JP7522943B2 - Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類 - Google Patents

Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類 Download PDF

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JP7522943B2
JP7522943B2 JP2023567928A JP2023567928A JP7522943B2 JP 7522943 B2 JP7522943 B2 JP 7522943B2 JP 2023567928 A JP2023567928 A JP 2023567928A JP 2023567928 A JP2023567928 A JP 2023567928A JP 7522943 B2 JP7522943 B2 JP 7522943B2
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alkyl
methyl
cycloalkyl
chloro
substituted
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JP2024515895A (ja
Inventor
アラサッパン，アショク
ベル，イアン・エム
コックス，ジェイソン・エム
ケリー，マイケル・ジェイ・ザ・サード
レイトン，マーク・エリック
リウ，ホン
リウ，ジャン
シャー，アクシェイ・エー
ヴァンヘイスト，マイケル・ディー
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メルク・シャープ・アンド・ドーム・エルエルシー
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Priority to JP2024000646A priority Critical patent/JP2024038267A/ja
Publication of JP2024515895A publication Critical patent/JP2024515895A/ja
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Publication of JP7522943B2 publication Critical patent/JP7522943B2/ja
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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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2023567928A 2021-05-07 2022-05-05 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類 Active JP7522943B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2024000646A JP2024038267A (ja) 2021-05-07 2024-01-05 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類
JP2025264265A JP2026048891A (ja) 2021-05-07 2025-12-18 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202163185637P 2021-05-07 2021-05-07
US63/185,637 2021-05-07
US202163286691P 2021-12-07 2021-12-07
US63/286,691 2021-12-07
PCT/US2022/027763 WO2022235859A1 (en) 2021-05-07 2022-05-05 Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors

Related Child Applications (1)

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JP2024000646A Division JP2024038267A (ja) 2021-05-07 2024-01-05 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類

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JP2024515895A JP2024515895A (ja) 2024-04-10
JP7522943B2 true JP7522943B2 (ja) 2024-07-25

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JP2023567928A Active JP7522943B2 (ja) 2021-05-07 2022-05-05 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類
JP2024000646A Pending JP2024038267A (ja) 2021-05-07 2024-01-05 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類
JP2025264265A Pending JP2026048891A (ja) 2021-05-07 2025-12-18 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類

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JP2024000646A Pending JP2024038267A (ja) 2021-05-07 2024-01-05 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類
JP2025264265A Pending JP2026048891A (ja) 2021-05-07 2025-12-18 Ｎａｖ１．８阻害薬としてのシクロアルキル ３－オキソピペラジンカルボキサミド類及びシクロヘテロアルキル ３－オキソピペラジンカルボキサミド類

Country Status (21)

Country Link
US (1) US20220380338A1 (https=)
EP (1) EP4334293A1 (https=)
JP (3) JP7522943B2 (https=)
KR (1) KR20240005878A (https=)
CN (1) CN117881664A (https=)
AR (1) AR125786A1 (https=)
AU (1) AU2022270115B2 (https=)
BR (1) BR112023023239A2 (https=)
CA (1) CA3217565A1 (https=)
CL (1) CL2023003295A1 (https=)
CO (1) CO2023015096A2 (https=)
CR (1) CR20230519A (https=)
DO (1) DOP2023000242A (https=)
EC (1) ECSP23083881A (https=)
GE (2) GEP20257795B (https=)
IL (1) IL308215A (https=)
JO (1) JOP20230284A1 (https=)
MX (1) MX2023013146A (https=)
PE (1) PE20250021A1 (https=)
TW (1) TWI827037B (https=)
WO (1) WO2022235859A1 (https=)

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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
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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
WO2024123815A1 (en) 2022-12-06 2024-06-13 Vertex Pharmaceuticals Incorporated Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
WO2025085564A1 (en) * 2023-10-16 2025-04-24 Kronos Bio, Inc. Lysine acetyltransferase inhibitors
CN117645533B (zh) * 2023-10-20 2024-10-11 泰州精英化成医药科技有限公司 一种4-(三氟甲基)环己酮的合成方法
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
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
CN117567323A (zh) * 2023-10-30 2024-02-20 湖北泰盛化工有限公司 一种(s)-4-氯-2-((甲氧基羰基)氨基)丁酸乙酯的制备方法
US20250186419A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens for treating 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
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JP2017114764A (ja) 2014-04-25 2017-06-29 武田薬品工業株式会社 片頭痛治療剤
WO2019101970A1 (en) 2017-11-23 2019-05-31 Oslo University Hospital Hf Treatment of tachycardia
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JP2007514769A (ja) 2003-12-18 2007-06-07 シーブイ・セラピューティクス・インコーポレイテッド １−アルカン−２−オール置換ピペラジンおよびピペリジン化合物
US20120088915A1 (en) 2010-07-16 2012-04-12 Johnston Jeffrey N Stereoselective methods, catalysts and intermediates for the synthesis of (-)-nutlin-3 and related compounds
JP2017114764A (ja) 2014-04-25 2017-06-29 武田薬品工業株式会社 片頭痛治療剤
WO2015184383A1 (en) 2014-05-29 2015-12-03 St. Jude Children's Research Hospital Aryl-substituted imidazoles and methods of making and using same
WO2019101970A1 (en) 2017-11-23 2019-05-31 Oslo University Hospital Hf Treatment of tachycardia
WO2019226931A1 (en) 2018-05-25 2019-11-28 VenatoRx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors
WO2021108023A1 (en) 2019-11-26 2021-06-03 VenatoRx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors

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GEAP202416407A (en) 2024-03-25
JP2024515895A (ja) 2024-04-10
CO2023015096A2 (es) 2023-11-20
ECSP23083881A (es) 2023-12-29
MX2023013146A (es) 2023-11-28
EP4334293A1 (en) 2024-03-13
TWI827037B (zh) 2023-12-21
CR20230519A (es) 2024-01-19
CA3217565A1 (en) 2022-11-10
US20220380338A1 (en) 2022-12-01
DOP2023000242A (es) 2023-12-15
BR112023023239A2 (pt) 2024-01-23
PE20250021A1 (es) 2025-01-07
GEP20257795B (en) 2025-09-25
CN117881664A (zh) 2024-04-12
JOP20230284A1 (ar) 2023-11-06
AU2022270115B2 (en) 2025-08-07
CL2023003295A1 (es) 2024-07-12
JP2024038267A (ja) 2024-03-19
TW202308999A (zh) 2023-03-01
AU2022270115A1 (en) 2023-11-16
JP2026048891A (ja) 2026-03-17
KR20240005878A (ko) 2024-01-12
WO2022235859A1 (en) 2022-11-10
AR125786A1 (es) 2023-08-16
IL308215A (en) 2024-01-01

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