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AR129104A1 - Compuestos heteroarilo para el tratamiento del dolor - Google Patents

Compuestos heteroarilo para el tratamiento del dolor

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Publication number
AR129104A1
AR129104A1 ARP230100957A ARP230100957A AR129104A1 AR 129104 A1 AR129104 A1 AR 129104A1 AR P230100957 A ARP230100957 A AR P230100957A AR P230100957 A ARP230100957 A AR P230100957A AR 129104 A1 AR129104 A1 AR 129104A1
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AR
Argentina
Prior art keywords
alkyl
halo
membered
haloalkyl
alkylene
Prior art date
Application number
ARP230100957A
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English (en)
Inventor
Dennis James Hurley
Timothy Donald Neubert
Vijayalaksmi Arumugam
Ruah Sara Sabina Hadida
Jason Mcartney
Mark Thomas Miller
Jinglan Zhou
Jaclyn Chau
Robert Martin Demoret
Senait G Ghirmai
Roman Askatovich Valiulin
Alexander Frederik Kintzer
David Robert Slochower
Kathleen Aertgeerts
Elizabeth Mary Beck
James Jun Bon MUI
Miranda Adele Wright
Ronald Marcellus Alphonsus Knegtel
Ewa Iwona Chudyk
Joanne Louise Pinder
James Dodd
Iain Simpson
Original Assignee
Vertex Pharma
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Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR129104A1 publication Critical patent/AR129104A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se proporcionan compuestos, y sales farmacéuticamente aceptables de estos, útiles como inhibidores de canales de sodio. También se proporcionan composiciones farmacéuticas que comprenden los compuestos o sales farmacéuticamente aceptables y métodos de uso de los compuestos, sales farmacéuticamente aceptables y composiciones farmacéuticas en el tratamiento de diversos trastornos, incluido el dolor. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable de este, en donde: A es un compuesto del grupo de fórmulas (4); L es -O-, un enlace simple, -O-C(R)₂-, -C(R)₂-, -C(R)₂-O-, o -N(R)-; cada R es de forma independiente H, halo, o alquilo de C₁-C₆; X² es N o CR²; X⁴ es N o CR⁴; X⁵ es N o CR⁵; X⁶ es N o CR⁶; X⁷ es N o CR⁷; Y¹ es N o CR¹ᵃ; Y² es N, ⁺N-O⁻ o CR²ᵃ; Y³ es N o CR³ᵃ; R² es H, halo, alquilo de C₁-C₆, (alquileno de C₁-C₆)-NR⁸R⁹, alquenilo de C₂-C₆, alcoxi de C₁-C₆, (alquileno de C₁-C₆)-OH, C(O)OR⁸, o CH(OH)(CH₂)ₘ(CHOH)ₙ(CH₂)ₚH; R⁴, R⁵, R⁶ y R⁷ se definen de la siguiente manera: (i) R⁴, R⁵, R⁶ y R⁷ son cada uno de forma independiente H, halo, alquilo de C₁-C₆, haloalquilo de C₁-C₆ o cicloalquilo de C₃-C₆ opcionalmente sustituido con uno o más alquilo, halo u OH; (ii) R⁴ y R⁷ son cada uno de forma independiente es H, halo, alquilo de C₁-C₆, haloalquilo de C₁-C₆, o cicloalquilo de C₃-C₆ opcionalmente sustituido con uno o más halo; y R⁵ y R⁶, junto con los átomos de carbono a los que se unen, forman un anillo de la fórmula: (5); o (iii) R⁴ y R⁷ son cada uno de forma independiente es H, halo, alquilo de C₁-C₆, haloalquilo de C₁-C₆, cicloalquilo de C₃-C₆, o cicloalquilo de C₃-C₆ sustituido con uno o más halo; y R⁵ y R⁶, junto con los átomos de carbono a los que están unidos, forman un anillo de la fórmula: (6); R⁸ y R⁹ son cada de forma independiente H o alquilo de C₁-C₆; cada R¹⁰ es de forma independiente H o halo; R¹ᵃ es H, halo, CN, alquilo de C₁-C₆, OH, C(O)NR¹²R¹³, alcoxi de C₁-C₆, NR¹²R¹³, NR⁸C(O)NR⁸R⁹, (alquileno de C₁-C₆)-C(O)NR⁸R⁹, (alquileno de C₁-C₆)-OH, C(O)OR¹², OR¹², CH(OH)(CH₂)ₘ(CHOH)ₙ(CH₂)ₚH, N=S(=O)(CH₃)₂, N=S(=O)R’R’’, heteroarilo de 5 - 10 miembros, o heterociclilo de 4 - 10 miembros, en donde el heterociclilo o heteroarilo en dicho heteroarilo de 5 - 10 miembros o heterociclilo de 4 - 10 miembros se sustituye opcionalmente con 1 - 4 sustituyentes seleccionados de OH, halo, oxo, C(O)NR⁸R⁹, NR⁸R⁹, alquilo de C₁-C₆, alcoxi de C₁-C₆, (alquileno de C₁-C₆)-OH, (alquileno de C₁-C₆)-O-(alquilo de C₁C₆), y (alquileno de C₁-C₆)-NR⁸R⁹; R’ y R’’, junto con el átomo S al que se unen, forman un heterociclilo de 4 - 7 miembros; R¹¹, R²ᵃ y R³ᵃ son cada uno de forma independiente H, halo, CN, alquilo de C₁-C₆, C(O)NR⁸R⁹ o alcoxi de C₁-C₆; R¹² y R¹³ son cada uno de forma independiente H, C(O)(alquilo de C₁-C₆), (alquileno de C₁-C₆)-NR⁸R⁹, CH₂CH(OH)(CH₂)ₘ(CHOH)ₙ(CH₂)ₚH, alquilo de C₁-C₆ opcionalmente sustituido con uno o más OH, indanilo, (alquileno de C₁-C₆)-(cicloalquilo de C₃-C₆), (alquileno de C₁-C₆)-fenilo, (alquileno de C₁-C₆)-(heterociclilo de 5 miembros), cicloalquilo de C₄-C₇, arilo de C₆-C₁₀, heteroarilo de 5 - 6 miembros, o heterociclilo de 4 - 7 miembros, en donde el indanilo, (alquileno de C₁-C₆)-(cicloalquilo de C₃-C₆), (alquileno de C₁-C₆)-fenilo, (alquileno de C₁-C₆)-(heterociclilo de 5 miembros), cicloalquilo de C₄-C₇, arilo de C₆-C₁₀, heteroarilo de 5 - 6 miembros, o heterociclilo de 4 - 7 miembros se sustituye opcionalmente con 1 - 4 sustituyentes seleccionados de OH, oxo, alquilo de C₁-C₆, (alquileno de C₁-C₆)-OH, y alquilo de C₁-C₆; Z¹ es cicloalquilo de 3 - 10 miembros, cicloalquenilo de 3 - 10 miembros, fenilo, heterociclilo de 4 - 10 miembros, o heteroarilo de 5 - 6 miembros, en donde dicho cicloalquilo de 3 - 10 miembros, cicloalquenilo de 3 - 10 miembros, fenilo, heterociclilo de 4 - 10 miembros, o heteroarilo de 5 - 6 miembros puede no sustituirse o puede sustituirse con 1 - 4 sustituyentes seleccionados de halo, OH, CD₃, alquilo de C₁-C₆, alcoxi de C₁-C₆, haloalquilo de C₁-C₆, CH₂OH, C(O)H, y haloalcoxi de C₁-C₆; m, n, y p son cada uno de forma independiente 0 o 1; y q es 1, 2 o 3, en donde cuando X² es N, entonces: L es O, y Z¹ es fenilo, en donde dicho fenilo se sustituye con 2 - 4 sustituyentes seleccionados de halo, OH, alquilo de C₁-C₆, alcoxi de C₁-C₆, haloalquilo de C₁-C₆ y haloalcoxi de C₁-C₆; o L es un enlace simple, y Z¹ es heterociclilo de 4 - 10 miembros, en donde dicho heterociclilo de 4 - 10 miembros se sustituye con 2 - 4 sustituyentes seleccionados de halo, OH, alquilo de C₁-C₆, alcoxi de C₁-C₆, haloalquilo de C₁-C₆ y haloalcoxi de C₁-C₆; y en donde cuando X², X⁴, X⁵, X⁶ y X⁷ son cada uno CH, L es un enlace simple, y Z¹ es fenilo, entonces dicho fenilo se sustituye con 1 - 4 sustituyentes seleccionados de halo, OH, alquilo de C₁-C₆, alcoxi de C₁-C₆, haloalquilo de C₁-C₆, y haloalcoxi de C₁-C₆. Reivindicación 49: Un compuesto de la fórmula (2) o (3), o una sal farmacéuticamente aceptable de este, en donde: B es un compuesto de fórmula (7); L² es un enlace simple o -CH₂-; X¹² es CH o N; R¹⁴ es H, halo o alcoxi de C₁-C₆; R⁸ᵃ y R⁹ᵃ se definen de la siguiente manera: (i) R⁸ᵃ y R⁹ᵃ son cada uno de forma independiente H, halo, alquilo de C₁-C₆, haloalquilo de C₁-C₆, o cicloalquilo de C₃-C₆ opcionalmente sustituido con 1 - 4 sustituyentes seleccionados de alquilo de C₁-C₆, halo, y haloalquilo de C₁-C₆; (ii) R⁸ᵃ y R⁹ᵃ, junto con los átomos de carbono a los que están unidos, forman un anillo de la fórmula: (8), en donde dicho anillo se sustituye opcionalmente con 1 - 4 alquilo de C₁-C₆; R¹⁰ᵃ es H, halo, alquilo de C₁-C₆, haloalquilo de C₁-C₆ o cicloalquilo de C₃-C₆ opcionalmente sustituido con 1 - 4 sustituyentes seleccionados de alquilo de C₁-C₆, halo y haloalquilo de C₁-C₆; R¹¹ᵃ es H o alquilo de C₁-C₆; R¹⁵ es C(O)NR¹⁶R¹⁷ o heteroarilo de 5 miembros en donde el heteroarilo de 5 miembros se sustituye opcionalmente con 1 - 4 alquilo de C₁-C₆; R¹⁶ y R¹⁷ son cada uno de forma independiente H o alquilo de C₁-C₆; Z² es fenilo o cicloalquilo de C₄-C₆, en donde dicho fenilo o cicloalquilo de C₄-C₆ se sustituye opcionalmente con 1 - 4 sustituyentes seleccionados de halo y alquilo de C₁-C₆; y q² es 1, 2 o 3. Reivindicación 63: Un método para inhibir un canal de sodio activado por voltaje en un sujeto que comprende administrar al sujeto el compuesto de cualquiera de las reivindicaciones 1 - 59, o una sal farmacéuticamente aceptable de este, el compuesto de la reivindicación 60, o la composición farmacéutica de la reivindicación 61 o 62. Reivindicación 64: El método de acuerdo con la reivindicación 63, en donde el canal de sodio activado por voltaje es NaV1,8. Reivindicación 65: Un método para tratar o disminuir la gravedad en un sujeto de dolor crónico, dolor intestinal, dolor neuropático, dolor musculoesquelético, dolor agudo, dolor inflamatorio, dolor por cáncer, dolor idiopático, dolor posquirúrgico, dolor visceral, esclerosis múltiple, síndrome de Charcot-Marie-Tooth, incontinencia, tos patológica, o arritmia cardíaca que comprende administrar al sujeto una cantidad eficaz del compuesto de cualquiera de las reivindicaciones 1 - 59, o una sal farmacéuticamente aceptable de este, el compuesto de la reivindicación 60 o la composición farmacéutica de la reivindicación 61 o 62.
ARP230100957A 2022-04-22 2023-04-21 Compuestos heteroarilo para el tratamiento del dolor AR129104A1 (es)

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EP4511116A1 (en) 2022-04-22 2025-02-26 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
WO2025098515A1 (en) * 2023-11-10 2025-05-15 Danatlas Pharmaceuticals Co., Ltd. Heterocyclic derivatives, compositions and uses thereof
WO2025240895A1 (en) * 2024-05-17 2025-11-20 Siteone Therapeutics, Inc. SUBSTITUTED CYCLOALKYL AND HETEROCYCLOALKYL INHIBITORS OF NAv1.8 FOR THE TREATMENT OF PAIN
WO2025256572A1 (zh) * 2024-06-13 2025-12-18 海思科医药集团股份有限公司 一种Nav1.8抑制剂及其在医药上的应用
WO2026001999A1 (zh) * 2024-06-25 2026-01-02 江苏恒瑞医药股份有限公司 芳香环类化合物、其制备方法及其在医药上的应用
WO2026008013A1 (zh) * 2024-07-03 2026-01-08 江苏恒瑞医药股份有限公司 氧代杂芳基类化合物、其制备方法及其在医药上的应用

Family Cites Families (318)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1338235A (en) 1970-12-15 1973-11-21 May & Baker Ltd Azapurinones
CA1317298C (en) 1987-03-03 1993-05-04 Upjohn Company (The) Antibiotic sulfonylaminocarbonyl activated .beta.-lactams
DE3854684T2 (de) 1987-07-23 1996-03-28 Zeneca Pharma Sa Cephalosporinverbindungen, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Präparate.
US4950585A (en) 1987-08-18 1990-08-21 Konica Corporation Coupler for photographic use
DE68908786T2 (de) 1988-06-16 1994-03-17 Smith Kline French Lab Condensierte Pyrimidinderivate, Verfahren und Zwischenprodukte zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen.
GB8814352D0 (en) 1988-06-16 1988-07-20 Smith Kline French Lab Chemical compounds
US4923874A (en) 1988-07-21 1990-05-08 G. D. Searle & Co. Use of 8-azapurin-6-one derivatives for control of hypertension
GB8817651D0 (en) 1988-07-25 1988-09-01 Smith Kline French Lab Chemical compounds
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
JP2952706B2 (ja) 1990-10-26 1999-09-27 大塚化学株式会社 ４―キノロン誘導体の製造法
MX9200299A (es) 1991-02-07 1992-12-01 Roussel Uclaf Nuevos derivados biciclicos nitrogenados, su procedimiento de preparacion los nuevos compuestos intermedios obtenidos su aplicacion como medicamentos y las composiciones farmaceuticas que los contienen.
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5316906A (en) 1991-08-23 1994-05-31 Molecular Probes, Inc. Enzymatic analysis using substrates that yield fluorescent precipitates
US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
IT1254469B (it) 1992-02-25 1995-09-25 Recordati Chem Pharm Derivati benzopiranici e benzotiopiranici
EP0558245A1 (en) 1992-02-25 1993-09-01 RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY Heterobicyclic compounds as antagogists of alpha-1 adrenergic and SHT1A receptors
US5294612A (en) 1992-03-30 1994-03-15 Sterling Winthrop Inc. 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
DE4233717A1 (de) 1992-10-07 1994-04-14 Bayer Ag Substituierte 3,4-Hetaryl-pyrazoline
TW299333B (es) 1992-12-29 1997-03-01 Takeda Pharm Industry Co Ltd
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
CA2211729A1 (en) 1995-03-10 1996-09-19 Sanofi Pharmaceuticals, Inc. 6-aryl pyrazolo[3,4-d¦pyrimidin-4-ones and compositions and methods of use thereof
US5741657A (en) 1995-03-20 1998-04-21 The Regents Of The University Of California Fluorogenic substrates for β-lactamase and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
US6200980B1 (en) 1995-06-07 2001-03-13 Cell Pathways, Inc. Method of treating a patient having precancerous lesions with phenyl purinone derivatives
US6060477A (en) 1995-06-07 2000-05-09 Cell Pathways, Inc. Method of treating a patient having precancerous lesions with phenyl cycloamino pyrimidinone derivatives
AU4153496A (en) 1995-10-20 1997-05-07 Flora Inc. Transdermal delivery of alpha adrenoceptor blocking agents
US6080757A (en) 1996-06-06 2000-06-27 Pfizer Inc Antibiotic quinolones and derivatives
US5700821A (en) 1996-07-30 1997-12-23 University Of Pittsburgh Phosphatase inhibitors and methods of use thereof
JP2001503414A (ja) 1996-10-31 2001-03-13 ハーバー ブランチ オーシャノグラフィック インスティテューション インク． 抗神経性炎症化合物および組成物ならびにその使用法
WO1998027080A1 (en) 1996-12-19 1998-06-25 Agrevo Uk Limited Chromones useful as fungicides
US5942508A (en) 1997-02-04 1999-08-24 Senju Pharmaceutical Co., Ltd. Method for solubilizing pyridonecarboxylic acid solubilizer thereof and aqueous solution containing solubilized pyridonecarboxylic acid
US6274592B1 (en) 1997-02-04 2001-08-14 Senju Pharmaceutical Co., Ltd. Method for stabilizing arylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized arylcarboxylic acid
US5994367A (en) 1997-03-07 1999-11-30 The University Of North Carolina At Chapel Hill Method for treating tumors using 2-aryl-naphthyridin-4-ones
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
PT1073658E (pt) 1998-04-20 2003-12-31 Pfizer Inibidores de ogmp pdes de pirazolopirimidinona para o tratamento da disfuncao sexual
MXPA00011889A (es) 1998-06-02 2003-04-25 Osi Pharm Inc Composiciones de pirrolo (2,3d) piridina y su uso.
JP2002528456A (ja) 1998-10-23 2002-09-03 ファイザー・インク 性的機能障害の処置のためのピラゾロピリミジノン系ｃＧＭＰ阻害薬
JP3539628B2 (ja) 1999-09-17 2004-07-07 富士写真フイルム株式会社 発光素子材料、それを使用した発光素子およびアミン化合物
EA200200240A1 (ru) 1999-10-11 2002-10-31 Пфайзер Инк. 5-(2-ЗАМЕЩЕННЫЕ-5-ГЕТЕРОЦИКЛИЛСУЛЬФОНИЛПИРИД-3-ИЛ)-ДИГИДРОПИРАЗОЛО[4,3-d]ПИРИМИДИН-7-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ФОСФОДИЭСТЕРАЗЫ
TWI265925B (en) 1999-10-11 2006-11-11 Pfizer Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them
BR0016821A (pt) 1999-12-31 2002-12-10 Texas Biotechnology Corp Sulfonamidas e derivados da mesma que modulam a atividade de endotelina
EP1276739A2 (en) 2000-04-24 2003-01-22 Bristol-Myers Squibb Company Heterocycles that are inhibitors of impdh enzyme
US20020028799A1 (en) 2000-07-06 2002-03-07 Naylor Alasdair Mark Treatment of male sexual dysfunction
JP5209835B2 (ja) 2000-07-10 2013-06-12 ヴァーテックス ファーマシューティカルズ （サンディエゴ）エルエルシー イオンチャネルアッセイ法
EP1176147A1 (en) 2000-07-28 2002-01-30 Pfizer Limited Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-ones and intermediates thereof
GB0023918D0 (en) 2000-09-29 2000-11-15 King S College London Antiparasitic compounds
GB0025782D0 (en) 2000-10-20 2000-12-06 Pfizer Ltd Use of inhibitors
JP2002189128A (ja) 2000-12-22 2002-07-05 Fuji Photo Film Co Ltd 光学フイルム、偏光選択素子、偏光板および液晶表示装置
EP1353913A2 (en) 2001-01-16 2003-10-22 AstraZeneca AB Therapeutic heterocyclic compounds
CA2434066A1 (en) 2001-01-26 2002-09-12 Pharmacia Italia S.P.A. Chromane derivatives, process for their preparation and their use as antitumor agents
GB0106661D0 (en) 2001-03-16 2001-05-09 Pfizer Ltd Pharmaceutically active compounds
EP2181985B1 (en) 2001-08-10 2011-10-26 Shionogi & Co., Ltd. Antiviral Agent
SE0103648D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic quinolone compounds
GB0130416D0 (en) 2001-12-20 2002-02-06 Eastman Kodak Co Photographic elements containing a de-aggregating compound dye-forming coupler and stabilizer
GB0130418D0 (en) 2001-12-20 2002-02-06 Eastman Kodak Co Photographic elements containing a deaggregating compound and dye forming coupler
JP2005531617A (ja) 2002-07-01 2005-10-20 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング 重合可能なルミネセント化合物および混合物、ルミネセントポリマー材料およびこれらの使用
EP1537102A4 (en) 2002-08-16 2010-12-08 Astrazeneca Ab INHIBITORS OF PHOSPHOINOSITIDE-3-KINASE BETA
WO2004058787A2 (en) 2002-12-27 2004-07-15 Tibotec Bvba Fluorogenic enzyme substrates and methods of preparation
JP2005008789A (ja) 2003-06-20 2005-01-13 Toray Ind Inc 有機エレクトロルミネッセンス用材料、および有機エレクトロルミネッセンス用材料の製造方法、ならびに有機エレクトロルミネッセンス素子
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
US7049318B2 (en) 2003-07-25 2006-05-23 Amgen Inc. Substituted heterocyclic compounds and methods of use
JP4795634B2 (ja) 2003-10-31 2011-10-19 出光興産株式会社 有機薄膜トランジスタ
JP2007510706A (ja) 2003-11-10 2007-04-26 メルク シャープ エンド ドーム リミテッド 痛みを治療するためのバニロイド−１受容体アンタゴニストとしての、置換された含窒素六員アミノ複素環
JP4521182B2 (ja) 2003-12-26 2010-08-11 富士フイルム株式会社 有機電界発光素子
WO2005071096A2 (en) 2004-01-21 2005-08-04 Molecular Probes, Inc. Derivatives of cephalosporin and clavulanic acid for detecting beta-lacamase in a sample
US7119214B2 (en) 2004-04-13 2006-10-10 Cephalon France Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
ES2241496B1 (es) 2004-04-15 2006-12-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridina.
WO2005103052A1 (en) 2004-04-21 2005-11-03 Pfizer Products Inc. Pyrazolo [1,5-a] pyrimidin-7-one compounds and uses thereof
BRPI0513717A (pt) 2004-07-23 2008-05-13 Pfizer derivados de piridina
CN101014572B (zh) 2004-09-15 2011-07-06 盐野义制药株式会社 具有hiv整合酶抑制活性的氨基甲酰基吡啶酮衍生物
GB0421911D0 (en) 2004-10-01 2004-11-03 Univ Cambridge Tech Methods and means
WO2006038041A1 (en) 2004-10-08 2006-04-13 Merck Sharp & Dohme Limited Besylate salts of six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
US8697674B2 (en) 2004-12-29 2014-04-15 Naturon, Inc. Xanthurenic acid derivative pharmaceutical compositions and methods related thereto
US20070135437A1 (en) 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
WO2006094604A1 (en) 2005-03-11 2006-09-14 Merck Patent Gmbh Tetrahydro- and dihydroquinazolinones
TW200700064A (en) 2005-03-24 2007-01-01 Glaxo Group Ltd Novel compounds
AR056347A1 (es) 2005-05-12 2007-10-03 Tibotec Pharm Ltd Uso de compuestos de pteridina para fabricar medicamentos y composiciones farmaceuticas
WO2006138418A2 (en) 2005-06-14 2006-12-28 President And Fellows Of Harvard College Improvement of cognitive performance with sirtuin activators
ATE474829T1 (de) 2005-06-27 2010-08-15 Amgen Inc Entzündungshemmende arylnitrilverbindungen
WO2007057782A2 (en) 2005-10-11 2007-05-24 Centre National De La Recherche Scientifique (Cnrs) 3 -hydroxyflavone derivatives for the detection and the quantification of cell apoptosis
US20090306102A1 (en) 2005-12-20 2009-12-10 Eriksen Birgitte L 2-pyridin-2-yl-quinazoline derivatives as potassium channel modulating agents for the treatment of respiratory diseases
WO2007079180A2 (en) 2005-12-29 2007-07-12 N.V. Organon Inhibitors of fatty acid amide hydrolase
US20070203236A1 (en) 2006-01-11 2007-08-30 Smith Jeffrey W Novel antagonists of the human fatty acid synthase thioesterase
WO2007095187A2 (en) 2006-02-13 2007-08-23 Trustees Of Boston University Compositions and methods for antibiotic potentiation and drug discovery
JP2007230145A (ja) 2006-03-02 2007-09-13 Mitsubishi Chemicals Corp 光学記録媒体の記録層形成用色素、及びそれを用いた光学記録媒体、その光学記録媒体の記録方法
SI2656841T1 (sl) 2006-03-27 2016-11-30 The Regents Of The University Of California Modulator androgenih receptorjev za zdravljanje raka prostate in bolezni, povezanih z androgenimi receptorji
US8841483B2 (en) 2006-04-11 2014-09-23 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of voltage-gated sodium channels
EP1849781A1 (en) 2006-04-28 2007-10-31 Laboratorios del Dr. Esteve S.A. Substituted 3-Amino-4-hydroxy pyrrolidines compounds, their preparation and use as medicaments
WO2008024139A2 (en) 2006-08-18 2008-02-28 N.V. Organon Inhibitors of fatty acid amide hydrolase
WO2008030120A1 (en) 2006-09-07 2008-03-13 Auckland Uniservices Limited A method for the fluorescent detection of nitroreductase activity using nitro-substituted aromatic compounds
US20080234355A1 (en) 2006-09-11 2008-09-25 Xiong Cai Dna methyl transferase inhibitors containing a zinc binding moiety
US20080161320A1 (en) 2006-09-11 2008-07-03 Xiong Cai Fused bicyclic pyrimidines as ptk inhibitors containing a zinc binding moiety
WO2008033743A1 (en) 2006-09-11 2008-03-20 Curis, Inc. Substituted 2-indolinone as ptk inhibitors containing a zinc binding moiety
EP2061468A4 (en) 2006-09-11 2011-05-04 Curis Inc TYROSINE KINASE INHIBITORS CONTAINING ZINC BINDING CHARACTERISTIC GROUP
US8604044B2 (en) 2006-09-11 2013-12-10 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
WO2008037607A1 (de) 2006-09-25 2008-04-03 Basf Se Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen
RU2009117642A (ru) 2006-10-12 2010-11-20 Ксенон Фармасьютикалз Инк. (Ca) Применение спирооксиндоловых соединений в качестве терапевтических средств
UA96964C2 (ru) 2006-12-04 2011-12-26 Астразенека Аб Соединения полициклической мочевины с антибактериальными свойствами
DE102006059710A1 (de) 2006-12-18 2008-06-19 Freie Universität Berlin Substituierte 4-Hydroxypyridine
CA2674118A1 (en) 2007-01-04 2008-07-10 Do-Coop Technologies Ltd. Detection of analytes
US20080176225A1 (en) 2007-01-18 2008-07-24 Steve Roffler Membrane bound reporter gene system
WO2008094507A2 (en) 2007-01-26 2008-08-07 Cellicon Biotechnologies, Inc. Novel fusion compounds
CN101641339B (zh) 2007-02-01 2013-07-17 雷斯韦洛吉克斯公司 用于预防和治疗心血管疾病的化合物
CA2680398A1 (en) 2007-03-20 2008-09-25 Curis, Inc. Raf kinase inhibitors containing a zinc binding moiety
WO2008115262A2 (en) 2007-03-20 2008-09-25 Curis, Inc. Hsp90 inhibitors containing a zinc binding moiety
GEP20125379B (en) 2007-05-03 2012-01-10 Pfizer Ltd 2 -pyridine carboxamide derivatives as sodium channel modulators
ES2637999T3 (es) 2007-05-17 2017-10-18 Helperby Therapeutics Limited Uso de compuestos de 4-(pirrolidin-1-il)quinolina para eliminar microorganismos clínicamente latentes
WO2009036066A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Vegfr inhibitors containing a zinc binding moiety
TW200920357A (en) 2007-09-10 2009-05-16 Curis Inc HSP90 inhibitors containing a zinc binding moiety
TW200922590A (en) 2007-09-10 2009-06-01 Curis Inc VEGFR inhibitors containing a zinc binding moiety
TW200922564A (en) 2007-09-10 2009-06-01 Curis Inc CDK inhibitors containing a zinc binding moiety
US8519137B2 (en) 2007-10-11 2013-08-27 Vertex Pharmaceuticals Incorporated Heteroaryl amides useful as inhibitors of voltage-gated sodium channels
EP2212292B1 (en) 2007-10-11 2012-12-05 Vertex Pharmaceuticals Incorporated Amides useful as inhibitors of voltage-gated sodium channels
MX2010003865A (es) 2007-10-11 2010-06-01 Vertex Pharma Aril amidas utiles como inhibidores de canales de sodio dependientes de voltaje.
WO2009086012A1 (en) 2007-12-20 2009-07-09 Curis, Inc. Aurora inhibitors containing a zinc binding moiety
PT2247558T (pt) 2008-02-14 2022-03-21 Lilly Co Eli Novos agentes de imagiologia para deteção de disfunção neurológica
JP5530599B2 (ja) 2008-02-28 2014-06-25 富士フイルム株式会社 フォトレジスト液、およびこれを用いるエッチング方法
WO2009114470A2 (en) 2008-03-10 2009-09-17 Curis, Inc. Tetrahydroindole and tetrahdyroindazole as hsp90 inhibitors containing a zinc binding moiety
JP2011518174A (ja) 2008-04-18 2011-06-23 シェノゲン ファーマ グループ リミテッド エストロゲン受容体に関連する疾患を処置するための化合物及び方法
KR20110031419A (ko) 2008-06-04 2011-03-28 아스트라제네카 아베 항박테리아제로서의 티아졸로［５,４­ｂ］피리딘 및 옥사졸로［５,４­ｂ］피리딘 유도체
US8822513B2 (en) 2010-03-01 2014-09-02 Gtx, Inc. Compounds for treatment of cancer
JP5507552B2 (ja) 2008-06-16 2014-05-28 ユニバーシティ オブ テネシー リサーチ ファウンデーション 癌を処置するための化合物
GB0815962D0 (en) 2008-09-02 2008-10-08 Merlion Pharmaceuticals Pte Ltd Hybrid antibacterial compounds and their use
ES2517690T3 (es) 2008-09-29 2014-11-03 Glaxosmithkline Llc Quinazolinona, quinolona y análogos relacionados como moduladores de sirtuina
TW201016676A (en) 2008-10-03 2010-05-01 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8491891B2 (en) 2008-11-26 2013-07-23 Academia Sinica Human beta-glucuronidase mutants with elevated enzymatic activity under physiological conditions and method for identifying such
JP2012512863A (ja) 2008-12-19 2012-06-07 ファイザー・インク モノカルバム
ES2620446T3 (es) 2008-12-26 2017-06-28 Sumitomo Dainippon Pharma Co., Ltd. Nuevo compuesto heterocíclico bicíclico
HRP20150947T1 (hr) 2009-01-08 2015-10-09 Curis, Inc. Inhibitori fosfoinositid 3-kinaze sa skupinom koja veže cink
JP6186125B2 (ja) 2009-05-07 2017-08-30 ザ ボード オブ トラスティーズ オブ ザ リーランド スタンフォード ジュニア ユニバーシティ 疼痛の研究、画像化および治療方法、ならびに疼痛の研究、画像化および治療のための組成物
EP2264035A1 (en) 2009-06-04 2010-12-22 Merz Pharma GmbH & Co. KGaA Glycine B antagonists
CN101906105B (zh) 2009-06-08 2013-01-16 河北医科大学 吡唑并[1，5-a]嘧啶酮衍生物及其药物组合物以及其用途
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
CA2771472A1 (en) 2009-09-04 2011-03-10 Zalicus Pharmaceuticals Ltd. Oxopiperazine derivatives for the treatment of pain and epilepsy
US20110124597A1 (en) 2009-09-25 2011-05-26 Anacor Pharmaceuticals, Inc. Boron containing small molecules
EP3421476A1 (en) 2009-10-16 2019-01-02 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
JP5879273B2 (ja) 2010-03-01 2016-03-08 ジーティーエックス・インコーポレイテッド 癌を処置するための化合物
AU2011239537A1 (en) 2010-04-16 2012-11-15 Curis, Inc. Treatment of cancers having K-ras mutations
HUE028983T2 (en) 2010-05-06 2017-01-30 Vertex Pharma Heterocyclic chromene-spirocyclic piperidine amides as ion channel modulators
JP2013541493A (ja) 2010-06-17 2013-11-14 フュジアンス バイオメディカルズ インコーポレイテッド 抗ウイルス剤として有用な化合物、組成物、及び使用の方法
US8889638B2 (en) 2010-06-22 2014-11-18 The Regents Of The University Of California Stimulus-triggered prodrugs
US8524740B2 (en) 2010-07-15 2013-09-03 Tairx, Inc. Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives
CN107648216B (zh) 2010-07-27 2021-03-30 波士顿大学管理委员会 作为新型癌症疗法的芳烃受体(AhR)调节剂
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
GB201017315D0 (en) 2010-10-13 2010-11-24 Antoxis Ltd Compound
GB201020076D0 (en) 2010-11-26 2011-01-12 Liverpool School Tropical Medicine Antimalarial compounds
DK2646436T3 (en) 2010-11-29 2015-06-29 Pfizer monobactams
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
TWI574687B (zh) 2011-01-03 2017-03-21 古利斯股份有限公司 具有鋅結合部份之刺蝟拮抗劑
RU2634900C2 (ru) 2011-02-02 2017-11-08 Вертекс Фармасьютикалз Инкорпорейтед Спироциклические пирролопиразин(пиперидин)амиды в качестве модуляторов ионных каналов
WO2012106534A2 (en) 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
US10385070B2 (en) 2011-02-18 2019-08-20 Vertex Pharmaceuticals Incorporated Chroman-spirocyclic piperidine amides as modulators of ion channels
EP2681200A4 (en) 2011-03-03 2015-05-27 Zalicus Pharmaceuticals Ltd INHIBITORS OF BENZIMIDAZOLE TYPE OF SODIUM CHANNEL
AU2012229187B2 (en) 2011-03-14 2016-11-10 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
CA2830065A1 (en) 2011-03-16 2012-09-20 Amgen Inc. Potent and selective inhibitors of nav1.3 and nav1.7
US10953012B2 (en) 2011-04-26 2021-03-23 Bioenergenix Llc Heterocyclic compounds for the inhibition of pask
EP2701512B1 (en) 2011-04-26 2017-04-05 Merck Sharp & Dohme Corp. Aldosterone synthase inhibitors
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
WO2012170371A1 (en) 2011-06-10 2012-12-13 N30 Pharmaceuticals, Llc Compounds as s-nitrosoglutathione reductase inhibitors
EP2736904B1 (en) 2011-07-27 2016-03-16 AB Science Oxazole and thiazole derivatives as selective protein kinase inhibitors (c-kit)
WO2013022740A2 (en) 2011-08-05 2013-02-14 Corning Incorporated Gpr35 ligands and the uses thereof
EP2760844B1 (fr) 2011-09-29 2018-11-21 Ecole Normale Superieure De Lyon Substrat de peptidase fluorogene
EP2760833A1 (en) 2011-09-30 2014-08-06 Endo Pharmaceuticals Inc. Pyridine derivatives
MD20140037A2 (ro) 2011-10-26 2014-08-31 Pfizer Limited Derivaţi de (4-fenilimidazol-2-il)etilamină utili ca modulatori ai canalului de sodiu
WO2013086229A1 (en) 2011-12-07 2013-06-13 Amgen Inc. Bicyclic aryl and heteroaryl sodium channel inhibitors
CN103159738B (zh) 2011-12-19 2016-09-07 上海泓博智源医药股份有限公司 炔基桥连的杂芳香化合物及其应用
EP3290413B9 (en) 2011-12-21 2020-04-29 ONO Pharmaceutical Co., Ltd. Pyridinone and pyrimidinone derivatives as factor xia inhibitors
MX2014008591A (es) 2012-01-16 2014-08-22 Vertex Pharma Piperidinamidas piranoespirociclicas como moduladores de canales de iones.
JP6002785B2 (ja) 2012-02-03 2016-10-05 ファイザー・インク ナトリウムチャネルモジュレーターとしてのベンゾイミダゾールおよびイミダゾピリジン誘導体
WO2013131018A1 (en) 2012-03-02 2013-09-06 Zalicus Pharmaceuticals Ltd. Biaryl inhibitors of the sodium channel
WO2013134518A1 (en) 2012-03-09 2013-09-12 Amgen Inc. Sulfamide sodium channel inhibitors
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20140005181A1 (en) 2012-06-21 2014-01-02 Sanford-Burnham Medical Research Institute Small molecule antagonists of the apelin receptor for the treatment of disease
TWI520962B (zh) 2012-06-29 2016-02-11 As the c-Met tyrosine kinase inhibitors novel fused pyridine derivatives
EP2877461B1 (en) 2012-07-27 2018-05-09 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
FR2994180B1 (fr) 2012-08-02 2014-08-22 Ecole Norm Superieure Lyon Substrat de glycosidase fluorogene et procede de detection associe
EP2885287B1 (en) 2012-08-20 2017-09-20 Syngenta Participations AG Pesticidally active pyridyl- and pyrimidyl- substituted pyrazole derivatives
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
WO2014066795A1 (en) 2012-10-25 2014-05-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
JP6482466B2 (ja) 2012-11-03 2019-03-13 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング サイトメガロウイルスの阻害剤
WO2014078479A2 (en) 2012-11-14 2014-05-22 The Board Of Regents Of The University Of Texas System INHIBITION OF HIF-2α HETERODIMERIZATION WITH HIF1β (ARNT)
US9802949B2 (en) 2012-11-29 2017-10-31 Sunshine Lake Pharma Co., Ltd. Fused ring compounds as hepatitis C virus inhibitors, pharmaceutical compositions and uses thereof
CN103848821B (zh) 2012-11-29 2016-10-12 广东东阳光药业有限公司 作为丙型肝炎抑制剂的螺环化合物、药物组合物及它们的用途
RU2015125570A (ru) 2013-01-08 2017-02-10 Савира Фармасьютикалз Гмбх Пиридоновые производные и их применение в лечении, уменьшении интенсивности симптомов или предотвращении вирусного заболевания
TWI659945B (zh) 2013-01-31 2019-05-21 維泰克斯製藥公司 作爲鈉通道調節劑之醯胺
KR102226587B1 (ko) 2013-01-31 2021-03-11 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 조절제로서의 퀴놀린 및 퀴나졸린 아미드
NZ710270A (en) 2013-01-31 2020-09-25 Vertex Pharma Pyridone amides as modulators of sodium channels
CA2897585C (en) 2013-02-20 2021-03-23 Basf Se Anthranilamide compounds, their mixtures and the use thereof as pesticides
MX2015011898A (es) 2013-03-13 2016-05-05 Genentech Inc Compuestos de pirazolo y usos de los mismos.
US20140323478A1 (en) 2013-04-30 2014-10-30 Afraxis Holdings, Inc. Serine/threonine kinase inhibitors
US20140323477A1 (en) 2013-04-30 2014-10-30 Genentech, Inc. Serine/threonine kinase inhibitors
US9212182B2 (en) 2013-06-12 2015-12-15 Amgen Inc. Bicyclic sulfonamide compounds as sodium channel inhibitors
MX364155B (es) 2013-07-19 2019-04-12 Vertex Pharma Sulfonamidas como moduladores de canales de sodio.
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
MX2016002178A (es) 2013-08-21 2016-06-06 Resverlogix Corp Composiciones y metodos terapeuticos para la regresion acelerada de placa.
EP3041470A4 (en) 2013-09-04 2017-05-03 Board Of Regents Of the University Of Texas System Methods and compositions for selective and targeted cancer therapy
WO2015035062A1 (en) 2013-09-05 2015-03-12 Genentech, Inc. Antiproliferative compounds
WO2015085238A1 (en) 2013-12-05 2015-06-11 The Regents Of The University Of California, A California Corporation Inhibitors of lpxc
DK3080134T3 (en) 2013-12-13 2018-10-22 Vertex Pharma PRODRUGS OF PYRIDONAMIDS USED AS MODULATORS OF SODIUM CHANNELS
CN104761524A (zh) 2014-01-07 2015-07-08 清华大学 一种化合物及其在制备抗寄生虫病药物中的应用
EP3138839B1 (en) 2014-02-14 2020-10-28 Sichuan Haisco Pharmaceutical Co., Ltd. Pyridone or pyrimidone derivative, preparation method therefor and application thereof
WO2015135094A1 (en) 2014-03-13 2015-09-17 Genentech, Inc. Therapeutic compounds and uses thereof
AU2015243437B2 (en) 2014-04-09 2019-08-29 Siteone Therapeutics, Inc. 10',11'-modified saxitoxins useful for the treatment of pain
FR3022784B1 (fr) 2014-06-26 2017-09-08 Ecole Normale Superieure Lyon Sondes moleculaires activables hydrosolubles, intermediaires pour leur synthese et procedes de detection associes
US9818959B2 (en) 2014-07-29 2017-11-14 Arizona Board of Regents on behlaf of Arizona State University Metal-assisted delayed fluorescent emitters containing tridentate ligands
JP2016079098A (ja) 2014-10-10 2016-05-16 塩野義製薬株式会社 セフェム化合物
ES2927307T3 (es) 2014-12-10 2022-11-04 Ono Pharmaceutical Co Derivado de dihidroindolizinona
CR20170392A (es) 2015-03-02 2018-02-20 Amgen Inc Compuestos bicíclicos de sulfonamida cetona
CN105936635B (zh) 2015-03-06 2019-06-21 南京圣和药业股份有限公司 作为磷脂酰肌醇3-激酶δ抑制剂的化合物及其应用
CN106008479B (zh) 2015-03-06 2020-01-10 南京圣和药业股份有限公司 作为磷脂酰肌醇3-激酶δ抑制剂的取代嘧啶类化合物及其应用
GB201507464D0 (en) 2015-04-30 2015-06-17 Syngenta Participations Ag Herbicidal compounds
GB201507463D0 (en) 2015-04-30 2015-06-17 Syngenta Participations Ag Herbicidal compounds
CN108349968A (zh) 2015-07-28 2018-07-31 维奥梅生物科学私人有限公司 抗菌治疗剂和预防剂
US10112953B2 (en) 2015-09-30 2018-10-30 Siteone Therapeutics, Inc. 11,13-modified saxitoxins for the treatment of pain
DE102015121035A1 (de) 2015-12-03 2017-06-08 Airbus Defence and Space GmbH Verfahren zur Detektion coliformer Keime
GB201522232D0 (en) 2015-12-16 2016-01-27 Liverpool School Tropical Medicine Combination product
CN106946775B (zh) 2016-01-07 2020-04-10 清华大学 一种化合物及其在制备抗丙肝病毒药物中的应用
US10889556B2 (en) 2016-03-08 2021-01-12 The Regents Of The University Of California Compositions and methods for inhibiting influenza RNA polymerase PA endonuclease
WO2017156194A1 (en) 2016-03-08 2017-09-14 The Regents Of The University Of California Compositions and methods for inhibiting influenza rna polymerase pa endonuclease
JP6992284B2 (ja) 2016-06-06 2022-01-13 小野薬品工業株式会社 ジヒドロインドリジノン誘導体を含有する医薬組成物
EP3260445A1 (en) 2016-06-24 2017-12-27 Universität Konstanz Compounds for use as an anti-bacterial or anti-fungal agent and as a zinc sensor
GB201612938D0 (en) 2016-07-26 2016-09-07 Almac Discovery Ltd Pharmaceutical compounds
CN107661333B (zh) 2016-07-27 2020-12-29 清华大学 化合物在治疗肺癌中的应用
HUE061016T2 (hu) 2016-08-19 2023-05-28 Univ Bristol Citizin-származékok a szenvedélybetegségek kezelésére
CN107773562B (zh) 2016-08-25 2020-04-07 清华大学 化合物在抗登革和寨卡病毒感染中的应用
EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
EP3309154A1 (en) 2016-10-13 2018-04-18 Universite De Geneve New compounds and uses thereof for detection of target molecules in a sample
FR3060567B1 (fr) 2016-12-19 2019-05-24 Ecole Normale Superieure De Lyon Substrat de glycosidase fluorogene et procede de detection associe
CN106810548B (zh) 2017-01-13 2019-02-15 苏州爱科百发生物医药技术有限公司 一种二氢异喹啉类化合物
WO2018161033A1 (en) 2017-03-02 2018-09-07 Wright, Adrian Small molecule ire1-alpha inhibitors
CN108623562A (zh) 2017-03-24 2018-10-09 中国海洋大学 一种喹啉酮生物碱类化合物及其制备方法和应用
CN108623588A (zh) 2017-03-24 2018-10-09 中国海洋大学 一种含内酰胺的四环衍生物及其制备方法和应用
CN108623587A (zh) 2017-03-24 2018-10-09 中国海洋大学 一种含羰基的胺类化合物及其制备方法和用途
JP7090100B2 (ja) 2017-03-29 2022-06-23 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１１，１３－修飾サキシトキシン：
JP2020515611A (ja) 2017-03-29 2020-05-28 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１１，１３−修飾サキシトキシン
JP2020100564A (ja) 2017-04-03 2020-07-02 京都薬品工業株式会社 リードスルー誘導剤およびその医薬用途
WO2018204765A1 (en) 2017-05-05 2018-11-08 Pairnomix, Llc Methods of treating epilepsy and kcnq2 related conditions
EP3625214B1 (en) 2017-05-16 2022-07-06 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
CN106977486B (zh) 2017-05-25 2019-09-24 南方科技大学 一种手性二氢黄酮类化合物及其衍生物的制备方法和应用
WO2018226976A1 (en) 2017-06-08 2018-12-13 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
BR112020000553A2 (pt) 2017-07-11 2020-07-21 Vertex Pharmaceuticals Incorporated carboxamidas como moduladores de canal de sódio
WO2019018119A1 (en) 2017-07-18 2019-01-24 Pairnomix, Llc METHODS FOR TREATING EPILEPSY AND DISORDERS ASSOCIATED WITH KCNTI
CN107365326B (zh) 2017-07-24 2019-08-20 湖北大学 一种用于检测活细胞内氟离子的荧光探针及其制备方法
CA3108484A1 (en) 2017-08-04 2019-02-07 Anthony Stewart Campbell Inhibitors of microbially induced amyloid
EP3502095A1 (en) 2017-12-22 2019-06-26 Universität Konstanz Compound for use against pathogenic neisseria and haemophilus species and moraxella catarrhalis
CN111315744B (zh) 2018-01-09 2023-07-14 四川科伦博泰生物医药股份有限公司 杂芳基并四氢吡啶类化合物、其制备方法、药物组合物及应用
US20190343817A1 (en) 2018-02-12 2019-11-14 Vertex Pharmaceuticals Incorporated Method of treating pain
CN108329366A (zh) 2018-03-07 2018-07-27 南京工业大学 一种用于检测β-半乳糖苷酶的荧光探针化合物及其制备方法
WO2019213006A1 (en) 2018-05-01 2019-11-07 Amgen Inc. Substituted pyrimidinones as agonists of the apj receptor
TWI815887B (zh) 2018-05-15 2023-09-21 美商愛彼特生物製藥股份有限公司 經取代的2,2'-雙嘧啶基化合物、其類似物及其使用方法
EP3802544A1 (en) 2018-06-05 2021-04-14 RAPT Therapeutics, Inc. Pyrazolo-pyrimidin-amino-cycloalkyl compounds and their therapeutic uses
WO2019238057A1 (zh) 2018-06-13 2019-12-19 中国科学院上海有机化学研究所 Fso 2n 3在制备叠氮化合物中的应用
TWI812739B (zh) 2018-06-21 2023-08-21 景凱生物科技股份有限公司 Nadph氧化酶抑制劑、含其的醫藥組合物、及其應用
WO2020003219A1 (en) 2018-06-29 2020-01-02 Oat & Iil India Laboratories Private Limited Substituted pyrazole derivatives as insecticides and fungicides
EP3820860B1 (en) 2018-07-09 2025-10-15 Lieber Institute, Inc. Pyridazine compounds for inhibiting nav1.8
CA3105657A1 (en) 2018-07-09 2020-01-16 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting nav1.8
KR20210066820A (ko) 2018-08-27 2021-06-07 베이징 위에즈캉타이 바이오메디슨스 컴퍼니, 리미티드 다중-치환된 피리돈 유도체 및 이의 의학적 용도
CN113260609A (zh) 2018-09-04 2021-08-13 美真达治疗公司 芳烃受体拮抗剂及其使用方法
US12162886B2 (en) 2018-10-03 2024-12-10 Siteone Therapeutics, Inc. 11,13-modified saxitoxins for the treatment of pain
CN113454080B (zh) 2018-10-30 2025-10-28 修复治疗公司 化合物、药物组合物和制备化合物的方法以及其使用方法
WO2020092187A1 (en) 2018-11-02 2020-05-07 Merck Sharp & Dohme Corp. 2-amino-n-phenyl-nicotinamides as nav1.8 inhibitors
KR102860523B1 (ko) 2018-11-02 2025-09-16 머크 샤프 앤드 돔 엘엘씨 Nav1.8 억제제로서의 2-아미노-n-헤테로아릴-니코틴아미드
CN111153899B (zh) 2018-11-08 2023-12-01 四川科伦博泰生物医药股份有限公司 一种取代吡啶化合物、其制备方法和用途
WO2020094156A1 (zh) 2018-11-11 2020-05-14 上海海雁医药科技有限公司 双杂环取代的吡啶-2(1h)-酮衍生物、其制法与医药上的用途
WO2020113373A1 (en) 2018-12-03 2020-06-11 Zhuhai Qiwei Bio-Technology Ltd. Method of treating age-related macular degeneration
US12246008B2 (en) 2018-12-05 2025-03-11 Merck Sharp & Dohme Llc 4-amino or 4-alkoxy-substituted aryl sulfonamide compounds with selective activity in voltage-gated sodium channels
WO2020118036A1 (en) 2018-12-06 2020-06-11 The Children's Medical Center Corporation Antibacterial compounds and uses thereof
AU2020205139A1 (en) 2019-01-04 2021-08-19 Jiangsu Hengrui Medicine Co., Ltd. 6-oxo-1,6-dihydropyridazine derivative, preparation method therefor and medical use thereof
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
PE20211733A1 (es) 2019-01-11 2021-09-06 Gruenenthal Chemie Amidas de pirrolidina sustituidas
TWI845600B (zh) 2019-01-24 2024-06-21 美商普羅米修斯生物科學股份有限公司 Gpr35調節劑
CN112996774B (zh) 2019-01-25 2022-11-22 江苏恒瑞医药股份有限公司 2-氧代-1,2-二氢吡啶类衍生物、其制备方法及其在医药上的应用
CN111848731B (zh) 2019-04-19 2022-11-29 国家纳米科学中心 一种原位自组装的抗菌分子及其制备方法和应用
CN110498784B (zh) 2019-05-20 2022-06-14 广东克冠达医药科技有限公司 一类川陈皮素衍生物或其药学上可接受的盐及其制备方法和应用
US20230103791A1 (en) 2019-06-27 2023-04-06 Glaxosmithkline Intellectual Property Development Limited 2,3-dihydroquinazolin compounds as nav1.8 inhibitors
EP3999512B1 (en) 2019-07-18 2023-08-23 Bristol-Myers Squibb Company Pyrazolo[3,4-d]pyrrolo[1,2-b]pyridazinyl compounds useful as irak4 inhibitors
CN112300051A (zh) 2019-07-31 2021-02-02 明慧医药（上海）有限公司 一种选择性钠通道调节剂及其制备和应用
CN112300069A (zh) 2019-07-31 2021-02-02 明慧医药（上海）有限公司 一种选择性钠通道调节剂及其制备和应用
WO2021032074A1 (zh) 2019-08-19 2021-02-25 江苏恒瑞医药股份有限公司 苯甲酰胺稠芳环类衍生物、其制备方法及其在医药上的应用
CN112390745B (zh) 2019-08-19 2022-10-21 江苏恒瑞医药股份有限公司 吡啶烟酰胺类衍生物、其制备方法及其在医药上的应用
CN112409331B (zh) 2019-08-21 2024-02-20 上海翰森生物医药科技有限公司 杂环类衍生物抑制剂、其制备方法和应用
CN112441969A (zh) 2019-08-30 2021-03-05 明慧医药（上海）有限公司 一种选择性钠通道调节剂及其制备和应用
CN112479996B (zh) 2019-09-12 2023-05-26 上海济煜医药科技有限公司 吡啶氮氧化合物及其制备方法和用途
CN112812014B (zh) 2019-11-15 2024-05-10 石家庄诚志永华显示材料有限公司 化合物、液晶组合物、液晶显示器
BR112022010382A2 (pt) 2019-11-29 2022-08-16 Molsid Substrato de beta-lactamase fluorogênica e método de detecção associado
AU2020397059A1 (en) 2019-12-06 2022-07-21 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
EP4077690A4 (en) 2019-12-20 2024-04-10 Engine Biosciences Pte. Ltd. METHODS AND COMPOSITIONS FOR TREATING CANCER
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
CN111217776A (zh) 2020-01-19 2020-06-02 中国人民解放军军事科学院军事医学研究院 含苯并杂环结构的酰胺衍生物、组合物和应用
US20230128972A1 (en) 2020-01-31 2023-04-27 Atomwise Inc. Anat Inhibitors and Methods of Use Thereof
CA3183948A1 (en) 2020-06-10 2021-12-16 Amgen Inc. Heteroalkyl dihydroquinoline sulfonamide compounds
JP2021195367A (ja) 2020-06-10 2021-12-27 アムジエン・インコーポレーテツド シクロプロピルジヒドロキノリンスルホンアミド化合物
JP7739051B2 (ja) 2020-06-10 2025-09-16 アムジエン・インコーポレーテツド シクロブチルジヒドロキノリンスルホンアミド化合物
US12516046B2 (en) 2020-06-17 2026-01-06 Merck Sharp & Dohme Llc 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors
BR112022024476A2 (pt) 2020-06-17 2022-12-27 Merck Sharp & Dohme Llc 5-oxopirrolidino-3-carboxamidas como inibidores de nav1.8
CR20220642A (es) 2020-06-17 2023-02-15 Merck Sharp & Dohme Llc 2-oxoimidazolidin-4-carboxamidas como inhibidores de nav1.8
BR112023002659A2 (pt) 2020-08-14 2023-05-02 Siteone Therapeutics Inc Inibidores de cetona não hidratados de nav1.7 para o tratamento da dor
CN111808019B (zh) 2020-09-08 2020-11-27 上海济煜医药科技有限公司 一种并环化合物及其应用
CN112047880B (zh) 2020-10-15 2022-11-01 天津科技大学 一类氮杂黄酮衍生物及其作为抗肿瘤药物的应用
CN114591293A (zh) 2020-12-07 2022-06-07 成都康弘药业集团股份有限公司 作为Nav1.8抑制剂的并环化合物及其用途
CN112225695B (zh) 2020-12-15 2021-03-02 上海济煜医药科技有限公司 一种氮氧化合物及其制备方法和用途
CN112778288B (zh) 2021-01-22 2022-08-09 湖南大学 一种近红外固态发光的荧光探针及其制备方法与应用
CN112457294B (zh) 2021-01-27 2021-06-04 上海济煜医药科技有限公司 一种作为NaV1.8阻滞剂的化合物及其制备方法和用途
CA3217565A1 (en) 2021-05-07 2022-11-10 Ashok Arasappan Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors
WO2022235558A1 (en) 2021-05-07 2022-11-10 Merck Sharp & Dohme Llc Aryl 3-oxopiperazine carboxamides and heteroaryl 3-oxopiperazine carboxamides as nav1.8 inhibitors
CN113200926B (zh) 2021-05-10 2022-09-23 四川大学 一种修饰2-芳基喹唑啉-4(3h)-酮类化合物的方法
CN117794920A (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)四氢呋喃甲酰胺作为钠通道调节剂
US20240368135A1 (en) 2021-06-04 2024-11-07 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
US20240400544A1 (en) 2021-06-04 2024-12-05 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
AU2022286511A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
IL308954A (en) 2021-06-04 2024-01-01 Vertex Pharma 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
TW202317520A (zh) 2021-06-15 2023-05-01 德商歌林達有限公司 經取代之吡唑醯胺
CN113754594B (zh) 2021-09-16 2025-01-21 中国药科大学 喹唑啉酮类化合物或其可药用的盐、异构体及其制备方法、药物组合物和用途
EP4511116A1 (en) 2022-04-22 2025-02-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CN119522214A (zh) * 2022-04-22 2025-02-25 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

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