TW201141477A - Alpha-2 adrenergic agonist having long duration of intraocular pressure-lowering effect - Google Patents
Alpha-2 adrenergic agonist having long duration of intraocular pressure-lowering effect Download PDFInfo
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- TW201141477A TW201141477A TW100102411A TW100102411A TW201141477A TW 201141477 A TW201141477 A TW 201141477A TW 100102411 A TW100102411 A TW 100102411A TW 100102411 A TW100102411 A TW 100102411A TW 201141477 A TW201141477 A TW 201141477A
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- LRBQNJMCXXYXIU-QWKBTXIPSA-N gallotannic acid Chemical compound OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@H]2[C@@H]([C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-QWKBTXIPSA-N 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 229940093915 gynecological organic acid Drugs 0.000 description 1
- 239000001307 helium Substances 0.000 description 1
- 229910052734 helium Inorganic materials 0.000 description 1
- SWQJXJOGLNCZEY-UHFFFAOYSA-N helium atom Chemical compound [He] SWQJXJOGLNCZEY-UHFFFAOYSA-N 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- XNTOBBRAVPYVOU-UHFFFAOYSA-N imidazolidin-2-amine Chemical compound NC1NCCN1 XNTOBBRAVPYVOU-UHFFFAOYSA-N 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 229940095437 iopidine Drugs 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 238000011866 long-term treatment Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 208000018769 loss of vision Diseases 0.000 description 1
- 231100000864 loss of vision Toxicity 0.000 description 1
- FBDWCTWJJMORIU-UHFFFAOYSA-N magnesium;hexahydrate Chemical compound O.O.O.O.O.O.[Mg] FBDWCTWJJMORIU-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- OLXYLDUSSBULGU-UHFFFAOYSA-N methyl pyridine-4-carboxylate Chemical compound COC(=O)C1=CC=NC=C1 OLXYLDUSSBULGU-UHFFFAOYSA-N 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 210000001328 optic nerve Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 125000005430 oxychloro group Chemical group 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 238000013148 permeation assay Methods 0.000 description 1
- 229940067107 phenylethyl alcohol Drugs 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920001993 poloxamer 188 Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229940068965 polysorbates Drugs 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000000955 prescription drug Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000037452 priming Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 229960003981 proparacaine Drugs 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 229940107700 pyruvic acid Drugs 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 208000026451 salivation Diseases 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 210000003786 sclera Anatomy 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
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- 229940075582 sorbic acid Drugs 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
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- 235000015523 tannic acid Nutrition 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
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- 230000001225 therapeutic effect Effects 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
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Classifications
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29691210P | 2010-01-21 | 2010-01-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201141477A true TW201141477A (en) | 2011-12-01 |
Family
ID=44169074
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW100102411A TW201141477A (en) | 2010-01-21 | 2011-01-21 | Alpha-2 adrenergic agonist having long duration of intraocular pressure-lowering effect |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9889088B2 (enExample) |
| EP (1) | EP2525793B1 (enExample) |
| JP (3) | JP2013518051A (enExample) |
| KR (1) | KR20120125305A (enExample) |
| CN (1) | CN102770135A (enExample) |
| AU (1) | AU2011207301A1 (enExample) |
| BR (1) | BR112012018154A2 (enExample) |
| CA (1) | CA2787573A1 (enExample) |
| CL (1) | CL2012002038A1 (enExample) |
| CO (1) | CO6592108A2 (enExample) |
| IL (1) | IL221030A0 (enExample) |
| MX (1) | MX2012008516A (enExample) |
| RU (1) | RU2012134065A (enExample) |
| SG (1) | SG182637A1 (enExample) |
| TW (1) | TW201141477A (enExample) |
| WO (1) | WO2011091225A2 (enExample) |
| ZA (1) | ZA201205470B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130046003A1 (en) * | 2011-07-22 | 2013-02-21 | Mohammed I. Dibas | Pharmaceutical compositions comprising 4-bromo-n-(imidazolidin-2-ylidene)-1h-benzimidazol-5-amine for treating retinal diseases |
| WO2013016072A1 (en) * | 2011-07-22 | 2013-01-31 | Allergan, Inc. | Pharmaceutical compositions comprising 4-bromo-n-(imidazolidin-2-ylidene)-1h-benzimidazol-5-amine for treating skin diseases |
| BR112014001501A2 (pt) * | 2011-07-22 | 2017-02-14 | Allergan Inc | moduladores alfa-2 adrenérgicos para tratamento de distúrbios visuais mediados por projeções visuais centrais do olho |
| WO2014159576A1 (en) * | 2013-03-14 | 2014-10-02 | Allergan, Inc. | Alpha-2 adrenergic agonist for treating intraocular pressure and ocular diseases through intravitreal and intracameral routes |
| TWI699205B (zh) * | 2014-12-12 | 2020-07-21 | 日商興和股份有限公司 | 用於預防或治療青光眼之藥物療法 |
| WO2019004080A1 (ja) | 2017-06-27 | 2019-01-03 | 国立大学法人東京大学 | 融合遺伝子及び／又はエクソンスキッピングにより生ずる転写産物を検出するためのプローブ及び方法 |
| US11077053B2 (en) | 2018-08-21 | 2021-08-03 | Allergan, Inc. | Alpha-2-adrenergic receptor agonists for treatment of presbyopia, visual glare, visual starbursts, visual halos and night myopia |
| PT4236932T (pt) * | 2020-11-02 | 2026-02-23 | Visus Therapeutics Inc | Composto degradante num medicamento |
| WO2023086878A1 (en) * | 2021-11-10 | 2023-05-19 | Visus Therapeutics, Inc. | Carbachol formulations to enhance anti-presbyopia effects |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5478858A (en) * | 1993-12-17 | 1995-12-26 | The Procter & Gamble Company | 5-(2-imidazolinylamino) benzimidazole compounds useful as alpha-2 adrenoceptor agonists |
| AU704972B2 (en) * | 1994-08-04 | 1999-05-13 | H. Lundbeck A/S | Novel benzimidazole derivatives |
| US6495583B1 (en) * | 1997-03-25 | 2002-12-17 | Synaptic Pharmaceutical Corporation | Benzimidazole derivatives |
| US20050244463A1 (en) | 2004-04-30 | 2005-11-03 | Allergan, Inc. | Sustained release intraocular implants and methods for treating ocular vasculopathies |
| CA2603044A1 (en) * | 2005-06-29 | 2007-01-11 | Allergan, Inc. | Alpha-2 adrenergic agonists for the treatment of pain |
| CA2641501A1 (en) | 2006-02-06 | 2007-08-16 | Nicox S.A. | Nitrooxy-comprising derivatives of apraclonidine and brimodnidine as al pha2 -adrenergic receptor agonists |
| US8821870B2 (en) * | 2008-07-18 | 2014-09-02 | Allergan, Inc. | Method for treating atrophic age related macular degeneration |
-
2011
- 2011-01-21 MX MX2012008516A patent/MX2012008516A/es unknown
- 2011-01-21 JP JP2012550140A patent/JP2013518051A/ja active Pending
- 2011-01-21 KR KR1020127021719A patent/KR20120125305A/ko not_active Withdrawn
- 2011-01-21 AU AU2011207301A patent/AU2011207301A1/en not_active Abandoned
- 2011-01-21 CN CN2011800111530A patent/CN102770135A/zh active Pending
- 2011-01-21 TW TW100102411A patent/TW201141477A/zh unknown
- 2011-01-21 EP EP11702342.4A patent/EP2525793B1/en not_active Not-in-force
- 2011-01-21 RU RU2012134065/15A patent/RU2012134065A/ru unknown
- 2011-01-21 BR BR112012018154A patent/BR112012018154A2/pt not_active IP Right Cessation
- 2011-01-21 WO PCT/US2011/022001 patent/WO2011091225A2/en not_active Ceased
- 2011-01-21 CA CA2787573A patent/CA2787573A1/en not_active Abandoned
- 2011-01-21 US US13/010,958 patent/US9889088B2/en not_active Expired - Fee Related
- 2011-01-21 SG SG2012053815A patent/SG182637A1/en unknown
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2012
- 2012-07-19 IL IL221030A patent/IL221030A0/en unknown
- 2012-07-20 ZA ZA2012/05470A patent/ZA201205470B/en unknown
- 2012-07-20 CL CL2012002038A patent/CL2012002038A1/es unknown
- 2012-08-17 CO CO12140238A patent/CO6592108A2/es not_active Application Discontinuation
-
2015
- 2015-10-28 JP JP2015211447A patent/JP2016026206A/ja active Pending
-
2017
- 2017-04-26 JP JP2017086952A patent/JP6466504B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| SG182637A1 (en) | 2012-08-30 |
| ZA201205470B (en) | 2013-05-29 |
| CA2787573A1 (en) | 2011-07-28 |
| WO2011091225A3 (en) | 2012-05-18 |
| JP6466504B2 (ja) | 2019-02-06 |
| CO6592108A2 (es) | 2013-01-02 |
| JP2013518051A (ja) | 2013-05-20 |
| KR20120125305A (ko) | 2012-11-14 |
| US9889088B2 (en) | 2018-02-13 |
| JP2017125074A (ja) | 2017-07-20 |
| BR112012018154A2 (pt) | 2016-04-05 |
| AU2011207301A1 (en) | 2012-08-09 |
| EP2525793A2 (en) | 2012-11-28 |
| WO2011091225A2 (en) | 2011-07-28 |
| IL221030A0 (en) | 2012-09-24 |
| US20110178145A1 (en) | 2011-07-21 |
| CN102770135A (zh) | 2012-11-07 |
| JP2016026206A (ja) | 2016-02-12 |
| MX2012008516A (es) | 2012-10-15 |
| RU2012134065A (ru) | 2014-02-27 |
| EP2525793B1 (en) | 2018-09-05 |
| CL2012002038A1 (es) | 2012-11-16 |
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