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A compound for treating pulmonary hypertension and its application

A technique for pulmonary hypertension and compounds, applied in medical preparations containing active ingredients, organic chemistry, drug combinations, etc., can solve the problems that cannot be treated with pulmonary hypertension

Active Publication Date: 2017-12-15
南京易亨制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Common drugs that lower blood pressure, such as ACEI and ARB, cannot be used for the treatment of pulmonary hypertension

Method used

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  • A compound for treating pulmonary hypertension and its application
  • A compound for treating pulmonary hypertension and its application
  • A compound for treating pulmonary hypertension and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: Preparation of CS303

[0019] (1) Synthesis of compound Ⅰ

[0020]

[0021] Add ethyl 1,4-diazacyclo-1-carboxylate (159g, 0.924mol) into a three-necked flask, then add pyridine (2.5L), add ethylsulfonyl chloride (141.9, 1.1mol) dropwise at room temperature, After the dropwise addition was completed, continue to stir at room temperature for 2 hours, monitor the disappearance of the raw material spots by TLC spotting (iodine color development), add dilute hydrochloric acid and ethyl acetate, extract, leave to stand and separate the layers, separate the organic layer, add anhydrous sodium sulfate to dry, After filtration, the filtrate was concentrated under reduced pressure to obtain 268.4 g of compound I as a white solid, with a yield of 91%. 1 HNMR (400MHz, DMSO-d6): δppm4.12(t, 2H), 3.61(t, 2H), 3.09(m, 2H), 2.98-2.86(m, 4H), 2.64(m, 2H), 1.68( m, 2H), 1.29(m, 3H), 1.27(m, 3H); ESI / MS: m / z=265(M+H) + .

[0022] (2) Synthesis of compound CS303 (formu...

Embodiment 2

[0025] Example 2: Effect test of CS303 on pulmonary hypertension caused by hypoxia

[0026] SD rats, male, weighing 200±20g, were randomly divided into five groups, namely normal control group, model control group, CS303 low-dose group (13mg / kg / d), CS303 medium-dose group (26mg / kg / d), CS303 high-dose group (52mg / kg / d), 10 rats in each group. The rats in the normal control group were raised in a normal pressure environment, and the rats in the other groups were raised in a fully automatic adjustment low-pressure hypoxic chamber (atmospheric pressure about 50kPa, oxygen concentration 10%), and intermittent hypoxia was carried out for 8 hours a day for a continuous 6 weeks. In the CS303 treatment group, 2 weeks after the start of modeling, intragastric administration was administered once before each hypoxia, and lasted for 4 weeks. Two weeks after the start of modeling, the normal control group and the model control group were intragastrically administered a considerable amoun...

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PUM

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Abstract

The invention discloses a compound for treating pulmonary hypertension, a preparation method of the compound, a pharmaceutical composition containing the compound and application of the pharmaceutical composition. The pharmaceutical composition is prepared by an active constituent and pharmaceutically-acceptable auxiliary materials. The formula of the active constituent is as shown in formula II. The compound is capable of treating the pulmonary hypertension and especially suitable for treating the pulmonary hypertension caused by hypoxemia.

Description

technical field [0001] The invention belongs to the technical field of compound biological activity, in particular, it relates to a compound for treating pulmonary hypertension, a pharmaceutical composition containing the compound and application thereof. Background technique [0002] Pulmonary hypertension is a disease characterized by pulmonary arteriolar vascular remodeling and pulmonary artery smooth muscle proliferation, which causes chronic precapillary pulmonary hypertension, increases pulmonary artery vascular tone, and leads to right heart failure, a disease that seriously threatens human life and health. Different from hypertension, pulmonary hypertension has the characteristics of low survival rate, poor prognosis and difficult clinical treatment. The 5-year survival rate of patients is comparable to that of breast cancer. Common drugs that lower blood pressure, such as ACEI and ARB, cannot be used for the treatment of pulmonary hypertension. The current treatme...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D243/08A61K31/551A61P9/12A61P11/00
CPCC07D243/08
Inventor 郝洁冯宪军石广灿李建华栗艳茹钟加滕
Owner 南京易亨制药有限公司