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 (enExample) | 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 (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 |
|---|---|---|---|---|
| HK1199262A1 (en) * | 2011-09-14 | 2015-06-26 | Dow Agrosciences Llc | Methods and systems for forming boronic acids and intermediates thereof |
| LT3080134T (lt) | 2013-12-13 | 2018-11-12 | Vertex Pharmaceuticals Incorporated | Piridono amidų provaistai, naudotini kaip natrio kanalų moduliatoriai |
| KR102192572B1 (ko) | 2014-06-09 | 2020-12-18 | 삼성전자주식회사 | 광원 모듈의 불량 검사방법, 광원 모듈의 제조 방법 및 광원 모듈 검사장치 |
| CN107206015A (zh) * | 2014-10-24 | 2017-09-26 | 阿维塔斯有限公司 | 透细胞质膜的传递 |
| 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 |
| CN116676292A (zh) | 2015-12-30 | 2023-09-01 | 阿维塔斯有限公司 | 基因编辑蛋白和组合物向细胞和组织的无载体递送 |
| AU2017292173B2 (en) | 2016-07-06 | 2022-01-13 | Vertex Pharmaceuticals Incorporated | Materials and methods for treatment of pain related disorders |
| CN110214149B (zh) | 2016-07-06 | 2024-05-14 | 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 |
| US11358977B2 (en) | 2017-05-16 | 2022-06-14 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
| ES3008911T3 (en) | 2017-07-11 | 2025-03-25 | Vertex Pharma | Carboxamides as modulators of sodium channels |
| US20190343817A1 (en) | 2018-02-12 | 2019-11-14 | Vertex Pharmaceuticals Incorporated | Method of treating pain |
| 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 |
| CR20220316A (es) | 2019-12-06 | 2022-10-07 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio |
| 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 |
| AU2022285758A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| 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 |
| 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 |
| JP2024522292A (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ｎ－（ヒドロキシアルキル（ヘテロ）アリール）テトラヒドロフランカルボキサミド |
| CN117813302A (zh) | 2021-06-04 | 2024-04-02 | 沃泰克斯药物股份有限公司 | 经取代的四氢呋喃-2-甲酰胺作为钠通道调节剂 |
| PE20251179A1 (es) | 2022-04-22 | 2025-04-23 | Vertex Pharma | Compuestos de heteroarilo para el tratamiento del dolor |
| TW202408501A (zh) | 2022-04-22 | 2024-03-01 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| 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 |
| EP4511117A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| 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 |
| KR20250120351A (ko) | 2022-12-06 | 2025-08-08 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법 |
| 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 |
| 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 |
| WO2025090465A1 (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 |
| 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| SI1747210T1 (sl) * | 2004-05-07 | 2010-09-30 | Warner Lambert Co | ali monosubstituirani fenolin in tiofenolni derivati uporabni kot ligandi H |
| US7456164B2 (en) * | 2004-05-07 | 2008-11-25 | Pfizer, Inc | 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands |
| CA2584785A1 (en) | 2004-10-27 | 2006-05-04 | Schering Corporation | Compositions and methods for short interfering nucleic acid inhibition of nav1.8 |
| EP1963280B1 (en) * | 2005-12-22 | 2015-10-28 | Newron Pharmaceuticals S.p.A. | 2-phenylethylamino derivatives as calcium and/or sodium channel modulators |
| GEP20125425B (en) | 2006-10-18 | 2012-03-26 | Pfizer Prod Inc | Biaryl ether urea compounds |
| CL2008000835A1 (es) | 2007-03-23 | 2008-10-03 | Icagen Inc Pfizer Ltd | Compuestos derivados de sulfonamidas, inhibidores de los canales de calcio; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del dolor, sindrome de intestino irritable, enfermedad de crohn, taquiarritm |
| 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 EA EA201490864A patent/EA023375B1/ru not_active IP Right Cessation
- 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 BR BR112014009102A patent/BR112014009102A2/pt active Search and Examination
- 2012-10-15 CN CN201280052591.6A patent/CN103906746B/zh not_active Expired - Fee Related
- 2012-10-15 CA CA2850925A patent/CA2850925C/en not_active Expired - Fee Related
- 2012-10-15 SG SG11201401032YA patent/SG11201401032YA/en unknown
- 2012-10-15 AU AU2012328034A patent/AU2012328034B2/en not_active Ceased
- 2012-10-15 KR KR1020147010826A patent/KR101586966B1/ko not_active Expired - Fee Related
- 2012-10-15 EP EP12794777.8A patent/EP2771335A2/en not_active Withdrawn
- 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 US US14/351,893 patent/US9079878B2/en not_active Expired - Fee Related
- 2012-10-15 AP AP2014007579A patent/AP2014007579A0/xx unknown
- 2012-10-15 UA UAA201404440A patent/UA109220C2/uk unknown
- 2012-10-15 WO PCT/IB2012/055610 patent/WO2013061205A2/en not_active Ceased
- 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 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
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