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)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (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)
| Country | Link |
|---|---|
| US (2) | US20110136872A1 (https=) |
| EP (1) | EP2509582A1 (https=) |
| JP (2) | JP5955774B2 (https=) |
| KR (1) | KR20120106788A (https=) |
| CN (1) | CN102762195B (https=) |
| AR (1) | AR078929A1 (https=) |
| AU (1) | AU2010328555B2 (https=) |
| CA (1) | CA2783707A1 (https=) |
| CL (1) | CL2012001545A1 (https=) |
| IL (1) | IL220240A0 (https=) |
| MX (1) | MX2012006622A (https=) |
| NZ (1) | NZ600577A (https=) |
| RU (1) | RU2012127869A (https=) |
| SG (1) | SG181600A1 (https=) |
| TW (1) | TW201138766A (https=) |
| WO (1) | WO2011071620A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR201900863T4 (tr) | 2012-08-27 | 2019-02-21 | Allergan Inc | Beta-klorosiklopentanların hidrofilik ester ön ilaçlarının kullanılmasıyla merkezi korneal kalınlaşmanın azaltılması. |
| KR101535825B1 (ko) | 2012-09-25 | 2015-07-10 | 엘지디스플레이 주식회사 | 표시장치 및 이의 라인결함 검출방법 |
| TR201902864T4 (tr) * | 2014-02-20 | 2019-03-21 | Allergan Inc | Beta-klorosiklopentanların hidrofilik ester ön ilaçlarının kullanımı ile azaltılmış merkezi korneal kalınlaşma. |
| CA2962766A1 (en) | 2014-10-02 | 2016-04-07 | Allergan, Inc. | Ester prodrugs of gamma-lactams and their use |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5034413A (en) | 1989-07-27 | 1991-07-23 | Allergan, Inc. | Intraocular pressure reducing 9,11-diacyl prostaglandins |
| US4994274A (en) * | 1989-07-27 | 1991-02-19 | Allergan, Inc. | Intraocular pressure reducing 11,15-diacyl prostaglandins and method of using |
| WO2000004898A1 (en) * | 1998-07-21 | 2000-02-03 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| CA2422031C (en) * | 2000-09-13 | 2011-11-15 | Santen Pharmaceutical Co., Ltd. | Ophthalmic solutions comprising difluoroprostaglandin f2 alpha |
| DK1532981T3 (da) * | 2002-08-23 | 2008-01-28 | Santen Pharmaceutical Co Ltd | Stabile öjendråber, der indeholder latanoprost som den aktive bestanddel |
| PL1759702T3 (pl) * | 2004-05-26 | 2009-06-30 | Bayardo Arturo Jimenez | Sposób wytwarzania roztworu latanoprostu do oczu oraz roztwór otrzymany tym sposobem |
| US20050276867A1 (en) * | 2004-06-09 | 2005-12-15 | Allergan, Inc. | Stabilized compositions comprising a therapeutically active agent and an oxidizing preservative |
| CA2599425C (en) * | 2005-03-10 | 2013-04-30 | Allergan, Inc. | Substituted gamma lactams as therapeutic agents |
| WO2008096804A1 (ja) * | 2007-02-07 | 2008-08-14 | Teika Pharmaceutical Co., Ltd. | ラタノプロスト含有点眼剤 |
| MY150518A (en) * | 2008-04-24 | 2014-01-30 | Allergan Inc | Substituted gamma lactams as therapeutic 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 EP EP10782082A patent/EP2509582A1/en not_active Withdrawn
- 2010-11-05 MX MX2012006622A patent/MX2012006622A/es not_active Application Discontinuation
- 2010-11-05 WO PCT/US2010/055590 patent/WO2011071620A1/en not_active Ceased
- 2010-11-05 RU RU2012127869/15A patent/RU2012127869A/ru not_active Application Discontinuation
- 2010-11-05 CA CA2783707A patent/CA2783707A1/en not_active Abandoned
- 2010-11-05 AR ARP100104122A patent/AR078929A1/es unknown
- 2010-11-05 AU AU2010328555A patent/AU2010328555B2/en not_active Ceased
- 2010-11-05 TW TW099138227A patent/TW201138766A/zh unknown
- 2010-11-05 JP JP2012543111A patent/JP5955774B2/ja not_active Expired - Fee Related
- 2010-11-05 CN CN201080063225.1A patent/CN102762195B/zh not_active Expired - Fee Related
- 2010-11-05 NZ NZ600577A patent/NZ600577A/en not_active IP Right Cessation
- 2010-11-05 KR KR1020127017676A patent/KR20120106788A/ko not_active Ceased
- 2010-11-05 SG SG2012042461A patent/SG181600A1/en 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 |
|---|---|
| CL2012001545A1 (es) | 2012-08-31 |
| AR078929A1 (es) | 2011-12-14 |
| WO2011071620A1 (en) | 2011-06-16 |
| JP2013513606A (ja) | 2013-04-22 |
| IL220240A0 (en) | 2012-07-31 |
| NZ600577A (en) | 2014-10-31 |
| JP2016056207A (ja) | 2016-04-21 |
| US20160220677A1 (en) | 2016-08-04 |
| EP2509582A1 (en) | 2012-10-17 |
| SG181600A1 (en) | 2012-07-30 |
| TW201138766A (en) | 2011-11-16 |
| CN102762195B (zh) | 2016-05-18 |
| CN102762195A (zh) | 2012-10-31 |
| AU2010328555A1 (en) | 2012-07-05 |
| JP5955774B2 (ja) | 2016-07-20 |
| CA2783707A1 (en) | 2011-06-16 |
| US20110136872A1 (en) | 2011-06-09 |
| KR20120106788A (ko) | 2012-09-26 |
| MX2012006622A (es) | 2012-08-15 |
| AU2010328555B2 (en) | 2016-05-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20170209 |