼痛的杂芳基化合物
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
GEAP202516637A (en) 2022-04-25 2025-03-25 Siteone Therapeutics Inc Bicyclic heterocyclic amide inhibitors of na v1.8 for the treatment of pain
WO2024123815A1 (en) 2022-12-06 2024-06-13 Vertex Pharmaceuticals Incorporated Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
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
AU2024365648A1 (en) 2023-10-23 2026-04-30 Vertex Pharmaceuticals Incorporated Methods of preparing modulators of sodium channels and solid forms of the same for treating pain
AU2024367861A1 (en) 2023-10-23 2026-05-07 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
TW202606663A (zh) 2024-06-28 2026-02-16 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
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
TW200524888A (en) * 2003-08-08 2005-08-01 Vertex Pharma Compositions useful as inhibitors of voltage-gated ion channels
GB0514017D0 (en) * 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
MY157429A (en) * 2011-06-24 2016-06-15 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
US9682985B2 (en) * 2015-03-13 2017-06-20 Abbvie Inc. (Indazol-4-yl) hexahydropyrrolopyrrolones and methods of use

Also Published As

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

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