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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Neurology (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 (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2847858A1 (en) * | 2011-09-14 | 2013-03-21 | Dow Agrosciences Llc | Methods and systems for forming boronic acids and intermediates thereof |
| US9163042B2 (en) | 2013-12-13 | 2015-10-20 | Vertex Pharmaceuticals Incorporated | Prodrugs of pyridone amides useful as modulators of sodium channels |
| KR102192572B1 (ko) | 2014-06-09 | 2020-12-18 | 삼성전자주식회사 | 광원 모듈의 불량 검사방법, 광원 모듈의 제조 방법 및 광원 모듈 검사장치 |
| JP6779217B2 (ja) * | 2014-10-24 | 2020-11-04 | アヴェクタス リミテッド | 細胞原形質膜を越える送達方法 |
| MX2017010682A (es) | 2015-02-19 | 2018-04-24 | Purdue Pharma Lp | Metodos y composiciones para disminuir el vaciado gastrico. |
| 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 |
| CA3029132A1 (en) * | 2016-07-06 | 2018-01-11 | Crispr Therapeutics Ag | Materials and methods for treatment of pain related disorders |
| 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 |
| AU2018271110A1 (en) | 2017-05-16 | 2019-12-05 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
| CN111065383A (zh) | 2017-07-11 | 2020-04-24 | 沃泰克斯药物股份有限公司 | 用作钠通道调节剂的羧酰胺 |
| US11529337B2 (en) | 2018-02-12 | 2022-12-20 | Vertex Pharmaceuticals Incorporated | Method of treating pain |
| CN113272293B (zh) | 2018-11-02 | 2024-06-14 | 默沙东有限责任公司 | 作为nav1.8抑制剂的2-胺基-n-杂芳基-烟酰胺 |
| US12440481B2 (en) | 2019-01-10 | 2025-10-14 | 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 |
| LT4069691T (lt) | 2019-12-06 | 2024-12-10 | Vertex Pharmaceuticals Incorporated | Pakeistieji tetrahidrofuranai kaip natrio kanalų moduliatoriai |
| DK4347031T3 (da) | 2021-06-04 | 2025-12-01 | Vertex Pharma | N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler |
| CA3221938A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| EP4346818B1 (en) | 2021-06-04 | 2025-12-03 | Vertex Pharmaceuticals Incorporated | Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide |
| CN117794919A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | N-(羟烷基(杂)芳基)四氢呋喃甲酰胺类似物作为钠通道调节剂 |
| CN117858875A (zh) | 2021-06-04 | 2024-04-09 | 沃泰克斯药物股份有限公司 | 羟基和(卤代)烷氧基取代的四氢呋喃作为钠通道调节剂 |
| EP4347032A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| CR20240513A (es) | 2022-04-22 | 2025-04-30 | Vertex Pharma | Compuestos de heteroarilo para el tratamiento del dolor |
| WO2023205778A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2023205468A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| CN119487003A (zh) | 2022-04-22 | 2025-02-18 | 沃泰克斯药物股份有限公司 | 用于治疗疼痛的杂芳基化合物 |
| JP2025516005A (ja) | 2022-04-25 | 2025-05-23 | サイトワン セラピューティクス インコーポレイテッド | 疼痛の処置のためのnav1.8の二環式複素環アミド阻害剤 |
| 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 |
| 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 |
| 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 |
| TW202523313A (zh) | 2023-10-23 | 2025-06-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| 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 |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating 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 |
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 |
| 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 |
| 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 |
| US7112366B2 (en) | 2001-01-05 | 2006-09-26 | The Ohio State University | Chemical monolayer and micro-electronic junctions and devices containing same |
| US7456164B2 (en) * | 2004-05-07 | 2008-11-25 | Pfizer, Inc | 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands |
| PT1747210E (pt) * | 2004-05-07 | 2010-08-31 | Warner Lambert Co | Derivados de fenol e de tiofenol 3- ou 4-monossubstituídos úteis enquanto ligandos de h3 |
| AP2780A (en) | 2006-10-18 | 2013-09-30 | Pfizer Prod Inc | Biaryl ether urea compounds |
| 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 |
| EP2155727A1 (en) * | 2007-05-03 | 2010-02-24 | Pfizer Limited | N-[6-amino-5-(phenyl)pyrazin-2-yl]-isoxazole-4-carboxamide derivatives and related compounds as nav1.8 channel modulators for the treatment of pain |
| CA2684105C (en) | 2007-05-03 | 2011-09-06 | Pfizer Limited | Pyridine derivatives |
| CA2693588C (en) | 2007-07-13 | 2015-11-17 | Icagen, Inc. | Sodium channel inhibitors |
-
2012
- 2012-10-15 MX MX2014004738A patent/MX337469B/es active IP Right Grant
- 2012-10-15 UA UAA201404440A patent/UA109220C2/uk unknown
- 2012-10-15 PH PH1/2014/500919A patent/PH12014500919A1/en unknown
- 2012-10-15 JP JP2014537760A patent/JP5946538B2/ja not_active Expired - Fee Related
- 2012-10-15 CA CA2850925A patent/CA2850925C/en not_active Expired - Fee Related
- 2012-10-15 AU AU2012328034A patent/AU2012328034B2/en not_active Ceased
- 2012-10-15 EP EP12794777.8A patent/EP2771335A2/en not_active Withdrawn
- 2012-10-15 BR BR112014009102A patent/BR112014009102A2/pt active Search and Examination
- 2012-10-15 AP AP2014007579A patent/AP2014007579A0/xx unknown
- 2012-10-15 MD MDA20140037A patent/MD20140037A2/ro not_active Application Discontinuation
- 2012-10-15 SG SG11201401032YA patent/SG11201401032YA/en unknown
- 2012-10-15 EA EA201490864A patent/EA023375B1/ru not_active IP Right Cessation
- 2012-10-15 US US14/351,893 patent/US9079878B2/en not_active Expired - Fee Related
- 2012-10-15 CN CN201280052591.6A patent/CN103906746B/zh not_active Expired - Fee Related
- 2012-10-15 KR KR1020147010826A patent/KR101586966B1/ko not_active Expired - Fee Related
- 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
-
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 GT GT201400079A patent/GT201400079A/es unknown
- 2014-04-25 EC ECSP14013324 patent/ECSP14013324A/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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