CN104136442B - 作为离子通道调节剂的吡喃‑螺环哌啶酰胺类 - Google Patents

作为离子通道调节剂的吡喃‑螺环哌啶酰胺类 Download PDF

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Publication number
CN104136442B
CN104136442B CN201380010104.4A CN201380010104A CN104136442B CN 104136442 B CN104136442 B CN 104136442B CN 201380010104 A CN201380010104 A CN 201380010104A CN 104136442 B CN104136442 B CN 104136442B
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och
pain
compound
mmol
isopropoxy
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CN104136442A (zh
Inventor
S·S·阿迪达-鲁阿
V·阿鲁姆加姆
M·P·丹尼诺
B·A·弗里曼
E·A·卡莱勒
M·T·米勒
J·威
周竞兰
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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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (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)
CN201380010104.4A 2012-01-16 2013-01-15 作为离子通道调节剂的吡喃‑螺环哌啶酰胺类 Expired - Fee Related CN104136442B (zh)

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 (2)

Publication Number Publication Date
CN104136442A CN104136442A (zh) 2014-11-05
CN104136442B true CN104136442B (zh) 2016-12-21

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Country Status (10)

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

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LT3080134T (lt) 2013-12-13 2018-11-12 Vertex Pharmaceuticals Incorporated Piridono amidų provaistai, naudotini kaip natrio kanalų moduliatoriai
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
US11358977B2 (en) 2017-05-16 2022-06-14 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
SG11202000230VA (en) 2017-07-11 2020-02-27 Vertex Pharma Carboxamides as modulators of sodium channels
KR102731924B1 (ko) * 2017-11-01 2024-11-19 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 스피로시클릭 화합물
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
WO2019157505A1 (en) 2018-02-12 2019-08-15 Vertex Pharmaceuticals Incorporated A method of treating pain
TWI707849B (zh) 2018-02-13 2020-10-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
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
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
AU2019301628C1 (en) 2018-07-09 2025-02-06 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting NaV1.8
AU2019302534B2 (en) 2018-07-09 2024-10-03 Lieber Institute, Inc. Pyridazine compounds for inhibiting NaV1.8
EP3820572B1 (en) 2018-07-13 2023-08-16 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates 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
CA3164134A1 (en) 2019-12-06 2021-06-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans 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
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
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
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
WO2022256676A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
UY40234A (es) 2022-04-22 2023-11-15 Vertex Pharma Compuestos heteroarilo para el tratamiento del dolor
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
GEAP202516634A (en) 2022-04-22 2025-02-25 Vertex Pharma Heteroaryl compounds for the treatment of pain
AU2023257313A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds 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
WO2025090465A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2025090480A1 (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
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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WO2010002483A1 (en) * 2008-07-03 2010-01-07 Cv Therapeutics, Inc. Optionally condensed dihydro pyridine, dihydropyrimidine and dihydro pyrane derivatives acting as late sodium channel blockers
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CN102036985A (zh) * 2007-11-13 2011-04-27 沃泰克斯药物股份有限公司 用于治疗疼痛的作为离子通道调节剂的4(-3-(-2-(苯基)吗啉代)-2-氧代吡咯烷-1-基)-n-(噻唑-2-基)苯磺酰胺衍生物和相关化合物
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US20060052597A1 (en) * 2002-10-22 2006-03-09 Best Desmond J Aryloxyalkylamine derivatives as h3 receptor ligands
CN101910166A (zh) * 2007-11-13 2010-12-08 沃泰克斯药物股份有限公司 用作钠离子通道调节剂的杂环衍生物
CN102036985A (zh) * 2007-11-13 2011-04-27 沃泰克斯药物股份有限公司 用于治疗疼痛的作为离子通道调节剂的4(-3-(-2-(苯基)吗啉代)-2-氧代吡咯烷-1-基)-n-(噻唑-2-基)苯磺酰胺衍生物和相关化合物
CN102099356A (zh) * 2008-07-01 2011-06-15 沃泰克斯药物股份有限公司 用作离子通道调节剂的杂环衍生物
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WO2012125613A1 (en) * 2011-03-14 2012-09-20 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels

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Publication number Publication date
JP2015505321A (ja) 2015-02-19
US20150005304A1 (en) 2015-01-01
JP6215230B2 (ja) 2017-10-18
CN104136442A (zh) 2014-11-05
EP2804868A1 (en) 2014-11-26
EP2804868B1 (en) 2017-04-12
AU2013209958B2 (en) 2017-09-07
CA2863343A1 (en) 2013-07-25
WO2013109521A1 (en) 2013-07-25
AU2013209958A1 (en) 2014-08-07
US9403839B2 (en) 2016-08-02
MX2014008591A (es) 2014-08-22
NZ627259A (en) 2016-12-23
ES2631611T3 (es) 2017-09-01
HK1203074A1 (zh) 2015-10-16

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