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PE20230300A1 - Tetrahidrofuranos sustituidos como moduladores de canales de sodio - Google Patents

Tetrahidrofuranos sustituidos como moduladores de canales de sodio

Info

Publication number
PE20230300A1
PE20230300A1 PE2022001030A PE2022001030A PE20230300A1 PE 20230300 A1 PE20230300 A1 PE 20230300A1 PE 2022001030 A PE2022001030 A PE 2022001030A PE 2022001030 A PE2022001030 A PE 2022001030A PE 20230300 A1 PE20230300 A1 PE 20230300A1
Authority
PE
Peru
Prior art keywords
pain
alkyl
sodium channel
compounds
rac
Prior art date
Application number
PE2022001030A
Other languages
English (en)
Inventor
Steven John Durrant
Nadia M Ahmad
Elizabeth Mary Beck
Meireles Lidio Carvalho
Ewa Iwona Chudyk
Jardi Gorka Etxebarria
Bhairavi Galan
Ruah Sara S Hadida
Dennis James Hurley
Ronald Marcellus Knegtel
Timothy Donald Neubert
Joanne Louise Pinder
Joseph Pontillo
Robert Pullin
Yvonne Schmidt
David Matthew Shaw
Sarah Skerratt
Dean Stamos
Steven Andrew Thomson
Anisa Nizarali Virani
Christopher Wray
Original Assignee
Vertex Pharma
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of PE20230300A1 publication Critical patent/PE20230300A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Liquid Crystal Substances (AREA)
  • Details Of Television Scanning (AREA)
  • Amplitude Modulation (AREA)
  • Amplifiers (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Esta referido a compuestos de Formula I, en donde: R es H, alquilo C1-6; R2c es H, OH, halo, alquilo, alquenilo, entre otras opciones; R5b1 y R5b2 son H, alquilo, cicloalquilo, haloalquilo; R4b1 y R4b2 son H, alquilo, cicloalquilo, haloalquilo; X2a es N, NO, CR2a; X3c es N, CR3c; X4a es N, NO, CR4a; X4c es N, CR4c; X5a es N, NO, CR5a; X5c es N, CR5c; X6a es N, NO, CR6a; y, X6c es N, CR6c. Entre los compuestos preferidos tenemos los siguientes: rac-(2S,3R,4R,5R)-4-[[3- [2-(difluorometoxi)-4- fluoro-fenil]-4,5-dimetil-5- (trifluorometil)tetrahidrofuran -2-carbonil]amino]piridin-2- carboxamida; rac-(2S,3R,4R,5R)-4-[[3- (3,4-difluoro-2-metoxi- fenil)-4,5-dimetil-5- (trifluorometil)tetrahidrofuran -2-carbonil]amino]piridin-2- carboxamida; entre otros. Estos compuestos son inhibidores de canales de sodio y se emplean para tratar o reducir el dolor cronico, dolor intestinal, dolor neuropatico, dolor musculoesqueletico, dolor agudo, dolor inflamatorio, dolor por cancer, dolor idiopatico, entre otros.
PE2022001030A 2019-12-06 2020-12-04 Tetrahidrofuranos sustituidos como moduladores de canales de sodio PE20230300A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962944869P 2019-12-06 2019-12-06
PCT/US2020/063290 WO2021113627A1 (en) 2019-12-06 2020-12-04 Substituted tetrahydrofurans as modulators of sodium channels

Publications (1)

Publication Number Publication Date
PE20230300A1 true PE20230300A1 (es) 2023-02-13

Family

ID=73854989

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022001030A PE20230300A1 (es) 2019-12-06 2020-12-04 Tetrahidrofuranos sustituidos como moduladores de canales de sodio

Country Status (21)

Country Link
US (2) US11834441B2 (es)
EP (1) EP4069691B1 (es)
JP (1) JP2023504546A (es)
KR (1) KR20220124176A (es)
AR (1) AR120680A1 (es)
AU (1) AU2020397059A1 (es)
BR (1) BR112022010924A2 (es)
CA (1) CA3164134A1 (es)
CL (1) CL2022001489A1 (es)
CO (1) CO2022008969A2 (es)
CR (1) CR20220316A (es)
DK (1) DK4069691T3 (es)
DO (1) DOP2022000115A (es)
EC (1) ECSP22052564A (es)
IL (1) IL293592A (es)
JO (1) JOP20220130A1 (es)
MX (1) MX2022006865A (es)
PE (1) PE20230300A1 (es)
TW (1) TW202128675A (es)
UY (1) UY38979A (es)
WO (1) WO2021113627A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2021014441A (es) 2019-05-31 2022-01-06 Ikena Oncology Inc Inhibidores del dominio asociado mejorador de la transcripcion (tead) y usos de los mismos.
PE20230300A1 (es) 2019-12-06 2023-02-13 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio
CA3221939A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
WO2022256708A1 (en) 2021-06-04 2022-12-08 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
WO2022256702A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
EP4347583A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
IL308934A (en) * 2021-06-04 2024-01-01 Vertex Pharma Manufacturing process of converted natran tetrahydrofuran channel modulators
CA3221960A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
PE20241335A1 (es) 2021-06-04 2024-07-03 Vertex Pharma N-(hidroxialquil (hetero)aril) tetrahidrofurano carboxamidas como moduladores de canales de sodio
EP4355733A1 (en) 2021-06-15 2024-04-24 Grünenthal GmbH Substituted pyrazole amides
WO2023211990A1 (en) 2022-04-25 2023-11-02 Siteone Therapeutics, Inc. Bicyclic heterocyclic amide inhibitors of na v1.8 for the treatment of pain
TW202409017A (zh) * 2022-08-24 2024-03-01 大陸商江蘇恆瑞醫藥股份有限公司 雜環類化合物、其製備方法及其在醫藥上的應用
WO2024123815A1 (en) * 2022-12-06 2024-06-13 Vertex Pharmaceuticals Incorporated Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
WO2024126648A1 (en) 2022-12-14 2024-06-20 Grünenthal GmbH SULFOXIMINES AS INHIBITORS OF NaV1.8
EP4385980A1 (en) 2022-12-14 2024-06-19 Grünenthal GmbH Indazoles as inhibitors of nav1.8
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EP4069691B1 (en) 2024-09-18
JOP20220130A1 (ar) 2023-01-30

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