RU2012127869A - Устойчивые водные композиции пролекарств агонистов простагладина и способы их применения - Google Patents
Устойчивые водные композиции пролекарств агонистов простагладина и способы их применения Download PDFInfo
- Publication number
- RU2012127869A RU2012127869A RU2012127869/15A RU2012127869A RU2012127869A RU 2012127869 A RU2012127869 A RU 2012127869A RU 2012127869/15 A RU2012127869/15 A RU 2012127869/15A RU 2012127869 A RU2012127869 A RU 2012127869A RU 2012127869 A RU2012127869 A RU 2012127869A
- Authority
- RU
- Russia
- Prior art keywords
- composition according
- carboxylic acid
- composition
- hydroxyalkyl
- alkyl
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract 37
- 239000000556 agonist Substances 0.000 title claims abstract 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title claims abstract 4
- 238000000034 method Methods 0.000 title claims 9
- 150000001735 carboxylic acids Chemical class 0.000 claims abstract 15
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims abstract 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims abstract 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims abstract 9
- 125000000217 alkyl group Chemical group 0.000 claims abstract 8
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 8
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 8
- 229940127293 prostanoid Drugs 0.000 claims abstract 6
- 150000003814 prostanoids Chemical class 0.000 claims abstract 6
- 229940061607 dibasic sodium phosphate Drugs 0.000 claims abstract 5
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims abstract 5
- 239000011780 sodium chloride Substances 0.000 claims abstract 5
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 4
- 229910052799 carbon Inorganic materials 0.000 claims abstract 3
- 150000002148 esters Chemical class 0.000 claims abstract 3
- 125000005020 hydroxyalkenyl group Chemical group 0.000 claims abstract 3
- 229940002612 prodrug Drugs 0.000 claims abstract 3
- 239000000651 prodrug Substances 0.000 claims abstract 3
- 239000002904 solvent Substances 0.000 claims abstract 3
- 125000003118 aryl group Chemical group 0.000 claims abstract 2
- 125000000732 arylene group Chemical group 0.000 claims abstract 2
- 150000004820 halides Chemical group 0.000 claims abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 2
- 125000005549 heteroarylene group Chemical group 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 2
- 208000002780 macular degeneration Diseases 0.000 claims 5
- 206010064930 age-related macular degeneration Diseases 0.000 claims 4
- 230000001154 acute effect Effects 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 201000007737 Retinal degeneration Diseases 0.000 claims 2
- 208000029977 White Dot Syndromes Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000004410 intraocular pressure Effects 0.000 claims 2
- 230000004258 retinal degeneration Effects 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 208000003569 Central serous chorioretinopathy Diseases 0.000 claims 1
- 208000005590 Choroidal Neovascularization Diseases 0.000 claims 1
- 206010060823 Choroidal neovascularisation Diseases 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010022557 Intermediate uveitis Diseases 0.000 claims 1
- 208000033463 Ischaemic neuropathy Diseases 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 206010061323 Optic neuropathy Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010038903 Retinal vascular occlusion Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 208000014286 Serpiginous choroiditis Diseases 0.000 claims 1
- 208000036038 Subretinal fibrosis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 208000023564 acute macular neuroretinopathy Diseases 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 238000011065 in-situ storage Methods 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000001491 myopia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000020911 optic nerve disease Diseases 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 238000002428 photodynamic therapy Methods 0.000 claims 1
- 239000000049 pigment Substances 0.000 claims 1
- 230000003169 placental effect Effects 0.000 claims 1
- 229920001992 poloxamer 407 Polymers 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 229920000053 polysorbate 80 Polymers 0.000 claims 1
- 229940068968 polysorbate 80 Drugs 0.000 claims 1
- 201000004849 posterior scleritis Diseases 0.000 claims 1
- 239000000790 retinal pigment Substances 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- 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
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- A61K31/559—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing hetero atoms other than oxygen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26789709P | 2009-12-09 | 2009-12-09 | |
| US61/267,897 | 2009-12-09 | ||
| PCT/US2010/055590 WO2011071620A1 (en) | 2009-12-09 | 2010-11-05 | Stable aqueous compositions of prostglandin agonist prodrugs and methods for use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012127869A true RU2012127869A (ru) | 2014-01-20 |
Family
ID=43503864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012127869/15A RU2012127869A (ru) | 2009-12-09 | 2010-11-05 | Устойчивые водные композиции пролекарств агонистов простагладина и способы их применения |
Country Status (16)
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6270848B2 (ja) | 2012-08-27 | 2018-01-31 | アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ | ベータ−クロロシクロペンタンの親水性エステルプロドラッグの使用による角膜中央部肥厚の低下 |
| KR101535825B1 (ko) | 2012-09-25 | 2015-07-10 | 엘지디스플레이 주식회사 | 표시장치 및 이의 라인결함 검출방법 |
| WO2015175075A1 (en) * | 2014-02-20 | 2015-11-19 | Allergan, Inc. | Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes |
| ES2757798T3 (es) | 2014-10-02 | 2020-04-30 | Allergan Inc | Profármacos de éster de gamma-lactamas y su uso |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4994274A (en) * | 1989-07-27 | 1991-02-19 | Allergan, Inc. | Intraocular pressure reducing 11,15-diacyl prostaglandins and method of using |
| US5034413A (en) | 1989-07-27 | 1991-07-23 | Allergan, Inc. | Intraocular pressure reducing 9,11-diacyl prostaglandins |
| CA2021316C (en) * | 1989-07-27 | 2000-10-24 | Ming Fai Chan | Intraocular pressure reducing 11-acyl prostaglandins |
| US5028624A (en) * | 1989-07-27 | 1991-07-02 | Allergan, Inc. | Intraocular pressure reducing 9,15-diacyl prostaglandins |
| WO2000004898A1 (en) * | 1998-07-21 | 2000-02-03 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| PT1321144E (pt) * | 2000-09-13 | 2011-03-10 | Santen Pharmaceutical Co Ltd | Colírio |
| EP1532981B1 (en) * | 2002-08-23 | 2007-09-26 | Santen Pharmaceutical Co., Ltd. | Stable eye drops containing latanoprost as the active ingredient |
| ES2320770T3 (es) * | 2004-05-26 | 2009-05-28 | Arturo Jimenez Bayardo | Metodo de preparacion de una solucion oftalmica de latanoprost y la solucion asi producida. |
| US20050276867A1 (en) * | 2004-06-09 | 2005-12-15 | Allergan, Inc. | Stabilized compositions comprising a therapeutically active agent and an oxidizing preservative |
| EP1856042B1 (en) * | 2005-03-10 | 2012-06-27 | Allergan, Inc. | Substituted gamma lactams as therapeutic agents |
| EP2123278B1 (en) * | 2007-02-07 | 2013-01-09 | Teika Pharmaceutical Co., Ltd. | Eye drop preparation comprising latanoprost |
| US7820661B2 (en) * | 2008-04-24 | 2010-10-26 | Allergan, Inc. | Substituted gamma lactams as therapeutics agents |
| EP2127638A1 (en) * | 2008-05-30 | 2009-12-02 | Santen Pharmaceutical Co., Ltd | Method and composition for treating ocular hypertension and glaucoma |
-
2010
- 2010-11-04 US US12/939,861 patent/US20110136872A1/en not_active Abandoned
- 2010-11-05 JP JP2012543111A patent/JP5955774B2/ja not_active Expired - Fee Related
- 2010-11-05 EP EP10782082A patent/EP2509582A1/en not_active Withdrawn
- 2010-11-05 WO PCT/US2010/055590 patent/WO2011071620A1/en not_active Ceased
- 2010-11-05 TW TW099138227A patent/TW201138766A/zh unknown
- 2010-11-05 CN CN201080063225.1A patent/CN102762195B/zh not_active Expired - Fee Related
- 2010-11-05 KR KR1020127017676A patent/KR20120106788A/ko not_active Ceased
- 2010-11-05 CA CA2783707A patent/CA2783707A1/en not_active Abandoned
- 2010-11-05 NZ NZ600577A patent/NZ600577A/en not_active IP Right Cessation
- 2010-11-05 AU AU2010328555A patent/AU2010328555B2/en not_active Ceased
- 2010-11-05 SG SG2012042461A patent/SG181600A1/en unknown
- 2010-11-05 MX MX2012006622A patent/MX2012006622A/es not_active Application Discontinuation
- 2010-11-05 RU RU2012127869/15A patent/RU2012127869A/ru not_active Application Discontinuation
- 2010-11-05 AR ARP100104122A patent/AR078929A1/es unknown
-
2012
- 2012-06-07 IL IL220240A patent/IL220240A0/en unknown
- 2012-06-08 CL CL2012001545A patent/CL2012001545A1/es unknown
-
2015
- 2015-08-26 US US14/836,785 patent/US20160220677A1/en not_active Abandoned
-
2016
- 2016-01-14 JP JP2016005576A patent/JP2016056207A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP5955774B2 (ja) | 2016-07-20 |
| AR078929A1 (es) | 2011-12-14 |
| CL2012001545A1 (es) | 2012-08-31 |
| IL220240A0 (en) | 2012-07-31 |
| KR20120106788A (ko) | 2012-09-26 |
| WO2011071620A1 (en) | 2011-06-16 |
| CN102762195B (zh) | 2016-05-18 |
| US20110136872A1 (en) | 2011-06-09 |
| MX2012006622A (es) | 2012-08-15 |
| NZ600577A (en) | 2014-10-31 |
| JP2013513606A (ja) | 2013-04-22 |
| SG181600A1 (en) | 2012-07-30 |
| TW201138766A (en) | 2011-11-16 |
| AU2010328555A1 (en) | 2012-07-05 |
| JP2016056207A (ja) | 2016-04-21 |
| CN102762195A (zh) | 2012-10-31 |
| EP2509582A1 (en) | 2012-10-17 |
| CA2783707A1 (en) | 2011-06-16 |
| AU2010328555B2 (en) | 2016-05-26 |
| US20160220677A1 (en) | 2016-08-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20170209 |