CN105814067B - 作为钠通道调节剂的吡啶酮酰胺的前药 - Google Patents

作为钠通道调节剂的吡啶酮酰胺的前药 Download PDF

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CN105814067B
CN105814067B CN201480068225.9A CN201480068225A CN105814067B CN 105814067 B CN105814067 B CN 105814067B CN 201480068225 A CN201480068225 A CN 201480068225A CN 105814067 B CN105814067 B CN 105814067B
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compound
pain
another embodiment
fluoro
benzamido
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CN105814067A (zh
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C·安德森
S·S·阿迪达-鲁阿
J·M·C·格莱克
B·张
B·J·利特勒
A·科沙瓦尔兹-舒克立
T·E·阿尔卡桥
D·T·贝尔蒙特
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
    • C07D213/16—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
    • C07D213/18—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings

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  • Neurology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Thermistors And Varistors (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201480068225.9A 2013-12-13 2014-12-12 作为钠通道调节剂的吡啶酮酰胺的前药 Active CN105814067B (zh)

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US201361915937P 2013-12-13 2013-12-13
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PCT/US2014/069916 WO2015089361A1 (en) 2013-12-13 2014-12-12 Prodrugs of pyridone amides useful as modulators of sodium channels

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108395452A (zh) * 2013-12-13 2018-08-14 沃泰克斯药物股份有限公司 作为钠通道调节剂的吡啶酮酰胺的前药
WO2021047622A1 (zh) * 2019-09-12 2021-03-18 上海济煜医药科技有限公司 吡啶氮氧化合物及其制备方法和用途

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KR102200176B1 (ko) 2012-05-08 2021-01-11 에어로믹스, 인코포레이티드 신규 방법
BR112015017997B1 (pt) 2013-01-31 2023-03-07 Vertex Pharmaceuticals Incorporated Amidas de quinolina e quinoxalina como moduladores de canais de sódio, seus usos, e composição farmacêutica
ES2857687T3 (es) 2013-01-31 2021-09-29 Vertex Pharma Piridona amidas como moduladores de los canales de sodio
BR112016000825B1 (pt) 2013-07-19 2023-04-25 Vertex Pharmaceuticals Incorporated Compostos moduladores de sulfonamidas dos canais de sódio, composição farmacêutica, e uso dos mesmos
RU2691951C2 (ru) 2013-11-06 2019-06-19 Аэромикс, Инк. Новые составы
WO2017075222A1 (en) * 2015-10-30 2017-05-04 Lieber Institute For Brain Development Treatment of neurological and neurodevelopmental diseases and disorders associated with aberrant ion channel expression and activity
US20170239183A1 (en) * 2016-02-23 2017-08-24 PixarBio Corporation COMPOSITIONS COMPRISING NAv1.7 SELECTIVE INHIBITORS FOR TREATING ACUTE, POST-OPERATIVE, OR CHRONIC PAIN AND METHODS OF USING THE SAME
KR20190005991A (ko) 2016-05-13 2019-01-16 에어로믹스, 인코포레이티드 결정
AU2018271110A1 (en) 2017-05-16 2019-12-05 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
CN111065383A (zh) 2017-07-11 2020-04-24 沃泰克斯药物股份有限公司 用作钠通道调节剂的羧酰胺
US10495175B2 (en) * 2017-08-08 2019-12-03 Ford Global Technologies, Llc Composite materials having embedded metal ropes for increased damping capacity and methods of manufacturing same
US11529337B2 (en) 2018-02-12 2022-12-20 Vertex Pharmaceuticals Incorporated Method of treating pain
US12234221B2 (en) 2018-07-09 2025-02-25 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting NAV1.8
SG11202100137TA (en) 2018-07-09 2021-02-25 Lieber Institute Inc PYRIDAZINE COMPOUNDS FOR INHIBITING Nav1.8
CN113272293B (zh) 2018-11-02 2024-06-14 默沙东有限责任公司 作为nav1.8抑制剂的2-胺基-n-杂芳基-烟酰胺
EP3873468A4 (en) 2018-11-02 2022-10-26 Merck Sharp & Dohme LLC 2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
CN112996774B (zh) * 2019-01-25 2022-11-22 江苏恒瑞医药股份有限公司 2-氧代-1,2-二氢吡啶类衍生物、其制备方法及其在医药上的应用
TW202102480A (zh) * 2019-02-20 2021-01-16 大陸商江蘇恆瑞醫藥股份有限公司 ６－側氧基－１，６－二氫噠嗪類前藥衍生物、其製備方法及其在醫藥上的應用
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020206119A1 (en) 2019-04-02 2020-10-08 Vertex Pharmaceuticals Incorporated Process for making pyridone amides and prodrugs thereof useful as modulators of sodium channels
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
WO2021018165A1 (zh) * 2019-07-30 2021-02-04 江苏恒瑞医药股份有限公司 吡啶苯甲酰胺类衍生物、其制备方法及其在医药上的应用
WO2021032074A1 (zh) * 2019-08-19 2021-02-25 江苏恒瑞医药股份有限公司 苯甲酰胺稠芳环类衍生物、其制备方法及其在医药上的应用
LT4069691T (lt) 2019-12-06 2024-12-10 Vertex Pharmaceuticals Incorporated Pakeistieji tetrahidrofuranai kaip natrio kanalų moduliatoriai
CN114437062B (zh) * 2020-04-30 2024-05-17 成都海博为药业有限公司 一种可作为钠通道调节剂的化合物及其用途
CA3182633A1 (en) 2020-06-17 2021-12-23 Ashok Arasappan 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors
CN113880771B (zh) * 2020-07-03 2023-09-19 福建盛迪医药有限公司 一种选择性Nav抑制剂的结晶形式及其制备方法
US20230293556A1 (en) * 2020-08-05 2023-09-21 Jiangsu Simcere Pharmaceutical Co., Ltd. Pharmaceutical composition of aquaporin inhibitor and preparation method thereof
TW202214259A (zh) * 2020-08-19 2022-04-16 大陸商江蘇恆瑞醫藥股份有限公司 一種選擇性ＮａＶ抑制劑的前藥及其晶型
CN111808019B (zh) * 2020-09-08 2020-11-27 上海济煜医药科技有限公司 一种并环化合物及其应用
WO2022121805A1 (zh) * 2020-12-07 2022-06-16 成都康弘药业集团股份有限公司 作为Nav1.8抑制剂的并环化合物及其用途
CN114031518B (zh) * 2020-12-08 2023-08-18 成都海博为药业有限公司 一种苄胺或苄醇衍生物及其用途
MX2023007244A (es) * 2020-12-18 2023-06-29 Glaxosmithkline Ip Dev Ltd Compuestos quimicos utiles para inhibir los canales de sodio activados por voltaje de nav1.8 y tratar las enfermedades mediadas por nav1.8.
TW202302118A (zh) * 2021-02-26 2023-01-16 大陸商江蘇恒瑞醫藥股份有限公司 一種選擇性ｎａｖ抑制劑的可藥用鹽、結晶形式及其製備方法
GEP20257795B (en) 2021-05-07 2025-09-25 Merck Sharp & Dohme Llc Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors
EP4346818B1 (en) 2021-06-04 2025-12-03 Vertex Pharmaceuticals Incorporated Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide
EP4347032A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
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