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Novel compounds and applications thereof

A compound, pentanediol technology, applied in the field of new compounds, can solve the problem of no pharmacological activity, and achieve the effects of excellent cardiovascular and cerebrovascular pharmacological activity, improvement of neurological symptoms, and inhibition of thrombosis

Inactive Publication Date: 2016-04-27
米文君
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And 2-(1R, 4S-pentanediol) benzoic acid, 2-(1R, 4R-pentanediol) benzoic acid and salts thereof do not show this pharmacological activity

Method used

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  • Novel compounds and applications thereof
  • Novel compounds and applications thereof
  • Novel compounds and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Effects on neurological symptoms and cerebral infarction range in middle cerebral artery thrombosis model (Middle Cerebral Artery Thrombosis, MCAT) rats.

[0060] 1. Animals

[0061]SD rats, half male and half male, weighing 190-250 g.

[0062] 2. Drugs and reagents

[0063] Test drug

[0064] 2-(1,4-pentanediol)benzoic acid, 2-(1,4-pentanediol)benzoic acid N,N'-dibenzylethylenediamine salt, 2-(1S,4S-pentanediol ) Benzoic acid, 2-(1S, 4S-pentanediol) benzoic acid N, N'-dibenzylethylenediamine salt, 2-(1S, 4R-pentanediol) benzoic acid, 2-(1S, 4R -pentanediol) benzoic acid N,N'-dibenzylethylenediamine salt.

[0065] Reagent

[0066] FeCl3*6H20 (A.R.), prepared with 1mol / L hydrochloric acid; red tetrazolium (TTC), (C.P.).

[0067] 3. Instruments

[0068] XTT solid microscope; constant temperature water bath oscillator; electronic analytical balance.

[0069] 4. Test methods and results

[0070] (1) Effects on neurological symptoms of MCAT rats

[0071]...

Embodiment 2

[0092] Example 2: Effects on Thrombosis of Arterial-Venous Bypass in Rats This example selects:

[0093] 1. Animals

[0094] SD rats, half male and half male, weighing 220-260 g.

[0095] 2. Drugs and reagents

[0096] Test drug

[0097] 2-(1,4-pentanediol)benzoic acid, 2-(1,4-pentanediol)benzoic acid N,N'-dibenzylethylenediamine salt, 2-(1S,4S-pentanediol ) Benzoic acid, 2-(1S, 4S-pentanediol) benzoic acid N, N'-dibenzylethylenediamine salt, 2-(1S, 4R-pentanediol) benzoic acid, 2-(1S, 4R -pentanediol) benzoic acid N,N'-dibenzylethylenediamine salt.

[0098] 3. Instruments

[0099] AEG-220 electronic analytical balance; Df-206 blast drying oven.

[0100] 4. Test methods and results

[0101] 1. See Table 4 for grouping

[0102]

[0103]

[0104] Table 4

[0105] 2. Administration

[0106] Oral administration was administered once a day for 3 consecutive days, and the thrombosis model group was given the same amount of vehicle. Surgery was performed after the la...

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Abstract

The invention relates to novel compounds and applications thereof. The novel compounds are specifically 2-(1S,4S-pentanediol)benzoic acid, 2-(1S,4R-pentanediol)benzoic acid, 2-(1S,4S-pentanediol)benzoate, and 2-(1S,4R-pentanediol)benzoate. The invention also relates to the applications of the novel compounds in preventing and treating cardio-cerebral ischemic diseases, ameliorating cardio-cerebral circulation disorders, resisting thrombosis, and the like. In animal pharmacodynamics model tests, the novel compounds provided by the invention show excellent protection effects upon brain tissue damage caused by middle cerebral artery occlusion. With the novel compound, neurological symptoms of middle cerebral artery thrombosis model rats can be substantially ameliorated, infarct sizes can be substantially reduced, and rat artery-vein bypass thrombosis can be substantially inhibited. Therefore, the compounds provided by the invention assists in effectively inhibiting thrombosis, and have good prevention and treatment effects against cardio-cerebral ischemic diseases.

Description

technical field [0001] The present invention relates to new compounds and uses thereof, specifically, the present invention relates to 2-(1S, 4S-pentanediol) benzoic acid, 2-(1S, 4R-pentanediol) benzoic acid, 2-(1S, 4S- Pentylene glycol) benzoate, 2-(1S, 4R-pentanediol) benzoate, also relates to the use of such compounds in the prevention and treatment of cardio-cerebral ischemic diseases and improving cardio-cerebral circulation disorders, antithrombotic etc. aspects of application. Background technique [0002] Cerebral ischemic disease has the characteristics of high morbidity, disability and mortality. It is a common and frequently-occurring disease that endangers human life and health. Therefore, the search for anti-ischemic drugs has attracted widespread attention from scholars at home and abroad. [0003] Butylphthalide, also known as apigenin, was originally found in celery seeds. Its pharmacodynamic characteristics cover many aspects: 1. It can improve the energy m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C65/01C07C51/09C07C51/41C07C211/27C07C209/00A61K31/192A61P9/10A61P7/02
Inventor 不公告发明人
Owner 米文君
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