Drug for curing corneal and conjunctival disease

A therapeutic agent, corneal technology, applied in sensory diseases, organic active ingredients, medical preparations containing active ingredients, etc., can solve problems such as no hint of biphenylmethyl derivatives

Inactive Publication Date: 2008-04-16
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, there is no report on the study of the pharmacological effects of the above-mentioned biphenylmethyl derivatives on eye diseases, especially on keratoconjunctival lesions, and there is no suggestion at all that the biphenylmethyl derivatives with what basic chemical structure have effects on keratoconjunctival lesions. it works

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  • Drug for curing corneal and conjunctival disease
  • Drug for curing corneal and conjunctival disease
  • Drug for curing corneal and conjunctival disease

Examples

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Comparison scheme
Effect test

Embodiment Construction

[0083] The results of pharmacological tests and preparation examples are given below. The above examples are used to better understand the present invention, and do not limit the scope of the present invention.

[0084] [pharmacological test]

[0085] Curative Effect Trial of Corneal Lesions

[0086] Using male SD rats, a corneal lesion model was produced based on the method of Fujihara et al. (Invest. Ophthalmol. Vis. Sci 42(1): 96-100 (2001)). After the corneal lesion model was prepared, the corneal lesion was scored and judged based on the method of Murakami et al. (Shin Ophthalmology 21(1):87-90 (2004)), and the improvement rate of the corneal lesion after instillation was calculated.

[0087] (experimental method)

[0088] Male SD rats were given general anesthesia with pentobarbital sodium, and then the extraorbital lacrimal glands were removed to induce corneal lesions for 2 months.

[0089] Then, 4'-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propylbenzimidazol-1-y...

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Abstract

The purpose is to provide a therapeutic agent for a corneal / conjunctival disorder. A compound represented by the general formula (1) or a salt thereof shows an excellent ameliorating effect in a corneal disorder model, and therefore is useful as a therapeutic agent for a corneal / conjunctival disorder such as dry eye, corneal ulcer, keratitis and conjunctivitis. In the general formula, the ring Y represents a substituted or unsubstituted nitrogenated heterocyclic ring; R1 represents a carboxyl group or a substituted or unsubstituted nitrogenated 5-membered heterocyclic ring; and R2 and R3 independently represent a hydrogen atom, a substituted or unsubstituted alkyl group or a substituted or unsubstituted alkylcarbonyl group.

Description

technical field [0001] The present invention relates to dry eye, corneal ulcer, keratitis, conjunctivitis, superficial punctate keratopathy, corneal epithelial defect, conjunctival epithelial defect, keratoconjunctivitis sicca, superior keratoconjunctivitis limbickeratoconjunctivitis), filamentary keratitis (Filamentary Keratitis) and other keratoconjunctival diseases, the therapeutic agent contains a biphenylmethyl derivative or a salt thereof as an active ingredient. Background technique [0002] The cornea is a transparent, avascular tissue with a diameter of about 1 cm and a thickness of about 1 mm. In addition, the conjunctiva is the mucous membrane that covers the surface of the eyeball behind the limbus and the back of the eyelid. Significant impact on visual function when known corneal or conjunctival lesions. Keratoconjunctival disease caused by various diseases such as corneal ulcer, keratitis, conjunctivitis, dry eye, etc., adversely affects the normal remodeling...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/41A61P27/02
CPCA61K31/41A61P27/02A61K31/4152
Inventor 柴垣圭一平井慎一郎中村雅胤
Owner SANTEN PHARMA CO LTD
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