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
-
- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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
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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
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- 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
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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)
- 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)
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 (52)
| 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 |
Family Cites Families (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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| 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 |
| AU2012229187B2 (en) | 2016-11-10 |
| 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 |
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