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Flavonoid derivative with ROCK kinase inhibiting effect

A drug and application technology, applied in the field of flavonoid derivatives, can solve the problems of no effective drugs for diseases, destroying the protective effect of VEGF, etc.

Active Publication Date: 2018-09-21
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing drugs for diabetic retinopathy are mainly anti-VEGF antibodies, such as conbocept and ranibizumab, but these drugs are used in the late stage of the disease, that is, the stage of retinal angiogenesis, and there is no effective drug for the early stage of the disease, and Long-term application of anti-VEGF drugs may destroy the protective effect of VEGF on normal retinal tissue

Method used

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  • Flavonoid derivative with ROCK kinase inhibiting effect
  • Flavonoid derivative with ROCK kinase inhibiting effect
  • Flavonoid derivative with ROCK kinase inhibiting effect

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Experimental program
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Embodiment 1

[0103] Embodiment 1 Preparation of compound 11 of the present invention

[0104]

[0105] Intermediate (2): Preparation of 7-Hydroxy-4-Hydrochromanone

[0106]

[0107] Put raw material (1) (2,4-dihydroxyacetophenone 1.0g, 6.57mmol) and triethyl orthoformate (6mL) in a round bottom flask at room temperature and stir, then add perchloric acid 600μL dropwise, and react for 1.5h , adding 50mL of ether, a large amount of red solid precipitated out. Suction filtration, the red solid was dissolved into a suspension with 30mL water and stirred at 80°C for 4 hours, extracted with ethyl acetate, water, and saturated sodium chloride after cooling, dried the organic phase with magnesium sulfate, suction filtration, and column chromatography white solid. The yield is 90%.

[0108] 1 H NMR (400MHz, DMSO) δ10.76(s, 1H), 8.14(d, J=6.0Hz, 1H), 7.87(d, J=8.7Hz, 1H), 6.91(dd, J=8.7, 2.2Hz , 1H), 6.84(d, J=2.2Hz, 1H), 6.21(d, J=6.0Hz, 1H).; MS (ESI, positive ion) m / z: 162.87[M+H] + ....

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Abstract

The invention relates to a flavonoid derivative with a ROCK kinase inhibiting effect, belongs to the technical field of organic synthetic medicines, and solves the technical problems that the existingglaucoma treating medicines are poor in effect, especially effective therapeutic medicines for treating glaucoma with normal intraocular pressure lack, and medicines for treating diabetic retinopathy, such as conbercept and ranibizumab, can only be applied to the later stage of a disease, are ineffective for the early stage of the disease and destroy the protective effect of VEGF on a normal retinal tissue after long-term use. A technical scheme for solving the problems is achieved by providing a compound shown as a formula I. Experimental results show that the compound has the significant ROCK kinase inhibiting effect, can effectively reduce the intraocular pressure, protect retinal ganglion cells, reduce the retinal reactive oxygen level and inhibit retinal angiogenesis, and provides anovel medication choice for clinical treatment of the glaucoma and the diabetic retinopathy.

Description

technical field [0001] The invention relates to flavonoid derivatives with ROCK kinase inhibitory effect, and belongs to the technical field of organic synthetic medicines. Background technique [0002] ROCK kinases belong to serine / threonine protein kinases and are divided into ROCK I (ROCKβ) and ROCKII (ROCKα). ROCK kinase plays an important role in a series of cell life activities such as cell mitotic adhesion, cytoskeleton adjustment, muscle cell contraction, and tumor cell infiltration. Studies have shown that ROCK kinase is associated with a variety of diseases, including hypertension, pulmonary hypertension, cardiovascular disease, inflammation, autoimmune disease, lung disease and ophthalmic disease, etc. [0003] Existing treatments for glaucoma mainly focus on promoting aqueous humor outflow or reducing aqueous humor production to reduce intraocular pressure, such as prostaglandin derivative latanoprost that promotes aqueous humor outflow, or β-adrenergic receptor...

Claims

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Application Information

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IPC IPC(8): C07D311/22C07D311/36C07D413/12C07D405/12C07D417/12C07D215/227C07D317/64C07D319/18C07C237/40C07C255/57A61K31/352A61K31/422A61K31/427A61K31/4155A61K31/4704A61K31/277A61K31/167A61P27/02A61P27/06
CPCA61P27/02A61P27/06C07C237/40C07C255/57C07D215/227C07D311/22C07D311/36C07D317/64C07D319/18C07D405/12C07D413/12C07D417/12
Inventor 杨胜勇李琳丽
Owner SICHUAN UNIV
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