Compounds for treating ocular diseases associated with excessive vascularization

An eye disease, compound technology, applied in sensory diseases, antibody medical components, fusion with soluble cell surface receptors, etc., can solve problems such as loss, retinal pigment epithelium shedding, irreversible damage to vision by photoreceptors

Pending Publication Date: 2022-08-02
ACTIVE BIOTECH AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bleeding, leaking, and scarring of these vessels can lead to detachment of the retinal pigment epithelium and irreversible damage to photoreceptors and rapid vision loss if left untreated

Method used

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  • Compounds for treating ocular diseases associated with excessive vascularization
  • Compounds for treating ocular diseases associated with excessive vascularization
  • Compounds for treating ocular diseases associated with excessive vascularization

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0425] Example 1: Inhibition of choroidal neovascularization in a rat model of laser-induced choroidal neovascularization

[0426] Research design

[0427] Forty-eight (48) Brown Norway pigmented rats were divided into six (6) groups of eight (8) animals each. On day 0, choroidal neovascularization was induced in the right eye using a 532 nm argon laser photocoagulator (six (6) spots of 75 μm size, 150 mW, duration 0.1 sec). From day 0 (D0) just after induction with ChNV to day 21 (the last day of the study), the test items were administered by instillation 3 times a day or by oral twice a day. From day 0 to day 21 immediately after induction of neovascularization, the control item (vehicle) was instilled 3 times a day and the reference item (dexamethasone in olive oil) was administered daily by oral administration. Fundus neovascularization was assessed in the right eye on days 14 and 21 using Heidelberg retinal angiography (HRA). At the end of the in vivo phase, lesion ...

Embodiment 2

[0455] Example 2: Inhibition of VEGF and bFGF-induced neovascularization

[0456] Methods of assessing the area of ​​neovascularization

[0457] The area of ​​neovascularization can be measured using the following formula:

[0458] Area = 0.2·VL·CH·π

[0459] Among them such as figure 1 Vessel length (VL) and continuous circumferential area (expressed in clock hours = CH) were measured as defined in .

[0460] Treatment of VEGF-induced corneal angiogenesis with laquinimod

[0461] Hydron beads for inducing angiogenesis were prepared from a stimulating agent (VEGF) and a binding agent (sucralfate).

[0462] Anesthetized by intraperitoneal injection of 90 mg / kg pentobarbital, 53 CR female C57BL / 6 mice aged 6 to 8 weeks were prepared for surgery. Corneal vascularization was induced by placing the pellets in an incised corneal pocket in one eye. Monitor carefully for signs of eye irritation or infection.

[0463] Doses of laquinimod, vehicle (DDW = double distilled wat...

Embodiment 3

[0490] Example 3: Laquinimod and ABR-215174 have effects on LPS-activated microglia-induced tube formation in human retinal microvascular endothelial cells

[0491] method

[0492] The following experimental groups were included in the study:

[0493] Group 1: Control (vehicle, 0.1% DMSO)

[0494] Group 2: Sulforaphane (10 μM, positive control, anti-angiogenic effect)

[0495] Group 3: Aflibercept ("Aliya" 40μg / ml, positive control, partial anti-angiogenic effect)

[0496] Group 4: ABR-215174 (0.1 μM)

[0497] Group 5: ABR-215062 (10 μM)

[0498] Human retinal microvascular endothelial cells (HRMEC) were purchased from Neuromics (Cat. No. HEC09, Lot No. 2872) and grown at 37°C, 5% CO according to the manufacturer's instructions 2 Cultures were performed in Endo-Growth Medium (Cat. No. EKG001, Lot No. EKG0011902269) supplemented with Endothelial Growth Factor (Cat. No. EKG001, Lot No. EGK00125) under AlphaBiocoat-coated T25 flasks.

[0499] Primary human microglia from ...

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Abstract

The present invention relates to compounds for use in the treatment of diseases or conditions associated with excessive vascularization of the eye, such diseases or conditions are such as corneal neovascularization, iris neovascularization, ciliary body neovascularization, corneal nebula, choroidal neovascularization, retinal neovascularization, wet age-related macular degeneration, hyperplastic diabetic retinopathy, preterm retinopathy, and ischemic retinopathy.

Description

technical field [0001] The present invention relates to compounds and compositions for the treatment of diseases or conditions associated with excessive vascularization of the eye, such as corneal neovascularization, iris neovascularization, ciliary body neovascularization, corneal pannus (corneal pannus), choroidal neovascularization, retinal neovascularization, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy. Background technique [0002] laquinimod and taquinimod [0003] Laquinimod and tasquinimod are second-generation quinoline-3-carboxamide compounds that have been developed as oral immunomodulators, respectively, expected to treat relapsing multiple sclerosis (MS). ) and metastatic prostate cancer (metastatic chemo) prostate cancer, mCRPC). [0004] The efficacy and safety of laquinimod have been evaluated in Phase 1-3 clinical studies based on exposure to daily doses of up to 0.6 mg ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4704A61P27/02A61K38/17A61K39/395
CPCA61K31/4704A61K39/395A61P27/02A61K38/179C07K2319/30C07K2319/32C07K16/22C07K16/00C07K2317/24C07K2317/76A61K2300/00C07K14/70503A61K47/6811A61K39/3955A61K2039/505
Inventor H·埃里克斯森乔尔·凯耶M·特恩格伦
Owner ACTIVE BIOTECH AB
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