CA3205816A1 - Azabicyclo and diazepine derivatives for treating ocular disorders - Google Patents

Azabicyclo and diazepine derivatives for treating ocular disorders

Info

Publication number
CA3205816A1
CA3205816A1 CA3205816A CA3205816A CA3205816A1 CA 3205816 A1 CA3205816 A1 CA 3205816A1 CA 3205816 A CA3205816 A CA 3205816A CA 3205816 A CA3205816 A CA 3205816A CA 3205816 A1 CA3205816 A1 CA 3205816A1
Authority
CA
Canada
Prior art keywords
mmol
methyl
nmr
azabicyclo
vacuo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3205816A
Other languages
English (en)
French (fr)
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Alcon Inc filed Critical Alcon Inc
Publication of CA3205816A1 publication Critical patent/CA3205816A1/en
Pending legal-status Critical Current

Links

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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (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)
CA3205816A 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders Pending CA3205816A1 (en)

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
CA3076457A CA3076457C (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Related Parent Applications (1)

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

Publications (1)

Publication Number Publication Date
CA3205816A1 true CA3205816A1 (en) 2019-05-09

Family

ID=64267873

Family Applications (2)

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
CA3076457A Active CA3076457C (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
CA3076457A Active CA3076457C (en) 2017-11-03 2018-11-02 Azabicyclo and diazepine derivatives for treating ocular disorders

Country Status (12)

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) CA3205816A1 (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
JP7665519B2 (ja) * 2019-02-01 2025-04-21 アルコン インコーポレイティド 近視を治療するための化合物、組成物及び医薬組成物
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
IL158904A0 (en) 2001-05-25 2004-05-12 Valley Forge Pharmaceuticals Pirenzepine ophthalmic 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
PL2657234T3 (pl) 2010-12-22 2017-06-30 Meiji Seika Pharma Co., Ltd. Optycznie czynna pochodna diazabicyklooktanowa i sposób jej wytwarzania

Also Published As

Publication number Publication date
JP2022101654A (ja) 2022-07-06
TWI826399B (zh) 2023-12-21
JP7065180B2 (ja) 2022-05-11
WO2019087146A1 (en) 2019-05-09
US11884666B2 (en) 2024-01-30
US12247028B2 (en) 2025-03-11
AU2018362010A1 (en) 2020-04-09
EP3704117B1 (en) 2026-01-28
AU2021205100B2 (en) 2023-01-05
JP7777613B2 (ja) 2025-11-28
RU2020117733A (ru) 2021-12-03
AU2023202036B2 (en) 2024-08-08
JP2020536922A (ja) 2020-12-17
TWI852865B (zh) 2024-08-11
CN111247147B (zh) 2026-02-24
AU2021205100A1 (en) 2021-08-12
AU2018362010B2 (en) 2021-05-13
WO2019087149A1 (en) 2019-05-09
CA3076457A1 (en) 2019-05-09
TW202417440A (zh) 2024-05-01
TW201922731A (zh) 2019-06-16
MX2022011310A (es) 2022-10-07
JP2024041971A (ja) 2024-03-27
US11306090B2 (en) 2022-04-19
CN111247147A (zh) 2020-06-05
US20240132497A1 (en) 2024-04-25
US20220267328A1 (en) 2022-08-25
SG11202002692XA (en) 2020-05-28
EP3704117A1 (en) 2020-09-09
KR20200083976A (ko) 2020-07-09
AU2023202036A1 (en) 2023-05-04
US20210179616A1 (en) 2021-06-17
CA3076457C (en) 2023-09-19
BR112020007744A2 (pt) 2020-10-13
MX2020004580A (es) 2020-12-03

Similar Documents

Publication Publication Date Title
US20250129057A1 (en) Solid Forms of 2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid, 1,3-Dihydroxy-2-(hydroxymethyl)propan-2-amine Salt
JP7777613B2 (ja) 眼疾患を治療するためのアザビシクロ及びジアゼピン誘導体
US20240383920A1 (en) Synthesis of ras inhibitors
US20240368190A1 (en) Synthesis of ras inhibitors
US11766443B2 (en) Cyclopentathiophene carboxamide derivatives as platelet activating factor receptor antagonists
RU2795521C2 (ru) Азабициклические и диазепиновые производные для лечения офтальмологических нарушений
US11992494B2 (en) Cyclopentathiophene carboxamide derivatives as platelet activating factor receptor antagonists
WO2024040009A2 (en) Inhibitors of methionine aminopeptidase-2 and methods of preparation and uses thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20230706

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20240829

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 6TH ANNIV.) - STANDARD

Year of fee payment: 6

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241029

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20241029

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20241029

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20241104

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20250203

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20250527

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20250527

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20250822

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 7TH ANNIV.) - STANDARD

Year of fee payment: 7

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20251023

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20251023

B12 Application deemed to be withdrawn, abandoned or lapsed

Free format text: ST27 STATUS EVENT CODE: N-2-6-B10-B12-B303 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: DEEMED ABANDONED - FAILURE TO RESPOND TO AN EXAMINER'S REQUISITION

Effective date: 20251222