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Ophthalmic composition of heteroaryl sulfamoyl carboxylic ester carbonic anhydrase inhibitor

A technology of sulfamoyl nicotinic acid ester and heteroaromatic group, which is applied in the field of solution preparations containing cyclodextrin, and can solve the problems such as the same effect cannot be explained

Inactive Publication Date: 2011-03-23
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, the drug in this patent application involves multiple compound nuclei, such as steroidal compounds, antimalarial agents, nucleosides, and isoflavones. The pharmacological experiments only prove that this type of compound has the effect of inhibiting carbonic acid enzymes, combined with the introduction in the specification , this type of drug should be mainly effective through oral administration, but it does not mean that this type of compound has the same effect when used directly in the eyes

Method used

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  • Ophthalmic composition of heteroaryl sulfamoyl carboxylic ester carbonic anhydrase inhibitor
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  • Ophthalmic composition of heteroaryl sulfamoyl carboxylic ester carbonic anhydrase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Synthesis Example 1: Mometasone-17-6'-sulfamoyl nicotinate

[0076] Put 1 mmol of mometasone in 30 ml of pyridine under nitrogen, add 1.3 mmol of 6-aminosulfonyl nicotinic acid at 0 degrees, add DMAP0.1 mmol and stir for 3 hours, stir the reaction mixture into 300 ml of water and use Acidify with 10% HCl. After 10 minutes, it was filtered off with suction, washed with water and dried. The residue was chromatographically purified on silica gel to obtain 0.47 mmol of mometasone-17-6'-sulfamoyl nicotinate.

Embodiment 2

[0077] Synthesis Example 2: Prednisolone-21-2'-ethyl-5'-sulfamoylthiophene-3'-carboxylate

[0078] 1.3 mmol of 5-(sulfamoyl)-2-ethyl-3-thiophenecarboxylic acid were dissolved in 50 ml of pyridine under argon. Add 1mmol of prednisolone at -5°C, add PTS0.05mmol and DCC0.05mmol and stir for 8 hours, stir and dilute the reaction mixture in 500ml of water, adjust the pH to 6 with hydrochloric acid. After 10 minutes, suction filter, wash with water and dry. The residue was purified by chromatography on silica gel to obtain 0.62 mmol of prednisolone-21-2'-ethyl-5'-sulfamoylthiophene-3'-carboxylate.

[0079] Hydrocortisone-17-butyrate-21-6'-sulfamoyl nicotinate, fluorometholone-17-6'-sulfamoyl nicotinate, dexamethasone-21-5'-sulfamoyl nicotinate Acyl-thiophene-3'-carboxylates can also be prepared analogously.

Embodiment 1-1

[0081] 3-Hydroxyestro-1,3,5(10)-trien-17β-yl-6’-sulfamoylnicotinate (particle size 5-20μm) 1.0g

[0082] Accessories:

[0083] Sodium Carboxymethyl Cellulose 2.0g

[0084] Tween-80 0.8g

[0085] Sodium dihydrogen phosphate amount

[0086] Disodium hydrogen phosphate appropriate amount

[0087] Sodium chloride appropriate amount

[0088] Ethylparaben 0.1g

[0089] Propylparaben 0.1g

[0090] Water for injection 1000ml

[0091] Dissolve the prescribed amount of ethylparaben and propylparaben in water for injection with 50% of the prescribed amount, heat to 80-90°C, add the prescribed amount of Tween-80 to dissolve, and use No. 3 vertical melting Filter through a funnel and use as solution. Dissolve sodium carboxymethyl cellulose in water for injection with 30% of the prescription volume, filter with a Buchner funnel with 200-mesh nylon cloth, heat to 80-90°C, and add to the prescription Amount of 3-hydroxyestra-1,3,5(10)-trien-17β-yl-6'-sulfamoyl nicotinate was stirred ...

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Abstract

The invention relates to an ophthalmic composition of a heteroaryl sulfamoyl carboxylic ester carbonic anhydrase inhibitor, and discloses a compound in formula (II), wherein X is non-substituted or substituted heteroaryl or alkyl heteroaryl, Drug is a steroid which can form the carboxylic ester through OH group, and the X and the Drug can be selectively substituted.

Description

Technical field: [0001] The invention relates to components and preparation methods of an ophthalmic pharmaceutical composition of a carbonic anhydrase inhibitor and its derivatives, especially the composition is a solution-type preparation containing cyclodextrin. Background technique: [0002] Carbonic anhydrase (CA) is a zinc-containing metalloenzyme that reversibly catalyzes CO 2 The hydration reaction of the human body produces HCO3 that participates in various physiological functions of the human body - and H + . The human body also contains a variety of isoenzymes of carbonic anhydrase, which are widely distributed in various tissues and organs, and catalyze CO 2 The most efficient and well-studied form of hydration is carbonic anhydrase II (CA II). Although carbonic anhydrase II catalyzes only a simple physiological reaction, its catalyzed substrate CO 2 and product HCO3 - 、H + However, it is closely related to various physiological and pathological activities...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P27/02A61K31/565A61K31/573A61K31/57A61K31/58
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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