AU2019239955B2 - Kv7 channel activators compositions and methods of use - Google Patents

Kv7 channel activators compositions and methods of use Download PDF

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Publication number
AU2019239955B2
AU2019239955B2 AU2019239955A AU2019239955A AU2019239955B2 AU 2019239955 B2 AU2019239955 B2 AU 2019239955B2 AU 2019239955 A AU2019239955 A AU 2019239955A AU 2019239955 A AU2019239955 A AU 2019239955A AU 2019239955 B2 AU2019239955 B2 AU 2019239955B2
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isomers
disorder
stereoisomer
formula
alkyl
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AU2019239955A1 (en
Inventor
Justin K. Belardi
Michael E. Bozik
Charles A. Flentge
James S. Hale
Scott S. Harried
David A. Mareska
Lynn Resnick
George T. Topalov
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Biohaven Therapeutics Ltd
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Biohaven Therapeutics Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C07D235/32—Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
    • 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
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • 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
    • C07D401/02—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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
AU2019239955A 2018-03-19 2019-03-19 Kv7 channel activators compositions and methods of use Active AU2019239955B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2023266373A AU2023266373B2 (en) 2018-03-19 2023-11-17 Kv7 channel activators compositions and methods of use
AU2024202496A AU2024202496A1 (en) 2018-03-19 2024-04-17 Kv7 channel activators compositions and methods of use

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201862644932P 2018-03-19 2018-03-19
US201862644902P 2018-03-19 2018-03-19
US62/644,902 2018-03-19
US62/644,932 2018-03-19
US201862663438P 2018-04-27 2018-04-27
US62/663,438 2018-04-27
US201862697198P 2018-07-12 2018-07-12
US62/697,198 2018-07-12
PCT/US2019/023039 WO2019183148A1 (en) 2018-03-19 2019-03-19 Kv7 channel activators compositions and methods of use

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AU2019239955A1 AU2019239955A1 (en) 2020-10-01
AU2019239955B2 true AU2019239955B2 (en) 2023-08-24

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US (5) US10851067B2 (enExample)
EP (1) EP3768677A4 (enExample)
JP (2) JP7757036B2 (enExample)
KR (3) KR102868652B1 (enExample)
CN (6) CN118955402A (enExample)
AU (3) AU2019239955B2 (enExample)
BR (1) BR112020018933A2 (enExample)
CA (1) CA3093976A1 (enExample)
IL (2) IL277419B2 (enExample)
MX (2) MX2020009693A (enExample)
SG (1) SG11202008030WA (enExample)
WO (1) WO2019183148A1 (enExample)
ZA (1) ZA202308070B (enExample)

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SMT202300362T1 (it) * 2014-09-12 2023-11-13 Biohaven Therapeutics Ltd Benzoimidazol-1,2-il-ammidi come attivatori di canale kv7
SG11202008030WA (en) * 2018-03-19 2020-10-29 Knopp Biosciences Llc Kv7 channel activators compositions and methods of use
BR112022004847A2 (pt) * 2019-09-17 2022-06-07 Knopp Biosciences Llc Método para tratar uma doença ou distúrbio de neurodesenvolvimento
CN120435316A (zh) * 2022-08-30 2025-08-05 拜奥海芬治疗学有限公司 包括金属通道激活剂和nmda受体拮抗剂的组合疗法
EP4584250A4 (en) * 2022-09-06 2026-02-25 Biohaven Therapeutics Ltd POLYTHERAPIES INCLUDING METAL CHANNEL ACTIVATORS
WO2025035066A1 (en) * 2023-08-10 2025-02-13 Biohaven Therapeutics Ltd. Extended-release formulations of kv7.2/7.3 potassium channel activators
AU2024340894A1 (en) * 2023-09-15 2026-04-02 Biohaven Therapeutics Ltd. Methods of treating epilepsy and related disorders with potent and selective potassium channel activators
WO2025103406A1 (zh) * 2023-11-15 2025-05-22 南京明德新药研发有限公司 6并5杂芳基衍生物及其应用
WO2025137661A1 (en) * 2023-12-22 2025-06-26 Biohaven Therapeutics Ltd. Combination treatment of neurological disorders
WO2025198930A1 (en) * 2024-03-18 2025-09-25 Humanwell Pharmacuetical Us, Inc. Small molecules as kcnq2/3 (kv7.2/3) channel activators and their medical use thereof
WO2026042005A1 (en) 2024-08-18 2026-02-26 Biohaven Therapeutics Ltd. Prodrugs of benzimidazol-1,2-yl amide compounds

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MX2020009693A (es) 2021-01-08
CN119118926A (zh) 2024-12-13
JP7757036B2 (ja) 2025-10-21
CN118955403A (zh) 2024-11-15
US20190284142A1 (en) 2019-09-19
US11724990B2 (en) 2023-08-15
US10851067B2 (en) 2020-12-01
KR102868652B1 (ko) 2025-10-13
JP2021518844A (ja) 2021-08-05
KR20240163771A (ko) 2024-11-19
KR102731128B1 (ko) 2024-11-18
CN112771039A (zh) 2021-05-07
US20260062389A1 (en) 2026-03-05
IL277419B1 (en) 2024-03-01
WO2019183148A1 (en) 2019-09-26
IL277419A (en) 2020-11-30
EP3768677A4 (en) 2021-12-22
ZA202308070B (en) 2025-04-30
US20210130299A1 (en) 2021-05-06
AU2024202496A1 (en) 2024-05-09
NZ767228A (en) 2023-11-24
AU2023266373A1 (en) 2023-12-07
CA3093976A1 (en) 2019-09-26
EP3768677A1 (en) 2021-01-27
MX2023001153A (es) 2023-02-22
IL310136A (en) 2024-03-01
CN118955401A (zh) 2024-11-15
CN118955400A (zh) 2024-11-15
JP2024026104A (ja) 2024-02-28
SG11202008030WA (en) 2020-10-29
US12286408B2 (en) 2025-04-29
BR112020018933A2 (pt) 2020-12-29
KR20200133259A (ko) 2020-11-26
CN118955402A (zh) 2024-11-15
AU2023266373B2 (en) 2024-02-08
AU2019239955A1 (en) 2020-10-01
KR20250150168A (ko) 2025-10-17
US20230000831A1 (en) 2023-01-05
IL277419B2 (en) 2024-07-01
US11261162B2 (en) 2022-03-01
US20240002349A1 (en) 2024-01-04

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