AU2012229187B2 - Morpholine-spirocyclic piperidine amides as modulators of ion channels - Google Patents

Morpholine-spirocyclic piperidine amides as modulators of ion channels Download PDF

Info

Publication number
AU2012229187B2
AU2012229187B2 AU2012229187A AU2012229187A AU2012229187B2 AU 2012229187 B2 AU2012229187 B2 AU 2012229187B2 AU 2012229187 A AU2012229187 A AU 2012229187A AU 2012229187 A AU2012229187 A AU 2012229187A AU 2012229187 B2 AU2012229187 B2 AU 2012229187B2
Authority
AU
Australia
Prior art keywords
pain
mmol
optionally substituted
alkyl
halo
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.)
Ceased
Application number
AU2012229187A
Other languages
English (en)
Other versions
AU2012229187A1 (en
Inventor
Vijayalaksmi Arumugam
Hayley Marie Binch
Michael Paul Deninno
Lev Tyler Dewey Fanning
Bryan A. Frieman
Peter Diederik Jan Grootenhuis
Sara Sabina Hadida-Ruah
Nicole Hilgraf
Dennis James Hurley
Pramod Joshi
Edward Adam Kallel
Mark Thomas Miller
Joseph Pontillo
Urvi Jagdishbhai Sheth
Alina Silina
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
Publication of AU2012229187A1 publication Critical patent/AU2012229187A1/en
Application granted granted Critical
Publication of AU2012229187B2 publication Critical patent/AU2012229187B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • 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
    • A61P25/06Antimigraine 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2012229187A 2011-03-14 2012-03-13 Morpholine-spirocyclic piperidine amides as modulators of ion channels Ceased AU2012229187B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161452538P 2011-03-14 2011-03-14
US61/452,538 2011-03-14
US201161567809P 2011-12-07 2011-12-07
US61/567,809 2011-12-07
PCT/US2012/028882 WO2012125613A1 (en) 2011-03-14 2012-03-13 Morpholine-spirocyclic piperidine amides as modulators of ion channels

Publications (2)

Publication Number Publication Date
AU2012229187A1 AU2012229187A1 (en) 2013-09-19
AU2012229187B2 true AU2012229187B2 (en) 2016-11-10

Family

ID=45888492

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012229187A Ceased AU2012229187B2 (en) 2011-03-14 2012-03-13 Morpholine-spirocyclic piperidine amides as modulators of ion channels

Country Status (9)

Country Link
US (2) US8828996B2 (enExample)
EP (1) EP2686325B1 (enExample)
JP (1) JP6088443B2 (enExample)
CN (1) CN103517910B (enExample)
AU (1) AU2012229187B2 (enExample)
CA (1) CA2829803A1 (enExample)
ES (1) ES2618929T3 (enExample)
MX (1) MX347982B (enExample)
WO (1) WO2012125613A1 (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8598164B2 (en) 2010-05-06 2013-12-03 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
SG192248A1 (en) 2011-02-02 2013-09-30 Vertex Pharma Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels
MX2013009393A (es) 2011-02-18 2013-08-29 Vertex Pharma Piperidinamidas cromano-espirociclicas como moduladores de canales de iones.
CN104136442B (zh) * 2012-01-16 2016-12-21 沃泰克斯药物股份有限公司 作为离子通道调节剂的吡喃‑螺环哌啶酰胺类
US9139529B2 (en) 2013-01-31 2015-09-22 Vertex Pharmaceuticals Incorporated Substituted quinoxalines as sodium channel modulators
IL269964B1 (en) 2013-01-31 2025-09-01 Vertex Pharma Pyridone amide compounds, compositions containing them and uses thereof
SG11201600383SA (en) 2013-07-19 2016-02-26 Vertex Pharma Sulfonamides as modulators of sodium channels
UA120039C2 (uk) 2013-10-14 2019-09-25 ЕЙСАЙ Ар ЕНД Ді МЕНЕДЖМЕНТ КО., ЛТД. Селективно заміщені сполуки хіноліну
BR112016008378B1 (pt) 2013-10-14 2022-11-08 Eisai R&D Management Co., Ltd Compostos de quinolina seletivamente substituídos ou sal dos mesmos, e composição farmacêutica contendo os ditos compostos
GEP20207082B (en) 2013-12-13 2020-04-10 Vertex Pharma Prodrugs of pyridone amides useful as modulators of sodium channels
TW201615643A (zh) * 2014-06-02 2016-05-01 伊史帝夫博士實驗室股份有限公司 具有多重模式抗疼痛活性之1-氧雜-4,9-二氮雜螺十一烷化合物之烷基與芳基衍生物
TWI685497B (zh) * 2014-06-02 2020-02-21 西班牙商伊史帝夫製藥公司 具有多重模式抗疼痛活性的1-氧雜-4,9-二氮雜螺十一烷化合物之烷基衍生物
TW201615642A (zh) 2014-06-02 2016-05-01 伊史帝夫博士實驗室股份有限公司 具有多重模式抗疼痛活性的1-氧雜-4,9-二氮雜螺十一烷化合物之醯胺衍生物
CR20180047A (es) 2015-07-31 2018-03-07 Pfizer Derivados de 1,1,1-trifluoro-3-hidroxipropan-2-il carbamato y derivados de 1,1,1-trifluoro-4-hidroxibutan-2-il carbamato como inhibidores de magl
PT3365345T (pt) * 2015-10-23 2020-05-27 Esteve Labor Dr Composto de oxa- azaespiro tendo atividade contra a dor
TW201734009A (zh) 2015-10-23 2017-10-01 艾斯提夫博士實驗股份有限公司 具有抗疼痛活性的經取代的□啉衍生物
SI3365346T1 (sl) * 2015-10-23 2020-04-30 Esteve Pharmaceuticals, S.A. Spojine oksa diazaspiro s protibolečinskim delovanjem
AR106697A1 (es) 2015-11-16 2018-02-07 Esteve Labor Dr Compuestos oxadiazoespíricos para el tratamiento del abuso y la adicción a las drogas
PL3429352T3 (pl) * 2016-03-17 2022-08-22 Fmc Corporation Sposób konwersji enancjomeru-S do jego postaci racemicznej
MX2019008626A (es) 2017-01-20 2019-09-19 Pfizer Derivados de 1,1,1-trifluoro-3-hidroxipropan-2-ilcarbamato como inhibidores de monoacilglicerol lipasa (magl).
CA3050853A1 (en) 2017-01-23 2018-07-26 Pfizer Inc. Heterocyclic spiro compounds as magl inhibitors
CN110740993B (zh) 2017-05-16 2023-09-01 沃泰克斯药物股份有限公司 用作钠通道调节剂的氘代吡啶酮酰胺及其前药
AU2018300150A1 (en) 2017-07-11 2020-01-30 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
EP3697795B1 (en) 2017-10-17 2023-11-22 Acondicionamiento Tarrasense Salts of (r)-9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one
CA3091012A1 (en) 2018-02-12 2019-08-15 Vertex Pharmaceuticals Incorporated A method of treating pain
EP3820860B1 (en) 2018-07-09 2025-10-15 Lieber Institute, Inc. Pyridazine compounds for inhibiting nav1.8
WO2020014246A1 (en) 2018-07-09 2020-01-16 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting nav1.8
WO2020146682A1 (en) 2019-01-10 2020-07-16 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
CN110452183B (zh) * 2019-09-04 2023-03-14 中国科学院上海有机化学研究所 一种手性杂环化合物的制备方法
HRP20241695T1 (hr) 2019-12-06 2025-02-14 Vertex Pharmaceuticals Incorporated Supstituirani tetrahidrofurani kao modulatori natrijevih kanala
CN114901640A (zh) * 2019-12-24 2022-08-12 兹杜斯生命科学有限公司 适用于治疗血脂异常的新型化合物
CN113278021B (zh) * 2021-05-29 2022-09-23 天津全和诚科技有限责任公司 1,7-二氮杂螺[3.5]壬烷-7-甲酸叔丁酯及其草酸盐的制备方法
US20240368135A1 (en) 2021-06-04 2024-11-07 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
KR20240031300A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널 조절제로서의 n-(하이드록시알킬 (헤테로)아릴) 테트라하이드로푸란 카르복스아미드
AU2022285758A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
JP2024520649A (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 (2r,3s,4s,5r)-4-[[3-(3,4-ジフルオロ-2-メトキシ-フェニル)-4,5-ジメチル-5-(トリフルオロメチル)テトラヒドロフラン-2-カルボニル]アミノ]ピリジン-2-カルボキサミドを含む固体剤形及び投与レジメン
EP4347033A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
CA3221939A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
CN118382436A (zh) * 2021-10-13 2024-07-23 凡况生化公司 葡糖脑苷脂酶活性的小分子调节剂及其用途
AR129104A1 (es) 2022-04-22 2024-07-17 Vertex Pharma Compuestos heteroarilo para el tratamiento del dolor
AU2023255771A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
AU2023255558A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CA3256248A1 (en) 2022-04-22 2023-10-26 Vertex Pharma HETEROARYL COMPOUNDS FOR PAIN RELIEF
IL321269A (en) 2022-12-06 2025-08-01 Vertex Pharma 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
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
US20250186419A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens for treating pain

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020013325A1 (en) * 1995-09-29 2002-01-31 Fisher Matthew J. Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation
US20060052597A1 (en) * 2002-10-22 2006-03-09 Best Desmond J Aryloxyalkylamine derivatives as h3 receptor ligands
WO2011092198A1 (en) * 2010-01-26 2011-08-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3939159A (en) 1974-05-29 1976-02-17 American Hoechst Corporation Spiro(pyrrolo (1,2-A)quinoxalines)
PT67194B (en) 1976-11-02 1979-03-23 Lilly Co Eli Process for preparing 4a-aryl-octahydro-1h-2-pyrindines
BG30927A3 (bg) 1977-12-27 1981-09-15 Eli Lilly And Company Метод за получаване на транс-4-алфа-фенил-октахидро-1н-2 пиридини
US4353901A (en) 1981-10-19 1982-10-12 Syntex (U.S.A.) Inc. 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones
GB8827479D0 (en) 1988-11-24 1988-12-29 Zambeletti Spa L Novel compounds
IL96507A0 (en) 1989-12-08 1991-08-16 Merck & Co Inc Nitrogen-containing spirocycles and pharmaceutical compositions containing them
US5206240A (en) 1989-12-08 1993-04-27 Merck & Co., Inc. Nitrogen-containing spirocycles
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
JPH04297458A (ja) 1991-03-27 1992-10-21 Toray Ind Inc イソキノリン誘導体およびその製造方法
GB9104656D0 (en) 1991-03-05 1991-04-17 Zambeletti Spa L Pharmaceuticals
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
DE4341403A1 (de) 1993-12-04 1995-06-08 Basf Ag N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung
US6017768A (en) 1994-05-06 2000-01-25 Pharmacopeia, Inc. Combinatorial dihydrobenzopyran library
CA2189634A1 (en) 1994-05-06 1995-11-16 John J. Baldwin Combinatorial dihydrobenzopyran library
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
IT1276462B1 (it) 1995-07-03 1997-10-31 Rotta Research Lab Diamidi aromatiche acide ad attivita' antigastrinica, procedimento per la loro preparazione e loro uso farmaceutico
JP4297458B2 (ja) 1999-04-16 2009-07-15 クラリオン株式会社 ナビゲーションシステム及び方法並びにナビゲーション用ソフトウェアを記録した記録媒体
US20040266802A1 (en) 1999-06-07 2004-12-30 Alain Calvet Tricyclic analgesics
US20020151712A1 (en) 1999-09-14 2002-10-17 Nan-Horng Lin 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission
AU2001289831A1 (en) 2000-09-06 2002-03-22 Bayer Aktiengesellschaft Medicaments against viral infections
US20040014744A1 (en) 2002-04-05 2004-01-22 Fortuna Haviv Substituted pyridines having antiangiogenic activity
WO2003095427A1 (en) 2002-05-10 2003-11-20 Taisho Pharmaceutical Co.,Ltd. Spiro-ring compound
CA2489255A1 (en) 2002-06-11 2003-12-18 Sankyo Company Limited Process for producing cyclic thioether and synthetic intermediate thereof
CN1729196A (zh) 2002-10-24 2006-02-01 三共株式会社 旋光亚砜的制备方法
CN1744899A (zh) 2002-12-13 2006-03-08 史密丝克莱恩比彻姆公司 作为ccr5拮抗剂的哌啶衍生物
WO2004076418A1 (en) 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
WO2004092179A1 (ja) 2003-04-14 2004-10-28 Nippon Soda Co. Ltd. スピロ誘導体、製造法および抗酸化薬
FR2856685B1 (fr) 2003-06-25 2005-09-23 Merck Sante Sas Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
CN101921279A (zh) 2003-10-01 2010-12-22 阿得罗公司 螺环杂环衍生物及其应用方法
JPWO2005037269A1 (ja) 2003-10-21 2006-12-28 住友製薬株式会社 新規ピペリジン誘導体
TWI350168B (en) 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
WO2005121090A1 (en) 2004-06-02 2005-12-22 Abbott Laboratories Substituted piperidines that have antiangiogenic activity
US7598261B2 (en) 2005-03-31 2009-10-06 Adolor Corporation Spirocyclic heterocyclic derivatives and methods of their use
JP2008540395A (ja) 2005-05-03 2008-11-20 ファイザー・インク アミドレソルシノール化合物
WO2007050124A1 (en) 2005-05-19 2007-05-03 Xenon Pharmaceuticals Inc. Fused piperidine derivatives and their uses as therapeutic agents
US7935712B2 (en) 2005-07-19 2011-05-03 Merck Sharp & Dohme Corp. Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors
EP1931652A2 (en) 2005-09-21 2008-06-18 Incyte Corporation Amido compounds and their use as pharmaceuticals
DK1961744T3 (da) 2005-11-18 2013-07-15 Ono Pharmaceutical Co Forbindelse indeholdende basiske grupper samt anvendelse deraf
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
US20080027072A1 (en) 2006-04-20 2008-01-31 Ampla Pharmaceuticals, Inc. Potentiation of MC4 receptor activity
EP2024370A1 (en) 2006-05-05 2009-02-18 Boehringer Ingelheim International GmbH Spiro- (tho) benzopyran-2, 4' -piperidine-and cyclohexane derivatives as inhibitors of specific cell cycle enzymes
JP5257068B2 (ja) 2006-05-16 2013-08-07 小野薬品工業株式会社 保護されていてもよい酸性基を含有する化合物およびその用途
AU2007254359A1 (en) 2006-05-18 2007-11-29 Merck Sharp & Dohme Corp. Aryl-fused spirocyclic compounds
JP5245827B2 (ja) 2006-07-31 2013-07-24 小野薬品工業株式会社 スピロ結合した環状基を含有する化合物およびその用途
US20100210633A1 (en) 2006-10-12 2010-08-19 Epix Delaware, Inc. Carboxamide compounds and their use
RS20090249A (sr) 2006-11-29 2010-06-30 Pfizer Products Inc. Spiroketon inhibitori acetil-coa karboksilaze
WO2008088692A2 (en) 2007-01-12 2008-07-24 Merck & Co., Inc. Spirochromanon derivatives
PE20081559A1 (es) 2007-01-12 2008-11-20 Merck & Co Inc DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA
EP2123652A1 (en) 2007-02-20 2009-11-25 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP2110377A1 (en) 2008-04-15 2009-10-21 DAC S.r.l. Spirocyclic derivatives as histone deacetylase inhibitors
JP5435592B2 (ja) 2008-05-28 2014-03-05 ファイザー・インク ピラゾロスピロケトンアセチルCoAカルボキシラーゼ阻害剤
US8524730B2 (en) 2008-07-04 2013-09-03 Msd K.K. Spirochromanone carboxylic acids
MX2011000664A (es) 2008-07-16 2011-02-24 Schering Corp Derivados biciclicos heterociclicos y uso de los mismos como moduladores de gpr119.
EP2318388A2 (en) 2008-07-23 2011-05-11 Schering Corporation Tricyclic spirocycle derivatives and methods of use thereof
CA2779261C (en) 2008-10-31 2015-03-24 Pain Therapeutics, Inc. Filamin a binding anti-inflammatory and analgesic
CA2779252C (en) 2008-10-31 2015-05-05 Pain Therapeutics, Inc. Filamin a-binding anti-inflammatory analgesic
US8580807B2 (en) 2009-04-03 2013-11-12 Merck Sharp & Dohme Corp. Bicyclic piperidine and piperazine derivatives as GPCR modulators for the treatment of obesity, diabetes and other metabolic disorders
WO2010151597A1 (en) 2009-06-26 2010-12-29 Schering Corporation Methods for using pyrrolo-benzo-1,4-diazines as sodium channel blockers
WO2011025690A1 (en) 2009-08-27 2011-03-03 Merck Sharp & Dohme Corp. Novel pyrrolidine derived beta 3 adrenergic receptor agonists
US8598164B2 (en) 2010-05-06 2013-12-03 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
SG192248A1 (en) 2011-02-02 2013-09-30 Vertex Pharma Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels
MX2013009393A (es) 2011-02-18 2013-08-29 Vertex Pharma Piperidinamidas cromano-espirociclicas como moduladores de canales de iones.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020013325A1 (en) * 1995-09-29 2002-01-31 Fisher Matthew J. Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation
US20060052597A1 (en) * 2002-10-22 2006-03-09 Best Desmond J Aryloxyalkylamine derivatives as h3 receptor ligands
WO2011092198A1 (en) * 2010-01-26 2011-08-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines

Also Published As

Publication number Publication date
US20120264749A1 (en) 2012-10-18
EP2686325B1 (en) 2016-12-14
AU2012229187A1 (en) 2013-09-19
WO2012125613A1 (en) 2012-09-20
US20150025073A1 (en) 2015-01-22
CN103517910A (zh) 2014-01-15
US9181273B2 (en) 2015-11-10
ES2618929T3 (es) 2017-06-22
US8828996B2 (en) 2014-09-09
EP2686325A1 (en) 2014-01-22
CN103517910B (zh) 2016-12-14
JP2014508169A (ja) 2014-04-03
NZ615014A (en) 2016-08-26
CA2829803A1 (en) 2012-09-20
MX347982B (es) 2017-05-22
MX2013010476A (es) 2013-10-30
JP6088443B2 (ja) 2017-03-01

Similar Documents

Publication Publication Date Title
AU2012229187B2 (en) Morpholine-spirocyclic piperidine amides as modulators of ion channels
AU2013209958B2 (en) Pyran-spirocyclic piperidine amides as modulators of ion channels
US9511067B2 (en) Substituted spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]s as modulators of ion channels
AU2012217616B2 (en) Chroman - spirocyclic piperidine amides as modulators of ion channels
AU2014287471C1 (en) Fused piperidine amides as modulators of ion channels
US20140171427A1 (en) Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
WO2014022639A1 (en) Solid forms of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3',4'-dihydro-2'h-spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]-1-yl)methanone
HK1223611B (en) Fused piperidine amides as modulators of ion channels
HK1192552A (en) Morpholine-spirocyclic piperidine amides as modulators of ion channels

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ HADIDA-RUAH, SARA SABINA; BINCH, HAYLEY MARIE; DENINNO, MICHAEL PAUL; FANNING, LEV TYLER DEWEY; FRIEMAN, BRYAN A.; GROOTENHUIS, PETER DIEDERIK JAN; HILGRAF, NICOLE; JOSHI, PRAMOD; KALLEL, EDWARD ADAM; PONTILLO, JOSEPH; SILINA, ALINA; SHETH, URVI JAGDISHBHAI; HURLEY, DENNIS JAMES; ARUMUGAM, VIJAYALAKSMI AND MILLER, MARK THOMAS

MK14 Patent ceased section 143(a) (annual fees not paid) or expired