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Compositions and methods for treating ophthalmic diseases

An eye disease, compound technology, applied in metabolic diseases, drug combinations, sensory diseases, etc., can solve problems such as damage to the peripheral retina, visual loss, etc.

Inactive Publication Date: 2007-09-12
MERCK & CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For DR, laser therapy is effective in reducing blood vessel growth in many patients, however, laser therapy destroys part of the peripheral retina, which itself may cause vision loss

Method used

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  • Compositions and methods for treating ophthalmic diseases
  • Compositions and methods for treating ophthalmic diseases
  • Compositions and methods for treating ophthalmic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0248] (3S)-3-[N-(R)-α-(hydroxymethyl)benzyl]aminomethyl-1-[2-(5-(1,2,4-triazol-4-yl)- 1H-indol-3-yl)ethyl]pyrrolidine. 2.4 Hydrogen oxalate. 0.1 Hydrate

[0249] 1. (3S)-N(H)-3-[(R)-α-(hydroxymethyl)benzyl]aminomethylpyrrolidine

[0250] a) (3S)-N-tert-butyloxycarbonyl-3-(R)-α(hydroxymethyl)benzyl]aminomethylpyrrolidine

[0251] (R)-(-)-phenylglycinol (2.20 g, 16.1 mmol) and (3R)-N-tert-butyloxycarbonyl-3-methylsulfonyloxymethylpyrrolidine ( A solution of 1.0 g, 3.58 mmol) in toluene (20 ml) was heated at 150° C. for 6 hours in a sealed pressure tube (Aldrich). The solvent was then removed under vacuum and the residue was dissolved in ethyl acetate (200ml) and washed 4 times with water (x4). Dried organic matter (MgSO 4 ), evaporated, and chromatographed on silica gel with CH 2 Cl 2 / MeOH (97:3) eluted to give the title compound α-(hydroxymethyl)benzylaminomethylpyrrolidine (1.0 g, 87%), δ (360 MHz, CDCl 3 )1.45(9H,s,OC(Me) 3 ), 1.52-2.60 (5H, m, CH 2 and CH), 2.90...

Embodiment 2

[0257] (3S)-3-[N-(S)-α-(Hydroxymethyl)benzyl]aminomethyl-1-[2-(5-(1,2,4-triazol-4-yl)- 1H-indol-3-yl)ethyl]pyrrolidine. 2.4 Hydrogen oxalate. 0.1 Hydrate.

[0258] a) (3S)-N(H)-3-[(S)-α-(hydroxymethyl)benzyl]aminomethylpyrrolidine

[0259] Prepared from (S)-(+)-phenylaminoethanol and (3R)-N-tert-butyloxycarbonyl-3-methylsulfonyloxymethylpyrrolidine using the method described in Example 45, 1a part.

[0260] b) (3S)-3-[N-(S)-α-(hydroxymethyl)benzyl]aminomethyl-1-[2-(5-(1,2,4-triazol-4-yl )-1H-indol-3-yl)ethyl]pyrrolidine. 2.4 Hydrogen oxalate. 0.1 Hydrate.

[0261] Prepared from intermediate 3 and previous pyrrolidine using the method described in Example 41, mp 155°C, (found: C, 55.35; H, 5.71; N, 12.82.C 25 h 30 N 6 O 2.4 (C 2 h 2 o 4 ) 0.1 H 2 O calcd: C, 55.20; H, 5.44; N, 12.96%), m / e 431 (M+1) + .

Embodiment 3

[0263] (3S)-3-[N-Benzyl-N-(2-hydroxy)ethyl]aminomethyl-1-[2-(5-(1,2,4-triazol-4-yl)-1H -indol-3-yl)ethyl]pyrrolidine. 2.4 Hydrogen oxalate

[0264] a) (3S)-N(H)-3-[N-benzyl-N-(2-hydroxy)ethyl]aminomethylpyrrolidine

[0265] Prepared from N-benzylethanolamine and (3R)-N-tert-butyloxycarbonyl-3-methylsulfonyloxymethylpyrrolidine using the method described in Example 5, part b and c, δ (250 MHz, CDCl 3 )1.24-1.60 (2H, m, CH 2 ), 1.82-1.94 (2H, m, CH 2 ), 2.26-3.06 (9H, m, 4 CH 2 and CH), 3.56-3.60 (2H, m, CH 2 ), 7.20-7.36 (5H, m, Ar-H).

[0266] b) (3S)-3-[N-benzyl-N-(2-hydroxy)ethyl]aminomethyl-1-[2-(5-(1,2,4-triazol-4-yl) -1H-indol-3-yl)ethyl]pyrrolidine. 2.4 Hydrogen oxalate.

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Abstract

This invention relates to CXCR4 inhibitors and their use in treating and / or preventing a variety of angiogenic, microvascular and ocular disorders including primary indications for diabetic retinopathy, macular degeneration (such as wet or neovascular age-related macular degeneration (AMD) and dry or atrophic AMD), macular edema, and secondary indications for inhibiting tumor vascularization, and corneal and iris neovascularization.

Description

Background of the invention [0001] Inappropriate growth of blood vessels in adults contributes to a variety of pathogenic conditions. For example, supporting tumor growth by providing oxygen and nutrients through the formation of new blood vessels. In the eye, growth of the normally resting vasculature can lead to retinal damage, visual impairment or blindness. Neovascular (or wet) AMD and diabetic retinopathy are the most prevalent diseases of the ocular vasculature and are the leading causes of blindness in populations in developed countries. The current standard of care for ocular neovascular disease is laser surgery (photocoagulation or photodynamic therapy). Unfortunately laser surgery is moderately effective and only available in a small fraction of the AMD patient population. For DR, laser therapy is effective in reducing blood vessel growth in many patients, however, laser therapy destroys portions of the peripheral retina, which itself can lead to vision loss. The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517
CPCA61K31/517A61K31/198A61P17/02A61P27/02A61P43/00A61P9/00A61P3/10
Inventor K·A·萨利文C·J·塔特
Owner MERCK & CO INC
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