Drugs and compositions for ocular delivery

A composition and compound technology, applied in drug delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc.

Pending Publication Date: 2020-07-28
GRAYBUG VISION INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, sunitinib has been observed in both clinical trials and post-marketing clinical use

Method used

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  • Drugs and compositions for ocular delivery
  • Drugs and compositions for ocular delivery
  • Drugs and compositions for ocular delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0653] Example 1. Non-limiting examples of compounds of formula I

[0654]

Embodiment 2

[0655] Example 2A. Non-limiting Examples of Compounds of Formula II

[0656]

[0657]

[0658]

Embodiment 2B

[0659] Example 2B. Non-limiting Examples of Compounds of Formula II

[0660]

[0661]

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PUM

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Abstract

New prodrugs of therapeutically active compounds, including oligomeric prodrugs of ethacrynic acid, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality relatedto an increase in intraocular pressure (IOP), a disorder requiring neuro-protection, age-related macular degeneration, or diabetic retinopathy. Also a method for the controlled administration of timolol to a patient in need thereof, such as a human, comprising administering a prodrug of timolol in a micro-particle in vivo, wherein the timolol prodrug containing micro-particle exhibits in vitro drug release kinetics in an aqueous solution at a pH between 6-8 at body temperature of a substantially consistent release of at least 60% timolol itself by molar ratio to the prodrug of timolol or an intermediate metabolite thereof over at least 100 days.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of U.S. Provisional Application No. 62 / 598,943, filed December 14, 2017, and U.S. Provisional Application No. 62 / 663,134, filed April 26, 2018. The entire contents of these applications are hereby incorporated by reference for all purposes. Background technique [0003] The eye is a complex organ with unique anatomy and physiology. The structure of the eye can be divided into two parts, the front and the back. The cornea, conjunctiva, aqueous humor, iris, ciliary body, and lens are located anteriorly. The posterior part includes the sclera, choroid, retinal pigment epithelium, neural retina, optic nerve, and vitreous humor. The most prevalent diseases affecting the back of the eye are age-related macular degeneration (AMD) and diabetic retinopathy, both dry and wet. The most important diseases affecting the front include glaucoma, allergic conjunctivitis, anterior uveitis, and cat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/225C07C69/738
CPCC07C69/738C07D285/10C07D403/12C07D417/14C07D495/04C07D403/06A61K9/0019C07D417/04
Inventor J·L·克兰德杨明J·G·鲍曼N·霍安格J·齐泽姆
Owner GRAYBUG VISION INC
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