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 PDFInfo
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- 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
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- alkyl
- pain
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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2686325B1 (OSRAM) |
| JP (1) | JP6088443B2 (OSRAM) |
| CN (1) | CN103517910B (OSRAM) |
| AU (1) | AU2012229187B2 (OSRAM) |
| CA (1) | CA2829803A1 (OSRAM) |
| ES (1) | ES2618929T3 (OSRAM) |
| MX (1) | MX347982B (OSRAM) |
| WO (1) | WO2012125613A1 (OSRAM) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011140425A1 (en) | 2010-05-06 | 2011-11-10 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
| RU2634900C2 (ru) | 2011-02-02 | 2017-11-08 | Вертекс Фармасьютикалз Инкорпорейтед | Спироциклические пирролопиразин(пиперидин)амиды в качестве модуляторов ионных каналов |
| JP5940562B2 (ja) | 2011-02-18 | 2016-06-29 | 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 | イオンチャネルのモジュレーターとしてのクロマン−スピロ環式ピペリジンアミド |
| US9403839B2 (en) | 2012-01-16 | 2016-08-02 | Vertex Pharmaceuticals Incorporated | Pyran-spirocyclic piperidine amides as modulators of ion channels |
| RS56015B1 (sr) | 2013-01-31 | 2017-09-29 | Vertex Pharma | Piridon amidi kao modulatori natrijumovih kanala |
| AR095192A1 (es) | 2013-01-31 | 2015-09-30 | Vertex Pharma | Quinolina y quinazolinamidas como modulares de canales de sodio |
| CN105683157B (zh) | 2013-07-19 | 2019-07-19 | 沃泰克斯药物股份有限公司 | 用作钠通道调节剂的磺酰胺类 |
| JP6483666B2 (ja) | 2013-10-14 | 2019-03-13 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 選択的に置換されたキノリン化合物 |
| WO2015057659A1 (en) | 2013-10-14 | 2015-04-23 | Eisai R&D Management Co., Ltd. | Selectively substituted quinoline compounds |
| SI3080134T1 (sl) | 2013-12-13 | 2018-11-30 | Vertex Pharmaceuticals Incorporated | Predzdravila piridon amidov uporabna kot modulatorji natrijevih kanalov |
| 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 |
| 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 |
| CN107849017B (zh) | 2015-07-31 | 2021-03-30 | 辉瑞公司 | 作为magl抑制剂的1,1,1-三氟-3-羟基丙-2-基氨基甲酸酯衍生物及1,1,1-三氟-4-羟基丁-2-基氨基甲酸酯衍生物 |
| AU2016343551A1 (en) * | 2015-10-23 | 2018-04-19 | Esteve Pharmaceuticals, S.A. | Oxa-diazaspiro compounds having activity against pain |
| EP3365345B1 (en) * | 2015-10-23 | 2020-02-26 | Esteve Pharmaceuticals, S.A. | Oxa-azaspiro compounds having activity against pain |
| 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 |
| HRP20221343T1 (hr) | 2015-11-16 | 2022-12-23 | Esteve Pharmaceuticals, S.A. | Oksadiazaspiro spojevi za liječenje zlouporabe droga i ovisnosti |
| EA036086B1 (ru) * | 2016-03-17 | 2020-09-24 | Фмк Корпорейшн | Способ превращения s-энантиомера в его рацемическую форму |
| AU2018208846A1 (en) | 2017-01-20 | 2019-07-25 | Pfizer Inc. | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors |
| WO2018134698A1 (en) | 2017-01-23 | 2018-07-26 | Pfizer Inc. | Heterocyclic spiro compounds as magl inhibitors |
| US11358977B2 (en) | 2017-05-16 | 2022-06-14 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
| JP7277431B2 (ja) | 2017-07-11 | 2023-05-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | ナトリウムチャネルのモジュレーターとしてのカルボキサミド |
| US11236110B2 (en) | 2017-10-17 | 2022-02-01 | Esteve Pharmaceuticals, S.A. | Salts of (R)-9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one |
| US11529337B2 (en) | 2018-02-12 | 2022-12-20 | 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 |
| KR102840599B1 (ko) | 2018-07-09 | 2025-07-29 | 리버 인스티튜트, 아이엔씨 | Nav1.8을 억제하기 위한 피리다진(PYRIDAZINE) 화합물 |
| US12440481B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| US12441703B2 (en) | 2019-01-10 | 2025-10-14 | 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 |
| MX2022006865A (es) | 2019-12-06 | 2022-07-11 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio. |
| WO2021130723A1 (en) * | 2019-12-24 | 2021-07-01 | Cadila Healthcare Limited | Novel compounds suitable for the treatment of dyslipidemia |
| 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 |
| BR112023025264A2 (pt) | 2021-06-04 | 2024-02-20 | Vertex Pharma | Formas farmacêuticas sólidas e regimes posológicos compreendendo (2r,3s,4s,5r)-4-[[3- (3,4-difluoro-2-metóxi-fenil)-4,5-dimetil-5-(trifluorometil) tetra-hidrofuran-2-carbonil]amino ]piridina-2-carboxamida |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| JP2024520648A (ja) | 2021-06-04 | 2024-05-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | ナトリウムチャネルの調節因子としての置換テトラヒドロフラン-2-カルボキサミド |
| DK4347031T3 (da) | 2021-06-04 | 2025-12-01 | Vertex Pharma | N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler |
| WO2022256676A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs 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 |
| KR20240102969A (ko) * | 2021-10-13 | 2024-07-03 | 밴쿠아 바이오, 인크. | 글루코세레브로시다제 활성의 소분자 조절제 및 이의 용도 |
| EP4511117A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| JP2025513454A (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 |
| CA3256604A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | HETEROARYL COMPOUNDS FOR PAIN RELIEF |
| GEAP202516632A (en) | 2022-04-22 | 2025-02-25 | Vertex Pharma | Heteroaryl compounds for the treatment of pain |
| 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 |
| 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 |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090465A1 (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 |
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| US20150025073A1 (en) | 2015-01-22 |
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| EP2686325A1 (en) | 2014-01-22 |
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| AU2012229187B2 (en) | 2016-11-10 |
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