JP5946538B2 - ナトリウムチャネルモジュレーターとして有用な（４−フェニルイミダゾール−２−イル）エチルアミン誘導体 - Google Patents
ナトリウムチャネルモジュレーターとして有用な（４−フェニルイミダゾール−２−イル）エチルアミン誘導体 Download PDFInfo
- Publication number
- JP5946538B2 JP5946538B2 JP2014537760A JP2014537760A JP5946538B2 JP 5946538 B2 JP5946538 B2 JP 5946538B2 JP 2014537760 A JP2014537760 A JP 2014537760A JP 2014537760 A JP2014537760 A JP 2014537760A JP 5946538 B2 JP5946538 B2 JP 5946538B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- phenyl
- formula
- tautomer
- imidazol
- 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
- 0 Cc1ccc(*)c(*)c1 Chemical compound Cc1ccc(*)c(*)c1 0.000 description 3
- ONVPCYBBFGHZSZ-UHFFFAOYSA-N CCC(C1(COC1)N)c1nc(-c(cc2)ccc2OC(F)(F)F)c[nH]1 Chemical compound CCC(C1(COC1)N)c1nc(-c(cc2)ccc2OC(F)(F)F)c[nH]1 ONVPCYBBFGHZSZ-UHFFFAOYSA-N 0.000 description 1
- WEAFAWYVJKPGDN-SECBINFHSA-N C[C@@H](C1(COC1)N)c1nc(-c2ccc(C(F)(F)F)cc2)c[nH]1 Chemical compound C[C@@H](C1(COC1)N)c1nc(-c2ccc(C(F)(F)F)cc2)c[nH]1 WEAFAWYVJKPGDN-SECBINFHSA-N 0.000 description 1
- WEAFAWYVJKPGDN-VIFPVBQESA-N C[C@H](C1(COC1)N)c1nc(-c2ccc(C(F)(F)F)cc2)c[nH]1 Chemical compound C[C@H](C1(COC1)N)c1nc(-c2ccc(C(F)(F)F)cc2)c[nH]1 WEAFAWYVJKPGDN-VIFPVBQESA-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)
- Rheumatology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2014530900A JP2014530900A (ja) | 2014-11-20 |
| JP2014530900A5 JP2014530900A5 (show.php) | 2015-12-03 |
| JP5946538B2 true JP5946538B2 (ja) | 2016-07-06 |
Family
ID=47278356
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014537760A Expired - Fee Related JP5946538B2 (ja) | 2011-10-26 | 2012-10-15 | ナトリウムチャネルモジュレーターとして有用な（４−フェニルイミダゾール−２−イル）エチルアミン誘導体 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9079878B2 (show.php) |
| EP (1) | EP2771335A2 (show.php) |
| JP (1) | JP5946538B2 (show.php) |
| KR (1) | KR101586966B1 (show.php) |
| CN (1) | CN103906746B (show.php) |
| AP (1) | AP2014007579A0 (show.php) |
| AU (1) | AU2012328034B2 (show.php) |
| BR (1) | BR112014009102A2 (show.php) |
| CA (1) | CA2850925C (show.php) |
| CL (1) | CL2014000956A1 (show.php) |
| CO (1) | CO6940427A2 (show.php) |
| CR (1) | CR20140185A (show.php) |
| CU (1) | CU20140046A7 (show.php) |
| DO (1) | DOP2014000085A (show.php) |
| EA (1) | EA023375B1 (show.php) |
| EC (1) | ECSP14013324A (show.php) |
| GT (1) | GT201400079A (show.php) |
| IL (1) | IL232267A (show.php) |
| MD (1) | MD20140037A2 (show.php) |
| MX (1) | MX337469B (show.php) |
| NI (1) | NI201400031A (show.php) |
| PE (1) | PE20141682A1 (show.php) |
| PH (1) | PH12014500919A1 (show.php) |
| SG (1) | SG11201401032YA (show.php) |
| TN (1) | TN2014000147A1 (show.php) |
| UA (1) | UA109220C2 (show.php) |
| WO (1) | WO2013061205A2 (show.php) |
| ZA (1) | ZA201402281B (show.php) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2755980T3 (pl) * | 2011-09-14 | 2020-05-18 | Dow Agrosciences Llc | Sposoby i układy do wytwarzania kwasów boronowych i ich związków pośrednich |
| SI3080134T1 (sl) | 2013-12-13 | 2018-11-30 | Vertex Pharmaceuticals Incorporated | Predzdravila piridon amidov uporabna kot modulatorji natrijevih kanalov |
| 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 |
| KR20170117170A (ko) | 2015-02-19 | 2017-10-20 | 퍼듀 퍼머 엘피 | 위 배출을 감소시키기 위한 방법 및 조성물 |
| IS2977B (is) | 2015-02-23 | 2017-07-15 | Actavis Group Ptc Ehf. | Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni |
| WO2017115128A2 (en) | 2015-12-30 | 2017-07-06 | 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 |
| US11459587B2 (en) | 2016-07-06 | 2022-10-04 | Vertex Pharmaceuticals Incorporated | Materials and methods for treatment of pain related disorders |
| 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 |
| US11529337B2 (en) | 2018-02-12 | 2022-12-20 | Vertex Pharmaceuticals Incorporated | Method of treating pain |
| AR116939A1 (es) | 2018-11-02 | 2021-06-30 | Merck Sharp & Dohme | 2-amino-n-heteroaril-nicotinamidas como inhibidores de nav1.8 |
| 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 |
| MX2022006865A (es) | 2019-12-06 | 2022-07-11 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio. |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2023211990A1 (en) | 2022-04-25 | 2023-11-02 | Siteone Therapeutics, Inc. | Bicyclic heterocyclic amide inhibitors of na v1.8 for the treatment of pain |
| 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 |
| 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 |
| 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 |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| 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 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2000035296A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Improved release of medicament active agents from a chewing gum coating |
| 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 |
| TWI283577B (en) * | 1999-10-11 | 2007-07-11 | Sod Conseils Rech Applic | Pharmaceutical composition of imidazole derivatives acting 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 |
| TWI248438B (en) * | 2001-04-10 | 2006-02-01 | Sod Conseils Rech Applic | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
| FR2842808B1 (fr) * | 2002-07-25 | 2004-09-10 | Sod Conseils Rech Applic | Nouveaux derives d'arylimidazoles, leur preparation et leurs applications therapeutiques |
| US7456164B2 (en) * | 2004-05-07 | 2008-11-25 | Pfizer, Inc | 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands |
| BRPI0510664B8 (pt) * | 2004-05-07 | 2021-05-25 | Warner Lambert Co | derivados de fenol e tiofenol 3 ou 4-monosubstituído, composição farmacêutica, combinação e uso dos compostos para tratamento de doenças relacionadas ao h3, incluindo transtornos do sistema nervoso central e transtornos inflamatórios |
| AU2005299310A1 (en) * | 2004-10-27 | 2006-05-04 | Canji, Inc. | Compositions and methods for short interfering nucleic acid inhibition of Nav1.8 |
| HRP20160005T1 (hr) * | 2005-12-22 | 2016-02-12 | Newron Pharmaceuticals S.P.A. | 2-feniletilamono derivati kao modulatori kalcijskih i/ili natrijskih kanala |
| SI2076508T1 (sl) | 2006-10-18 | 2011-04-29 | Pfizer Prod Inc | Spojine biaril eter sečnine |
| DE602008000809D1 (de) | 2007-03-23 | 2010-04-29 | Icagen Inc | Ionenkanal-Hemmer |
| AU2008247102B2 (en) | 2007-05-03 | 2011-11-24 | Pfizer Limited | 2 -pyridine carboxamide derivatives as sodium channel modulators |
| US20100227872A1 (en) | 2007-05-03 | 2010-09-09 | Mark Ian Kemp | Pyrazine derivatives |
| CA2693588C (en) | 2007-07-13 | 2015-11-17 | Icagen, Inc. | Sodium channel inhibitors |
-
2012
- 2012-10-15 CN CN201280052591.6A patent/CN103906746B/zh not_active Expired - Fee Related
- 2012-10-15 MX MX2014004738A patent/MX337469B/es active IP Right Grant
- 2012-10-15 AU AU2012328034A patent/AU2012328034B2/en not_active Ceased
- 2012-10-15 BR BR112014009102A patent/BR112014009102A2/pt active Search and Examination
- 2012-10-15 EA EA201490864A patent/EA023375B1/ru not_active IP Right Cessation
- 2012-10-15 UA UAA201404440A patent/UA109220C2/uk unknown
- 2012-10-15 CA CA2850925A patent/CA2850925C/en not_active Expired - Fee Related
- 2012-10-15 US US14/351,893 patent/US9079878B2/en not_active Expired - Fee Related
- 2012-10-15 WO PCT/IB2012/055610 patent/WO2013061205A2/en not_active Ceased
- 2012-10-15 PE PE2014000605A patent/PE20141682A1/es not_active Application Discontinuation
- 2012-10-15 AP AP2014007579A patent/AP2014007579A0/xx unknown
- 2012-10-15 SG SG11201401032YA patent/SG11201401032YA/en unknown
- 2012-10-15 EP EP12794777.8A patent/EP2771335A2/en not_active Withdrawn
- 2012-10-15 JP JP2014537760A patent/JP5946538B2/ja not_active Expired - Fee Related
- 2012-10-15 PH PH1/2014/500919A patent/PH12014500919A1/en unknown
- 2012-10-15 KR KR1020147010826A patent/KR101586966B1/ko not_active Expired - Fee Related
- 2012-10-15 MD MDA20140037A patent/MD20140037A2/ro not_active Application Discontinuation
-
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 CR CR20140185A patent/CR20140185A/es unknown
- 2014-04-24 CU CU2014000046A patent/CU20140046A7/es unknown
- 2014-04-25 GT GT201400079A patent/GT201400079A/es unknown
- 2014-04-25 DO DO2014000085A patent/DOP2014000085A/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
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