RU2014123471A - ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ПРОИЗВОДНЫХ 4-ПРЕГЕНЕН-11β-17-21-ТРИОЛ-3,20-ДИОНА - Google Patents
ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ПРОИЗВОДНЫХ 4-ПРЕГЕНЕН-11β-17-21-ТРИОЛ-3,20-ДИОНА Download PDFInfo
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- tetradecahydro
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 5
- 150000001875 compounds Chemical class 0.000 claims abstract 12
- 208000030533 eye disease Diseases 0.000 claims abstract 5
- FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 claims abstract 3
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims abstract 3
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims abstract 3
- MNWFXJYAOYHMED-UHFFFAOYSA-N heptanoic acid Chemical compound CCCCCCC(O)=O MNWFXJYAOYHMED-UHFFFAOYSA-N 0.000 claims abstract 3
- KQNPFQTWMSNSAP-UHFFFAOYSA-N isobutyric acid Chemical compound CC(C)C(O)=O KQNPFQTWMSNSAP-UHFFFAOYSA-N 0.000 claims abstract 3
- 229940049953 phenylacetate Drugs 0.000 claims abstract 3
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims abstract 2
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims abstract 2
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims abstract 2
- 102100021316 Mineralocorticoid receptor Human genes 0.000 claims abstract 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000003862 glucocorticoid Substances 0.000 claims abstract 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
- 206010013774 Dry eye Diseases 0.000 claims 2
- 206010065062 Meibomian gland dysfunction Diseases 0.000 claims 2
- 241001303601 Rosacea Species 0.000 claims 2
- 208000010217 blepharitis Diseases 0.000 claims 2
- 210000005252 bulbus oculi Anatomy 0.000 claims 2
- 210000000795 conjunctiva Anatomy 0.000 claims 2
- 210000004087 cornea Anatomy 0.000 claims 2
- 201000004700 rosacea Diseases 0.000 claims 2
- 208000009043 Chemical Burns Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 206010011715 Cyclitis Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010070245 Foreign body Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000001344 Macular Edema Diseases 0.000 claims 1
- 206010025415 Macular oedema Diseases 0.000 claims 1
- 206010030865 Ophthalmic herpes zoster Diseases 0.000 claims 1
- 206010063562 Radiation skin injury Diseases 0.000 claims 1
- 206010038848 Retinal detachment Diseases 0.000 claims 1
- 206010053615 Thermal burn Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- IPBVNPXQWQGGJP-UHFFFAOYSA-N acetic acid phenyl ester Natural products CC(=O)OC1=CC=CC=C1 IPBVNPXQWQGGJP-UHFFFAOYSA-N 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002458 infectious effect Effects 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 230000004410 intraocular pressure Effects 0.000 claims 1
- 201000004614 iritis Diseases 0.000 claims 1
- 206010023332 keratitis Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 201000010230 macular retinal edema Diseases 0.000 claims 1
- WWZKQHOCKIZLMA-UHFFFAOYSA-M octanoate Chemical compound CCCCCCCC([O-])=O WWZKQHOCKIZLMA-UHFFFAOYSA-M 0.000 claims 1
- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 230000004264 retinal detachment Effects 0.000 claims 1
- 208000004644 retinal vein occlusion Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 230000036575 thermal burns Effects 0.000 claims 1
- -1 1H-cyclopenta [a] phenanthrene-17-yloctanoate Chemical compound 0.000 abstract 1
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Abstract
1. Способ лечения глазного заболевания, связанного с модулированием глюкокортикоидного и/или минералокортикоидного рецептора, который включает введение пациенту, нуждающемуся в этом, фармацевтической композиции, содержащей терапевтически эффективное количество по меньшей мере одного соединения, выбранного из:(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илфенилацетата;(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илбутирата;(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илпропионата;(8S,9S,10R,11,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илоктаноата;(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илгексаноата;(8R,9R,10S,11R,13R,14R,17S)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илбензоата;(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Η-циклопента[а]фенантрен-17-ил гептаноата;(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил 2-метилпропаноата; и(8R,9R,10S,11R,13R,14R,17S)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил rel-циклопентанкарбоксилата.2. Способ по п. 1, отличающийся тем, что указанное глазное заболевание выбрано из повышенного внутриглазного да�
Claims (14)
1. Способ лечения глазного заболевания, связанного с модулированием глюкокортикоидного и/или минералокортикоидного рецептора, который включает введение пациенту, нуждающемуся в этом, фармацевтической композиции, содержащей терапевтически эффективное количество по меньшей мере одного соединения, выбранного из:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илфенилацетата;
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илбутирата;
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илпропионата;
(8S,9S,10R,11,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илоктаноата;
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илгексаноата;
(8R,9R,10S,11R,13R,14R,17S)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-илбензоата;
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Η-циклопента[а]фенантрен-17-ил гептаноата;
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил 2-метилпропаноата; и
(8R,9R,10S,11R,13R,14R,17S)-17-гликолоил-11-гидрокси-10,13-диметил-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил rel-циклопентанкарбоксилата.
2. Способ по п. 1, отличающийся тем, что указанное глазное заболевание выбрано из повышенного внутриглазного давления, глаукомы, увеита, окклюзии вены сетчатки, дегенерации желтого пятна, диабетической ретинопатии, различных форм макулярного отека, послеоперационного воспаления, воспалительных состояний конъюнктивы век и конъюнктивы глазного яблока, роговицы и переднего сегмента глазного яблока, такие как аллергические конъюнктивиты, розовые угри на глазах, сухость глаз, блефариты, отслоение сетчатки, дисфункции мейбомиевой железы, точечного поверхностного кератита, кератита с опоясывающим герпесом, ирита, циклита, некоторых инфекционных конъюнктивитов, травмы роговицы из-за химического, радиационного или термического ожога, проникновения инородных тел, аллергии и их комбинаций.
3. Способ по п. 1, отличающийся тем, что указанное глазное заболевание выбрано из розовых угрей на глазах, сухости глаз, блефарита, дисфункции мейбомиевой железы.
4. Фармацевтическая композиция, содержащая носитель и соединение по п. 1.
5. Фармацевтическая композиция по п. 1, которая предназначена для локального офтальмического применения.
6. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил бензоат.
7. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил гексаноат.
8. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил октаноат.
9. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил фенилацетат.
10. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил бутират.
11. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил пропионат.
12. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил гептаноат.
13. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил 2-метилпропаноат.
14. Способ по п. 1, отличающийся тем, что указанное соединение представляет собой:
(8S,9S,10R,11S,13S,14S,17R)-17-гликолоил-11-гидрокси-10,13-диметид-3-оксо-2,3,6,7,8,9,10,11,12,13,14,15,16,17-тетрадекагидро-1Н-циклопента[а]фенантрен-17-ил rel-циклопентанкарбоксилат.
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| US61/558,775 | 2011-11-11 | ||
| PCT/US2012/064296 WO2013071010A1 (en) | 2011-11-11 | 2012-11-09 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF 4-PREGENEN-11ß-17-21-TRIOL-3,20-DIONE DERIVATIVES |
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| RU2014123471A RU2683775C2 (ru) | 2011-11-11 | 2012-11-09 | ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ПРОИЗВОДНЫХ 4-ПРЕГЕНЕН-11β-17-21-ТРИОЛ-3,20-ДИОНА |
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| EP2386555A1 (en) | 2010-05-13 | 2011-11-16 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities |
| EP2592078A1 (en) | 2011-11-11 | 2013-05-15 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities |
| UA111867C2 (uk) | 2011-11-11 | 2016-06-24 | Аллерган, Інк. | ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ І СПОСІБ ЗАСТОСУВАННЯ ПОХІДНИХ 4-ПРЕГНЕН-11β-17-21-ТРІОЛ-3,20-ДІОНУ |
| HK1215166A1 (zh) | 2012-12-18 | 2016-08-19 | Almirall, S.A. | 具有β2肾上腺素激动剂及M3毒蕈碱拮抗剂活性的新型环己基和奎宁环基氨基甲酸酯衍生物 |
| TWI643853B (zh) | 2013-02-27 | 2018-12-11 | 阿爾米雷爾有限公司 | 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類 |
| TW201517906A (zh) | 2013-07-25 | 2015-05-16 | Almirall Sa | 含有maba化合物和皮質類固醇之組合 |
| TWI641373B (zh) | 2013-07-25 | 2018-11-21 | 阿爾米雷爾有限公司 | 具有蕈毒鹼受體拮抗劑和β2腎上腺素受體促效劑二者之活性的2-胺基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽 |
| AR098747A1 (es) * | 2013-12-13 | 2016-06-08 | Allergan Inc | Formas polimórficas de un compuesto similar a esteroides y métodos para su preparación y uso |
| TW201617343A (zh) | 2014-09-26 | 2016-05-16 | 阿爾米雷爾有限公司 | 具有β2腎上腺素促效劑及M3蕈毒拮抗劑活性之新穎雙環衍生物 |
| RU2746083C2 (ru) | 2015-03-05 | 2021-04-06 | Аллерган, Инк. | Самоэмульгирующиеся системы доставки лекарств (sedds) для доставки офтальмологического лекарства |
| US20190216726A1 (en) * | 2016-09-16 | 2019-07-18 | Kala Pharmaceuticals, Inc. | Particles, Compositions and Methods for Ophthalmic and/or Other Applications |
| WO2019055028A1 (en) * | 2017-09-15 | 2019-03-21 | Kala Pharmaceuticals, Inc. | PARTICLES, COMPOSITIONS AND METHODS FOR OPHTHALMIC APPLICATIONS AND / OR OTHER APPLICATIONS |
| CN116023425B (zh) * | 2023-03-28 | 2023-06-20 | 南京师范大学 | 曲安西龙衍生物及其医药用途 |
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