JP6215230B2 - イオンチャネルのモジュレーターとしてのピラン−スピロ環式ピペリジンアミド - Google Patents

イオンチャネルのモジュレーターとしてのピラン−スピロ環式ピペリジンアミド Download PDF

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JP6215230B2
JP6215230B2 JP2014552376A JP2014552376A JP6215230B2 JP 6215230 B2 JP6215230 B2 JP 6215230B2 JP 2014552376 A JP2014552376 A JP 2014552376A JP 2014552376 A JP2014552376 A JP 2014552376A JP 6215230 B2 JP6215230 B2 JP 6215230B2
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pain
alkyl
heterocycloalkyl
pharmaceutically acceptable
alkoxy
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JP2015505321A5 (enExample
JP2015505321A (ja
Inventor
サラ サビーナ ハディダ−ルア,
サラ サビーナ ハディダ−ルア,
ヴィジャヤラクスミ アルムガム,
ヴィジャヤラクスミ アルムガム,
マイケル ポール デニノ,
マイケル ポール デニノ,
ブライアン エー. フリーマン,
ブライアン エー. フリーマン,
エドワード アダム カレル,
エドワード アダム カレル,
マーク トーマス ミラー,
マーク トーマス ミラー,
ジョニー ウイ,
ジョニー ウイ,
ジンラン ゾウ,
ジンラン ゾウ,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2014552376A 2012-01-16 2013-01-15 イオンチャネルのモジュレーターとしてのピラン−スピロ環式ピペリジンアミド Active JP6215230B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261586875P 2012-01-16 2012-01-16
US61/586,875 2012-01-16
PCT/US2013/021535 WO2013109521A1 (en) 2012-01-16 2013-01-15 Pyran-spirocyclic piperidine amides as modulators of ion channels

Publications (3)

Publication Number Publication Date
JP2015505321A JP2015505321A (ja) 2015-02-19
JP2015505321A5 JP2015505321A5 (enExample) 2016-03-03
JP6215230B2 true JP6215230B2 (ja) 2017-10-18

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JP2014552376A Active JP6215230B2 (ja) 2012-01-16 2013-01-15 イオンチャネルのモジュレーターとしてのピラン−スピロ環式ピペリジンアミド

Country Status (10)

Country Link
US (1) US9403839B2 (enExample)
EP (1) EP2804868B1 (enExample)
JP (1) JP6215230B2 (enExample)
CN (1) CN104136442B (enExample)
AU (1) AU2013209958B2 (enExample)
CA (1) CA2863343A1 (enExample)
ES (1) ES2631611T3 (enExample)
MX (1) MX2014008591A (enExample)
NZ (1) NZ627259A (enExample)
WO (1) WO2013109521A1 (enExample)

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CN105683157B (zh) 2013-07-19 2019-07-19 沃泰克斯药物股份有限公司 用作钠通道调节剂的磺酰胺类
SI3080134T1 (sl) 2013-12-13 2018-11-30 Vertex Pharmaceuticals Incorporated Predzdravila piridon amidov uporabna kot modulatorji natrijevih kanalov
US11358977B2 (en) 2017-05-16 2022-06-14 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
JP7277431B2 (ja) 2017-07-11 2023-05-19 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カルボキサミド
JP7228595B2 (ja) * 2017-11-01 2023-02-24 ブリストル-マイヤーズ スクイブ カンパニー ファルネソイドx受容体モジュレーターとしてのスピロ環化合物
CN108276307A (zh) * 2018-01-17 2018-07-13 常熟浸大科技有限公司 3-氰基-4-烃氧基苯甲酸酯的合成方法
US11529337B2 (en) 2018-02-12 2022-12-20 Vertex Pharmaceuticals Incorporated Method of treating pain
KR102708681B1 (ko) 2018-02-13 2024-09-26 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
CN110156674A (zh) * 2018-02-13 2019-08-23 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的螺环化合物
EP3781556B1 (en) 2018-04-19 2025-06-18 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
SG11202100130QA (en) 2018-07-09 2021-02-25 Lieber Institute Inc Pyridine carboxamide compounds for inhibiting nav1.8
KR102840599B1 (ko) * 2018-07-09 2025-07-29 리버 인스티튜트, 아이엔씨 Nav1.8을 억제하기 위한 피리다진(PYRIDAZINE) 화합물
CN118221646A (zh) 2018-07-13 2024-06-21 吉利德科学公司 Pd-1/pd-l1抑制剂
KR102635333B1 (ko) 2018-10-24 2024-02-15 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
MX2022006865A (es) 2019-12-06 2022-07-11 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio.
BR112023025264A2 (pt) 2021-06-04 2024-02-20 Vertex Pharma Formas farmacêuticas sólidas e regimes posológicos compreendendo (2r,3s,4s,5r)-4-[[3- (3,4-difluoro-2-metóxi-fenil)-4,5-dimetil-5-(trifluorometil) tetra-hidrofuran-2-carbonil]amino ]piridina-2-carboxamida
WO2022256676A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs 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
US20240400544A1 (en) 2021-06-04 2024-12-05 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
JP2024520648A (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置換テトラヒドロフラン-2-カルボキサミド
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
EP4511117A1 (en) 2022-04-22 2025-02-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CA3256604A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
GEAP202516632A (en) 2022-04-22 2025-02-25 Vertex Pharma Heteroaryl compounds for the treatment of pain
CN120603815A (zh) 2022-12-06 2025-09-05 沃泰克斯药物股份有限公司 钠通道的取代四氢呋喃调节剂的合成方法
TW202535867A (zh) 2023-10-23 2025-09-16 美商維泰克斯製藥公司 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法
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WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
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Also Published As

Publication number Publication date
HK1203074A1 (zh) 2015-10-16
CN104136442A (zh) 2014-11-05
AU2013209958B2 (en) 2017-09-07
CA2863343A1 (en) 2013-07-25
AU2013209958A1 (en) 2014-08-07
EP2804868B1 (en) 2017-04-12
EP2804868A1 (en) 2014-11-26
MX2014008591A (es) 2014-08-22
US20150005304A1 (en) 2015-01-01
ES2631611T3 (es) 2017-09-01
WO2013109521A1 (en) 2013-07-25
CN104136442B (zh) 2016-12-21
JP2015505321A (ja) 2015-02-19
US9403839B2 (en) 2016-08-02
NZ627259A (en) 2016-12-23

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