JP6088443B2 - イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド - Google Patents

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

Info

Publication number
JP6088443B2
JP6088443B2 JP2013558104A JP2013558104A JP6088443B2 JP 6088443 B2 JP6088443 B2 JP 6088443B2 JP 2013558104 A JP2013558104 A JP 2013558104A JP 2013558104 A JP2013558104 A JP 2013558104A JP 6088443 B2 JP6088443 B2 JP 6088443B2
Authority
JP
Japan
Prior art keywords
alkyl
pain
och
substituted
compound
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.)
Expired - Fee Related
Application number
JP2013558104A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014508169A5 (enExample
JP2014508169A (ja
Inventor
サラ サビーナ ハディダ−ルア,
サラ サビーナ ハディダ−ルア,
ヘイリー マリー ビンチ,
ヘイリー マリー ビンチ,
マイケル ポール デニノ,
マイケル ポール デニノ,
レブ タイラー デュイー ファニング,
レブ タイラー デュイー ファニング,
ブライアン エー. フリーマン,
ブライアン エー. フリーマン,
ピーター ディーデリック ジャン グルーテンフイ,
ピーター ディーデリック ジャン グルーテンフイ,
ニコール ヒルグラフ,
ニコール ヒルグラフ,
プラモド ジョシ,
プラモド ジョシ,
エドワード アダム カレル,
エドワード アダム カレル,
ジョセフ ポンティーロ,
ジョセフ ポンティーロ,
アリーナ セリーナ,
アリーナ セリーナ,
アービー ジャグディシュバイ セス,
アービー ジャグディシュバイ セス,
デニス ジェイムズ ハーリー,
デニス ジェイムズ ハーリー,
ヴィジャヤラクスミ アルムガム,
ヴィジャヤラクスミ アルムガム,
マーク トーマス ミラー,
マーク トーマス ミラー,
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 JP2014508169A publication Critical patent/JP2014508169A/ja
Publication of JP2014508169A5 publication Critical patent/JP2014508169A5/ja
Application granted granted Critical
Publication of JP6088443B2 publication Critical patent/JP6088443B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed systems
    • 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
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives

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)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2013558104A 2011-03-14 2012-03-13 イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド Expired - Fee Related JP6088443B2 (ja)

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 (3)

Publication Number Publication Date
JP2014508169A JP2014508169A (ja) 2014-04-03
JP2014508169A5 JP2014508169A5 (enExample) 2015-04-30
JP6088443B2 true JP6088443B2 (ja) 2017-03-01

Family

ID=45888492

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013558104A Expired - Fee Related JP6088443B2 (ja) 2011-03-14 2012-03-13 イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド

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 (55)

* 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
KR101923367B1 (ko) 2011-02-02 2018-12-04 버텍스 파마슈티칼스 인코포레이티드 이온 채널의 조절제로서의 피롤로피라진―스피로사이클릭 피페리딘 아미드
WO2012112743A1 (en) 2011-02-18 2012-08-23 Vertex Pharmaceuticals Incorporated Chroman - spirocyclic piperidine amides as modulators of ion channels
WO2013109521A1 (en) * 2012-01-16 2013-07-25 Vertex Pharmaceuticals Incorporated Pyran-spirocyclic piperidine amides as modulators of ion channels
KR102226587B1 (ko) 2013-01-31 2021-03-11 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 조절제로서의 퀴놀린 및 퀴나졸린 아미드
CN105026373B (zh) 2013-01-31 2018-03-30 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
JP6337109B2 (ja) 2013-07-19 2018-06-06 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Vertex Pharmaceuticals Incorporated ナトリウムチャネルの調節剤としてのスルホンアミド
ES2670550T3 (es) 2013-10-14 2018-05-30 Eisai R&D Management Co., Ltd. Derivados de quinolina selectivamente sustituidos
KR101823488B1 (ko) 2013-10-14 2018-01-30 에자이 알앤드디 매니지먼트 가부시키가이샤 선택적으로 치환된 퀴놀린 화합물
SG11201604477SA (en) 2013-12-13 2016-07-28 Vertex Pharma Prodrugs of pyridone amides useful as modulators of sodium channels
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
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
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
MX375424B (es) 2015-07-31 2025-03-06 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
RS59956B1 (sr) * 2015-10-23 2020-03-31 Esteve Pharmaceuticals Sa Oksa-diazaspiro jedinjenja koja imaju aktivnost protiv bola
AR106444A1 (es) * 2015-10-23 2018-01-17 Esteve Labor Dr Compuestos oxaazaespíricos con actividad contra el dolor
JP6844822B2 (ja) * 2015-10-23 2021-03-17 エステベ ファーマシューティカルズ, ソシエダッド アノニマEsteve Pharmaceuticals, S.A. 疼痛に対して活性を有する置換モルホリン誘導体
TN2018000122A1 (en) 2015-11-16 2019-10-04 Esteve Labor Dr Oxadiazaspiro compounds for the treatment of drug abuse and addiction
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).
JP2020506903A (ja) 2017-01-23 2020-03-05 ファイザー・インク Magl阻害薬としての複素環式スピロ化合物
KR102714561B1 (ko) 2017-05-16 2024-10-10 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 조절제로서의 중수소화 피리돈 아미드 및 이의 프로드럭
AU2018300150A1 (en) 2017-07-11 2020-01-30 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
FI3697795T3 (fi) 2017-10-17 2024-02-23 Acondicionamiento Tarrasense (R)-9-(2,5-difluorifenetyyli)-4-etyyli-2-metyyli-1-oksa-4,9-diatsaspiro[5.5]undekan-3-onin suoloja
US20190343817A1 (en) 2018-02-12 2019-11-14 Vertex Pharmaceuticals Incorporated Method of treating pain
SG11202100130QA (en) 2018-07-09 2021-02-25 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
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
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
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
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
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
SMT202600064T1 (it) 2021-06-04 2026-03-09 Vertex Pharma Forme farmaceutiche solide e regimi di dosaggio comprendenti (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-metossi-fenil)-4,5-dimetil-5-(trifluorometil) tetraidrofuran-2-carbonil]ammino]piridin-2-carbossammide
CA3221939A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
CN117794918A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 经取代的四氢呋喃类似物作为钠通道调节剂
US20240368135A1 (en) 2021-06-04 2024-11-07 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
WO2022256842A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
CA3235270A1 (en) * 2021-10-13 2023-04-20 Vanqua Bio, Inc. Small molecule modulators of glucocerebrosidase activity and uses thereof
AU2023257313A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
IL316422A (en) 2022-04-22 2024-12-01 Vertex Pharma Heteroaryl compounds for pain treatment
AU2023255558A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
JP2025513455A (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
KR20250120351A (ko) 2022-12-06 2025-08-08 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법
KR20260116141A (ko) 2023-10-23 2026-07-28 버텍스 파마슈티칼스 인코포레이티드 통증 치료용 화합물 및 이의 고체 형태의 제조방법
KR20260118418A (ko) 2023-10-23 2026-07-30 버텍스 파마슈티칼스 인코포레이티드 통증 치료를 위한 헤테로아릴 화합물
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
KR20260116140A (ko) 2023-10-23 2026-07-28 버텍스 파마슈티칼스 인코포레이티드 통증 치료를 위한 헤테로아릴 화합물
AU2024393245A1 (en) 2023-12-07 2026-06-18 Vertex Pharmaceuticals Incorporated Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic pain
TW202606663A (zh) 2024-06-28 2026-02-16 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
LU605402B1 (en) 2024-07-11 2026-07-14 Sea4Us Biotecnologia E Recursos Marinhos Sa Oxazolidone-derived compounds and their use in the treatment of chronic and acute pain
WO2026030525A1 (en) 2024-07-31 2026-02-05 Vertex Pharmaceuticals Incorporated Zilvetrigine dosage forms and dosing regimens for treating pain

Family Cites Families (65)

* 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
PT68934A (en) 1977-12-27 1979-01-01 Lilly Co Eli Process for preparing 4a-aryl-octahydro-1h-2-pyrindines
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
US5206240A (en) 1989-12-08 1993-04-27 Merck & Co., Inc. Nitrogen-containing spirocycles
IL96507A0 (en) 1989-12-08 1991-08-16 Merck & Co Inc Nitrogen-containing spirocycles and pharmaceutical compositions containing them
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
JPH10500112A (ja) 1994-05-06 1998-01-06 ファーマコピーア,インコーポレイテッド 組合せ ジヒドロベンゾピラン ライブラリー
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
WO1997011940A1 (en) * 1995-09-29 1997-04-03 Eli Lilly And Company Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation
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
WO2002020509A2 (de) 2000-09-06 2002-03-14 Bayer Aktiengesellschaft Arzneimittel gegen virale erkrankungen
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
BR0311749A (pt) 2002-06-11 2005-03-08 Sankyo Co Processo para produzir um composto, e, composto
JP2006512404A (ja) * 2002-10-22 2006-04-13 グラクソ グループ リミテッド H3受容体リガンドとしてのアリールオキシアルキルアミン誘導体
EP1557420A4 (en) 2002-10-24 2007-06-27 Sankyo Co PROCESS FOR PRODUCING OPTICALLY ACTIVE SULFOXIDE
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
CA2512886A1 (en) 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
JPWO2004092179A1 (ja) 2003-04-14 2006-07-06 日本曹達株式会社 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
KR20140015122A (ko) 2003-10-01 2014-02-06 아돌로 코포레이션 스피로시클릭 헤테로시클릭 유도체 및 이의 사용 방법
WO2005037269A1 (ja) 2003-10-21 2005-04-28 Dainippon Sumitomo Pharma Co., Ltd. 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
ATE509023T1 (de) 2005-07-19 2011-05-15 Merck Sharp & Dohme Spirochromanon-derivate als acetyl-koenzym-a- carboxylase-hemmer
CA2621255A1 (en) 2005-09-21 2007-04-05 Incyte Corporation Amido compounds and their use as pharmaceuticals
PT1961744E (pt) 2005-11-18 2013-05-15 Ono Pharmaceutical Co Composto que contém um grupo básico e sua utilização
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
JP2009536175A (ja) 2006-05-05 2009-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 特定の細胞サイクル酵素の阻害剤としてのスピロ−(tho)ベンゾピラン−2,4’−ピペリジン−及びシクロヘキサン誘導体
US8618122B2 (en) 2006-05-16 2013-12-31 Ono Pharmaceutical Co., Ltd. Compound having acidic group which may be protected, and use thereof
CA2651681A1 (en) 2006-05-18 2007-11-29 Merck & Co., Inc. Aryl-fused spirocyclic compounds
WO2008016006A1 (fr) 2006-07-31 2008-02-07 Ono Pharmaceutical Co., Ltd. Composé auquel un groupe cyclique est lié par une liaison spiro et son utilisation
US20100210633A1 (en) 2006-10-12 2010-08-19 Epix Delaware, Inc. Carboxamide compounds and their use
WO2008065508A1 (en) 2006-11-29 2008-06-05 Pfizer Products Inc. Spiroketone acetyl-coa carboxylase inhibitors
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
EP2307422B1 (en) 2008-07-04 2014-03-26 Msd K.K. Novel 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
EP2488177B1 (en) 2008-10-31 2016-10-12 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
EP2414348B1 (en) 2009-04-03 2013-11-20 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
US8354403B2 (en) 2009-08-27 2013-01-15 Merck Sharp & Dohme Corp. Pyrrolidine derived beta 3 adrenergic receptor agonists
US8633183B2 (en) * 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US8598164B2 (en) 2010-05-06 2013-12-03 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
KR101923367B1 (ko) 2011-02-02 2018-12-04 버텍스 파마슈티칼스 인코포레이티드 이온 채널의 조절제로서의 피롤로피라진―스피로사이클릭 피페리딘 아미드
WO2012112743A1 (en) 2011-02-18 2012-08-23 Vertex Pharmaceuticals Incorporated Chroman - spirocyclic piperidine amides as modulators of ion channels

Also Published As

Publication number Publication date
US8828996B2 (en) 2014-09-09
CN103517910A (zh) 2014-01-15
US20120264749A1 (en) 2012-10-18
CN103517910B (zh) 2016-12-14
CA2829803A1 (en) 2012-09-20
US20150025073A1 (en) 2015-01-22
US9181273B2 (en) 2015-11-10
WO2012125613A1 (en) 2012-09-20
ES2618929T3 (es) 2017-06-22
EP2686325B1 (en) 2016-12-14
EP2686325A1 (en) 2014-01-22
NZ615014A (en) 2016-08-26
MX2013010476A (es) 2013-10-30
MX347982B (es) 2017-05-22
AU2012229187A1 (en) 2013-09-19
AU2012229187B2 (en) 2016-11-10
JP2014508169A (ja) 2014-04-03

Similar Documents

Publication Publication Date Title
CN103517910B (zh) 作为离子通道调节剂的吗啉-螺环哌啶酰胺
US9403839B2 (en) Pyran-spirocyclic piperidine amides as modulators of ion channels
CN105473554B (zh) 作为离子通道调节剂的稠合的哌啶酰胺类
US10385070B2 (en) Chroman-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
HK1192552A (en) Morpholine-spirocyclic piperidine amides as modulators of ion channels
HK1192552B (en) Morpholine-spirocyclic piperidine amides as modulators of ion channels
HK1191952A (en) Chroman-spirocyclic piperidine amides as modulators of ion channels
HK1223611B (en) Fused piperidine amides as modulators of ion channels
HK1203074B (en) Pyran-spirocyclic piperidine amides as modulators of ion channels
HK1191642A (en) Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150312

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150312

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20151119

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20151209

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160308

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160815

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161114

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170110

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170203

R150 Certificate of patent or registration of utility model

Ref document number: 6088443

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees