CN111247147B - 用于治疗眼部病症的氮杂双环和二氮杂环庚三烯衍生物 - Google Patents
用于治疗眼部病症的氮杂双环和二氮杂环庚三烯衍生物Info
- Publication number
- CN111247147B CN111247147B CN201880068606.5A CN201880068606A CN111247147B CN 111247147 B CN111247147 B CN 111247147B CN 201880068606 A CN201880068606 A CN 201880068606A CN 111247147 B CN111247147 B CN 111247147B
- Authority
- CN
- China
- Prior art keywords
- methyl
- mmol
- azabicyclo
- oct
- nmr
- 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.)
- Active
Links
Classifications
-
- 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
- C07D471/08—Bridged 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- 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
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic 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
-
- 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
- C07D451/00—Heterocyclic 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
- C07D451/02—Heterocyclic 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
- C07D451/04—Heterocyclic 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
- C07D451/06—Oxygen atoms
- C07D451/10—Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
-
- 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
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)
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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111247147A CN111247147A (zh) | 2020-06-05 |
| CN111247147B true CN111247147B (zh) | 2026-02-24 |
Family
ID=64267873
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880068606.5A Active CN111247147B (zh) | 2017-11-03 | 2018-11-02 | 用于治疗眼部病症的氮杂双环和二氮杂环庚三烯衍生物 |
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)
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5223528A (en) * | 1986-03-17 | 1993-06-29 | University Of Florida | Anticholinergic compounds, composititons and methods of treatment |
| 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 |
Family Cites Families (8)
| 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 |
| 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 |
| PL2657234T3 (pl) | 2010-12-22 | 2017-06-30 | Meiji Seika Pharma Co., Ltd. | Optycznie czynna pochodna diazabicyklooktanowa i sposób jej wytwarzania |
-
2018
- 2018-11-02 CA CA3205816A patent/CA3205816A1/en active Pending
- 2018-11-02 MX MX2020004580A patent/MX2020004580A/es unknown
- 2018-11-02 US US16/760,192 patent/US11306090B2/en active Active
- 2018-11-02 KR KR1020207010292A patent/KR20200083976A/ko active Pending
- 2018-11-02 JP JP2020520577A patent/JP7065180B2/ja active Active
- 2018-11-02 BR BR112020007744-5A patent/BR112020007744A2/pt unknown
- 2018-11-02 TW TW107138927A patent/TWI826399B/zh active
- 2018-11-02 CN CN201880068606.5A patent/CN111247147B/zh active Active
- 2018-11-02 TW TW112150515A patent/TWI852865B/zh active
- 2018-11-02 CA CA3076457A patent/CA3076457C/en active Active
- 2018-11-02 WO PCT/IB2018/058637 patent/WO2019087149A1/en not_active Ceased
- 2018-11-02 EP EP18800336.2A patent/EP3704117B1/en active Active
- 2018-11-02 AU AU2018362010A patent/AU2018362010B2/en active Active
- 2018-11-02 WO PCT/IB2018/058631 patent/WO2019087146A1/en not_active Ceased
- 2018-11-02 SG SG11202002692XA patent/SG11202002692XA/en unknown
-
2020
- 2020-07-13 MX MX2022011310A patent/MX2022011310A/es unknown
-
2021
- 2021-07-16 AU AU2021205100A patent/AU2021205100B2/en active Active
-
2022
- 2022-03-21 US US17/699,606 patent/US11884666B2/en active Active
- 2022-04-25 JP JP2022071400A patent/JP2022101654A/ja active Pending
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2023
- 2023-04-03 AU AU2023202036A patent/AU2023202036B2/en active Active
- 2023-11-30 US US18/524,807 patent/US12247028B2/en active Active
-
2024
- 2024-01-18 JP JP2024006023A patent/JP7777613B2/ja active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5223528A (en) * | 1986-03-17 | 1993-06-29 | University Of Florida | Anticholinergic compounds, composititons and methods of treatment |
| 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 |
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Legal Events
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |