ES2688590T3 - Profármacos de amidas de piridona útiles como moduladores de los canales de sodio - Google Patents

Profármacos de amidas de piridona útiles como moduladores de los canales de sodio Download PDF

Info

Publication number
ES2688590T3
ES2688590T3 ES14824658.0T ES14824658T ES2688590T3 ES 2688590 T3 ES2688590 T3 ES 2688590T3 ES 14824658 T ES14824658 T ES 14824658T ES 2688590 T3 ES2688590 T3 ES 2688590T3
Authority
ES
Spain
Prior art keywords
pain
alkyl
compound
another embodiment
halogen
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.)
Active
Application number
ES14824658.0T
Other languages
English (en)
Spanish (es)
Inventor
Corey Anderson
Sara Sabina Hadida-Ruah
Julian Marian Charles Golec
Beili Zhang
Benjamin Joseph Littler
Ali Keshavarz-Shokri
Tim Edward Alcacio
Daniel T. Belmont
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2688590T3 publication Critical patent/ES2688590T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/06Heterocyclic 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
    • C07D213/16Heterocyclic 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
    • C07D213/18Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/59Hydrogenated pyridine rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • 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)
ES14824658.0T 2013-12-13 2014-12-12 Profármacos de amidas de piridona útiles como moduladores de los canales de sodio Active ES2688590T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361915937P 2013-12-13 2013-12-13
US201361915937P 2013-12-13
PCT/US2014/069916 WO2015089361A1 (en) 2013-12-13 2014-12-12 Prodrugs of pyridone amides useful as modulators of sodium channels

Publications (1)

Publication Number Publication Date
ES2688590T3 true ES2688590T3 (es) 2018-11-05

Family

ID=52293220

Family Applications (2)

Application Number Title Priority Date Filing Date
ES14824658.0T Active ES2688590T3 (es) 2013-12-13 2014-12-12 Profármacos de amidas de piridona útiles como moduladores de los canales de sodio
ES18186616T Active ES2986650T3 (es) 2013-12-13 2014-12-12 Proceso y productos intermedios para preparar profármacos de amidas de piridona útiles como moduladores de los canales de sodio

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES18186616T Active ES2986650T3 (es) 2013-12-13 2014-12-12 Proceso y productos intermedios para preparar profármacos de amidas de piridona útiles como moduladores de los canales de sodio

Country Status (33)

Country Link
US (6) US9163042B2 (enExample)
EP (2) EP3459958B1 (enExample)
JP (3) JP6463580B2 (enExample)
KR (1) KR102435145B1 (enExample)
CN (2) CN105814067B (enExample)
AP (1) AP2016009287A0 (enExample)
AU (2) AU2014362255B2 (enExample)
BR (1) BR122020007729B1 (enExample)
CA (1) CA2931550C (enExample)
CL (1) CL2016001400A1 (enExample)
CY (1) CY1121030T1 (enExample)
DK (1) DK3080134T3 (enExample)
EC (1) ECSP16025201A (enExample)
ES (2) ES2688590T3 (enExample)
GE (2) GEP20207082B (enExample)
HR (1) HRP20181563T1 (enExample)
IL (1) IL246061B (enExample)
LT (1) LT3080134T (enExample)
MX (2) MX379264B (enExample)
NZ (2) NZ760006A (enExample)
PE (1) PE20161131A1 (enExample)
PH (1) PH12016501028A1 (enExample)
PL (1) PL3080134T3 (enExample)
PT (1) PT3080134T (enExample)
RS (1) RS57700B1 (enExample)
RU (1) RU2692766C1 (enExample)
SG (2) SG11201604477SA (enExample)
SI (1) SI3080134T1 (enExample)
SM (1) SMT201800521T1 (enExample)
TW (3) TWI703154B (enExample)
UA (1) UA121379C2 (enExample)
WO (1) WO2015089361A1 (enExample)
ZA (1) ZA201603546B (enExample)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US9163042B2 (en) * 2013-12-13 2015-10-20 Vertex Pharmaceuticals Incorporated Prodrugs of pyridone amides useful as modulators of sodium channels
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
PH12022550584A1 (en) * 2019-09-12 2024-03-04 Orion Corp Pyridine oxynitride, preparation method therefor and use thereof
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
CN117858875A (zh) 2021-06-04 2024-04-09 沃泰克斯药物股份有限公司 羟基和(卤代)烷氧基取代的四氢呋喃作为钠通道调节剂
CA3221938A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
CN117794919A (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)四氢呋喃甲酰胺类似物作为钠通道调节剂
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
UY39881A (es) 2021-08-02 2023-06-15 Eurofarma Laboratorios S A “COMPUESTOS N-ACILHIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS”
UY39882A (es) 2021-08-02 2023-06-15 Eurofarma Laboratorios S A COMPUESTOS NACILHIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS
CN114288289A (zh) * 2022-02-17 2022-04-08 昆山彭济凯丰生物科技有限公司 具有镇痛和/或止痒功能的药物组合物及其应用
WO2023160509A1 (zh) * 2022-02-25 2023-08-31 中国科学院上海药物研究所 脒类衍生化合物及其制备方法和用途
WO2023205778A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CR20240513A (es) 2022-04-22 2025-04-30 Vertex Pharma Compuestos de heteroarilo para el tratamiento del dolor
WO2023205468A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
JP2025516005A (ja) 2022-04-25 2025-05-23 サイトワン セラピューティクス インコーポレイテッド 疼痛の処置のためのnav1.8の二環式複素環アミド阻害剤
EP4534529A1 (en) * 2022-06-02 2025-04-09 Shanghai Jemincare Pharmaceutical Co., Ltd. Method for preparing pyridine oxynitride compound
EP4536673A1 (en) * 2022-06-09 2025-04-16 GlaxoSmithKline Intellectual Property Development Ltd Chemical compounds
WO2024067783A1 (zh) * 2022-09-28 2024-04-04 上海济煜医药科技有限公司 含磷类化合物及其制备方法和医药应用
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
AR131690A1 (es) 2023-01-30 2025-04-23 Eurofarma Laboratorios S A COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y LOS KITS
WO2024159287A1 (pt) 2023-01-30 2024-08-08 Eurofarma Laboratórios S.A. Hidroxamatos bloqueadores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits
EP4660182A1 (en) 2023-01-30 2025-12-10 Eurofarma Laboratórios S.A. Nav1.7- and/or nav1.8-inhibiting aryl pyridine compounds, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits
AR131715A1 (es) 2023-01-30 2025-04-23 Eurofarma Laboratorios S A AMIDAS BLOQUEADORAS DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y KITS
AR131658A1 (es) 2023-01-30 2025-04-16 Eurofarma Laboratorios S A Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y sus kits
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
TW202523313A (zh) 2023-10-23 2025-06-16 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
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

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02245793A (ja) 1989-03-20 1990-10-01 Hitachi Ltd マトリックス表示装置
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
AU7588101A (en) 2000-07-10 2002-02-05 Aurora Biosciences Corp Ion channel assay methods
JP2003034671A (ja) 2001-05-17 2003-02-07 Nippon Nohyaku Co Ltd ベンズアミド誘導体及び農園芸用薬剤並びにその使用方法
SI1490064T1 (sl) 2002-02-14 2010-01-29 Pharmacia Corp Substituirani piridinoni kot modulatorji p38 MAP kinaze
CA2539227A1 (en) * 2003-08-08 2005-02-17 Vertex Pharmaceuticals Incorporated Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
WO2006011050A2 (en) 2004-07-23 2006-02-02 Pfizer Limited Pyridine derivatives
KR20080109918A (ko) 2006-04-11 2008-12-17 버텍스 파마슈티칼스 인코포레이티드 전압 개폐 나트륨 채널의 억제제로서 유용한 조성물
CN103271906A (zh) 2006-10-12 2013-09-04 泽农医药公司 螺-吲哚酮化合物作为治疗剂的用途
CA2684105C (en) 2007-05-03 2011-09-06 Pfizer Limited Pyridine derivatives
KR20100075631A (ko) 2007-10-11 2010-07-02 버텍스 파마슈티칼스 인코포레이티드 전압­개폐 나트륨 채널의 억제제로서 유용한 아릴 아미드
JP5436434B2 (ja) * 2007-10-11 2014-03-05 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 電位開口型ナトリウムチャネルの阻害剤として有用なアミド
AU2008310660A1 (en) 2007-10-11 2009-04-16 Vertex Pharmaceuticals Incorporated Heteroaryl amides useful as inhibitors of voltage-gated sodium channels
MX2011000656A (es) * 2008-07-23 2011-02-23 Hoffmann La Roche Compuestos heterociclicos antiviricos.
BRPI0919648A2 (pt) 2008-10-29 2015-12-08 Hoffmann La Roche novos derivados de fenil amida ou piridil amida e seu uso como agonistas de gpbar1
KR101370185B1 (ko) 2008-12-23 2014-03-05 에프. 호프만-라 로슈 아게 P2x7 조절제로서의 디히드로피리돈 아미드
MX2011006904A (es) 2008-12-26 2011-07-20 Dainippon Sumitomo Pharma Co Compuesto heterociclico biciclico novedoso.
JP5685203B2 (ja) 2009-05-29 2015-03-18 ラクオリア創薬株式会社 カルシウムチャネル遮断薬またはナトリウムチャネル遮断薬としてのアリール置換カルボキサミド誘導体
TW201103904A (en) 2009-06-11 2011-02-01 Hoffmann La Roche Janus kinase inhibitor compounds and methods
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
CA2771472A1 (en) 2009-09-04 2011-03-10 Zalicus Pharmaceuticals Ltd. Oxopiperazine derivatives for the treatment of pain and epilepsy
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
JP2014500303A (ja) * 2010-12-22 2014-01-09 パーデュー、ファーマ、リミテッド、パートナーシップ ナトリウムチャネル遮断剤としての置換ピリジン
TW201604196A (zh) 2011-02-02 2016-02-01 維泰克斯製藥公司 作為離子通道調節劑之吡咯并吡-螺環哌啶醯胺
MX2013009393A (es) 2011-02-18 2013-08-29 Vertex Pharma Piperidinamidas cromano-espirociclicas como moduladores de canales de iones.
US20140187533A1 (en) 2011-03-03 2014-07-03 Zalicus Pharmaceuticals Ltd. Benzimidazole inhibitors of the sodium channel
EP2686325B1 (en) 2011-03-14 2016-12-14 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
TWI567061B (zh) * 2011-07-01 2017-01-21 吉李德科學股份有限公司 用於治療成癮之化合物
WO2013012104A1 (ko) 2011-07-18 2013-01-24 엘지전자 주식회사 전자기기 및 전자기기의 동작 방법
EP3255041A1 (en) * 2011-09-02 2017-12-13 Purdue Pharma L.P. Pyrimidines as sodium channel blockers
MX337469B (es) 2011-10-26 2016-03-02 Pfizer Ltd Derivados de (4-fenilimidazol-2-il)etilamina utiles como moduladores de canal de sodio.
US9403839B2 (en) 2012-01-16 2016-08-02 Vertex Pharmaceuticals Incorporated Pyran-spirocyclic piperidine amides as modulators of ion channels
ES2548228T3 (es) 2012-02-03 2015-10-15 Pfizer Inc Derivados de bencimidazol e imidazopiridina como moduladores de canal de sodio
US20130225529A1 (en) * 2012-02-27 2013-08-29 Basil Rigas Phospho-ester derivatives and uses thereof
WO2013131018A1 (en) 2012-03-02 2013-09-06 Zalicus Pharmaceuticals Ltd. Biaryl inhibitors of the sodium channel
GEP201606560B (en) 2012-03-06 2016-10-25 Pfizer Macrocyclic derivatives for the treatment of proliferative diseases
TWI606048B (zh) 2013-01-31 2017-11-21 帝人製藥股份有限公司 唑苯衍生物
CA2898653C (en) 2013-01-31 2021-09-28 Vertex Pharmaceuticals Incorporated Amides as modulators of sodium channels
ES2857687T3 (es) 2013-01-31 2021-09-29 Vertex Pharma Piridona amidas como moduladores de los canales de sodio
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
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
US9163042B2 (en) 2013-12-13 2015-10-20 Vertex Pharmaceuticals Incorporated Prodrugs of pyridone amides useful 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
US11529337B2 (en) 2018-02-12 2022-12-20 Vertex Pharmaceuticals Incorporated Method of treating pain

Also Published As

Publication number Publication date
US11773119B2 (en) 2023-10-03
EP3080134B1 (en) 2018-08-01
CN108395452A (zh) 2018-08-14
HRP20181563T1 (hr) 2018-11-30
TW201609779A (zh) 2016-03-16
JP6463580B2 (ja) 2019-02-06
SG10201913313QA (en) 2020-03-30
PT3080134T (pt) 2018-11-08
US20200377535A1 (en) 2020-12-03
WO2015089361A1 (en) 2015-06-18
UA121379C2 (uk) 2020-05-25
IL246061A0 (en) 2016-07-31
EP3080134A1 (en) 2016-10-19
GEP20217223B (en) 2021-02-10
JP2019055974A (ja) 2019-04-11
MX2016007258A (es) 2016-08-04
US9163042B2 (en) 2015-10-20
US10253054B2 (en) 2019-04-09
US10787472B2 (en) 2020-09-29
AU2019271928B2 (en) 2021-04-22
AU2014362255B2 (en) 2019-08-29
TW202014425A (zh) 2020-04-16
US9464102B2 (en) 2016-10-11
TWI703154B (zh) 2020-09-01
CN105814067A (zh) 2016-07-27
JP2020189862A (ja) 2020-11-26
GEP20207082B (en) 2020-04-10
EP3459958B1 (en) 2024-08-07
SI3080134T1 (sl) 2018-11-30
CY1121030T1 (el) 2019-12-11
ZA201603546B (en) 2023-12-20
MX2021000781A (es) 2021-04-28
TWI668226B (zh) 2019-08-11
US9828397B2 (en) 2017-11-28
US20190276483A1 (en) 2019-09-12
TW201920221A (zh) 2019-06-01
NZ720444A (en) 2022-07-29
AU2014362255A1 (en) 2016-06-09
RU2019117783A (ru) 2020-02-20
KR102435145B1 (ko) 2022-08-24
ECSP16025201A (es) 2017-02-24
BR122020007729B1 (pt) 2023-05-09
CA2931550C (en) 2023-09-26
CN105814067B (zh) 2018-05-18
LT3080134T (lt) 2018-11-12
CA2931550A1 (en) 2015-06-18
TWI651329B (zh) 2019-02-21
CL2016001400A1 (es) 2016-12-16
MX379264B (es) 2025-03-11
AP2016009287A0 (en) 2016-06-30
PL3080134T3 (pl) 2019-01-31
RS57700B1 (sr) 2018-12-31
NZ760006A (en) 2022-07-29
ES2986650T3 (es) 2024-11-12
US20150166589A1 (en) 2015-06-18
JP7465174B2 (ja) 2024-04-10
EP3459958A1 (en) 2019-03-27
PH12016501028A1 (en) 2016-07-04
DK3080134T3 (en) 2018-10-22
AU2019271928A1 (en) 2019-12-19
PE20161131A1 (es) 2016-10-29
US20160009743A1 (en) 2016-01-14
RU2692766C1 (ru) 2019-06-27
SMT201800521T1 (it) 2018-11-09
US20160376295A1 (en) 2016-12-29
IL246061B (en) 2021-12-01
SG11201604477SA (en) 2016-07-28
GEAP201914203A (enExample) 2019-11-25
KR20160098380A (ko) 2016-08-18
US20180044361A1 (en) 2018-02-15
CN108395452B (zh) 2021-08-03
JP2017504591A (ja) 2017-02-09

Similar Documents

Publication Publication Date Title
ES2688590T3 (es) Profármacos de amidas de piridona útiles como moduladores de los canales de sodio
ES2575478T3 (es) Compuesto de guanidina
CN103492370B (zh) 取代的二氨基甲酰胺和二氨基甲腈嘧啶,其组合物,和用其治疗的方法
AU2016306555B2 (en) Salts of an LSD1 inhibitor
ES2685819T3 (es) Formas mórficas de ésteres de hexadeciloxipropil-fosfonato
ES2639052T3 (es) Forma polimórfica de hidrocloruro de pridopidina
ES2875384T3 (es) Forma cristalina del inhibidor de la quinasa BTK y método de preparación del mismo
TW202311259A (zh) 化合物i的新形式及其應用
KR102666390B1 (ko) 고체 형태
JP2020097526A (ja) 複素環化合物
AU2023201010B2 (en) Solid forms of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-n-benzylacetamide
AU2014239520A1 (en) Methods of synthesizing substituted purine compounds
BR112019012340B1 (pt) Forma a de citrato cristalino de 5-(2,4-diamino-pirimidin-5-iloxi)-4-isopropil-2-metoxibenzenossulfonamida, bem como sua composição farmacêutica e usos
TW202124373A (zh) 1,3,5-三衍生物或其溶劑合物之結晶及其製造方法
CN116964052A (zh) 调节nlrp3的4-氨基-6-氧代-哒嗪衍生物
AU2019206118A1 (en) Salts and polymorphs of a substituted imidazopyridinyl-aminopyridine compound
CN116332904A (zh) Hpk1抑制剂及其在医药上的应用
Break et al. Design, synthesis, and greener pasture biological assessment of a novel nucleoside: 1-(α-D-ribofuranosyl)-6, 7-difluoro-2-methyl-4-quinazolinone as an inhibitor of COVID-19 and Alzheimer's disease
WO2024114663A1 (zh) 三嗪基甲基环烷基羧酸衍生物的晶型及其应用
AU2022347682A1 (en) Polymorph and application of pyrimidine derivative and pharmaceutically acceptable salt thereof
HK40024686A (en) Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
JPWO2016181894A1 (ja) 環状化合物
HK40025304A (en) Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
HK40024686B (zh) 取代的二氨基甲醯胺和二氨基甲腈嘧啶,其组合物,和用其治疗的方法
BR112019022457B1 (pt) Composto, medicamento, e, uso do composto