CA3093976A1 - 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
CA3093976A1
CA3093976A1 CA3093976A CA3093976A CA3093976A1 CA 3093976 A1 CA3093976 A1 CA 3093976A1 CA 3093976 A CA3093976 A CA 3093976A CA 3093976 A CA3093976 A CA 3093976A CA 3093976 A1 CA3093976 A1 CA 3093976A1
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Prior art keywords
stereoisomer
disorder
compound
benzo
neonatal
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Pending
Application number
CA3093976A
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English (en)
French (fr)
Inventor
Michael E. Bozik
Scott S. Harried
Lynn Resnick
George T. Topalov
Justin K. Belardi
Charles A. Flentge
David A. Mareska
James S. Hale
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Biohaven Therapeutics Ltd
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Knopp Biosciences LLC
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Publication of CA3093976A1 publication Critical patent/CA3093976A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; 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
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • C07D235/32Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; 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
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D405/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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)
CA3093976A 2018-03-19 2019-03-19 Kv7 channel activators compositions and methods of use Pending CA3093976A1 (en)

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

Publications (1)

Publication Number Publication Date
CA3093976A1 true CA3093976A1 (en) 2019-09-26

Family

ID=67905138

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3093976A Pending CA3093976A1 (en) 2018-03-19 2019-03-19 Kv7 channel activators compositions and methods of use

Country Status (13)

Country Link
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)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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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JPH0772181B2 (ja) 1989-06-26 1995-08-02 株式会社大塚製薬工場 ベンズイミダゾール誘導体
JPH0772181A (ja) 1993-09-03 1995-03-17 Advantest Corp 電位波形測定方法および装置
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US6855714B2 (en) 2001-07-06 2005-02-15 Schering Aktiengesellschaft 1-alkyl-2-aryl-benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
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CA2607219A1 (en) * 2005-05-18 2007-02-15 Neuraxon, Inc. Substituted benzimidazole compounds with dual nos inhibitory activity and mu opioid agonist activity
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CN101778833A (zh) 2007-08-10 2010-07-14 日本曹达株式会社 含氮杂环化合物和有害生物防除剂
ES2539714T3 (es) 2007-11-22 2015-07-03 Zenyaku Kogyo Kabushikikaisha Dispersiones sólidas que comprenden un cuerpo amorfo compuesto por un compuesto antitumoral heterocíclico
GB0723794D0 (en) 2007-12-05 2008-01-16 Lectus Therapeutics Ltd Potassium ion channel modulators and uses thereof
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WO2010051819A1 (en) 2008-11-10 2010-05-14 Neurosearch A/S Novel 2,3-diamino-quinazolinone derivatives and their medical use
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AU2011275393B2 (en) 2010-07-08 2014-04-10 Pfizer Inc. Piperidinyl pyrimidine amides as Kv7 potassium channel openers
SG10201505997TA (en) 2010-08-05 2015-09-29 Amgen Inc Benzimidazole And Azabenzimidazole Compounds That Inhibit Anaplastic Lymphoma Kinase
WO2014145852A2 (en) * 2013-03-15 2014-09-18 Knopp Biosciences Llc Imidazo(4,5-b) pyridin-2-yl amides as kv7 channel activators
US10471139B2 (en) 2013-08-15 2019-11-12 The University Of Kansas Toll-like receptor agonists
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

Also Published As

Publication number Publication date
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
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
AU2019239955B2 (en) 2023-08-24
IL277419B2 (en) 2024-07-01
US11261162B2 (en) 2022-03-01
US20240002349A1 (en) 2024-01-04

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