CA3076457C - Azabicyclo and diazepine derivatives for treating ocular disorders - Google Patents

Azabicyclo and diazepine derivatives for treating ocular disorders Download PDF

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Publication number
CA3076457C
CA3076457C CA3076457A CA3076457A CA3076457C CA 3076457 C CA3076457 C CA 3076457C CA 3076457 A CA3076457 A CA 3076457A CA 3076457 A CA3076457 A CA 3076457A CA 3076457 C CA3076457 C CA 3076457C
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CA
Canada
Prior art keywords
pharmaceutically acceptable
compound
composition
acceptable salt
branched
Prior art date
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Active
Application number
CA3076457A
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English (en)
French (fr)
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CA3076457A1 (en
Inventor
David Ellis
Howard Allen Ketelson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Alcon Inc
Original Assignee
Alcon Inc
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Publication date
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Priority to CA3205816A priority Critical patent/CA3205816A1/en
Publication of CA3076457A1 publication Critical patent/CA3076457A1/en
Application granted granted Critical
Publication of CA3076457C publication Critical patent/CA3076457C/en
Active legal-status Critical Current
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Classifications

    • 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms
    • C07D451/10Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/10Ophthalmic agents for accommodation disorders, e.g. myopia
    • 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/38[b, e]- or [b, f]-condensed with six-membered rings
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3076457A 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders Active CA3076457C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA3205816A CA3205816A1 (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762581073P 2017-11-03 2017-11-03
US62/581,073 2017-11-03
US201862749610P 2018-10-23 2018-10-23
US62/749,610 2018-10-23
PCT/IB2018/058631 WO2019087146A1 (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA3205816A Division CA3205816A1 (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Publications (2)

Publication Number Publication Date
CA3076457A1 CA3076457A1 (en) 2019-05-09
CA3076457C true CA3076457C (en) 2023-09-19

Family

ID=64267873

Family Applications (2)

Application Number Title Priority Date Filing Date
CA3076457A Active CA3076457C (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders
CA3205816A Pending CA3205816A1 (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA3205816A Pending CA3205816A1 (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Country Status (13)

Country Link
US (3) US11306090B2 (https=)
EP (1) EP3704117B1 (https=)
JP (3) JP7065180B2 (https=)
KR (1) KR20200083976A (https=)
CN (1) CN111247147B (https=)
AU (3) AU2018362010B2 (https=)
BR (1) BR112020007744A2 (https=)
CA (2) CA3076457C (https=)
ES (1) ES3064457T3 (https=)
MX (2) MX2020004580A (https=)
SG (1) SG11202002692XA (https=)
TW (2) TWI826399B (https=)
WO (2) WO2019087149A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3128224A1 (en) * 2019-02-01 2020-08-06 Aerie Pharmaceuticals, Inc. Compounds, compositions and methods for treatment of myopia
US12527739B2 (en) 2022-09-11 2026-01-20 Alcon Inc. Aqueous pharmaceutical compositions comprising benzyl atropine and uses thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1165037B (de) * 1961-11-21 1964-03-12 Dr. Schwarz Arzneimittelfabrik G.m.b.H., Monheim (RhId.) Verfahren zur Herstellung von Estern quaternärer Atropiniumsalze.
GB994493A (en) * 1963-02-06 1965-06-10 Lepetit Spa Tropine derivative
DE1670177A1 (de) 1966-12-28 1970-11-12 Boehringer Sohn Ingelheim Verfahren zur Herstellung von neuen N-substituierten Noratropiniumsalzen
US5223528A (en) 1986-03-17 1993-06-29 University Of Florida Anticholinergic compounds, composititons and methods of treatment
EP1397132A4 (en) * 2001-05-25 2006-12-13 Valley Forge Pharmaceuticals I OPHTHALMIC PIRENZEPINE GEL
FR2834511B1 (fr) 2002-01-07 2004-02-13 Sanofi Synthelabo Derives de 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, leur preparation et leur application en therapeutique
CN1546490A (zh) 2003-12-15 2004-11-17 常俊标 不对称双羟基托品类生物碱及其合成新方法和药物用途
CN1283639C (zh) 2004-06-08 2006-11-08 吴建梅 治疗近视眼的哌仑西平有机酸盐及其滴眼剂
US20070254914A1 (en) * 2006-05-01 2007-11-01 Non-Profit Organization Chang Gung Memorial Hospital Low-concentration atropine solution for preventing myopia progression and preparing method thereof
SI2657234T1 (sl) 2010-12-22 2017-06-30 Meiji Seika Pharma Co., Ltd. Derivat optično-aktivnega diazabiciklooktana in metoda za njegovo izdelavo

Also Published As

Publication number Publication date
MX2020004580A (es) 2020-12-03
JP2020536922A (ja) 2020-12-17
CN111247147A (zh) 2020-06-05
RU2020117733A (ru) 2021-12-03
AU2018362010A1 (en) 2020-04-09
TWI826399B (zh) 2023-12-21
SG11202002692XA (en) 2020-05-28
KR20200083976A (ko) 2020-07-09
US20210179616A1 (en) 2021-06-17
CA3205816A1 (en) 2019-05-09
AU2021205100A1 (en) 2021-08-12
EP3704117A1 (en) 2020-09-09
JP2024041971A (ja) 2024-03-27
AU2018362010B2 (en) 2021-05-13
US20220267328A1 (en) 2022-08-25
WO2019087149A1 (en) 2019-05-09
TW202417440A (zh) 2024-05-01
US11884666B2 (en) 2024-01-30
AU2023202036A1 (en) 2023-05-04
AU2023202036B2 (en) 2024-08-08
AU2021205100B2 (en) 2023-01-05
MX2022011310A (es) 2022-10-07
TWI852865B (zh) 2024-08-11
US12247028B2 (en) 2025-03-11
CA3076457A1 (en) 2019-05-09
US11306090B2 (en) 2022-04-19
JP7065180B2 (ja) 2022-05-11
JP2022101654A (ja) 2022-07-06
EP3704117B1 (en) 2026-01-28
US20240132497A1 (en) 2024-04-25
TW201922731A (zh) 2019-06-16
JP7777613B2 (ja) 2025-11-28
WO2019087146A1 (en) 2019-05-09
BR112020007744A2 (pt) 2020-10-13
CN111247147B (zh) 2026-02-24
ES3064457T3 (en) 2026-04-24

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