CN103906746B - 用作钠通道调节剂的(4-苯基咪唑-2-基)乙胺衍生物 - Google Patents
用作钠通道调节剂的(4-苯基咪唑-2-基)乙胺衍生物 Download PDFInfo
- Publication number
- CN103906746B CN103906746B CN201280052591.6A CN201280052591A CN103906746B CN 103906746 B CN103906746 B CN 103906746B CN 201280052591 A CN201280052591 A CN 201280052591A CN 103906746 B CN103906746 B CN 103906746B
- Authority
- CN
- China
- Prior art keywords
- phenyl
- compound
- formula
- tautomer
- amine
- 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
Links
- ZOLJCKFHSARQLR-UHFFFAOYSA-N COc(cc1)ccc1-c1c[nH]c(CC2(COCC2)N)n1 Chemical compound COc(cc1)ccc1-c1c[nH]c(CC2(COCC2)N)n1 ZOLJCKFHSARQLR-UHFFFAOYSA-N 0.000 description 1
- ARCAJTAMUQLDKI-UHFFFAOYSA-N NC1(Cc2nc(-c(cc3)ccc3OC(F)(F)F)c[nH]2)COCCC1 Chemical compound NC1(Cc2nc(-c(cc3)ccc3OC(F)(F)F)c[nH]2)COCCC1 ARCAJTAMUQLDKI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161551628P | 2011-10-26 | 2011-10-26 | |
| US61/551,628 | 2011-10-26 | ||
| PCT/IB2012/055610 WO2013061205A2 (en) | 2011-10-26 | 2012-10-15 | Chemical compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103906746A CN103906746A (zh) | 2014-07-02 |
| CN103906746B true CN103906746B (zh) | 2015-12-09 |
Family
ID=47278356
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280052591.6A Expired - Fee Related CN103906746B (zh) | 2011-10-26 | 2012-10-15 | 用作钠通道调节剂的(4-苯基咪唑-2-基)乙胺衍生物 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9079878B2 (enExample) |
| EP (1) | EP2771335A2 (enExample) |
| JP (1) | JP5946538B2 (enExample) |
| KR (1) | KR101586966B1 (enExample) |
| CN (1) | CN103906746B (enExample) |
| AP (1) | AP2014007579A0 (enExample) |
| AU (1) | AU2012328034B2 (enExample) |
| BR (1) | BR112014009102A2 (enExample) |
| CA (1) | CA2850925C (enExample) |
| CL (1) | CL2014000956A1 (enExample) |
| CO (1) | CO6940427A2 (enExample) |
| CR (1) | CR20140185A (enExample) |
| CU (1) | CU20140046A7 (enExample) |
| DO (1) | DOP2014000085A (enExample) |
| EA (1) | EA023375B1 (enExample) |
| EC (1) | ECSP14013324A (enExample) |
| GT (1) | GT201400079A (enExample) |
| IL (1) | IL232267A (enExample) |
| MD (1) | MD20140037A2 (enExample) |
| MX (1) | MX337469B (enExample) |
| NI (1) | NI201400031A (enExample) |
| PE (1) | PE20141682A1 (enExample) |
| PH (1) | PH12014500919A1 (enExample) |
| SG (1) | SG11201401032YA (enExample) |
| TN (1) | TN2014000147A1 (enExample) |
| UA (1) | UA109220C2 (enExample) |
| WO (1) | WO2013061205A2 (enExample) |
| ZA (1) | ZA201402281B (enExample) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2014003064A (es) * | 2011-09-14 | 2014-05-07 | Dow Agrosciences Llc | Metodos y sistemas para formar acidos boronicos y sus intermedios. |
| JP6463580B2 (ja) | 2013-12-13 | 2019-02-06 | 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有用なピリドンアミドのプロドラッグ |
| KR102192572B1 (ko) | 2014-06-09 | 2020-12-18 | 삼성전자주식회사 | 광원 모듈의 불량 검사방법, 광원 모듈의 제조 방법 및 광원 모듈 검사장치 |
| US10612042B2 (en) | 2014-10-24 | 2020-04-07 | Avectas Limited | Delivery across cell plasma membranes |
| AU2016219879A1 (en) | 2015-02-19 | 2017-08-24 | Purdue Pharma L.P. | Methods and compositions for decreasing gastric emptying |
| IS2977B (is) | 2015-02-23 | 2017-07-15 | Actavis Group Ptc Ehf. | Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni |
| EP3397760A2 (en) | 2015-12-30 | 2018-11-07 | Avectas Limited | Vector-free delivery of gene editing proteins and compositions to cells and tissues |
| CN109843914B (zh) | 2016-07-06 | 2024-03-15 | 沃泰克斯药物股份有限公司 | 用于治疗疼痛相关病症的材料和方法 |
| US11801313B2 (en) * | 2016-07-06 | 2023-10-31 | Vertex Pharmaceuticals Incorporated | Materials and methods for treatment of pain related disorders |
| BR112019024016A2 (pt) | 2017-05-16 | 2020-06-09 | Vertex Pharma | amidas de piridona deuteradas e profármacos das mesmas como moduladores de canais de sódio |
| CA3069720A1 (en) | 2017-07-11 | 2019-01-17 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| EP3752152A1 (en) | 2018-02-12 | 2020-12-23 | Vertex Pharmaceuticals Incorporated | A method of treating pain |
| EP3873893A1 (en) | 2018-11-02 | 2021-09-08 | Merck Sharp & Dohme Corp. | 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors |
| US12441703B2 (en) | 2019-01-10 | 2025-10-14 | 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 |
| DK4069691T3 (da) | 2019-12-06 | 2024-10-28 | Vertex Pharma | Substituerede tetrahydrofuraner som modulatorer af natriumkanaler |
| MA64853B1 (fr) | 2021-06-04 | 2025-11-28 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hétéro)aryl) tétrahydrofuran carboxamides utilisés en tant que modulateurs de canaux sodiques |
| 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 |
| CA3221939A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| EP4347033A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans 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 |
| 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 |
| 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 |
| EP4511115A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| JP2025513452A (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 |
| AU2023255771A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| CR20240512A (es) | 2022-04-25 | 2025-03-03 | Siteone Therapeutics Inc | Inhibidores de amida heterocíclica bicíclica de sodio activado por voltaje 1.8 (nav1.8) para el tratamiento del dolor |
| CN115656380B (zh) * | 2022-11-09 | 2025-04-01 | 武汉海特生物创新医药研究有限公司 | 一种mtv对映异构体的hplc-uv检测方法 |
| EP4630405A1 (en) | 2022-12-06 | 2025-10-15 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
| 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 |
| WO2025090465A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| WO2025122953A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic pain |
| WO2025160286A1 (en) | 2024-01-24 | 2025-07-31 | Siteone Therapeutics, Inc. | 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain |
| WO2025231324A1 (en) * | 2024-05-02 | 2025-11-06 | Genep Inc. | Imidazole compounds and their use as sodium channel inhibitors |
| US20260001877A1 (en) | 2024-06-28 | 2026-01-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2026013449A2 (en) | 2024-07-11 | 2026-01-15 | 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002083656A2 (fr) * | 2001-04-10 | 2002-10-24 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derives d'heterocycles a 5 chainons et leur utilisation en tant qu'inhibiteurs de la mao et/ou peroxydation lipidique, leur preparation et leur application comme medicaments |
| US20050234118A1 (en) * | 2002-07-25 | 2005-10-20 | Dennis Bigg | Novel aryllimidazole derivatives, preparation and therapeutic used thereof |
| CN101103112A (zh) * | 2004-10-27 | 2008-01-09 | 先灵公司 | 抑制Nav1.8的短干扰核酸组合物和方法 |
| US20110046129A1 (en) * | 2005-12-22 | 2011-02-24 | Newron Pharmaceuticals S.P.A. | 2-Phenylethylamino Derivatives as Calcium and/or Sodium Channel Modulators |
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| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035298A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Chewing gum containing medicament active agents |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| TWI292316B (en) * | 1999-10-11 | 2008-01-11 | Sod Conseils Rech Applic | Pharmaceutical composition of thiazole derivatives intended to inhibit mao and/or lipidic peroxidation and/or to act as modulators of sodium channels and the use thereof |
| US7291641B2 (en) * | 1999-10-11 | 2007-11-06 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
| US7112366B2 (en) | 2001-01-05 | 2006-09-26 | The Ohio State University | Chemical monolayer and micro-electronic junctions and devices containing same |
| RS51403B (sr) * | 2004-05-07 | 2011-02-28 | Warner-Lambert Company Llc | Derivati 3-ili 4-monosupstituisanih fenola i tiofenola, koji su korisni kao h3 ligandi |
| US7456164B2 (en) * | 2004-05-07 | 2008-11-25 | Pfizer, Inc | 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands |
| SI2076508T1 (sl) | 2006-10-18 | 2011-04-29 | Pfizer Prod Inc | Spojine biaril eter sečnine |
| JP5361857B2 (ja) | 2007-03-23 | 2013-12-04 | ファイザー・リミテッド | イオンチャネルの阻害剤 |
| JP2010526051A (ja) * | 2007-05-03 | 2010-07-29 | ファイザー・リミテッド | 疼痛を治療するためのｎａｖ１．８チャネルモジュレーターとしてのｎ−［６−アミノ−５−（フェニル）ピラジン−２−イル］−イソオキサゾール−４−カルボキサミド誘導体および関連化合物 |
| WO2008135826A2 (en) | 2007-05-03 | 2008-11-13 | Pfizer Limited | 2 -pyridine carboxamide derivatives as sodium channel modulators |
| WO2009012242A2 (en) | 2007-07-13 | 2009-01-22 | Icagen, Inc. | Sodium channel inhibitors |
-
2012
- 2012-10-15 UA UAA201404440A patent/UA109220C2/uk unknown
- 2012-10-15 PE PE2014000605A patent/PE20141682A1/es not_active Application Discontinuation
- 2012-10-15 WO PCT/IB2012/055610 patent/WO2013061205A2/en not_active Ceased
- 2012-10-15 US US14/351,893 patent/US9079878B2/en not_active Expired - Fee Related
- 2012-10-15 KR KR1020147010826A patent/KR101586966B1/ko not_active Expired - Fee Related
- 2012-10-15 PH PH1/2014/500919A patent/PH12014500919A1/en unknown
- 2012-10-15 CN CN201280052591.6A patent/CN103906746B/zh not_active Expired - Fee Related
- 2012-10-15 JP JP2014537760A patent/JP5946538B2/ja not_active Expired - Fee Related
- 2012-10-15 BR BR112014009102A patent/BR112014009102A2/pt active Search and Examination
- 2012-10-15 SG SG11201401032YA patent/SG11201401032YA/en unknown
- 2012-10-15 CA CA2850925A patent/CA2850925C/en not_active Expired - Fee Related
- 2012-10-15 MX MX2014004738A patent/MX337469B/es active IP Right Grant
- 2012-10-15 MD MDA20140037A patent/MD20140037A2/ro not_active Application Discontinuation
- 2012-10-15 AP AP2014007579A patent/AP2014007579A0/xx unknown
- 2012-10-15 AU AU2012328034A patent/AU2012328034B2/en not_active Ceased
- 2012-10-15 EA EA201490864A patent/EA023375B1/ru not_active IP Right Cessation
- 2012-10-15 EP EP12794777.8A patent/EP2771335A2/en not_active Withdrawn
-
2014
- 2014-03-27 ZA ZA2014/02281A patent/ZA201402281B/en unknown
- 2014-04-08 TN TNP2014000147A patent/TN2014000147A1/fr unknown
- 2014-04-14 CL CL2014000956A patent/CL2014000956A1/es unknown
- 2014-04-23 NI NI201400031A patent/NI201400031A/es unknown
- 2014-04-24 CU CU2014000046A patent/CU20140046A7/es unknown
- 2014-04-24 CR CR20140185A patent/CR20140185A/es unknown
- 2014-04-25 DO DO2014000085A patent/DOP2014000085A/es unknown
- 2014-04-25 EC ECSP14013324 patent/ECSP14013324A/es unknown
- 2014-04-25 GT GT201400079A patent/GT201400079A/es unknown
- 2014-04-27 IL IL232267A patent/IL232267A/en not_active IP Right Cessation
- 2014-04-28 CO CO14090473A patent/CO6940427A2/es active IP Right Grant
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002083656A2 (fr) * | 2001-04-10 | 2002-10-24 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derives d'heterocycles a 5 chainons et leur utilisation en tant qu'inhibiteurs de la mao et/ou peroxydation lipidique, leur preparation et leur application comme medicaments |
| US20050234118A1 (en) * | 2002-07-25 | 2005-10-20 | Dennis Bigg | Novel aryllimidazole derivatives, preparation and therapeutic used thereof |
| CN101103112A (zh) * | 2004-10-27 | 2008-01-09 | 先灵公司 | 抑制Nav1.8的短干扰核酸组合物和方法 |
| US20110046129A1 (en) * | 2005-12-22 | 2011-02-24 | Newron Pharmaceuticals S.P.A. | 2-Phenylethylamino Derivatives as Calcium and/or Sodium Channel Modulators |
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