ES2570659T3 - Agonistas de adenosina A1 para el tratamiento del glaucoma y de la hipertensión ocular - Google Patents
Agonistas de adenosina A1 para el tratamiento del glaucoma y de la hipertensión ocularInfo
- Publication number
- ES2570659T3 ES2570659T3 ES11752517T ES11752517T ES2570659T3 ES 2570659 T3 ES2570659 T3 ES 2570659T3 ES 11752517 T ES11752517 T ES 11752517T ES 11752517 T ES11752517 T ES 11752517T ES 2570659 T3 ES2570659 T3 ES 2570659T3
- Authority
- ES
- Spain
- Prior art keywords
- hydrogen
- methyl
- formula
- group
- pyrrolidine
- 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.)
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Classifications
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- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- 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
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Abstract
Compuesto de fórmula (I)**Fórmula** en la que A es oxígeno o azufre, R1 es hidrógeno o un grupo de fórmula**Fórmula** o en la que es la unión al átomo de oxígeno, L1 es alcanodiílo (C2-C4) lineal, L2 es alcanodiílo (C1-C3) lineal, R5 y R8 son idénticos o diferentes y se seleccionan independientemente entre el grupo que consiste en hidrógeno, metilo, propan-2-ilo, propan-1-ilo, 2-metilpropan-1-ilo, 1-metilpropan-1-ilo, butan-1-ilo, terc-butilo, fenilo, bencilo, p-hidroxibencilo, indol-3-ilmetilo, imidazol-4-ilmetilo, hidroximetilo, 2-hidroxietilo, 1-hidroxietilo, mercaptometilo, metiltiometilo, 2-mercaptoetilo, 2-metiltioetilo, carbamoílmetilo, 2-carbamoíletilo, carboximetilo, 2-carboxietilo, 4-aminobutan-1-ilo, 4-amino-3-hidroxibutan-1-ilo, 3-aminopropan-1-ilo, 2- aminoetilo, aminometilo, 3-guanidinopropan-1-ilo, 3-ureidopropan-1-ilo, R6 y R9 se seleccionan independientemente entre hidrógeno o metilo, R7 es hidrógeno o alquilo (C1-C4), o R7 y R5 forman, junto con los átomos a los que están unidos, un anillo de pirrolidina o de piperidina, R10 y R11 son idénticos o diferentes y se seleccionan independientemente entre hidrógeno o alquilo (C1-C4), en el que el alquilo (C1-C4) puede estar sustituido con un grupo seleccionado entre hidroxi, alcoxi (C1-C4), amino, mono-alquilamino (C1-C4) o di-alquilamino (C1-C4), o R10 y R8 forman, junto con los átomos a los que están unidos, un anillo de pirrolidina o de piperidina, y R12 es hidrógeno o hidroxicarbonilo, R2 es hidrógeno o un grupo de fórmula -CH2OR1, en la que R1 es como se ha definido anteriormente, R3 es hidrógeno, metilo o etilo, R4 es hidrógeno, metilo o etilo, o R3 y R4 forman junto con el átomo de nitrógeno, al que están unidos, un anillo de azetidina, pirrolidina o piperidina, en los que el anillo de azetidina, pirrolidina o piperidina puede estar sustituido con uno o 2 sustituyentes seleccionados independientemente entre el grupo flúor, trifluorometilo, metilo, etilo, metoxi y etoxi, o sus sales, solvatos y solvatos de las sales para su uso en un procedimiento para el tratamiento y/o profilaxis del glaucoma, el glaucoma normotensivo, la hipertensión ocular y/o combinaciones de los mismos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10175151 | 2010-09-02 | ||
| PCT/EP2011/064829 WO2012028585A1 (en) | 2010-09-02 | 2011-08-29 | Adenosine a1 agonists for the treatment of glaucoma and ocular hypertension |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2570659T3 true ES2570659T3 (es) | 2016-05-19 |
Family
ID=44582992
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11752517T Active ES2570659T3 (es) | 2010-09-02 | 2011-08-29 | Agonistas de adenosina A1 para el tratamiento del glaucoma y de la hipertensión ocular |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US20120058983A1 (es) |
| EP (1) | EP2611415B1 (es) |
| JP (1) | JP5875585B2 (es) |
| KR (1) | KR20140091457A (es) |
| CN (1) | CN103249400B (es) |
| AP (1) | AP3413A (es) |
| AU (1) | AU2011298430B2 (es) |
| BR (1) | BR112013005224A2 (es) |
| CA (1) | CA2809700A1 (es) |
| CL (2) | CL2013000599A1 (es) |
| CR (1) | CR20130094A (es) |
| CY (1) | CY1117458T1 (es) |
| DK (1) | DK2611415T3 (es) |
| EA (1) | EA028411B1 (es) |
| ES (1) | ES2570659T3 (es) |
| HK (1) | HK1188138A1 (es) |
| HR (1) | HRP20160532T1 (es) |
| HU (1) | HUE027295T2 (es) |
| MA (1) | MA34489B1 (es) |
| MX (1) | MX2013002396A (es) |
| MY (1) | MY160383A (es) |
| NZ (1) | NZ607624A (es) |
| PL (1) | PL2611415T3 (es) |
| RS (1) | RS54743B1 (es) |
| SG (1) | SG187974A1 (es) |
| SI (1) | SI2611415T1 (es) |
| TW (1) | TWI516266B (es) |
| UA (1) | UA111947C2 (es) |
| WO (1) | WO2012028585A1 (es) |
| ZA (1) | ZA201302340B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA027109B1 (ru) | 2012-01-26 | 2017-06-30 | Инотек Фармасьютикалс Корпорейшн | Безводные полиморфы [(2r,3s,4r,5r)-5-(6-(циклопентиламино)-9h-пурин-9-ил)-3,4-дигидрокситетрагидрофуран-2-ил]метилнитрата и способы их получения |
| US20160317542A1 (en) | 2013-12-09 | 2016-11-03 | Respira Therapeutics, Inc. | Pde5 inhibitor powder formulations and methods relating thereto |
| MX2016007343A (es) * | 2013-12-12 | 2016-09-13 | Bayer Pharma AG | Agonistas de a1 de adenosina como medicamentos para trastornos renales. |
| MY166210A (en) * | 2014-01-10 | 2018-06-22 | Santen Pharmaceutical Co Ltd | Pyridylaminoacetic acid compound and polyoxyethylene castor oil-containing pharmaceutical composition |
| CU20170136A7 (es) * | 2015-05-06 | 2018-02-08 | Bayer Pharma AG | Procedimiento para la preparación de 2-{4-[2-({[2-(4-clorofenil)-1 ,3-tiazol-4-il]metil}sulfanil)-3,5-dician0-6-(pirrolidin-1-il)piridina-4-il]fenoxi}etil-l-alanil-l-alaninato-monohidrocloruro |
| WO2017137528A1 (en) | 2016-02-12 | 2017-08-17 | Charité - Universitätsmedizin Berlin | Adenosine a1 receptor agonist for use in treatment of status epilepticus |
| CN112545983A (zh) * | 2020-12-18 | 2021-03-26 | 合肥中龙神力动物药业有限公司 | 一种复方硫酸新霉素滴眼液及其制备方法和应用 |
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| DE102007035367A1 (de) * | 2007-07-27 | 2009-01-29 | Bayer Healthcare Ag | Substituierte Aryloxazole und ihre Verwendung |
| DE102007036075A1 (de) | 2007-08-01 | 2009-02-05 | Bayer Healthcare Ag | Prodrugs und ihre Verwendung |
| DE102007036076A1 (de) * | 2007-08-01 | 2009-02-05 | Bayer Healthcare Aktiengesellschaft | Dipeptoid-Produgs und ihre Verwendung |
| DE102008013587A1 (de) | 2008-03-11 | 2009-09-17 | Bayer Schering Pharma Aktiengesellschaft | Heteroaryl-substituierte Dicyanopyridine und ihre Verwendung |
| WO2009143992A1 (de) | 2008-05-29 | 2009-12-03 | Bayer Schering Pharma Aktiengesellschaft | 2-alkoxy-substituierte dicyanopyridine und ihre verwendung |
| DE102008062566A1 (de) * | 2008-12-16 | 2010-06-17 | Bayer Schering Pharma Aktiengesellschaft | Aminosäureester-Prodrugs und ihre Verwendung |
| DE102008062561A1 (de) * | 2008-12-16 | 2010-06-24 | Maxon Motor Ag | Bausatz für einen Elektromotor mit einem Drehwinkelgeber |
| DE102008062567A1 (de) * | 2008-12-16 | 2010-06-17 | Bayer Schering Pharma Aktiengesellschaft | Dipeptoid-Prodrugs und ihre Verwendung |
| DE102009006602A1 (de) | 2009-01-29 | 2010-08-05 | Bayer Schering Pharma Aktiengesellschaft | Alkylamino-substituierte Dicyanopyridine und deren Aminosäureester-Prodrugs |
| CN102413832B (zh) | 2009-05-01 | 2015-11-25 | 伊诺泰克制药公司 | 降低人眼内压的方法 |
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