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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2771335A2 (OSRAM) |
| JP (1) | JP5946538B2 (OSRAM) |
| KR (1) | KR101586966B1 (OSRAM) |
| CN (1) | CN103906746B (OSRAM) |
| AP (1) | AP2014007579A0 (OSRAM) |
| AU (1) | AU2012328034B2 (OSRAM) |
| BR (1) | BR112014009102A2 (OSRAM) |
| CA (1) | CA2850925C (OSRAM) |
| CL (1) | CL2014000956A1 (OSRAM) |
| CO (1) | CO6940427A2 (OSRAM) |
| CR (1) | CR20140185A (OSRAM) |
| CU (1) | CU20140046A7 (OSRAM) |
| DO (1) | DOP2014000085A (OSRAM) |
| EA (1) | EA023375B1 (OSRAM) |
| EC (1) | ECSP14013324A (OSRAM) |
| GT (1) | GT201400079A (OSRAM) |
| IL (1) | IL232267A (OSRAM) |
| MD (1) | MD20140037A2 (OSRAM) |
| MX (1) | MX337469B (OSRAM) |
| NI (1) | NI201400031A (OSRAM) |
| PE (1) | PE20141682A1 (OSRAM) |
| PH (1) | PH12014500919A1 (OSRAM) |
| SG (1) | SG11201401032YA (OSRAM) |
| TN (1) | TN2014000147A1 (OSRAM) |
| UA (1) | UA109220C2 (OSRAM) |
| WO (1) | WO2013061205A2 (OSRAM) |
| ZA (1) | ZA201402281B (OSRAM) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6425543B2 (ja) * | 2011-09-14 | 2018-11-21 | ダウ アグロサイエンシィズ エルエルシー | ボロン酸およびその中間体を生成させるための方法およびシステム |
| GEP20207082B (en) | 2013-12-13 | 2020-04-10 | Vertex Pharma | 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 |
| WO2016065341A1 (en) * | 2014-10-24 | 2016-04-28 | Avectas Limited | Delivery across cell plasma membranes |
| BR112017017619A2 (pt) | 2015-02-19 | 2018-05-08 | Purdue Pharma Lp | métodos e composições para diminuir esvaziamento gástrico |
| IS2977B (is) | 2015-02-23 | 2017-07-15 | Actavis Group Ptc Ehf. | Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni |
| CA3009715A1 (en) | 2015-12-30 | 2017-07-06 | Avectas Limited | Vector-free delivery of gene editing proteins and compositions to cells and tissues |
| EP4650364A3 (en) * | 2016-07-06 | 2026-01-21 | Vertex Pharmaceuticals Incorporated | Materials and methods for treatment of pain related disorders |
| CN118542952A (zh) | 2016-07-06 | 2024-08-27 | 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 |
| JP7104070B2 (ja) | 2017-05-16 | 2022-07-20 | 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重水素化ピリドンアミドおよびそのプロドラッグ |
| EP3651752B1 (en) | 2017-07-11 | 2024-11-20 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| JP2021512935A (ja) | 2018-02-12 | 2021-05-20 | 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 | 疼痛を処置する方法 |
| MA54076A (fr) | 2018-11-02 | 2022-02-09 | Merck Sharp & Dohme | 2-amino-n-hétéroaryl-nicotinamides utilisés en tant qu'inhibiteurs de nav1.8 |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | 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 |
| UA130303C2 (uk) | 2019-12-06 | 2026-01-14 | Вертекс Фармасьютикалз Інкорпорейтед | Заміщені тетрагідрофурани як модулятори натрієвих каналів |
| AU2022286438A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide 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 |
| CA3221960A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| CA3221788A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| JP2024522293A (ja) | 2021-06-04 | 2024-06-13 | 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置換テトラヒドロフラン類似体 |
| PE20241335A1 (es) | 2021-06-04 | 2024-07-03 | Vertex Pharma | N-(hidroxialquil (hetero)aril) tetrahidrofurano carboxamidas como moduladores de canales de sodio |
| IL316422A (en) | 2022-04-22 | 2024-12-01 | Vertex Pharma | Heteroaryl compounds for pain treatment |
| US20250388541A1 (en) | 2022-04-22 | 2025-12-25 | 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 |
| PE20251179A1 (es) | 2022-04-22 | 2025-04-23 | Vertex Pharma | Compuestos de heteroarilo para el tratamiento del dolor |
| 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 |
| 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 |
| WO2025090480A1 (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 |
| 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 |
| US20260001877A1 (en) | 2024-06-28 | 2026-01-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| 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 |
| 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 |
| JP4173191B2 (ja) * | 2004-05-07 | 2008-10-29 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | H3リガンドとして有用な3‐または4‐一置換フェノールおよびチオフェノール誘導体 |
| KR20070083828A (ko) | 2004-10-27 | 2007-08-24 | 쉐링 코포레이션 | Nav1.8의 짧은 간섭 핵산 억제를 위한 조성물 및방법 |
| JP5271087B2 (ja) * | 2005-12-22 | 2013-08-21 | ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー | カルシウム及び/又はナトリウムチャネル調節物質としての2−フェニルエチルアミノ誘導体 |
| HRP20110158T1 (hr) | 2006-10-18 | 2011-04-30 | Pfizer Products Inc. | Biaril eterski spojevi ureje |
| CA2681572C (en) | 2007-03-23 | 2014-02-11 | Icagen, Inc. | Inhibitors of ion channels |
| US20100227872A1 (en) * | 2007-05-03 | 2010-09-09 | Mark Ian Kemp | Pyrazine derivatives |
| AP2516A (en) | 2007-05-03 | 2012-11-26 | Pfizer Ltd | 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 PH PH1/2014/500919A patent/PH12014500919A1/en unknown
- 2012-10-15 AU AU2012328034A patent/AU2012328034B2/en not_active Ceased
- 2012-10-15 CN CN201280052591.6A patent/CN103906746B/zh not_active Expired - Fee Related
- 2012-10-15 EP EP12794777.8A patent/EP2771335A2/en not_active Withdrawn
- 2012-10-15 SG SG11201401032YA patent/SG11201401032YA/en unknown
- 2012-10-15 KR KR1020147010826A patent/KR101586966B1/ko not_active Expired - Fee Related
- 2012-10-15 BR BR112014009102A patent/BR112014009102A2/pt active Search and Examination
- 2012-10-15 UA UAA201404440A patent/UA109220C2/uk unknown
- 2012-10-15 MD MDA20140037A patent/MD20140037A2/ro not_active Application Discontinuation
- 2012-10-15 EA EA201490864A patent/EA023375B1/ru not_active IP Right Cessation
- 2012-10-15 WO PCT/IB2012/055610 patent/WO2013061205A2/en not_active Ceased
- 2012-10-15 CA CA2850925A patent/CA2850925C/en not_active Expired - Fee Related
- 2012-10-15 AP AP2014007579A patent/AP2014007579A0/xx unknown
- 2012-10-15 PE PE2014000605A patent/PE20141682A1/es not_active Application Discontinuation
- 2012-10-15 MX MX2014004738A patent/MX337469B/es active IP Right Grant
- 2012-10-15 US US14/351,893 patent/US9079878B2/en not_active Expired - Fee Related
- 2012-10-15 JP JP2014537760A patent/JP5946538B2/ja not_active Expired - Fee Related
-
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 EC ECSP14013324 patent/ECSP14013324A/es unknown
- 2014-04-25 GT GT201400079A patent/GT201400079A/es unknown
- 2014-04-25 DO DO2014000085A patent/DOP2014000085A/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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